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Sample records for possessed prescription-strength ibuprofen

  1. Ibuprofen: Synthesis, production and properties

    Directory of Open Access Journals (Sweden)

    Mijin Dušan Ž.

    2003-01-01

    Full Text Available Since its introduction in 1969, ibuprofen has become one of the most common painkillers in the world. Ibuprofen in an NSAID (non-steroidal anti-inflammatory drug and like other drugs of its class it possesses analgetic, antipyretic and anti-inflammatory properties. While ibuprofen is a relatively simple molecule, there is still sufficient structural complexity to ensure that a large number of different synthetic approaches are possible. Since the introduction of pharmaceutical products containing ibuprofen, industrial and academic scientists have developed many potential production processes. This paper describes the history, synthesis and production, as well as the properties and stability of ibuprofen.

  2. Ibuprofen overdose

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/article/002655.htm Ibuprofen overdose To use the sharing features on this page, please enable JavaScript. Ibuprofen is a type of nonsteroidal anti-inflammatory drug ( ...

  3. Ibuprofen dosing for children

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/patientinstructions/000772.htm Ibuprofen dosing for children To use the sharing features ... much of this medicine can be harmful. How Ibuprofen can Help Your Child Ibuprofen is a type ...

  4. Bioavailability of ibuprofen following oral administration of standard ibuprofen, sodium ibuprofen or ibuprofen acid incorporating poloxamer in healthy volunteers

    OpenAIRE

    Dewland, Peter M; Reader, Sandie; Berry, Phillip

    2009-01-01

    Background The aim of this study was to compare the pharmacokinetic properties of sodium ibuprofen and ibuprofen acid incorporating poloxamer with standard ibuprofen acid tablets. Methods Twenty-two healthy volunteers were enrolled into this randomised, single-dose, 3-way crossover, open-label, single-centre, pharmacokinetic study. After 14 hours' fasting, participants received a single dose of 2 × 200 mg ibuprofen acid tablets (standard ibuprofen), 2 × 256 mg ibuprofen sodium dihydrate table...

  5. Pelepasan Ibuprofen Dari Gel Karbomer 940 Kokristal Ibuprofen-Nikotinamida

    OpenAIRE

    Agustin, Rini; Sari, Novica; Zaini, Erizal

    2014-01-01

    Salah satu metode untuk meningkatkan kelarutan adalah co-kristalisasi. Ibuprofen dapat digunakan dalam aplikasi topikal untuk rheumatoid arthrisi, sehingga telah dilakukan sebuah studi tentang formulasi dan pelepasan kokristal ibuprofen-nikotinamida dari gel karbomer 940. Kokristal diperoleh dari metode penguapan pelarut dengan komposisi equimol (1:1). Gel terdiri dari dua formula dengan jumlah ibuprofen yang sama (5%). Formula pertama adalah gel kokristal ibuprofen-nicotinamida dan Formula d...

  6. Hydrolysis of Ibuprofen Nitrile and Ibuprofen Amide and Deracemisation of Ibuprofen Using Nocardia corallina B-276

    OpenAIRE

    Myrna Solís-Oba; Norberto Manjarrez; Aida Solís; Ricardo Lievano; Herminia Inés Pérez

    2012-01-01

    A novel application of whole cells of Nocardia corallina B-276 for the deracemisation of ibuprofen is reported. This microorganism successfully hydrolysed ibuprofen nitrile to ibuprofen amide, and ibuprofen amide to ibuprofen, using a suspension of cells in a potassium phosphate buffer solution (0.1 M, pH = 7.0). These results can be explained by the presence of NHase and amidase enzymes, but the reactions are not enantioselective and low ee values were obtained. However, (R)-ibuprofen was is...

  7. How to Safely Give Ibuprofen

    Science.gov (United States)

    ... of ibuprofen are available in similar forms. How to Give When giving ibuprofen, refer to the following dosage ... of Use Notice of Nondiscrimination Visit the Nemours Web site. Note: All information on KidsHealth® is for ...

  8. Synthesis of deuterium labelled ibuprofen

    International Nuclear Information System (INIS)

    Cappon, V.J.; Halstead, G.W.; Theis, D.L.

    1986-01-01

    The preparations of [ar- 2 H 4 ]-ibuprofen and [ar, 3,3,3- 2 H 7 ]-ibuprofen are described. The deuterium was incorporated into the aromatic ring of [ar- 2 H 4 ]-ibuprofen which is a metabolically stable position. [ar, 3,3,3- 2 H 7 ]-ibuprofen was synthesized by the same route using [ 2 H 3 ]-CH 3 I instead of CH 3 I for use as a GC/MS internal standard in stable isotope labelled bioavailability studies. (author)

  9. Compound list: ibuprofen [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available ibuprofen IBU 00072 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/in..._vitro/ibuprofen.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitr...o/ibuprofen.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/...Single/ibuprofen.Rat.in_vivo.Liver.Single.zip ftp://ftp.biosciencedbc.jp/archive/

  10. IBUPROFEN IN PAIN TREATMENT IN CHILDREN

    Directory of Open Access Journals (Sweden)

    R. V. Denisova

    2012-01-01

    Full Text Available The article contains results of therapeutic efficacy of ibuprofen in pain syndrome management in children. Validity of its use is doubtless. Analgesic effect of Ibuprofen has been confirmed in clinical trials in patients with migraine and ENT-disorders. In this article we also review international experience of ibuprofen use in juvenile arthritis..

  11. Potential of Essential Oils as Penetration Enhancers for Transdermal Administration of Ibuprofen to Treat Dysmenorrhoea

    Directory of Open Access Journals (Sweden)

    Jun Chen

    2015-10-01

    Full Text Available The present study was conducted to evaluate and compare five essential oils (EOs as penetration enhancers (PEs to improve the transdermal drug delivery (TDD of ibuprofen to treat dysmenorrhoea. The EOs were prepared using the steam distillation method and their chemical compositions were identified by GC-MS. The corresponding cytotoxicities were evaluated in epidermal keartinocyte HaCaT cell lines by an MTT assay. Furthermore, the percutaneous permeation studies were carried out to compare the permeation enhancement effect of EOs. Then the therapeutic efficacy of ibuprofen with EOs was evaluated using dysmenorrheal model mice. The data supports a decreasing trend of skin cell viability in which Clove oil >Angelica oil > Chuanxiong oil > Cyperus oil > Cinnamon oil >> Azone. Chuanxiong oil and Angelica oil had been proved to possess a significant permeation enhancement for TDD of ibuprofen. More importantly, the pain inhibitory intensity of ibuprofen hydrogel was demonstrated to be greater with Chuanxiong oil when compared to ibuprofen without EOs (p < 0.05. The contents of calcium ion and nitric oxide (NO were also significantly changed after the addition of Chuanxiong oil (p < 0.05. In summary, we suggest that Chuanxiong oil should be viewed as the best PE for TDD of ibuprofen to treat dysmenorrhea.

  12. In vitro effect of calcium-containing prescription-strength fluoride toothpastes on bovine enamel erosion under hyposalivation-simulating conditions.

    Science.gov (United States)

    Scaramucci, Taís; Borges, Alessandra B; Lippert, Frank; Zero, Domenick T; Hara, Anderson T

    2015-02-01

    To evaluate the ability of calcium-containing prescription-strength fluoride (F) toothpastes in preventing enamel erosion under low salivary flow simulating conditions. Enamel and dentin bovine specimens were assigned to the following groups: A - placebo; B - 1,100 ppm F/NaF (Aquafresh Advanced); C - 5,000 ppm F/NaF (Prevident 5000 Booster); D - 5000 ppm F/NaF+calcium sodium phosphosilicate (Topex Renew); and E - 5,000 ppm F/NaF+tri-calcium phosphate (Clinpro 5000). Specimens were positioned in custom-made devices, creating a sealed chamber on the surface, connected to peristaltic pumps. Citric acid was injected into the chamber for 2 minutes, followed by artificial saliva (0.05 ml/minute), for 60 minutes, 4x/day, for 3 days. Aquafresh was also tested under normal salivary flow (0.5 ml/minute), as reference (Group F). Specimens were exposed to the toothpastes for 2 minutes, 2x/day. After cycling, surface loss (SL) and concentration of loosely- and firmly-bound F were determined. Data were analyzed by ANOVA. Results: Group A (placebo) presented highest surface loss (SL), while Group F had the lowest, for both substrates. For enamel, none of the dentifrices differed from Group B or among each other. For dentin, none of the dentifrices differed from Group B, but Group E showed greater protection than Group C. Group E presented the highest F concentrations for both substrates, only matched by Group D for firmly-bound fluoride on enamel. All fluoridated dentifrices tested reduced SL, with no additional benefit from higher F concentrations. Some formulations, especially Clinpro 5000, increased F availability on the dental substrates, but no further erosion protection was observed.

  13. Multiple binding modes of ibuprofen in human serum albumin identified by absolute binding free energy calculations

    KAUST Repository

    Evoli, Stefania

    2016-11-10

    Human serum albumin possesses multiple binding sites and transports a wide range of ligands that include the anti-inflammatory drug ibuprofen. A complete map of the binding sites of ibuprofen in albumin is difficult to obtain in traditional experiments, because of the structural adaptability of this protein in accommodating small ligands. In this work, we provide a set of predictions covering the geometry, affinity of binding and protonation state for the pharmaceutically most active form (S-isomer) of ibuprofen to albumin, by using absolute binding free energy calculations in combination with classical molecular dynamics (MD) simulations and molecular docking. The most favorable binding modes correctly reproduce several experimentally identified binding locations, which include the two Sudlow\\'s drug sites (DS2 and DS1) and the fatty acid binding sites 6 and 2 (FA6 and FA2). Previously unknown details of the binding conformations were revealed for some of them, and formerly undetected binding modes were found in other protein sites. The calculated binding affinities exhibit trends which seem to agree with the available experimental data, and drastically degrade when the ligand is modeled in a protonated (neutral) state, indicating that ibuprofen associates with albumin preferentially in its charged form. These findings provide a detailed description of the binding of ibuprofen, help to explain a wide range of results reported in the literature in the last decades, and demonstrate the possibility of using simulation methods to predict ligand binding to albumin.

  14. Cocrystal Screening of Ibuprofen with Oxalic Acid and Citric Acid via Grinding Method

    Science.gov (United States)

    Othman, M. F.; Anuar, N.; Rahman, S. Ad; Taifuddin, N. A. Ahmad

    2018-05-01

    Ibuprofen is a Class II Biological Safety Class (BSC) drugs used for relief of arthritis, as an analgesic and possesses the effect of antiplatelet. The major problem involves in ibuprofen is it has a low solubility and high permeability thus causes an unsatisfactory therapeutic effect to humans. Thus, in this work, alteration of ibuprofen’s physicochemical properties is conducted by means of cocrystallization technique. Co-crystallizations of ibuprofen were prepared with selected coformers using dry grinding and liquid assisted grinding (LAG) techniques in different molar ratios while ethanol and propanol were used as a solvent. The new crystalline forms were identified and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and fourier transform infrared spectroscopy (FTIR). Analysis for Ibuprofen-Citric acid (IBP-CA) system, co-crystal was successfully formed in 1:2, 1:3, 2:1 and 3:1 molar ratios for neat grinding method although the co-crystal produced is unstable. Meanwhile, for Ibuprofen-Oxalic acid (IBP-OA) system, the co-crystal formation was identified only in 1:1, 1:2 and 1:3 molar ratios for the neat grinding method. LAG method shows that co-crystal formation was unsuccessful in both solvents for IBP-CA, while IBP-OA co-crystal was formed in the molar ratio 1:1, 2:1 and 3:1 in ethanol, and 2:1 and 3:1 in propanol.

  15. The protection of possession

    Directory of Open Access Journals (Sweden)

    Popov Danica

    2011-01-01

    Full Text Available Protection in disputes for the protection of possession can be attained through the following actions a for dispossession (interdictum recuperande possessionis and b with an action for the disturbance of possession (interdictum retinendae possessionis. The general feature of these disputes is that there is only discussion on the facts and not a legal matters. Subject matter jurisdiction for the resolution of such disputes belongs to the court of general jurisdiction, while the dispute itself is a litigation. The special rule of proceedings of action for disturbance are: provisionality of the protection of possession; urgency in proceedings; initiation of the proceedings; limiting of objection; prescribing temporary measures; rendering a ruling in the form of order; appeals which may be filed within a short deadline and which does not have suspensive effect (do not delay the execution of the order; revision is not allowed etc.

  16. Bioequivalence assessment of two formulations of ibuprofen

    KAUST Repository

    Al-Talla, Zeyad; Akrawi, Sabah H; Tolley, Luke T; Sioud, Salim H; Zaater, Mohammed F; Emwas, Abdul-Hamid M

    2011-01-01

    Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz , produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen , manufactured by Boots

  17. Thiamine potentiates chemoprotective effects of ibuprofen in DEN induced hepatic cancer via alteration of oxidative stress and inflammatory mechanism.

    Science.gov (United States)

    Afzal, Muhammad; Kazmi, Imran; Khan, Ruqaiyah; Rana, Poonam; Kumar, Vikas; Al-Abbasi, Fahad A; Zamzami, Mazin A; Anwar, Firoz

    2017-06-01

    Present study, was an effort to scrutinize the molecular and biochemical role of ibuprofen and thiamine combination in diethylnitrosamine (DEN)-induced HCC in Wistar rats. Single intraperitoneal injection of DEN (200 mg/kg) was used for induction of HCC in rats. The rats were divided into eight various groups. DEN induced rats were treated with pure ibuprofen (40 mg/kg) and thiamine in combination for the period of 12th weeks. The protocol was terminated after the 16th week. Exposure of DEN up-regulated the levels of different serum biochemical parameters, antioxidant enzyme level, Alfa-fetoprotein (AFP) and reduced the level of High density lipoprotein (HDL) in Wistar rats along with the alteration in pro-inflammatory cytokines viz., interlukin-6 (IL-6), Tumor necrosis factor (TNF-α) and Interleukin-1β (IL-1β) with decrease in body weight. Macroscopic evaluation, revealed DEN group rats confirmed the expansion of hepatic nodules, which were reduced by the individual treatment of ibuprofen and thiamine, but the synergistic treatment of ibuprofen and thiamine confirm the significant reduction of hepatic nodules. Further, this combination possesses the significant chemoprotective effect in DEN-induced HCC by restoring the hepatic enzymes and other biomarkers along with an alteration in pro-inflammatory cytokines. The above result concludes that ibuprofen and thiamine combination possess potent anti-cancerous activity. Copyright © 2017 Elsevier Inc. All rights reserved.

  18. Hydroxyl radical induced degradation of ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Illés, Erzsébet, E-mail: erzsebet.illes@chem.u-szeged.hu [Institute of Chemistry, Research Group of Environmental Chemistry, University of Szeged, Szeged (Hungary); Institute of Isotopes, Centre for Energy Research, Hungarian Academy of Sciences, Budapest (Hungary); Takács, Erzsébet [Institute of Isotopes, Centre for Energy Research, Hungarian Academy of Sciences, Budapest (Hungary); Dombi, András [Institute of Chemistry, Research Group of Environmental Chemistry, University of Szeged, Szeged (Hungary); Gajda-Schrantz, Krisztina [Institute of Chemistry, Research Group of Environmental Chemistry, University of Szeged, Szeged (Hungary); Department of Inorganic and Analytical Chemistry, University of Szeged, Szeged (Hungary); EMPA, Laboratory for High Performance Ceramics, Duebendorf (Switzerland); Rácz, Gergely; Gonter, Katalin; Wojnárovits, László [Institute of Isotopes, Centre for Energy Research, Hungarian Academy of Sciences, Budapest (Hungary)

    2013-03-01

    Pulse radiolysis experiments were used to characterize the intermediates formed from ibuprofen during electron beam irradiation in a solution of 0.1 mmol dm{sup −3}. For end product characterization {sup 60}Co γ-irradiation was used and the samples were evaluated either by taking their UV–vis spectra or by HPLC with UV or MS detection. The reactions of {sup ·}OH resulted in hydroxycyclohexadienyl type radical intermediates. The intermediates produced in further reactions hydroxylated the derivatives of ibuprofen as final products. The hydrated electron attacked the carboxyl group. Ibuprofen degradation is more efficient under oxidative conditions than under reductive conditions. The ecotoxicity of the solution was monitored by Daphnia magna standard microbiotest and Vibrio fischeri luminescent bacteria test. The toxic effect of the aerated ibuprofen solution first increased upon irradiation indicating a higher toxicity of the first degradation products, then decreased with increasing absorbed dose. Highlights: ► In hydroxyl radical attack on the ring mainly hydroxylated products form ► The hydrated electron attacks the carboxyl group. ► Oxidative conditions are more effective in ibuprofen decomposition than reductive. ► Ecotoxicity of ibuprofen solution first increases then decreases with irradiation.

  19. Hydroxyl radical induced degradation of ibuprofen

    International Nuclear Information System (INIS)

    Illés, Erzsébet; Takács, Erzsébet; Dombi, András; Gajda-Schrantz, Krisztina; Rácz, Gergely; Gonter, Katalin; Wojnárovits, László

    2013-01-01

    Pulse radiolysis experiments were used to characterize the intermediates formed from ibuprofen during electron beam irradiation in a solution of 0.1 mmol dm −3 . For end product characterization 60 Co γ-irradiation was used and the samples were evaluated either by taking their UV–vis spectra or by HPLC with UV or MS detection. The reactions of · OH resulted in hydroxycyclohexadienyl type radical intermediates. The intermediates produced in further reactions hydroxylated the derivatives of ibuprofen as final products. The hydrated electron attacked the carboxyl group. Ibuprofen degradation is more efficient under oxidative conditions than under reductive conditions. The ecotoxicity of the solution was monitored by Daphnia magna standard microbiotest and Vibrio fischeri luminescent bacteria test. The toxic effect of the aerated ibuprofen solution first increased upon irradiation indicating a higher toxicity of the first degradation products, then decreased with increasing absorbed dose. Highlights: ► In hydroxyl radical attack on the ring mainly hydroxylated products form ► The hydrated electron attacks the carboxyl group. ► Oxidative conditions are more effective in ibuprofen decomposition than reductive. ► Ecotoxicity of ibuprofen solution first increases then decreases with irradiation

  20. Analgesic efficacy with rapidly absorbed ibuprofen sodium dihydrate in postsurgical dental pain

    DEFF Research Database (Denmark)

    Nørholt, Sven Erik; Hallmer, F; Hartlev, Jens

    2011-01-01

    To evaluate the onset of analgesic effect for a new formulation of ibuprofen sodium dihydrate versus conventional ibuprofen (ibuprofen acid).......To evaluate the onset of analgesic effect for a new formulation of ibuprofen sodium dihydrate versus conventional ibuprofen (ibuprofen acid)....

  1. Detection and Analysis of the Quality of Ibuprofen Granules

    Science.gov (United States)

    Yu-bin, Ji; Xin, LI; Guo-song, Xin; Qin-bing, Xue

    2017-12-01

    The Ibuprofen Granules comprehensive quality testing to ensure that it is in accordance with the provisions of Chinese pharmacopoeia. With reference of Chinese pharmacopoeia, the Ibuprofen Granules is tested by UV, HPLC, in terms of grain size checking, volume deviation, weight loss on drying detection, dissolution rate detection, and quality evaluation. Results indicated that Ibuprofen Granules conform to the standards. The Ibuprofen Granules are qualified and should be permitted to be marketed.

  2. Effect of Ibuprofen on masking endodontic diagnosis.

    Science.gov (United States)

    Read, Jason K; McClanahan, Scott B; Khan, Asma A; Lunos, Scott; Bowles, Walter R

    2014-08-01

    An accurate diagnosis is of upmost importance before initiating endodontic treatment; yet, there are occasions when the practitioner cannot reproduce the patient's chief complaint because the patient has become asymptomatic. Ibuprofen taken beforehand may "mask" or eliminate the patient's symptoms. In fact, 64%-83% of patients with dental pain take analgesics before seeing a dentist. The purpose of this study was to examine the possible "masking" effect of ibuprofen on endodontic diagnostic tests. Forty-two patients with endodontic pain underwent testing (cold, percussion, palpation, and bite force measurement) and then received either placebo or 800 mg ibuprofen. Both patients and operators were blinded to the medication received. One hour later, diagnostic testing was repeated and compared with pretreatment testing. Ibuprofen affected testing values for vital teeth by masking palpation 40%, percussion 25%, and cold 25% on affected teeth with symptomatic irreversible pulpitis and symptomatic apical periodontitis. There was no observed masking effect in the placebo group on palpation, percussion, or cold values. When nonvital teeth were included, the masking effect of ibuprofen was decreased. However, little masking occurred with the bite force measurement differences. Analgesics taken before the dental appointment can affect endodontic diagnostic testing results. Bite force measurements can assist in identifying the offending tooth in cases in which analgesics "mask" the endodontic diagnosis. Copyright © 2014 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.

  3. Bioequivalence assessment of two formulations of ibuprofen

    KAUST Repository

    Al-Talla, Zeyad

    2011-10-19

    Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz , produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen , manufactured by Boots Company, Nottingham, UK. Methods and results: A prestudy validation of ibuprofen demonstrated long-term stability, freeze-thaw stability, precision, and accuracy. Twenty-four healthy volunteers were enrolled in this study. After overnight fasting, the two formulations (test and reference) of ibuprofen (100 mg ibuprofen/5 mL suspension) were administered as a single dose on two treatment days separated by a one-week washout period. After dosing, serial blood samples were drawn for a period of 14 hours. Serum harvested from the blood samples was analyzed for the presence of ibuprofen by high-pressure liquid chromatography with ultraviolet detection. Pharmacokinetic parameters were determined from serum concentrations for both formulations. The 90% confidence intervals of the ln-transformed test/reference treatment ratios for peak plasma concentration and area under the concentration-time curve (AUC) parameters were found to be within the predetermined acceptable interval of 80%-125% set by the US Food and Drug Administration. Conclusion: Analysis of variance for peak plasma concentrations and AUC parameters showed no significant difference between the two formulations and, therefore, Doloraz was considered bioequivalent to Brufen. 2011 Al-Talla et al, publisher and licensee Dove Medical Press Ltd.

  4. Ibuprofen in paediatrics: pharmacology, prescribing and controversies.

    Science.gov (United States)

    Moriarty, Camilla; Carroll, Will

    2016-12-01

    Ibuprofen, a propionic acid derivative, is a non-steroidal anti-inflammatory drug. The oral formulation is widely used in paediatric practice and after paracetamol it is one of the most common drugs prescribed for children in hospital. The treatment of fever with antipyretics such as ibuprofen is controversial as fever is the normal response of the body to infection and unless the child becomes distressed or symptomatic, fever alone should not be routinely treated. Combined treatment with paracetamol and ibuprofen is commonly undertaken but almost certainly is not helpful. This article aims to describe the indications and mode of action of the drug, outline its pharmacokinetics and highlight the important key messages regarding its use in clinical practice. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://www.bmj.com/company/products-services/rights-and-licensing/.

  5. Bioequivalence assessment of two formulations of ibuprofen

    Directory of Open Access Journals (Sweden)

    Al-Talla ZA

    2011-10-01

    Full Text Available Zeyad A Al-Talla1, Sabah H Akrawi2, Luke T Tolley3, Salim H Sioud1, Mohammed F Zaater4, Abdul-Hamid M Emwas1 1Analytical and NMR Core Laboratories, King Abdullah University of Science and Technology, Thuwal, Kingdom of Saudia Arabia; 2College of Pharmacy, Al-Ain University, Al-Ain, United Arab Emirates; 3Department of Chemistry and Biochemistry, Southern Illinois University Carbondale, Carbondale, IL, USA; 4Department of Chemistry, Jordan University of Science and Technology, Jordan University of Science and Technology, Irbid, Jordan Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz®, produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen®, manufactured by Boots Company, Nottingham, UK. Methods and results: A prestudy validation of ibuprofen demonstrated long-term stability, freeze-thaw stability, precision, and accuracy. Twenty-four healthy volunteers were enrolled in this study. After overnight fasting, the two formulations (test and reference of ibuprofen (100 mg ibuprofen/5 mL suspension were administered as a single dose on two treatment days separated by a one-week washout period. After dosing, serial blood samples were drawn for a period of 14 hours. Serum harvested from the blood samples was analyzed for the presence of ibuprofen by high-pressure liquid chromatography with ultraviolet detection. Pharmacokinetic parameters were determined from serum concentrations for both formulations. The 90% confidence intervals of the ln-transformed test/reference treatment ratios for peak plasma concentration and area under the concentration-time curve (AUC parameters were found to be within the predetermined acceptable interval of 80%–125% set by the US Food and Drug Administration. Conclusion: Analysis of variance for peak plasma concentrations and AUC parameters showed no significant difference between the two formulations and

  6. Synthesis of carbon-13 labeled ibuprofen

    International Nuclear Information System (INIS)

    Hsi, R.S.P.; Stelzer, L.S.; Stolle, W.T.

    1989-01-01

    This report describes the synthesis of 2-[4-(2-methyl)propyl-phenyl]propionic acid (ibuprofen) labeled with carbon-13 either at the terminal methyl carbons, or at the methine carbon of the isobutyl side chain. The synthetic route involves the removal of the isopropyl group in the isobutyl side-chain of ibuprofen via 2-[4-(2-methyl-1-propenyl)phenyl]propionic acid, followed by restoration of the isopropyl group with a Wittig reaction, using appropriate carbon-13 labeled acetone as the precursor of the isopropyl group. Interesting NMR coupling data attributable to phosphorous and carbon-13 are presented in the experimental section. (author)

  7. Impact of Chiral Bioanalytical Methods on the Bioequivalence of Ibuprofen Products Containing Ibuprofen Lysinate and Ibuprofen Base.

    Science.gov (United States)

    García-Arieta, Alfredo; Ferrero-Cafiero, Juan Manuel; Puntes, Montse; Gich, Ignasi; Morales-Alcelay, Susana; Tarré, Maite; Font, Xavier; Antonijoan, Rosa Maria

    2016-05-01

    The purpose was to assess the impact of the use of a chiral bioanalytical method on the conclusions of a bioequivalence study that compared two ibuprofen suspensions with different rates of absorption. A comparison of the conclusion of bioequivalence between a chiral method and an achiral approach was made. Plasma concentrations of R-ibuprofen and S-ibuprofen were determined using a chiral bioanalytical method; bioequivalence was tested for R-ibuprofen and for S-ibuprofen separately and for the sum of both enantiomers as an approach for an achiral bioanalytical method. The 90% confidence interval (90% CI) that would have been obtained with an achiral bioanalytical method (90% CI: Cmax: 117.69-134.46; AUC0 (t) : 104.75-114.45) would have precluded the conclusion of bioequivalence. This conclusion cannot be generalized to the active enantiomer (90% CI: Cmax : 103.36-118.38; AUC0 (t) : 96.52-103.12), for which bioequivalence can be concluded, and/or the distomer (90% CI: Cmax : 132.97-151.33; AUC0 (t) : 115.91-135.77) for which a larger difference was observed. Chiral bioanalytical methods should be required when 1) the enantiomers exhibit different pharmacodynamics and 2) the exposure (AUC or Cmax ) ratio of enantiomers is modified by a difference in the rate of absorption. Furthermore, the bioequivalence conclusion should be based on all enantiomers, since the distomer(s) might not be completely inert, in contrast to what is required in the current regulatory guidelines. In those cases where it is unknown if the ratio between enantiomers is modified by changing the rate of absorption, chiral bioanalytical methods should be employed unless enantiomers exhibit the same pharmacodynamics. Chirality 28:429-433, 2016. © 2016 Wiley Periodicals, Inc. © 2016 Wiley Periodicals, Inc.

  8. Preparation, Characterization and Optimization of Ibuprofen ...

    African Journals Online (AJOL)

    Purpose: To develop an ibuprofen ointment with a potential for both topical and systemic delivery of the drug. Method: A co-solvency technique with a trial and error approach was used to develop a 10% ibioprofen ointment in petrolatum base, with the entire drug dissolved in the base. An insertion cell was used to evaluate ...

  9. The tritium labelling of ibuprofen by heterogeneous catalytic exchange

    International Nuclear Information System (INIS)

    Santamaria, J.; Rebollo, D.V.; Rivera, P.; Estaban, M.

    1986-01-01

    The tritium labelling of 2-(4-isobutylphenyl) propionic acid (ibuprofen) was performed. The method employed was heterogeneous catalytic exchange between ibuprofen and tritiated water. Prior to labelling, thermic stability of ibuprofen was studied. Purification was accomplished through thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Concentration, purity and specific activity of the labelled compound were determined by ultraviolet, HPLC and liquid scintillation techniques. (author)

  10. Ibuprofen regulation of microtubule dynamics in cystic fibrosis epithelial cells.

    Science.gov (United States)

    Rymut, Sharon M; Kampman, Claire M; Corey, Deborah A; Endres, Tori; Cotton, Calvin U; Kelley, Thomas J

    2016-08-01

    High-dose ibuprofen, an effective anti-inflammatory therapy for the treatment of cystic fibrosis (CF), has been shown to preserve lung function in a pediatric population. Despite its efficacy, few patients receive ibuprofen treatment due to potential renal and gastrointestinal toxicity. The mechanism of ibuprofen efficacy is also unclear. We have previously demonstrated that CF microtubules are slower to reform after depolymerization compared with respective wild-type controls. Slower microtubule dynamics in CF cells are responsible for impaired intracellular transport and are related to inflammatory signaling. Here, it is identified that high-dose ibuprofen treatment in both CF cell models and primary CF nasal epithelial cells restores microtubule reformation rates to wild-type levels, as well as induce extension of microtubules to the cell periphery. Ibuprofen treatment also restores microtubule-dependent intracellular transport monitored by measuring intracellular cholesterol transport. These effects are specific to ibuprofen as other cyclooxygenase inhibitors have no effect on these measures. Effects of ibuprofen are mimicked by stimulation of AMPK and blocked by the AMPK inhibitor compound C. We conclude that high-dose ibuprofen treatment enhances microtubule formation in CF cells likely through an AMPK-related pathway. These findings define a potential mechanism to explain the efficacy of ibuprofen therapy in CF. Copyright © 2016 the American Physiological Society.

  11. Ibuprofen plus paracetamol versus ibuprofen in acute low back pain: a randomized open label multicenter clinical study.

    Science.gov (United States)

    Ostojic, Predrag; Radunovic, Goran; Lazovic, Milica; Tomanovic-Vujadinovic, Sanja

    2017-01-01

    to estimate whether combination of ibuprofen and paracetamol is more effective than ibuprofen in monotherapy, in the treatment of acute low back pain. 80 adult patients with acute low back pain were randomized into two subgroups. In the first subgroup, 40 patients were treated with ibuprofen 400mg three times a day (TID), whilst patients in the second subgroup (n=40) were treated with a fixed-dose combination tablet of ibuprofen 200mg plus paracetamol 325mg TID, for three consecutive days. Patients were followed for another 7 days. Efficacy and tolerability of both treatment options was assessed. A statistically significant decrease in pain intensity, assessed using a visual analogue scale (pibuprofen monotherapy reported minor gastric intolerability. compared to ibuprofen monotherapy, combination of ibuprofen and paracetamol may provide faster and longer analgesia in patients with acute low back pain, with equally favorable effect on mobility and functional ability and similar tolerability.

  12. Design and study of some novel ibuprofen derivatives with potential nootropic and neuroprotective properties.

    Science.gov (United States)

    Siskou, Ioanna C; Rekka, Eleni A; Kourounakis, Angeliki P; Chrysselis, Michael C; Tsiakitzis, Kariofyllis; Kourounakis, Panos N

    2007-01-15

    Six novel ibuprofen derivatives and related structures, incorporating a proline moiety and designed for neurodegenerative disorders, are studied. They possess anti-inflammatory properties and three of them inhibited lipoxygenase. One compound was found to inhibit cyclooxygenase (COX)-2 production in spleenocytes from arthritic rats. The HS-containing compounds are potent antioxidants and one of them protected against glutathione loss after cerebral ischemia/reperfusion. They demonstrated lipid-lowering ability and seem to acquire low gastrointestinal toxicity. Acetylcholinesterase inhibitory activity, found in two of these compounds, may be an asset to their actions.

  13. Formulation and evaluation of a novel matrix-type orally disintegrating Ibuprofen tablet.

    Science.gov (United States)

    Tayebi, Hoda; Mortazavi, Seyed Alireza

    2011-01-01

    Orally disintegrating tablets (ODTs) are capable of turning quickly into a liquid dosage form in contact with the saliva, thus possessing the advantages of both the solid dosage forms particularly stability and liquid dosage forms specially ease of swallowing and pre-gastric absorption of drug. The aim of this study was to prepare a novel matrix-type buccal fast disintegrating ibuprofen tablet formulation using special polymers, water soluble excipients, super-disintegrants and quickly soluble granules. For this purpose different tablet formulations of ibuprofen were prepared. The amount of ibuprofen in each formulation was 100 mg. Eight groups of formulation were prepared (A-H series), accounting for a total number of 45 formulations. Formulations prepared were examined in terms of different physicochemical tests including powder/granule flowability, appearance, thickness, uniformity of weight, hardness, friability and disintegration time. Results of formulation F22a (in series F), was found to be acceptable, making it the chosen formulation for further studies. Then, by adding various flavorants and sweeteners to this formulation, complementary series of formulations, named G and H, were prepared. Following the comparison of their taste with each other through asking 10 volunteers, the most suitable formulation regarding the taste, being formulation F22s, was chosen as the ultimate formulation. This formulation had PVP, ibuprofen and croscarmellose as the intra-granular components and xylitol and saccharin as the extra-granular ingredients. Formulation F22s was found to be acceptable in terms of physicochemical tests conducted, showing quick disintegration within the buccal cavity, appropriate hardness and rather low friability. Hence formulation F22s was selected as the final formulation.

  14. Effect Of Formulating Additives On The Properties Of Ibuprofen Tablets

    African Journals Online (AJOL)

    A study of the comparative effects of different formulating additives and film coating on the properties of ibuprofen tablets was made. The tested properties were hardeness (H), friability (F), the disintegration time (D) and dissolution characteristics of ibuprofen tablets. The hardeness, friability, the hardeness friability ratio ...

  15. Ibuprofen pharmacokinetics in preterm infants with patent ductus arteriosus

    NARCIS (Netherlands)

    Van Overmeire, B; Touw, D; Schepens, P J; Kearns, G L; van den Anker, J N

    2001-01-01

    OBJECTIVE: Our objective was to study the pharmacokinetics of ibuprofen in premature infants with patent ductus arteriosus on day 3 and day 5 after birth. METHODS: Ibuprofen was administered on days 3, 4, and 5 by a 15-minute intravenous infusion of 10, 5, and 5 mg/kg, respectively, with the aim of

  16. Polyuria, acidosis, and coma following massive ibuprofen ingestion.

    Science.gov (United States)

    Levine, Michael; Khurana, Amandeep; Ruha, Anne-Michelle

    2010-09-01

    Ibuprofen was the first over-the-counter nonsteroidal anti-inflammatory drug available in the United States. Despite being a common agent of ingestion, significant toxicity in overdose is rare. We report a case of a massive ibuprofen ingestion who developed polyuria, acidosis, and coma but survived, despite having a serum ibuprofen concentration greater than previous fatal cases. A 19-year-old man ingested 90 g (1,200 mg/kg) ibuprofen. He was initially awake and alert, but his level of consciousness deteriorated over several hours. Seven hours following the ingestion, he was intubated and mechanically ventilated secondary to loss of airway reflexes. He developed a lactic acidosis and polyuria, which lasted for nearly 24 h. His serum creatinine peaked at 1.12 mg/dL. An ibuprofen level drawn 7 h postingestion was 739.2 mg/L (therapeutic 5-49 mg/L). We describe a case of a massive ibuprofen overdose characterized by metabolic acidosis, coma, and a state of high urine output who survived with aggressive supportive care. This case is unique in several ways. First, ibuprofen levels this high have only rarely been described. Second, polyuria is very poorly described following ibuprofen ingestions.

  17. Fulvic Acid Mediated Photolysis of Ibuprofen in Water.

    Science.gov (United States)

    Photolysis of the nonsteroidal anti-inflammatory drug ibuprofen was studied in solutions of fulvic acid (FA) isolated from Pony Lake, Antarctica; Suwannee River, GA, USA; and Old Woman Creek, OH, USA. At an initial concentration of 10 µM ibuprofen degrades by direct photolysis...

  18. Serum ibuprofen levels of extremely preterm infants treated prophylactically with oral ibuprofen to prevent patent ductus arteriosus

    NARCIS (Netherlands)

    Kanmaz, Gozde; Erdeve, Omer; Canpolat, Fuat Emre; Oguz, Serife Suna; Uras, Nurdan; Altug, Nahide; Greijdanus, Ben; Dilmen, Ugur

    The aim of this study was to explore the effects of early oral ibuprofen administration on the incidence of hemodynamically significant patent ductus arteriosus (hsPDA) and define the association between serum ibuprofen levels and ductal closure. Preterm infants with a gestational age of <28 weeks

  19. Ibuprofen - a Safe Analgesic During Cardiac Surgery Recovery?

    DEFF Research Database (Denmark)

    Qazi, Saddiq Mohammad; Sindby, Eske Jesper; Nørgaard, Martin Agge

    2015-01-01

    were undergoing cardiac surgery for the first time, were randomly allocated either to a regimen of slow-release oxycodone (10 mg twice daily) or slow-release ibuprofen (800 mg twice daily) combined with lansoprazole. Data relating to blood-tests, angiographies, surgical details and administered...... if short term slow release ibuprofen combined with lansoprazole treatment is used when compared to an oxycodone based regimen. Renal function should, however, be closely monitored and in the event of any decrease in renal function ibuprofen must be discontinued....

  20. Individual ball possession in soccer.

    Directory of Open Access Journals (Sweden)

    Daniel Link

    Full Text Available This paper describes models for detecting individual and team ball possession in soccer based on position data. The types of ball possession are classified as Individual Ball Possession (IBC, Individual Ball Action (IBA, Individual Ball Control (IBC, Team Ball Possession (TBP, Team Ball Control (TBC und Team Playmaking (TPM according to different starting points and endpoints and the type of ball control involved. The machine learning approach used is able to determine how long the ball spends in the sphere of influence of a player based on the distance between the players and the ball together with their direction of motion, speed and the acceleration of the ball. The degree of ball control exhibited during this phase is classified based on the spatio-temporal configuration of the player controlling the ball, the ball itself and opposing players using a Bayesian network. The evaluation and application of this approach uses data from 60 matches in the German Bundesliga season of 2013/14, including 69,667 IBA intervals. The identification rate was F = .88 for IBA and F = .83 for IBP, and the classification rate for IBC was κ = .67. Match analysis showed the following mean values per match: TBP 56:04 ± 5:12 min, TPM 50:01 ± 7:05 min and TBC 17:49 ± 8:13 min. There were 836 ± 424 IBC intervals per match and their number was significantly reduced by -5.1% from the 1st to 2nd half. The analysis of ball possession at the player level indicates shortest accumulated IBC times for the central forwards (0:49 ± 0:43 min and the longest for goalkeepers (1:38 ± 0:58 min, central defenders (1:38 ± 1:09 min and central midfielders (1:27 ± 1:08 min. The results could improve performance analysis in soccer, help to detect match events automatically, and allow discernment of higher value tactical structures, which is based on individual ball possession.

  1. Importance of acute renal failure with ibuprofen

    Directory of Open Access Journals (Sweden)

    Tufan F

    2014-05-01

    Full Text Available Fatih Tufan Sevket Yilmaz Training and Research Hospital, Geriatrics Unit, Yildirim, Bursa, TurkeyKuptniratsaikul et al report the efficacy of Curcuma domestica extracts in the treatment of knee osteoarthritis.1 One of my concerns about this well designed study is lack of one important adverse event assessment. One of the most important adverse effects of ibuprofen, which is a non-selective non-steroid anti-inflammatory drug, is acute renal failure.2 Although one of the exclusion criteria in this study is renal failure, especially in the elderly population, it is crucial to follow up kidney functions under non-steroid anti-inflammatory treatment.View original paper by Kuptniratsaikul and colleagues. 

  2. Layered zinc hydroxide–ibuprofen nanohybrids: synthesis and ...

    Indian Academy of Sciences (India)

    The nonsteroidal anti-inflammatory drug (NSAID), ibuprofen (IBU) anion, was intercalated into the layered zinc ... surface morphology, Fourier transform infrared (FTIR) spectrophotometer to study the chemical interactions and ..... J. Food Sci.

  3. Impact of pore characteristics of silica materials on loading capacity and release behavior of ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Numpilai, Thanapha [Department of Chemical Engineering, Faculty of Engineering, Kasetsart University, Bangkok 10900 (Thailand); Muenmee, Suthaporn [Department of Chemical Engineering, Faculty of Engineering, Kasetsart University, Bangkok 10900 (Thailand); Center for Advanced Studies in Nanotechnology and Its Applications in Chemical Food and Agricultural Industries, Kasetsart University, Bangkok 10900 (Thailand); Witoon, Thongthai, E-mail: fengttwi@ku.ac.th [Department of Chemical Engineering, Faculty of Engineering, Kasetsart University, Bangkok 10900 (Thailand); Center for Advanced Studies in Nanotechnology and Its Applications in Chemical Food and Agricultural Industries, Kasetsart University, Bangkok 10900 (Thailand); NANOTEC-KU-Center of Excellence on Nanoscale Materials Design for Green Nanotechnology, Kasetsart University, Bangkok 10900 (Thailand)

    2016-02-01

    Impact of pore characteristics of porous silica supports on loading capacity and release behavior of ibuprofen was investigated. The porous silica materials and ibuprofen-loaded porous silica materials were thoroughly characterized by N{sub 2}-sorption, thermal gravimetric and derivative weight analyses (TG-DTW), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), transmission electron microscope (TEM) to determine the physical properties of materials, amount of ibuprofen adsorbed and position of ibuprofen. The detailed characterization reveals that the ibuprofen molecules adsorbed inside the mesopores. Increasing the mesopore size from 5 nm to 10 nm increased the ibuprofen loading from 0.74 to 0.85 mmol/g, respectively. Incorporation of macropore into the structure of porous silica materials enhanced the ibuprofen loading capacity of 11.8–20.3%. The ibuprofen-loaded bimodal meso-macroporous silica materials exhibited the highest dissolution of 92 wt.% within an hour. The ibuprofen particles deposited on the external surface of the porous silica materials showed a lower dissolution rate than the ibuprofen adsorbed inside the mesopores due to the formation of ibuprofen crystalline. - Highlights: • Impacts of pore characteristics of supports on adsorption and release of ibuprofen • Increasing mesopore size increased the ibuprofen loading and dissolution rate. • Macropores reduced the diffusion pathway of ibuprofen and dissolution medium.

  4. Impact of pore characteristics of silica materials on loading capacity and release behavior of ibuprofen

    International Nuclear Information System (INIS)

    Numpilai, Thanapha; Muenmee, Suthaporn; Witoon, Thongthai

    2016-01-01

    Impact of pore characteristics of porous silica supports on loading capacity and release behavior of ibuprofen was investigated. The porous silica materials and ibuprofen-loaded porous silica materials were thoroughly characterized by N 2 -sorption, thermal gravimetric and derivative weight analyses (TG-DTW), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), transmission electron microscope (TEM) to determine the physical properties of materials, amount of ibuprofen adsorbed and position of ibuprofen. The detailed characterization reveals that the ibuprofen molecules adsorbed inside the mesopores. Increasing the mesopore size from 5 nm to 10 nm increased the ibuprofen loading from 0.74 to 0.85 mmol/g, respectively. Incorporation of macropore into the structure of porous silica materials enhanced the ibuprofen loading capacity of 11.8–20.3%. The ibuprofen-loaded bimodal meso-macroporous silica materials exhibited the highest dissolution of 92 wt.% within an hour. The ibuprofen particles deposited on the external surface of the porous silica materials showed a lower dissolution rate than the ibuprofen adsorbed inside the mesopores due to the formation of ibuprofen crystalline. - Highlights: • Impacts of pore characteristics of supports on adsorption and release of ibuprofen • Increasing mesopore size increased the ibuprofen loading and dissolution rate. • Macropores reduced the diffusion pathway of ibuprofen and dissolution medium.

  5. MODELLING DICLOFENAC AND IBUPROFEN RESIDUES IN MAJOR ESTONIAN SEASIDE CITIES

    Directory of Open Access Journals (Sweden)

    Erki Lember

    2016-06-01

    Full Text Available A theoretical model was developed to model the fate of two common pharmaceutical residues: diclofenac and ibuprofen in eight Estonian seaside cities that discharge their wastewaters directly into the Baltic Sea. The consumption rates of the active ingredients of diclofenac and ibuprofen from 2006-2014 were analysed. A decrease of 19.9% for diclofenac consumption and an increase of 14.1% for ibuprofen were found. The fate of diclofenac and ibuprofen were modelled by considering the human metabolism removal rate for pharmaceuticals, the removal rate of diclofenac and ibuprofen in activated sludge wastewater treatment plants (WWTP and annual flow rates. An average decrease from 1 to 0.8 µg/l (decrease of 20% for diclofenac and an increase from 11.4 to 13.4 µg/l (increase of 14.9% for ibuprofen for the concentration in the effluents of the WWTP were modelled. The model gives us a good overview about the theoretical concentrations of pharmaceutical residues in the environment and is helpful for evaluating environmental impacts.

  6. Controlled release of ibuprofen using Mg Al LDH nano carrier

    Science.gov (United States)

    Dasgupta, Sudip

    2017-08-01

    In the present study, NSAID (non-steroidal anti-inflammatory drugs) such as ibuprofen in anionic form has been intercalated in-situ into the interlayer space of Mg Al LDH nanoparticle during co-precipitation of hydroxides. LDH nanohybrids are characterized by XRD, FTIR and UV spectroscopy. Mg1-xAlx(NO3)x(OH)2.nH2O nanoparticles were synthesized using co-precipitation method from an aqueous solution of Mg(NO3)2.6H2O and Al(NO3)3.9H2O. Ibuprofen was intercalated in inter layer space of Mg-Al LDH during coprecipitation of drug LDH conjugate in nitrogen atmosphere. The nanopowders synthesised were in the size range between 25 to 90 nm with an average particle size of 55 nm. XRD analysis proved that there is an increase in d003 spacing from 7.89 Å for pristine LDH to 14.71 Å for ibuprofen intercalated LDH due to the intercalation of bigger ibuprofen molecule in the interlayer space of LDH. FTIR analysis showed hydroxyl and carbonyl stretching of ibuprofen in LDH-IBU sample confirming the intercalation of ibuprofen in the interlayer structure of LDH. The drug release study in phosphate buffer solution at pH 7.4 using UV-Vis spectroscopy demonstrated that 50 % drug molecules were released in 15 hours and more than 85 % release was achieved after 36 hours.

  7. Ibuprofen plus paracetamol versus ibuprofen in acute low back pain: a randomized open label multicenter clinical study

    Directory of Open Access Journals (Sweden)

    Predrag Ostojic

    2017-01-01

    Full Text Available Objective: to estimate whether combination of ibuprofen and paracetamol is more effective than ibuprofen in monotherapy, in the treatment of acute low back pain. Methods: 80 adult patients with acute low back pain were randomized into two subgroups. In the first subgroup, 40 patients were treated with ibuprofen 400mg three times a day (TID, whilst patients in the second subgroup (n=40 were treated with a fixed-dose combination tablet of ibuprofen 200mg plus paracetamol 325mg TID, for three consecutive days. Patients were followed for another 7 days. Efficacy and tolerability of both treatment options was assessed. Results: A statistically significant decrease in pain intensity, assessed using a visual analogue scale (p

  8. Randomized comparative trial of efficacy of paracetamol, ibuprofen and paracetamol-ibuprofen combination for treatment of febrile children

    Directory of Open Access Journals (Sweden)

    Falgun Indravadan Vyas

    2014-01-01

    Full Text Available Objective: Paracetamol and ibuprofen are widely used for fever in children as monotherapy and as combined therapy. None of the treatments is proven clearly superior to others. Hence, the study was planned to compare the efficacy of paracetamol, ibuprofen and paracetamol-ibuprofen combination for treatment of febrile children. Materials and Methods: This was an investigator blind, randomized, comparative, parallel clinical trial conducted in 99 febrile children, 6 months to 12 years of age, allocated to three groups. First group received paracetamol 15 mg/kg, second group received ibuprofen 10 mg/kg and third group received both paracetamol and ibuprofen, all as a single dose by the oral route. Patients were followed-up at intervals of 1, 2, 3 and 4 h post dose by tympanic thermometry. Results: Mean tympanic temperature after 4 h of drug administration was significantly lower in the combination group compared with paracetamol group (P < 0.05; however, the difference was not clinically significant (<1΀C. The rate of fall of temperature was highest in the combination group. Number of afebrile children any time post dose until 4 h was highest in the combination group. Difference between combination and paracetamol was significant for the 1 st h (P = 0.04. Highest fall of temperature was noted in the 1 st h of drug administration in all the groups. No serious adverse events were observed in any of the groups. Conclusion: Paracetamol and ibuprofen combination caused quicker temperature reduction than either paracetamol or ibuprofen alone. If quicker reduction of body temperature is the desired goal of therapy, the use of combination of paracetamol + ibuprofen may be advocated.

  9. Ibuprofen: from invention to an OTC therapeutic mainstay.

    Science.gov (United States)

    Rainsford, K D

    2013-01-01

    The discovery of ibuprofen's anti-inflammatory activity by Dr (now Professor) Stewart Adams and colleagues (Boots Pure Chemical Company Ltd, Nottingham, UK) 50 years ago represented a milestone in the development of anti-inflammatory analgesics. Subsequent clinical studies were the basis for ibuprofen being widely accepted for treating painful conditions at high anti-rheumatic doses (≤ 2400 mg/d), with lower doses (≤ 1200 mg/d for ≤ 10 days) for mild-moderate acute pain (e.g. dental pain, headache, dysmenorrhoea, respiratory symptoms and acute injury). The early observations have since been verified in studies comparing ibuprofen with newer cyclo-oxygenase-2 selective inhibitors ('coxibs'), paracetamol and other non-steroidal anti-inflammatory drugs (NSAIDs). The use of the low-dose, non-prescription, over-the-counter (OTC) drug was based on marketing approval in 1983 (UK) and 1984 (USA); and it is now available in over 80 countries. The relative safety of OTC ibuprofen has been supported by large-scale controlled studies. It has the same low gastro-intestinal (GI) effects as paracetamol (acetaminophen) and fewer GI effects than aspirin. Ibuprofen is a racemate. Its physicochemical properties and the short plasma-elimination half-life of the R(-) isomer, together with its limited ability to inhibit cyclo-oxygenase-1 (COX-1) and thus prostaglandin (PG) synthesis, compared with that of S(+)-ibuprofen, are responsible for the relatively low GI toxicity. The R(-) isomer is then converted in the body to the S(+) isomer after absorption in the GI tract. Ex vivo inhibition of COX-1 (thromboxane A(2)) and COX-2 (PGE(2)) at the plasma concentrations of S(+)-ibuprofen corresponding to those found in the plasma following ingestion of 400 mg ibuprofen in dental and other inflammatory pain models provides evidence of the anti-inflammatory mechanism at OTC dosages. R(-)-ibuprofen has effects on leucocytes, suggesting that ibuprofen has anti-leucocyte effects, which

  10. A novel NSAID derivative, phospho-ibuprofen, prevents AOM-induced colon cancer in rats

    Science.gov (United States)

    OUYANG, NENGTAI; JI, PING; WILLIAMS, JENNIE L.

    2013-01-01

    The cancer chemopreventive properties and gastrointestinal toxicity of ibuprofen are well documented. Modification of existing NSAIDs has improved on the chemopreventive efficacy of this agent and reduced its toxicity. In this study, ibuprofen and a modified derivative (phospho-modified ibuprofen or p-ibuprofen) were used in a chemically induced model of colon cancer. Fisher 344 rats were injected with azoxymethane then treated with either ibuprofen (500 ppm) or p-ibuprofen (900 ppm) for 20 weeks to observe aberrant crypt foci (ACF) or 40 weeks to evaluate tumor incidence and multiplicity. β-catenin and p65 were measured in colonic tissues by immunofluorescence staining. Equal molar doses of ibuprofen (75 and 670 mg/kg) and p-ibuprofen (135 and 1,215 mg/kg) were administered to rats for 7 days to assess acute toxicity. The in vitro effect of p-ibuprofen on COX-2 and PGE2 synthesis, β-catenin expression and NF-κB activity were examined in RAW 264.7 macrophage and HCT 116 colon cancer cells. At week 20, p-ibuprofen and ibuprofen significantly reduced the multiplicity of ACF compared with control (pibuprofen and ibuprofen reduced the multiplicity of colon tumors compared with control (pibuprofen (670 mg/kg) and p-ibuprofen (1,215 mg/kg) resulted in stomach ulceration in 85.7% (6 out of 7) and 14.3% (1 out of 7) of rats, respectively, with pibuprofen and p-ibuprofen suppressed β-catenin nuclear translocation in colon cancer cells. In addition, p-ibuprofen but not ibuprofen inhibited NF-κB activation in colon cancer cells. Collectively, these results suggest that p-ibuprofen is a potential effective novel drug for long-term use in colon cancer prevention. PMID:23291777

  11. Formulation and in vitro evaluation of ibuprofen-loaded poly(D,L ...

    African Journals Online (AJOL)

    co-glycolide) (PLGA) microparticles. Methods: Ibuprofen-loaded microparticles containing PLGA were formulated using a emulsification/solvent evaporation method. Various concentrations of ibuprofen (200, 300, 400 and 0 mg) were loaded ...

  12. Cubic phase nanoparticles for sustained release of ibuprofen: formulation, characterization, and enhanced bioavailability study

    Science.gov (United States)

    Dian, Linghui; Yang, Zhiwen; Li, Feng; Wang, Zhouhua; Pan, Xin; Peng, Xinsheng; Huang, Xintian; Guo, Zhefei; Quan, Guilan; Shi, Xuan; Chen, Bao; Li, Ge; Wu, Chuanbin

    2013-01-01

    In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment. PMID:23468008

  13. Morpho-physiological effects of ibuprofen on Scenedesmus rubescens.

    Science.gov (United States)

    Moro, Isabella; Matozzo, Valerio; Piovan, Anna; Moschin, Emanuela; Vecchia, Francesca Dalla

    2014-09-01

    The pollution of aquatic bodies by drugs is an emerging environmental problem, because of their extensive use in animal and human context. Ibuprofen, 2-[4-(2-methylpropyl)phenyl]propanoic acid, is the non-steroidal anti-inflammatory drug mainly present both in wastewater and in rivers and lakes in Europe. Since in literature there is little information about the effects of ibuprofen on microalgae, in this paper we presented the results on the effects of this molecule at different concentrations (62.5μgL(-1), 250μgL(-1) and 1000μgL(-1)) on cultures of the freshwater microalga Scenedesmus rubescens (P.J.L. Dangeard) E. Kesslet et al. Ibuprofen effects on the alga were assayed at first through analyses of the growth curve. Moreover, analyses of cell morphology, ultrastructure, and photosynthetic pigments were additionally performed. The first negative effect of the drug was on the microalga growth, suggesting a drug action dose-dependent mechanism type, more evident at the concentration of 1000μgL(-1) ibuprofen and in the last phase of the growth curve. In support of this, following ibuprofen exposure, the cells exhibited morphological and ultrastructural alterations, mainly consisting in large cytoplasmic inclusions, probably of lipids and/or carotenoids. The decrease of chlorophyll amounts and, on the contrary, the increase of carotenoids were correlated with a stressful condition induced by drug. Copyright © 2014 Elsevier B.V. All rights reserved.

  14. APPLICATION OF POWDERY ACTIVATED CARBONS FOR REMOVAL IBUPROFEN FROM WATER

    Directory of Open Access Journals (Sweden)

    Alicja Puszkarewicz

    2017-07-01

    Full Text Available The paper presents results of studies on the use of adsorptive properties of selected powdered activated carbons (Norit SA Super and Carbopol MB5 for removal of ibuprofen from water. The tests were performed on non-flow conditions, series depending on the type and dose of powdered adsorbents. The research was carried out on a model solution of ibuprofen at initial concentration C0 = 20 mg/dm3, at 200 C. Froundlich and Langmuir adsorption isotherms were used. Lagergrene kinetic models (PFO and Ho (PSO were used to describe adsorption kinetics. Both carbons exhibited a higher affinity for the adsorbent at a pH above 7. The better adsorbent was the Norit SA Super, for which, the highest adsorption capacity q = 0.448 g/g was achieved with dose D = 35 mg/dm3. The effectiveness of adsorption (decrease of ibuprofen in water was 78%. Total removal of ibuprofen was obtained for a dose of carbon D = 200 mg/dm3. With respect to Carbopol, the highest adsorption capacity (q = 0.353 g / g was achieved at a dose of 30 mg / dm3, resulting in a 53% efficiency. Studies have shown that both tested powdered activated carbons have contributed to effective cleaning of aqueous solutions containing ibuprofen.

  15. Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen

    DEFF Research Database (Denmark)

    Lynagh, Timothy; Romero-Rojo, José Luis; Lund, Camilla

    2017-01-01

    -clamp fluorometry. Our results show that ibuprofen is an allosteric inhibitor of ASIC1a, which binds to a crucial site in the agonist transduction pathway and causes conformational changes that oppose channel activation. Ibuprofen inhibits several ASIC subtypes, but certain ibuprofen derivatives show some...

  16. Enhancement of transdermal delivery of ibuprofen using microemulsion vehicle.

    Science.gov (United States)

    Hu, Liandong; Hu, Qiaofeng; Yang, Jianxue

    2014-10-01

    The objective of this study was to find a stable microemulsion vehicle for transdermal delivery of ibuprofen to improve the skin permeability. Microemulsion was prepared using different sorts of oils, surfactants and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The effects of oleic acid and surfactant mixture on skin permeation of ibuprofen were evaluated with excised skins. The optimum formulation F3 consisting of 6% oleic acid, 30% Cremophor RH40/Transcutol P (2:1, w/w) and 59% water phase, showed a high permeation rate of 42.98 µg/cm(2)/hr. The mean droplet size of microemulsion was about 43 nm and no skin irritation signs were observed on the skin of rabbits. These results indicated that this novel microemulsion is a useful formulation for the transdermal delivery of ibuprofen.

  17. Growth, spectral and thermal studies of ibuprofen crystals

    Energy Technology Data Exchange (ETDEWEB)

    Ramukutty, S.; Ramachandran, E. [Department of Physics, Thiruvalluvar College, Papanasam (India)

    2012-01-15

    RS -Ibuprofen was crystallized for the first time in silica gel under suitable pH conditions by reduction of solubility method. The grown crystals were characterized by single crystal X-ray diffraction and density measurement. The functional groups present in the crystal were identified using Fourier transform infrared spectroscopy. Optical bandgap energy of ibuprofen was estimated as 3.19(3) eV from UV-Vis spectrum. Thermogravimetric analysis revealed that ibuprofen is thermally stable upto 102.9 C and the initial loss of mass was due to evaporation only. Morphological study showed that the growth is prominent along b-axis and the prominent face is {l_brace}100{r_brace}. (copyright 2012 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim) (orig.)

  18. Impregnation of Ibuprofen into Polycaprolactone using supercritical carbon dioxide

    Energy Technology Data Exchange (ETDEWEB)

    Yoganathan, Roshan; Mammucari, Raffaella; Foster, Neil R, E-mail: n.foster@unsw.edu.a [Supercritical Fluids Research Group, School of Chemical Sciences and Engineering, University of New South Wales, NSW 2052 (Australia)

    2010-03-01

    Polycaprolactone (PCL) is a Food and Drug Administration (FDA) approved biodegradable polyester used in tissue engineering applications. Ibuprofen is an anti-inflammatory drug which has good solubility in supercritical CO{sub 2} (SCCO{sub 2}). The solubility of CO{sub 2} in PCL allows for the impregnation of CO{sub 2}-soluble therapeutic agents into the polymer via a supercritical fluid (SCF) process. Polymers impregnated with bio-active compounds are highly desired for medical implants and controlled drug delivery. In this study, the use of CO{sub 2} to impregnate PCL with ibuprofen was investigated. The effect of operating conditions on the impregnation of ibuprofen into PCL was investigated over two pressure and two temperature levels, 150bar and 200bar, 35{sup 0}C and 40 {sup 0}C, respectively. Polycaprolactone with drug-loadings as high as 27% w/w were obtained. Impregnated samples exhibited controlled drug release profiles over several days.

  19. Impregnation of Ibuprofen into Polycaprolactone using supercritical carbon dioxide

    International Nuclear Information System (INIS)

    Yoganathan, Roshan; Mammucari, Raffaella; Foster, Neil R

    2010-01-01

    Polycaprolactone (PCL) is a Food and Drug Administration (FDA) approved biodegradable polyester used in tissue engineering applications. Ibuprofen is an anti-inflammatory drug which has good solubility in supercritical CO 2 (SCCO 2 ). The solubility of CO 2 in PCL allows for the impregnation of CO 2 -soluble therapeutic agents into the polymer via a supercritical fluid (SCF) process. Polymers impregnated with bio-active compounds are highly desired for medical implants and controlled drug delivery. In this study, the use of CO 2 to impregnate PCL with ibuprofen was investigated. The effect of operating conditions on the impregnation of ibuprofen into PCL was investigated over two pressure and two temperature levels, 150bar and 200bar, 35 0 C and 40 0 C, respectively. Polycaprolactone with drug-loadings as high as 27% w/w were obtained. Impregnated samples exhibited controlled drug release profiles over several days.

  20. The qualified possession turn into ownership

    Directory of Open Access Journals (Sweden)

    Popov Danica

    2011-01-01

    Full Text Available Possession is prima facie evidence of ownership. Possession is ninetents of the law, means that possession is good against all other, except the true owner. The possession ripens into ownership if it is qualified and by effluxion of time. In Serbian law there are two kinds of adverse possession ripens into ownership. The first one is named ordinary and second one extraordinary adverse possession. Ordinary possession need to be legal, conscientious and genuine. Extraordinary possession is only conscientious, but in a wide sense. Adverse possession destroys the title of the owner and vests it in possessor. An occupation of land inconsistent with the right of the true owner: the possession of those against whom a right action has accured to the true owner. It is actual possession in the absence of possession by the rightful owner and without lawful title. If the adverse possession continues, the effect at the expiration of the prescribed period is that not only the remedy but the title of former owner is extinguished. The person in adverse possession gains a new possessory title which cannot, normally exceed in extent of duration the interest of the former owner.

  1. Ibuprofen Blunts Ventilatory Acclimatization to Sustained Hypoxia in Humans.

    Directory of Open Access Journals (Sweden)

    Kemal Erdem Basaran

    Full Text Available Ventilatory acclimatization to hypoxia is a time-dependent increase in ventilation and the hypoxic ventilatory response (HVR that involves neural plasticity in both carotid body chemoreceptors and brainstem respiratory centers. The mechanisms of such plasticity are not completely understood but recent animal studies show it can be blocked by administering ibuprofen, a nonsteroidal anti-inflammatory drug, during chronic hypoxia. We tested the hypothesis that ibuprofen would also block the increase in HVR with chronic hypoxia in humans in 15 healthy men and women using a double-blind, placebo controlled, cross-over trial. The isocapnic HVR was measured with standard methods in subjects treated with ibuprofen (400 mg every 8 hrs or placebo for 48 hours at sea level and 48 hours at high altitude (3,800 m. Subjects returned to sea level for at least 30 days prior to repeating the protocol with the opposite treatment. Ibuprofen significantly decreased the HVR after acclimatization to high altitude compared to placebo but it did not affect ventilation or arterial O2 saturation breathing ambient air at high altitude. Hence, compensatory responses prevent hypoventilation with decreased isocapnic ventilatory O2-sensitivity from ibuprofen at this altitude. The effect of ibuprofen to decrease the HVR in humans provides the first experimental evidence that a signaling mechanism described for ventilatory acclimatization to hypoxia in animal models also occurs in people. This establishes a foundation for the future experiments to test the potential role of different mechanisms for neural plasticity and ventilatory acclimatization in humans with chronic hypoxemia from lung disease.

  2. IBUPROFEN IN COMPLEX TREATMENT OF FEVER IN CHILDREN

    Directory of Open Access Journals (Sweden)

    А.А. Alexeeva

    2011-01-01

    Full Text Available Pain and fever are one of the most frequent conditions in pediatric practice. Frequent occurrence of fever accompanied by a pain syndrome stipulates combined antipyretic and analgesic medications. This article contains information upon ibuprofen use («Nurofen for children» in pediatric patients as an antipyretic and analgesic medication to be used as part of complex treatment of acute respiratory infections.Key words: fewer, children, ibuprofen. (Voprosy sovremennoi pediatrii — Current Pediatrics. — 2011; 10 (6: 137–140

  3. Spectral Analyses of a Novel Ibuprofen-Phillygenin Ester

    Directory of Open Access Journals (Sweden)

    FAN Hong-yu

    2018-03-01

    Full Text Available An ibuprofen-phillygenin ester was synthesized through the Schotten-Baumann reaction with ibuprofen and phillygenin as the starting materials. Ultraviolet absorption (UV spectrum, infrared absorption (IR spectrum, matrix-assisted laser desorption/ionization-mass spectra (MALDI-TOF-MS, and one-dimensional/two dimensional nuclear magnetic resonance (NMR spectra (i.e., 1H-NMR, 13C-NMR, 13C-DEPT, 1H-1H COSY, 1H-1H NOESY, 1H-13C HSQC and 1H-13C HMBC of the compound were collected. All 1H and 13C NMR signals were assigned.

  4. Cutaneous irritancy of an ibuprofen medicated plaster in healthy volunteers.

    Science.gov (United States)

    Maganji, Manisha; Connolly, Mark P; Bhatt, Aomesh

    2018-04-01

    To assess the irritation and contact sensitization potential of a 200 mg ibuprofen medicated plaster. This double-blind, phase-1 placebo controlled study had two phases; the induction phase to evaluate the irritant potential of continuous application of the plaster, and the challenge phase to assess contact sensitivity (allergy). The cumulative irritancy potential was evaluated using an adaptation of the Shelanski method. Healthy adults (≥18 years of age) (N = 210) were treated simultaneously with one ibuprofen medicated and one placebo plaster applied in a randomized fashion to either the left or right side of the lower back. During the induction phase, plasters were applied on Days 1, 3, 5, 8, 10, 12, 15, 17, and 19 and the final plaster removed on Day 22. At each scheduled visit plasters and applications sites were assessed for degree of adhesion and skin irritation (score of 1 = no irritation to 7 = strong reaction spreading beyond test sites), respectively. The challenge phase followed a two-week washout period. A plaster was applied on Day 36 for 48 h and assessment occurred on Days 38, 39, and 40. The mean cumulative irritation score during the induction phase was lower for the ibuprofen medicated plaster than the placebo plaster (0.32 vs. 1.23, respectively). Three (1.4%) subjects experience a dermal reaction of grade ≥3 for the ibuprofen medicated plaster compared with 27 (12.7%) for the placebo plaster. Following challenge with ibuprofen or placebo plasters, 12 subjects (6.2%) with the ibuprofen medicated plaster and four (2.2%) with the placebo plaster had skin reaction of assessment grade higher than the induction phase. One subject for the ibuprofen and two for the placebo plaster had reactions with grade >2. No subjects showed an increase in sensitization on Day 39 or 40 compared with Day 38. The findings indicate that the both the irritancy and contact sensitization of the ibuprofen medicated plaster is acceptable.

  5. Modeling the onset and offset of dental pain relief by ibuprofen.

    Science.gov (United States)

    Li, Hanbin; Mandema, Jaap; Wada, Russell; Jayawardena, Shyamalie; Desjardins, Paul; Doyle, Geraldine; Kellstein, David

    2012-01-01

    Onset and offset of dental pain relief by ibuprofen following third molar extraction were modeled in a randomized, double-blind, placebo-controlled, parallel-group, 8-hour study of patients receiving either a novel effervescent ibuprofen tablet (400 mg; N = 30), standard ibuprofen tablets (Nurofen(®) 2 × 200 mg; N = 22), or placebo (N = 37). An Emax model was fit to pain relief scores. Linear hazard models were used to analyze the time to first perceptible relief (TFPR), the time to meaningful pain relief (TMPR), and time to remedication (REMD). Nomograms were created to correlate TFPR, TMPR, and REMD with different ibuprofen pharmacokinetic profiles. Effervescent ibuprofen was absorbed rapidly with 95% completion within 15 minutes. Maximum pain relief score by ibuprofen was 1.8 units greater than placebo, with an EC50 (effect-site) for ibuprofen concentration of 10.2 µg·mL(-1). The likelihood to achieve TFPR and TMPR was doubled for every 10 µg·mL(-1) increase in ibuprofen plasma concentration. REMD risk decreased 40-fold as the categorical pain relief score increased from 0 to 3. Rapid absorption of ibuprofen effervescent resulted in an earlier TFPR and TMPR, and a lower REMD rate than standard ibuprofen. The nomograms may be useful in predicting the onset and offset of new faster acting ibuprofen formulations, based on pharmacokinetic profiles.

  6. Impact of pore characteristics of silica materials on loading capacity and release behavior of ibuprofen.

    Science.gov (United States)

    Numpilai, Thanapha; Muenmee, Suthaporn; Witoon, Thongthai

    2016-02-01

    Impact of pore characteristics of porous silica supports on loading capacity and release behavior of ibuprofen was investigated. The porous silica materials and ibuprofen-loaded porous silica materials were thoroughly characterized by N2-sorption, thermal gravimetric and derivative weight analyses (TG-DTW), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), transmission electron microscope (TEM) to determine the physical properties of materials, amount of ibuprofen adsorbed and position of ibuprofen. The detailed characterization reveals that the ibuprofen molecules adsorbed inside the mesopores. Increasing the mesopore size from 5nm to 10nm increased the ibuprofen loading from 0.74 to 0.85mmol/g, respectively. Incorporation of macropore into the structure of porous silica materials enhanced the ibuprofen loading capacity of 11.8-20.3%. The ibuprofen-loaded bimodal meso-macroporous silica materials exhibited the highest dissolution of 92wt.% within an hour. The ibuprofen particles deposited on the external surface of the porous silica materials showed a lower dissolution rate than the ibuprofen adsorbed inside the mesopores due to the formation of ibuprofen crystalline. Copyright © 2015 Elsevier B.V. All rights reserved.

  7. Radioiodination of ibuprofen with 125I and its biological behavior in mice

    International Nuclear Information System (INIS)

    Amin, A. M.; Abd El-bary, A.; Shoukry, M. and other

    2012-12-01

    A procedure for radioiodination of Ibuprofen with iodine-125 is carried out via an electrophilic substitution reaction. The reaction parameters were studied Ibuprofen concentration, pH of the reaction mixture, reaction time temperature, and different oxidizing agents to optimize the conditions for the labeling of Ibuprofen to abstain a high radiochemical yield of 1 25I -Ibuprofen (1 25I -Ib up). Using 3.7 MBq of of Na 1 25I , 100μg of ibuprofen as substrate and 100μg of iodogen as oxidizing agent in ethanol at 60 O C for 10 min, a maximum radiochemical yield of 1 25I -Ib up (78%) was obtained. The labeled compound was separated and purified from inactive Ibuprofen by means of high-pressure liquid chromatography (HPLC). The biological distribution in normal and inflamed mice indicates the suitability of radioiodinated Ibuprofen for imaging of inflammation only induced with turpentine oil. (Author)

  8. In vitro and in vivo therapeutic activity of ibuprofen against dermatophytes

    International Nuclear Information System (INIS)

    AlJanabi, Ali S

    2009-01-01

    To evaluate the in vitro and in vivo therapeutic activity of ibuprofen against dermatophytes. The period of study ranged from June to September 2008. For in vitro investigation of ibuprofen activity, measurement of colony diameter, and dry weight were employed against 4 isolated strains of dermatophytes from 46 patients (30-43 years) suffering from dermatophytoses at Morgan Hospital, Hilla City, Iraq in June 2008. For the in vivo evaluation of ibuprofen, rabbits as the main subjects, were infected with dermatophytes and treated with prepared ibuprofen cream (15mg/gm). In vitro application of ibuprofen showed cidal activity on 4 strains of dermatophytes at minimum inhibitory concentrations of 200 ug/ml. The infected rabbits were successfully cured of dermatophytoses after treatment with ibuprofen cream. Based on in vitro and in vivo application, Ibuprofen can be used as a short-term cure for dermatophytoses. (author)

  9. Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives

    Directory of Open Access Journals (Sweden)

    A Nokhodchi

    2010-06-01

    Full Text Available "n  "n Background and the purpose of the study: The success of any direct-tableting procedure is strongly affected by the quality of the crystals used in the process. Ibuprofen is a poorly compactible drug with a high tendency for capping. In order to use ibuprofen in direct compression formulations, physico-mechanical properties of ibuprofen should be improved considerably. The aim of the present investigation was to employ crystallization techniques in order to improve the physico-mechanical properties of ibuprofen for direct compression. "nMethods:The experimental methods involved the preparation of ibuprofen crystals by solvent change technique. Ibuprofen was dissolved in ethanol and crystallized out with water in the absence or presence of various hydrophilic additives (PEG 6000, 8000, Brij 98P and polyvinyl alcohol 22000, PVA 22000 with different concentrations. The physico-mechanical properties of the ibuprofen crystals were studied in terms of flow, density, tensile strength and dissolution behaviour. Morphology of ibuprofen crystals was studied by scanning electron microscopic (SEM. Solid state of the recrystallized particles was also investigated using differential scanning calorimeter (DSC and FT-IR. "nResults:Ibuprofen samples crystallized in the presence of PEG 6000 and 8000 and PVA showed remarkable increase in the tensile strengths of the directly compressed tablets, while some other additives, i.e. Brij 98P did not produce improved ibuprofen crystals. Ibuprofen powders made from particles obtained in the presence of PVA and Brij 98P showed similar dissolution profiles to the commercial ibuprofen particles. DSC and FT-IR results ruled out any significant interaction between ibuprofen and additives except for the samples crystallized in the presence of PEG 8000. Conclusion:The crystal habit of ibuprofen can be altered successfully by the crystallization technique which was developed in this study. The crystals developed in the

  10. Development and evaluation of ibuprofen transdermal gel formulations

    African Journals Online (AJOL)

    A commercial ibuprofen gel product (Ibutop®) was used as a reference. Results: The formulations containing 5 % of either menthol or glycerol as permeation enhancers gave drug release patterns comparable to that of the reference product. Propanol increased the apparent viscosity of the test gels to the same extent as that ...

  11. Silver-functionalized carbon nanofiber composite electrodes for ibuprofen detection

    NARCIS (Netherlands)

    Manea, F.; Motoc, S.; Pop, A.; Remes, A.; Schoonman, J.

    2012-01-01

    The aim of this study is to prepare and characterize two types of silver-functionalized carbon nanofiber (CNF) composite electrodes, i.e., silver-decorated CNF-epoxy and silver-modified natural zeolite-CNF-epoxy composite electrodes suitable for ibuprofen detection in aqueous solution. Ag carbon

  12. Premarketing surveillance of ibuprofen suppositories in febrile children.

    Science.gov (United States)

    Hadas, Dan; Youngster, Ilan; Cohen, Avner; Leibovitch, Eugene; Shavit, Itai; Erez, Ilan; Uziel, Yosef; Berkovitch, Matitiahu

    2011-03-01

    In many countries, ibuprofen is available only in oral formulations. The authors aimed to investigate parental satisfaction and possible adverse reactions among children receiving newly marketed ibuprofen suppositories, prior to their arrival at the pharmaceutical points of distribution. Children needing antipyretic medication were recruited from 11 pediatric wards and clinics in Israel. Each patient received ibuprofen suppositories (5-10 mg/kg/dose) after completing a data collection form. After 3 to 7 days of treatment, information regarding parent satisfaction, possible adverse reactions, and concomitant use of drugs was obtained. Overall, 490 children completed the study. Parents' satisfaction was high (4.5 ± 0.47 on a scale of 1-5), and 92.2% reported that they would use the medication in the future. Adverse reactions were reported in 8 patients (1.63%, 95% confidence interval = 1.77-3.25), the most common being diarrhea. Rectal administration of ibuprofen suppositories is well tolerated and overall satisfaction and the repeated expected use were high.

  13. Jejunal perforation by swallowed ibuprofen caplet | Njoku | Nigerian ...

    African Journals Online (AJOL)

    We present a case of jejunal perforation caused by an unusual foreign body, an ibuprofen caplet in its blister packing believed to be the first of its kind, perforation of the intestine caused by an ingested medication. The patient eventually developed an enterocutaneous fistula through the weak wall of a preexisting incisional ...

  14. Synthesis of Ibuprofen in the Introductory Organic Laboratory

    Science.gov (United States)

    Kjonaas, Richard A.; Williams, Peggy E.; Counce, David A.; Crawley, Lindsey R.

    2011-01-01

    A method for the synthesis of ibuprofen in introductory organic chemistry laboratory courses is reported. This experiment requires two 3-h lab sessions. All of the reactions and techniques are a standard part of any introductory organic chemistry course. In the first lab session, students reduce p-isobutylacetophenone to an alcohol and then…

  15. Controlled release of ibuprofen by meso–macroporous silica

    Energy Technology Data Exchange (ETDEWEB)

    Santamaría, E., E-mail: esthersantamaria@ub.edu; Maestro, A.; Porras, M.; Gutiérrez, J.M.; González, C.

    2014-02-15

    Structured meso–macroporous silica was successfully synthesized from an O/W emulsion using decane as a dispersed phase. Sodium silicate solution, which acts as a silica source and a poly(ethylene oxide)–poly(propylene oxide)–poly(ethylene oxide) (EO{sub 19}PO{sub 39}EO{sub 19}) denoted as P84 was used in order to stabilize the emulsion and as a mesopore template. The materials obtained were characterized through transmission electron microscopy (TEM), scanning electron microscopy (SEM), small-angle X-ray diffraction scattering (SAXS) and nitrogen adsorption–desorption isotherms. Ibuprofen (IBU) was selected as the model drug and loaded into ordered meso–macroporous materials. The effect of the materials’ properties on IBU drug loading and release was studied. The results showed that the loading of IBU increases as the macropore presence in the material is increased. The IBU adsorption process followed the Langmuir adsorption isotherm. A two-step release process, consisting of an initial fast release and then a slower release was observed. Macropores enhanced the adsorption capacity of the material; this was probably due to the fact that they allowed the drug to access internal pores. When only mesopores were present, ibuprofen was probably adsorbed on the mesopores close to the surface. Moreover, the more macropore present in the material, the slower the release behaviour observed, as the ibuprofen adsorbed in the internal pores had to diffuse along the macropore channels up to the surface of the material. The material obtained from a highly concentrated emulsion was functionalized with amino groups using two methods, the post-grafting mechanism and the co-condensation mechanism. Both routes improve IBU adsorption in the material and show good behaviour as a controlled drug delivery system. - Graphical abstract: Ibuprofen release profiles for the materials obtained from samples P84{sub m}eso (black diamonds), P84{sub 2}0% (white squares), P84{sub 5

  16. Pharmacokinetics of Cromolyn and Ibuprofen in Healthy Elderly Volunteers.

    Science.gov (United States)

    Brazier, David; Perry, Robert; Keane, Jim; Barrett, Katie; Elmaleh, David R

    2017-11-01

    BACKGROUND AND OBJECTIVES: The combination of cromolyn and ibuprofen is being investigated as a treatment for early Alzheimer's disease (AD). This study investigated the pharmacokinetics, safety, and tolerability of cromolyn and ibuprofen co-administration in healthy elderly adult volunteers. In this open-labeled study, 26 subjects, aged 55-75 years, received co-administration of inhaled cromolyn (single dose 17.1 mg; double dose 34.2 mg total) and oral ibuprofen (single dose 10 mg; double dose 20 mg total). Blood sampling was performed for 6 h after co-administration in all subjects; cerebrospinal fluid (CSF) was collected in three to four subjects per cohort for 4 h following co-administration. Safety parameters, including adverse events (AEs), were monitored throughout the study. For cromolyn, the mean (±SD) maximum observed concentration (C max ) in plasma was 46.69 ± 32.97 and 96.75 ± 46.22 ng/ml after single- and double-dose inhalation, respectively [time to C max (t max ) ~22 min for each; terminal elimination half-life (t ½ ) ~1.8 h for each]. For ibuprofen, the plasma C max was 1090.98 ± 474.64 ng/ml and 2062.96 ± 655.13 ng/ml after single- and double-dose oral administration, respectively (t max ~1.6-1.8 h; t ½ ~1.9 h for each). For cromolyn, the CSF C max was 0.24 ± 0.08 ng/ml at 3.72 ± 0.70 h after single-dose administration and 0.34 ± 0.17 ng/ml at 3.45 ± 0.95 h after double-dose administration, and for ibuprofen, the CSF C max was 3.94 ± 1.29 ng/ml at 2.55 ± 0.96 h after single-dose administration and 8.93 ± 3.29 ng/ml at 3.15 ± 1.05 h after double-dose administration. Three (12%) subjects reported mild or moderate AEs which were unlikely to be related to study drug. The combination of cromolyn and ibuprofen was safe and well tolerated. The concentrations of cromolyn and ibuprofen observed in the CSF are considered sufficient to titrate the estimated daily amyloid production and the associated inflammatory response

  17. Controlled release of ibuprofen by meso–macroporous silica

    International Nuclear Information System (INIS)

    Santamaría, E.; Maestro, A.; Porras, M.; Gutiérrez, J.M.; González, C.

    2014-01-01

    Structured meso–macroporous silica was successfully synthesized from an O/W emulsion using decane as a dispersed phase. Sodium silicate solution, which acts as a silica source and a poly(ethylene oxide)–poly(propylene oxide)–poly(ethylene oxide) (EO 19 PO 39 EO 19 ) denoted as P84 was used in order to stabilize the emulsion and as a mesopore template. The materials obtained were characterized through transmission electron microscopy (TEM), scanning electron microscopy (SEM), small-angle X-ray diffraction scattering (SAXS) and nitrogen adsorption–desorption isotherms. Ibuprofen (IBU) was selected as the model drug and loaded into ordered meso–macroporous materials. The effect of the materials’ properties on IBU drug loading and release was studied. The results showed that the loading of IBU increases as the macropore presence in the material is increased. The IBU adsorption process followed the Langmuir adsorption isotherm. A two-step release process, consisting of an initial fast release and then a slower release was observed. Macropores enhanced the adsorption capacity of the material; this was probably due to the fact that they allowed the drug to access internal pores. When only mesopores were present, ibuprofen was probably adsorbed on the mesopores close to the surface. Moreover, the more macropore present in the material, the slower the release behaviour observed, as the ibuprofen adsorbed in the internal pores had to diffuse along the macropore channels up to the surface of the material. The material obtained from a highly concentrated emulsion was functionalized with amino groups using two methods, the post-grafting mechanism and the co-condensation mechanism. Both routes improve IBU adsorption in the material and show good behaviour as a controlled drug delivery system. - Graphical abstract: Ibuprofen release profiles for the materials obtained from samples P84 m eso (black diamonds), P84 2 0% (white squares), P84 5 0% (black triangles), P84 7

  18. Thermodynamic study of ibuprofen by adiabatic calorimetry and thermal analysis

    International Nuclear Information System (INIS)

    Xu Fen; Sun Lixian; Tan Zhicheng; Liang Jianguo; Li Ruilian

    2004-01-01

    Molar heat capacities of ibuprofen were precisely measured with a small sample precision automated adiabatic calorimeter over the temperature range from 80 to 400 K. The polynomial functions of C p,m (J K -1 mol -1 ) versus T were established on the heat capacity measurements by means of the least fitting square method. The functions are as follows: for solid ibuprofen, at the temperature range of 79.105 K≤T≤333.297 K, C p,m =144.27+77.046X+3.5171X 2 +10.925X 3 +11.224X 4 , where X=(T-206.201)/127.096; for liquid ibuprofen, at the temperature range of 353.406 K≤T≤378.785 K, C p,m =325.79+8.9696X-1.6073X 2 -1.5145X 3 , where X=(T-366.095)/12.690. A fusion transition at T=348.02 K was found from the C p -T curve. The molar enthalpy and entropy of the fusion transition were determined to be 26.65 kJ mol -1 and 76.58 J mol -1 K -1 , respectively. The thermodynamic functions on the base of the reference temperature of 298.15 K, (H T -H 298.15 ) and (S T -S 298.15 ), were derived. Thermal characteristic of ibuprofen was studied by thermo-gravimetric analysis (TG-DTG) and differential scanning calorimeter (DSC). The temperature of fusion, the molar enthalpy and entropy of fusion obtained by DSC were well consistent with those obtained by adiabatic calorimeter. The evaporation process of ibuprofen was investigated further by TG and DTG, and the activation energy of the evaporation process was determined to be 80.3±1.4 kJ mol -1

  19. Dissolution of ibuprofen enantiomers from coprecipitates and suspensions containing chiral excipients.

    Science.gov (United States)

    Janjikhel, R K; Adeyeye, C M

    1999-01-01

    The purpose of this research was to evaluate the stereospecific interaction of ibuprofen with chiral excipients such as hydroxypropyl-beta-cyclodextrin (HPCD), tartaric acid, sucrose, hydroxypropylmethylcellulose (HPMC), methylcellulose (MC), and a nonchiral excipient, citric acid. Coprecipitates of ibuprofen were prepared in molar ratios ranging between 1:0.5 and 1:10 by a solvent evaporation method and characterized using x-ray diffraction, Fourier-transform infrared (FTIR) spectroscopy, and dissolution testing. Phase solubility studies of ibuprofen were carried out by adding excess amount of ibuprofen to aqueous excipient solutions of varying concentrations. Interaction was studied in suspensions of ibuprofen with HPMC, MC, and sucrose stored at room temperature and 60 degrees C for 12 weeks. Solubility of ibuprofen in HPCD solutions increased 10-fold, whereas solubility decreased in the tartaric and citric acid solutions, a result of decreased pH with increased amount of the acids in which ibuprofen (pKa 4.8) is less soluble. Phase solubility diagrams of ibuprofen in aqueous HPCD, citric acid, and tartaric acid solutions showed no stereospecific differences in solubility of the two enantiomers. X-ray diffraction studies showed that ibuprofen exists in a crystalline form at low ibuprofen-to-excipient ratios, whereas at the higher ratios, it exists in an amorphous form. FTIR spectroscopy for HPCD coprecipitates showed a shift of the carbonyl stretching band of ibuprofen to a higher wavelength with a markedly decreased intensity, probably because of a breakdown in the intermolecular hydrogen bonding with ibuprofen and restriction of the drug molecule in the HPCD cavity, respectively. Dissolution profiles of the coprecipitates demonstrated higher dissolution rates than those of pure ibuprofen. The presence of chiral excipients did not appear to cause stereoselective release of the drug from the coprecipitates and the suspensions.

  20. Thermodynamic study of complex formation of β-cyclodextrin with ibuprofen by conductometric method and determination of ibuprofen in pharmaceutical drugs

    Directory of Open Access Journals (Sweden)

    Somayeh Heydari

    2017-02-01

    Based on the obtained results, a conductometric method for the determination of ibuprofen in the presence of β-CD at 25 °C was developed in the range of 10−3–10−5 mol dm−1. The method was satisfactorily applied to the quantification of ibuprofen in pharmaceutical preparations.

  1. Acetaminophen versus Ibuprofen in Young Children with Mild Persistent Asthma.

    Science.gov (United States)

    Sheehan, William J; Mauger, David T; Paul, Ian M; Moy, James N; Boehmer, Susan J; Szefler, Stanley J; Fitzpatrick, Anne M; Jackson, Daniel J; Bacharier, Leonard B; Cabana, Michael D; Covar, Ronina; Holguin, Fernando; Lemanske, Robert F; Martinez, Fernando D; Pongracic, Jacqueline A; Beigelman, Avraham; Baxi, Sachin N; Benson, Mindy; Blake, Kathryn; Chmiel, James F; Daines, Cori L; Daines, Michael O; Gaffin, Jonathan M; Gentile, Deborah A; Gower, W Adam; Israel, Elliot; Kumar, Harsha V; Lang, Jason E; Lazarus, Stephen C; Lima, John J; Ly, Ngoc; Marbin, Jyothi; Morgan, Wayne J; Myers, Ross E; Olin, J Tod; Peters, Stephen P; Raissy, Hengameh H; Robison, Rachel G; Ross, Kristie; Sorkness, Christine A; Thyne, Shannon M; Wechsler, Michael E; Phipatanakul, Wanda

    2016-08-18

    Studies have suggested an association between frequent acetaminophen use and asthma-related complications among children, leading some physicians to recommend that acetaminophen be avoided in children with asthma; however, appropriately designed trials evaluating this association in children are lacking. In a multicenter, prospective, randomized, double-blind, parallel-group trial, we enrolled 300 children (age range, 12 to 59 months) with mild persistent asthma and assigned them to receive either acetaminophen or ibuprofen when needed for the alleviation of fever or pain over the course of 48 weeks. The primary outcome was the number of asthma exacerbations that led to treatment with systemic glucocorticoids. Children in both groups received standardized asthma-controller therapies that were used in a simultaneous, factorially linked trial. Participants received a median of 5.5 doses (interquartile range, 1.0 to 15.0) of trial medication; there was no significant between-group difference in the median number of doses received (P=0.47). The number of asthma exacerbations did not differ significantly between the two groups, with a mean of 0.81 per participant with acetaminophen and 0.87 per participant with ibuprofen over 46 weeks of follow-up (relative rate of asthma exacerbations in the acetaminophen group vs. the ibuprofen group, 0.94; 95% confidence interval, 0.69 to 1.28; P=0.67). In the acetaminophen group, 49% of participants had at least one asthma exacerbation and 21% had at least two, as compared with 47% and 24%, respectively, in the ibuprofen group. Similarly, no significant differences were detected between acetaminophen and ibuprofen with respect to the percentage of asthma-control days (85.8% and 86.8%, respectively; P=0.50), use of an albuterol rescue inhaler (2.8 and 3.0 inhalations per week, respectively; P=0.69), unscheduled health care utilization for asthma (0.75 and 0.76 episodes per participant, respectively; P=0.94), or adverse events. Among

  2. [Plasma ibuprofen enantiomers and their pharmacokinetics in Beagle dogs determined by HPLC].

    Science.gov (United States)

    Wang, Hong-yan; Kong, Ai-ying; Yang, Bo; Yan, Liang-ping; Di, Xin

    2015-12-01

    A chiral high-performance liquid chromatography method was developed for the simultaneous determination of ibuprofen enantiomers in dog plasma. It was used to study the pharmacokinetics in the Beagle dog after intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen. Ketoprofen was chosen as the internal standard. After a simple precipitation using methanol as the precipitating solvent, both analytes and IS were separated on a Kromasil 100-5CHI-TBB chiral column (250 mm x4.6 mm, 5 μm) with isocratic elution using acetonitrile - 20 mmol x L(-1) phosphate buffer (pH 3.0, containing 5% methanol) (6 : 4) as the mobile phase. The detection wavelength was 220 nm. Liner calibration curves for both of the ibuprofen enantiomers were over the concentration range from 0.5 to 50 μg x mL(-1) with a lower limit of quantification of 0.5 μg x mL(-1), the accuracies were all in standard ranges. The intra- and inter- assay precisions were all below 7%. The recovery rate was 93.1% to 100.4%. The experiments proved that the method was simple, rapid and sensitive. It can be used in the quantitative determination of ibuprofen enantiomers in dog plasma. The method was used to determine the concentration of ibuprofen enantiomers in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen (9 mg x kg(-1)) and the pharmacokinetics parameters were calculated based on the concentration-time curves. The C(max) of S-ibuprofen in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen were 30.8 ± 4.7, 46.1 ± 5.9 and 20.0 ± 2.6 μg x mL(-1), respectively. In terms of the exposure of active ingredient, it revealed a significant difference between the administration of S-ibuprofen and the other two groups. The systematical R- to S- chiral inversion was discussed. Comparing the pharmacokinetic parameters at different doses, chiral inversion were 70.1% ± 36.6% and 76

  3. {beta}-TCP porous pellets as an orthopaedic drug delivery system: ibuprofen/carrier physicochemical interactions

    Energy Technology Data Exchange (ETDEWEB)

    Baradari, Hiba; Damia, Chantal; Dutreih-Colas, Maggy; Champion, Eric; Chulia, Dominique; Viana, Marylene, E-mail: hiva.baradari@etu.unilim.fr [SPCTS-Centre Europeen de la Ceramique, 12 Rue Atlantis, 87068 Limoges CEDEX (France)

    2011-10-15

    Calcium phosphate bone substitute materials can be loaded with active substances for in situ, targeted drug administration. In this study, porous {beta}-TCP pellets were investigated as an anti-inflammatory drug carrier. Porous {beta}-TCP pellets were impregnated with an ethanolic solution of ibuprofen. The effects of contact time and concentration of ibuprofen solution on drug adsorption were studied. The ibuprofen adsorption equilibrium time was found to be one hour. The adsorption isotherms fitted to the Freundlich model, suggesting that the interaction between ibuprofen and {beta}-TCP is weak. The physicochemical characterizations of loaded pellets confirmed that the reversible physisorption of ibuprofen on {beta}-TCP pellets is due to Van der Waals forces, and this property was associated with the 100% ibuprofen release.

  4. β-TCP porous pellets as an orthopaedic drug delivery system: ibuprofen/carrier physicochemical interactions

    International Nuclear Information System (INIS)

    Baradari, Hiba; Damia, Chantal; Dutreih-Colas, Maggy; Champion, Eric; Chulia, Dominique; Viana, Marylene

    2011-01-01

    Calcium phosphate bone substitute materials can be loaded with active substances for in situ, targeted drug administration. In this study, porous β-TCP pellets were investigated as an anti-inflammatory drug carrier. Porous β-TCP pellets were impregnated with an ethanolic solution of ibuprofen. The effects of contact time and concentration of ibuprofen solution on drug adsorption were studied. The ibuprofen adsorption equilibrium time was found to be one hour. The adsorption isotherms fitted to the Freundlich model, suggesting that the interaction between ibuprofen and β-TCP is weak. The physicochemical characterizations of loaded pellets confirmed that the reversible physisorption of ibuprofen on β-TCP pellets is due to Van der Waals forces, and this property was associated with the 100% ibuprofen release.

  5. 50 CFR 648.164 - Possession restrictions.

    Science.gov (United States)

    2010-10-01

    ... Atlantic Bluefish Fishery § 648.164 Possession restrictions. (a) No person shall possess more than 15 bluefish in, or harvested from, the EEZ unless that person is the owner or operator of a fishing vessel issued a bluefish commercial permit or is issued a bluefish dealer permit. Persons aboard a vessel that...

  6. The Evidence Base on the Efficacy and Safety of Ibuprofen in Pediatrics

    Directory of Open Access Journals (Sweden)

    Yu.V. Marushko

    2013-10-01

    Full Text Available The article deals with an analysis of the world literature of recent years, the aim of which was to study the efficacy and safety of ibuprofen use as first-line antipyretic in pediatric practice. Special attention was paid to researches on the study the pharmacokinetics, efficacy and safety of ibuprofen in fever in children of all ages, as well as the use of different forms of ibuprofen (suspension, suppositories.

  7. Pilot monitoring study of ibuprofen in surface waters of north of Portugal

    OpenAIRE

    Paíga, Paula; Santos, Lúcia; Amorim, Célia G.; Araújo, Alberto N.; Montenegro, M. Conceição B. S. M.; Pena, Angelina; Delerue-Matos, Cristina

    2013-01-01

    Ibuprofen is amongst the most worldwide consumed pharmaceuticals. The present work presents the first data in the occurrence of ibuprofen in Portuguese surface waters, focusing in the north area of the country, which is one of the most densely populated areas of Portugal. Analysis of ibuprofen is based on pre-concentration of the analyte with solid phase extraction and subsequent determination with liquid chromatography coupled to fluorescence detection. A total of 42 ...

  8. Comparative study of anti-inflammatory, ulcerogenic and cytotoxic activities of racemate and S-ibuprofen

    Directory of Open Access Journals (Sweden)

    Flavio Henrique Nuevo Benez

    2013-08-01

    Full Text Available Ibuprofen is widely commercialized in racemic form. Although metabolic chiral inversion occurs through the conversion of R(--ibuprofen to S(+-ibuprofen and the latter enantiomer is considered the active form, clinical trials involving the administration of a racemate to S-enantiomer dosage ratio of 1:0.5 have demonstrated that S(+-ibuprofen is as efficacious as the racemic formulation. Moreover, the R(--enantiomer has been implicated in adverse gastrointestinal effects found with the racemic form, but the mechanisms involved in this process are not yet fully understood. The aim of the present study was to evaluate the anti-inflammatory activity of a racemate to S(+-ibuprofen dosage ratio of 1:0.5 using the carrageenan air pouch model of inflammation and determine both ulcerogenic activity and the chiral conversion rate in rats. An in vitro study of the cytotoxicity of racemate and S(+-ibuprofen in gastric cells was also performed. Although the plasma level of S(+-ibuprofen was raised after racemate administration, no significant difference was found in anti-inflammatory activity, as assessed by exudate formation, PGE2 production and leukocyte migration to the air pouches. Fewer gastric lesions were found after S(+-ibuprofen administration, despite the low gastric PGE2 content. In the in vitro study, the racemic compound proved more cytotoxic than S(+-ibuprofen. The present findings suggest that the S-enantiomer of ibuprofen could be considered a therapeutic alternative to minimize gastrointestinal side effects, since the chiral inversion of R(--ibuprofen to S(+-ibuprofen did not result in an improved anti-inflammatory response.

  9. Formulation and delivery strategies of ibuprofen: challenges and opportunities.

    Science.gov (United States)

    Irvine, Jake; Afrose, Afrina; Islam, Nazrul

    2018-02-01

    Ibuprofen, a non-steroidal anti-inflammatory drug (NSAID), is mostly administered orally and topically to relieve acute pain and fever. Due to its mode of action this drug may be useful in the treatment regimens of other, more chronic conditions, like cystic fibrosis. This drug is poorly soluble in aqueous media and thus the rate of dissolution from the currently available solid dosage forms is limited. This leads to poor bioavailability at high doses after oral administration, thereby increasing the risk of unwanted adverse effects. The poor solubility is a problem for developing injectable solution dosage forms. Because of its poor skin permeability, it is difficult to obtain an effective therapeutic concentration from topical preparations. This review aims to give a brief insight into the status of ibuprofen dosage forms and their limitations, particle/crystallization technologies for improving formulation strategies as well as suggesting its incorporation into the pulmonary drug delivery systems for achieving better therapeutic action at low dose.

  10. Optimization of Process Variables for Grinding of Ibuprofen using Response Surface Methodology

    Energy Technology Data Exchange (ETDEWEB)

    Sim, Chol-Ho [Sangji University, Wonju (Korea, Republic of)

    2013-12-15

    Ibuprofen, non-steroidal anti-inflammatory drugs; NSAIDs, is a highly crystalline substance with the pharmaceutical properties of poor solubility and low bioavailability. The size reduction of ibuprofen is needed to improve the solubility. The objective of this study is to optimize the grinding condition of ibuprofen. Grinding of ibuprofen was carried out using a planetary mill. Grinding parameters were optimized using Box-Behnken experimental design method. The physical characteristics of ground ibuprofen were investigated for the particle size by particle size analyzer, for the crystal size by X-ray diffraction (XRD), and for the tensile strength by tensile/compression tester. The optimum conditions for the milling of ibuprofen were 290 rpm of the revolution number of mill, 24.6 g of the weight of sample, and 10minutes of grinding time. The measured value of the particle size of ground ibuprofen at these optimum conditions was 13.5 µm. The results showed that the crystal size of ibuprofen was reduced by the planetary milling process. In case the relative density of the tablets formulated of ground ibuprofen was range of 0.85-0.90, the tensile strength of them was range of 12-14 Kg{sub f}/cm{sup 2}.

  11. Optimization of Process Variables for Grinding of Ibuprofen using Response Surface Methodology

    International Nuclear Information System (INIS)

    Sim, Chol-Ho

    2013-01-01

    Ibuprofen, non-steroidal anti-inflammatory drugs; NSAIDs, is a highly crystalline substance with the pharmaceutical properties of poor solubility and low bioavailability. The size reduction of ibuprofen is needed to improve the solubility. The objective of this study is to optimize the grinding condition of ibuprofen. Grinding of ibuprofen was carried out using a planetary mill. Grinding parameters were optimized using Box-Behnken experimental design method. The physical characteristics of ground ibuprofen were investigated for the particle size by particle size analyzer, for the crystal size by X-ray diffraction (XRD), and for the tensile strength by tensile/compression tester. The optimum conditions for the milling of ibuprofen were 290 rpm of the revolution number of mill, 24.6 g of the weight of sample, and 10minutes of grinding time. The measured value of the particle size of ground ibuprofen at these optimum conditions was 13.5 µm. The results showed that the crystal size of ibuprofen was reduced by the planetary milling process. In case the relative density of the tablets formulated of ground ibuprofen was range of 0.85-0.90, the tensile strength of them was range of 12-14 Kg f /cm 2

  12. Does ibuprofen treatment in patent ductus arteriosus alter oxygen free radicals in premature infants?

    Science.gov (United States)

    Akar, Melek; Yildirim, Tulin G; Sandal, Gonca; Bozdag, Senol; Erdeve, Omer; Altug, Nahide; Uras, Nurdan; Oguz, Serife S; Dilmen, Ugur

    2017-04-01

    Introduction Ibuprofen is used widely to close patent ductus arteriosus in preterm infants. The anti-inflammatory activity of ibuprofen may also be partly due to its ability to scavenge reactive oxygen species and reactive nitrogen species. We evaluated the interaction between oxidative status and the medical treatment of patent ductus arteriosus with two forms of ibuprofen. Materials and methods This study enrolled newborns of gestational age ⩽32 weeks, birth weight ⩽1500 g, and postnatal age 48-96 hours, who received either intravenous or oral ibuprofen to treat patent ductus arteriosus. Venous blood was sampled before ibuprofen treatment from each patient to determine antioxidant and oxidant concentrations. Secondary samples were collected 24 hours after the end of the treatment. Total oxidant status and total antioxidant capacity were measured using Erel's method. This prospective randomised study enrolled 102 preterm infants with patent ductus arteriosus. The patent ductus arteriosus closure rate was significantly higher in the oral ibuprofen group (84.6 versus 62%) after the first course of treatment (p=0.011). No significant difference was found between the pre- and post-treatment total oxidant status and total antioxidant capacity in the groups. Discussion Ibuprofen treatment does not change the total oxidant status or total antioxidant capacity. We believe that the effect of ibuprofen treatment in inducing ischaemia overcomes the scavenging effect of ibuprofen.

  13. Ibuprofen versus steroids: risk and benefit, efficacy and safety

    Directory of Open Access Journals (Sweden)

    M. Giovannini

    2013-10-01

    Full Text Available In the last few years we have observed an upward trend in the employment of ibuprofen as anti-inflammatory and antipyretic therapy. Therefore the pediatrician has often a precious option in the anti-inflammatory and antipyretic treatment in children instead of using steroids and paracetamol. In clinical practice ibuprofen can be used in the treatment of headache, toothache, otalgy, dysmenorrhea, neuralgia, arthralgia, myalgia, abdominal pain and fever: it is the first choice for these common diseases. However, the use of steroids is a routine, even if non-corticosteroid anti-inflammatory molecules could be useful. Certainly steroids are powerful anti-inflammatory, indicated for the treatment of chronic inflammatory disorders and in acute respiratory and allergic diseases. Beside, thanks to their chemical and pharmacological profile, they also provide patients with an antipyretic effect. However, the use of steroids must be reserved to cases in which other classical antipyretics such as non-steroidal anti-inflammatory drugs are not effective. The possible side effects and risks associated with stepping down steroids must be considered. Although “steroids-phobia” should be discouraged, steroids are to be reserved only as the first indication. In all other cases the pediatrician can use ibuprofen, whose efficacy and safety are widely demonstrated by now.

  14. Thermodynamic study of ibuprofen by adiabatic calorimetry and thermal analysis

    Energy Technology Data Exchange (ETDEWEB)

    Xu Fen; Sun Lixian; Tan Zhicheng; Liang Jianguo; Li Ruilian

    2004-03-23

    Molar heat capacities of ibuprofen were precisely measured with a small sample precision automated adiabatic calorimeter over the temperature range from 80 to 400 K. The polynomial functions of C{sub p,m} (J K{sup -1} mol{sup -1}) versus T were established on the heat capacity measurements by means of the least fitting square method. The functions are as follows: for solid ibuprofen, at the temperature range of 79.105 K{<=}T{<=}333.297 K, C{sub p,m}=144.27+77.046X+3.5171X{sup 2}+10.925X{sup 3}+11.224X{sup 4}, where X=(T-206.201)/127.096; for liquid ibuprofen, at the temperature range of 353.406 K{<=}T{<=}378.785 K, C{sub p,m}=325.79+8.9696X-1.6073X{sup 2}-1.5145X{sup 3}, where X=(T-366.095)/12.690. A fusion transition at T=348.02 K was found from the C{sub p}-T curve. The molar enthalpy and entropy of the fusion transition were determined to be 26.65 kJ mol{sup -1} and 76.58 J mol{sup -1} K{sup -1}, respectively. The thermodynamic functions on the base of the reference temperature of 298.15 K, (H{sub T}-H{sub 298.15}) and (S{sub T}-S{sub 298.15}), were derived. Thermal characteristic of ibuprofen was studied by thermo-gravimetric analysis (TG-DTG) and differential scanning calorimeter (DSC). The temperature of fusion, the molar enthalpy and entropy of fusion obtained by DSC were well consistent with those obtained by adiabatic calorimeter. The evaporation process of ibuprofen was investigated further by TG and DTG, and the activation energy of the evaporation process was determined to be 80.3{+-}1.4 kJ mol{sup -1}.

  15. POSSESSION, REVIEW FROM CULTURAL AND PSYCHIATRY

    Directory of Open Access Journals (Sweden)

    Ni Ketut Sri Diniari

    2013-03-01

    Full Text Available Possession is a culture related syndrome, commonly found in Indonesia including Bali. We can see this event in religion and cultural ceremony and at other times at school, home, and in society. This syndrome consist of temporary loss of self identification and environment awareness; in several events a person acts as if he/she was controlled by other being, magic force, spirit or ‘other forces’. There are still several different opinions about trance-possession, whether it is related to certain culture or is a part of mental disorder. DSM-IV-TR and PPDGJ-III defined trance-possession as mental disorder (dissociative for involuntary possession, if it is not a common activity, and if it is not a part of religion or cultural event. (MEDICINA 2012;43:37-40.

  16. Subself theory and reincarnation/possession.

    Science.gov (United States)

    Lester, David

    2004-12-01

    A subself model of the mind is used to account for multiple personality, possession, the spirit controls of mediums, reincarnation, and the auditory hallucinations of schizophrenics, with suggestions for empirical research.

  17. Encapsulation of Ibuprofen in CD-MOF and Related Bioavailability Studies.

    Science.gov (United States)

    Hartlieb, Karel J; Ferris, Daniel P; Holcroft, James M; Kandela, Irawati; Stern, Charlotte L; Nassar, Majed S; Botros, Youssry Y; Stoddart, J Fraser

    2017-05-01

    Although ibuprofen is one of the most widely used nonsteroidal anti-inflammatory drugs (NSAIDs), it exhibits poor solubility in aqueous and physiological environments as a free acid. In order to improve its oral bioavailability and rate of uptake, extensive research into the development of new formulations of ibuprofen has been undertaken, including the use of excipients as well as ibuprofen salts, such as ibuprofen lysinate and ibuprofen, sodium salt. The ultimate goals of these studies are to reduce the time required for maximum uptake of ibuprofen, as this period of time is directly proportional to the rate of onset of analgesic/anti-inflammatory effects, and to increase the half-life of the drug within the body; that is, the duration of action of the effects of the drug. Herein, we present a pharmaceutical cocrystal of ibuprofen and the biocompatible metal-organic framework called CD-MOF. This metal-organic framework (MOF) is based upon γ-cyclodextrin (γ-CD) tori that are coordinated to alkali metal cations (e.g., K + ions) on both their primary and secondary faces in an alternating manner to form a porous framework built up from (γ-CD) 6 cubes. We show that ibuprofen can be incorporated within CD-MOF-1 either by (i) a crystallization process using the potassium salt of ibuprofen as the alkali cation source for production of the MOF or by (ii) absorption and deprotonation of the free-acid, leading to an uptake of 23-26 wt % of ibuprofen within the CD-MOF. In vitro viability studies revealed that the CD-MOF is inherently not affecting the viability of the cells with no IC 50 value determined up to a concentration of 100 μM. Bioavailability investigations were conducted on mice, and the ibuprofen/CD-MOF pharmaceutical cocrystal was compared to control samples of the potassium salt of ibuprofen in the presence and absence of γ-CD. From these animal studies, we observed that the ibuprofen/CD-MOF-1 cocrystal exhibits the same rapid uptake of ibuprofen as the

  18. The Impact of Banning Juvenile Gun Possession.

    OpenAIRE

    Marvell, Thomas B

    2001-01-01

    A 1994 federal law bans possession of handguns by persons under 18 years of age. Also in 1994, 11 states passed their own juvenile gun possession bans. Eighteen states had previously passed bans, 15 of them between 1975 and 1993. These laws were intended to reduce homicides, but arguments can be made that they have no effect on or that they even increase the homicide rate. This paper estimates the laws' impacts on various crime measures, primarily juvenile gun homicide victimizations and suic...

  19. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model.

    Science.gov (United States)

    Rooney, Sarah Ilkhanipour; Baskin, Rachel; Torino, Daniel J; Vafa, Rameen P; Khandekar, Pooja S; Kuntz, Andrew F; Soslowsky, Louis J

    2016-09-01

    Previous studies have shown that ibuprofen is detrimental to tissue healing after acute injury; however, the effects of ibuprofen when combined with noninjurious exercise are debated. Administration of ibuprofen to rats undergoing a noninjurious treadmill exercise protocol will abolish the beneficial adaptations found with exercise but will have no effect on sedentary muscle and tendon properties. Controlled laboratory study. A total of 167 male Sprague-Dawley rats were divided into exercise or cage activity (sedentary) groups and acute (a single bout of exercise followed by 24 hours of rest) and chronic (2 or 8 weeks of repeated exercise) response times. Half of the rats were administered ibuprofen to investigate the effects of this drug over time when combined with different activity levels (exercise and sedentary). Supraspinatus tendons were used for mechanical testing and histologic assessment (organization, cell shape, cellularity), and supraspinatus muscles were used for morphologic (fiber cross-sectional area, centrally nucleated fibers) and fiber type analysis. Chronic intake of ibuprofen did not impair supraspinatus tendon organization or mechanical adaptations (stiffness, modulus, maximum load, maximum stress, dynamic modulus, or viscoelastic properties) to exercise. Tendon mechanical properties were not diminished and in some instances increased with ibuprofen. In contrast, total supraspinatus muscle fiber cross-sectional area decreased with ibuprofen at chronic response times, and some fiber type-specific changes were detected. Chronic administration of ibuprofen does not impair supraspinatus tendon mechanical properties in a rat model of exercise but does decrease supraspinatus muscle fiber cross-sectional area. This fundamental study adds to the growing literature on the effects of ibuprofen on musculoskeletal tissues and provides a solid foundation on which future work can build. The study findings suggest that ibuprofen does not detrimentally affect

  20. Influence of acidic beverage (Coca-Cola) on pharmacokinetics of ibuprofen in healthy rabbits.

    Science.gov (United States)

    Kondal, Amit; Garg, S K

    2003-11-01

    The study was aimed at determining the effect of Coca-Cola on the pharmacokinetics of ibuprofen in rabbits. In a cross-over study, ibuprofen was given orally in a dose of 56 mg/kg, prepared as 0.5% suspension in carboxymethyl cellulose (CMC) and blood samples (1 ml) were drawn at different time intervals from 0-12 hr. After a washout period of 7 days, Coca-Cola in a dose of (5 ml/kg) was administered along with ibuprofen (56 mg/kg) and blood samples were drawn from 0-12 hr. To these rabbits, 5 ml/kg Coca-Cola was administered once daily for another 7 days. On 8th day, Coca-Cola (5 ml/kg) along with ibuprofen (56 mg/kg), prepared as a suspension was administered and blood samples (1 ml each) were drawn at similar time intervals. Plasma was separated and assayed for ibuprofen by HPLC technique and various pharmacokinetic parameters were calculated. The Cmax and AUC0-alpha of ibuprofen were significantly increased after single and multiple doses of Coca-Cola, thereby indicating increased extent of absorption of ibuprofen. The results warrant the reduction of ibuprofen daily dosage, frequency when administered with Coca-Cola.

  1. CLINICAL EFFICACY OF IBUPROFEN IN THERAPY FOR VIRAL UPPER RESPIRATORY TRACT INFECTIONS IN INFANTS

    Directory of Open Access Journals (Sweden)

    I.O. Skugarevskaya

    2006-01-01

    Full Text Available A study of use of ibuprofen in cases of viral upper respiratory tract infections (Vuri in children of early childhood has proved its' safety and efficacy. This medical agent has not only terminate fever but also diminished some other symptoms of Vuri.Key words: ibuprofen, viral upper respiratory tract infections, children.

  2. Effects of constructed wetland design on ibuprofen removal – A mesocosm scale study

    DEFF Research Database (Denmark)

    Zhang, Liang; Lyu, Tao; Zhang, Yang

    2017-01-01

    This study aimed to investigate the effects of constructed wetland design (unsaturated, saturated and aerated saturated) and plant species (Juncus, Typha, Berula, Phragmites and Iris) on the mass removal and removal kinetics of the pharmaceutical ibuprofen. Planted systems had higher ibuprofen...

  3. Selective degradation of ibuprofen and clofibric acid in two model river biofilm systems.

    Science.gov (United States)

    Winkler, M; Lawrence, J R; Neu, T R

    2001-09-01

    A field survey indicated that the Elbe and Saale Rivers were contaminated with both clofibric acid and ibuprofen. In Elbe River water we could detect the metabolite hydroxy-ibuprofen. Analyses of the city of Saskatoon sewage effluent discharged to the South Saskatchewan river detected clofibric acid but neither ibuprofen nor any metabolite. Laboratory studies indicated that the pharmaceutical ibuprofen was readily degraded in a river biofilm reactor. Two metabolites were detected and identified as hydroxy- and carboxy-ibuprofen. Both metabolites were observed to degrade in the biofilm reactors. However, in human metabolism the metabolite carboxy-ibuprofen appears and degrades second whereas the opposite occurs in biofilm systems. In biofilms the pharmacologically inactive stereoisomere of ibuprofen is degraded predominantly. In contrast, clofibric acid was not biologically degraded during the experimental period of 21 days. Similar results were obtained using biofilms developed using waters from either the South Saskatchewan or Elbe River. In a sterile reactor no losses of ibuprofen were observed. These results suggested that abiotic losses and adsorption played only a minimal role in the fate of the pharmaceuticals in the river biofilm reactors.

  4. Thermodynamics of chiral selectivity in capillary electrophoresis : separation of ibuprofen enantiomers with beta-cyclodextrin

    NARCIS (Netherlands)

    Reijenga, J.C.; Ingelse, B.A.; Everaerts, F.M.

    1997-01-01

    The effect of temperature on the electrophoretic chiral separation of ibuprofen with ß-CD was investigated. Background electrolytes with sodium acetate or formate were chosen because of their constant pK within 0.03 units in the temperature range 25–50°C. Ibuprofen has a temperature independent pK

  5. EFFICACY OF IBUPROFEN IN TREATMENT OF PAIN IN CHILDREN: SYSTEMATIC REVIEW OF RANDOMIZED CONTROLLED STUDIES

    Directory of Open Access Journals (Sweden)

    R.T. Saygitov

    2010-01-01

    Full Text Available The article presents results of systematic review of data on prophylactic and therapeutic efficacy of ibuprofen. Data search was performed by PubMed database and Google search. 27 publications for analysis were available. Prophylactic efficacy of ibuprofen was studied in 14 studies. Summarizing of the results showed that ibuprofen prevents pain and decreases its following intensity after different surgical or dental operations. There is no significant difference in prophylactic efficacy of single dose ibuprofen and acetaminophen. Therapeutic efficacy of ibuprofen was described in 13 studies. Administration of the drug for pain stopping in children is reasonable. The analgesic effect of ibuprofen compared to placebo was shown in all studies of patients with migraine and diseases of ENT-organs. 5 studies performed in last 5 years showed efficacy of ibuprofen in trauma patients, including children with non-complicated fractures of extremities.Key words: children, pain, ibuprofen, prophylaxis, treatment.(Voprosy sovremennoi pediatrii — Current Pediatrics. 2010;9(6:52-62

  6. Ibuprofen - a Safe Analgesic During Cardiac Surgery Recovery? A Randomized Controlled Trial?

    Directory of Open Access Journals (Sweden)

    Saddiq Mohammad Qazi

    2015-12-01

    Conclusion: The results of this study suggest that patients treated postoperatively, following cardiac surgery, are at no greater risk of harm if short term slow release ibuprofen combined with lansoprazole treatment is used when compared to an oxycodone based regimen. Renal function should, however, be closely monitored and in the event of any decrease in renal function ibuprofen must be discontinued.

  7. Ibuprofen and/or paracetamol (acetaminophen) for pain relief after surgical removal of lower wisdom teeth

    NARCIS (Netherlands)

    Bailey, E.; Worthington, H.V.; van Wijk, A.; Yates, J.M.; Coulthard, P.; Afzal, Z.

    2013-01-01

    Background Both paracetamol and ibuprofen are commonly used analgesics for the relief of pain following the surgical removal of lower wisdom teeth (third molars). In 2010, a novel analgesic (marketed as Nuromol) containing both paracetamol and ibuprofen in the same tablet was launched in the United

  8. 75 FR 48352 - Determination That MOTRIN (Ibuprofen) Tablets and Four Other Drug Products Were Not Withdrawn...

    Science.gov (United States)

    2010-08-10

    ... DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2010-N-0391] Determination That MOTRIN (Ibuprofen) Tablets and Four Other Drug Products Were Not Withdrawn From Sale for... Applicant NDA 17-463 MOTRIN (ibuprofen) Tablets, 300 milligrams (mg), McNeil Consumer Healthcare, 7050 Camp...

  9. Possession divestment by sales in later life.

    Science.gov (United States)

    Ekerdt, David J; Addington, Aislinn

    2015-08-01

    Residential relocation in later life is almost always a downsizing, with many possessions to be divested in a short period of time. This article examines older movers' capacities for selling things, and ways that selling attenuates people's ties to those things, thus accomplishing the human dis-possession of the material convoy. In qualitative interviews in 79 households in the Midwestern United States, older adults reported their experience with possession sales associated with residential relocation. Among this group, three-quarters of the households downsized by selling some belongings. Informal sales seemed the least fraught of all strategies, estate sales had mixed reviews, and garage sales were recalled as laborious. Sellers' efforts were eased by social relations and social networks as helpers and buyers came forward. As selling proceeded, sentiment about possessions waned as their materiality and economic value came to the fore, easing their detachment from the household. Possession selling is challenging because older adults are limited in the knowledge, skills, and efforts that they can apply to the recommodification of their belongings. Selling can nonetheless be encouraged as a divestment strategy as long as the frustrations and drawbacks are transparent, and the goal of ridding is kept in view. Copyright © 2015 Elsevier Inc. All rights reserved.

  10. Quantitative proteomic analysis of ibuprofen-degrading Patulibacter sp. strain I11

    DEFF Research Database (Denmark)

    Almeida, Barbara; Kjeldal, Henrik; Lolas, Ihab Bishara Yousef

    2013-01-01

    was identified and quantified by gel based shotgun-proteomics. In total 251 unique proteins were quantitated using this approach. Biological process and pathway analysis indicated a number of proteins that were up-regulated in response to active degradation of ibuprofen, some of them are known to be involved...... in the degradation of aromatic compounds. Data analysis revealed that several of these proteins are likely involved in ibuprofen degradation by Patulibacter sp. strain I11.......Ibuprofen is the third most consumed pharmaceutical drug in the world. Several isolates have been shown to degrade ibuprofen, but very little is known about the biochemistry of this process. This study investigates the degradation of ibuprofen by Patulibacter sp. strain I11 by quantitative...

  11. Disposable screen printed graphite electrode for the direct electrochemical determination of ibuprofen in surface water

    KAUST Repository

    Amin, Sidra

    2014-08-01

    The potential of square wave voltammetry (SWV) for the determination of ibuprofen in aqueous solution, applying baseline correction, is reported. A screen printed graphite electrodes (SPGEs), especially pretreated for this purpose, were used to investigate the electrochemical oxidation and detection of ibuprofen. After optimization of SWV parameters, measurements were carried out at 200 Hz modulation frequency, 4 mV step potential and 40 mV pulse amplitude for the determination of ibuprofen. The surfaces of both untreated and pretreated SPGEs were characterized by scanning electron microscopy (SEM) and electrochemical impedance spectroscopy (EIS). The electro-catalytic properties of both the electrodes were correlated with the surface treatment. The pretreated screen printed graphite electrode exhibited a high sensitivity toward ibuprofen even in low concentration. The developed method was found rapid, cost-effective and reproducible for in-field ibuprofen detection.

  12. Disposable screen printed graphite electrode for the direct electrochemical determination of ibuprofen in surface water

    KAUST Repository

    Amin, Sidra; Soomro, M. Tahir; Memon, Najma; Solangi, Amber R.; Sirajuddin; Qureshi, Tahira; Behzad, Ali Reza

    2014-01-01

    The potential of square wave voltammetry (SWV) for the determination of ibuprofen in aqueous solution, applying baseline correction, is reported. A screen printed graphite electrodes (SPGEs), especially pretreated for this purpose, were used to investigate the electrochemical oxidation and detection of ibuprofen. After optimization of SWV parameters, measurements were carried out at 200 Hz modulation frequency, 4 mV step potential and 40 mV pulse amplitude for the determination of ibuprofen. The surfaces of both untreated and pretreated SPGEs were characterized by scanning electron microscopy (SEM) and electrochemical impedance spectroscopy (EIS). The electro-catalytic properties of both the electrodes were correlated with the surface treatment. The pretreated screen printed graphite electrode exhibited a high sensitivity toward ibuprofen even in low concentration. The developed method was found rapid, cost-effective and reproducible for in-field ibuprofen detection.

  13. SIMULTANEOUS DETERMINATION OF PARACETAMOL AND IBUPROFENE MIXTURES BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

    Directory of Open Access Journals (Sweden)

    Sophi Damayanti

    2010-06-01

    Full Text Available Analytical method for the determination of paracetamol and ibuprofene mixtures has been developed by High Performance Liquid Chromatography using C-18 column and acetinitrile - phosphate buffer pH = 4.5 (75:25 containing 0.075% sodium hexanesulfunate as a mobile phase. The detector was set at 215 nm. Using such conditions, retention time for paracetamol and ibuprofen was 4.89 and 7.11 min, respectively. The recovery for paracetamol and ibuprofen was found to be 101.07± 0.73% and 102.02 ± 1.58%, respectively. The detector limits of the method was 1.30 and 1.60 μg/mL with the relative standard deviation (RSD 0.74 and 1.52% for paracetamol and ibuprofen, respectively.   Keywords: paracetamol, ibuprofen, multi-component, validation, HPLC.

  14. Clinically relevant pain relief with an ibuprofen-releasing foam dressing

    DEFF Research Database (Denmark)

    Fogh, Karsten; Andersen, Maibritt B; Bischoff-Mikkelsen, Morten

    2012-01-01

    The objective of this 6-week, 120-patient, double-blind, randomized, controlled trial was to investigate if a foam dressing with ibuprofen provided clinically relevant pain relief (PAR) for exuding, painful venous leg ulcers in comparison with a similar foam dressing without ibuprofen. Primary......) and the corresponding number needed to treat (NNT). Wound-related parameters such as ulcer healing, ulcer area reduction, and peri-ulcer skin condition as well as adverse events were recorded during all 6 weeks of the investigation. PAR was significantly greater in the ibuprofen foam group than the comparator group (p...... = 0.0438). There were 34% responders in the ibuprofen foam group vs. 19% in the comparator group (NNT = 6.8). When evening data were analyzed separately to evaluate PAR over daytime, NNT was 5.3. Wound healing parameters and adverse events were comparable. In conclusion, in this study, the ibuprofen...

  15. A comparative study of ibuprofen with paracetamol versus oxyphenbutazone with analgin combination in ophthalmic practice

    Directory of Open Access Journals (Sweden)

    Roy I

    1988-01-01

    Full Text Available A total of 200 patients of either sex with various ophthalmic inflammatory disorders of surgical and non-surgical types were treated with ibuprofen with paracetamol 1 tablet tid. or a combination of oxyphenbutazone and analgin-1 tablet t. i. d. for 7 days/ Patients in the ibuprofen with Paracetamol group recorded a signifi-cantly greater reduction in pain scores; on day 1 and 2 and in swelling scores on day 2, 5 and 7 as compared to patients receiving the combination of ox yphenbutazone and analgin. A significantly lesserr number of patients in the ibuprofen with paraeetamol group required escape analgesics. Seventy six per cent of patients in the Ibuprofen with paracetamol group were judged as showing a Very good - Good, response to treatment as against 55 per cent in the oxvphenbutazone-analgin group. It is concluded that ibuprofen with Paracetamol is superior in efficacy and a safer alternative to a combination of oxyphenbutazone and analgin.

  16. Controlled release of ibuprofen by meso-macroporous silica

    Science.gov (United States)

    Santamaría, E.; Maestro, A.; Porras, M.; Gutiérrez, J. M.; González, C.

    2014-02-01

    Structured meso-macroporous silica was successfully synthesized from an O/W emulsion using decane as a dispersed phase. Sodium silicate solution, which acts as a silica source and a poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (EO19PO39EO19) denoted as P84 was used in order to stabilize the emulsion and as a mesopore template. The materials obtained were characterized through transmission electron microscopy (TEM), scanning electron microscopy (SEM), small-angle X-ray diffraction scattering (SAXS) and nitrogen adsorption-desorption isotherms. Ibuprofen (IBU) was selected as the model drug and loaded into ordered meso-macroporous materials. The effect of the materials’ properties on IBU drug loading and release was studied. The results showed that the loading of IBU increases as the macropore presence in the material is increased. The IBU adsorption process followed the Langmuir adsorption isotherm. A two-step release process, consisting of an initial fast release and then a slower release was observed. Macropores enhanced the adsorption capacity of the material; this was probably due to the fact that they allowed the drug to access internal pores. When only mesopores were present, ibuprofen was probably adsorbed on the mesopores close to the surface. Moreover, the more macropore present in the material, the slower the release behaviour observed, as the ibuprofen adsorbed in the internal pores had to diffuse along the macropore channels up to the surface of the material. The material obtained from a highly concentrated emulsion was functionalized with amino groups using two methods, the post-grafting mechanism and the co-condensation mechanism. Both routes improve IBU adsorption in the material and show good behaviour as a controlled drug delivery system.

  17. [Recurrent aseptic meningitis secondary to taking ibuprofen and ketorolac].

    Science.gov (United States)

    Cano Vargas-Machuca, E; Mondéjar-Marín, B; Navarro-Muñoz, S; Pérez-Molina, I; Garrido-Robres, J A; Alvarez-Tejerina, A

    Aseptic meningitis is a process that is characterised by an inflammatory reaction of the meninges that is not due to any infectious agent. Its aetiology is varied and is most frequently caused by rheumatologic and/or autoimmune processes, chemical or medication-induced meningitis, the most notable drugs involved being antibiotics and non-steroidal anti-inflammatory drugs (NSAI). We report the case of a 70-year-old male, with no relevant history, who was admitted to hospital five times over a period of 16 months because of acute meningitis with polymorphonuclear pleocytosis, high protein levels in cerebrospinal fluid and normal glucose in cerebrospinal fluid. No evidence of an infectious causation, chemical meningitis, carcinomatosis or autoimmune disease was found and the patient was diagnosed with recurrent aseptic meningitis. It was found that the patient had taken ibuprofen or ketorolac on several occasions, a few hours before the appearance of symptoms. These episodes were quickly resolved after withdrawal of this medication. A number of NSAI have been reported as inducers of aseptic meningitis, one of the most notable being ibuprofen. We report the case of a patient who, as a consequence of taking ibuprofen and ketorolac, presented episodes of recurrent aseptic meningitis. To our knowledge this side effect of ketorolac has not been reported before. Its clinical features are impossible to differentiate from those of infectious meningitis. Diagnosis is reached by exclusion and a careful pharmacological study, including over-the-counter drugs like some of the NSAI, must be performed in patients with this condition, since it is a problem that can easily be solved by withdrawing the drug that causes it.

  18. The Failed Image and the Possessed

    DEFF Research Database (Denmark)

    Suhr, Christian

    2015-01-01

    This article asks if the recurrent queries regarding the value of images in visual anthropology could find new answers by exploring responses to visual media in neo-orthodox Islam. It proposes that the visual display of the photographic image shares a curious resemblance to the bodies of people...... possessed by invisible spirits called jinn. The image as a failed example or model of reality works like the possessed body as an amplifier of invisibility pointing towards that which cannot be seen, depicted visually, or represented in writing. This suggests a negative epistemology in which images obtain...

  19. Digital possessions after a romantic break up

    NARCIS (Netherlands)

    Herron, Daniel; Moncur, Wendy; van den Hoven, Elise

    2016-01-01

    With technology becoming more pervasive in everyday life, it is common for individuals to use digital media to support the enactment and maintenance of romantic relationships. Partners in a relationship may create digital possessions frequently. However, after a relationship ends, individuals

  20. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model

    Science.gov (United States)

    Rooney, Sarah Ilkhanipour; Baskin, Rachel; Torino, Daniel J.; Vafa, Rameen P.; Khandekar, Pooja S.; Kuntz, Andrew F.; Soslowsky, Louis J.

    2017-01-01

    Background Previous studies have shown that ibuprofen is detrimental to tissue healing following acute injury; however, the effects of ibuprofen when combined with non-injurious exercise are debated. Hypothesis We hypothesized that administration of ibuprofen to rats undergoing a non-injurious treadmill exercise protocol would abolish the beneficial adaptations found with exercise but have no effect on sedentary muscle and tendon properties. Study Design Controlled laboratory study Methods Rats were divided into exercise or cage activity (sedentary) groups and acute (a single bout of exercise followed by 24 hours of rest) and chronic (2 or 8 weeks of repeated exercise) time points. Half of the rats received ibuprofen to investigate the effects of this drug over time when combined with different activity levels (exercise and sedentary). Supraspinatus tendons were used for mechanical testing and histology (organization, cell shape, cellularity), and supraspinatus muscles were used for morphological (fiber CSA, centrally nucleated fibers) and fiber type analysis. Results Chronic intake of ibuprofen did not impair supraspinatus tendon organization or mechanical adaptations (stiffness, modulus, max load, max stress, dynamic modulus, or viscoelastic properties) to exercise. Tendon mechanical properties were not diminished and in some instances increased with ibuprofen. In contrast, total supraspinatus muscle fiber cross-sectional area decreased with ibuprofen at chronic time points, and some fiber type-specific changes were detected. Conclusions Chronic administration of ibuprofen does not impair supraspinatus tendon mechanical properties in a rat model of exercise but does decrease supraspinatus muscle fiber cross-sectional area. Clinically, these findings suggest that ibuprofen does not detrimentally affect regulation of supraspinatus tendon adaptions to exercise but does decrease muscle growth. Individuals should be advised on the risk of decreased muscle hypertrophy

  1. POSSESSION VERSUS POSITION: STRATEGIC EVALUATION IN AFL

    Directory of Open Access Journals (Sweden)

    Darren M. O'Shaughnessy

    2006-12-01

    Full Text Available In sports like Australian Rules football and soccer, teams must battle to achieve possession of the ball in sufficient space to make optimal use of it. Ultimately the teams need to score, and to do that the ball must be brought into the area in front of goal - the place where the defence usually concentrates on shutting down space and opportunity time. Coaches would like to quantify the trade-offs between contested play in good positions and uncontested play in less promising positions, in order to inform their decision-making about where to put their players, and when to gamble on sending the ball to a contest rather than simply maintain possession. To evaluate football strategies, Champion Data has collected the on-ground locations of all 350,000 possessions and stoppages in the past two seasons of AFL (2004, 2005. By following each chain of play through to the next score, we can now reliably estimate the scoreboard "equity" of possessing the ball at any location, and measure the effect of having sufficient time to dispose of it effectively. As expected, winning the ball under physical pressure (through a "hard ball get" is far more difficult to convert into a score than winning it via a mark. We also analyse some equity gradients to show how getting the ball 20 metres closer to goal is much more important in certain areas of the ground than in others. We conclude by looking at the choices faced by players in possession wanting to maximise their likelihood of success

  2. Alternating ibuprofen and acetaminophen in the treatment of febrile children: a pilot study [ISRCTN30487061

    Directory of Open Access Journals (Sweden)

    Sabra Ramzi

    2006-03-01

    Full Text Available Abstract Background Alternating ibuprofen and acetaminophen for the treatment of febrile children is a prevalent practice among physicians and parents, despite the lack of evidence on effectiveness or safety. This randomized, double-blind and placebo-controlled clinical trial aims at comparing the antipyretic effectiveness and safety of a single administration of alternating ibuprofen and acetaminophen doses to that of ibuprofen mono-therapy in febrile children. Methods Seventy febrile children were randomly allocated to receive either a single oral dose of 10 mg/kg ibuprofen and 15 mg/kg oral acetaminophen after 4 hours, or a similar dose of ibuprofen and placebo at 4 hours. Rectal temperature was measured at baseline, 4, 5, 6, 7 and 8 hours later. Endpoints included proportions of afebrile children at 6, 7 and 8 hours, maximum decline in temperature, time to recurrence of fever, and change in temperature from baseline at each time point. Intent-to-treat analysis was planned with statistical significance set at P Results A higher proportion of subjects in the intervention group (83.3% became afebrile at 6 hours than in the control group (57.6%; P = 0.018. This difference was accentuated at 7 and 8 hours (P Conclusion A single dose of alternating ibuprofen and acetaminophen appears to be a superior antipyretic regimen than ibuprofen mono-therapy. Further studies are needed to confirm these findings.

  3. Single dose oral ibuprofen plus paracetamol (acetaminophen) for acute postoperative pain.

    Science.gov (United States)

    Derry, Christopher J; Derry, Sheena; Moore, R Andrew

    2013-06-24

    Combining two different analgesics in fixed doses in a single tablet can provide better pain relief than either drug alone in acute pain. This appears to be broadly true across a range of different drug combinations, in postoperative pain and migraine headache. Some combinations of ibuprofen and paracetamol are available for use without prescription in some acute pain situations. To assess the efficacy and adverse effects of single dose oral ibuprofen plus paracetamol for acute postoperative pain using methods that permit comparison with other analgesics evaluated in standardised trials using almost identical methods and outcomes. We searched the Cochrane Central Register of Controlled Trials (CENTRAL) on The Cochrane Library (Issue 4 of 12, 2013), MEDLINE (1950 to May 21st 2013), EMBASE (1974 to May 21st 2013), the Oxford Pain Database, ClinicalTrials.gov, and reference lists of articles. Randomised, double-blind clinical trials of single dose, oral ibuprofen plus paracetamol compared with placebo or the same dose of ibuprofen alone for acute postoperative pain in adults. Two review authors independently considered trials for inclusion in the review, assessed quality, and extracted data. We used validated equations to calculate the area under the pain relief versus time curve and derive the proportion of participants with at least 50% of maximum pain relief over six hours. We calculated relative risk (RR) and number needed to treat to benefit (NNT) for ibuprofen plus paracetamol, ibuprofen alone, or placebo. We used information on use of rescue medication to calculate the proportion of participants requiring rescue medication and the weighted mean of the median time to use. We also collected information on adverse events. Searches identified three studies involving 1647 participants. Each of them examined several dose combinations. Included studies provided data from 508 participants for the comparison of ibuprofen 200 mg + paracetamol 500 mg with placebo, 543

  4. Effects of acetaminophen and ibuprofen in children with migraine receiving preventive treatment with magnesium.

    Science.gov (United States)

    Gallelli, Luca; Avenoso, Tiziana; Falcone, Daniela; Palleria, Caterina; Peltrone, Francesco; Esposito, Maria; De Sarro, Giovambattista; Carotenuto, Marco; Guidetti, Vincenzo

    2014-02-01

    The purpose of this study was to evaluate both the effects of ibuprofen and/or acetaminophen for the acute treatment of primary migraine in children in or out prophylactic treatment with magnesium. Children ranging from the ages of 5 to 16 years with at least 4 attack/month of primary migraine were eligible for participation the study. A visual analog scale was used to evaluate pain intensity at the moment of admission to the study (start of the study) and every month up to 18 months later (end of the study). One hundred sixty children of both sexes aged 5-16 years were enrolled and assigned in 4 groups to receive a treatment with acetaminophen or ibuprofen without or with magnesium. Migraine pain endurance and monthly frequency were similar in the 4 groups. Both acetaminophen and ibuprofen induced a significant decrease in pain intensity (P < .01), without a time-dependent correlation, but did not modify its frequency. Magnesium pretreatment induced a significant decrease in pain intensity (P < .01) without a time-dependent correlation in both acetaminophen- and ibuprofen-treated children and also significantly reduced (P < .01) the pain relief timing during acetaminophen but not during ibuprofen treatment (P < .01). In both acetaminophen and ibuprofen groups, magnesium pretreatment significantly reduced the pain frequency (P < .01). Magnesium increased the efficacy of ibuprofen and acetaminophen with not age-related effects. © 2013 American Headache Society.

  5. Characteristics and clinical implications of the pharmacokinetic profile of ibuprofen in patients with knee osteoarthritis.

    Science.gov (United States)

    Gallelli, L; Galasso, O; Urzino, A; Saccà, S; Falcone, D; Palleria, C; Longo, P; Corigliano, A; Terracciano, R; Savino, R; Gasparini, G; De Sarro, G; Southworth, S R

    2012-12-01

    Ibuprofen is a non-selective cyclo-oxygenase (COX)-1/COX-2 inhibitor used to treat pain conditions and inflammation. Limited data have been published concerning the pharmacokinetic profile and clinical effects of ibuprofen in patients with osteoarthritis (OA). In this paper we compared the pharmacokinetic and clinical profile of ibuprofen (at a dosage of from 800 mg/day to 1800 mg/day) administered in patients affected by severe knee OA. Ibuprofen was administered for 7 days to patients who were scheduled to undergo knee arthroplasty due to OA. After 7 days, the ibuprofen concentration in plasma and synovial fluid was measured through both high-performance liquid chromatography (HPLC)-UV and gas chromatography-mass spectroscopy (GC/MS), while clinical effects were evaluated through both visual analogue scale (VAS) and Western Ontario and McMaster Universities (WOMAC) scores. The Naranjo scale and the WHO causality assessment scale were used for estimating the probability of adverse drug reactions (ADRs). The severity of ADRs was assessed by the modified Hartwig and Siegel scale. Ibuprofen showed a dose-dependent diffusion in both plasma and synovial fluid, which was related to the reduction of pain intensity and improvement of health status, without the development of ADRs. Ibuprofen at higher dosages can be expected to provide better control of OA symptoms as a result of higher tissue distribution.

  6. Treatment of ibuprofen intoxication in a dog via therapeutic plasma exchange.

    Science.gov (United States)

    Walton, Stuart; Ryan, Kirk A; Davis, Jennifer L; Acierno, Mark

    2017-07-01

    To describe the treatment of ibuprofen intoxication with therapeutic plasma exchange in a dog (TPE). A 13-year-old male neutered mixed breed dog presented after ingesting approximately 200 mg/kg of ibuprofen. Treatment consisted of supportive medical therapy with IV fluids, gastrointestinal protectants, antiemetics and prostaglandin analogs, and TPE. A cycle of TPE was performed over 180 minutes, achieving 1.5 plasma volume exchanges. During therapy, heparinized blood and effluent samples were collected. Ibuprofen concentrations were determined in the samples by high-pressure liquid chromatography. Post TPE, the dog was continued on supportive medical therapy and was discharged 96 hours after the overdose. This report describes the use of TPE as an adjunct for ibuprofen intoxication. An 85% reduction in plasma ibuprofen concentration occurred and recovery from a potentially lethal ingestion of ibuprofen was achieved with TPE and supportive care. TPE should be considered when presented with acute ibuprofen intoxication due to the rapid and efficacious nature of therapy. © Veterinary Emergency and Critical Care Society 2017.

  7. Mechanistic studies of the metabolic chiral inversion of (R)-ibuprofen in humans

    International Nuclear Information System (INIS)

    Baillie, T.A.; Adams, W.J.; Kaiser, D.G.; Olanoff, L.S.; Halstead, G.W.; Harpootlian, H.; Van Giessen, G.J.

    1989-01-01

    The metabolic chiral inversion of R-(-)-ibuprofen has been studied in human subjects by means of specific deuterium labeling and stereoselective gas chromatography-mass spectrometry methodology. After simultaneous p.o. administration of a mixture of R-(-)-ibuprofen (300 mg) and R-(-)-[3,3,3-2H3]ibuprofen (304 mg) to four adult male volunteers, the enantiomeric composition and deuterium content of the drug in serum, and of the drug and its principal metabolites in urine, were followed over a period of 24 hr. The results of these analyses indicated that: (1) conversion of R-(-)- to S-(+)-ibuprofen takes place with complete retention of deuterium at the beta-methyl (C-3) position; (2) chiral inversion of R-(-)-[2H3]ibuprofen is not subject to a discernible deuterium isotope effect; and (3) replacement of the beta-methyl hydrogen atoms by deuterium has no effect on any of the serum pharmacokinetic parameters for R-(-)- or S-(+)-ibuprofen. These data indicate that the process whereby R-(-)-ibuprofen undergoes metabolic inversion in human subjects does not involve 2,3-dehydroibuprofen as an intermediate, and that the underlying mechanism cannot, therefore, entail a desaturation/reduction sequence

  8. Ibuprofen and Diclofenac Restrict Migration and Proliferation of Human Glioma Cells by Distinct Molecular Mechanisms

    Science.gov (United States)

    Leidgens, Verena; Seliger, Corinna; Jachnik, Birgit; Welz, Tobias; Leukel, Petra; Vollmann-Zwerenz, Arabel; Bogdahn, Ulrich; Kreutz, Marina; Grauer, Oliver M.; Hau, Peter

    2015-01-01

    Background Non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with anti-tumorigenic effects in different tumor entities. For glioma, research has generally focused on diclofenac; however data on other NSAIDs, such as ibuprofen, is limited. Therefore, we performed a comprehensive investigation of the cellular, molecular, and metabolic effects of ibuprofen and diclofenac on human glioblastoma cells. Methods Glioma cell lines were treated with ibuprofen or diclofenac to investigate functional effects on proliferation and cell motility. Cell cycle, extracellular lactate levels, lactate dehydrogenase-A (LDH-A) expression and activity, as well as inhibition of the Signal Transducer and Activator of Transcription 3 (STAT-3) signaling pathway, were determined. Specific effects of diclofenac and ibuprofen on STAT-3 were investigated by comparing their effects with those of the specific STAT-3 inhibitor STATTIC. Results Ibuprofen treatment led to a stronger inhibition of cell growth and migration than treatment with diclofenac. Proliferation was affected by cell cycle arrest at different checkpoints by both agents. In addition, diclofenac, but not ibuprofen, decreased lactate levels in all concentrations used. Both decreased STAT-3 phosphorylation; however, diclofenac led to decreased c-myc expression and subsequent reduction in LDH-A activity, whereas treatment with ibuprofen in higher doses induced c-myc expression and less LDH-A alteration. Conclusions This study indicates that both ibuprofen and diclofenac strongly inhibit glioma cells, but the subsequent metabolic responses of both agents are distinct. We postulate that ibuprofen may inhibit tumor cells also by COX- and lactate-independent mechanisms after long-term treatment in physiological dosages, whereas diclofenac mainly acts by inhibition of STAT-3 signaling and downstream modulation of glycolysis. PMID:26485029

  9. Acute pain management: acetaminophen and ibuprofen are often under-dosed.

    Science.gov (United States)

    Milani, Gregorio P; Benini, Franca; Dell'Era, Laura; Silvagni, Davide; Podestà, Alberto F; Mancusi, Rossella Letizia; Fossali, Emilio F

    2017-07-01

    Most children with pain are managed by either acetaminophen or ibuprofen. However, no study has so far investigated if children are prescribed adequate doses of acetaminophen or ibuprofen in emergency department. Aim of this retrospective study was to investigate the prevalence of under-dosage of these drugs in children presenting with pain in emergency department. Children initially prescribed with acetaminophen or ibuprofen for pain management were included. The χ 2 automatic interaction detection method was used considering the percentage variation from the minimum of the appropriate dose as dependent variable while prescribed drug, age, gender, body weight, type of hospital (pediatric or general), and availability of internal guidelines on pediatric pain management in the emergency department as independent variables. Data on 1471 children managed for pain were available. Under-dosage was prescribed in 893 subjects (61%), of whom 577 were prescribed acetaminophen and 316 ibuprofen. The use of acetaminophen suppositories, body weight 40 kg, and the use of oral ibuprofen identified clusters of children associated with under-dosage prescription. Prescription of acetaminophen and ibuprofen was frequently under-dosed. The use of suppositories, lower and higher body weight, and the use of ibuprofen were associated with under-dosage. Under-dosing may reflect prescription of anti-pyretic doses. Agenzia Italiana del Farmaco-Observational Study Register (RSO). Registration code: PIERRE/1 What is Known: • Pain is frequent in children presented to emergency department. • International recommendations on pain management are often not implemented. What is New: • Acetaminophen and ibuprofen were frequently underdosed in children prescribed for pain in the Italian emergency departments. • Under-dosage may be related to the habit of using acetaminophen and ibuprofen in the recommended range for fever treatment.

  10. A Randomized Placebo Controlled Trial of Ibuprofen for Respiratory Syncytial Virus Infection in a Bovine Model.

    Directory of Open Access Journals (Sweden)

    Paul Walsh

    Full Text Available Respiratory syncytial virus (RSV is the most common cause of bronchiolitis and hospital admission in infants. An analogous disease occurs in cattle and costs US agriculture a billion dollars a year. RSV causes much of its morbidity indirectly via adverse effects of the host response to the virus. RSV is accompanied by elevated prostaglandin E2 (PGE2 which is followed by neutrophil led inflammation in the lung. Ibuprofen is a prototypical non-steroidal anti-inflammatory drug that decreases PGE2 levels by inhibiting cyclooxygenase.We hypothesized that treatment of RSV with ibuprofen would decrease PGE2 levels, modulate the immune response, decrease clinical illness, and decrease the histopathological lung changes in a bovine model of RSV. We further hypothesized that viral replication would be unaffected.We performed a randomized placebo controlled trial of ibuprofen in 16 outbred Holstein calves that we infected with RSV. We measured clinical scores, cyclooxygenase, lipoxygenase and endocannabinoid products in plasma and mediastinal lymph nodes and interleukin (Il-4, Il-13, Il-17 and interferon-γ in mediastinal lymph nodes. RSV shedding was measured daily and nasal Il-6, Il-8 and Il-17 every other day. The calves were necropsied on Day 10 post inoculation and histology performed.One calf in the ibuprofen group required euthanasia on Day 8 of infection for respiratory distress. Clinical scores (p<0.01 and weight gain (p = 0.08 seemed better in the ibuprofen group. Ibuprofen decreased cyclooxygenase, lipoxygenase, and cytochrome P450 products, and increased monoacylglycerols in lung lymph nodes. Ibuprofen modulated the immune response as measured by narrowed range of observed Il-13, Il-17 and IFN-γ gene expression in mediastinal lymph nodes. Lung histology was not different between groups, and viral shedding was increased in calves randomized to ibuprofen.Ibuprofen decreased PGE2, modulated the immune response, and improved clinical outcomes

  11. Efficacy of ibuprofen on prevention of high altitude headache: A systematic review and meta-analysis.

    Directory of Open Access Journals (Sweden)

    Juan Xiong

    Full Text Available Ibuprofen is used to prevent high altitude headache (HAH but its efficacy remains controversial. We conducted a systematic review and meta-analysis of randomized, placebo-controlled trials (RCTs of ibuprofen for the prevention of HAH.Studies reporting efficacy of ibuprofen for prevention of HAH were identified by searching electronic databases (until December 2016. The primary outcome was the difference in incidence of HAH between ibuprofen and placebo groups. Risk ratios (RR were aggregated using a Mantel-Haenszel random effect model. Heterogeneity of included trials was assessed using the I2 statistics.In three randomized-controlled clinical trials involving 407 subjects, HAH occurred in 101 of 239 subjects (42% who received ibuprofen and 96 of 168 (57% who received placebo (RR = 0.79, 95% CI 0.66 to 0.96, Z = 2.43, P = 0.02, I2 = 0%. The absolute risk reduction (ARR was 15%. Number needed to treat (NNT to prevent HAH was 7. Similarly, The incidence of severe HAH was significant in the two groups (RR = 0.40, 95% CI 0.17 to 0.93, Z = 2.14, P = 0.03, I2 = 0%. Severe HAH occurred in 3% treated with ibuprofen and 10% with placebo. The ARR was 8%. NNT to prevent severe HAH was 13. Headache severity using a visual analogue scale was not different between ibuprofen and placebo. Similarly, the difference between the two groups in the change in SpO2 from baseline to altitude was not different. One included RCT reported one participant with black stools and three participants with stomach pain in the ibuprofen group, while seven participants reported stomach pain in the placebo group.Based on a limited number of studies ibuprofen seems efficacious for the prevention of HAH and may therefore represent an alternative for preventing HAH with acetazolamide or dexamethasone.

  12. Taking Possession: Rituals, Space and Authority

    Directory of Open Access Journals (Sweden)

    Jennifer Mara DeSilva

    2016-12-01

    Full Text Available In early modern Europe authority over communities, both people and spaces, was visualized through ritual gestures and processions. Communities gathered to witness ceremonial entries that drew on accepted forms of gestures and speech identifying individuals and articulating their place in the urban power relationship. Ceremonial entries by rulers, ambassadors, bishops, and other office-holders drew on ritual acts projecting messages of possession in order to establish reputations of prestige and authority. This introductory essay draws on cultural anthropology and recent historiography to build a framework for understanding rituals of possession that went beyond the tradition triumphal entry to incorporate substitutes, new modes of prestigious display, and attend to conflicts. By “taking possession” of communities, offices, and spaces using accepted ritual forms, early moderns initiated conversations about authority and power that were far more flexible in their scope, practice, and participants than expected.

  13. Akut pankreatitis hos en 16-årig dreng efter indtag af ibuprofen

    DEFF Research Database (Denmark)

    Bruusgaard-Mouritsen, Mads Emil; Leerhøy, Bonna; Hansen, Mark Berner

    2015-01-01

    This is a case report of a 16-year-old boy with possible drug-induced pancreatitis (DIP) caused by ibuprofen. The patient had a history of psychiatric, but no somatic, disease, and he was admitted with a clinical presentation consistent with acute pancreatitis after a bolus ingestion of 10 g...... of ibuprofen in a suicidal attempt. No evidence of other causality for acute pancreatitis was identified. The patient was treated with a standard pancreatitis treatment regime and was discharged against medical advice after four days. The case represents a possible causality between ibuprofen and DIP....

  14. IBUPROFEN AS A MEDICATION FOR A CORRECTION OF SYMPTOMS OF NORMAL VACCINAL PROCESS IN CHILDREN

    Directory of Open Access Journals (Sweden)

    T.A. Chebotareva

    2008-01-01

    Full Text Available The pathogenetic approach to treatment of symptoms of normal vaccinal process in children after standard vaccination, based on the results of application of anti9inflammatory medications — ibuprofen (nurofen for children and paracetamol is presented in this article. Clinical activity of ibuprofen was established on the basis of clinica catamnestic observation of 856 vaccinated children aged from 3 months to 3 years. recommendations for application of these medications as a treatment for a correction of vaccinal reactions are given.Key words: children, ibuprofen, paracetamol, vaccination.

  15. Resolution of ibuprofen: a project for an experimental organic chemistry course

    International Nuclear Information System (INIS)

    Romero, Adriano L.; Baptistella, Lucia H.B.; Coelho, Fernando; Imamura, Paulo M.

    2012-01-01

    A practical and didactic sequence of experiments was proposed to illustrate the stereochemistry concept, optically active compounds, resolution of racemates, and use of the NMR technique, including 2D-COSY for identification of organic compounds, on a laboratory course for undergraduate students. The sequence was: extractions of racemic ibuprofen and chiral naproxen from commercial tablets; syntheses of diastereoisomeric amides reacting chiral (S)-(-)-α-methylbenzylamine with (+-)-ibuprofen; separation and determination of absolute configuration of amides by 1 H NMR spectroscopy and GC analysis, and hydrolysis of amides to obtain (+)- and (-)-ibuprofen. (author)

  16. Phytoextraction, phytotransformation and rhizodegradation of ibuprofen associated with Typha angustifolia in a horizontal subsurface flow constructed wetland.

    Science.gov (United States)

    Li, Yifei; Zhang, Jiefeng; Zhu, Guibing; Liu, Yu; Wu, Bing; Ng, Wun Jern; Appan, Adhityan; Tan, Soon Keat

    2016-10-01

    Widespread occurrence of trace pharmaceutical residues in aquatic environments is of great concerns due to the potential chronic toxicity of certain pharmaceuticals including ibuprofen on aquatic organisms even at environmental levels. In this study, the phytoextraction, phytotransformation and rhizodegradation of ibuprofen associated with Typha angustifolia were investigated in a horizontal subsurface flow constructed wetland system. The experimental wetland system consisted of a planted bed with Typha angustifolia and an unplanted bed (control) to treat ibuprofen-loaded wastewater (∼107.2 μg L(-1)). Over a period of 342 days, ibuprofen was accumulated in leaf sheath and lamina tissues at a mean concentration of 160.7 ng g(-1), indicating the occurrence of the phytoextraction of ibuprofen. Root-uptake ibuprofen was partially transformed to ibuprofen carboxylic acid, 2-hydroxy ibuprofen and 1-hydroxy ibuprofen which were found to be 1374.9, 235.6 and 301.5 ng g(-1) in the sheath, respectively, while they were 1051.1, 693.6 and 178.7 ng g(-1) in the lamina. The findings from pyrosequencing analysis of the rhizosphere bacteria suggest that the Dechloromonas sp., the Clostridium sp. (e.g. Clostridium saccharobutylicum), the order Sphingobacteriales, and the Cytophaga sp. in the order Cytophagales were most probably responsible for the rhizodegradation of ibuprofen. Copyright © 2016 Elsevier Ltd. All rights reserved.

  17. Phospho-Ibuprofen (MDC-917) Is a Novel Agent against Colon Cancer: Efficacy, Metabolism, and Pharmacokinetics in Mouse Models

    Science.gov (United States)

    Xie, Gang; Sun, Yu; Nie, Ting; Mackenzie, Gerardo G.; Huang, Liqun; Kopelovich, Levy; Komninou, Despina

    2011-01-01

    We have developed a novel chemical modification of conventional nonsteroidal anti-inflammatory drugs to reduce their toxicity and enhance their efficacy. Phospho-ibuprofen [(PI) 2-(4-isobutyl-phenyl)-propionic acid-4-(diethoxy-phosphoryloxy)-butyl ester (MDC-917)], a novel derivative of ibuprofen, strongly inhibited the growth of human colon cancer cells in vitro and SW480 human colon cancer xenografts in nude mice. PI was metabolized minimally by cultured cells, but extensively by liver microsomes and mice, undergoing regioselective oxidation to produce 1-OH-PI and carboxyl-PI, which can be hydrolyzed to 1-OH-ibuprofen and carboxyl-ibuprofen, respectively. PI also can be hydrolyzed to release ibuprofen, which can generate 2-OH-ibuprofen, carboxyl-ibuprofen, and ibuprofen glucuronide. After a single oral administration (400 mg/kg) of PI, ibuprofen and ibuprofen glucuronide are the main plasma metabolites of PI; they have, respectively, Cmax of 530 and 215 μM, Tmax of 1 and 2 h, elimination t1/2 of 7.7 and 5.3 h, and area under the concentration-time curve (0–24 h) of 1816 and 832 μM × h. Intact PI was detected in several tissues but not in plasma; at a higher PI dose (1200 mg/kg), PI plasma levels were 12.4 μM. PI generated the same metabolites in mouse plasma as conventional ibuprofen, but with much lower levels, perhaps accounting for the enhanced safety of PI. The antitumor effect of PI was significantly associated with plasma ibuprofen levels (p = 0.016) but not with xenograft ibuprofen levels (p = 0.08), suggesting a complex anticancer effect. These results provide a pharmacological basis to explain, at least in part, the anticancer efficacy and safety of this promising compound and indicate that PI merits further evaluation as an anticancer agent. PMID:21422165

  18. Thermodynamic and Calorimetric Study of Acetylsalicylic Acid (Aspirin and Ibuprofen

    Directory of Open Access Journals (Sweden)

    Juan Carlos Moreno-Piraján

    2011-01-01

    Full Text Available Enthalpies of solution and dilution of aqueous solutions of sodium acetylsalicylic acid salt and ibuprofen salt were measured with an isoperibolic calorimeter at 293.15 K, 298.15 K, 303.15 K, 308.15 K and 318.15 K. The concentration of the electrolyte was restricted to the solubility of the salt at various temperatures and did not exceed 0.035–0.057 mol kg-1, depending on the temperature studied. The Virial coefficients were derived from Pitzer's model and the excess thermodynamic functions of both the solution and the components of the solution were calculated. An analysis of the thermodynamic characteristics of the solution in terms of concentration and temperature interval was carried out and discussed. Additionally, an analysis was performed by differential scanning calorimetry (DSC.

  19. Formulation and evaluation of transparent ibuprofen soft gelatin capsule

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    A Lodha

    2012-01-01

    A medication suitable to combat acute pain is demanded to display its effects fast which action, in turn, is only achieved by a quick release and good bio-availability of the active-ingredient. It is for the commercial forms in particular that the conditions of preparation must be strictly observed, as minor alterations in production procedures such as mixing, pressure of compression and type of machine will affect the physical properties of the particles of he active ingredient and will deteriorate its bio-availability. It is an object of this presentation to provide a medicament that can be readily taken that contains an active amount of ibuprofen in a carrier, that is simple to prepare and that will quickly display a high activity.

  20. Application of SeDeM expert systems in preformulation studies of pediatric ibuprofen ODT tablets

    Directory of Open Access Journals (Sweden)

    Sipos Emese

    2017-06-01

    Full Text Available Pediatric, ibuprofen containing orodispersible tablets (ODTs were prepared using the SeDeM expert system methodology. In order to facilitate formulation, directly compressible ibuprofen was employed (Ibuprofen DC 8TM and characterized using its SeDeM profile. The mannitol based superdisintegrant Ludiflash® was characterized by the SeDeM-ODT expert system, which also allowed calculation of the optimal excipient concentration in order to obtain suitable tablet hardness and disintegration time. After adding a sweetener and a standard combination of lubricants, the optimized formulation was directly compressed into tablets and evaluated in terms of tablet hardness, friability, disintegration time and dissolution profile. The SeDeM method was applied to determine the amount of corrective excipient (Ludiflash® required for the compression of Ibuprofen DC 85TM in order to achieve suitable ODTs. Adequate tablet hardness, disintegration time, friability and dissolution profiles were found during tablet evaluation.

  1. Microbial Removal of the Pharmaceutical Compounds Ibuprofen and Diclofenac from Wastewater

    NARCIS (Netherlands)

    Langenhoff, A.A.M.; Inderfurth, N.S.; Veuskens, T.; Schraa, G.; Blokland, M.; Kujawa-Roeleveld, K.; Rijnaarts, H.H.M.

    2013-01-01

    Studies on the occurrence of pharmaceuticals show that the widely used pharmaceuticals ibuprofen and diclofenac are present in relevant concentrations in the environment. A pilot plant treating hospital wastewater with relevant concentrations of these pharmaceuticals was evaluated for its

  2. Enantioselective analysis of ibuprofen and its biotransformation products in water/sediment systems,

    DEFF Research Database (Denmark)

    Sundström, Maria; Escola, Monica; Radke, Michael

    2015-01-01

    of the sediments in the aquatic systems has neither been taken in account previously. In this study, four water-sediment systems were chosen according to anthropogenic exposure and sediment conditions. A low anthropogenic impact lake (Largen), a river receiving wastewater (Fyrisån) and two sediments (anoxic......As ibuprofen degrades enantioselectively in activated sludge, the same process is assumed to occur in surface lake-water and in river-water based biofilms. Yet, the effects of the wastewater inflow, containing non-racemic ibuprofen, into natural systems have never been studied. The role......-7 days in Tvären and B1 respectively. Largen sediments, not impacted by wastewater, degraded ibuprofen faster than Fyrisån sediments did. Yet, these two sediments sediments showed no significant difference with respect to the degradation rates of the ibuprofen enantiomers. A connection between wastewater...

  3. Ibuprofen Release from Poly(ethyl cyanoacrylate Nanoparticles Prepared by Semicontinuous Heterophase Polymerization

    Directory of Open Access Journals (Sweden)

    J. A. Balleño

    2018-01-01

    Full Text Available Ibuprofen-loaded poly(ethyl cyanoacrylate nanoparticles were prepared by semicontinuous heterophase polymerization of ethyl cyanoacrylate in the presence of ibuprofen; different surfactant concentration, pH, and temperature were used. Particle size was measured by quasi-light scattering and transmission electron microscopy, while the amount of drug released was determined by UV spectroscopy. Nanoparticles with diameters between 10 and 58 nm, loaded with ibuprofen, were obtained. The smallest particles and the higher drug loading were obtained at the highest pH tested. The analysis of the release data showed that the drug release profiles correspond to the Weibull model. Moreover, it was found that most of the ibuprofen is released within the first 80–120 min; initially the release rate is slow, but then it increases to finally decrease. This behavior contrasts with the reported burst of drug concentration in the plasma after oral administration of IB.

  4. Application of SeDeM expert systems in preformulation studies of pediatric ibuprofen ODT tablets.

    Science.gov (United States)

    Sipos, Emese; Oltean, Andrea Ramona; Szabó, Zoltán-István; Rédai, Emőke-Margit; Nagy, Gabriella Dónáth

    2017-06-27

    Pediatric, ibuprofen containing orodispersible tablets (ODTs) were prepared using the SeDeM expert system methodology. In order to facilitate formulation, directly compressible ibuprofen was employed (Ibuprofen DC 8TM) and characterized using its SeDeM profile. The mannitol based superdisintegrant Ludiflash® was characterized by the SeDeM-ODT expert system, which also allowed calculation of the optimal excipient concentration in order to obtain suitable tablet hardness and disintegration time. After adding a sweetener and a standard combination of lubricants, the optimized formulation was directly compressed into tablets and evaluated in terms of tablet hardness, friability, disintegration time and dissolution profile. The SeDeM method was applied to determine the amount of corrective excipient (Ludiflash®) required for the compression of Ibuprofen DC 85TM in order to achieve suitable ODTs. Adequate tablet hardness, disintegration time, friability and dissolution profiles were found during tablet evaluation.

  5. Differential renal adverse effects of ibuprofen and indomethacin in preterm infants: a review

    Directory of Open Access Journals (Sweden)

    Pacifici GM

    2014-07-01

    Full Text Available Gian Maria Pacifici Medical School, Department of Translational Research and New Technologies in Medicine and Surgery, Section of Pharmacology, University of Pisa, Pisa, Italy Objective: The objective of this study was to evaluate the extent of renal adverse effects caused by ibuprofen or indomethacin in order to choose the safer drug to administer to preterm infants. Methods: The following three parameters of renal function were taken into consideration: 1 the urine output; 2 the serum creatinine concentration; and 3 the frequency of oliguria. The bibliographic search was performed using PubMed and Embase databases as search engines. Results: Urine output ranged from 3.5±1.2 to 4.0±1.4 mL/kg/h after ibuprofen treatment, and from 2.8±1.1 to 3.6±1.4 mL/kg/h after indomethacin treatment. The values for ibuprofen are significantly (P<0.05 higher than those for indomethacin. The serum creatinine concentrations ranged from 0.98±0.24 to 1.48±0.2 mg/dL after ibuprofen treatment, and from 1.06±0.24 and 2.03±2.10 mg/dL after indomethacin treatment. The values for ibuprofen are significantly (P<0.05 lower than those for indomethacin. The frequency of oliguria ranged from 1.0% to 9.6% (ibuprofen and from 14.8% to 40.0% (indomethacin, and was significantly lower following ibuprofen than indomethacin administration. In infants with body weight lower than 1,000 g, oliguria appeared in 5% (ibuprofen and 40% (indomethacin; P=0.02. Conclusion: Indomethacin is associated with more severe renal adverse effects than ibuprofen. Ibuprofen is less nephrotoxic than indomethacin and should be used to treat patent ductus arteriosus in preterm infants. Immaturity increases the frequency of adverse effects of indomethacin. Keywords: ibuprofen, indomethacin, patent-ductus-arteriosus, renal-side-effects

  6. Comparison of Analgesic Effects of Novafen and Ibuprofen after Periodontal Surgeries

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    Amirreza Babaloo

    2017-01-01

    Full Text Available Introduction: Management of pain after dental procedures is one of the most important issues for dentists. Non-steroidal antiinflammatory agents, such as ibuprofen, are one of the most commonly used medications to relieve pain. Recently a new medication, Novafen, has been introduced into the Iranian pharmaceutical market, which is a combination of ibuprofen, acetaminophen and caffeine. Considering the importance of management of pain after periodontal surgeries and a paucity of studies in this respect, the present study was undertaken to compare the analgesic efficacy of Novafen and ibuprofen in alleviating pain after periodontal surgeries. Materials and methods: In the present controlled randomized clinical trial, 30 systemically healthy subjects with moderate to severe generalized chronic periodontitis, who were candidates for flap surgeries were evaluated in two groups with 30 areas in each group (two areas in each patient. After the periodontal surgical procedures, the subjects in group 1 received Novafen capsules (containing 325 mg of acetaminophen, 200 mg of ibuprofen and 40 mg of caffeine and the subjects in group 2 received ibuprofen (400 mg. The medications were selected from one pharmaceutical company and the patients only used the medications they received. The severity of pain was determined and compared at 3-minute, 1-hour and 3-hour intervals using VAS and 1, 2 and 3 days postoperatively using VRS. Results: Severity of pain at 30-minute interval in the Novafen group was significantly less than that in the ibuprofen group, with no significant differences at 1- and 3-hour intervals. However, VRS revealed significantly less pain 1, 2 and 3 days postoperatively in the Novafen group compared to the ibuprofen group. Conclusion: Based on the results of the present study, it can be concluded than Novafen can be more effective after periodontal surgeries in alleviating pain. However, its pain control capacity was similar to that of

  7. Maternal use of acetaminophen, ibuprofen, and acetylsalicylic acid during pregnancy and risk of cryptorchidism

    DEFF Research Database (Denmark)

    Jensen, Morten Søndergaard; Rebordosa, Cristina; Thulstrup, Ane Marie

    2010-01-01

    Cyclooxygenase (COX) inhibitors-acetaminophen, ibuprofen and acetylsalicylic acid-have endocrine-disruptive properties in the rainbow trout. In humans, aspirin blocks the androgen response to human chorionic gonadotropin (hCG), and, because hCG-stimulated androgen production in utero is crucial...... for normal testicular descent, exposure to COX inhibitors at vulnerable times during gestation may impair testicular descent. We examined whether prenatal exposure to acetaminophen, ibuprofen, and acetylsalicylic acid was associated with increased occurrence of cryptorchidism....

  8. The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol

    OpenAIRE

    Tanner, Trevor; Aspley, Sue; Munn, Andrew; Thomas, Tracy

    2010-01-01

    Background Ibuprofen and paracetamol differ in their mode of action and related therapeutic effects, suggesting that combined administration may offer improved analgesia. Reported here are the results of two studies on the pharmacokinetic properties of a novel ibuprofen (200 mg) and paracetamol (500 mg) fixed-dose combination tablet. Methods Both studies were open-label, randomised studies in healthy volunteers: Study 1 was a four-way crossover, single-dose study; Study 2 was a two-way cross-...

  9. Ibuprofen Ameliorates Fatigue- and Depressive-like Behavior in Tumor-bearing Mice

    Science.gov (United States)

    Norden, Diana M.; McCarthy, Donna O.; Bicer, Sabahattin; Devine, Raymond; Reiser, Peter J.; Godbout, Jonathan P.; Wold, Loren E.

    2015-01-01

    Aims Cancer-related fatigue (CRF) is often accompanied by depressed mood, both of which reduce functional status and quality of life. Research suggests that increased expression of pro-inflammatory cytokines are associated with skeletal muscle wasting and depressive- and fatigue- like behaviors in rodents and cancer patients. We have previously shown that treatment with ibuprofen, a nonsteroidal anti-inflammatory drug, preserved muscle mass in tumor-bearing mice. Therefore, the purpose of the present study was to determine the behavioral effects of ibuprofen in a mouse model of CRF. Main Methods Mice were injected with colon-26 adenocarcinoma cells and treated with ibuprofen (10mg/kg) in the drinking water. Depressive-like behavior was determined using the forced swim test (FST). Fatigue-like behaviors were determined using voluntary wheel running activity (VWRA) and grip strength. The hippocampus, gastrocnemius muscle, and serum were collected for cytokine analysis. Key Findings Tumor-bearing mice showed depressive-like behavior in the FST, which was not observed in mice treated with ibuprofen. VWRA and grip strength declined in tumor-bearing mice, and ibuprofen attenuated this decline. Tumor-bearing mice had decreased gastrocnemius muscle mass and increased expression of IL-6, MAFBx and MuRF mRNA, biomarkers of protein degradation, in the muscle. Expression of IL-1β and IL-6 was also increased in the hippocampus. Treatment with ibuprofen improved muscle mass and reduced cytokine expression in both the muscle and hippocampus of tumor-bearing mice. Significance Ibuprofen treatment reduced skeletal muscle wasting, inflammation in the brain, and fatigue- and depressive-like behavior in tumor-bearing mice. Therefore, ibuprofen warrants evaluation as an adjuvant treatment for CRF. PMID:26498217

  10. A Randomized Placebo Controlled Trial of Ibuprofen for Respiratory Syncytial Virus Infection in a Bovine Model

    Science.gov (United States)

    Walsh, Paul; Behrens, Nicole; Carvallo Chaigneau, Francisco R.; McEligot, Heather; Agrawal, Karan; Newman, John W.; Anderson, Mark; Gershwin, Laurel J.

    2016-01-01

    Background Respiratory syncytial virus (RSV) is the most common cause of bronchiolitis and hospital admission in infants. An analogous disease occurs in cattle and costs US agriculture a billion dollars a year. RSV causes much of its morbidity indirectly via adverse effects of the host response to the virus. RSV is accompanied by elevated prostaglandin E2 (PGE2) which is followed by neutrophil led inflammation in the lung. Ibuprofen is a prototypical non-steroidal anti-inflammatory drug that decreases PGE2 levels by inhibiting cyclooxygenase. Hypotheses We hypothesized that treatment of RSV with ibuprofen would decrease PGE2 levels, modulate the immune response, decrease clinical illness, and decrease the histopathological lung changes in a bovine model of RSV. We further hypothesized that viral replication would be unaffected. Methods We performed a randomized placebo controlled trial of ibuprofen in 16 outbred Holstein calves that we infected with RSV. We measured clinical scores, cyclooxygenase, lipoxygenase and endocannabinoid products in plasma and mediastinal lymph nodes and interleukin (Il)-4, Il-13, Il-17 and interferon-γ in mediastinal lymph nodes. RSV shedding was measured daily and nasal Il-6, Il-8 and Il-17 every other day. The calves were necropsied on Day 10 post inoculation and histology performed. Results One calf in the ibuprofen group required euthanasia on Day 8 of infection for respiratory distress. Clinical scores (pibuprofen group. Ibuprofen decreased cyclooxygenase, lipoxygenase, and cytochrome P450 products, and increased monoacylglycerols in lung lymph nodes. Ibuprofen modulated the immune response as measured by narrowed range of observed Il-13, Il-17 and IFN-γ gene expression in mediastinal lymph nodes. Lung histology was not different between groups, and viral shedding was increased in calves randomized to ibuprofen. Conclusions Ibuprofen decreased PGE2, modulated the immune response, and improved clinical outcomes. However lung

  11. Phase III study of ibuprofen versus placebo for radiation-induced genitourinary side effects

    International Nuclear Information System (INIS)

    Coleman, C. Norman; Kelly, Laura; Riese Daly, Nancy; Beard, Clair; Kaplan, Irving; Lamb, Carolyn; Propert, Kathleen; Manola, Judith

    2002-01-01

    Purpose: On the basis of our anecdotal clinical observations that nonsteroidal anti-inflammatory agents relieved dysuria during radiotherapy for patients with prostate cancer, we conducted a Phase III randomized trial of ibuprofen vs. placebo for patients who had an increase in acute urinary symptoms. Our in vitro and in vivo laboratory data with a higher concentration of ibuprofen than achievable in this study demonstrated radiosensitization. This study examined whether the inflammatory response within the prostate during radiotherapy would respond to the standard dose of ibuprofen as assessed by a symptom score. Methods and Materials: Patients were registered to the study and were followed weekly with a formal symptom assessment. A double-blind randomization to ibuprofen, 400 mg q.i.d., vs. placebo for 7 days was done at a time when the severity score increased. The symptom response was evaluated at the end of the week. Results: Between 1995 and 1998, 100 patients were entered, 28 did not have a sufficient change in symptom score to be randomized, and 19 were either unable to take ibuprofen or withdrew before randomization. Of the 53 patients randomized, 27 received placebo and 26 ibuprofen. No statistically significant differences were found between the placebo and ibuprofen groups between baseline and randomization or between randomization and the 1-week posttreatment assessment. Neither group had a change in symptom severity between randomization and the 1-week posttreatment evaluation. Conclusion: The standard anti-inflammatory dose of ibuprofen did not relieve the acute urinary or rectal symptoms during radiotherapy for prostate cancer. The nonsteroidal anti-inflammatory drugs are potential radiation sensitizers with the mechanism of action as yet unknown. Clinical trials of the cyclooxygenase inhibitors as radiation sensitizers should explore a range of doses and evaluate potential mechanisms of action, including cyclooxygenase inhibition and other non

  12. Pilot monitoring study of ibuprofen in surface waters of north of Portugal.

    Science.gov (United States)

    Paíga, Paula; Santos, Lúcia H M L M; Amorim, Célia G; Araújo, Alberto N; Montenegro, M Conceição B S M; Pena, Angelina; Delerue-Matos, Cristina

    2013-04-01

    Ibuprofen is amongst the most worldwide consumed pharmaceuticals. The present work presents the first data in the occurrence of ibuprofen in Portuguese surface waters, focusing in the north area of the country, which is one of the most densely populated areas of Portugal. Analysis of ibuprofen is based on pre-concentration of the analyte with solid phase extraction and subsequent determination with liquid chromatography coupled to fluorescence detection. A total of 42 water samples, including surface waters, landfill leachates, Wastewater Treatment Plant (WWTP), and hospital effluents, were analyzed in order to evaluate the occurrence of ibuprofen in the north of Portugal. In general, the highest concentrations were found in the river mouths and in the estuarine zone. The maximum concentrations found were 48,720 ng L(-1) in the landfill leachate, 3,868 ng L(-1) in hospital effluent, 616 ng L(-1) in WWTP effluent, and 723 ng L(-1) in surface waters (Lima river). Environmental risk assessment was evaluated and at the measured concentrations only landfill leachates reveal potential ecotoxicological risk for aquatic organisms. Owing to a high consumption rate of ibuprofen among Portuguese population, as prescribed and non-prescribed medicine, the importance of hospitals, WWTPs, and landfills as sources of entrance of pharmaceuticals in the environment was pointed out. Landfill leachates showed the highest contribution for ibuprofen mass loading into surface waters. On the basis of our findings, more studies are needed as an attempt to assess more vulnerable areas.

  13. Differing disintegration and dissolution rates, pharmacokinetic profiles and gastrointestinal tolerability of over the counter ibuprofen formulations.

    Science.gov (United States)

    Bjarnason, Ingvar; Sancak, Ozgur; Crossley, Anne; Penrose, Andrew; Lanas, Angel

    2018-02-01

    Formulations of over the counter (OTC) NSAIDs differ substantially, but information is lacking on whether this alters their gastrointestinal profiles. To assess disintegration and dissolution rates and pharmacokinetics of four preparations of OTC ibuprofen and relate these with spontaneously reported gastrointestinal adverse events. Disintegration and dissolution rates of ibuprofen tablets as (a) acid, (b) sodium salt, (c) lysine salt, and (d) as a liquid gelatine capsule were assessed. Pharmacokinetic data gastrointestinal and spontaneously reported adverse events arising from global sales were obtained from files from Reckitt Benckiser. Disintegration at low pH was progressively shorter for the preparations from a-to-d with formation of correspondingly smaller ibuprofen crystals, while dissolution was consistently poor. Dissolution at a neutral pH was least rapid for the liquid gelatine capsule. Pharmacokinetic data showed a shorter t max and a higher C max for preparations b-d as compared with ibuprofen acid. Spontaneously reported abdominal symptoms were rare with the liquid gelatine preparation. The formulations of OTC ibuprofen differ in their disintegration and dissolution properties, pharmacokinetic profiles and apparent gastrointestinal tolerability. Spontaneously reported abdominal symptoms were five times lower with the liquid gelatine capsule as compared with ibuprofen acid despite a 30% increase in C max . © 2017 Royal Pharmaceutical Society.

  14. Design of Agglomerated Crystals of Ibuprofen During Crystallization: Influence of Surfactant

    Directory of Open Access Journals (Sweden)

    Maryam Maghsoodi

    2011-01-01

    Full Text Available Objective(sIbuprofen is a problematic drug in tableting, and dissolution due to its poor solubility, hydrophobicity, and tendency to stick to surface. Because of the bad compaction behavior ibuprofen has to be granulated usually before tableting. However, it would be more satisfactory to obtain directly during the crystallization step crystalline particles that can be directly compressed and quickly dissolved. Materials and Methods Crystallization of ibuprofen was carried out using the quasi emulsion solvent diffusion method in presence of surfactant (sodium lauryl sulfate (SLS, Tween 80. The particles were characterized by differential scanning calorimetry (DSC, powder X-ray diffraction (XRPD and were evaluated for particle size, flowability, drug release and tableting behavior. ResultsIbuprofen particles obtained in the presence of surfactants consisted of numerous plate- shaped crystals which had agglomerated together as near spherical shape. The obtained agglomerates exhibited significantly improved micromeritic properties as well as tableting behavior than untreated drug crystals. The agglomerates size and size distribution was largely controlled by surfactant concentration, but there was no significant influence found on the tableting properties. The dissolution tests showed that the agglomerates obtained in presence of SLS exhibited enhanced dissolution rate while the agglomerates made in the presence of Tween 80 had no significant impact on dissolution rate of ibuprofen in comparison to untreated sample. The XRPD and DSC results showed that during the agglomeration process, ibuprofen did not undergo any polymorphic changes.Conclusion The study highlights the influence of surfactants on crystallization process leading to modified performance.

  15. A Transporter of Ibuprofen is Upregulated in MDCK I Cells under Hyperosmotic Culture Conditions

    DEFF Research Database (Denmark)

    Nielsen, Carsten Uhd; Rasmussen, Rune N; Mo, Junying

    2016-01-01

    Ibuprofen is a widely used drug. It has been identified as an inhibitor of several transporters, but it is not clear if ibuprofen is a substrate of any transporter itself. In the present work, we have characterized a transporter of ibuprofen, which is upregulated by hyperosmotic culture conditions...... in Madin-Darby canine kidney I (MDCK I) renal cells. [(3)H]-Ibuprofen uptake rate was measured in MDCK I cell cultured under normal (300 mOsm) and hyperosmotic (500 mOsm) conditions. Hyperosmotic conditions were obtained by supplementing urea, NaCl, mannitol, or raffinose to culture medium. The effect...... of increased osmolarity was investigated for different incubation times. [(3)H]-Ibuprofen uptake in MDCK I cells was upregulated by hyperosmotic culture condition, and was saturable with a Km value of 0.37 ± 0.08 μM and a Vmax of 233.1 ± 17.2 pmol· cm(-2)· min(-1). Racemic [(3)H]-ibuprofen uptake could...

  16. Enhanced longevity by ibuprofen, conserved in multiple species, occurs in yeast through inhibition of tryptophan import.

    Directory of Open Access Journals (Sweden)

    Chong He

    2014-12-01

    Full Text Available The common non-steroidal anti-inflammatory drug ibuprofen has been associated with a reduced risk of some age-related pathologies. However, a general pro-longevity role for ibuprofen and its mechanistic basis remains unclear. Here we show that ibuprofen increased the lifespan of Saccharomyces cerevisiae, Caenorhabditis elegans and Drosophila melanogaster, indicative of conserved eukaryotic longevity effects. Studies in yeast indicate that ibuprofen destabilizes the Tat2p permease and inhibits tryptophan uptake. Loss of Tat2p increased replicative lifespan (RLS, but ibuprofen did not increase RLS when Tat2p was stabilized or in an already long-lived strain background impaired for aromatic amino acid uptake. Concomitant with lifespan extension, ibuprofen moderately reduced cell size at birth, leading to a delay in the G1 phase of the cell cycle. Similar changes in cell cycle progression were evident in a large dataset of replicatively long-lived yeast deletion strains. These results point to fundamental cell cycle signatures linked with longevity, implicate aromatic amino acid import in aging and identify a largely safe drug that extends lifespan across different kingdoms of life.

  17. Enhanced Longevity by Ibuprofen, Conserved in Multiple Species, Occurs in Yeast through Inhibition of Tryptophan Import

    Science.gov (United States)

    He, Chong; Tsuchiyama, Scott K.; Nguyen, Quynh T.; Plyusnina, Ekaterina N.; Terrill, Samuel R.; Sahibzada, Sarah; Patel, Bhumil; Faulkner, Alena R.; Shaposhnikov, Mikhail V.; Tian, Ruilin; Tsuchiya, Mitsuhiro; Kaeberlein, Matt; Moskalev, Alexey A.; Kennedy, Brian K.; Polymenis, Michael

    2014-01-01

    The common non-steroidal anti-inflammatory drug ibuprofen has been associated with a reduced risk of some age-related pathologies. However, a general pro-longevity role for ibuprofen and its mechanistic basis remains unclear. Here we show that ibuprofen increased the lifespan of Saccharomyces cerevisiae, Caenorhabditis elegans and Drosophila melanogaster, indicative of conserved eukaryotic longevity effects. Studies in yeast indicate that ibuprofen destabilizes the Tat2p permease and inhibits tryptophan uptake. Loss of Tat2p increased replicative lifespan (RLS), but ibuprofen did not increase RLS when Tat2p was stabilized or in an already long-lived strain background impaired for aromatic amino acid uptake. Concomitant with lifespan extension, ibuprofen moderately reduced cell size at birth, leading to a delay in the G1 phase of the cell cycle. Similar changes in cell cycle progression were evident in a large dataset of replicatively long-lived yeast deletion strains. These results point to fundamental cell cycle signatures linked with longevity, implicate aromatic amino acid import in aging and identify a largely safe drug that extends lifespan across different kingdoms of life. PMID:25521617

  18. Ibuprofen 400 mg is effective in women, and women are well represented in trials

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    Moore R Andrew

    2002-11-01

    Full Text Available Abstract Background A recent article in the New Scientist argued that women were under-represented in clinical trials which, until now, had masked the finding that ibuprofen 400 mg was ineffective in women. Methods Meta-analysis of randomised, double-blind placebo-controlled trials of ibuprofen 400 mg in acute pain, and use of individual patient information were planned to test the hypothesis that ibuprofen is ineffective in women. For each trial the proportion of women participating, the number of patients with at least 50% pain relief and the overall event rate for ibuprofen 400 mg and placebo was calculated. For each patient percentage pain relief was calculated, and the numbers of women and men achieving at least 50% pain relief used to calculate number-needed-to-treat (NNT for ibuprofen 400 mg compared to placebo. Results Thirty-seven included trials had 3,577 patients, 67% of whom were women. The proportion with at least 50% pain relief was unaffected by how many women were included. In an analysis of 678 individual patients the proportion of women and men with at least 50% pain relief was the same, NNT 3.4 (2.6 to 4.6 and 2.5 (2.0 to 3.3 respectively. Conclusion There is no clinically meaningful difference in the efficacy of ibuprofen 400 mg between men and women experiencing moderate to severe postoperative pain and women were well represented.

  19. Mucoadhesive microemulsion of ibuprofen: design and evaluation for brain targeting efficiency through intranasal route

    Directory of Open Access Journals (Sweden)

    Surjyanarayan Mandal

    2015-09-01

    Full Text Available This study aimed at designing mucoadhesive microemulsion gel to enhance the brain uptake of Ibuprofen through intranasal route. Ibuprofen loaded mucoadhesive microemulsion (MMEI was developed by incorporating polycarbophil as mucoadhesive polymer into Capmul MCM based optimal microemulsion (MEI and was subjected to characterization, stability, mucoadhesion and naso-ciliotoxicity study. Brain uptake of ibuprofen via nasal route was studied by performing biodistribution study in Swiss albino rats. MEI was found to be transparent, stable and non ciliotoxic with 66.29 ± 4.15 nm, -20.9 ± 3.98 mV and 98.66 ± 1.01% as average globule size, zeta potential and drug content respectively. Transmission Electron Microscopy (TEM study revealed the narrow globule size distribution of MEI. Following single intranasal administration of MMEI and MEI at a dose of 2.86 mg/kg, uptake of ibuprofen in the olfactory bulb was around 3.0 and 1.7 folds compared with intravenous injection of ibuprofen solution (IDS. The ratios of AUC in brain tissues to that in plasma obtained after nasal administration of MMEI were significantly higher than those after intravenous administration of IDS. Findings of the present investigation revealed that the developed mucoadhesive microemulsion gel could be a promising approach for brain targeting of ibuprofen through intranasal route.

  20. Evaluation of a Non-aqueous Ibuprofen-Phospholipid Complex Formulation in Rats.

    Science.gov (United States)

    Li, Chunhua; Xu, Songlin; Liu, Zhidong; Ding, Lingling; Zhao, Xiaobin; Lee, Robert J

    2016-01-01

    In the present study, a non-aqueous ibuprofen-phospholipid complex was developed to reduce the gastrointestinal (GI) toxicity of ibuprofen. A non-aqueous ibuprofen-phospholipid complex (IBU-PC) was prepared by mixing phosal-35SB and ibuprofen. In vitro release behavior was studied using a dissolution apparatus. Irritation to gastrointestinal (GI) tract and pharmacokinetics of IBU-PC were studied in rats. Rapid release of drug occurred with approximately 85% of ibuprofen released from the composition within the first 30 min. The GI injury in IBU-PC-treated rats was minimal compared to those of Advil Liqui-gels-treated group. There was no significant difference between IBU-PC and Motrin-treated groups. The area under the concentration-time curve (AUC0~24) of IBU-PC and Motrin were 366±115 and 391±105 μg/h/ml, respectively. The relative bioavailability of IBU-PC was 94.2%. IBU-PC can decrease GI adverse reaction induced by ibuprofen. Copyright © 2016 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.

  1. Gastroprotective effects of several H2RAs on ibuprofen-induced gastric ulcer in rats.

    Science.gov (United States)

    Liu, Jing; Sun, Dan; He, Jinfeng; Yang, Chengli; Hu, Tingting; Zhang, Lijing; Cao, Hua; Tong, Ai-Ping; Song, Xiangrong; Xie, Yongmei; He, Gu; Guo, Gang; Luo, Youfu; Cheng, Ping; Zheng, Yu

    2016-03-15

    Ibuprofen is the first line of treatment for osteoarthritis and arthritis. The main side effects of ibuprofen especially in long-term treatment include gastric ulcer, duodenal ulcer and indigestion etc. Therefore, screening drugs with effective gastric protective effects and low toxicity for combination therapy with ibuprofen is necessary. The mechanism of gastric damage induced by ibuprofen is still unclear, however, cell damage caused by reactive oxygen species (ROS) is considered as the main reason. Preliminary screening of literature with the criteria of low toxicity led to four histamine-2 receptor antagonists (H2RAs): nizatidine, famotidine, lafutidine, and roxatidine acetate, which were selected for further investigation. These drugs were evaluated systemically by examining the gastric ulcer index, lipid peroxidation (LPO), membrane permeability, toxicity to main organs, and the influence on the activity of antioxidant enzymes, and myeloperoxidase (MPO). Nizatidine was found to be the best gastric protective agent. It exhibited excellent protective effect by increasing antioxidant enzyme activity, decreasing MPO activity, reducing LPO, and membrane permeability. Combination treatment with nizatidine and ibuprofen did not show any significant toxicity. Nizatidine was considered as a good option for combination therapy with ibuprofen especially for diseases that require long-term treatment such as arthritis and osteoarthritis. Copyright © 2016 Elsevier Inc. All rights reserved.

  2. Repurposing of Aspirin and Ibuprofen as Candidate Anti-Cryptococcus Drugs

    Science.gov (United States)

    Ogundeji, Adepemi O.; Pohl, Carolina H.

    2016-01-01

    The usage of fluconazole and amphotericin B in clinical settings is often limited by, among other things, drug resistance development and undesired side effects. Thus, there is a constant need to find new drugs to better manage fungal infections. Toward this end, the study described in this paper considered the repurposing of aspirin (acetylsalicylic acid) and ibuprofen as alternative drugs to control the growth of cryptococcal cells. In vitro susceptibility tests, including a checkerboard assay, were performed to assess the response of Cryptococcus neoformans and Cryptococcus gattii to the above-mentioned anti-inflammatory drugs. Next, the capacity of these two drugs to induce stress as well as their mode of action in the killing of cryptococcal cells was determined. The studied fungal strains revealed a response to both aspirin and ibuprofen that was dose dependent, with ibuprofen exerting greater antimicrobial action. More importantly, the MICs of these drugs did not negatively (i) affect growth or (ii) impair the functioning of macrophages; rather, they enhanced the ability of these immune cells to phagocytose cryptococcal cells. Ibuprofen was also shown to act in synergy with fluconazole and amphotericin B. The treatment of cryptococcal cells with aspirin or ibuprofen led to stress induction via activation of the high-osmolarity glycerol (HOG) pathway, and cell death was eventually achieved through reactive oxygen species (ROS)-mediated membrane damage. The presented data highlight the potential clinical application of aspirin and ibuprofen as candidate anti-Cryptococcus drugs. PMID:27246782

  3. Male homosexuality and spirit possession in Brazil.

    Science.gov (United States)

    Fry, P

    1985-01-01

    This paper examines the relationship between male homosexuality and the Afro-Brazilian possession cults in Belém do Parà. After a discussion of the literature follows a description of the cults' beliefs, rites and social organization. Male sex roles are then discussed and the two categories, bicha and man, analyzed. It is noted that there is no term which is equivalent to the western category of "homosexual" in this taxonomic system. After putting forward folk explanations for the presence of many bichas in the cults, an analysis is put forward of the social rewards available to bichas within these cults, and the structural relationship between homosexuality and these regions in terms of their congruent marginality vis-à-vis "normal society."

  4. Predicative possession in Medieval Slavic Bible translations Predicative Possession in Early Biblical Slavic

    Directory of Open Access Journals (Sweden)

    Julia McAnallen

    2011-08-01

    Full Text Available Late Proto-Slavic (LPS had an inventory of three constructions for expressing predicative possession. Using the earliest Slavic Bible translations from Old Church Slavic (OCS, and to a lesser degree Old Czech, a number of conclusions can be drawn about the status of predicative possession for LPS. The verb iměti ‘have’ was the most frequent and least syntactically and semantically restricted predicative possessive construction (PPC. Existential PPCs with a dative possessor appear primarily with kinship relations, abstract possessums, and in a number of other fixed construction types; existential PPCs with the possessor in an u + genitive prepositional phrase primarily appear with concrete and countable possessums. Both existential PPCs call for an animate, most often pronominal, possessor. The u + genitive was the rarest type of PPC in LPS, though it had undoubtedly grammaticalized as a PPC.

  5. 50 CFR 20.38 - Possession of live birds.

    Science.gov (United States)

    2010-10-01

    ... 50 Wildlife and Fisheries 6 2010-10-01 2010-10-01 false Possession of live birds. 20.38 Section 20... WILDLIFE AND PLANTS (CONTINUED) MIGRATORY BIRD HUNTING Possession § 20.38 Possession of live birds. Every migratory game bird wounded by hunting and reduced to possession by the hunter shall be immediately killed...

  6. Pharmacokinetics of acetaminophen and ibuprofen when coadministered with telmisartan in healthy volunteers.

    Science.gov (United States)

    Stangier, J; Su, C A; Fraunhofer, A; Tetzloff, W

    2000-12-01

    Two open-label, two-way, crossover studies were performed to assess any pharmacokinetic interaction of telmisartan with either acetaminophen or ibuprofen. Healthy male adult volunteers (n = 12) received a single oral dose of acetaminophen 1 g alone and with oral telmisartan 120 mg in one study. Oral ibuprofen 400 mg three times daily with and without oral once-daily telmisartan 120 mg was given for 7 days in the other study conducted in 6 males and 6 females. In both studies, there was a washout period of > or = 13 days between single and combination medication administration. The primary end points Cmax and AUC were compared between combination (acetaminophen or ibuprofen + telmisartan) and single-agent medication (acetaminophen or ibuprofen). Pharmacokinetic drug interaction was assessed by analysis of variance (ANOVA) and calculation of 90% confidence intervals (CI) for treatment ratios using log-transformed parameters. Bioequivalence (i.e., lack of interaction) was concluded if the 90% CI of the ratios for both Cmax and AUC were within the acceptance limit of 0.80 to 1.25. Geometric mean Cmax values for acetaminophen and R-(-)- and S-(+)-ibuprofen enantiomers were similar with and without telmisartan coadministration (12.6 micrograms/mL vs. 14.1 micrograms/mL; 17.3 micrograms/mL vs. 16.7 micrograms/mL; 19.4 micrograms/mL vs. 19.5 micrograms/mL, respectively), and values for R-(-)- as well as S-(+)-ibuprofen were bioequivalent. Geometric mean AUC values for acetaminophen and R-(-)- and S-(+)-ibuprofen were also bioequivalent with and without telmisartan. The distribution and elimination parameters of both acetaminophen and ibuprofen were comparable in the presence or absence of telmisartan. The concomitant and single-agent medications were all well tolerated. In conclusion, the long half-life and excellent safety profile of telmisartan were unaffected by concurrent acetaminophen or ibuprofen medication; thus, once-daily dosing of telmisartan can be maintained

  7. Compatibility of intravenous ibuprofen with lipids and parenteral nutrition, for use as a continuous infusion.

    Science.gov (United States)

    Garcia, Jowell; Garg, Alka; Song, Yunmei; Fotios, Ambados; Andersen, Chad; Garg, Sanjay

    2018-01-01

    There is increasing interest to administer ibuprofen as a continuous infusion instead of a traditional bolus for treating Patent Ductus Arteriosus (PDA). However, its compatibility data with commonly used drugs in the neonatal period, including parenteral nutrition (PN) and lipids is unavailable. The aim is to determine the compatibility of intravenous ibuprofen lysine with various ANZNN parenteral nutrition consensus group standard neonatal PN formulations and lipids. The PN and lipid solutions used in a tertiary neonatal unit were obtained. These included a Starter, Standard Preterm and low carbohydrate PN, and IV SMOF lipid admixture (SMOFLipid 20% 15 mL; Vitalipid N infant 4 mL, Soluvit N 1 mL) plus vitamin mixtures. 10% glucose was used as a control. 1:1 mixtures of different concentrations (1.25 to 5mg/mL) of ibuprofen lysine and each of the PN/glucose/lipid formulations were made. Samples were taken at hourly intervals for a total of 4 hours and tested for both physical (visual assessment, pH and microscopy) and chemical compatibility (High Performance Liquid Chromatography analysis). Zeta potential and particle diameter were measured for SMOF lipid admixture and ibuprofen combination to assess emulsion stability. 24 hour stability of ibuprofen dilution in 5 mL BD Luer-lok polypropylene syringes at 25°C was also assessed. Most PN formed opaque solutions when mixed with ibuprofen 2.5 and 5mg/mL solutions. However, ibuprofen dilution of 1.25mg/mL produced clear, colourless solutions with no microscopic particles when mixed with all PN/glucose/lipid formulations tested. Ibuprofen was chemically stable with all PN and SMOF lipid admixture, for a period of 4 hours. The zeta potential and particle diameter were within acceptable limits. Ibuprofen lysine was stable over 24 hours in Luer-lok polypropylene syringes. Ibuprofen 1.25mg/mL is physically and chemically compatible with 10% glucose, starter PN, standard preterm and low carbohydrate PN, and SMOF lipid

  8. Efficacy and safety of rectal ibuprofen for patent ductus arteriosus closure in very low birth weight preterm infants.

    Science.gov (United States)

    Demir, Nihat; Peker, Erdal; Ece, İbrahim; Balahoroğlu, Ragıp; Tuncer, Oğuz

    2017-09-01

    To compare rectal ibuprofen with oral ibuprofen for the closure of hemodynamically significant patent ductus arteriosus (hsPDA) in very low birth weight (VLBW) preterm infants. In a prospective, randomized study, 72 VLBW infants who had hsPDA received either rectal or oral ibuprofen. The plasma concentration of ibuprofen and renal functions were determined in both groups by the high-performance liquid chromatography (HPLC) method and cystatin-C (cys-C), respectively. The hsPDA closure rate of the group that received rectal ibuprofen was similar to oral ibuprofen (86.1% versus 83.3%) after the first course of the treatment (p = 0.745). A statistically significant difference was identified between the mean plasma cys-C levels before and after treatment in both the rectal and oral ibuprofen groups (p = 0.004 and p 0.05 for all values). Rectal ibuprofen is as effective as oral ibuprofen for hsPDA closure in VLBW infants. The rise in the cys-C level with rectal and oral treatment shows that patients with borderline renal function should be evaluated and followed closely.

  9. Ibuprofen analysis in blood samples by palladium particles-impregnated sodium montmorillonite electrodes: Validation using high performance liquid chromatography.

    Science.gov (United States)

    Loudiki, A; Boumya, W; Hammani, H; Nasrellah, H; El Bouabi, Y; Zeroual, M; Farahi, A; Lahrich, S; Hnini, K; Achak, M; Bakasse, M; El Mhammedi, M A

    2016-12-01

    The electrochemical detection of ibuprofen has been studied on Palladium-Montmorillonite (Mt) modified carbon paste electrode using differential pulse voltammetry. The optimization of the modifier preparation and the instrumental parameters was investigated. The results indicate that ibuprofen oxidation was favored in the presence of Pd-PdO particles. The quantitative determination of ibuprofen was statistically analyzed and validated using HPLC method. The detection and quantification limits, specificity and precision were found to be acceptable. Finally, the developed method was successfully applied for ibuprofen determination in human blood samples. Copyright © 2016 Elsevier B.V. All rights reserved.

  10. Preemptive Analgesia with Ibuprofen and Acetaminophen in Pediatric Lower Abdominal Surgery

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    P Kashefi

    2005-07-01

    Full Text Available Background: Postoperative pain is a significant problem in pediatrics. Preemptive administration of analgesics has recently emerged as a method to enhance pain management associated with surgery. The objective of this study was to compare the analgesic efficacy of a single-dose of preoperative oral ibuprofen versus acetaminophen in preventing pain after lower abdominal surgery in pediatrics. Methods: In this randomized, double-blind study, following lower abdominal surgery, 75 children, aging 3 to 12 years, were assigned to receive either ibuprofen 20 mg /kg (n=25 or acetaminophen 35 mg/kg (n=25 or placebo (n=25 2 hours before surgery. Agitation in recovery was measured and postoperative pain was quantified 3 and 24 hours after surgery by Oucher’s scale. The amount of postoperative analgesic needed in the ward was also assessed. Results: It was found that preoperative administration of ibuprofen and acetaminophen can reduce agitation in recovery but there was no difference in the agitation score between ibuprofen and acetaminophen groups (P=0.145. Agitation score was significantly lower in ibuprofen group compared to placebo (P>0.005. Similarly, patients in the acetaminophen group were considerably less agitated than those in the placebo group (P=0.002. No significant difference was observed in pain intensity 3 and 24 hours after operation between the three groups [(P=0.495 and (P=0.582 respectively]. The amount of postoperative analgesic needed during ward hospitalization was not significantly different among the three groups (P>0.005. Conclusion: These results provide evidence that preemptive acetaminophen and ibuprofen may reduce agitation during recovery but they neither improve the postoperative pain nor reduce analgesics consumption in ward Key words: Postoperative analgesia, Acetaminophen, Ibuprofen, Preemptive analgesia

  11. Effects of Ibuprofen on the physiology and outcome of rabbit endotoxic shock

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    Canbaz Mukaddes

    2002-10-01

    Full Text Available Abstract Background Despite major developments in the management of septic shock, the mortality rate had progressively increased. Ibuprofen has been shown to have beneficial physiological effects when used as a treatment. However, there are conflicting results with respect to survival. This study aims to investigate the effect of ibuprofen on vital functions, various physiological parameters and survival during endotoxic shock in rabbits. Methods Twenty-eight New Zealand rabbits were randomly separated into four groups. The first group received only saline, the second was given 2 mg/kg intravenous endotoxin at t0, the third received 30 mg/kg ibuprofen 30 minutes after endotoxin administration, whilst the fourth group received ibuprofen 30 minutes before the endotoxin. Respiratory and heart rate, mean arterial blood pressure and rectal temperature were recorded. Complete blood counts were performed and thromboxane B2 was measured every 30 minutes for the first two hours, and then hourly over the course of the experiment. Urine samples were collected at the same time points for the measurement of prostaglandin E2. Results Ibuprofen was found to improve respiratory rate, heart rate, and arterial pressure. However, it did not improve the negative effects of endotoxin on body temperature, haematocrit values, white blood cell count, and thrombocyte number. Thromboxane B2 levels in group IV were significantly lower than in the other groups, and the increase started at a later timepoint. In ibuprofen-treated animals, Prostaglandin E2 levels stayed low for at least 90 minutes, but started to rise thereafter. While the average survival in Group II animals was 192.9 ± 46.9 minutes, those of groups III and IV were 339.1 ± 33.5 minutes (p Conclusions Ibuprofen appears to increase survival in endotoxic shock-induced animals. Therefore, it may be helpful for the prophylaxis and treatment of patients with, or who are likely to develop, septic shock.

  12. Overview review: Comparative efficacy of oral ibuprofen and paracetamol (acetaminophen) across acute and chronic pain conditions.

    Science.gov (United States)

    Moore, R A; Derry, S; Wiffen, P J; Straube, S; Aldington, D J

    2015-10-01

    Ibuprofen and paracetamol have long been used as analgesics in a range of acute, intermittent and chronic pain conditions. Paracetamol is often the first line analgesic recommended, without consensus about which is the better analgesic. An overview review of systematic reviews and meta-analyses directly compares ibuprofen and paracetamol at standard doses in particular painful conditions, or uses indirect comparisons against placebo. Electronic searches for systematic reviews were sought published since 1995 using outcomes approximating to ≥50% pain intensity reduction. Painful conditions were acute post-operative pain, dysmenorrhoea, tension-type headache (TTH), migraine, osteoarthritis and rheumatoid arthritis, back pain, cancer and paediatric pain. There was no systematic assessment of harm. Sixteen systematic reviews and four individual patient data meta-analyses were included. Ibuprofen was consistently superior to paracetamol at conventional doses in a range of painful conditions. Two direct comparisons favoured ibuprofen (acute pain, osteoarthritis). Three of four indirect comparisons favoured ibuprofen (acute pain, migraine, osteoarthritis); one showed no difference (TTH), although there were methodological problems. In five pain conditions (dysmenorrhoea, paediatric pain, cancer pain, back pain and rheumatoid arthritis), there were limited data on paracetamol and ibuprofen. At standard doses in different painful conditions, ibuprofen was usually superior producing more patients with the degree of pain relief that patients feel worthwhile. Neither of the drugs will be effective for everyone, and both are needed. This overview questions the practice of routinely using paracetamol as a first line analgesic because there is no good evidence for efficacy of paracetamol in many pain conditions. © 2014 The Authors. European Journal of Pain published by John Wiley & Sons Ltd on behalf of European Pain Federation - EFICC®.

  13. Ibuprofen-induced patent ductus arteriosus closure: physiologic, histologic, and biochemical effects on the premature lung.

    Science.gov (United States)

    McCurnin, Donald; Seidner, Steven; Chang, Ling-Yi; Waleh, Nahid; Ikegami, Machiko; Petershack, Jean; Yoder, Brad; Giavedoni, Luis; Albertine, Kurt H; Dahl, Mar Janna; Wang, Zheng-ming; Clyman, Ronald I

    2008-05-01

    The goal was to study the pulmonary, biochemical, and morphologic effects of a persistent patent ductus arteriosus in a preterm baboon model of bronchopulmonary dysplasia. Preterm baboons (treated prenatally with glucocorticoids) were delivered at 125 days of gestation (term: 185 days), given surfactant, and ventilated for 14 days. Twenty-four hours after birth, newborns were randomly assigned to receive either ibuprofen (to close the patent ductus arteriosus; n = 8) or no drug (control; n = 13). After treatment was started, the ibuprofen group had significantly lower pulmonary/systemic flow ratio, higher systemic blood pressure, and lower left ventricular end diastolic diameter, compared with the control group. There were no differences in cardiac performance indices between the groups. Ventilation index and dynamic compliance were significantly improved with ibuprofen. The improved pulmonary mechanics in ibuprofen-treated newborns were not attributable to changes in levels of surfactant protein B, C, or D, saturated phosphatidylcholine, or surfactant inhibitory proteins. There were no differences in tracheal concentrations of cytokines commonly associated with the development of bronchopulmonary dysplasia. The groups had similar messenger RNA expression of genes that regulate inflammation and remodeling in the lung. Lungs from ibuprofen-treated newborns were significantly drier (lower wet/dry ratio) and expressed 2.5 times more epithelial sodium channel protein than did control lungs. By 14 days after delivery, control newborns had morphologic features of arrested alveolar development (decreased alveolar surface area and complexity), compared with age-matched fetuses. In contrast, there was no evidence of alveolar arrest in the ibuprofen-treated newborns. Ibuprofen-induced patent ductus arteriosus closure improved pulmonary mechanics, decreased total lung water, increased epithelial sodium channel expression, and decreased the detrimental effects of preterm birth

  14. An integrated safety analysis of intravenous ibuprofen (Caldolor® in adults

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    Southworth SR

    2015-10-01

    Full Text Available Stephen R Southworth,1 Emily J Woodward,2 Alex Peng,2 Amy D Rock21North Mississippi Sports Medicine and Orthopaedic Clinic, PLLC, Tupelo, MS, 2Department of Research and Development, Cumberland Pharmaceuticals Inc., Nashville, TN, USAAbstract: Intravenous (IV nonsteroidal anti-inflammatory drugs such as IV ibuprofen are increasingly used as a component of multimodal pain management in the inpatient and outpatient settings. The safety of IV ibuprofen as assessed in ten sponsored clinical studies is presented in this analysis. Overall, 1,752 adult patients have been included in safety and efficacy trials over 11 years; 1,220 of these patients have received IV ibuprofen and 532 received either placebo or comparator medication. The incidence of adverse events (AEs, serious AEs, and changes in vital signs and clinically significant laboratory parameters have been summarized and compared to patients receiving placebo or active comparator drug. Overall, IV ibuprofen has been well tolerated by hospitalized and outpatient patients when administered both prior to surgery and postoperatively as well as for nonsurgical pain or fever. The overall incidence of AEs is lower in patients receiving IV ibuprofen as compared to those receiving placebo in this integrated analysis. Specific analysis of hematological and renal effects showed no increased risk for patients receiving IV ibuprofen. A subset analysis of elderly patients suggests that no dose adjustment is needed in this higher risk population. This integrated safety analysis demonstrates that IV ibuprofen can be safely administered prior to surgery and continued in the postoperative period as a component of multimodal pain management.Keywords: NSAID, surgical pain, fever, perioperative analgesia, critical care, multimodal pain management

  15. The Use of Ibuprofen in Posttonsillectomy Analgesia and Its Effect on Posttonsillectomy Hemorrhage Rate.

    Science.gov (United States)

    Pfaff, Julia A; Hsu, Kevin; Chennupati, Sri Kiran

    2016-09-01

    To determine the effect of ibuprofen on posttonsillectomy bleeding when compared with codeine in posttonsillectomy analgesia. Case series with chart review. Tertiary care children's hospital, Philadelphia, Pennsylvania. On July 1, 2012, our institution transitioned from acetaminophen with codeine to ibuprofen for posttonsillectomy analgesia. Pediatric patients (0-18 years old) who underwent surgery from July 1, 2010, to June 30, 2012, were placed in the codeine cohort, and those who underwent surgery from July 1, 2012, to June 30, 2014, were placed in the ibuprofen cohort. A total of 6014 patients underwent tonsillectomy between July 1, 2010, and June 30, 2014, and 211 patients presented for posttonsillectomy hemorrhage during the same period. The incidence of readmission for posttonsillectomy hemorrhage was 3.4% and 3.6% (P = .63; odds ratio [OR] = 1.07; 95% confidence interval [95% CI]: 0.811-1.410) for the codeine and ibuprofen groups, respectively, and the incidence of second operation for control of posttonsillectomy bleeding for the codeine and ibuprofen groups was 1.9% and 2.2% (P = .54; OR = 1.117; 95% CI: 0.781-1.600), respectively. Patients aged 11 to 18 years demonstrated a higher incidence of posttonsillectomy bleeding events overall. When age is controlled, multivariate logistic regression demonstrated no statistically significant increase in posttonsillectomy bleeding events among pediatric patients treated with ibuprofen versus patients treated with codeine (readmission: P = .617; OR = 0.932; 95% CI: 0.707-1.228; reoperation: P = .513; OR = 0.887; 95% CI: 0.618-1.272). Age is an independent risk factor for posttonsillectomy bleeding. When age is controlled, there is no statistically significant increase in the incidence of posttonsillectomy bleeding events among patients treated with ibuprofen when compared to patients treated with codeine. © American Academy of Otolaryngology—Head and Neck Surgery Foundation 2016.

  16. Effects of ibuprofen on cognition and NMDA receptor subunit expression across aging.

    Science.gov (United States)

    Márquez Loza, Alejandra; Elias, Valerie; Wong, Carmen P; Ho, Emily; Bermudez, Michelle; Magnusson, Kathy R

    2017-03-06

    Age-related declines in long- and short-term memory show relationships to decreases in N-methyl-d-aspartate (NMDA) receptor expression, which may involve inflammation. This study was designed to determine effects of an anti-inflammatory drug, ibuprofen, on cognitive function and NMDA receptor expression across aging. Male C57BL/6 mice (ages 5, 14, 20, and 26months) were fed ibuprofen (375ppm) in NIH31 diet or diet alone for 6weeks prior to testing. Behavioral testing using the Morris water maze showed that older mice performed significantly worse than younger in spatial long-term memory, reversal, and short-term memory tasks. Ibuprofen enhanced overall performance in the short-term memory task, but this appeared to be more related to improved executive function than memory. Ibuprofen induced significant decreases over all ages in the mRNA densities for GluN2B subunit, all GluN1 splice variants, and GluN1-1 splice forms in the frontal cortex and in protein expression of GluN2A, GluN2B and GluN1 C2' cassettes in the hippocampus. GluN1-3 splice form mRNA and C2' cassette protein were significantly increased across ages in frontal lobes of ibuprofen-treated mice. Ibuprofen did not alter expression of pro-inflammatory cytokines IL-1β and TNFα, but did reduce the area of reactive astrocyte immunostaining in frontal cortex of aged mice. Enhancement in executive function showed a relationship to increased GluN1-3 mRNA and decreased gliosis. These findings suggest that inflammation may play a role in executive function declines in aged animals, but other effects of ibuprofen on NMDA receptors appeared to be unrelated to aging or inflammation. Copyright © 2016 IBRO. Published by Elsevier Ltd. All rights reserved.

  17. 22 CFR 72.14 - Nominal possession; property not normally taken into physical possession.

    Science.gov (United States)

    2010-04-01

    ... possession. (a) When a consular officer take articles of a decedent's personal property from a foreign... Department discharging the consular officer of any responsibility for the articles transferred. (b) A... effects; (2) Motor vehicles, airplanes or watercraft; (3) Toiletries, such as toothpaste or razors; (4...

  18. Ibuprofen arginate retains eNOS substrate activity and reverses endothelial dysfunction: implications for the COX-2/ADMA axis.

    Science.gov (United States)

    Kirkby, Nicholas S; Tesfai, Abel; Ahmetaj-Shala, Blerina; Gashaw, Hime H; Sampaio, Walkyria; Etelvino, Gisele; Leão, Nádia Miricéia; Santos, Robson A; Mitchell, Jane A

    2016-12-01

    Nonsteroidal antiinflammatory drugs, including ibuprofen, are among the most commonly used medications and produce their antiinflammatory effects by blocking cyclooxygenase (COX)-2. Their use is associated with increased risk of heart attacks caused by blocking COX-2 in the vasculature and/or kidney, with our recent work implicating the endogenous NOS inhibitor asymmetric dimethylarginine (ADMA), a cardiotoxic hormone whose effects can be prevented by l-arginine. The ibuprofen salt ibuprofen arginate (Spididol) was created to increase solubility but we suggest that it could also augment the NO pathway through codelivery of arginine. Here we investigated the idea that ibuprofen arginate can act to simultaneously inhibit COX-2 and preserve the NO pathway. Ibuprofen arginate functioned similarly to ibuprofen sodium for inhibition of mouse/human COX-2, but only ibuprofen arginate served as a substrate for NOS. Ibuprofen arginate but not ibuprofen sodium also reversed the inhibitory effects of ADMA and N G -nitro-l-arginine methyl ester on inducible NOS (macrophages) and endothelial NOS in vitro (aorta) and in vivo (blood pressure). These observations show that ibuprofen arginate provides, in one preparation, a COX-2 inhibitor and NOS substrate that could act to negate the harmful cardiovascular consequences mediated by blocking renal COX-2 and increased ADMA. While remarkably simple, our findings are potentially game-changing in the nonsteroidal antiinflammatory drug arena.-Kirkby, N. S., Tesfai, A., Ahmetaj-Shala, B., Gashaw, H. H., Sampaio, W., Etelvino, G., Leão, N. M., Santos, R. A., Mitchell, J. A. Ibuprofen arginate retains eNOS substrate activity and reverses endothelial dysfunction: implications for the COX-2/ADMA axis. © The Author(s).

  19. Ibuprofen prevents synthetic smoke-induced pulmonary edema

    Energy Technology Data Exchange (ETDEWEB)

    Shinozawa, Y.; Hales, C.; Jung, W.; Burke, J.

    1986-12-01

    Multiple potentially injurious agents are present in smoke but the importance of each of these agents in producing lung injury as well as the mechanisms by which the lung injury is produced are unknown. In order to study smoke inhalation injury, we developed a synthetic smoke composed of a carrier of hot carbon particles of known size to which a single known common toxic agent in smoke, in this case HCI, could be added. We then exposed rats to the smoke, assayed their blood for the metabolites of thromboxane and prostacyclin, and intervened shortly after smoke with the cyclooxygenase inhibitors indomethacin or ibuprofen to see if the resulting lung injury could be prevented. Smoke exposure produced mild pulmonary edema after 6 h with a wet-to-dry weight ratio of 5.6 +/- 0.2 SEM (n = 11) compared with the non-smoke-exposed control animals with a wet-to-dry weight ratio of 4.3 +/- 0.2 (n = 12), p less than 0.001. Thromboxane B, and 6-keto-prostaglandin F1 alpha rose to 1660 +/- 250 pg/ml (p less than 0.01) and to 600 +/- 100 pg/ml (p greater than 0.1), respectively, in the smoke-injured animals compared with 770 +/- 150 pg/ml and 400 +/- 100 pg/ml in the non-smoke-exposed control animals. Indomethacin (n = 11) blocked the increase in both thromboxane and prostacyclin metabolites but failed to prevent lung edema.

  20. Ibuprofen delivered by poly(lactic-co-glycolic acid) (PLGA) nanoparticles to human gastric cancer cells exerts antiproliferative activity at very low concentrations

    Science.gov (United States)

    Bonelli, Patrizia; Tuccillo, Franca M; Federico, Antonella; Napolitano, Maria; Borrelli, Antonella; Melisi, Daniela; Rimoli, Maria G; Palaia, Raffaele; Arra, Claudio; Carinci, Francesco

    2012-01-01

    Purpose Epidemiological, clinical, and laboratory studies have suggested that ibuprofen, a commonly used nonsteroidal anti-inflammatory drug, inhibits the promotion and proliferation of certain tumors. Recently, we demonstrated the antiproliferative effects of ibuprofen on the human gastric cancer cell line MKN-45. However, high doses of ibuprofen were required to elicit these antiproliferative effects in vitro. The present research compared the antiproliferative effects of ibuprofen delivered freely and released by poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) in MKN-45 cells. Methods MKN-45 human gastric adenocarcinoma cells were treated with ibuprofen-loaded PLGA NPs. The proliferation of MKN-45 cells was then assessed by cell counting. The uptake of NPs was imaged by fluorescence microscopy and flow cytometry. The release of ibuprofen from ibuprofen-loaded PLGA NPs in the cells was evaluated by gas chromatography–mass spectrometry. Results Dramatic inhibition of cellular proliferation was observed in cells treated with ibuprofen-loaded PLGA NPs versus those treated with free ibuprofen at the same concentration. The localization of NPs was cytoplasmic. The initiation of ibuprofen release was rapid, commencing within 2 hours, and then increased slowly over time, reaching a maximum concentration at 24 hours. The inhibition of proliferation was confirmed to be due to the intracellular release of ibuprofen from the NPs. Using PLGA NPs as carriers, ibuprofen exerted an antiproliferative activity at concentrations > 100 times less than free ibuprofen, suggesting greater efficiency and less cellular toxicity. In addition, when carried by PLGA NPs, ibuprofen more quickly induced the expression of transcripts involved in proliferation and invasiveness processes. Conclusion Ibuprofen exerted an antiproliferative effect on MKN-45 cells at low concentrations. This effect was achieved using PLGA NPs as carriers of low doses of ibuprofen. PMID:23180963

  1. Effects of Humidity and Surfaces on the Melt Crystallization of Ibuprofen

    Directory of Open Access Journals (Sweden)

    Il Won Kim

    2012-08-01

    Full Text Available Melt crystallization of ibuprofen was studied to understand the effects of humidity and surfaces. The molecular self-assembly during the amorphous-to-crystal transformation was examined in terms of the nucleation and growth of the crystals. The crystallization was on Al, Au, and self-assembled monolayers with –CH3, –OH, and –COOH functional groups. Effects of the humidity were studied at room temperature (18–20 °C with relative humidity 33%, 75%, and 100%. Effects of the surfaces were observed at −20 °C (relative humidity 36% to enable close monitoring with slower crystal growth. The nucleation time of ibuprofen was faster at high humidity conditions probably due to the local formation of the unfavorable ibuprofen melt/water interface. The crystal morphologies of ibuprofen were governed by the nature of the surfaces, and they could be associated with the growth kinetics by the Avrami equation. The current study demonstrated the effective control of the melt crystallization of ibuprofen through the melt/atmosphere and melt/surface interfaces.

  2. Effects of humidity and surfaces on the melt crystallization of ibuprofen.

    Science.gov (United States)

    Lee, Dong-Joo; Lee, Suyang; Kim, Il Won

    2012-01-01

    Melt crystallization of ibuprofen was studied to understand the effects of humidity and surfaces. The molecular self-assembly during the amorphous-to-crystal transformation was examined in terms of the nucleation and growth of the crystals. The crystallization was on Al, Au, and self-assembled monolayers with -CH(3), -OH, and -COOH functional groups. Effects of the humidity were studied at room temperature (18-20 °C) with relative humidity 33%, 75%, and 100%. Effects of the surfaces were observed at -20 °C (relative humidity 36%) to enable close monitoring with slower crystal growth. The nucleation time of ibuprofen was faster at high humidity conditions probably due to the local formation of the unfavorable ibuprofen melt/water interface. The crystal morphologies of ibuprofen were governed by the nature of the surfaces, and they could be associated with the growth kinetics by the Avrami equation. The current study demonstrated the effective control of the melt crystallization of ibuprofen through the melt/atmosphere and melt/surface interfaces.

  3. Ibuprofen-loaded poly(lactic-co-glycolic acid films for controlled drug release

    Directory of Open Access Journals (Sweden)

    Pang JM

    2011-04-01

    Full Text Available Jianmei Pang1, Yuxia Luan1, Feifei Li1, Xiaoqing Cai1, Jimin Du2, Zhonghao Li31School of Pharmaceutical Science, Shandong University, Jinan, Shandong Province, PR China; 2School of Chemistry and Chemical Engineering, Anyang Normal University, Henan Province, PR China; 3School of Materials Science and Engineering, Shandong University, Jinan, Shandong Province, PR ChinaAbstract: Ibuprofen- (IBU loaded biocompatible poly(lactic-co-glycolic acid (PLGA films were prepared by spreading polymer/ibuprofen solution on the nonsolvent surface. By controlling the weight ratio of drug and polymer, different drug loading polymer films can be obtained. The synthesized ibuprofen-loaded PLGA films were characterized with scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry. The drug release behavior of the as-prepared IBU-loaded PLGA films was studied to reveal their potential application in drug delivery systems. The results show the feasibility of the as-obtained films for controlling drug release. Furthermore, the drug release rate of the film could be controlled by the drug loading content and the release medium. The development of a biodegradable ibuprofen system, based on films, should be of great interest in drug delivery systems.Keywords: ibuprofen, controlled release, poly(lactic-co-glycolic acid, films

  4. Craving and drug reward: A comparison of celecoxib and ibuprofen in detoxifying opiate addicts

    Directory of Open Access Journals (Sweden)

    sara jafari

    2017-10-01

    Full Text Available OBJECTIVE: Craving for substance abuse is a usual and complicated problem in patients, with opioid addiction, who are in their opioid cessation process. Craving has been added as one of the diagnostic criteria of substance use disorders in DSM-5. AIM: The present trial was intended to compare effects of celecoxib versus ibuprofen in reducing pain and in decreasing the desire to use opiates in patients undergoing opiate detoxification. (n=32. PATIENTS AND METHOD: A total of 32 patients (both inpatients and outpatients, who were undergoing opiate detoxification procedure entered this 4 week study. Subjects who suffered pain due to opiate withdrawal were randomized into two groups; group one received celecoxib 200 milligrams once daily and group two received ibuprofen 400 milligrams four times per day.  Self-reported Desire for Drug Questionnaire (DDQ was utilized at baseline and at the end of the study to evaluate changes in opiate craving. RESULTS: After 4 weeks of treatment, with either ibuprofen or celecoxib, significant improvements in pain and craving were noted in each group. However no significant difference between the two groups was observed after 4 weeks of treatment with celecoxib and ibuprofen. CONCLUSION: The study noted that both celecoxib and ibuprofen, reduce craving in patients with opiate craving after 4 weeks of treatment without any significant difference between the two groups. The results suggest further study of celecoxib and other NSAIDs in the maintenance treatment of opiate craving.

  5. Inhibition of endocannabinoid metabolism by the metabolites of ibuprofen and flurbiprofen.

    Science.gov (United States)

    Karlsson, Jessica; Fowler, Christopher J

    2014-01-01

    In addition to their effects upon prostaglandin synthesis, the non-steroidal anti-inflammatory drugs ibuprofen and flurbiprofen inhibit the metabolism of the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA) by cyclooxygenase-2 (COX-2) and fatty acid amide hydrolase (FAAH), respectively. Here, we investigated whether these effects upon endocannabinoid metabolism are shared by the main metabolites of ibuprofen and flurbiprofen. COX activities were measured via changes in oxygen consumption due to oxygenation of arachidonic acid (for COX-1) and arachidonic acid and 2-AG (for COX-2). FAAH activity was quantified by measuring hydrolysis of tritium labelled AEA in rat brain homogenates. The ability of ibuprofen and flurbiprofen to inhibit COX-2-catalysed oxygenation of 2-AG at lower concentrations than the oxygenation of arachidonic acid was seen with 4'-hydroxyflurbiprofen and possibly also 3'-hydroxyibuprofen, albeit at lower potencies than the parent compounds. All ibuprofen and flurbiprofen metabolites retained the ability to inhibit FAAH in a pH-dependent manner, although the potency was lower than seen with the parent compounds. It is concluded that the primary metabolites of ibuprofen and flurbiprofen retain some of the properties of the parent compound with respect to inhibition of endocannabinoid metabolism. However, these effects are unlikely to contribute to the actions of the parent compounds in vivo.

  6. Inhibition of endocannabinoid metabolism by the metabolites of ibuprofen and flurbiprofen.

    Directory of Open Access Journals (Sweden)

    Jessica Karlsson

    Full Text Available In addition to their effects upon prostaglandin synthesis, the non-steroidal anti-inflammatory drugs ibuprofen and flurbiprofen inhibit the metabolism of the endocannabinoids 2-arachidonoylglycerol (2-AG and anandamide (AEA by cyclooxygenase-2 (COX-2 and fatty acid amide hydrolase (FAAH, respectively. Here, we investigated whether these effects upon endocannabinoid metabolism are shared by the main metabolites of ibuprofen and flurbiprofen.COX activities were measured via changes in oxygen consumption due to oxygenation of arachidonic acid (for COX-1 and arachidonic acid and 2-AG (for COX-2. FAAH activity was quantified by measuring hydrolysis of tritium labelled AEA in rat brain homogenates. The ability of ibuprofen and flurbiprofen to inhibit COX-2-catalysed oxygenation of 2-AG at lower concentrations than the oxygenation of arachidonic acid was seen with 4'-hydroxyflurbiprofen and possibly also 3'-hydroxyibuprofen, albeit at lower potencies than the parent compounds. All ibuprofen and flurbiprofen metabolites retained the ability to inhibit FAAH in a pH-dependent manner, although the potency was lower than seen with the parent compounds.It is concluded that the primary metabolites of ibuprofen and flurbiprofen retain some of the properties of the parent compound with respect to inhibition of endocannabinoid metabolism. However, these effects are unlikely to contribute to the actions of the parent compounds in vivo.

  7. Pain from copper intrauterine device insertion: randomized trial of prophylactic ibuprofen.

    Science.gov (United States)

    Hubacher, David; Reyes, Veronica; Lillo, Sonia; Zepeda, Ana; Chen, Pai-Lien; Croxatto, Horacio

    2006-11-01

    This study was undertaken to determine whether 400 mg of prophylactic ibuprofen can alleviate pain from insertion of an intrauterine device (IUD) and to measure level of pain with improved techniques. We conducted a randomized, double-blind, placebo-controlled trial of 2019 first-time IUD users: 1008 women received placebo and 1011 women received 400 mg of ibuprofen. Participants took the single tablet at least 45 minutes before IUD insertion. Immediately after insertion, participants recorded level of pain by using a 10-cm visual analog scale, with the value of 10 meaning "worst imaginable pain." Median level of pain was 1.0 for both ibuprofen and placebo participants; rank test statistics confirmed no difference. Some subgroups of women experienced higher pain (eg, nulliparous women), but ibuprofen still had no important impact on level of pain. Even among first-time users, pain from IUD insertion is generally low. Prophylactic ibuprofen as used in this protocol does not reduce IUD insertion pain.

  8. Self-Microemulsifying Drug Delivery System: Formulation and Study Intestinal Permeability of Ibuprofen in Rats

    Directory of Open Access Journals (Sweden)

    Bharat Bhushan Subudhi

    2013-01-01

    Full Text Available The study was aimed at developing a self-microemulsifying drug delivery system (SMEDDS of Ibuprofen for investigating its intestinal transport behavior using the single-pass intestinal perfusion (SPIP method in rat. Methods. Ibuprofen loaded SMEDDS (ISMEDDS was developed and was characterized. The permeability behavior of Ibuprofen over three different concentrations (20, 30, and 40 µg/mL was studied in each isolated region of rat intestine by SPIP method at a flow rate of 0.2 mL/min. The human intestinal permeability was predicted using the Lawrence compartment absorption and transit (CAT model since effective permeability coefficients (Peff values for rat are highly correlated with those of human, and comparative intestinal permeability of Ibuprofen was carried out with plain drug suspension (PDS and marketed formulation (MF. Results. The developed ISMEDDS was stable, emulsified upon mild agitation with 44.4 nm ± 2.13 and 98.86% ± 1.21 as globule size and drug content, respectively. Higher Peff in colon with no significant Peff difference in jejunum, duodenum, and ileum was observed. The estimated human absorption of Ibuprofen for the SMEDDS was higher than that for PDS and MF (P<0.01. Conclusion. Developed ISMEDDS would possibly be advantageous in terms of minimized side effect, increased bioavailability, and hence the patient compliance.

  9. Acute cigarette smoke exposure causes lung injury in rabbits treated with ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Witten, M.L.; Lemen, R.J.; Quan, S.F.; Sobonya, R.E.; Magarelli, J.L.; Bruck, D.C.

    1987-01-01

    We studied lung clearance of aerosolized technetium-labeled diethylenetriamine pentaacetic acid (/sup 99m/TcDTPA), plasma concentrations of 6-keto-PGF1 alpha and thromboxane B2, and pulmonary edema as indices of lung injury in rabbits exposed to cigarette smoke (CSE). Forty-six rabbits were randomly assigned to 4 groups: control sham smoke exposure (SS, N = 9), sham smoke exposure ibuprofen-pretreated (SS-I, N = 10), CSE (N = 9), sham smoke exposure ibuprofen-pretreated (SS-I, N = 10), CSE (N = 9), and CSE ibuprofen-pretreated (CSE-I, N = 19). Ibuprofen (cyclooxygenase eicosanoid inhibitor) was administered as a single daily intramuscular injection (25 mg/kg) for 7 days before the experiment. Cigarette or sham smoke was delivered by syringe in a series of 5, 10, 20, and 30 tidal volume breaths with a 15-min counting period between each subset of breaths to determine /sup 99m/TcDTPA biological half-life (T1/2). In the ibuprofen pretreated group, CSE caused significant decreases in /sup 99m/TcDTPA T1/2 and dynamic lung compliance. Furthermore, these changes in lung function were accompanied by severe injury to type I alveolar cell epithelium, pulmonary edema, and frequently death of the rabbits. These findings suggest that inhibition of the cyclooxygenase pathway before CSE exacerbates lung injury in rabbits.

  10. Ibuprofen Versus Fennel for the Relief of Postpartum Pain: A Randomized Controlled Trial

    Directory of Open Access Journals (Sweden)

    Parvin Asti

    2011-06-01

    Full Text Available Objective: The present study aimed to compare the value of ibuprofen and fennel for postpartum painrelief in women with normal vaginal delivery.Materials and methods:In this randomized clinical trial we studied 90 women referring to obstetricsward for Normal Vaginal Delivery (NVD in Assali hospital in Khoramabad. Women were randomlyallocated to receive either oral ibuprofen or oral fennel by stratified random sampling technique. Allwomen were asked to give pain score by visual analogue scale before and at 1, 2, 3 and 4 hours aftertreatment.Results: Difference between fennel and ibuprofen groups was not significant considering severity of painbefore (P=0.22. Difference between two groups considering mean severity of pain one hour aftertreatment (P=0.57 was not significant. But comparing the mean of pain severity in two groups, showedsignificant difference after two (p<0.023, three (p<0.001 and four (p<0.001 hours after treatment.Conclusion: Ibuprofen and fennel were effective for relief of postpartum pain without any notable sideeffects, but in general ibuprofen was more effective than fennel. More studies are needed to confirm theefficacy of fennel in pain relief especially in postpartum women which must be compared to a notreatment control group.

  11. Ibuprofen exposure in early neonatal life does not affect renal function in young adolescence.

    Science.gov (United States)

    Raaijmakers, Anke; Zhang, Zhen-Yu; Levtchenko, Elena; Simons, Sinno Hp; Cauwenberghs, Nicholas; Heuvel, Lambertus P van den; Jacobs, Lotte; Staessen, Jan A; Allegaert, Karel

    2018-03-01

    Ibuprofen exposure results in acute transient renal dysfunction in preterm neonates, but we are unaware of data on long-term renal safety. In a previously studied cohort of extreme low birth weight (ELBW, ibuprofen. In this post hoc analysis, we linked markers of renal function in young adolescence in ELBW cases with their perinatal (prenatal maternal, setting at birth, treatment modalities including drug prescription during neonatal stay, neonatal creatinine values, postdischarge growth) characteristics, including but not limited to ibuprofen exposure during neonatal stay. Ibuprofen exposure was not associated with significant differences in renal length or eGFR cysC . Moreover, we were unable to identify any other risk factor (perinatal characteristics, postnatal creatinine trends, postdischarge growth) on renal outcome in this cohort. Neonatal exposure to ibuprofen did not affect renal function. Larger studies are needed to explore the confounders of variability in renal function in former ELBW cases. This matters since ELBW relates to risk for hypertension, cardiovascular events and renal disease in later life and identification of risk factors holds the promise of secondary prevention. NCT02147457. © Article author(s) (or their employer(s) unless otherwise stated in the text of the article) 2018. All rights reserved. No commercial use is permitted unless otherwise expressly granted.

  12. p53 is important for the anti-proliferative effect of ibuprofen in colon carcinoma cells

    International Nuclear Information System (INIS)

    Janssen, Astrid; Schiffmann, Susanne; Birod, Kerstin; Maier, Thorsten J.; Wobst, Ivonne; Geisslinger, Gerd; Groesch, Sabine

    2008-01-01

    S-ibuprofen which inhibits the cyclooxygenase-1/-2 and R-ibuprofen which shows no COX-inhibition at therapeutic concentrations have anti-carcinogenic effects in human colon cancer cells; however, the molecular mechanisms for these effects are still unknown. Using HCT-116 colon carcinoma cell lines, expressing either the wild-type form of p53 (HCT-116 p53 wt ) or being p(HCT-116 p53 -/- ), we demonstrated that both induction of a cell cycle block and apoptosis after S- and R-ibuprofen treatment is in part dependent on p53. Also in the in vivo nude mice model HCT-116 p53 -/- xenografts were less sensitive for S- and R-ibuprofen treatment than HCT-116 p53 wt cells. Furthermore, results indicate that induction of apoptosis in HCT-116 p53 wt cells after ibuprofen treatment is in part dependent on a signalling pathway including the neutrophin receptor p75 NTR , p53 and Bax

  13. Acute cigarette smoke exposure causes lung injury in rabbits treated with ibuprofen

    International Nuclear Information System (INIS)

    Witten, M.L.; Lemen, R.J.; Quan, S.F.; Sobonya, R.E.; Magarelli, J.L.; Bruck, D.C.

    1987-01-01

    We studied lung clearance of aerosolized technetium-labeled diethylenetriamine pentaacetic acid (/sup 99m/TcDTPA), plasma concentrations of 6-keto-PGF1 alpha and thromboxane B2, and pulmonary edema as indices of lung injury in rabbits exposed to cigarette smoke (CSE). Forty-six rabbits were randomly assigned to 4 groups: control sham smoke exposure (SS, N = 9), sham smoke exposure ibuprofen-pretreated (SS-I, N = 10), CSE (N = 9), sham smoke exposure ibuprofen-pretreated (SS-I, N = 10), CSE (N = 9), and CSE ibuprofen-pretreated (CSE-I, N = 19). Ibuprofen (cyclooxygenase eicosanoid inhibitor) was administered as a single daily intramuscular injection (25 mg/kg) for 7 days before the experiment. Cigarette or sham smoke was delivered by syringe in a series of 5, 10, 20, and 30 tidal volume breaths with a 15-min counting period between each subset of breaths to determine /sup 99m/TcDTPA biological half-life (T1/2). In the ibuprofen pretreated group, CSE caused significant decreases in /sup 99m/TcDTPA T1/2 and dynamic lung compliance. Furthermore, these changes in lung function were accompanied by severe injury to type I alveolar cell epithelium, pulmonary edema, and frequently death of the rabbits. These findings suggest that inhibition of the cyclooxygenase pathway before CSE exacerbates lung injury in rabbits

  14. Efficacy and Safety of Ibuprofen in Infants Aged Between 3 and 6 Months.

    Science.gov (United States)

    Ziesenitz, Victoria C; Zutter, Andreas; Erb, Thomas O; van den Anker, Johannes N

    2017-08-01

    Ibuprofen is a non-steroidal anti-inflammatory drug frequently administered to children of various ages for relief of fever and pain and is approved as an over-the-counter medication in many countries worldwide. Although there are extensive data on its efficacy and safety in children and adults, there are divergent dosing recommendations for analgesia and treatment of fever in infants, especially in the age group between 3 and 6 months of age. In this article, we have assessed the safety and efficacy of ibuprofen use in infants in an attempt to find the optimal method of pain and fever management in this specific age group. Based on the current evidence, short-term use of ibuprofen is considered safe in infants older than 3 months of age having a body weight above 5-6 kg when special attention is given to the hydration of the patient. Ibuprofen should be prescribed based on body weight using a dose of 5-10 mg/kg. This dose can be administered 3-4 times a day resulting in a maximum total daily dose of 30-40 mg/kg. The rectal route has been shown to be less reliable because of erratic absorption, especially in young infants. Since most efficacy and safety data have been derived from trials in infants with fever, future studies should focus on the efficacy of ibuprofen in young infants with pain.

  15. Comparison of oral ibuprofen and intravenous indomethacin for the treatment of patent ductus arteriosus in extremely low birth weight infants

    Directory of Open Access Journals (Sweden)

    Eun Mi Yang

    2013-01-01

    Conclusion: In ELBW infants, oral ibuprofen is as efficacious as intravenous indomethacin for the treatment of PDA. There were no differences between the two drugs with respect to safety. Oral ibuprofen could be used as an alternative agent for the treatment of PDA in ELBW infants.

  16. Possession States: Approaches to Clinical Evaluation and Classification

    Directory of Open Access Journals (Sweden)

    S. McCormick

    1992-01-01

    Full Text Available The fields of anthropology and sociology have produced a large quantity of literature on possession states, physicians however rarely report on such phenomena. As a result clinical description of possession states has suffered, even though these states may be more common and less deviant than supposed. Both ICD-10 and DSM-IV may include specific criteria for possession disorders. The authors briefly review Western notions about possession and kindred states and present guidelines for evaluation and classification.

  17. Synthesis and characterization of thermosensitive hydrogels and the investigation of modified release of ibuprofen

    Directory of Open Access Journals (Sweden)

    Ilić-Stojanović Snežana S.

    2013-01-01

    Full Text Available The method of the synthesis of poly(N-isopropylacrylamide-co-2-hydroxypropyl methacrylate hydrogels obtained by radical polymerization is described. Their characterization was carried out by the determination of the quantity of residual monomers and by investigating their structure using the FTIR. Three glass transitions were detected by DSC method. The porous surfaces of hydrogels with incorporated ibuprofen were shown in SEM micrographs. The swelling ratio of hydrogels decreased with the temperature increase and the swelling transport mechanism was changed from non-Fickian to Fickian. Ibuprofen was incorporated in hydrogel as a drug carrier and released quantity was monitored by HPLC method depending on the temperature. Hydrogel with the lower cross-linker content had the highest swelling degree (α = 34.72 at 10°C and released the largest amount of ibuprofen (64.21 mg/gxerogel at 40°C. [Projekat Ministarstva nauke Republike Srbije, br. TR-34012

  18. Combined use of an ibuprofen-releasing foam dressing and silver dressing on infected leg ulcers

    DEFF Research Database (Denmark)

    Jorgensen, B.; Gottrup, F.; Karlsmark, T.

    2008-01-01

    OBJECTIVE: To investigate the effect and safety of an ibuprofen-releasing foam (Biatain-Ibu, Coloplast A/S) combined with an ionised silver-releasing wound contact layer (Physiotulle Ag, Coloplast A/S) on painful, infected venous leg ulcers. METHOD: This open non-comparative study involved 24...... patients with painful, exuding, locally infected, and stalled venous leg ulcers. Persistent pain and pain at dressing change were monitored using a 11-point numerical box scale (NBS). The composition of the wound bed, the dressing combination's ability to absorb exudate and minimise leakage, ibuprofen...... dressing application, the mean concentration of ibuprofen in the wound exudate reached a constant level of 35 +/- 21 microg/ml.After 31 days, the relative wound area had reduced by 42%, with an associated decrease in fibrin and an increase in granulation tissue.The number of patients with wound malodour...

  19. Dynamic plantwide modeling, uncertainty and sensitivity analysis of a pharmaceutical upstream synthesis: Ibuprofen case study

    DEFF Research Database (Denmark)

    Montes, Frederico C. C.; Gernaey, Krist; Sin, Gürkan

    2018-01-01

    A dynamic plantwide model was developed for the synthesis of the Active pharmaceutical Ingredient (API) ibuprofen, following the Hoescht synthesis process. The kinetic parameters, reagents, products and by-products of the different reactions were adapted from literature, and the different process...... operations integrated until the end process, crystallization and isolation of the ibuprofen crystals. The dynamic model simulations were validated against available measurements from literature and then used as enabling tool to analyze the robustness of design space. To this end, sensitivity of the design...... space towards input disturbances and process uncertainties (from physical and model parameters) is studied using Monte Carlo simulations. The results quantify the uncertainty of the quality of product attributes, with particular focus on crystal size distribution and ibuprofen crystalized. The ranking...

  20. Cyclic resolution of racemic ibuprofen via coupled efficient lipase and acid-base catalysis.

    Science.gov (United States)

    Liu, Ying; Wang, Fang; Tan, Tianwei

    2009-03-01

    Extracellular lipase LIP prepared in our lab from the yeast Yarrowia lipolytica was used for the resolution of racemic ibuprofen. The (S)-enantiomer was preferred by lipase LIP, and the unreacted (R)-enantiomer was extracted and racemized in basic solvent-water medium to be re-resolved. Solvent, content of solvent, base concentration, and temperature have a strong effect on racemization. The (S)-ester was separated and hydrolyzed to (S)-ibuprofen in acidic dimethyl sulfoxide-water mixture containing 70% dimethyl sulfoxide. The high purity (S)-ibuprofen (ee = 0.98) was obtained using lipase LIP to catalyze hydrolysis of (S)-ester in 0.1 M phosphate buffer (pH = 8). (c) 2008 Wiley-Liss, Inc.

  1. Ibuprofen alters human testicular physiology to produce a state of compensated hypogonadism

    DEFF Research Database (Denmark)

    Kristensen, David Møbjerg; Desdoits-Lethimonier, Christèle; Mackey, Abigail L

    2018-01-01

    Concern has been raised over increased male reproductive disorders in the Western world, and the disruption of male endocrinology has been suggested to play a central role. Several studies have shown that mild analgesics exposure during fetal life is associated with antiandrogenic effects...... with reproductive and physical disorders. In the men, luteinizing hormone (LH) and ibuprofen plasma levels were positively correlated, and the testosterone/LH ratio decreased. Using adult testis explants exposed or not exposed to ibuprofen, we demonstrate that the endocrine capabilities from testicular Leydig...... and Sertoli cells, including testosterone production, were suppressed through transcriptional repression. This effect was also observed in a human steroidogenic cell line. Our data demonstrate that ibuprofen alters the endocrine system via selective transcriptional repression in the human testes, thereby...

  2. Accelerating the design of molecularly imprinted nanocomposite membranes modified by Au@polyaniline for selective enrichment and separation of ibuprofen

    Science.gov (United States)

    Wu, Xiuling; Wu, Yilin; Dong, Hongjun; Zhao, Juan; Wang, Chen; Zhou, Shi; Lu, Jian; Yan, Yongsheng; Li, He

    2018-01-01

    A novel system for harvesting molecularly imprinted nanocomposite membranes (MINcMs) with Au-modified polyaniline (Au@polyaniline) nanocomposite structure was developed for selective enrichment and separation of ibuprofen. This unique nanocomposite structure obviously enhanced the adsorption capacity, perm-selectivity performance, and regeneration ability of MINcMs. The as-prepared MINcMs showed outstanding adsorption capacity (22.02 mg g-1) of ibuprofen, which was four times higher than that of non-imprinted nanocomposite membranes (NINcMs). Furthermore, the selectivity factor of MINcMs for ibuprofen reached up to 4.67 and the perm-selectivity factor β was about 8.74, which indicated MINcMs had a good selective separation performance of ibuprofen. We envision that this novel synthesis method will open a new direction to manipulation of molecularly imprinted membrane materials and provide a simple yet convenient way to selective separation of ibuprofen.

  3. Evaporation Behavior and Characterization of Eutectic Solvent and Ibuprofen Eutectic Solution.

    Science.gov (United States)

    Phaechamud, Thawatchai; Tuntarawongsa, Sarun; Charoensuksai, Purin

    2016-10-01

    Liquid eutectic system of menthol and camphor has been reported as solvent and co-solvent for some drug delivery systems. However, surprisingly, the phase diagram of menthol-camphor eutectic has not been reported previously. The evaporation behavior, physicochemical, and thermal properties of this liquid eutectic and ibuprofen eutectic solution were characterized in this study. Differential scanning calorimetry (DSC) analysis indicated that a eutectic point of this system was near to 1:1 menthol/camphor and its eutectic temperature was -1°C. The solubility of ibuprofen in this eutectic was 282.11 ± 6.67 mg mL(-1) and increased the drug aqueous solubility fourfold. The shift of wave number from Fourier transform infrared spectroscopy (FTIR) indicated the hydrogen bonding of each compound in eutectic mixture. The weight loss from thermogravimetric analysis of menthol and camphor related to the evaporation and sublimation, respectively. Menthol demonstrated a lower apparent sublimation rate than camphor, and the evaporation rate of eutectic solvent was lower than the sublimation rate of camphor but higher than the evaporation of menthol. The evaporation rate of the ibuprofen eutectic solution was lower than that of the eutectic solvent because ibuprofen did not sublimate. This eutectic solvent prolonged the ibuprofen release with diffusion control. Thus, the beneficial information for thermal behavior and related properties of eutectic solvent comprising menthol-camphor and ibuprofen eutectic solution was attained successfully. The rather low evaporation of eutectic mixture will be beneficial for investigation and tracking the mechanism of transformation from nanoemulsion into nanosuspension in the further study using eutectic as oil phase.

  4. Effects of upper respiratory tract illnesses, ibuprofen and caffeine on reaction time and alertness.

    Science.gov (United States)

    Smith, Andrew P; Nutt, David J

    2014-05-01

    Compared with healthy individuals, those with upper respiratory tract illnesses (URTIs) report reduced alertness and have slower reaction times. It is important to evaluate medication that can remove this behavioural malaise. The aim of this study was to compare the effects of a combination of ibuprofen plus caffeine with ibuprofen and caffeine alone, and placebo on malaise associated with URTIs, as measured by psychomotor performance and mood testing. Volunteers were randomly assigned to one of four medication conditions as follows: 200 mg ibuprofen and 100 mg caffeine; 200 mg ibuprofen; 100 mg caffeine; placebo. A single oral dose was given and testing followed for 3 h. Efficacy variables were based on the volunteers' performance, measured by psychomotor performance and mood. The pre-drug results confirmed that those with an URTI had a more negative mood and impaired performance. Results from the simple reaction time task, at both 55- and 110-min post-dosing, showed that a single-dose of caffeinated products (I200/C100 and CAF100) led to significantly faster reaction times than IBU200 and placebo. These effects were generally confirmed with the other performance tasks. Subjective measures showed that the combination of ibuprofen and caffeine was superior to the other conditions. There were no serious adverse events reported, and study medication was well tolerated. The results from the post-drug assessments suggest that a combination of ibuprofen and caffeine was the optimum treatment for malaise associated with URTIs in that it had significant effects on objective performance and subjective measures.

  5. Ibuprofen-loaded poly(trimethylene carbonate-co-ε-caprolactone) electrospun fibres for nerve regeneration.

    Science.gov (United States)

    Pires, Liliana R; Guarino, Vincenzo; Oliveira, Maria J; Ribeiro, Cristina C; Barbosa, Mário A; Ambrosio, Luigi; Pêgo, Ana Paula

    2016-03-01

    The development of scaffolds that combine the delivery of drugs with the physical support provided by electrospun fibres holds great potential in the field of nerve regeneration. Here it is proposed the incorporation of ibuprofen, a well-known non-steroidal anti-inflammatory drug, in electrospun fibres of the statistical copolymer poly(trimethylene carbonate-co-ε-caprolactone) [P(TMC-CL)] to serve as a drug delivery system to enhance axonal regeneration in the context of a spinal cord lesion, by limiting the inflammatory response. P(TMC-CL) fibres were electrospun from mixtures of dichloromethane (DCM) and dimethylformamide (DMF). The solvent mixture applied influenced fibre morphology, as well as mean fibre diameter, which decreased as the DMF content in solution increased. Ibuprofen-loaded fibres were prepared from P(TMC-CL) solutions containing 5% ibuprofen (w/w of polymer). Increasing drug content to 10% led to jet instability, resulting in the formation of a less homogeneous fibrous mesh. Under the optimized conditions, drug-loading efficiency was above 80%. Confocal Raman mapping showed no preferential distribution of ibuprofen in P(TMC-CL) fibres. Under physiological conditions ibuprofen was released in 24 h. The release process being diffusion-dependent for fibres prepared from DCM solutions, in contrast to fibres prepared from DCM-DMF mixtures where burst release occurred. The biological activity of the drug released was demonstrated using human-derived macrophages. The release of prostaglandin E2 to the cell culture medium was reduced when cells were incubated with ibuprofen-loaded P(TMC-CL) fibres, confirming the biological significance of the drug delivery strategy presented. Overall, this study constitutes an important contribution to the design of a P(TMC-CL)-based nerve conduit with anti-inflammatory properties. Copyright © 2013 John Wiley & Sons, Ltd.

  6. An examination of the thermodynamics of fusion, vaporization, and sublimation of ibuprofen and naproxen by correlation gas chromatography.

    Science.gov (United States)

    Maxwell, Rachel; Chickos, James

    2012-02-01

    The vaporization enthalpies of (S)-ibuprofen and (S)-naproxen measured by correlation gas chromatography at T = 298.15 K are reported and compared with literature values. Adjustment of the fusion enthalpies of (RS)- and (S)-ibuprofen and (S)-naproxen to T = 298.15 K and combined with the vaporization enthalpy of the (S)-enantiomer of both ibuprofen and naproxen also at T = 298.15 K resulted in the sublimation enthalpies of both (S)-enantiomers. On the assumption that the vaporization enthalpy of the racemic form of ibuprofen is within the experimental uncertainty of the chiral form, the sublimation enthalpy of racemic ibuprofen was also evaluated. The vaporization and sublimation enthalpies compare favorably to the most of the literature values for the racemic form of ibuprofen but differ from the value reported for chiral ibuprofen. The literature values of (S)-naproxen are somewhat smaller than the values measured in this work. The following vaporization enthalpies were measured for (S)-ibuprofen and (S)-naproxen, respectively: ΔH(vap) (298.15 K), 106.0 ± 5.5, 132.2 ± 5.0 kJ·mol(-1) . Sublimation enthalpies of 122.7 ± 5.6 and 155.2 ± 7.1 kJ·mol(-1) were calculated for the (S)-enantiomers of ibuprofen and naproxen and a value of 128.9 ± 5.8 kJ·mol(-1) was estimated for the racemic form of ibuprofen. Copyright © 2011 Wiley Periodicals, Inc.

  7. New microbes as causative agents of Ibuprofen degradation capabilities in the hyporheic zone of a lowland stream

    Science.gov (United States)

    Njeru, Cyrus; Posselt, Malte; Horn, Marcus A.

    2017-04-01

    Ibuprofen is a non-steroidal anti-inflammatory pain reliever and among pharmaceutical residues detected in aquatic environments. Widespread use of the drug and incomplete removal during waste water treatment results in its persistence in effluents and receiving waters. Potential total removal by microbial activity in the hyporheic zone (HZ) of rivers downstream of wastewater treatment plant discharge sites has been hypothesized. Ibuprofen degradation associated microbial communities in are essentially unknown. To address this hypothesis, two sets of oxic HZ sediment microcosms spiked with ibuprofen only (5, 40, 200 and 400 µM), or ibuprofen and 1 mM acetate were set up under laboratory conditions. Ibuprofen degradation in non-sterile relative to autoclaved sediments indicated removal by microbial degradation. Ibuprofen was completely consumed in the absence and presence of supplemental acetate after approximately 11 and 16 days, respectively. Refeeding of ibuprofen and acetate after the first depletion resulted in complete degradation within 24 hours in all treatments. Metabolites of ibuprofen included 1-, 2-, 3-hydroxy- and carboxyibuprofen. Quantitative real-time PCR revealed no pronounced differences in copy numbers of 16S rRNA gene or transcripts between non-spiked controls and treatments. Time resolved triplicate amplicon Illumina MiSeq sequencing targeting the 16S rRNA genes and transcripts revealed increased relative abundances of Proteobacteria, Acidobacteria, Actinobacteria and Firmicutes in treatments with compared to those without ibuprofen. Alpha-, Beta- and Deltaproteobacteria were most active as indicated by RNA based analyses. Enrichment and isolation yielded new Alphaproteobacteria utilizing ibuprofen as sole carbon and energy source. The collective results indicated that (i) HZ sediments sustain efficient biotic (micro-)pollutant removal and (ii) are a reservoir of hitherto unknown microbial diversity associated with such ecosystem services

  8. Thin-coating as an alternative approach to improve flow properties of ibuprofen powder

    DEFF Research Database (Denmark)

    Genina, Natalja; Räikkönen, Heikki; Ehlers, Henrik

    2010-01-01

    In the present study, thin-coating as a potential method for improving flow properties of cohesive ibuprofen powder was introduced. Briefly, the technique was based on the successive deposition of ultrasound-assisted fine polymer mist onto the surface of the powdered active pharmaceutical...... ingredient (API), producing individual particles with a hydrophilic thin-coat. A 0.15% m/V aqueous solution of hydroxypropyl methylcellulose (HPMC) was used. Particle size and surface analysis revealed a decrease in the cohesiveness of ibuprofen powder and an increase in the homogeneity of particle surfaces...

  9. Ibuprofen versus mecillinam for uncomplicated cystitis - a randomized controlled trial study protocol

    DEFF Research Database (Denmark)

    Vik, Ingvild; Bollestad, Marianne; Grude, Nils

    2014-01-01

    , controlled, double blind trial following the principles of Good Clinical Practice. Women between the ages of 18 to 60 presenting with symptoms of uncomplicated cystitis are screened for eligibility. 500 women from four sites in Norway, Sweden and Denmark are allocated to treatment with 600 mg ibuprofen three.......DiscussionIf treatment of uncomplicated cystitis with ibuprofen is as effective as mecillinam for symptom relief, we can potentially reduce the use of antibiotics on a global scale.Trial registrationEudraCTnr: 2012-002776-14. ClinicalTrials.gov: NCT01849926....

  10. A Study of Analgesic Efficacy of Ibuprofen and Diclofenac Sodium in Acute Pulpitis Patients

    Directory of Open Access Journals (Sweden)

    G Komali

    2014-01-01

    Results: Time of onset of action of drugs, Time to peak effect, Total analgesic effect and tolerability of the drugs were assessed. From the present study it was found that there were statistically significant differences in the onset of action of drug and Time to peak effect. Onset of action was early in Ibuprofen and Time to peak effect was early in Diclofenac sodium. Patients rated both drugs to be equally good on Global evaluation scales. Conclusion: It was found that Diclofenac Sodium is more potent compared to Ibuprofen.

  11. Stereoelectronic model to explain the resolution of enantiomeric ibuprofen amides on the Pirkle chiral stationary phase.

    Science.gov (United States)

    Nicoll-Griffith, D A

    1987-07-31

    A chiral recognition model is proposed which incorporates the electronic and steric interactions between amide derivatives of ibuprofen and the (R)-N-(3,5-dinitrobenzoyl)phenylglycine-derived Pirkle chiral stationary phase during high-performance liquid chromatography. Based on this rationale, amide derivatives of ibuprofen were prepared using 4-chloroaniline, 4-bromoaniline, aniline, 4-methoxyaniline and 1-aminonaphthylene to improve the enantiomer separation over previously reported results with this column. The amides prepared gave separation values of 1.16, 1.16, 1.19, 1.21 and 1.23, respectively. These high separation values are consistent with the proposed model.

  12. Ibuprofen for acute treatment of episodic tension-type headache in adults.

    Science.gov (United States)

    Derry, Sheena; Wiffen, Philip J; Moore, R Andrew; Bendtsen, Lars

    2015-07-31

    Tension-type headache (TTH) affects about one person in five worldwide. It is divided into infrequent episodic TTH (fewer than one headache per month), frequent episodic TTH (1 to 14 headaches per month), and chronic TTH (15 headaches a month or more). Ibuprofen is one of a number of analgesics suggested for acute treatment of headaches in frequent episodic TTH. To assess the efficacy and safety of oral ibuprofen for treatment of acute episodic TTH in adults. We searched CENTRAL (The Cochrane Library), MEDLINE, EMBASE, and our own in-house database to January 2015. We sought unpublished studies by asking personal contacts and searching on-line clinical trial registers and manufacturers' websites. We included randomised, placebo-controlled studies (parallel-group or cross-over) using oral ibuprofen for symptomatic relief of an acute episode of TTH. Studies had to be prospective and include at least 10 participants per treatment arm. Two review authors independently assessed studies for inclusion, and extracted data. Numbers of participants achieving each outcome were used to calculate risk ratio (RR) and number needed to treat for an additional beneficial outcome (NNT) or number needed to treat for an additional harmful outcome (NNH) of oral ibuprofen compared to placebo for a range of outcomes, predominantly those recommended by the International Headache Society (IHS). We included 12 studies, all of which enrolled adult participants with frequent episodic TTH. Nine used the IHS diagnostic criteria, but two used the older classification of the Ad Hoc Committee, and one did not describe diagnostic criteria but excluded participants with migraines. While 3094 people with TTH participated in these studies, the numbers available for any form of analysis were lower than this; placebo was taken by 733, standard ibuprofen 200 mg by 127, standard ibuprofen 400 mg by 892, and fast-acting ibuprofen 400 mg by 230. Participants had moderate or severe pain at the start of

  13. Effect of racemic ibuprofen dose on the magnitude and duration of platelet cyclo-oxygenase inhibition: relationship between inhibition of thromboxane production and the plasma unbound concentration of S(+)-ibuprofen.

    Science.gov (United States)

    Evans, A M; Nation, R L; Sansom, L N; Bochner, F; Somogyi, A A

    1991-02-01

    1. Four healthy male subjects received racemic ibuprofen (200, 400, 800 and 1200 mg), orally, on four occasions, 2 weeks apart, according to a four-way Latin-square design, in order to investigate the influence of increasing dose of ibuprofen on the magnitude and duration of its antiplatelet effect as well as on the relationship between such effect and drug concentration. 2. The antiplatelet effect of ibuprofen was assessed by measuring the inhibition of platelet thromboxane B2 (TXB2) generation during the controlled clotting of whole blood. The plasma unbound concentration of S(+)-ibuprofen, the enantiomer shown in an in vitro study to be responsible for the inhibitory effect of platelet TXB2 generation, was measured using an enantioselective method. 3. The maximum percentage inhibition of TXB2 generation increased significantly with dose from a mean +/- s.d. of 93.4 +/- 1.2% after the 200 mg dose to 98.8 +/- 0.3% after the 1200 mg dose, and there was an increase with dose in the duration of inhibition of TXB2 generation. The effect of ibuprofen on platelet TXB2 generation was transient and mirrored the time-course of unbound S(+)-ibuprofen in plasma; on all but one of the 16 occasions, serum TXB2 concentrations returned to at least within 10% of the pretreatment concentrations within 24 h of ibuprofen administration. 4. For each subject, the relationship between the percentage inhibition of TXB2 generation and the unbound concentration of S(+)-ibuprofen in plasma was modelled according to a sigmoidal Emax equation. The mean plasma unbound concentration of S(+)-ibuprofen required to inhibit platelet TXB2 generation by 50% (EC50) was 9.8 +/- 1.0 micrograms l-1.(ABSTRACT TRUNCATED AT 250 WORDS)

  14. Comparison of the clinical efficacy of methylprednisolone with ibuprofen and ibuprofen alone on the postoperative sequelae of surgical removal of impacted third molar

    Directory of Open Access Journals (Sweden)

    Navneet Kaur

    2014-01-01

    Full Text Available Purpose: The aim of the study was to compare the clinical efficacy of methylprednisolone with ibuprofen to ibuprofen alone on the postoperative sequelae of surgical removal of impacted third molars. Materials and Methods: The present study was conducted on the 35 patients requiring surgical extraction of bilateral impacted third molars attending the Outpatient Department of Oral and Maxillofacial Surgery, Guru Nanak Dev Dental College and Research Institute. The impacted teeth were removed in two sessions at least 3 weeks apart. The selected patients were randomly put on regimen 1 or regimen II at either the first or second surgery in accordance with randomization plan. The measurements and recordings for pain, swelling, and interincisal distance (mouth opening, were made on 1 st , 3 rd , and 7 th day postoperatively on the scales designed for the purpose. The data recorded was compiled and put to statistical analysis. Results: It was observed from the present study that postoperative sequelae, that is, pain, swelling, and trismus was significantly less in the regimen I group than regimen II group on the 1 st and 3 rd postoperative day. Conclusion: The results of this study substantiate the fact that a single class of drugs (nonsteroidal anti-inflammatory drug (NSAID is less effective in controlling postoperative inflammatory sequelae than the combination of ibuprofen (NSAID and methylprednisolone (corticosteroid following the third molar surgery. Therefore, this pharmaceutical combination should be considered for attenuation of postoperative sequelae in healthy patients undergoing surgical removal of impacted mandibular third molar.

  15. Effects of Addition of Preoperative Intravenous Ibuprofen to Pregabalin on Postoperative Pain in Posterior Lumbar Interbody Fusion Surgery

    Directory of Open Access Journals (Sweden)

    Hüseyin Ulaş Pınar

    2017-01-01

    Full Text Available Objective. Ibuprofen and pregabalin both have independent positive effects on postoperative pain. The aim of the study is researching effect of 800 mg i.v. ibuprofen in addition to preoperative single dose pregabalin on postoperative analgesia and morphine consumption in posterior lumbar interbody fusion surgery. Materials and Methods. 42 adult ASA I-II physical status patients received 150 mg oral pregabalin 1 hour before surgery. Patients received either 250 ml saline with 800 mg i.v. ibuprofen or saline without ibuprofen 30 minutes prior to the surgery. Postoperative analgesia was obtained by morphine patient controlled analgesia (PCA and 1 g i.v. paracetamol every six hours. PCA morphine consumption was recorded and postoperative pain was evaluated by Visual Analog Scale (VAS in postoperative recovery room, at the 1st, 2nd, 4th, 8th, 12th, 24th, 36th, and 48th hours. Results. Postoperative pain was significantly lower in ibuprofen group in recovery room, at the 1st, 2nd, 36th, and 48th hours. Total morphine consumption was lower in ibuprofen group at the 2nd, 4th, 8th, 12th, and 48th hours. Conclusions. Multimodal analgesia with preoperative ibuprofen added to preoperative pregabalin safely decreases postoperative pain and total morphine consumption in patients having posterior lumbar interbody fusion surgery, without increasing incidences of bleeding or other side effects.

  16. Ibuprofen versus acetaminophen as a post-partum analgesic for women with severe pre-eclampsia: randomized clinical study.

    Science.gov (United States)

    Vigil-De Gracia, Paulino; Solis, Valentin; Ortega, Nelson

    2017-06-01

    To compare differences in blood pressure levels between patients with severe post-partum pre-eclampsia using ibuprofen or acetaminophen. A randomized controlled trial was made in women with severe pre-eclampsia or superimposed pre-eclampsia after vaginal birth. The patient was randomly selected to receive either 400 mg of ibuprofen every 8 h or 1 g of acetaminophen every 6 h during the post-partum. The primary variable was systolic hypertension ≥150 mmHg and/or diastolic hypertension ≥100 mmHg after the first 24 h post-partum. Secondary variables were the arterial blood pressure readings at 24, 48, 72, and 96 h post-partum and maternal complications. A total of 113 patients were studied: 56 in the acetaminophen group and 57 in the ibuprofen group. With regard to the primary outcome, more cases were significantly hypertensive in the ibuprofen group (36/57; 63.1%) than in the acetaminophen group (16/56; 28.6%). Severe hypertension (≥160/110 mmHg) was not significantly different between the groups, 14.5% (acetaminophen) and 24.5% (ibuprofen). The levels of arterial blood pressure show a hammock-shaped curve independent of the drug used, however, is more noticeable with ibuprofen. This study shows that ibuprofen significantly elevates blood pressure in women with severe pre-eclampsia during the post-partum period.

  17. High-dose ibuprofen therapy associated with esophageal ulceration after pneumonectomy in a patient with cystic fibrosis: a case report

    Directory of Open Access Journals (Sweden)

    Anbar Ran D

    2004-09-01

    Full Text Available Abstract Background Lung disease in patients with cystic fibrosis is thought to develop as a result of airway inflammation, infection, and obstruction. Pulmonary therapies for cystic fibrosis that reduce airway inflammation include corticosteroids, rhDNase, antibiotics, and high-dose ibuprofen. Despite evidence that high-dose ibuprofen slows the progression of lung disease in patients with cystic fibrosis, many clinicians have chosen not to use this therapy because of concerns regarding potential side effects, especially gastrointestinal bleeding. However, studies have shown a low incidence of gastrointestinal ulceration and bleeding in patients with cystic fibrosis who have been treated with high-dose ibuprofen. Case presentation The described case illustrates a life-threatening upper gastrointestinal bleed that may have resulted from high-dose ibuprofen therapy in a patient with CF who had undergone a pneumonectomy. Mediastinal shift post-pneumonectomy distorted the patient's esophageal anatomy and may have caused decreased esophageal motility, which led to prolonged contact of the ibuprofen with the esophagus. The concentrated effect of the ibuprofen, as well as its systemic effects, probably contributed to the occurrence of the bleed in this patient. Conclusions This report demonstrates that gastrointestinal tract anatomical abnormalities or dysmotility may be contraindications for therapy with high-dose ibuprofen in patients with cystic fibrosis.

  18. The effect of ibuprofen on accumulation of indium-111-labeled platelets and leukocytes in experimental myocardial infarction

    International Nuclear Information System (INIS)

    Romson, J.L.; Hook, B.G.; Rigot, V.H.; Schark, M.A.; Swanson, D.P.; Lucchesi, B.R.

    1982-01-01

    To assess the ability of ibuprofen to influence the extent of platelet aggregation and leukocyte infiltration during acute myocardial infarction, autologous indium-111 ( 111 In)-labeled platelets or leukocytes were injected before 60 minutes of left circumflex coronary artery (LCx) occlusion, followed by 24 hours of reperfusion in the canine heart. Myocardial infarct size, as a percent of the area at risk, was reduced in the ibuprofen-treated group (12.5 mg/kg i.v. every 4 hours beginning 30 minutes before LCx occulsion) by 40%, from 48 +/- 4% in control animals to 29 +/- 4% in ibuprofen-treated dogs (p=0.005). Quantification of the platelet-associated 111 In radioactivity in irreversibly injured myocardium indicated that ibuprofen did not alter the accumulation of platelets in infarcted myocardium. In contrast, leukocyte accumulation in infarcted tissue was reduced significantly. In tissue samples with 0.41-0.60 gram infarct, the infarcted/normal ratio of leukocyte radioactivity was 12 +/- 2 in control dogs and 4 +/- 1 in ibuprofen-treated dogs, which represents a 67% reduction in leukocyte accumulation in ibuprofen-treated compared with control dogs. Similar reductions were found in other gram-infarct-weight categories. Although both platelets and leukocytes acumulate in infarcted canine myocardium, ibuprofen may exert its beneficial effect on ischemic myocardium by suppressing the inflammatory response associated with myocardial ischemia and infarction

  19. The effect of ibuprofen on accumulation of 111In-labeled platelets and leukocytes in experimental myocardial infarction

    International Nuclear Information System (INIS)

    Romson, J.L.; Hook, B.G.; Rigot, V.H.; Schork, M.A.; Swanson, D.P.; Lucchesi, B.R.

    1982-01-01

    To assess the ability of ibuprofen to influence the extent of platelet aggregation and leukocyte infiltration during acute myocardial infarction, autologous indium-111 ( 111 In)-labeled platelets or leukocytes were injected before 60 minutes of left circumflex coronary artery (LCx) occlusion, followed by 24 hours of reperfusion in the canine heart. Myocardial infarct size, as a percent of the area at risk, was reduced in the ibuprofen-treated group (12.5 mg/kg i.v. every 4 hours beginning 30 minutes before LCx occlusion) by 40%, from 48 +/- 4% in control animals to 29 +/- 4% in ibuprofen-treated dogs (p . 0.005). Quantification of the platelet-associated 111 In radioactivity in irreversibly injured myocardium indicated that ibuprofen did not alter the accumulation of platelets in infarcted myocardium. In contrast, leukocyte accumulation in infarcted tissue was reduced significantly. In tissue samples with 0.41-0.60 gram infarct, the infarcted/normal ratio of leukocyte radioactivity was 12 +/- 2 in control dogs and 4 +/- 1 in ibuprofen-treated dogs, which represents a 67% reduction in leukocyte accumulation in ibuprofen-treated compared with control dogs. Similar reductions were found in other gram-infarct-weight categories. Although both platelets and leukocytes accumulate in infarcted canine myocardium, ibuprofen may exert its beneficial effect on ischemic myocardium by suppressing the inflammatory response associated with myocardial ischemia and infarction

  20. Ibuprofen enhances the anticancer activity of cisplatin in lung cancer cells by inhibiting the heat shock protein 70

    Science.gov (United States)

    Endo, H; Yano, M; Okumura, Y; Kido, H

    2014-01-01

    Hsp70 is often overexpressed in cancer cells, and the selective cellular survival advantage that it confers may contribute to the process of tumour formation. Thus, the pharmacological manipulation of Hsp70 levels in cancer cells may be an effective means of preventing the progression of tumours. We found that the downregulation of Hsp70 by ibuprofen in vitro enhances the antitumoural activity of cisplatin in lung cancer. Ibuprofen prominently suppressed the expression of Hsp70 in A549 cells derived from lung adenocarcinoma and sensitized them to cisplatin in association with an increase in the mitochondrial apoptotic cascade, whereas ibuprofen alone did not induce cell death. The cisplatin-dependent events occurring up- and downstream of mitochondrial disruption were accelerated by treatment with ibuprofen. The increase in cisplatin-induced apoptosis caused by the depletion of Hsp70 by RNA interference is evidence that the increased apoptosis by ibuprofen is mediated by its effect on Hsp70. Our observations indicate that the suppression of Hsp70 by ibuprofen mediates the sensitivity to cisplatin by enhancing apoptosis at several stages of the mitochondrial cascade. Ibuprofen, therefore, is a potential therapeutic agent that might allow lowering the doses of cisplatin and limiting the many challenge associated with its toxicity and development of drug resistance. PMID:24481441

  1. Association of Prenatal Ibuprofen Exposure with Birth Weight and Gestational Age: A Population-Based Sibling Study.

    Science.gov (United States)

    Nezvalová-Henriksen, Kateřina; Wood, Mollie; Spigset, Olav; Nordeng, Hedvig

    2016-01-01

    Three studies so far have investigated the effect of prenatal non-steroidal anti-inflammatory drug (NSAID) exposure on birth weight and gestational age. The aim in this study was to evaluate the association of prenatal ibuprofen with birth weight and gestational age at birth, using a sibling design in an attempt to adjust for the possibility of familial confounding. Using data from the Norwegian Mother and Child Cohort Study (MoBa) and the Medical Birth Registry of Norway (MBRN), we identified 28 597 siblings, of whom 1080 were prenatally exposed to ibuprofen and 26 824 were not exposed to any NSAID. Random and fixed effects models with propensity score adjustment were used to evaluate the effects of ibuprofen exposure on birth weight and gestational age. Ibuprofen exposure during the first trimester was associated with a decrease in birth weight of 79 grams (95% confidence interval -133 to -25 grams). In contrast, second and/or third trimester exposure, and duration of exposure had no impact on the effect estimates. We found no association between ibuprofen exposure and gestational age at birth. Our results suggest that prenatal exposure to ibuprofen during the first trimester is associated with a slight decrease in birth weight. The association does not seem to be attributable to shared genetics and family environment, and could be explained by either exposure to ibuprofen, or to non-shared confounding between pregnancies.

  2. Quantitative proteomic analysis of Ibuprofen-degrading Patulibacter sp. strain I11

    DEFF Research Database (Denmark)

    Kjeldal, Henrik; Lolas, Ihab Bishara Yousef; Knudsen, Anders Dahl

    The constant increase in diversity and quantity of Pharmaceutically Active Compounds (PhACs) detected in waste water treatment plants (WWTPs) effluents is an issue of rising concern due to the potential negative impact of the PhACs on the surrounding environment1. Of PhACs, Ibuprofen, a non-stero...

  3. Development and optimization of the synthesis of new thiazolidin-4-one derivatives of ibuprofen.

    Science.gov (United States)

    Vasincu, Ioana; Apotrosoaei, Maria; Panzariu, Andreea; Buron, F; Routier, S; Profire, Lenuta

    2014-01-01

    Ibuprofen, an important nonsteroidal anti-inflammatory agent, is one of the most prescribed drugs for the treatment of pain and inflammation from various rheumatic diseases, but some side effects can occur on long-term use. The method for synthesis optimization of new derivatives of Ibuprofen with thiazolidin-4-one moiety, with improved pharmacological and toxicological profile. To optimize the derivatization method of free carboxyl group of Ibuprofen (2-(4-isobutylphenyl)propionic acid) the reaction conditions were varied (reagent ratio, catalyst, reaction medium). The most favorable method was proved to be the reaction between ibuprofen hydrazone and mercaptoacetic acid, in excess, at 80-85 degrees C, for 6 h with 96% conversion rate. The synthesis of 2-phenyl-3-[2-(4-(isobutyl)phenyl)-2-methyl]acetamido-thiazolidin-4-one derivative was optimized in view of applying it as a general procedure for the synthesis of other derivatives with related structure. The chemical structure and molecular weight of the synthesized compound were confirmed by spectral methods (IR, 1H NMR, 13C NMR, HR-MS).

  4. Ibuprofen versus Acetaminophen in Controlling Postoperative Impacted Third Molar Tooth Extraction Pain

    International Nuclear Information System (INIS)

    Khan, I.; Bukhari, S. G. A.; Ahmad, W.; Rubbab,; Junaid, M.

    2013-01-01

    Objectives: To compare the efficacy of ibuprofen and acetaminophen in reducing postoperative third molar extraction pain in patients reporting to Armed Forces Institute of Dentistry. Study design: Randomized controlled trial. Place and duration of study: The study was carried out on patients who presented for surgical removal of impacted teeth at Armed Forces Institute of Dentistry Rawalpindi (AFID) from February 2008 to March 2--9 at the Department of Oral Surgery, Armed Forces Institute of Dentistry Rawalpindi. Patients and methods: One hundred and forty patients requiring surgical removal of mandibular impacted teeth were equally divided into two groups. Surgical extraction of third molar tooth was performed under local anesthesia. Patients in group A were given ibuprofen and in group B were given acetaminophen at 6 hourly intervals. First dose was given 3 hours postoperatively. Each patient rated pain on a visual analog scale at baseline and then at 12, 24, 48 and 72 hours postoperatively. Results: There was statistically significant difference (p=0.025) during first 12 hours with ibuprofen group showing better efficacy but afterwards there was no significant difference in the efficacy of both drugs. Conclusions: Ibuprofen is more effective in controlling severe third molar extraction pain as compared to acetaminophen but has similar efficacy in controlling moderate pain. (author)

  5. Quantitative analysis of ibuprofen in pharmaceuticals and human control serum using kinetic spectrophotometry

    Directory of Open Access Journals (Sweden)

    SNEZANA S. MITIC

    2008-08-01

    Full Text Available The aim of this work was to develop a new kinetic spectrophoto-metric method for the determination of ibuprofen in pharmaceutical for-mulations. Ibuprofen was determined in an acidic ethanolic medium by monitoring the rate of appearance of 1-nitroso-2-naphthol, resulting from the displacement by ibuprofen of Co(III from the tris(1-nitroso-2-naptholatocobalt(III complex. The optimum operating conditions regarding reagent concentrations and temperature were established. The tangent method was adopted for constructing the calibration curve, which was found to be linear over the concentration range 0.21–1.44 and 1.44–2.06 µg ml-1. The optimized conditions yielded a theoretical detection limit of 0.03 µg ml-1 based on the 3.3 S0 criterion. The interference effects of the usual excipients of powdery drugs, foreign ions and amino acids on the reaction rate were studied in order to assess the selectivity of the method. The developed procedure was successfully applied for the rapid determination of ibuprofen in commercial pharmaceutical formulations and human control serum. The unique features of this procedure are that the determination can be performed at room temperature and the analysis time is short. The newly developed method is simple, inexpensive and efficient for use in the analysis of a large number of samples.

  6. Intravenous ibuprofen: the first injectable product for the treatment of pain and fever

    Directory of Open Access Journals (Sweden)

    P Brandon Bookstaver

    2010-05-01

    Full Text Available P Brandon Bookstaver, April D Miller, Celeste N Rudisill, LeAnn B NorrisDepartment of Clinical Pharmacy and Outcomes Sciences, South Carolina College of Pharmacy, University of South Carolina Campus, Columbia, South Carolina, USAAbstract: This paper reviews the current data on the use of the first approved intravenous ibuprofen product for the management of post-operative pain and fever in the United States. The management of acute and post-operative pain and fever with nonsteroidal anti-inflammatory agents (NSAIDs is well documented. A search in Medline and International Pharmaceutical Abstracts of articles until the end of November 2009 and references of all citations were conducted. Available manufacturer data on file were also analyzed for this report. Several randomized controlled studies have demonstrated the opioid-sparing and analgesic effects of 400 and 800 mg doses of intravenous ibuprofen in a series of post-operative patient populations. Two recent studies have also noted the improvement in fever curves in critically ill and burn patients. These data, along with pharmacokinetic and pharmacologic properties, are explored in this review, which addresses the clinical utility of a parenteral NSAID in a hospitalized patient for post-operative pain management and fever reduction. Further data on intravenous ibuprofen are needed to define long-term utilization, management of acute pain, and use in special populations.Keywords: ibuprofen, intravenous, injectable, nonsteroidal anti-inflammatory drug

  7. A comparison of the blood pressure changes of lumiracoxib with those of ibuprofen and naproxen.

    NARCIS (Netherlands)

    Farkouh, M.E.; Verheugt, F.W.A.; Ruland, S.; Kirshner, H.; Jeger, R.; Gitton, X.; Krammer, G.; Stricker, K.; Sallstig, P.; Mellein, B.; Matchaba, P.; Chesebro, J.H.

    2008-01-01

    The 52-week Therapeutic Arthritis Research and Gastrointestinal Event Trial (TARGET) investigated the gastrointestinal and cardiovascular safety profile of lumiracoxib 400 mg once daily compared with 2 traditional nonsteroidal anti-inflammatory drugs (NSAIDs): ibuprofen 800 mg 3 times daily and

  8. Vapour-phase method in the synthesis of polymer-ibuprofen sodium-silica gel composites.

    Science.gov (United States)

    Kierys, Agnieszka; Krasucka, Patrycja; Grochowicz, Marta

    2017-11-01

    The study discusses the synthesis of polymer-silica composites comprising water soluble drug (ibuprofen sodium, IBS). The polymers selected for this study were poly(TRIM) and poly(HEMA- co -TRIM) produced in the form of permanently porous beads via the suspension-emulsion polymerization method. The acid and base set ternary composites were prepared by the saturation of the solid dispersions of drug (poly(TRIM)-IBS and/or poly(HEMA- co -TRIM)-IBS) with TEOS, and followed by their exposition to the vapour mixture of water and ammonia, or water and hydrochloric acid, at autogenous pressure. The conducted analyses reveal that the internal structure and total porosity of the resulting composites strongly depend on the catalyst which was used for silica precursor gelation. The parameters characterizing the porosity of both of the acid set composites are much lower than the parameters of the base set composites. Moreover, the basic catalyst supplied in the vapour phase does not affect the ibuprofen sodium molecules, whereas the acid one causes transformation of the ibuprofen sodium into the sodium chloride and a derivative of propanoic acid, which is poorly water soluble. The release profiles of ibuprofen sodium from composites demonstrate that there are differences in the rate and efficiency of drug desorption from them. They are mainly affected by the chemical character of the polymeric carrier but are also associated with the restricted swelling of the composites in the buffer solution after precipitation of silica gel.

  9. Timing of ibuprofen use and musculoskeletal adaptations to exercise training in older adults

    Directory of Open Access Journals (Sweden)

    Catherine M. Jankowski

    2015-01-01

    The difference between groups in the change in BMD was not significant when IP was compared with either PP (hip, −0.5% (−1.4, 0.4; spine, 0.1% (−0.9, 1.2 or PI (hip, 0.3% (−0.6, 1.2; spine, 0.5% (−0.5, 1.5. Ibuprofen use appeared to have more adverse effects on BMD in women than men. The study demonstrated that ibuprofen use did not significantly alter the BMD adaptations to exercise in older adults, but this finding should be interpreted cautiously. It had been expected that the inhibition of bone formation by ibuprofen would be more robust in men than in women, but this did not appear to be the case and may have limited the power to detect the effects of ibuprofen. Further research is needed to understand whether NSAID use counteracts, in part, the beneficial effects of exercise on bone.

  10. Effectiveness of piroxicam and ibuprofen premedication on orthodontic patients' pain experiences.

    Science.gov (United States)

    Kohli, Sarvraj Singh; Kohli, Virinder Singh

    2011-11-01

    To compare the effectiveness of preoperative administration of ibuprofen and piroxicam on orthodontic pain experienced after separator placement. Ninety patients aged between 13 years 9 months and 18 years 2 months who were to undergo fixed appliance orthodontic treatment were enrolled in this double-blind, parallel-arm, prospective study. Patients were evenly and randomly distributed to any of three experimental groups, as follows: (1) administration of placebo, (2) administration of 400 mg ibuprofen, and (3) administration of 20 mg piroxicam; medications were administered 1 hour before separator placement. The pain perceived was recorded by the patients on a linear and graded Visual Analogue Scale at time intervals of 2 hours; 6 hours; nighttime on the day of appointment; 24 hours after the appointment; and 2 days, 3 days, and 7 days after separator placement during each of the four activities (viz, chewing, biting, fitting front teeth, and fitting back teeth). The results revealed that preoperative administration of 20 mg of piroxicam 1 hour prior to separator placement resulted in a significant decrease in pain levels at 2 hours, 6 hours, nighttime, and 24 hours and on the second and third days after separator placement, compared to patients on a placebo or ibuprofen. Premedication with 20 mg of piroxicam results in significantly decreased pain experienced, compared to premedication with 400 mg of ibuprofen or placebo. Usage of 20 mg of piroxicam 1 hour prior to separator placement is recommended.

  11. USE OF A NEW FORM OF IBUPROFEN IN CHILDREN WITH FEVER AND ACUTE RESPIRATORY TRACT INFECTIONS

    Directory of Open Access Journals (Sweden)

    E. E. Lokshina

    2013-01-01

    Full Text Available Aim: to study clinical efficacy, tolerance and safety of a new pelleted ibuprofen form for children in treatment of fever in patients with acute respiratory tract infection. Patients and methods: children aged from 6 to 12 years old with clinical manifestation of respiratory tract infections and requiring antipyretic treatment were included into the study. Children (n = 50 were administered ibuprofen at a single dose of 5–10 mg/kg of body weight, not more than 3–4 times per day. The efficacy assessment included time needed for temperature decrease (assessment was performed in 15, 30 and 60 minutes and duration of the antipyretic effect (assessment in 6, 8 and 12 hours. Rapidity of analgesic effect in children with ear ache, headache and myalgias was performed in 15, 30, 60 minutes and 6, 8 and 12 hours after the drug intake. Results: antipyretic effect of pelleted ibuprofen for children begins in 15 minutes after its intake. Stable temperature decrease during the first 6 hours was observed in 58% of children (the mean temperature was 37,1 ± 0,3 and maintained up for 12 hours. Relief of pain intensity was established in 62,1% of patients during the first 3 hours, and in 37,9% the pain syndrome was arrested completely. Conclusions: the new pelleted form of ibuprofen for children was proved to have high clinical efficacy and safety in treatment of fever in children with acute respiratory tract infections.

  12. Thermal and spectroscopic studies on solid ibuprofen complexes of lighter trivalent lanthanides

    Energy Technology Data Exchange (ETDEWEB)

    Gálico, D.A.; Holanda, B.B.C.; Guerra, R.B.; Legendre, A.O.; Rinaldo, D. [UNESP – Univ Estadual Paulista, Faculdade de Ciências, Departamento de Química, São Paulo CEP 17033-260 (Brazil); Treu-Filho, O. [UNESP – Univ Estadual Paulista, Instituto de Química, São Paulo CEP 14800-900 (Brazil); Bannach, G., E-mail: gilbert@fc.unesp.br [UNESP – Univ Estadual Paulista, Faculdade de Ciências, Departamento de Química, São Paulo CEP 17033-260 (Brazil)

    2014-01-10

    Highlights: • Lighter trivalent lanthanide complexes of ibuprofen have been synthesized. • The TG-FTIR allowed the identification of propane as the gas evolved during the thermal decomposition of the neodymium compound. • The thermal analysis provided information about the composition, dehydration, thermal behavior and thermal decomposition of the samples. • The theoretical and experimental spectroscopic studies suggest that the carboxylate group of ibuprofen is coordinated to the metals by a bidentate bond. - Abstract: Solid-state compounds of general formula Ln(L){sub 3}, in which L is ibuprofen and Ln stands for trivalent La, Ce, Pr, Nd, Sm and Eu, have been synthesized. Simultaneous thermogravimetry and differential thermal analysis (TG-DTA), X-ray powder diffractometry (DRX), complexometry, Fourier-transformed infrared spectroscopy (FTIR) and thermogravimetry coupled to Fourier-transformed infrared spectroscopy (TG-FTIR) were used to characterize these compounds. The results provided information concerning the chemical composition, dehydration, coordination modes of the ligands, crystallinity of the samples, thermal behavior and thermal decomposition of the compounds. The theoretical and experimental spectroscopic studies suggest that ibuprofen coordinates through the carboxylate group as a chelating ligand.

  13. Effectiveness of Ibuprofen Administration on the Depth of Anesthesia in Inflamed Teeth

    Directory of Open Access Journals (Sweden)

    R Mahmodi

    2006-07-01

    Full Text Available Introduction: Incomplete anesthesia of inflamed teeth is a well known clinical occurrence and the purpose of this study was to evaluate the effectiveness of Ibuprofen as a premedication in improving the quality of anesthesia in patients with inflamed teeth pulps. Methods: Forty patients with the diagnosis of irreversible pulpitis in one mandibular tooth were selected. Two other teeth in the same quadrant were selected as controls. Electric pulp tester (EPT was used in this study to evaluate the quality of anesthesia. The subjects were divided into two groups randomly, and after recording of pulp tester response in each group, one of the two drugs; ibuprofen or placebo was administered 1 hour prior to anesthesia injection. After injection, EPT measurement was recorded. The reversed EPT scale was used for evaluation of the depth of anesthesia. Results : Data was analyzed to statistically compare the results before and after anesthesia and drug administration in cases and control group .Significantly lower TSLs were observed in the ibuprofen group (Pvalue= 0.001. Conclusion: This study concluded that preoperative administration of ibuprofen (if not contraindicated 1 hour before local anesthesia injection is an effective method for achieving deep anesthesia during RCT of teeth with irreversible pulpitis.

  14. Enantioselective adsorption of ibuprofen and lysine in metal-organic frameworks

    NARCIS (Netherlands)

    Bueno-Perez, R.; Martin-Calvo, A.; Gómez-Álvarez, P.; Gutiérrez-Sevillano, J.J.; Merkling, P.J.; Vlugt, T.J.H.; van Erp, T.S.; Dubbeldam, D.; Calero, S.

    2014-01-01

    This study reveals the efficient enantiomeric separation of bioactive molecules in the liquid phase. Chiral structure HMOF-1 separates racemic mixtures whereas heteroselectivity is observed for scalemic mixtures of ibuprofen using non-chiral MIL-47 and MIL-53. Lysine enantiomers are only separated

  15. An Experimental Verification of morphology of ibuprofen crystals from CAMD designed solvent

    DEFF Research Database (Denmark)

    Karunanithi, Arunprakash T.; Acquah, Charles; Achenie, Luke E.K.

    2007-01-01

    of crystals formed from solvents, necessitates additional experimental verification steps. In this work we report the experimental verification of crystal morphology for the case study, solvent design for ibuprofen crystallization, presented in Karunanithi et al. [2006. A computer-aided molecular design...

  16. Ibuprofen-loaded microspheres based on a co-polymer of Eudragit ...

    African Journals Online (AJOL)

    The objective of this study was to encapsulate ibuprofen in microspheres based on a co-polymer of Eudragit® RS100 and RL100 with a view to achieving a controlled release of the incorporated drug. The microparticles were prepared by an o/o emulsion-solvent evaporation method using varying polymer ratios and ...

  17. Formulation of Novel Layered Sodium Carboxymethylcellulose Film Wound Dressings with Ibuprofen for Alleviating Wound Pain

    Directory of Open Access Journals (Sweden)

    Lenka Vinklárková

    2015-01-01

    Full Text Available Effective assessment and management of wound pain can facilitate both improvements in healing rates and overall quality of life. From a pharmacological perspective, topical application of nonsteroidal anti-inflammatory drugs in the form of film wound dressings may be a good choice. Thus, the aim of this work was to develop novel layered film wound dressings containing ibuprofen based on partially substituted fibrous sodium carboxymethylcellulose (nonwoven textile Hcel NaT. To this end, an innovative solvent casting method using a sequential coating technique has been applied. The concentration of ibuprofen which was incorporated as an acetone solution or as a suspension in a sodium carboxymethylcellulose dispersion was 0.5 mg/cm2 and 1.0 mg/cm2 of film. Results showed that developed films had adequate mechanical and swelling properties and an advantageous acidic surface pH for wound application. An in vitro drug release study implied that layered films retained the drug for a longer period of time and thus could minimize the frequency of changing the dressing. Films with suspended ibuprofen demonstrated higher drug content uniformity and superior in vitro drug release characteristics in comparison with ibuprofen incorporation as an acetone solution. Prepared films could be potential wound dressings for the effective treatment of wound pain in low exuding wounds.

  18. Vapour-phase method in the synthesis of polymer-ibuprofen sodium-silica gel composites

    Directory of Open Access Journals (Sweden)

    Agnieszka Kierys

    2017-11-01

    Full Text Available The study discusses the synthesis of polymer-silica composites comprising water soluble drug (ibuprofen sodium, IBS. The polymers selected for this study were poly(TRIM and poly(HEMA-co-TRIM produced in the form of permanently porous beads via the suspension-emulsion polymerization method. The acid and base set ternary composites were prepared by the saturation of the solid dispersions of drug (poly(TRIM-IBS and/or poly(HEMA-co-TRIM-IBS with TEOS, and followed by their exposition to the vapour mixture of water and ammonia, or water and hydrochloric acid, at autogenous pressure. The conducted analyses reveal that the internal structure and total porosity of the resulting composites strongly depend on the catalyst which was used for silica precursor gelation. The parameters characterizing the porosity of both of the acid set composites are much lower than the parameters of the base set composites. Moreover, the basic catalyst supplied in the vapour phase does not affect the ibuprofen sodium molecules, whereas the acid one causes transformation of the ibuprofen sodium into the sodium chloride and a derivative of propanoic acid, which is poorly water soluble. The release profiles of ibuprofen sodium from composites demonstrate that there are differences in the rate and efficiency of drug desorption from them. They are mainly affected by the chemical character of the polymeric carrier but are also associated with the restricted swelling of the composites in the buffer solution after precipitation of silica gel.

  19. Ibuprofen ingestion does not affect markers of post-exercise muscle inflammation.

    Directory of Open Access Journals (Sweden)

    Luke eVella

    2016-03-01

    Full Text Available Purpose: We investigated if oral ingestion of ibuprofen influenced leucocyte recruitment and infiltration following an acute bout of traditional resistance exercise. Methods: Sixteen male subjects were divided into two groups that received the maximum over-the-counter dose of ibuprofen (1200 mg d-1 or a similarly administered placebo following lower body resistance exercise. Muscle biopsies were taken from m.vastus lateralis and blood serum samples were obtained before and immediately after exercise, and at 3 h and 24 h after exercise. Muscle cross-sections were stained with antibodies against neutrophils (CD66b and MPO and macrophages (CD68. Muscle damage was assessed via creatine kinase and myoglobin in blood serum samples, and muscle soreness was rated on a ten-point pain scale. Results: The resistance exercise protocol stimulated a significant increase in the number of CD66b+ and MPO+ cells when measured 3 h post exercise. Serum creatine kinase, myoglobin and subjective muscle soreness all increased post-exercise. Muscle leucocyte infiltration, creatine kinase, myoglobin and subjective muscle soreness were unaffected by ibuprofen treatment when compared to placebo. There was also no association between increases in inflammatory leucocytes and any other marker of cellular muscle damage. Conclusion: Ibuprofen administration had no effect on the accumulation of neutrophils, markers of muscle damage or muscle soreness during the first 24 h of post-exercise muscle recovery.

  20. Comparison of the efficacy of ibuprofen and belladonna in the control of orthodontic separator pain

    Directory of Open Access Journals (Sweden)

    Harshal Ashok Patil

    2018-01-01

    Full Text Available Background: The purpose of this study was to compare the efficacy of ibuprofen and Belladonna in the control of orthodontic pain and to ascertain the pain relief by Belladonna in comparison with ibuprofen during orthodontic separation. Materials and Methods: Patients, between 20 and 35 years of age, 51 females and 21 males, were included in this study. Patients were randomly divided into two groups; one group was assigned to ibuprofen 400 mg and second group was allocated to Belladonna 6C group. Patients were given two doses of medication of their respective groups, 1 h before placement of elastomeric separators (Ormco Separators, Ormco Corporation, CA, USA which was administered in the department and one dose 6 h after the placement. Pain scores recorded on visual analogue scale (VAS. VAS was a 10 cm scale with millimetre calibration to record their pain at the following intervals, 2 h after placement, 6 h after placement, bedtime, day 1 morning, day 2 morning, day 3 morning and day 5 morning. Results: Post hoc comparisons indicated that there was no difference between the two groups at 2 h (P = 0.77, 6 h (0.073, 1 day (P = 0.120, 2 days (P = 0.283, 3 days (P = 0.363, 5 days (P = 0.622 and 7 days. Conclusion: Ibuprofen and Belladonna 6C are effective and provide adequate analgesia with no statistically significant difference. Lack of adverse effects with Belladonna 6C makes it an effective and viable alternative.

  1. Ibuprofen-conjugated hyaluronate/polygalacturonic acid hydrogel for the prevention of epidural fibrosis.

    Science.gov (United States)

    Lin, Cheng-Yi; Peng, Hsiu-Hui; Chen, Mei-Hsiu; Sun, Jui-Sheng; Chang, Chih-Ju; Liu, Tse-Ying; Chen, Ming-Hong

    2016-05-01

    The formation of fibrous tissue is part of the natural healing response following a laminectomy. Severe scar tissue adhesion, known as epidural fibrosis, is a common cause of failed back surgery syndrome. In this study, by combining the advantages of drug treatment with a physical barrier, an ibuprofen-conjugated crosslinkable polygalacturonic acid and hyaluronic acid hydrogel was developed for epidural fibrosis prevention. Conjugation was confirmed and measured by 1D(1)H NMR spectroscopy.In vitroanalysis showed that the ibuprofen-conjugated polygalacturonic acid-hyaluronic acid hydrogel showed low cytotoxicity. In addition, the conjugated ibuprofen decreased prostaglandin E2production of the lipopolysaccharide-induced RAW264.7 cells. Histological data inin vivostudies indicated that the scar tissue adhesion of laminectomized male adult rats was reduced by the application of our ibuprofen-conjugated polygalacturonic acid-hyaluronic acid hydrogel. Its use also reduced the population of giant cells and collagen deposition of scar tissue without inducing extensive cell recruitment. The results of this study therefore suggest that the local delivery of ibuprofenviaa polygalacturonic acid-hyaluronic acid-based hydrogel reduces the possibility of epidural fibrosis. © The Author(s) 2016.

  2. Thermal and spectroscopic studies on solid ibuprofen complexes of lighter trivalent lanthanides

    International Nuclear Information System (INIS)

    Gálico, D.A.; Holanda, B.B.C.; Guerra, R.B.; Legendre, A.O.; Rinaldo, D.; Treu-Filho, O.; Bannach, G.

    2014-01-01

    Highlights: • Lighter trivalent lanthanide complexes of ibuprofen have been synthesized. • The TG-FTIR allowed the identification of propane as the gas evolved during the thermal decomposition of the neodymium compound. • The thermal analysis provided information about the composition, dehydration, thermal behavior and thermal decomposition of the samples. • The theoretical and experimental spectroscopic studies suggest that the carboxylate group of ibuprofen is coordinated to the metals by a bidentate bond. - Abstract: Solid-state compounds of general formula Ln(L) 3 , in which L is ibuprofen and Ln stands for trivalent La, Ce, Pr, Nd, Sm and Eu, have been synthesized. Simultaneous thermogravimetry and differential thermal analysis (TG-DTA), X-ray powder diffractometry (DRX), complexometry, Fourier-transformed infrared spectroscopy (FTIR) and thermogravimetry coupled to Fourier-transformed infrared spectroscopy (TG-FTIR) were used to characterize these compounds. The results provided information concerning the chemical composition, dehydration, coordination modes of the ligands, crystallinity of the samples, thermal behavior and thermal decomposition of the compounds. The theoretical and experimental spectroscopic studies suggest that ibuprofen coordinates through the carboxylate group as a chelating ligand

  3. Design, Synthesis, and Characterization of Novel Thiol-Derivatized Ibuprofen Monolayer Protected Gold Clusters

    International Nuclear Information System (INIS)

    Lee, K.H.; Lee, K.H.; Lin, Y.Sh.; Huang, P.J.

    2013-01-01

    A series of new thiol-derivatized ibuprofen monolayer protected gold clusters have been prepared by amidation of ibuprofen with alkyl alcohol or aminophenol affording the carboxamide, N-hydroxyalkyl amide 2, and N-hydroxyphenyl amide 6, which were then tosylate with p-toluenesulfonyl chloride at hydroxyl group to give 3 and 7. Reactions of 3 and 7 with NaSH afforded the mercapto derivatives 4 and 8. Conducting Brust’s reaction with a 3:1 mole ratio of thiolate ibuprofen/ AuCl 4 - yielded polydisperse thiol-derivatized ibuprofen-MPCs 5 and 9. All compounds have been identified by NMR, MS, UV, and IR spectroscopies. Compounds 4 and 8 and the MPCs 5 and 9 have been investigated by using the method of 1 H NMR spectroscopy. The broadening of the signals from 0.8 to 2.0 ppm in 1 H NMR spectrum of MPCs 5 and 9 confirmed the success of the conjugation of thiol-containing derivatives with nano gold cluster.

  4. Formulation of Novel Layered Sodium Carboxymethylcellulose Film Wound Dressings with Ibuprofen for Alleviating Wound Pain

    Science.gov (United States)

    Vinklárková, Lenka; Vetchý, David; Bernatonienė, Jurga

    2015-01-01

    Effective assessment and management of wound pain can facilitate both improvements in healing rates and overall quality of life. From a pharmacological perspective, topical application of nonsteroidal anti-inflammatory drugs in the form of film wound dressings may be a good choice. Thus, the aim of this work was to develop novel layered film wound dressings containing ibuprofen based on partially substituted fibrous sodium carboxymethylcellulose (nonwoven textile Hcel NaT). To this end, an innovative solvent casting method using a sequential coating technique has been applied. The concentration of ibuprofen which was incorporated as an acetone solution or as a suspension in a sodium carboxymethylcellulose dispersion was 0.5 mg/cm2 and 1.0 mg/cm2 of film. Results showed that developed films had adequate mechanical and swelling properties and an advantageous acidic surface pH for wound application. An in vitro drug release study implied that layered films retained the drug for a longer period of time and thus could minimize the frequency of changing the dressing. Films with suspended ibuprofen demonstrated higher drug content uniformity and superior in vitro drug release characteristics in comparison with ibuprofen incorporation as an acetone solution. Prepared films could be potential wound dressings for the effective treatment of wound pain in low exuding wounds. PMID:26090454

  5. Ibuprofen is superior to paracetamol for pain relief following third molar removal.

    Science.gov (United States)

    Ferraiolo, Debra M; Veitz-Keenan, Analia

    2014-12-01

    The Cochrane Oral Health Group's Trials Register, the Cochrane Central Register of Controlled Trials (CENTRAL), Medline, Embase and the metaRegister of Controlled Trials were searched with no language restrictions. Randomised controlled double-blinded clinical trials using the third molar model were included. Two review authors independently and in duplicate extracted data. The proportion of patients with at least 50% pain relief (based on total pain relief (TOTPAR) and summed pain intensity difference (SPID) data) was calculated for all three drugs at both two and six hours post-dosing and meta-analysed for comparison. Seven studies involving 2241 patients were included. Two studies were considered to be at low risk of bias, three at high risk and two unclear risk of bias. Ibuprofen was found to be a superior analgesic to paracetamol at several doses, with high quality evidence suggesting that ibuprofen 400 mg is superior to 1000 mg paracetamol based on pain relief (estimated from TOTPAR data) and the use of rescue medication meta-analyses. Risk ratio (RR) for at least 50% pain relief (based on TOTPAR) at six hours was 1.47 (95% confidence interval (CI) 1.28 to 1.69; five trials) favouring 400 mg ibuprofen over 1000 mg paracetamol, RR for not using rescue medication (also favouring ibuprofen) was 1.50 (95% CI 1.25 to 1.79; four trials). For combined drug RR for at least 50% of the maximum pain relief over six hours of 1.77 (95% CI 1.32 to 2.39) (paracetamol 1000 mg and ibuprofen 400 mg) (one trial; moderate quality evidence). RR not using rescue medication 1.60 (95% CI 1.36 to 1.88) (two trials; moderate quality evidence). Adverse events were comparable between the treatment groups, but no formal analysis could be undertaken. There is high quality evidence that ibuprofen is superior to paracetamol at doses of 200 mg to 512 mg and 600 mg to 1000 mg respectively based on pain relief and use of rescue medication data collected at six hours postoperatively. The

  6. A double-blind study comparing ibuprofen 1800 mg or 2400 mg daily and placebo in sports injuries.

    Science.gov (United States)

    Hutson, M A

    1986-01-01

    In a double-blind, placebo-controlled study of forty-six patients with acute ligamentous damage of the knee, ibuprofen in dosages 1800 mg and 2400 mg produced significant improvements in joint mobility, weight bearing ability and match fitness. Joint effusion, pain on stress and pain severity was significantly improved by all three treatments. Only two patients reported side-effects (one while taking placebo and one taking ibuprofen 2400 mg). The study confirmed the efficacy and excellent tolerance to ibuprofen in patients with sports injuries to the knee.

  7. Contribution of microorganisms to non-extractable residue formation during biodegradation of ibuprofen in soil

    Energy Technology Data Exchange (ETDEWEB)

    Nowak, Karolina M., E-mail: karolina.nowak@ufz.de [UFZ, Helmholtz Centre for Environmental Research, Department of Environmental Biotechnology, Permoserstraße 15, 04318 Leipzig (Germany); Department of Environmental Biology and Chemodynamics, Institute for Environmental Research (Biology V), RWTH Aachen University, Worringerweg 1, 52074 Aachen (Germany); Girardi, Cristobal; Miltner, Anja [UFZ, Helmholtz Centre for Environmental Research, Department of Environmental Biotechnology, Permoserstraße 15, 04318 Leipzig (Germany); Gehre, Matthias [UFZ, Helmholtz Centre for Environmental Research, Department of Isotope Biogeochemistry, Permoserstraße 15, 04318 Leipzig (Germany); Schäffer, Andreas [Department of Environmental Biology and Chemodynamics, Institute for Environmental Research (Biology V), RWTH Aachen University, Worringerweg 1, 52074 Aachen (Germany); Kästner, Matthias [UFZ, Helmholtz Centre for Environmental Research, Department of Environmental Biotechnology, Permoserstraße 15, 04318 Leipzig (Germany)

    2013-02-15

    Non-extractable residues (NER) formed during biodegradation of organic contaminants in soil are considered to be mainly composed of parent compounds or their primary metabolites with hazardous potential. However, in the case of biodegradable organic compounds, the soil NER may also contain microbial biomass components, for example fatty acids (FA) and amino acids (AA). After cell death, these biomolecules are subsequently incorporated into non-living soil organic matter (SOM) and are stabilised ultimately forming hardly extractable residues of biogenic origin. We investigated biodegradation of {sup 13}C{sub 6}-ibuprofen, in particular the metabolic incorporation of the {sup 13}C-label into FA and AA and their fate in soil over 90 days. {sup 13}C-FA and {sup 13}C-AA amounts in the living microbial biomass fraction initially increased, then decreased over time and were continuously incorporated into the non-living SOM pool. The {sup 13}C-FA in the non-living SOM remained stable from day 59 whereas the contents of {sup 13}C-AA slightly increased until the end. After 90 days, nearly all NER were biogenic as they were made up almost completely by natural biomass compounds. The presented data demonstrated that the potential environmental risks related to the ibuprofen-derived NER are overestimated. - Highlights: ► Biogenic residue formation during microbial degradation of ibuprofen was studied. ► Nearly all non-extractable residues derived from ibuprofen were biogenic. ► Fatty acids and amino acids formed biogenic non-extractable residues and were stabilised in soil. ► Environmental risks of ibuprofen-derived non-extractable residues are overestimated.

  8. Adsorption of ibuprofen from aqueous solution on chemically surface-modified activated carbon cloths

    Directory of Open Access Journals (Sweden)

    Hanen Guedidi

    2017-05-01

    Full Text Available This study aims to investigate the performance of an activated carbon cloth for adsorption of ibuprofen. The cloth was oxidized by a NaOCl solution (0.13 mol L−1 or thermally treated under N2 (700 °C for 1 hour. The raw and modified cloths were characterized by N2 adsorption–desorption measurement at 77 K, CO2 adsorption at 273 K, Boehm titrations, pHPZC measurements, X-ray Photoelectron Spectroscopy analysis, and by infrared spectroscopy. The NaOCl treatment increases the acidic sites, mostly creating phenolic and carboxylic groups and decreases both the specific surface area and slightly the micropore volume. However, the thermal treatment at 700 °C under N2 induced a slight increase in the BET specific surface area and yielded to the only increase in the carbonyl group content. Ibuprofen adsorption studies of kinetics and isotherms were carried out at pH = 3 and 7. The adsorption properties were correlated to the cloth porous textures, surface chemistry and pH conditions. The isotherms of adsorption were better reproduced by Langmuir–Freundlich models at 298, 313 and 328 K. The adsorption of ibuprofen on the studied activated carbon cloths at pH 3 was an endothermic process. The pore size distributions of all studied ibuprofen-loaded fabrics were determined by DFT method to investigate the accessible porosity of the adsorbate. Both treatments do not influence the kind of micropores where the adsorption of ibuprofen occurred.

  9. A clinical trial comparing Lanconone® with ibuprofen for rapid relief in acute joint pain.

    Science.gov (United States)

    Girandola, Robert N; Srivastava, Shalini; Loullis, Costas C

    2016-04-06

    To study the effect of Lanconone® (1000 mg) on acute pain on exertion as compared to the standard of care, Ibuprofen (400 mg). The study recruited 72 subjects diagnosed with mild to moderate knee joint pain on exertion. Subjects with Pain Visual Analogue Scale of more than 40 mm were included. Uphill walking was provided as the stressor using Naughton's protocol on a treadmill. The subjects walked for 10 minutes continuously followed by a rest period and baseline pain score for index knee joint was recorded. Subjects were administered a single dose of Lanconone® (1000 mg)/Ibuprofen (400 mg). Thereafter the same stressor was provided at 0.5, 1, 2, 3, 4, and 6 hours, subsequently, pain scores were recorded on a visual analogue scale. Double stopwatch method was used to evaluate the onset of pain relief and time taken to meaningful pain relief. Both Lanconone® and Ibuprofen showed the first perceived pain relief at 65.31 ± 35.57 mins as compared to 60.82 ± 32.56 mins respectively. The mean time taken to experience meaningful pain relief in Lanconone® group was 196.59 ± 70.85 mins compared to 167.13 ± 71.41 mins amongst Ibuprofen group. The meaningful pain relief continued for 6 hours. The current study successfully demonstrated rapid pain-relieving potential of Lanconone® which was comparable to Ibuprofen. No adverse event related to the interventions was reported in the study. Clinical trials.gov NCT02417506 . 21 January 2015.

  10. Application of non-thermal plasma reactor and Fenton reaction for degradation of ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Marković, Marijana [Center of Chemistry, Institute of Chemistry, Technology and Metallurgy, University of Belgrade, Studentski trg 12-16, 11000 Belgrade (Serbia); Jović, Milica; Stanković, Dalibor [Innovation Center, Faculty of Chemistry, University of Belgrade, P.O. Box 51, 11058 Belgrade 118 (Serbia); Kovačević, Vesna [Faculty of Physics, University of Belgrade, P.O. Box 44, 11000 Belgrade (Serbia); Roglić, Goran [Faculty of Chemistry, University of Belgrade, P.O. Box 51, 11058 Belgrade 118 (Serbia); Gojgić-Cvijović, Gordana [Center of Chemistry, Institute of Chemistry, Technology and Metallurgy, University of Belgrade, Studentski trg 12-16, 11000 Belgrade (Serbia); Manojlović, Dragan, E-mail: manojlo@chem.bg.ac.rs [Faculty of Chemistry, University of Belgrade, P.O. Box 51, 11058 Belgrade 118 (Serbia)

    2015-02-01

    Pharmaceutical compounds have been detected frequently in surface and ground water. Advanced Oxidation Processes (AOPs) were reported as very efficient for removal of various organic compounds. Nevertheless, due to incomplete degradation, toxic intermediates can induce more severe effects than the parent compound. Therefore, toxicity studies are necessary for the evaluation of possible uses of AOPs. In this study the effectiveness and capacity for environmental application of three different AOPs were estimated. They were applied and evaluated for removal of ibuprofen from water solutions. Therefore, two treatments were performed in a non-thermal plasma reactor with dielectric barrier discharge with and without a homogenous catalyst (Fe{sup 2+}). The third treatment was the Fenton reaction. The degradation rate of ibuprofen was measured by HPLC-DAD and the main degradation products were identified using LC–MS TOF. Twelve degradation products were identified, and there were differences according to the various treatments applied. Toxicity effects were determined with two bioassays: Vibrio fischeri and Artemia salina. The efficiency of AOPs was demonstrated for all treatments, where after 15 min degradation percentage was over 80% accompanied by opening of the aromatic ring. In the treatment with homogenous catalyst degradation reached 99%. V. fischeri toxicity test has shown greater sensitivity to ibuprofen solution after the Fenton treatment in comparison to A. salina. - Highlights: • Twelve ibuprofen degradation products were identified in total. • The degradation percentage differed between treatments (DBD/Fe{sup 2+} was 99%). • In DBD/Fe{sup 2+} only aliphatic degradation products were identified. • V. fischeri was sensitive to ibuprofen solution after the Fenton treatment. • A. salina showed no toxic effect when exposed to all post treatment solutions.

  11. Contribution of microorganisms to non-extractable residue formation during biodegradation of ibuprofen in soil

    International Nuclear Information System (INIS)

    Nowak, Karolina M.; Girardi, Cristobal; Miltner, Anja; Gehre, Matthias; Schäffer, Andreas; Kästner, Matthias

    2013-01-01

    Non-extractable residues (NER) formed during biodegradation of organic contaminants in soil are considered to be mainly composed of parent compounds or their primary metabolites with hazardous potential. However, in the case of biodegradable organic compounds, the soil NER may also contain microbial biomass components, for example fatty acids (FA) and amino acids (AA). After cell death, these biomolecules are subsequently incorporated into non-living soil organic matter (SOM) and are stabilised ultimately forming hardly extractable residues of biogenic origin. We investigated biodegradation of 13 C 6 -ibuprofen, in particular the metabolic incorporation of the 13 C-label into FA and AA and their fate in soil over 90 days. 13 C-FA and 13 C-AA amounts in the living microbial biomass fraction initially increased, then decreased over time and were continuously incorporated into the non-living SOM pool. The 13 C-FA in the non-living SOM remained stable from day 59 whereas the contents of 13 C-AA slightly increased until the end. After 90 days, nearly all NER were biogenic as they were made up almost completely by natural biomass compounds. The presented data demonstrated that the potential environmental risks related to the ibuprofen-derived NER are overestimated. - Highlights: ► Biogenic residue formation during microbial degradation of ibuprofen was studied. ► Nearly all non-extractable residues derived from ibuprofen were biogenic. ► Fatty acids and amino acids formed biogenic non-extractable residues and were stabilised in soil. ► Environmental risks of ibuprofen-derived non-extractable residues are overestimated

  12. Application of non-thermal plasma reactor and Fenton reaction for degradation of ibuprofen

    International Nuclear Information System (INIS)

    Marković, Marijana; Jović, Milica; Stanković, Dalibor; Kovačević, Vesna; Roglić, Goran; Gojgić-Cvijović, Gordana; Manojlović, Dragan

    2015-01-01

    Pharmaceutical compounds have been detected frequently in surface and ground water. Advanced Oxidation Processes (AOPs) were reported as very efficient for removal of various organic compounds. Nevertheless, due to incomplete degradation, toxic intermediates can induce more severe effects than the parent compound. Therefore, toxicity studies are necessary for the evaluation of possible uses of AOPs. In this study the effectiveness and capacity for environmental application of three different AOPs were estimated. They were applied and evaluated for removal of ibuprofen from water solutions. Therefore, two treatments were performed in a non-thermal plasma reactor with dielectric barrier discharge with and without a homogenous catalyst (Fe 2+ ). The third treatment was the Fenton reaction. The degradation rate of ibuprofen was measured by HPLC-DAD and the main degradation products were identified using LC–MS TOF. Twelve degradation products were identified, and there were differences according to the various treatments applied. Toxicity effects were determined with two bioassays: Vibrio fischeri and Artemia salina. The efficiency of AOPs was demonstrated for all treatments, where after 15 min degradation percentage was over 80% accompanied by opening of the aromatic ring. In the treatment with homogenous catalyst degradation reached 99%. V. fischeri toxicity test has shown greater sensitivity to ibuprofen solution after the Fenton treatment in comparison to A. salina. - Highlights: • Twelve ibuprofen degradation products were identified in total. • The degradation percentage differed between treatments (DBD/Fe 2+ was 99%). • In DBD/Fe 2+ only aliphatic degradation products were identified. • V. fischeri was sensitive to ibuprofen solution after the Fenton treatment. • A. salina showed no toxic effect when exposed to all post treatment solutions

  13. GC-MS and GC-MS/MS measurement of ibuprofen in 10-μL aliquots of human plasma and mice serum using [α-methylo-2H3]ibuprofen after ethyl acetate extraction and pentafluorobenzyl bromide derivatization: Discovery of a collision energy-dependent H/D isotope effect and pharmacokinetic application to inhaled ibuprofen-arginine in mice.

    Science.gov (United States)

    Tsikas, Dimitrios; Kayacelebi, Arslan Arinc; Hanff, Erik; Mitschke, Anja; Beckmann, Bibiana; Tillmann, Hanns-Christian; Gutzki, Frank-Mathias; Müller, Meike; Bernasconi, Corrado

    2017-02-01

    GC-MS and GC-MS/MS methods were developed and validated for the quantitative determination of ibuprofen (d 0 -ibuprofen), a non-steroidal anti-inflammatory drug (NSAID), in human plasma using α-methyl- 2 H 3 -4-(isobutyl)phenylacetic acid (d 3 -ibuprofen) as internal standard. Plasma (10μL) was diluted with acetate buffer (80μL, 1M, pH 4.9) and d 0 - and d 3 -ibuprofen were extracted with ethyl acetate (2×500μL). After solvent evaporation d 0 - and d 3 -ibuprofen were derivatized in anhydrous acetonitrile by using pentafluorobenzyl (PFB) bromide and N,N-diisopropylethylamine as the base catalyst. Under electron-capture negative-ion chemical ionization (ECNICI), the PFB esters of d 0 - and d 3 -ibuprofen readily ionize to form their carboxylate anions [M-PFB] - at m/z 205 and m/z 208, respectively. Collision-induced dissociation (CID) of m/z 205 and m/z 208 resulted in the formation of the anions at m/z 161 and m/z 164, respectively, due to neutral loss of CO 2 (44 Da). A collision energy-dependent H/D isotope effect was observed, which involves abstraction/elimination of H - from d 0 -ibuprofen and D - from d 3 -ibuprofen and is minimum at a CE value of 5eV. Quantitative GC-MS determination was performed by selected-ion monitoring of m/z 205 and m/z 208. Quantitative GC-MS/MS determination was performed by selected-reaction monitoring of the mass transitions m/z 205 to m/z 161 for d 0 -ibuprofen and m/z 208 to m/z 164 for d 3 -ibuprofen. In a therapeutically relevant concentration range (0-1000μM) d 0 -ibuprofen added to human plasma was determined with accuracy (recovery, %) and imprecision (relative standard deviation, %) ranging between 93.7 and 110%, and between 0.8 and 4.9%, respectively. GC-MS (y) and GC-MS/MS (x) yielded almost identical results (y=4.00+0.988x, r 2 =0.9991). In incubation mixtures of arachidonic acid (10μM), d 3 -ibuprofen (10μM) or d 0 -ibuprofen (10μM) with ovine cyclooxygenase (COX) isoforms 1 and 2, the concentration of d 3

  14. Possession experiences in dissociative identity disorder: a preliminary study.

    Science.gov (United States)

    Ross, Colin A

    2011-01-01

    Dissociative trance disorder, which includes possession experiences, was introduced as a provisional diagnosis requiring further study in the Diagnostic and Statistical Manual of Mental Disorders (4th ed.). Consideration is now being given to including possession experiences within dissociative identity disorder (DID) in the Diagnostic and Statistical Manual of Mental Disorders (5th ed.), which is due to be published in 2013. In order to provide empirical data relevant to the relationship between DID and possession states, I analyzed data on the prevalence of trance, possession states, sleepwalking, and paranormal experiences in 3 large samples: patients with DID from North America; psychiatric outpatients from Shanghai, China; and a general population sample from Winnipeg, Canada. Trance, sleepwalking, paranormal, and possession experiences were much more common in the DID patients than in the 2 comparison samples. The study is preliminary and exploratory in nature because the samples were not matched in any way.

  15. Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

    Directory of Open Access Journals (Sweden)

    Hugo Almeida

    2012-09-01

    Full Text Available Ibuprofen is one of the most important non-steroidal anti-inflammatory drugs used in the treatment of inflammatory diseases. In its pure state, ibuprofen presents poor physical and mechanical characteristics and its use in solid dosage forms needs the addition of excipients that improve these properties. The selection of the best excipients and the most suitable pharmaceutical dosage form to carry ibuprofen is very important for the industrial success of this drug. Given these factors, lipid microparticles and solid dispersions of ibuprofen with cetyl alcohol, stearic acid, and hydrogenated castor oil were prepared. These formulations were intended to improve the physical and mechanical characteristics and to sustain the release of this drug. Physical mixtures were also prepared with the same ingredients in similar proportions. The solid dispersions of ibuprofen/stearic acid and ibuprofen/hydrogenated castor oil showed the best flow characteristics compared with pure ibuprofen. Further, gelatin capsules filled with lipid microparticles and solid dispersions were submitted to dissolution tests in order to study the influence of the prepared systems in the release profiles of ibuprofen. Prolonged release of ibuprofen was achieved with the lipid microparticles and solid dispersions prepared with the different types of excipients.O ibuprofeno é um dos antiinflamatórios não esteróides mais utilizados no tratamento de patologias associadas a processos inflamatórios. Este fármaco, quando no seu estado puro, apresenta características físicas e mecânicas pouco satisfatórias e a sua utilização em formas sólidas só é possível se forem adicionados excipientes que permitam melhorar estas propriedades. A seleção dos excipientes ideais e da forma farmacêutica mais adequada para veicular o ibuprofeno é fundamental para o sucesso industrial deste fármaco. Tendo em conta estes fatores, prepararam-se micropartículas lipídicas e dispersões s

  16. Influence of acetaminophen and ibuprofen on in vivo patellar tendon adaptations to knee extensor resistance exercise in older adults

    DEFF Research Database (Denmark)

    Carroll, Chad C; Dickinson, Jared M; Lemoine, Jennifer K

    2011-01-01

    Millions of older individuals consume acetaminophen or ibuprofen daily and these same individuals are encouraged to participate in resistance training. Several in vitro studies suggest that cyclooxygenase-inhibiting drugs can alter tendon metabolism and may influence adaptations to resistance...... training. Thirty-six individuals were randomly assigned to a Placebo (67±2y), Acetaminophen (64±1y; 4000mg(.)d(-1)), or Ibuprofen (64±1y; 1200mg(.)d(-1)) group in a double-blind manner and completed 12-weeks of knee extensor resistance-training. Before and after training in vivo patellar tendon properties......, and this response was not influenced with ibuprofen consumption. Mean tendon CSA increased with training in the Acetaminophen group (3%, p0.05) with training in the Placebo group. These responses were generally uninfluenced by ibuprofen consumption. In the Acetaminophen group, tendon deformation and strain...

  17. Effect of Secondary Equilibria on the Adsorption of Ibuprofen Enantiomers on a Chiral Stationary Phase with a Grafted Antibiotic Eremomycin

    Science.gov (United States)

    Reshetova, E. N.; Asnin, L. D.; Kachmarsky, K.

    2018-02-01

    The chromatographic separation of ibuprofen enantiomers on a Nautilus-E chiral stationary phase with a grafted eremomycin antibiotic at high column loading is accompanied by distortion of the shape of chromatographic peaks. A model is proposed to explain this phenomenon. A number of factors are considered in the model: the ionization of ibuprofen in the mobile phase, the pH change in the mass transfer zone caused by ionization, and competitive adsorption involving buffer components. Simulations performed using this model within the theory of nonequilibrium chromatography allow the shape of chromatograms for large amounts of S- and R-ibuprofen samples to be predicted. The adsorption mechanism is found to be mainly ion-exchange. The contribution from the molecular adsorption of ibuprofen to the total retention is shown to be several percent.

  18. An unusual finding of massive pulmonary embolism in a patient during treatment with high-dose ibuprofen.

    Science.gov (United States)

    Bilora, Franca; Adamo, Angelo; Pomerri, Fabio; Prandoni, Paolo

    2016-02-01

    Non-steroidal anti-inflammatory drugs have been associated with an increased risk of venous thromboembolism. We report for the first time, the case of a patient who developed massive pulmonary embolism after a long period of treatment with high doses of ibuprofen. A 65-year-old woman was admitted with severe dyspnea while on treatment with high doses of ibuprofen for diffuse spine pain due to arthrosis. A spiral computed tomography showed a massive pulmonary embolism. No other explanation for the thromboembolic disorder was found. She was successfully treated with therapeutic doses of low-molecular-weight heparin followed by rivaroxaban. Ibuprofen was discontinued and replaced by tramadol. High-dose ibuprofen is likely to have accounted for the life-threatening thromboembolic disorder.

  19. Chiral auxiliary-mediated enantioenrichment of (+-)-ibuprofen, under Steglich conditions, with secondary alcohols derived from (R)-carvone

    Energy Technology Data Exchange (ETDEWEB)

    Amongero, Marcela; Visnovezky, Damian; Kaufman, Teodoro S., E-mail: kaufman@iquir-conicet.gov.a [Instituto de Quimica Rosario (IQUIR, CONICET-UNR) (Argentina); Universidad Nacional de Rosario (Argentina)

    2010-07-01

    The synthesis of a series of chiral secondary alcohols derived from (R)-carvone, and the stereochemical outcome of their reaction with (+-)-ibuprofen, is reported. The racemic drug was transformed into the corresponding diastereomeric esters mediated by DCC/DMAP, affording up to 5.7:1 diastereomeric ratios of the esters derived from either (S)- or (R)-ibuprofen, depending on the type of chiral auxiliary employed. (author)

  20. Ibuprofen slows migration and inhibits bowel colonization by enteric nervous system precursors in zebrafish, chick and mouse

    Science.gov (United States)

    Schill, Ellen Merrick; Lake, Jonathan I.; Tusheva, Olga A.; Nagy, Nandor; Bery, Saya K.; Foster, Lynne; Avetisyan, Marina; Johnson, Stephen L.; Stenson, William F.; Goldstein, Allan M.; Heuckeroth, Robert O.

    2016-01-01

    Hirschsprung Disease (HSCR) is a potentially deadly birth defect characterized by the absence of the enteric nervous system (ENS) in distal bowel. Although HSCR has clear genetic causes, no HSCR-associated mutation is 100% penetrant, suggesting gene-gene and gene-environment interactions determine HSCR occurrence. To test the hypothesis that certain medicines might alter HSCR risk we treated zebrafish with medications commonly used during early human pregnancy and discovered that ibuprofen caused HSCR-like absence of enteric neurons in distal bowel. Using fetal CF-1 mouse gut slice cultures, we found that ibuprofen treated enteric neural crest-derived cells (ENCDC) had reduced migration, fewer lamellipodia and lower levels of active RAC1/CDC42. Additionally, inhibiting ROCK, a RHOA effector and known RAC1 antagonist, reversed ibuprofen effects on migrating mouse ENCDC in culture. Ibuprofen also inhibited colonization of Ret+/− mouse bowel by ENCDC in vivo and dramatically reduced bowel colonization by chick ENCDC in culture. Interestingly, ibuprofen did not affect ENCDC migration until after at least three hours of exposure. Furthermore, mice deficient in Ptgs1 (COX 1) and Ptgs2 (COX 2) had normal bowel colonization by ENCDC and normal ENCDC migration in vitro suggesting COX-independent effects. Consistent with selective and strain specific effects on ENCDC, ibuprofen did not affect migration of gut mesenchymal cells, NIH3T3, or WT C57BL/6 ENCDC, and did not affect dorsal root ganglion cell precursor migration in zebrafish. Thus, ibuprofen inhibits ENCDC migration in vitro and bowel colonization by ENCDC in vivo in zebrafish, mouse and chick, but there are cell type and strain specific responses. These data raise concern that ibuprofen may increase Hirschsprung disease risk in some genetically susceptible children. PMID:26586201

  1. Chiral auxiliary-mediated enantioenrichment of (+-)-ibuprofen, under Steglich conditions, with secondary alcohols derived from (R)-carvone

    International Nuclear Information System (INIS)

    Amongero, Marcela; Visnovezky, Damian; Kaufman, Teodoro S.

    2010-01-01

    The synthesis of a series of chiral secondary alcohols derived from (R)-carvone, and the stereochemical outcome of their reaction with (±)-ibuprofen, is reported. The racemic drug was transformed into the corresponding diastereomeric esters mediated by DCC/DMAP, affording up to 5.7:1 diastereomeric ratios of the esters derived from either (S)- or (R)-ibuprofen, depending on the type of chiral auxiliary employed. (author)

  2. Effects of Ibuprofen and Resistance Training on Bone and Muscle: A Randomized Controlled Trial in Older Women.

    Science.gov (United States)

    Duff, Whitney R D; Chilibeck, Philip D; Candow, Darren G; Gordon, Julianne J; Mason, Riley S; Taylor-Gjevre, Regina; Nair, Bindu; Szafron, Michael; Baxter-Jones, Adam; Zello, Gordon A; Kontulainen, Saija A

    2017-04-01

    Resistance training with ibuprofen supplementation may improve musculoskeletal health in postmenopausal women. The study purpose was to determine the efficacy of resistance training and ibuprofen supplementation on bone and muscle properties in postmenopausal women. Participants (n = 90, 65.3 ± 4.9 yr) were randomly assigned to: supervised resistance training or stretching (placebo-exercise) with postexercise ibuprofen (400 mg) or placebo supplementation for 3 d·wk (9 months). Baseline and postintervention measurements included distal and shaft scans of the forearm and lower leg using peripheral quantitative computed tomography. Distal site outcomes included cross-sectional area, content, and density for total and trabecular bone, as well as estimated bone strength in compression. Shaft site outcomes included total bone area; cortical bone area, content, and density; estimated bone strength in torsion; and muscle area and density. Exercise-supplement-time interactions for total bone content at the distal radius (P = 0.009) and cortical density at the radius shaft (P = 0.038) were significant. Resistance training with ibuprofen decreased total bone content (-1.5%) at the distal radius in comparison to the resistance training (0.6%; P = 0.032) and ibuprofen alone (0.5%; P = 0.050). Change in cortical density at the radius shaft differed between the stretching with placebo and ibuprofen supplementation groups (-1.8% vs 1.1%; P = 0.050). Resistance training preserved muscle density in the lower leg more so than stretching (-3.1% vs -5.4%; P = 0.015). Ibuprofen consumed immediately after resistance training had a deleterious effect on bone mineral content at the distal radius, whereas resistance training or ibuprofen supplementation individually prevented bone loss. Resistance training prevented muscle density decline in the lower leg.

  3. Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate.

    Science.gov (United States)

    Qu, Li; Zhou, Qi Tony; Gengenbach, Thomas; Denman, John A; Stewart, Peter J; Hapgood, Karen P; Gamlen, Michael; Morton, David A V

    2015-05-01

    Intensive dry powder coating (mechanofusion) with tablet lubricants has previously been shown to give substantial powder flow improvement. This study explores whether the mechanofusion of magnesium stearate (MgSt), on a fine drug powder can substantially improve flow, without preventing the powder from being directly compacted into tablets. A fine ibuprofen powder, which is both cohesive and possesses a low-melting point, was dry coated via mechanofusion with between 0.1% and 5% (w/w) MgSt. Traditional low-shear blending was also employed as a comparison. No significant difference in particle size or shape was measured following mechanofusion. For the low-shear blended powders, only marginal improvement in flowability was obtained. However, after mechanofusion, substantial improvements in the flow properties were demonstrated. Both XPS and ToF-SIMS demonstrated high degrees of a nano-scale coating coverage of MgSt on the particle surfaces from optimized mechanofusion. The study showed that robust tablets were produced from the selected mechanofused powders, at high-dose concentration and tablet tensile strength was further optimized via addition of a Polyvinylpyrrolidone (PVP) binder (10% w/w). The tablets with the mechanofused powder (with or without PVP) also exhibited significantly lower ejection stress than those made of the raw powder, demonstrating good lubrication. Surprisingly, the release rate of drug from the tablets made with the mechanofused powder was not retarded. This is the first study to demonstrate such a single-step dry coating of model drug with MgSt, with promising flow improvement, flow-aid and lubrication effects, tabletability and also non-inhibited dissolution rate.

  4. Association Between Ibuprofen Use and Severity of Surgically Managed Posttonsillectomy Hemorrhage.

    Science.gov (United States)

    Mudd, Pamela A; Thottathil, Princy; Giordano, Terri; Wetmore, Ralph F; Elden, Lisa; Jawad, Abbas F; Ahumada, Luis; Gálvez, Jorge A

    2017-07-01

    Ibuprofen used in postoperative management of pain after tonsillectomy has not been shown to increase the overall risk for posttonsillectomy hemorrhage (PTH). The severity of bleeding is difficult to quantify but may be a more important outcome to measure. To evaluate the association between ibuprofen use and severity of PTH using transfusion events as a marker of severity. This retrospective cohort study identified 8868 patients who underwent tonsillectomy from January 20, 2011, through June 30, 2014, at the tertiary academic Children's Hospital of Philadelphia. Of these patients, 6710 met the inclusion criteria. Data were collected using electronic database acquisition and query. Multivariate analysis was performed to identify independent prognostic factors for PTH and receipt of transfusion. Of the 6710 patients who met criteria for analysis (3454 male [51.5%] and 3256 female [48.5%]; median age, 5.4 years [interquartile range, 3.7-8.2 years]), 222 (3.3%) presented with PTH that required surgical control (sPTH). A total of 15 of the 8868 patients required transfusion for an overall risk for transfusion after tonsillectomy of 0.2%. Fifteen of 222 patients undergoing sPTH (6.8%) received transfusions. No significant independent increased risk for sPTH was associated with use of ibuprofen (adjusted odds ratio [OR], 0.90; 95% CI, 0.68-1.19). A significant independent association was found in the risk for sPTH in patients 12 years or older (adjusted OR, 2.74; 95% CI, 1.99-3.76) and in patients with a history of recurrent tonsillitis (adjusted OR, 1.52; 95% CI, 1.12-2.06). When using transfusion rates as a surrogate for severity of sPTH, transfusion increased by more than 3-fold among ibuprofen users compared with nonusers (adjusted OR, 3.16; 95% CI, 1.01-9.91), and the upper limit of the 95% CI suggests the difference could be nearly 10 times greater. The risk for sPTH is not increased with use of postoperative ibuprofen but is increased in patients 12 years or older

  5. Crystal engineering of ibuprofen compounds: From molecule to crystal structure to morphology prediction by computational simulation and experimental study

    Science.gov (United States)

    Zhang, Min; Liang, Zuozhong; Wu, Fei; Chen, Jian-Feng; Xue, Chunyu; Zhao, Hong

    2017-06-01

    We selected the crystal structures of ibuprofen with seven common space groups (Cc, P21/c, P212121, P21, Pbca, Pna21, and Pbcn), which was generated from ibuprofen molecule by molecular simulation. The predicted crystal structures of ibuprofen with space group P21/c has the lowest total energy and the largest density, which is nearly indistinguishable with experimental result. In addition, the XRD patterns for predicted crystal structure are highly consistent with recrystallization from solvent of ibuprofen. That indicates that the simulation can accurately predict the crystal structure of ibuprofen from the molecule. Furthermore, based on this crystal structure, we predicted the crystal habit in vacuum using the attachment energy (AE) method and considered solvent effects in a systematic way using the modified attachment energy (MAE) model. The simulation can accurately construct a complete process from molecule to crystal structure to morphology prediction. Experimentally, we observed crystal morphologies in four different polarity solvents compounds (ethanol, acetonitrile, ethyl acetate, and toluene). We found that the aspect ratio decreases of crystal habits in this ibuprofen system were found to vary with increasing solvent relative polarity. Besides, the modified crystal morphologies are in good agreement with the observed experimental morphologies. Finally, this work may guide computer-aided design of the desirable crystal morphology.

  6. The modifying effect of ibuprofen on total body irradiation-induced elevation of oxidative reactions in male hamsters

    International Nuclear Information System (INIS)

    Dokmeci, D.; Akpolat, M.; Aydogdu, N.; Uzal, C.; Turan, N.F.

    2004-01-01

    Radiation therapy plays an important role in curative and palliative treatments of malignant diseases. Because of the lipid component in the membrane, lipid peroxidation has been reported to be particularly susceptible to radiation damage. However, lipid peroxidation is reversed by cellular defense mechanisms, and the use of various antioxidants involved in these mechanisms have recently been suggested to be beneficial. It is known that ibuprofen has antioxidative and/or free radical scavenging activities. Our purpose is to examine the antioxidant capacity of ibuprofen in hamsters undergoing total body irradiation (TBI). Ibuprofen was given by gavage at dose of 10 mg/kg for 15 consecutive days. After this period, animals were exposed to TBI 60 Co gamma irradiation with a single dose of 8 Gy. After 24 h radiation exposure, the hamsters were killed and samples were taken from blood. Plasma thiobarbituric acid reactive substances (TBARS) increased significantly after radiation exposure, and ibuprofen diminished the amounts of TBARS. Significant protection of the radiation-induced changes in the activities of superoxide dismutase (SOD) and catalase was also recorded in the blood of ibuprofen-treated and -irradiated hamsters. These results suggest that ibuprofen with its antioxidant capacity could play a modulatory role against cellular damage effected by free radicals induced by TBI. (author)

  7. Study of the Combined Effect of Ibuprofen and Cholesterol on the Microviscosity and Ordering of Model Lipid Membranes by Timeresolved Measurement of Fluorescence Anisotropy Decay

    Science.gov (United States)

    Yefimova, S. L.; Tkacheva, T. N.; Kasian, N. A.

    2017-05-01

    The timeresolved fluorescence anisotropy decay of perylene incorporated into the lipid Ladipalmitoylphosphatidylch oline (DPPC) membrane has been studied to evaluate the membranotropic action of the nonsteroidal antiinflammatory drug, ibuprofen, and the combined effect of ibuprofen and cholesterol. The rotation correlation times (φ) and limiting anisotropy (r∞ ) permit an independent estimation of the effects of these additives on the microviscosity and ordering of model lipid membranes in different phase states. Ibuprofen was shown to cause a significant decrease in the DPPC membrane microviscosity in the gel phase with hardly any effect on the liquidcrystal phase. However, in both phases, ibuprofen diminishes the ordering of the lipid hydrophobic chains. A marked additive effect is noted when ibuprofen is embedded in the liquid membrane enriched with cholesterol, which manifests itself in substantial fluidization and disordering or the liquid membrane by the action of the components on the lipid membrane. Ibuprofen in the liquidcrystal phase causes leveling of the fluidizing and ordering effects of cholesterol.

  8. Use of paracetamol, ibuprofen or aspirin in pregnancy and risk of cerebral palsy in the child

    DEFF Research Database (Denmark)

    Petersen, Tanja Gram; Liew, Zeyan; Nybo Andersen, Anne-Marie

    2018-01-01

    Background: It has been debated whether mild analgesics, mainly paracetamol, adversely affect aspects of neurodevelopment. We examined whether mother's use of paracetamol, aspirin or ibuprofen in pregnancy is associated with increased risk of cerebral palsy (CP) in the child. Method: We included...... registers. We estimated the average causal effect of analgesics on risk of CP using marginal structural models with stabilized inverse probability weights. Results: Paracetamol use was reported in 49% of all pregnancies, aspirin in 3% and ibuprofen in 4%. Prenatal exposure to paracetamol ever in pregnancy......% CI: 1.0-2.5). Children ever prenatally exposed to aspirin in pregnancy had an elevated risk of bilateral spastic CP (aOR 2.4, 95% CI: 1.1-5.3) compared with unexposed. Conclusion: We observed an increased risk of spastic CP in children prenatally exposed to paracetamol and aspirin. Although we...

  9. Potentiometric determination of ibuprofen, indomethacin and naproxen using an artificial neural network calibration

    Directory of Open Access Journals (Sweden)

    A. HAKAN AKTAŞ

    2008-01-01

    Full Text Available In this study, three anti-inflammatory agents, namely ibuprofen, indomethacin and naproxen, were titrated potentiometrically using tetrabutylammonium hydroxide in acetonitrile solvent under a nitrogen atmosphere at 25 °C. MATLAB 7.0 software was applied for data treatment as a multivariate calibration tool in the potentiometric titration procedure. An artificial neural network (ANN was used as a multivariate calibration tool in the potentiometric titration to model the complex non-linear relationship between ibuprofen, indomethacin and naproxen concentrations and the millivolt (mV of the solutions measured after the addition of different volumes of the titrant. The optimized network predicted the concentrations of agents in synthetic mixtures. The results showed that the employed ANN can precede the titration data with an average relative error of prediction of less than 2.30 %.

  10. Experimental substantiation of effectively administration of vinboron for analgesic activity increase of ibuprofen

    Directory of Open Access Journals (Sweden)

    F. V. Hladkykh

    2016-12-01

    Full Text Available Background. The increase of NSAIDs safety is current direction of modern pharmacology, because of so-called "class-specific" adverse reactions, which are common to this class, and the leading place among them is occupied by gastro-intestinal toxicity. In previous studies we have proved the ability of vinboron to neutralize ulcerogenic effect of ibuprofen (Hladkykh F.V. and al., 2014. The presence of the proven analgesic activity in the domestic antispasmodics (Stepaniuk H.I. and al., 2007 serves as the basis for research of vinboron action on analgesic aspect of ibuprofen pharmacotherapeutic effec. Aim is to conduct research in silico of the relation «molecular structure – anelgetic activity» of vinboron and to prove experimentally in vivo the practicability of vinboron using with the aim to increase the analgesic activity of ibuprofen on the model of adjuvant arthritis in rats. Materials and methods. The study of the relation «molecular structure – activity anelgetic» of vinboron was conducted in silico by PASS- analysis of biological activity spectrum. The analysis was set online with direct insertion of structural formula of vinboron in browser using Marvin JS web-resource «PASS Online» (http://www.way2drug.com/passonline. Analgesic activity in vivo was studied on the model of acute thermal pain, which was simulated in the conventional behavioral test of nociception «Hot plate». The lag of pain reaction was determined at the beginning («0» day, on 7, 14, 21 and 28 days of experiment. Results and discussion. According to the PASS-forecast the mechanisms of vinboron analgesic activity is caused by agonism towards the vanilloid (TRPV1 receptors (Pa=0,490; Pi=0,008, agonism to the μ (mu – receptor (Pa=0,323; Pi=0,036, inhibition of GABA (Pa=0,329; Pi=0,089 and others. Experimental studies have shown that the combined administration of ibuprofen and vinboron analgesic activity was higher than the results by ibuprofen monotherapy

  11. Handling Ibuprofen increases pain tolerance and decreases perceived pain intensity in a cold pressor test.

    Directory of Open Access Journals (Sweden)

    Abraham M Rutchick

    Full Text Available Pain contributes to health care costs, missed work and school, and lower quality of life. Extant research on psychological interventions for pain has focused primarily on developing skills that individuals can apply to manage their pain. Rather than examining internal factors that influence pain tolerance (e.g., pain management skills, the current work examines factors external to an individual that can increase pain tolerance. Specifically, the current study examined the nonconscious influence of exposure to meaningful objects on the perception of pain. Participants (N = 54 completed a cold pressor test, examined either ibuprofen or a control object, then completed another cold pressor test. In the second test, participants who previously examined ibuprofen reported experiencing less intense pain and tolerated immersion longer (relative to baseline than those who examined the control object. Theoretical and applied implications of these findings are discussed.

  12. An ibuprofen-antagonized plasmin inhibitor released by human endothelial cells.

    Science.gov (United States)

    Rockwell, W B; Ehrlich, H P

    1991-02-01

    Serum-free culture medium harvested from endothelial cell monolayer cultures derived from human scars and dermis was examined for inhibition of fibrinolysis using a fibrin plate assay. Human cultured fibroblasts and smooth muscle cells did not produce any detectable inhibitory activity. The inhibitor is spontaneously released from the cultured endothelial cells over time. In the fibrin plate assay of plasmin-induced fibrinolysis, one nonsteroidal antiinflammatory (NSAI) drug, ibuprofen, was demonstrated to antagonize the inhibition of fibrinolysis. The antagonistic activity of ibuprofen appears unrelated to its NSAI drug activity because other NSAI drugs such as indomethacin and tolmetin have minimal antagonistic activity. Heating the cultured endothelial cells to 42 degrees C stimulates greater release of the inhibitor in a shorter period of time. This plasmin inhibitor, which is produced by endothelial cells, may contribute to postburn vascular occlusion, leading to secondary progressive necrosis in burn-traumatized patients.

  13. 20 CFR 404.1093 - Possession of the United States.

    Science.gov (United States)

    2010-04-01

    ... DISABILITY INSURANCE (1950- ) Employment, Wages, Self-Employment, and Self-Employment Income Self-Employment... figuring your net earnings from self-employment, the term possession of the United States shall be deemed...

  14. Mental illness complicated by the santeria belief in spirit possession.

    Science.gov (United States)

    Alonso, L; Jeffrey, W D

    1988-11-01

    Santeria, a religious system that blends African and Catholic beliefs, is practiced by many Cuban Americans. One aspect of this system is the belief in spirit possession. Basic santeria beliefs and rituals, including the fiesta santera (a gathering at which some participants may become possessed), are briefly described, and four cases in which the patients' belief in possession played a role in their mental illness are presented. The belief in possession can complicate the diagnosis and treatment of mental illness, but it should not be considered a culture-bound syndrome. Rather, it may be a nonspecific symptom of a variety of mental illnesses and should be evaluated in the context of the patient's overall belief system and ability to carry out usual activities.

  15. Constitutional Law: Right of Privacy--Possession of Marijuana

    Science.gov (United States)

    Rohrer, David E.

    1976-01-01

    The Alaska Supreme Court in Ravin v. State accepted the defendant's contention that the prohibition of possession of marihuana infringed on his constitutional right to privacy. The significance of the case is discussed. (LBH)

  16. The epistemological significance of possession entering the DSM.

    Science.gov (United States)

    Stephenson, Craig

    2015-09-01

    The discourse of the American Psychiatric Association's DSM reflects the inherently dialogic or contradictory nature of its stated mandate to demonstrate both 'nosological completeness' and cultural 'inclusiveness'. Psychiatry employs the dialogic discourse of the DSM in a one-sided, positivistic manner by identifying what it considers universal mental disease entities stripped of their cultural context. In 1992 the editors of the Diagnostic and Statistical Manual of Mental Disorders proposed to introduce possession into their revisions. A survey of the discussions about introducing 'possession' as a dissociative disorder to be listed in the DSM-IV indicates a missed epistemological break. Subsequently the editors of the DSM-5 politically 'recuperated' possession into its official discourse, without acknowledging the anarchic challenges that possession presents to psychiatry as a cultural practice. © The Author(s) 2015.

  17. Criminalization of 'Possession of Unexplained Property' and the ...

    African Journals Online (AJOL)

    Worku_Y

    government operating costs, increases government spending for wages and ... revenues by plundering revenue generating agencies such as tax collection, ..... a) the assets under the ownership or possession of himself and his family; and.

  18. Metabolism of ibuprofen in higher plants: A model Arabidopsis thaliana cell suspension culture system

    Czech Academy of Sciences Publication Activity Database

    Maršík, Petr; Šíša, Miroslav; Lacina, O.; Moťková, Kateřina; Langhansová, Lenka; Rezek, Jan; Vaněk, Tomáš

    2017-01-01

    Roč. 220, JAN (2017), s. 383-392 ISSN 0269-7491 R&D Projects: GA ČR(CZ) GA14-22593S Grant - others:European Regional Development Fund(XE) CZ.2.16/3.1.00/24014 Institutional support: RVO:61389030 Keywords : Arabidopsis thaliana * Ibuprofen * Metabolism * Plant cells * Sequestration Subject RIV: CE - Biochemistry OBOR OECD: Plant sciences, botany Impact factor: 5.099, year: 2016

  19. Experimental substantiation of effectively administration of vinboron for analgesic activity increase of ibuprofen

    OpenAIRE

    F. V. Hladkykh; N. H. Stepaniuk

    2016-01-01

    Background. The increase of NSAIDs safety is current direction of modern pharmacology, because of so-called "class-specific" adverse reactions, which are common to this class, and the leading place among them is occupied by gastro-intestinal toxicity. In previous studies we have proved the ability of vinboron to neutralize ulcerogenic effect of ibuprofen (Hladkykh F.V. and al., 2014). The presence of the proven analgesic activity in the domestic antispasmodics (Stepaniuk H.I. and al., 2007) s...

  20. Combined isosorbide dinitrate and ibuprofen as a novel therapy for muscular dystrophies: evidence from Phase I studies in healthy volunteers

    Directory of Open Access Journals (Sweden)

    Cossu MV

    2014-05-01

    Full Text Available Maria Vittoria Cossu,1 Dario Cattaneo,1 Serena Fucile,1 Paolo Pellegrino,1 Sara Baldelli,1 Valeria Cozzi,1 Amedeo Capetti,2 Emilio Clementi1,3 1Unit of Clinical Pharmacology, Consiglio Nazionale delle Ricerche Institute of Neuroscience, Department of Biomedical and Clinical Sciences, University Hospital “Luigi Sacco”, Università di Milano, Milan, Italy; 2Unit of Infectious Diseases, University Hospital “Luigi Sacco”, Milan, Italy; 3Scientific Institute, IRCCS Eugenio Medea, Bosisio Parini, Lecco, Italy Abstract: We designed two Phase I studies that assessed healthy volunteers in order to evaluate the safety and to optimize the dosing of the combination of the drugs isosorbide dinitrate, a nitric oxide donor, and ibuprofen, a nonsteroidal antiinflammatory drug. We designed these studies with the aim of designing a Phase II trial to evaluate the drugs’ efficacy in patients affected by Duchenne muscular dystrophy. For the first trial, ISOFEN1, a single-dose, randomized-sequence, open-label, active control, three-treatment cross-over study, was aimed at comparing the pharmacokinetics of ibuprofen 200 mg and isosorbide dinitrate 20 mg when given alone and concomitantly. The pharmacokinetics of ibuprofen given alone versus ibuprofen given concomitantly with isosorbide dinitrate were similar, as documented by the lack of statistically significant differences in the main drug’s pharmacokinetic parameters (time to maximal concentration [Tmax], maximal concentration [Cmax], area under the curve [AUC]0–t, and AUC0–∞. Similarly, we found that the coadministration of ibuprofen did not significantly affect the pharmacokinetics of isosorbide dinitrate. No issues of safety were detected. The second trial, ISOFEN2, was a single-site, dose titration study that was designed to select the maximum tolerated dose for isosorbide dinitrate when coadministered with ibuprofen. Eighteen out of the 19 enrolled subjects tolerated the treatment well, and

  1. Ibuprofen, paracetamol, and steam for patients with respiratory tract infections in primary care: pragmatic randomised factorial trial.

    Science.gov (United States)

    Little, Paul; Moore, Michael; Kelly, Joanne; Williamson, Ian; Leydon, Geraldine; McDermott, Lisa; Mullee, Mark; Stuart, Beth

    2013-10-25

    To assess strategies for advice on analgesia and steam inhalation for respiratory tract infections. Open pragmatic parallel group factorial randomised controlled trial. Primary care in United Kingdom. Patients aged ≥ 3 with acute respiratory tract infections. 889 patients were randomised with computer generated random numbers in pre-prepared sealed numbered envelopes to components of advice or comparator advice: advice on analgesia (take paracetamol, ibuprofen, or both), dosing of analgesia (take as required v regularly), and steam inhalation (no inhalation v steam inhalation). Primary: mean symptom severity on days 2-4; symptoms rated 0 (no problem) to 7 (as bad as it can be). Secondary: temperature, antibiotic use, reconsultations. Neither advice on dosing nor on steam inhalation was significantly associated with changes in outcomes. Compared with paracetamol, symptom severity was little different with ibuprofen (adjusted difference 0.04, 95% confidence interval -0.11 to 0.19) or the combination of ibuprofen and paracetamol (0.11, -0.04 to 0.26). There was no evidence for selective benefit with ibuprofen among most subgroups defined before analysis (presence of otalgia; previous duration of symptoms; temperature >37.5 °C; severe symptoms), but there was evidence of reduced symptoms severity benefit in the subgroup with chest infections (ibuprofen -0.40, -0.78 to -0.01; combination -0.47; -0.84 to -0.10), equivalent to almost one in two symptoms rated as a slight rather than a moderately bad problem. Children might also benefit from treatment with ibuprofen (ibuprofen: -0.47, -0.76 to -0.18; combination: -0.04, -0.31 to 0.23). Reconsultations with new/unresolved symptoms or complications were documented in 12% of those advised to take paracetamol, 20% of those advised to take ibuprofen (adjusted risk ratio 1.67, 1.12 to 2.38), and 17% of those advised to take the combination (1.49, 0.98 to 2.18). Mild thermal injury with steam was documented for four patients

  2. Ibuprofen delivered by poly(lactic-co-glycolic acid (PLGA nanoparticles to human gastric cancer cells exerts antiproliferative activity at very low concentrations

    Directory of Open Access Journals (Sweden)

    Bonelli P

    2012-11-01

    Full Text Available Patrizia Bonelli,1 Franca M Tuccillo,1 Antonella Federico,5 Maria Napolitano,2 Antonella Borrelli,1 Daniela Melisi,6 Maria G Rimoli,6 Raffaele Palaia,3 Claudio Arra,4 Francesco Carinci71Laboratory of Molecular Biology and Viral Oncogenesis; 2Department of Clinical Immunology; 3Department of Gastrointestinal-Hepatobiliary-Pancreatic Cancer Oncology Surgery; 4Animal Facility, National Cancer Institute G Pascale, Naples, Italy; 5Microtech Laboratory, Naples, Italy; 6Pharmaceutical and Toxicological Chemistry Department, School of Pharmacy, University "Federico II", Naples, Italy; 7Department of Maxillofacial Surgery, University of Ferrara, Ferrara, ItalyPurpose: Epidemiological, clinical, and laboratory studies have suggested that ibuprofen, a commonly used nonsteroidal anti-inflammatory drug, inhibits the promotion and proliferation of certain tumors. Recently, we demonstrated the antiproliferative effects of ibuprofen on the human gastric cancer cell line MKN-45. However, high doses of ibuprofen were required to elicit these antiproliferative effects in vitro. The present research compared the antiproliferative effects of ibuprofen delivered freely and released by poly(lactic-co-glycolic acid (PLGA nanoparticles (NPs in MKN-45 cells.Methods: MKN-45 human gastric adenocarcinoma cells were treated with ibuprofen-loaded PLGA NPs. The proliferation of MKN-45 cells was then assessed by cell counting. The uptake of NPs was imaged by fluorescence microscopy and flow cytometry. The release of ibuprofen from ibuprofen-loaded PLGA NPs in the cells was evaluated by gas chromatography–mass spectrometry.Results: Dramatic inhibition of cellular proliferation was observed in cells treated with ibuprofen-loaded PLGA NPs versus those treated with free ibuprofen at the same concentration. The localization of NPs was cytoplasmic. The initiation of ibuprofen release was rapid, commencing within 2 hours, and then increased slowly over time, reaching a maximum

  3. Ibuprofen loaded PLA nanofibrous scaffolds increase proliferation of human skin cells in vitro and promote healing of full thickness incision wounds in vivo.

    Science.gov (United States)

    Mohiti-Asli, M; Saha, S; Murphy, S V; Gracz, H; Pourdeyhimi, B; Atala, A; Loboa, E G

    2017-02-01

    This article presents successful incorporation of ibuprofen in polylactic acid (PLA) nanofibers to create scaffolds for the treatment of both acute and chronic wounds. Nanofibrous PLA scaffolds containing 10, 20, or 30 wt % ibuprofen were created and ibuprofen release profiles quantified. In vitro cytotoxicity to human epidermal keratinocytes (HEK) and human dermal fibroblasts (HDF) of the three scaffolds with varying ibuprofen concentrations were evaluated and compared to pure PLA nanofibrous scaffolds. Thereafter, scaffolds loaded with ibuprofen at the concentration that promoted human skin cell viability and proliferation (20 wt %) were evaluated in vivo in nude mice using a full thickness skin incision model to determine the ability of these scaffolds to promote skin regeneration and/or assist with scarless healing. Both acellular and HEK and HDF cell-seeded 20 wt % ibuprofen loaded nanofibrous bandages reduced wound contraction compared with wounds treated with Tegaderm™ and sterile gauze. Newly regenerated skin on wounds treated with cell-seeded 20 wt % ibuprofen bandages exhibited significantly greater blood vessel formation relative to acellular ibuprofen bandages. We have found that degradable anti-inflammatory scaffolds containing 20 wt % ibuprofen promote human skin cell viability and proliferation in vitro, reduce wound contraction in vivo, and when seeded with skin cells, also enhance new blood vessel formation. The approaches and results reported here hold promise for multiple skin tissue engineering and wound healing applications. © 2015 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 105B: 327-339, 2017. © 2015 Wiley Periodicals, Inc.

  4. Effect of ibuprofen on menstrual blood prostaglandin levels in dysmenorrheic women.

    Science.gov (United States)

    Pulkkinen, M O; Csapo, A I

    1979-07-01

    In a randomized crossover study 15 dysmenorrheic women were treated during two consecutive menstrual period, once with the potent prostaglandin-synthesis inhibitor: ibuprofen and once with an identical looking placebo. Each patient was medicated for 12 hours during the first day of her menstrual flow and was subsequently fitted with a cervical cup for the collection of menstrual blood during three hours. In these samples the concentrations of prostaglandin (PG)F and PGE were measured by radioimmunoassay. The patients receiving placebo had high PGF levels 135 +/- 27 ng/ml (Mean +/- S.E.) which were significnatly reduced by Ibuprofen to 24 +/- 5 ng/ml (P less than 0.001). The PGE concentrations decreased from 5 +/- 1 ng/ml to 2 +/- 1 ng/ml (P less than 0.05). Ibuprofen also reduced the menstrual pain significantly (P less than 0.001). These results substantiate the earlier conclusion that a causal relationship exists between effective treatment with PG-synthesis inhibitors and decrease in menstrual blood PG levels, intrauterine pressure and dysmenorrheic pain.

  5. Temperature and pH Responsive Microfibers for Controllable and Variable Ibuprofen Delivery

    Directory of Open Access Journals (Sweden)

    Toan Tran

    2015-01-01

    Full Text Available Electrospun microfibers (MFs composed of pH and temperature responsive polymers can be used for controllable and variable delivery of ibuprofen. First, electrospinning technique was employed to prepare poly(ε-caprolactone (PCL and poly(N-isopropylacrylamide-co-methacrylic acid (pNIPAM-co-MAA MFs containing ibuprofen. It was found that drug release rates from PCL MFs cannot be significantly varied by either temperature (22–40°C or pH values (1.7–7.4. In contrast, the ibuprofen (IP diffusion rates from pNIPAM-co-MAA MFs were very sensitive to changes in both temperature and pH. The IP release from pNIPAM-co-MAA MFs was highly linear and controllable when the temperature was above the lower critical solution temperature (LCST of pNIPAM-co-MAA (33°C and the pH was lower than the pKa of carboxylic acids (pH 2. At room temperature, however, the release rate was dramatically increased by nearly ten times compared to that at higher temperature and lower pH. Such a unique and controllable drug delivery system could be naturally envisioned to find many practical applications in biomedical and pharmaceutical sciences such as programmable transdermal drug delivery.

  6. Synthesis and Study of Analgesic and Anti-inflammatory Activities of Amide Derivatives of Ibuprofen.

    Science.gov (United States)

    Ahmadi, Abbas; Khalili, Mohsen; Olama, Zahra; Karami, Shirin; Nahri-Niknafs, Babak

    2017-01-01

    Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used drugs worldwide and represent a mainstay in the therapy of acute and chronic pain and inflammation. The traditional NSAIDs like ibuprofen (I) contain free carboxylic acid group which can produce gastrointestinal (GI) damage for long-term use. In order to obtain the novel NSAIDs with less side effects; carboxylic acid moiety has been modified into various amide groups which is the most active area of research in this family. In this research, synthesis of various pharmacological heterocyclic amides of ibuprofen is described. All the new compounds were tested for their analgesic and anti-inflammatory activities in mice and compared with standard (Ibuprofen) and control (saline) groups. The results revealed that all the synthesized compounds (III-VI) exhibited more analgesic and anti-inflammatory activities in tail immersion (as a model of acute thermal pain), formalin (as a model of acute chemical and chronic pain) and paw edema (as a model of acute inflammation) tests when compared with standard and control animals. These pharmacological activities were significant for VI compared to other new compounds (III-V) which may be concern to more effective role of morpholin for the reduction of pain and inflammation compared to other used heterocyclic amines. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  7. Ibuprofen-associated acute kidney injury in dehydrated children with acute gastroenteritis.

    Science.gov (United States)

    Balestracci, Alejandro; Ezquer, Mauricio; Elmo, María Eugenia; Molini, Andrea; Thorel, Claudia; Torrents, Milagros; Toledo, Ismael

    2015-10-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) induce acute kidney injury (AKI) in volume-depleted patients; however the prevalence of this complication is likely underestimated. We assessed the impact of ibuprofen exposure on renal function among dehydrated children with acute gastroenteritis (AGE) to further characterize NSAID-associated AKI. Over a 1-year period dehydrated children with AGE (n = 105) were prospectively enrolled and grouped as cases, presenting with AKI (n = 46) or controls, not presenting with AKI (n = 59). AKI was defined by pediatric RIFLE (pRIFLE) criteria. Among the children enrolled in the study, AKI prevalence was 44 %, and 34 (54 %) of the 63 patients who received ibuprofen developed renal impairment. Relative to the controls, children presenting with AKI were younger (median age 0.66 vs. 1.74 years; p dehydration, ibuprofen exposure remained an independent risk factor for AKI (p dehydrated children with AGE. Drug exposure increased the risk for developing AKI by more than twofold, independent of the magnitude of the dehydration.

  8. Metabolite profiling of carbamazepine and ibuprofen in Solea senegalensis bile using high-resolution mass spectrometry.

    Science.gov (United States)

    Aceña, Jaume; Pérez, Sandra; Eichhorn, Peter; Solé, Montserrat; Barceló, Damià

    2017-09-01

    The widespread occurrence of pharmaceuticals in the aquatic environment has raised concerns about potential adverse effects on exposed wildlife. Very little is currently known on exposure levels and clearance mechanisms of drugs in marine fish. Within this context, our research was focused on the identification of main metabolic reactions, generated metabolites, and caused effects after exposure of fish to carbamazepine (CBZ) and ibuprofen (IBU). To this end, juveniles of Solea senegalensis acclimated to two temperature regimes of 15 and 20 °C for 60 days received a single intraperitoneal dose of these drugs. A control group was administered the vehicle (sunflower oil). Bile samples were analyzed by ultra-high-performance liquid chromatography-high-resolution mass spectrometry on a Q Exactive (Orbitrap) system, allowing to propose plausible identities for 11 metabolites of CBZ and 13 metabolites of IBU in fish bile. In case of CBZ metabolites originated from aromatic and benzylic hydroxylation, epoxidation, and ensuing O-glucuronidation, O-methylation of a catechol-like metabolite was also postulated. Ibuprofen, in turn, formed multiple hydroxyl metabolites, O-glucuronides, and (hydroxyl)-acyl glucuronides, in addition to several taurine conjugates. Enzymatic responses after drug exposures revealed a water temperature-dependent induction of microsomal carboxylesterases. The metabolite profiling in fish bile provides an important tool for pharmaceutical exposure assessment. Graphical abstract Studies of metabolism of carbamazepine and ibuprofen in fish.

  9. Efficacy of ibuprofen, naproxen and mefenamic acid for relief of pain from primary dysmenorrheal

    Directory of Open Access Journals (Sweden)

    Azita Norouzi

    2003-09-01

    Full Text Available Cyclic pain associated with menses during ovulatory cycles, but without demonstrable lesions affecting the reproductive cycle, is a common disability, which causes significant absence from school or work. To evaluate the efficacy of naproxen, ibuprofen and mefenamic acid in the treatment of primary dysmenorrheal, 120 girls were randomized to four groups (three as treatment groups and the other as placebo. The pain intensity was recorded using self visual analogue scale in 0, 1, 2, 4 and 6 hours after treatment. There was no significant difference in intensity of pain between groups at zero time, however the pain intensity decreased significantly in all treatment group in comparison to placebo (p<0.05. The mean of pain intensity was lower in ibuprofen in comparison to the other treatment groups, however there was no significant difference in pain intensity between the treatment groups in the sixth hour of treatment. Therefore, ibuprofen is recommended as a treatment choice for pain reduction in primary dysmenorrheal due to its rapid onset of action.

  10. A comparative study of ibuprofen and ketoprofen glass-forming liquids by molecular dynamics simulations

    Science.gov (United States)

    Ottou Abe, M. T.; Correia, N. T.; Ndjaka, J. M. B.; Affouard, F.

    2015-10-01

    In this paper, structural and dynamical properties of ibuprofen and ketoprofen glass-forming liquids have been investigated by means of molecular dynamics simulations. Molecular mobility of both materials is analyzed with respect to the different inter-molecular linear/cyclic hydrogen bonding associations. For ibuprofen, the dominant organization is found to be composed of small hydrogen bonding aggregates corresponding to cyclic dimers through the carboxyl group. For ketoprofen, the propensity of cyclic dimers is significantly reduced by the formation of hydrogen bonds with the ketone oxygen of the molecule altering the hydrogen bond (HB) associating structures that can be formed and thus molecular dynamics. The issue of the presence/absence of the peculiar low frequency Debye-type process in dielectric relaxation spectroscopy (DRS) data in these materials is addressed. Results obtained from simulations confirm that the Debye process originates from the internal cis-trans conversion of the —COOH carboxyl group. It is shown that the specific intermolecular HB structures associated to a given profen control the main dynamical features of this conversion, in particular its separation from the α-process, which make it detectable or not from DRS. For ibuprofen, the possible role of the —CCCO torsion motion, more "local" than the —COOH motion since it is less influenced by the intermolecular HBs, is suggested in the microscopic origin of the quite intense secondary γ-relaxation process detected from DRS.

  11. Design and evaluation of mucoadhesive microemulsion for neuroprotective effect of ibuprofen following intranasal route in the MPTP mice model.

    Science.gov (United States)

    Mandal, Surjyanarayan; Mandal, Snigdha Das; Chuttani, Krishna; Sawant, Krutika K; Subudhi, Bharat Bhushan

    2016-08-01

    The present study is to investigate the neuroprotective effect of ibuprofen by intranasal administration of mucoadhesive microemulsion (MMEI) against inflammation-mediated by dopaminergic neurodegeneration in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) model of Parkinson's disease (PD). Ibuprofen-loaded polycarbophil-based MMEI was developed by using response surface methodology (RSM). Ibuprofen with dose of 2.86 mg/kg/day was administered intranasally to male C57BL/6 mice for two consecutive weeks which were pre-treated with four intraperitoneal injections of MPTP (20 mg/kg of body weight) at 2 h intervals. Immunohistochemistry was performed. Optimal MMEI was stable and non-ciliotoxic with 66.29 ± 4.15 nm as average globule size and -20.9 ± 3.98 mV as zeta potential. PDI value and transmission electron microscopy result showed the narrow globule size distribution of MMEI. The result showed that all three independent variables had a significant effect (p open-field test findings revealed the significant improvement in motor performance and gross behavioral activity of the mice. The results from in vivo study and immunohistochemistry showed that nasal administration of Ibuprofen significantly reduced the MPTP-mediated dopamine depletion. Furthermore TH neurons count in the substantia nigra and the density of striatal dopaminergic nerve terminals were found to be significant higher for ibuprofen treated groups. Findings of the investigation revealed that Ibuprofen through developed MMEI was shown to protect neurons against MPTP-induced injury in the Substantia nigra pars compacta (SNpc) and striatum and hence, could be a promising approach for brain targeting of Ibuprofen through intranasal route to treat PD.

  12. Use of ibuprofen sustained release for treating osteoarthritic pain: findings from 15 general medical practices in Egypt

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    Khalifa N

    2014-05-01

    Full Text Available Nabil Khalifa,1 Timour El-Husseini,1 Ahmed Morrah,2 Elshenawy Mostafa,3 Hesham Hamoud41Department of Orthopedic Surgery, Ain Shams University, Cairo, Egypt; 2Department of Orthopedic Surgery, Cairo University, Cairo, Egypt; 3Department of Orthopedic Surgery, Mansoura University, Mansoura, Egypt; 4Department of Rheumatology, Azhar University, Cairo, EgyptPurpose: Ibuprofen sustained release (SR has been shown to provide effective symptomatic pain relief in chronic arthritic conditions such as osteoarthritis in European and US patient populations. Few studies have been conducted in other patient populations. A 4-week prospective multicenter open-label observational study was designed to explore and describe the combined effect of ibuprofen SR and standard medical care in patients suffering from osteoarthritis in 15 general medical practices in Egypt.Patients and methods: In total, 519 patients were prescribed ibuprofen SR 2 ×800 mg once daily for 4 weeks.Results: Ibuprofen SR combined with standard medical care significantly improved day and night pain, with 99.4% of the patients reporting improvement. The treatment reduced the symptom severity of joint tenderness/stiffness and the duration of morning stiffness, and allowed more patients to carry out normal activities. Overall compliance with the prescribed ibuprofen SR regimen was 98.6%. Ibuprofen SR was generally well tolerated with no serious adverse events reported during the study. There was no increase in blood pressure or heart rate.Conclusion: The combined treatment provided effective relief of pain in patients with osteoarthritis in a large real-life general medical practice setting in Egypt. Owing to its convenient once-daily dosing regimen, ibuprofen SR may enhance patient compliance.Keywords: chronic arthritis, compliance, pain score, real-life

  13. Comparison of oral paracetamol versus ibuprofen in premature infants with patent ductus arteriosus: a randomized controlled trial.

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    Dan Dang

    Full Text Available TRIAL DESIGN: Oral ibuprofen has demonstrated good effects on symptomatic patent ductus arteriosus (PDA but with many contraindications and potential side-effects. In the past two years, oral paracetamol administration to several preterm infants with PDA has been reported. Here, a randomized, non-blinded, parallel-controlled and non-inferiority trial was designed to evaluate the efficacy and safety profiles of oral paracetamol to those of standard ibuprofen for PDA closure in premature infants. METHODS: One hundred and sixty infants (gestational age ≤ 34 weeks with echocardiographically confirmed PDA were randomly assigned to receive either oral paracetamol (n = 80 or ibuprofen (n = 80. After the initial treatment course in both groups, the need for a second course was determined by echocardiographic evaluation. The main outcome was rate of ductal closure, and secondary outcomes were adverse effects and complications. RESULT: The ductus was closed in 65 (81.2% infants of the paracetamol group compared with 63 (78.8% of the ibuprofen group. The 95% confidence interval of the difference between these groups was [-0.080,0.128], demonstrating that the effectiveness of paracetamol treatment was not inferior to that of ibuprofen. In fact, the incidence of hyperbilirubinemia or gastrointestinal bleeding in the paracetamol group was significantly lower than that of the ibuprofen group. No significant differences in other clinical side effects or complications were noted. CONCLUSION: This comparison of drug efficacy and safety profiles in premature infants with PDA revealed that oral paracetamol was comparable to ibuprofen in terms of the rate of ductal closure and even showed a decreased risk of hyperbilirubinemia or gastrointestinal bleeding. Therefore, paracetamol may be accepted as a first-line drug treatment for PDA in preterm infants. TRIAL REGISTRATION: ChiCTR.org ChiCTR-TRC-12002177.

  14. Comparison of oral and intravenous Ibuprofen for medical closure of patent ductus arteriosus: which one is better?

    Science.gov (United States)

    Olukman, Ozgur; Calkavur, Sebnem; Ercan, Gulten; Atlihan, Fusun; Oner, Taliha; Tavli, Vedide; Kultursay, Nilgun

    2012-01-01

    Intravenous ibuprofen is an expensive drug that is being used currently for treating and preventing patent ductus arteriosus. Although oral ibuprofen is much cheaper, there is limited data published about its safety and efficacy. The aim of this study was to compare two forms of ibuprofen in terms of safety and efficacy in closure of patent ductus arteriosus. This is a single-center retrospective study. Data were collected from patients' files of preterm infants who were hospitalized at the Neonatal Intensive Care Unit of Dr. Behcet Uz Children's Hospital between April 2009 and June 2010. Six hundred sixty infants were evaluated by echocardiography between 24 and 48 postnatal hours. Clinically and hemodynamically significant ductus arteriosus was defined in 66 infants with gestational age less than 32 weeks and birth weight less than 1500 g. Oral or intravenous ibuprofen (loading dose: 10 mg/kg on day 1, followed by maintenance dose: 5 mg/kg on days 2 and 3) was administered. Treatment success was defined as a completely closed duct without reopening on follow-up. Drug-associated renal, gastrointestinal, cerebral, hematological, and metabolic side effects were monitored and compared between treatment groups. Ductal closure rates were 100% and 97.6%, respectively, in the oral and intravenous groups. Hypernatremia was the remarkable side effect in the intravenous group, whereas bronchopulmonary dysplasia and septicemia were prominent in the oral group. No statistically significant difference could be demonstrated between the groups in terms of mortality rates. Oral ibuprofen therapy is as efficacious as intravenous ibuprofen with some concerns about increased sepsis and bronchopulmonary dysplasia incidence. However, comprehensive and large-scale pharmacokinetic studies are required in order to prove this efficacy. On the other hand, intravenous ibuprofen still remains to be the drug of choice for patent ductus arteriosus but only with meticulous control of serum

  15. Prophylactic Acetaminophen or Ibuprofen Results in Equivalent Acute Mountain Sickness Incidence at High Altitude: A Prospective Randomized Trial.

    Science.gov (United States)

    Kanaan, Nicholas C; Peterson, Alicia L; Pun, Matiram; Holck, Peter S; Starling, Jennifer; Basyal, Bikash; Freeman, Thomas F; Gehner, Jessica R; Keyes, Linda; Levin, Dana R; O'Leary, Catherine J; Stuart, Katherine E; Thapa, Ghan B; Tiwari, Aditya; Velgersdyk, Jared L; Zafren, Ken; Basnyat, Buddha

    2017-06-01

    Recent trials have demonstrated the usefulness of ibuprofen in the prevention of acute mountain sickness (AMS), yet the proposed anti-inflammatory mechanism remains unconfirmed. Acetaminophen and ibuprofen were tested for AMS prevention. We hypothesized that a greater clinical effect would be seen from ibuprofen due to its anti-inflammatory effects compared with acetaminophen's mechanism of possible symptom reduction by predominantly mediating nociception in the brain. A double-blind, randomized trial was conducted testing acetaminophen vs ibuprofen for the prevention of AMS. A total of 332 non-Nepali participants were recruited at Pheriche (4371 m) and Dingboche (4410 m) on the Everest Base Camp trek. The participants were randomized to either acetaminophen 1000 mg or ibuprofen 600 mg 3 times a day until they reached Lobuche (4940 m), where they were reassessed. The primary outcome was AMS incidence measured by the Lake Louise Questionnaire score. Data from 225 participants who met inclusion criteria were analyzed. Twenty-five participants (22.1%) in the acetaminophen group and 18 (16.1%) in the ibuprofen group developed AMS (P = .235). The combined AMS incidence was 19.1% (43 participants), 14 percentage points lower than the expected AMS incidence of untreated trekkers in prior studies at this location, suggesting that both interventions reduced the incidence of AMS. We found little evidence of any difference between acetaminophen and ibuprofen groups in AMS incidence. This suggests that AMS prevention may be multifactorial, affected by anti-inflammatory inhibition of the arachidonic-acid pathway as well as other analgesic mechanisms that mediate nociception. Additional study is needed. Copyright © 2017 Wilderness Medical Society. Published by Elsevier Inc. All rights reserved.

  16. Evaluation of hepatic metabolism and pharmacokinetics of ibuprofen in rats under chronic hypobaric hypoxia for targeted therapy at high altitude.

    Science.gov (United States)

    Gola, Shefali; Gupta, Asheesh; Keshri, Gaurav K; Nath, Madhu; Velpandian, Thirumurthy

    2016-03-20

    With studies indicative of altered drug metabolism and pharmacokinetics (DMPK) under high altitude (HA)-induced hypobaric hypoxia, consideration of better therapeutic approaches has continuously been aimed in research for HA related illness management. DMPK of drugs like ibuprofen may get affected under hypoxia which establishes the requirement of different therapeutic dose regimen to ensure safe and effective therapy at HA. This study examined the effects of the chronic hypobaric hypoxia (CHH) on hepatic DMPK of ibuprofen in rats. Experimental animals were exposed to simulated altitude of 7620 m (∼25,000 ft) for CHH exposure (7 or 14 days) in decompression chamber and administered with ibuprofen (80 mg/kg, body weight, p.o.). Results demonstrated that CHH significantly altered PK variables of ibuprofen and activities of both phase-I and II hepatic metabolic enzymes as compared to the animals under normoxic conditions. Hepatic histopathological observations also revealed marked alterations. Increase in pro-inflammatory cytokines/chemokines viz. IL-1β, IL-2, IFN-γ, TNF-α exhibited close relevance with diminished CYP2C9 expression under CHH. Moreover, the down-regulated CYP2C9 level further supported the underlying mechanism for reduced metabolism of ibuprofen and as a result, increased retention of parent drug in the system. Increased mean retention time, Vd, T½ of ibuprofen, and decreased AUC, Cmax and clearance during CHH further strengthened the present findings. In conclusion, CHH exposure significantly affects hepatic DMPK of ibuprofen, which may further influence the usual therapeutic dose-regimen. Further, there is requirement of human studies to evaluate their susceptibility toward hypobaric hypoxia. Copyright © 2016 Elsevier B.V. All rights reserved.

  17. Oral morphine versus ibuprofen administered at home for postoperative orthopedic pain in children: a randomized controlled trial.

    Science.gov (United States)

    Poonai, Naveen; Datoo, Natasha; Ali, Samina; Cashin, Megan; Drendel, Amy L; Zhu, Rongbo; Lepore, Natasha; Greff, Michael; Rieder, Michael; Bartley, Debra

    2017-10-10

    Oral morphine for postoperative pain after minor pediatric surgery, while increasingly popular, is not supported by evidence. We evaluated whether oral morphine was superior to ibuprofen for at-home management of children's postoperative pain. We conducted a randomized superiority trial comparing oral morphine (0.5 mg/kg) with ibuprofen (10 mg/kg) in children 5 to 17 years of age who had undergone minor outpatient orthopedic surgery (June 2013 to September 2016). Participants took up to 8 doses of the intervention drug every 6 hours as needed for pain at home. The primary outcome was pain, according to the Faces Pain Scale - Revised, for the first dose. Secondary outcomes included additional analgesic requirements, adverse effects, unplanned health care visits and pain scores for doses 2 to 8. We analyzed data for 77 participants in each of the morphine and ibuprofen groups. Both interventions decreased pain scores with no difference in efficacy. The median difference in pain score before and after the first dose of medication was 1 (interquartile range 0-1) for both morphine and ibuprofen ( p = 0.2). For doses 2 to 8, the median differences in pain score before and after the dose were not significantly different between groups. Significantly more participants taking morphine reported adverse effects (45/65 [69%] v. 26/67 [39%], p ibuprofen groups, respectively; p = 0.003). Morphine was not superior to ibuprofen, and both drugs decreased pain with no apparent difference in efficacy. Morphine was associated with significantly more adverse effects, which suggests that ibuprofen is a better first-line option after minor surgery. ClinicalTrials.gov, no. NCT01686802. © 2017 Canadian Medical Association or its licensors.

  18. Human inflammatory and resolving lipid mediator responses to resistance exercise and ibuprofen treatment

    Science.gov (United States)

    Markworth, James F.; Vella, Luke; Lingard, Benjamin S.; Tull, Dedreia L.; Rupasinghe, Thusitha W.; Sinclair, Andrew J.; Maddipati, Krishna Rao

    2013-01-01

    Classical proinflammatory eicosanoids, and more recently discovered lipid mediators with anti-inflammatory and proresolving bioactivity, exert a complex role in the initiation, control, and resolution of inflammation. Using a targeted lipidomics approach, we investigated circulating lipid mediator responses to resistance exercise and treatment with the NSAID ibuprofen. Human subjects undertook a single bout of unaccustomed resistance exercise (80% of one repetition maximum) following oral ingestion of ibuprofen (400 mg) or placebo control. Venous blood was collected during early recovery (0–3 h and 24 h postexercise), and serum lipid mediator composition was analyzed by LC-MS-based targeted lipidomics. Postexercise recovery was characterized by elevated levels of cyclooxygenase (COX)-1 and 2-derived prostanoids (TXB2, PGE2, PGD2, PGF2α, and PGI2), lipooxygenase (5-LOX, 12-LOX, and 15-LOX)-derived hydroxyeicosatetraenoic acids (HETEs), and leukotrienes (e.g., LTB4), and epoxygenase (CYP)-derived epoxy/dihydroxy eicosatrienoic acids (EpETrEs/DiHETrEs). Additionally, we detected elevated levels of bioactive lipid mediators with anti-inflammatory and proresolving properties, including arachidonic acid-derived lipoxins (LXA4 and LXB4), and the EPA (E-series) and DHA (D-series)-derived resolvins (RvD1 and RvE1), and protectins (PD1 isomer 10S, 17S-diHDoHE). Ibuprofen treatment blocked exercise-induced increases in COX-1 and COX-2-derived prostanoids but also resulted in off-target reductions in leukotriene biosynthesis, and a diminished proresolving lipid mediator response. CYP pathway product metabolism was also altered by ibuprofen treatment, as indicated by elevated postexercise serum 5,6-DiHETrE and 8,9-DiHETrE only in those receiving ibuprofen. These findings characterize the blood inflammatory lipid mediator response to unaccustomed resistance exercise in humans and show that acute proinflammatory signals are mechanistically linked to the induction of a

  19. Ibuprofen and/or paracetamol (acetaminophen) for pain relief after surgical removal of lower wisdom teeth.

    Science.gov (United States)

    Bailey, Edmund; Worthington, Helen V; van Wijk, Arjen; Yates, Julian M; Coulthard, Paul; Afzal, Zahid

    2013-12-12

    Both paracetamol and ibuprofen are commonly used analgesics for the relief of pain following the surgical removal of lower wisdom teeth (third molars). In 2010, a novel analgesic (marketed as Nuromol) containing both paracetamol and ibuprofen in the same tablet was launched in the United Kingdom, this drug has shown promising results to date and we have chosen to also compare the combined drug with the single drugs using this model. In this review we investigated the optimal doses of both paracetamol and ibuprofen via comparison of both and via comparison with the novel combined drug. We have taken into account the side effect profile of the study drugs. This review will help oral surgeons to decide on which analgesic to prescribe following wisdom tooth removal. To compare the beneficial and harmful effects of paracetamol, ibuprofen and the novel combination of both in a single tablet for pain relief following the surgical removal of lower wisdom teeth, at different doses and administered postoperatively. We searched the Cochrane Oral Health Group'sTrials Register (to 20 May 2013); the Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library 2013, Issue 4); MEDLINE via OVID (1946 to 20 May 2013); EMBASE via OVID (1980 to 20 May 2013) and the metaRegister of Controlled Trials (to 20 May 2013). We checked the bibliographies of relevant clinical trials and review articles for further studies. We wrote to authors of the identified randomised controlled trials (RCTs), and searched personal references in an attempt to identify unpublished or ongoing RCTs. No language restriction was applied to the searches of the electronic databases. Only randomised controlled double-blinded clinical trials were included. Cross-over studies were included provided there was a wash out period of at least 14 days. There had to be a direct comparison in the trial of two or more of the trial drugs at any dosage. All trials used the third molar pain model. All trials

  20. Possessive Pronouns in European Portuguese and Old French

    Directory of Open Access Journals (Sweden)

    Matilde Miguel

    2002-12-01

    Full Text Available The aim of this paper is to bring European Portuguese (EP data into light, showing that, in spite of the lack of morphological evidence, the syntactic behaviour of possessives, across EP dialects, shows evidences for a tripartite possessive system (Cardinaletti, 1998; Cardinaletti & Starke, 1999. It will be argued that the syntactic position of possessives parallels the positions assumed for EP sentential subjects in non interrogative contexts: [Spec, AgrsP], [Spec, TP] and [Spec, VP]. As a matter of fact, depending on their syntactic properties and assuming, as null hypothesis, that the nominal head moves to Numb'º', possessives may occur in [Spec, AgrsNP], [Spec, NumbP] and [Spec, NP]. Furthermore, would it be so, this dialectal variation would be useful in order to understand the changes that have occurred in other romance languages in previous stages. It might be the case that the loss of weak possessive forms (“mien” in French parallels, among other things, the lack of sentential subjects in [Spec, TP].

  1. The goalkeeper influence on ball possession effectiveness in futsal

    Directory of Open Access Journals (Sweden)

    Vicente-Vila Pedro

    2016-06-01

    Full Text Available The aim of this study was to identify which variables were the best predictors of success in futsal ball possession when controlling for space and task related indicators, situational variables and the participation of the goalkeeper as a regular field player or not (5 vs. 4 or 4 vs. 4. The sample consisted of 326 situations of ball possession corresponding to 31 matches played by a team from the Spanish Futsal League during the 2010–2011, 2011–2012 and 2012–2013 seasons. Multidimensional qualitative data obtained from 10 ordered categorical variables were used. Data were analysed using chi-square analysis and multiple logistic regression analysis. Overall, the highest ball possession effectiveness was achieved when the goalkeeper participated as a regular field player (p<0.01, the duration of the ball possession was less than 10 s (p<0.01, the ball possession ended in the penalty area (p<0.01 and the defensive pressure was low (p<0.01. The information obtained on the relative effectiveness of offensive playing tactics can be used to improve team’s goal-scoring and goal preventing abilities.

  2. Ibuprofen-in-cyclodextrin-in-W/O/W emulsion - Improving the initial and long-term encapsulation efficiency of a model active ingredient.

    Science.gov (United States)

    Hattrem, Magnus N; Kristiansen, Kåre A; Aachmann, Finn L; Dille, Morten J; Draget, Kurt I

    2015-06-20

    A challenge in formulating water-in-oil-in-water (W/O/W) emulsions is the uncontrolled release of the encapsulated compound prior to application. Pharmaceuticals and nutraceuticals usually have amphipathic nature, which may contribute to leakage of the active ingredient. In the present study, cyclodextrins (CyDs) were used to impart a change in the relative polarity and size of a model compound (ibuprofen) by the formation of inclusion complexes. Various inclusion complexes (2-hydroxypropyl (HP)-β-CyD-, α-CyD- and γ-CyD-ibuprofen) were prepared and presented within W/O/W emulsions, and the initial and long-term encapsulation efficiency was investigated. HP-β-CyD-ibuprofen provided the highest encapsulation of ibuprofen in comparison to a W/O/W emulsion with unassociated ibuprofen confined within the inner water phase, with a four-fold increase in the encapsulation efficiency. An improved, although lower, encapsulation efficiency was obtained for the inclusion complex γ-CyD-ibuprofen in comparison to HP-β-CyD-ibuprofen, whereas α-CyD-ibuprofen had a similar encapsulation efficiency to that of unassociated ibuprofen. The lower encapsulation efficiency of ibuprofen in combination with α-CyD and γ-CyD was attributed to a lower association constant for the γ-CyD-ibuprofen inclusion complex and the ability of α-CyD to form inclusion complexes with fatty acids. For the W/O/W emulsion prepared with HP-β-CyD-ibuprofen, the highest encapsulation of ibuprofen was obtained at hyper- and iso-osmotic conditions and by using an excess molar ratio of CyD to ibuprofen. In the last part of the study, it was suggested that the chemical modification of the HP-β-CyD molecule did not influence the encapsulation of ibuprofen, as a similar encapsulation efficiency was obtained for an inclusion complex prepared with mono-1-glucose-β-CyD. Copyright © 2015 Elsevier B.V. All rights reserved.

  3. In Vivo Dissolution and Systemic Absorption of Immediate Release Ibuprofen in Human Gastrointestinal Tract under Fed and Fasted Conditions.

    Science.gov (United States)

    Koenigsknecht, Mark J; Baker, Jason R; Wen, Bo; Frances, Ann; Zhang, Huixia; Yu, Alex; Zhao, Ting; Tsume, Yasuhiro; Pai, Manjunath P; Bleske, Barry E; Zhang, Xinyuan; Lionberger, Robert; Lee, Allen; Amidon, Gordon L; Hasler, William L; Sun, Duxin

    2017-12-04

    In vivo drug dissolution in the gastrointestinal (GI) tract is largely unmeasured. The purpose of this clinical study was to evaluate the in vivo drug dissolution and systemic absorption of the BCS class IIa drug ibuprofen under fed and fasted conditions by direct sampling of stomach and small intestinal luminal content. Expanding current knowledge of drug dissolution in vivo will help to establish physiologically relevant in vitro models predictive of drug dissolution. A multilumen GI catheter was orally inserted into the GI tract of healthy human subjects. Subjects received a single oral dose of ibuprofen (800 mg tablet) with 250 mL of water under fasting and fed conditions. The GI catheter facilitated collection of GI fluid from the stomach, duodenum, and jejunum. Ibuprofen concentration in GI fluid supernatant and plasma was determined by LC-MS/MS. A total of 23 subjects completed the study, with 11 subjects returning for an additional study visit (a total of 34 completed study visits). The subjects were primarily white (61%) and male (65%) with an average age of 30 years. The subjects had a median [min, max] weight of 79 [52, 123] kg and body mass index of 25.7 [19.4, 37.7] kg/m 2 . Ibuprofen plasma levels were higher under fasted conditions and remained detectable for 28 h under both conditions. The AUC 0-24 and C max were lower in fed subjects vs fasted subjects, and T max was delayed in fed subjects vs fasted subjects. Ibuprofen was detected immediately after ingestion in the stomach under fasting and fed conditions until 7 h after dosing. Higher levels of ibuprofen were detected in the small intestine soon after dosing in fasted subjects compared to fed. In contrast to plasma drug concentration, overall gastric concentrations remained higher under fed conditions due to increased gastric pH vs fasting condition. The gastric pH increased to near neutrality after feedingbefore decreasing to acidic levels after 7 h. Induction of the fed state reduced systemic

  4. Optimisation of cosolvent concentration for topical drug delivery III--influence of lipophilic vehicles on ibuprofen permeation.

    Science.gov (United States)

    Watkinson, R M; Guy, R H; Oliveira, G; Hadgraft, J; Lane, M E

    2011-01-01

    Previously, we have reported the effects of water, ethanol, propylene glycol and various binary and ternary mixtures of these solvents on the permeation of ibuprofen in model membranes and in skin. The present study investigates the influence of lipophilic vehicles on the transport of ibuprofen in silicone membrane and in human skin. The permeation of ibuprofen was measured from mineral oil (MO), Miglyol® 812 (MG) and binary mixtures of MO and MG. The solubility of ibuprofen was 5-fold higher in MG than in MO, however, the permeation of ibuprofen from the pure vehicles and combinations of both was comparable in silicone membrane. Additionally, there were no significant differences in skin permeation for MO and MG vehicles. When the permeation of various hydrophilic and lipophilic vehicles is considered, a trend between flux values for the model membrane and skin is evident (r(2) = 0.71). The findings suggest that silicone membrane may provide information on qualitative trends in skin permeation for vehicles of diverse solubility and partition characteristics. Copyright © 2010 S. Karger AG, Basel.

  5. Antipyretic effect of ibuprofen in Gabonese children with uncomplicated falciparum malaria: a randomized, double-blind, placebo-controlled trial

    Directory of Open Access Journals (Sweden)

    Necek Magdalena

    2008-05-01

    Full Text Available Abstract Background Antipyretic drugs are widely used in children with fever, though there is a controversy about the benefit of reducing fever in children with malaria. In order to assess the effect of ibuprofen on fever compared to placebo in children with uncomplicated Plasmodium falciparum malaria in Gabon, a randomized double blind placebo controlled trial, was designed. Methods Fifty children between two and seven years of age with uncomplicated malaria were included in the study. For the treatment of fever, all patients "received" mechanical treatment when the temperature rose above 37.5°C. In addition to the mechanical treatment, continuous fanning and cooling blanket, patients were assigned randomly to receive ibuprofen (7 mg/kg body weight, every eight hours or placebo. Results The fever clearance time using a fever threshold of 37.5°C was similar in children receiving ibuprofen compared to those receiving placebo. The difference was also not statistically significant using a fever threshold of 37.8°C or 38.0°C. However, the fever time and the area under the fever curve were significantly smaller in the ibuprofen group compared to the placebo group. Conclusion Ibuprofen is effective in reducing the time with fever. The effect on fever clearance is less obvious and depends on definition of the fever threshold. Trial registration The trial registration number is: NCT00167713

  6. Effects of Exposure to Acetaminophen and Ibuprofen on Fetal Germ Cell Development in Both Sexes in Rodent and Human Using Multiple Experimental Systems

    DEFF Research Database (Denmark)

    Hurtado-Gonzalez, Pablo; Anderson, Richard A; Macdonald, Joni

    2018-01-01

    /ovaries using in vitro and xenograft approaches. METHODS: Gonocyte (TFAP2C+) number was reduced relative to controls in first-trimester human fetal testes exposed in vitro to acetaminophen (-28%) or ibuprofen (-22%) and also in ovaries exposed to acetaminophen (-43%) or ibuprofen (-49%). Acetaminophen exposure...

  7. Analgesic Efficacy of a New Immediate-Release/Extended-Release Formulation of Ibuprofen: Results From Single- and Multiple-Dose Postsurgical Dental Pain Studies.

    Science.gov (United States)

    Christensen, Steven; Paluch, Ed; Jayawardena, Shyamalie; Daniels, Stephen; Meeves, Suzanne

    2017-05-01

    Analgesic effects of ibuprofen immediate-release/extended-release (IR/ER) 600-mg tablets were evaluated in 2 randomized, double-blind, placebo-controlled dental pain studies. Patients 16-40 years old with moderate-severe pain following third-molar extraction received single-dose ibuprofen 600 mg IR/ER (formulation A or B), naproxen sodium 220 mg, or placebo (2:2:2:1; study 1) or 4 doses of ibuprofen 600 mg IR/ER (formulation A) or placebo (1:1; study 2). In study 1 (n = 196), mean (standard deviation [SD]) time-weighted sum of pain intensity difference scores for placebo, ibuprofen IR/ER A, ibuprofen IR/ER B, and naproxen, respectively, were 0.05 (9.2), 16.87 (9.4), 17.34 (10.5), and 12.66 (10.0) over 0-12 hours and -0.03 (4.1), 6.57 (4.4), 7.14 (5.2), and 5.14 (5.0) over 8-12 hours (all P ibuprofen IR/ER, respectively (P ibuprofen. Gastrointestinal adverse events predominated with placebo both after study medication administration and after rescue medication use, if applicable. Ibuprofen 600 mg IR/ER provided safe and effective analgesia after single and multiple doses. © 2016, The American College of Clinical Pharmacology.

  8. Themes in Spirit Possession in Ugandan Christianity | James ...

    African Journals Online (AJOL)

    . This paper discerns a number of common themes that run through many of these experiences. In particular, sex as a motif for deviance and evil is noted as a common feature of many of the possession stories and all contact with spirits is seen ...

  9. Gun Possession among Massachusetts Batterer Intervention Program Enrollees

    Science.gov (United States)

    Rothman, Emily F.; Johnson, Renee M.; Hemenway, David

    2006-01-01

    Batterers with access to firearms present a serious lethal threat to their partners. The purpose of this exploratory study is to estimate the prevalence of and risk markers for gun possession among Massachusetts men enrolled in batterer intervention programs. The authors found that 1.8% of the men reported having a gun in or around their home.…

  10. Licenses for possessing and applying radioactive sources, materials, etc

    International Nuclear Information System (INIS)

    Anon.

    1977-01-01

    Commercial and governmental institutions have been licensed by Dutch authorities to possess and apply radioactive sources, materials, etc. A summary is given and the list is subdivided into a number of sections such as radioactive sources, radioactive materials, X-ray equipment and technetium-generators

  11. 46 CFR 308.504 - Definition of territories and possessions.

    Science.gov (United States)

    2010-10-01

    ... 46 Shipping 8 2010-10-01 2010-10-01 false Definition of territories and possessions. 308.504 Section 308.504 Shipping MARITIME ADMINISTRATION, DEPARTMENT OF TRANSPORTATION EMERGENCY OPERATIONS WAR RISK INSURANCE War Risk Cargo Insurance I-Introduction § 308.504 Definition of territories and...

  12. Dynamics of the spirit possession phenomenon in Eastern Tanzania

    Directory of Open Access Journals (Sweden)

    Marja-Liisa Swantz

    1976-01-01

    Full Text Available The discussion on the spirit possession phenomenon is related in this study to the more general question of the role of religious institutions as part in the development process of a people living in a limited geographical area of a wider national society. It is assumed that religion, like culture in general, has its specific institutional forms as result of the historical development of a society, but at the same time religion is a force shaping that history. People's cultural resources influence their social and economic development and form a potential creative element in it'. Some of the questions to be asked are: "How are specific religious practices related to the dynamics of change in the societies in question? What is the social and religious context in which the spirit possession phenomenon occurs in them? What social and economic relations get their expression in them? To what extent is spirit possession in this case a means of exerting values and creatively overcoming a crisis or conflict which the changing social and economic relations impose on the people? The established spirit possession cults are here seen as the institutional forms of religious experience. At the same time it becomes evident that there is institutionalization in process as well as deinstitutionalization of spirit possession where it occurs outside established institutional forms. Institution is taken as a socially shared form of behaviour the significance of which is commonly recognized by those who share it. By the term spirit possession cult is meant a ritual form of spirit possession of a group which is loosely organized and without strict membership. The context of the study is four ethnic groups in Eastern Tanzania, near the coast of the Indian Ocean. The general theme of the project is The Role of Culture in the Restructuring of Tanzanian Rural Areas. The restructuring refers to a villagisation programme carried out in the whole country. People are being

  13. Differential blood pressure effects of ibuprofen, naproxen, and celecoxib in patients with arthritis: the PRECISION-ABPM (Prospective Randomized Evaluation of Celecoxib Integrated Safety Versus Ibuprofen or Naproxen Ambulatory Blood Pressure Measurement) Trial.

    Science.gov (United States)

    Ruschitzka, Frank; Borer, Jeffrey S; Krum, Henry; Flammer, Andreas J; Yeomans, Neville D; Libby, Peter; Lüscher, Thomas F; Solomon, Daniel H; Husni, M Elaine; Graham, David Y; Davey, Deborah A; Wisniewski, Lisa M; Menon, Venu; Fayyad, Rana; Beckerman, Bruce; Iorga, Dinu; Lincoff, A Michael; Nissen, Steven E

    2017-11-21

    Non-steroidal anti-inflammatory drugs (NSAIDs), both non-selective and selective cyclooxygenase-2 (COX-2) inhibitors, are among the most widely prescribed drugs worldwide, but associate with increased blood pressure (BP) and adverse cardiovascular (CV) events. PRECISION-ABPM, a substudy of PRECISION was conducted at 60 sites, to determine BP effects of the selective COX-2 inhibitor celecoxib vs. the non-selective NSAIDs naproxen and ibuprofen. In this double-blind, randomized, multicentre non-inferiority CV-safety trial, 444 patients (mean age 62 ± 10 years, 54% female) with osteoarthritis (92%) or rheumatoid arthritis (8%) and evidence of or at increased risk for coronary artery disease received celecoxib (100-200 mg bid), ibuprofen (600-800 mg tid), or naproxen (375-500 mg bid) with matching placebos in a 1: 1: 1 allocation, to assess the effect on 24-h ambulatory BP after 4 months. The change in mean 24-h systolic BP (SBP) in celecoxib, ibuprofen and naproxen-treated patients was -0.3 mmHg [95% confidence interval (CI), -2.25, 1.74], 3.7 (95% CI, 1.72, 5.58) and 1.6 mmHg (95% CI, -0.40, 3.57), respectively. These changes resulted in a difference of - 3.9 mmHg (P = 0.0009) between celecoxib and ibuprofen, of - 1.8 mmHg (P = 0.12) between celecoxib and naproxen, and of - 2.1 mmHg (P = 0.08) between naproxen and ibuprofen. The percentage of patients with normal baseline BP who developed hypertension (mean 24-h SBP ≥ 130 and/or diastolic BP ≥ 80 mmHg) was 23.2% for ibuprofen, 19.0% for naproxen, and 10.3% for celecoxib (odds ratio 0.39, P = 0.004 and odds ratio 0.49, P = 0.03 vs. ibuprofen and naproxen, respectively). In PRECISION-ABPM, allocation to the non-selective NSAID ibuprofen, compared with the COX-2 selective inhibitor celecoxib was associated with a significant increase of SBP, and a higher incidence of new-onset hypertension. gov number NCT00346216. Published on behalf of the European

  14. The digital code driven autonomous synthesis of ibuprofen automated in a 3D-printer-based robot.

    Science.gov (United States)

    Kitson, Philip J; Glatzel, Stefan; Cronin, Leroy

    2016-01-01

    An automated synthesis robot was constructed by modifying an open source 3D printing platform. The resulting automated system was used to 3D print reaction vessels (reactionware) of differing internal volumes using polypropylene feedstock via a fused deposition modeling 3D printing approach and subsequently make use of these fabricated vessels to synthesize the nonsteroidal anti-inflammatory drug ibuprofen via a consecutive one-pot three-step approach. The synthesis of ibuprofen could be achieved on different scales simply by adjusting the parameters in the robot control software. The software for controlling the synthesis robot was written in the python programming language and hard-coded for the synthesis of ibuprofen by the method described, opening possibilities for the sharing of validated synthetic 'programs' which can run on similar low cost, user-constructed robotic platforms towards an 'open-source' regime in the area of chemical synthesis.

  15. EXPERIENCE OF ADMINISTRATION OF IBUPROFEN IN COMPLEX TREATMENT OF INFANTS WITH MICROBIAL INFLAMMATORY DISEASES OF URINARY SYSTEM

    Directory of Open Access Journals (Sweden)

    O.K. Botvin’ev

    2009-01-01

    Full Text Available The microbial inflammatory diseases of urinary system in children can be often accompanied with fever and pain. The article presents an experience of ibuprofen (Nurofen for Children administration for the purpose of stopping fever and pain in 420 children in age 3 months — 3 years old with microbial inflammatory diseases of urinary system. The observation showed high effectiveness of short treatment with ibuprofen course (2–5 days. As clinical and laboratory observation showed, the short-termed administration of the drug was well-tolerated and did not cause significant adverse effects, excluding single cases of allergic rash and light dyspeptic disorders.Key words: children, microbial inflammatory diseases of urinary system, ibuprofen, treatment.(Voprosy sovremennoi pediatrii — Current Pediatrics. 2009;8(5:84-87

  16. The digital code driven autonomous synthesis of ibuprofen automated in a 3D-printer-based robot

    Directory of Open Access Journals (Sweden)

    Philip J. Kitson

    2016-12-01

    Full Text Available An automated synthesis robot was constructed by modifying an open source 3D printing platform. The resulting automated system was used to 3D print reaction vessels (reactionware of differing internal volumes using polypropylene feedstock via a fused deposition modeling 3D printing approach and subsequently make use of these fabricated vessels to synthesize the nonsteroidal anti-inflammatory drug ibuprofen via a consecutive one-pot three-step approach. The synthesis of ibuprofen could be achieved on different scales simply by adjusting the parameters in the robot control software. The software for controlling the synthesis robot was written in the python programming language and hard-coded for the synthesis of ibuprofen by the method described, opening possibilities for the sharing of validated synthetic ‘programs’ which can run on similar low cost, user-constructed robotic platforms towards an ‘open-source’ regime in the area of chemical synthesis.

  17. Novel HPC-ibuprofen conjugates: synthesis, characterization, thermal analysis and degradation kinetics

    International Nuclear Information System (INIS)

    Hussain, M.A.; Lodhi, B.A.; Abbas, K.

    2014-01-01

    Naturally occurring hydrophilic polysaccharides are advantageously used as drug carriers because they provide a mechanism to improve drug action. Hydroxypropylcellulose (HPC) is water-soluble, biocompatible and bears hydroxyl groups for drug conjugation outside the parent polymeric chains. This unique geometry allows the attachment of drug molecules with higher covalent loading. The HPC-Ibuprofen conjugates as macromolecular prodrugs were therefore synthesized employing homogenous and one pot reaction methodologies using p-toluenesulfonyl chloride in N,N-dimethylacetamide solvent at 80 degree C for 24 h under nitrogen atmosphere. The imidazole was used as a base for neutralization of acidic impurities. Present strategy appeared effective to get high yield (77-81%) and high degree of drug substitution (DS 0.88-1.40) onto the HPC polymer as determined by the acid-base titration and verified by 1H-NMR spectroscopy. The gel permeation chromatography has shown uni-modal absorption which indicates no significant degradation of polymer during reaction. Macromolecular prodrugs with different DS of ibuprofen were synthesized, purified, characterized and found soluble in organic solvents. From thermogravimetric analysis, initial, maximum and final degradation temperatures of the conjugates were calculated and compared for relative thermal stability. Thermal degradation kinetics was also studied and results have indicated that degradation of conjugates follows about first order kinetics as calculated by Kissinger model. The energy of activation was also found moderate 92.38, 99.34 and 87.34 kJ/mol as calculated using Friedman, Broido and Chang models. It was found that these novel prodrugs of ibuprofen were thermally stable therefore these may have potential pharmaceutical applications. (author)

  18. Antipyretic efficacy and tolerability of oral ibuprofen, oral dipyrone and intramuscular dipyrone in children: a randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Judith Prado

    Full Text Available CONTEXT AND OBJECTIVE: Dipyrone is a widely used over-the-counter antipyretic in Latin America, and elsewhere among Latin immigrants. Despite limited evidence, physicians often prescribe oral ibuprofen or intramuscular dipyrone as the most effective antipyretics. Our aim was to compare the antipyretic efficacy and tolerability of a single dose of oral ibuprofen, oral dipyrone or intramuscular dipyrone in febrile children. DESIGN AND SETTING: Randomized, single-blind clinical trial, at San Bartolomé Mother-Child National Teaching Hospital, Lima, Peru. METHODS: Children from six months to six years old with fever (rectal temperature: 38.3 to 39.8° C in the emergency ward between February and June 2003 were eligible. Seventy-five children were randomly assigned to receive a single dose of oral ibuprofen (10 mg/kg, oral dipyrone (15 mg/kg or intramuscular dipyrone (15 mg/kg. The primary outcome was mean temperature reduction after 30, 45, 60, 90 and 120 minutes. Secondary outcomes were fever-associated symptoms and clinical adverse events. RESULTS: Fever decreased by about 0.5° C after 45 minutes and by about 1.0° C after 120 minutes in all three groups. Mean temperatures were similar for the three groups at all times. There was a significant decrease in fever-associated symptoms for all groups. Six patients (four receiving oral dipyrone and two receiving ibuprofen were withdrawn because of vomiting within 20 minutes after first dose of study medication. One patient assigned to oral ibuprofen presented transient urticaria. CONCLUSIONS: Antipyretic efficacy and tolerability were similar for oral ibuprofen, oral dipyrone and intramuscular dipyrone. Oral antipyretics seem more appropriate for feverish children.

  19. [Has the use of antipyretics been modified after the introduction of different concentrations of ibuprofen into the market?].

    Science.gov (United States)

    García Blanes, C P; Rodríguez-Cantón Pascual, P; Morales-Carpi, C; Morales-Olivas, F J

    2014-12-01

    Due to the emergence of new pharmaceutical presentations of ibuprofen (40 mg/ml), an analysis was made on the use of antipyretics in pediatric outpatient in Spain. A cross-sectional, observational, descriptive study was carried out on a sample of children under 14 years old with treated febrile syndrome, seen in the Emergency Room of the Hospital General Universitario de Valencia from November 2012 to January 2013. Of the 217 children included, 144 were treated with paracetamol or ibuprofen, 69 received both drugs, and one received paracetamol and metamizol. There were 58.7% of exposures to paracetamol and 40.9% to ibuprofen. The parents decided the use of antipyretics in 63.2% of cases. In 98 exposures the dose was different from that authorized in the labeling of the drug (off-label use). Ibuprofen was used off-label in 40.2% of cases, mostly by underdosing (35.9%). Paracetamol was used off-label in 29.8% of cases, predominantly overdose (26.8%), with the difference being statistically significant. No significant differences were observed in the off-label use in either monotherapy or combined use. There were also no differences when antipyretics prescribed by doctors or given directly by parents were evaluated separately. The majority of children with treated febrile syndrome seen in the Emergency Room were receiving antipyretic drugs after a parental decision. Paracetamol is the most commonly used drug and one in three children received it simultaneously with ibuprofen. The antipyretics were used off label in one-third of the cases. Off label use of ibuprofen is increasing, and is probably due to the existence of different pharmaceutical presentations. Copyright © 2013 Asociación Española de Pediatría. Published by Elsevier Espana. All rights reserved.

  20. Comparison of analgesic efficacy of flupirtine maleate and ibuprofen in gynaecological ambulatory surgeries: A randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Vanita Ahuja

    2015-01-01

    Full Text Available Background and Aims: Flupirtine maleate is a centrally acting, non-opioid analgesic with unique muscle relaxant properties as compared to common analgesics. The aim of this study was to compare post-operative analgesic efficacy of flupirtine maleate and ibuprofen in patients undergoing gynaecological ambulatory surgeries. Methods: This prospective, randomised controlled study was conducted in 60 women of American Society of Anesthesiologists physical status I/II, 18-70 years of age and scheduled to undergo gynaecological ambulatory surgeries. The participants were randomised to receive either 100 mg oral flupirtine maleate (group flupirtine, n = 30 or 800 mg oral ibuprofen (group ibuprofen, n = 30, 1 h prior to surgery and then every 8 h for 48 h. Verbal Numerical Rating Scale (VNRS on movement was assessed at 0, 2, 4, 6 and 8 h following surgery. Following discharge from hospital, the patients were interviewed telephonically at 12, 24 and 48 h post-operatively. VNRS was statistically analysed using Mann-Whitney test. Results: VNRS on movement was statistically reduced at 2 h after surgery (P = 0.04 in group flupirtine as compared to group ibuprofen. The analgesic efficacy was similar in both the groups at 4, 6, 8, 12, 24 and 48 h after surgery. The satisfaction scores at 24 and 48 h post-operatively were superior in group flupirtine as compared to group ibuprofen (P < 0.001. Conclusion: Analgesic efficacy of flupirtine maleate was comparable with ibuprofen in patients in ambulatory gynaecological patients up to 48 h postoperatively with superior satisfaction scores.

  1. Comparison of the effect of ibuprofen and slow-released Diclofenac Sodium in controlling post endodontic pain

    Directory of Open Access Journals (Sweden)

    Saatchi M

    2010-01-01

    Full Text Available "nBackground and Aims: Despite the significant improvement in dentistry, pain after endodontic therapy is still of concern for patients. Non-steroidal anti-inflammatory drugs are the most commonly prescribed oral analgesics used for dental pain relief after root canal treatment. The purpose of this study was to compare the effectiveness of Ibuprofen versus slow-released Diclofenac Sodium in controlling pain following root canal treatment. "nMaterials and Methods: In this randomized clinical trial, mandibular molars with irreversible pulpitis in 90 patients were selected. The patients were divided into three groups (Ibuprofen, slow-released Diclofenac Sodium and placebo. After examination patients filled in the consent form. Then they received one of the mentioned drugs. After inferior alveolar nerve block, access cavity was prepared and the root canals were prepared using passive step back method. The canals were dried and temporary filling material was placed. Then the pain evaluation form (visual analog scale was explained and delivered to the patients. Data were analyzed using Repeated Measurement ANOVA, Kruskal-wallis and Man-Whitney U tests. "nResults: The mean pain intensity in slow-released Diclofenac Sodium group was 0.87 0.95, 1.17 1.10 for Ibuprofen group, and 2.14  1.70 for placebo group. The differences between groups were statistically significant (P<0.001. The effect of Ibuprofen in controlling post endodontic pain in the first 2 hours was more than slow-released Diclofenac Sodium (P=0.01, but in 10, 18, and 36 hours after treatment, slow-released Diclofenac Sodium was more effective than Ibuprofen (P<0.001. "nConclusion: Premedication with single dose of slow-released Diclofenac Sodium can control post endodontic pain for a longer period of time compared with Ibuprofen. "n.

  2. Efficacy of preoperative ibuprofen and meloxicam on the success rate of inferior alveolar nerve block for teeth with irreversible pulpitis.

    Science.gov (United States)

    Shantiaee, Yazdan; Javaheri, Sahar; Movahhedian, Amir; Eslami, Sarah; Dianat, Omid

    2017-04-01

    The purpose of this study was to determine whether premedication with ibuprofen or meloxicam increases the success rate of anaesthesia in teeth with irreversible pulpitis. In this parallel, double-blind clinical trial, 92 patients diagnosed with irreversible pulpitis were randomly divided into four groups of 23 patients. The first group (the no-premedication group) received no premedication, the second group (the meloxicam group) received 7.5 mg of meloxicam, the third group (the ibuprofen group) received 600 mg of ibuprofen, and the fourth group (the placebo group) received placebo 1 hour before intervention. Before taking the medication, electrical pulp testing (EPT) and the Heft-Parker visual analogue scale (VAS) were used to evaluate sensitivity and pain at baseline. Then, local anaesthesia was injected, and after 15 minutes, EPT was used again to evaluate tooth sensitivity. The pain during access preparation was also recorded using the Heft-Parker VAS. Ninety-two patients were analysed. The success rates of local anaesthesia were 21.7%, 34.8%, 78.3% and 73.9% in the no-premedication, placebo, ibuprofen and meloxicam groups, respectively, according to the EPT values. Considering the Heft-Parker VAS values, no premedication gave a 21.7% success rate, placebo gave a 34.8% success rate, ibuprofen gave an 82.6% success rate and meloxicam gave a 65.2% success rate. The ibuprofen and meloxicam groups showed significantly better results than the placebo and no-premedication groups (P inferior alveolar nerve block anaesthesia for teeth with irreversible pulpitis; however, neither drug provided profound anaesthesia. © 2016 FDI World Dental Federation.

  3. Paracetamol, Ibuprofen, and Recurrent Major Cardiovascular and Major Bleeding Events in 19 120 Patients With Recent Ischemic Stroke.

    Science.gov (United States)

    Gonzalez-Valcarcel, Jaime; Sissani, Leila; Labreuche, Julien; Bousser, Marie-Germaine; Chamorro, Angel; Fisher, Marc; Ford, Ian; Fox, Kim M; Hennerici, Michael G; Mattle, Heinrich P; Rothwell, Peter M; Steg, Philippe Gabriel; Vicaut, Eric; Amarenco, Pierre

    2016-04-01

    The presumed safety of paracetamol in high-cardiovascular risk patients has been questioned. We determined whether paracetamol or ibuprofen use is associated with major cardiovascular events (MACE) or major bleeding in 19 120 patients with recent ischemic stroke or transient ischemic attack of mainly atherothrombotic origin included in the Prevention of cerebrovascular and cardiovascular events of ischemic origin with terutroban in patients with a history of ischemic stroke or transient ischemic attack (PERFORM) trial. We performed 2 nested case-control analysis (2153 cases with MACE during trial follow-up and 4306 controls matched on Essen stroke risk score; 809 cases with major bleeding matched with 1616 controls) and a separate time-varying analysis. 12.3% were prescribed paracetamol and 2.5% ibuprofen. Median duration of treatment was 14 (interquartile range 5-145) days for paracetamol and 9 (5-30) days for ibuprofen. Paracetamol, but not ibuprofen, was associated with increased risk of MACE (odds ratio 1.21, 95% confidence interval [CI] 1.04-1.42) or a major bleeding (odds ratio 1.60, 95% CI 1.26-2.03), with no impact of daily dose and duration of paracetamol treatment. Time-varying analysis found an increased risk of MACE with both paracetamol (hazard ratio 1.22, 95% CI 1.05-1.43) and ibuprofen (hazard ratio 1.47, 95% CI 1.06-2.03) and of major bleeding with paracetamol (hazard ratio 1.95, 95% CI 1.45-2.62). There was a weak and inconsistent signal for association between paracetamol or ibuprofen and MACE or major bleeding, which may be related to either a genuine but modest effect of these drugs or to residual confounding. http://www.isrctn.com. Unique identifier: ISRCTN66157730. © 2016 American Heart Association, Inc.

  4. Effects of Humidity and Surfaces on the Melt Crystallization of Ibuprofen

    OpenAIRE

    Lee, Dong-Joo; Lee, Suyang; Kim, Il Won

    2012-01-01

    Melt crystallization of ibuprofen was studied to understand the effects of humidity and surfaces. The molecular self-assembly during the amorphous-to-crystal transformation was examined in terms of the nucleation and growth of the crystals. The crystallization was on Al, Au, and self-assembled monolayers with –CH3, –OH, and –COOH functional groups. Effects of the humidity were studied at room temperature (18–20 °C) with relative humidity 33%, 75%, and 100%. Effects of t...

  5. Patient-reported outcomes of therapy with two brands of ibuprofen

    Directory of Open Access Journals (Sweden)

    Nwidu LL

    2008-09-01

    Full Text Available Objective: To investigate patients’ reported outcome following medication with two brands of 400 mg ibuprofen used to alleviate musculoskeletal pains.Methods: Adult peasant manual laborers (85 who met criteria were randomly assigned to receive either of the brands (A or B. Data on pain alleviation were gathered using the Short-Form McGill Pain Questionnaire (SF-MPQ, Visual Analogue Scale (VAS, Present Pain Intensity (PPI, and Clinical Global Impression of Improvement (CGII scales. Interval data obtained from the two brands were compared using the Students’ t-test at 95% confidence interval.Results: There were 42 participants, mean age=29.2 (SD=1.37 assigned to brand A and 43 (mean age=28.8 SD=1.14 in brand B of ibuprofen 400 mg. Brand B was consistently rated higher than brand A. Scores for medication efficacy were 10.4 (SD=1.65 (brand A and 11.4 (SD=1.68 (brand B; t=2.768, P=0.007. Alleviation of pain symptoms: 10.8 (SD=1.64 and 11.6 (SD=1.72; t = 2.194, P=0.031. Similarly, rated scores on the impact of pain on quality of life were 10.5 (SD=2.00 and 12.1 (SD=1.85; t=3.830, P<0.001. There was a reduction in Present Pain Intensity scores by 32.7% and 34.3% for Brand A and brand B participants respectively. The decrease in Visual Analog pain scale score was 35.9% and 37.3% for brand A and brand B participants respectively. The decrease in SF-MPQ was by 85.1% and 69.9% for the brand A and brand B groups respectively. The clinical global impression of improvement for both groups of patients indicated an improvement rate of 71.4% and 61.9% for brand A and 81.4% and 74.4% for brand B participants. Conclusion: This clinical study infers that though the two brands of ibuprofen 400 mg are legally pharmaceutical equivalent, they are not clinically equivalent. In most of the parameters evaluated, brand B was rated more efficacious than brand A. This explains the patients’ preferences and demand for this brand of ibuprofen in the Nigerian community.

  6. Vaginal Use of Ibuprofen Isobutanolammonium (Ginenorm): Efficacy, Tolerability, and Pharmacokinetic Data: A Review of Available Data

    Science.gov (United States)

    Milani, Massimo; Iacobelli, Piero

    2012-01-01

    Vaginal infection and inflammation with or without vulvar involvement are very common gynecologicaly clinical conditions associated with morbidity and reduced quality of life. Vaginal infections are commonly treated with causal antimicrobial treatments. In addition to specific antimicrobial treatment, anti-inflammatory therapy, both systemic or topical (vaginal douche), could be useful in the integrated treatment approach of these conditions reducing symptoms and speeding up the recovery in vulvovaginitis. Ibuprofen is a well-known effective and well-tolerated anti-COX (anti-COX1 and COX2) compound. In addition, several in vitro studies suggest that Ibuprofen shares antimicrobial and antifungal activities. Ibuprofen isobutanolammonium (Ib-isb) (Ginenorm) is a soluble salt from formulation suitable for external and intravaginal use. This salt completely dissociates in aqueous solution. Ib-isob is available in sachet and vaginal douche pharmaceutical formulations. Clinical efficacy of Ib-isob has been documented in 10 clinical studies (6 controlled and 4 open trials) which have enrolled in total 399 women with vulvovaginitis. The six controlled clinical trials were performed both versus placebo (2 studies) or versus active comparators such as benzydamine. In these studied, Ib-Isb has been used in general for 7 consecutive days with a twice application daily regimen at the dose of 1 g per application. Topical application of Ib-isob induced a marked and rapid reduction in signs (erythema, oedema) and symptoms (itching and burning sensation) of vulvovaginitis. In head-to-head studies carried out in comparison with other topical products, Ib-isob induced a more rapid reduction in both subjective and objective symptoms. In particular a remarkable significant improvement of all the symptoms has been observed in the group of patients treated with Ib-isob in comparison with women receiving benzydamine. The clinical data available for Ib-isob confirm that this salt

  7. DRESS syndrome secondary to ibuprofen as a cause of hyperacute liver failure

    Directory of Open Access Journals (Sweden)

    Valentín Roales-Gómez

    2014-08-01

    Full Text Available Acute liver failure has a high mortality and its most frequent cause in Spain is viral infection. In this article, we present a case of fulminant liver failure. The failure is secondary to an idiosyncratic reaction to ibuprofen, an entity included in the DRESS syndrome. This syndrome plays a key role in the differential diagnosis of acute liver failure, since its unfortunate course often requires liver transplantation as the only useful therapeutic weapon. This case illustrates the need for an efficient coordination between hospitals as a key factor for improving the prognosis.

  8. Symptomatic treatment (ibuprofen or antibiotics (ciprofloxacin for uncomplicated urinary tract infection? - Results of a randomized controlled pilot trial

    Directory of Open Access Journals (Sweden)

    Wegscheider Karl

    2010-05-01

    Full Text Available Abstract Background Uncomplicated lower urinary tract infections (UTI are usually treated with antibiotics. However, there is little evidence for alternative therapeutic options. This pilot study was set out 1 to make a rough estimate of the equivalence of ibuprofen and ciprofloxacin for uncomplicated urinary tract infection with regard to symptom resolution, and 2 to demonstrate the feasibility of a double-blind, randomized controlled drug trial in German general practices. Methods We performed a double-blind, randomized controlled pilot trial in 29 German general practices. Eighty otherwise healthy women aged 18 to 85 years, presenting with at least one of the main UTI symptoms dysuria and frequency and without any complicating factors, were randomly assigned to receive either ibuprofen 3 × 400 mg oral or ciprofloxacin 2 × 250 mg (+1 placebo oral, both for three days. Intensity of main symptoms - dysuria, frequency, low abdominal pain - was recorded at inclusion and after 4, 7 and 28 days, scoring each symptom from 0 (none to 4 (very strong. The primary endpoint was symptom resolution on Day 4. Secondary outcomes were the burden of symptoms on Days 4 and 7 (based on the sum score of all symptoms, symptom resolution on Day 7 and frequency of relapses. Equivalence margins for symptom burden on Day 4 were pre-specified as +/- 0.5 sum score points. Data analysis was done by intention to treat and per protocol. Randomization was carried out on patient level by computer programme in blocks of six. Results Seventy-nine patients were analyzed (ibuprofen n = 40, ciprofloxacin n = 39. On Day 4, 21/36 (58.3% of patients in the ibuprofen-group were symptom-free versus 17/33 (51.5% in the ciprofloxacin-group. On Day 4, ibuprofen patients reported fewer symptoms in terms of total sum score (1; SD 1,42 than ciprofloxacin patients (1,3; SD 1,9, difference -0,33 (95% CI (-1,13 to +0,47, PP (per protocol analysis. During Days 0 and 9, 12/36 (33% of patients

  9. Descending with Angels: Jinn Possession, Islamic Exorcism, and Psychiatry

    DEFF Research Database (Denmark)

    Suhr, Christian

    What is it like to be a Muslim possessed by a jinn spirit? How do you find refuge from madness and evil in a place like Denmark? In this book I explore some of the ways in which Muslims in the West have sought to protect themselves. Over several years I followed Muslim patients being treated.......” In the book I analyze how these broader social and political issues are paralleled in the invisible dynamics of jinn possession and psychosis, proposing new theoretical perspectives on religious and psychiatric healing as ritual practices for dealing with the invisible in human life....... hypervisible in public discourse through intensive state monitoring, surveillance, and media coverage. Yet their religion of Islam remains poorly understood and is frequently identified by politicians, commentators, and even healthcare specialists as the underlying invisible cause of “integration problems...

  10. The Regulation of the Possession of Weapons at Gatherings

    Directory of Open Access Journals (Sweden)

    Pieter du Toit

    2013-12-01

    Full Text Available The Dangerous Weapons Act 15 of 2013 provides for certain prohibitions and restrictions in respect of the possession of a dangerous weapon and it repeals the Dangerous Weapons Act 71 of 1968 as well as the different Dangerous Weapons Acts in operation in the erstwhile TBVC States. The Act also amends the Regulation of Gatherings Act 205 of 1993 to prohibit the possession of any dangerous weapon at a gathering or demonstration. The Dangerous Weapons Act provides for a uniform system of law governing the use of dangerous weapons for the whole of South Africa and it furthermore no longer places the onus on the individual charged with the offence of the possession of a dangerous weapon to show that he or she did not have any intention of using the firearm for an unlawful purpose. The Act also defines the meaning of a dangerous weapon. According to our court’s interpretation of the Dangerous Weapons Act 71 of 1968 a dangerous weapon was regarded as an object used or intended to be used as a weapon even if it had not been designed for use as a weapon. The Act, however, requires the object to be capable of causing death or inflicting serious bodily harm if it were used for an unlawful purpose. The possession of a dangerous weapon, in circumstances which may raise a reasonable suspicion that the person intends to use it for an unlawful purpose, attracts criminal liability. The Act also provides a useful set of guidelines to assist courts to determine if a person charged with the offence of the possession of a dangerous weapon had indeed intended to use the weapon for an unlawful purpose. It seems, however, that the Act prohibits the possession of a dangerous weapon at gatherings, even if the person carrying the weapon does not intend to use it for an unlawful purpose. The state will, however, have to prove that the accused had the necessary control over the object and the intention to exercise such control, as well as that the object is capable of

  11. Emotional regulation, attachment to possessions and hoarding symptoms.

    Science.gov (United States)

    Phung, Philip J; Moulding, Richard; Taylor, Jasmine K; Nedeljkovic, Maja

    2015-10-01

    This study aimed to test which particular facets of emotion regulation (ER) are most linked to symptoms of hoarding disorder, and whether beliefs about emotional attachment to possessions (EA) mediate this relationship. A non-clinical sample of 150 participants (108 females) completed questionnaires of emotional tolerance (distress tolerance, anxiety sensitivity, negative urgency - impulsivity when experiencing negative emotions), depressed mood, hoarding, and beliefs about emotional attachment to possessions. While all emotional tolerance measures related to hoarding, when considered together and controlling for depression and age, anxiety sensitivity and urgency were the significant predictors. Anxiety sensitivity was fully mediated, and urgency partially mediated, via beliefs regarding emotional attachment to possessions. These findings provide further support for (1) the importance of anxiety sensitivity and negative urgency for hoarding symptoms, and (2) the view that individuals with HD symptoms may rely on items for emotion regulation, leading to stronger beliefs that items are integral to emotional wellbeing. © 2015 Scandinavian Psychological Associations and John Wiley & Sons Ltd.

  12. Release kinetics and cell viability of ibuprofen nanocrystals produced by melt-emulsification.

    Science.gov (United States)

    Fernandes, A R; Dias-Ferreira, J; Cabral, C; Garcia, M L; Souto, E B

    2018-06-01

    The clinical use of poorly water-soluble drugs has become a big challenge in pharmaceutical development due to the compromised bioavailability of the drugs in vivo. Nanocrystals have been proposed as a formulation strategy to improve the dissolution properties of these drugs. The benefits of using nanocrystals in drug delivery, when compared to other nanoparticles, are related to their production facilities, simple structure, and suitability for a variety of administration routes. High pressure homogenization (HPH) is the most promising production process, which can be employed at low or high temperatures. Ibuprofen nanocrystals with a mean size below 175 nm, and polydispersity below 0.18, have been produced by melt-emulsification, followed by HPH. Two nanocrystal formulations, differing on the surfactant composition, have been produced, their in vitro ibuprofen release tested in Franz diffusion cells and adjusted to several kinetic models (zero order, first order, Higuchi, Hixson-Crowell, Korsmeyer-Peppas, Baker-Lonsdale and Weibull model). Cell viability was assessed at 3, 6 and 24 h of incubation on human epithelial colorectal cells (Caco-2) by AlamarBlue ® colorimetric assay. For both formulations, Caco-2 cells viability was dependent on the drug concentration and time of exposure. Copyright © 2018 Elsevier B.V. All rights reserved.

  13. Contribution of microorganisms to non-extractable residue formation during biodegradation of ibuprofen in soil.

    Science.gov (United States)

    Nowak, Karolina M; Girardi, Cristobal; Miltner, Anja; Gehre, Matthias; Schäffer, Andreas; Kästner, Matthias

    2013-02-15

    Non-extractable residues (NER) formed during biodegradation of organic contaminants in soil are considered to be mainly composed of parent compounds or their primary metabolites with hazardous potential. However, in the case of biodegradable organic compounds, the soil NER may also contain microbial biomass components, for example fatty acids (FA) and amino acids (AA). After cell death, these biomolecules are subsequently incorporated into non-living soil organic matter (SOM) and are stabilised ultimately forming hardly extractable residues of biogenic origin. We investigated biodegradation of (13)C(6)-ibuprofen, in particular the metabolic incorporation of the (13)C-label into FA and AA and their fate in soil over 90 days. (13)C-FA and (13)C-AA amounts in the living microbial biomass fraction initially increased, then decreased over time and were continuously incorporated into the non-living SOM pool. The (13)C-FA in the non-living SOM remained stable from day 59 whereas the contents of (13)C-AA slightly increased until the end. After 90 days, nearly all NER were biogenic as they were made up almost completely by natural biomass compounds. The presented data demonstrated that the potential environmental risks related to the ibuprofen-derived NER are overestimated. Copyright © 2012 Elsevier B.V. All rights reserved.

  14. Degradation of ibuprofen by hydrodynamic cavitation: Reaction pathways and effect of operational parameters.

    Science.gov (United States)

    Musmarra, Dino; Prisciandaro, Marina; Capocelli, Mauro; Karatza, Despina; Iovino, Pasquale; Canzano, Silvana; Lancia, Amedeo

    2016-03-01

    Ibuprofen (IBP) is an anti-inflammatory drug whose residues can be found worldwide in natural water bodies resulting in harmful effects to aquatic species even at low concentrations. This paper deals with the degradation of IBP in water by hydrodynamic cavitation in a convergent-divergent nozzle. Over 60% of ibuprofen was degraded in 60 min with an electrical energy per order (EEO) of 10.77 kWh m(-3) at an initial concentration of 200 μg L(-1) and a relative inlet pressure pin=0.35 MPa. Five intermediates generated from different hydroxylation reactions were identified; the potential mechanisms of degradation were sketched and discussed. The reaction pathways recognized are in line with the relevant literature, both experimental and theoretical. By varying the pressure upstream the constriction, different degradation rates were observed. This effect was discussed according to a numerical simulation of the hydroxyl radical production identifying a clear correspondence between the maximum kinetic constant kOH and the maximum calculated OH production. Furthermore, in the investigated experimental conditions, the pH parameter was found not to affect the extent of degradation; this peculiar feature agrees with a recently published kinetic insight and has been explained in the light of the intermediates of the different reaction pathways. Copyright © 2015 Elsevier B.V. All rights reserved.

  15. The Metastability and Nucleation Thresholds of Ibuprofen in Ethanol and Water-Ethanol Mixtures

    Directory of Open Access Journals (Sweden)

    Abdur Rashid

    2015-01-01

    Full Text Available To investigate the crystallization of ibuprofen [((RS-2-(4-(2-methylpropyl phenyl propanoic acid] from ethanol and water-ethanol mixtures it is necessary to know the nucleation limits of its solutions. In the absence of crystals, nucleation will seldom occur below the PNT (primary nucleation threshold. If crystals are present, nucleation will seldom occur until below the lower SNT (secondary nucleation threshold. Below the SNT, crystals will still grow with negligible nucleation. PNT and SNT values (expressed as relative supersaturation σ have been measured at 10, 25, and 40°C for ibuprofen in ethanol and in a range of mixtures of different ethanol (E/water (W ratios. The induction times were determined from observing the times to nucleate for a range of different supersaturated solutions at a given temperature and E/W ratio. As expected, lowering the supersaturation leads to longer induction times. In ethanol, the SNT values are small and thus the secondary metastable zone width (MSZW is relatively narrow with a 1 h SNT relative supersaturation typically about σ ~ 0.05. The 1 h PNT values are much larger with values for σ around 0.3. In aqueous ethanolic mixtures at 25°C, both the PNT and SNT decrease as the water content increases.

  16. Influence of crystal habit on the compression and densification mechanism of ibuprofen

    Science.gov (United States)

    Di Martino, Piera; Beccerica, Moira; Joiris, Etienne; Palmieri, Giovanni F.; Gayot, Anne; Martelli, Sante

    2002-08-01

    Ibuprofen was recrystallized from several solvents by two different methods: addition of a non-solvent to a drug solution and cooling of a drug solution. Four samples, characterized by different crystal habit, were selected: sample A, sample E and sample T, recrystallized respectively from acetone, ethanol and THF by addition of water as non-solvent and sample M recrystallized from methanol by temperature decrease. By SEM analysis, sample were characterized with the respect of their crystal habit, mean particle diameter and elongation ratio. Sample A appears stick-shaped, sample E acicular with lamellar characteristics, samples T and M polyhedral. DSC and X-ray diffraction studies permit to exclude a polymorphic modification of ibuprofen during crystallization. For all samples micromeritics properties, densification behaviour and compression ability was analysed. Sample M shows a higher densification tendency, evidenciated by its higher apparent and tapped particle density. The ability to densificate is also pointed out by D0' value of Heckel's plot, which indicate the rearrangement of original particles at the initial stage of compression. This fact is related to the crystal habit of sample M, which is characterized by strongly smoothed coins. The increase in powder bed porosity permits a particle-particle interaction of greater extent during the subsequent stage of compression, which allows higher tabletability and compressibility.

  17. Stereoselective and nonstereoselective effects of ibuprofen enantiomers on mitochondrial beta-oxidation of fatty acids

    Energy Technology Data Exchange (ETDEWEB)

    Freneaux, E.; Fromenty, B.; Berson, A.; Labbe, G.; Degott, C.; Letteron, P.; Larrey, D.; Pessayre, D. (Unite de Recherches de Physiolopathologie Hepatique (INSERM U-24), Hopital Beaujon, Clichy (France))

    1990-11-01

    The effects of the R-(-) and S-(+)ibuprofen enantiomers were first studied in vitro with mouse liver mitochondria incubated in the presence of various concentrations of exogenous coenzyme A. In the presence of a low concentration of coenzyme A (2.5 microM), the R-(-)enantiomer (which forms an acylcoenzyme A) inhibited stereoselectively the beta oxidation of (1-{sup 14}C)palmitic acid but not that of (1-{sup 14}C)palmitoyl-L-carnitine (which can directly enter the mitochondria). In the presence, however, of a concentration of coenzyme A (50 microM) reproducing that present in liver cell cytosol, both enantiomers (2 mM) slightly inhibited the beta oxidation of (1-{sup 14}C)palmitic acid and markedly inhibited the beta oxidation of (1-{sup 14}C)octanoic acid and (1-{sup 14}C)butyric acid. In vivo, both enantiomers (1 mmol.kg-1) similarly inhibited the formation of ({sup 14}C)CO{sub 2} from (1-{sup 14}C)fatty acids. Both enantiomers similarly decreased plasma ketone bodies. Both similarly increased hepatic triglycerides, and both produced mild microvesicular steatosis of the liver. We conclude that both ibuprofen enantiomers inhibit beta oxidation of fatty acids in vitro and in vivo. In addition, the R-(-)enantiomer may stereoselectively sequester coenzyme A; at low concentrations of coenzyme A in vitro, this may stereoselectively inhibit the mitochondrial uptake and beta oxidation of long chain fatty acids.

  18. P25 nanoparticles decorated on titania nanotubes arrays as effective drug delivery system for ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Zhang; Xie, Chunlin; Luo, Fei; Li, Ping; Xiao, Xiufeng, E-mail: xfxiao@fjnu.edu.cn

    2015-01-01

    Highlights: • P25 nanoparticles decorated on titania nanotube arrays were prepared by hydrothermal treatment. • P25 nanoparticles were conducive to improve the loading effect of ibuprofen into nanotube arrays. • The diameters of the decorated nanotubes were decrease markedly which led to an effective and prolonged drug release. - Abstract: In this study, uniformly distributed layer of P25 nanoparticles (NPs) decorated on titania (TiO{sub 2}) nanotubes (TNTs) arrays was prepared in a teflon-lined stainless steel autoclave by the hydrothermal treatment. To investigate the influence of the P25 concentration, different concentrations of P25 NPs were added into the solution to obtain the optimal decorative effect. TNTs decorated with P25 (TNTs–P25) and TNTs without P25 decorated on its surface were loaded with ibuprofen (IBU) via vacuum drying and its release properties were investigated. The samples were characterized by field emission scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectroscopy. The results indicated that P25 NPs were successfully decorated on the surface of TNTs by hydrothermal method and the optimal concentration was found to be 7.5 × 10{sup −4} M. P25 NPs decorated on TNTs led to a significant increase in the specific surface area of TNTs which was conducive to improve the loading effect of IBU. Importantly, the diameters of the decorated nanotubes were reduced to 100 ± 10 nm and the increase in roughness led to an effective and prolonged drug release.

  19. Molecular Dynamics Simulation Study of the Selectivity of a Silica Polymer for Ibuprofen

    Directory of Open Access Journals (Sweden)

    Riccardo Concu

    2016-07-01

    Full Text Available In the past few years, the sol-gel polycondensation technique has been increasingly employed with great success as an alternative approach to the preparation of molecularly imprinted materials (MIMs. The main aim of this study was to study, through a series of molecular dynamics (MD simulations, the selectivity of an imprinted silica xerogel towards a new template—the (±-2-(P-Isobutylphenyl propionic acid (Ibuprofen, IBU. We have previously demonstrated the affinity of this silica xerogel toward a similar molecule. In the present study, we simulated the imprinting process occurring in a sol-gel mixture using the Optimized Potentials for Liquid Simulations-All Atom (OPLS-AA force field, in order to evaluate the selectivity of this xerogel for a template molecule. In addition, for the first time, we have developed and verified a new parameterisation for the Ibuprofen® based on the OPLS-AA framework. To evaluate the selectivity of the polymer, we have employed both the radial distribution functions, interaction energies and cluster analyses.

  20. Bartter Syndrome Type 3: Phenotype-Genotype Correlation and Favorable Response to Ibuprofen

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    Xuejun Yang

    2018-05-01

    Full Text Available Objective: To investigate the phenotype-genotype correlation in different genetic kinds of Bartter syndrome type 3 in children.Methods: Clinical and genetic data of 2 patients with different mutations in Bartter syndrome type 3 was analyzed while the prognosis was compared after a 6-year follow-up or 2-year follow-up, respectively.Results: Bartter syndrome is a kind of autosomal recessive inherited renal disorder. The manifestation and prognosis of Bartter syndrome change with mutation types, and severe mutation were often accompanied with unfavorable prognosis. Comprehensive therapy with ibuprofen, antisterone, captopril, and potassium have remarkable effect, while ibuprofen may improve growth retardation partly.Conclusion: Bartter syndrome should be considered when children have unreasonable continuous electrolyte disturbance, metabolic alkalosis and growth retardation.As a genetic disease, its clinical features depend on the mutation type. It can be ameliorated by electrolyte supplementation, prostaglandin synthetase inhibitors, angiotensin-converting enzyme inhibitors and potassium-sparing diuretic. Considering the following electrolyte disturbances, infections, growth retardation, kidney failure and even death, Bartter syndrome need lifelong treatment, early diagnosis and treatment is the most important.

  1. Impact of non-adherent Ibuprofen foam dressing in the lives of patients with venous ulcers

    Directory of Open Access Journals (Sweden)

    GERALDO MAGELA SALOMÉ

    Full Text Available ABSTRACT Objective : to evaluate pain in patients with lower limb venous ulcer who used non-adherent Ibuprofen foam dressing (IFD. Methods : we conducted a prospective study of patients with lower limb venous ulcers treated from April 2013 to August 2014. We used the Numerical Scale and McGill Pain Questionnaire, performing the assessments at the moment of inclusion of the patient in the study and every eight days thereafter, totaling five consultations. We divided the patients into two groups: 40 in the Study Group (SG, who were treated with IFD, and 40 in the Control Group (CG, treated with primary dressing, according to tissue type and exudate. Results : at the first consultation, patients from both groups reported intense pain. On the fifth day, SG patients reported no pain and the majority of CG reported moderate pain. Regarding the McGill Pain Questionnaire, most patients of both groups reported sensations related to sensory, affective, evaluative and miscellaneous descriptors at the beginning of data collection; after the second assessment, there was slight improvement among the patients in the SG. After the third consultation, they no longer reported the mentioned descriptors. CG patients displayed all the sensations of these descriptors until the fifth visit. Conclusion : non-adherent Ibuprofen foam dressing is effective in reducing the pain of patients with venous ulcers.

  2. Stereoselective and nonstereoselective effects of ibuprofen enantiomers on mitochondrial beta-oxidation of fatty acids

    International Nuclear Information System (INIS)

    Freneaux, E.; Fromenty, B.; Berson, A.; Labbe, G.; Degott, C.; Letteron, P.; Larrey, D.; Pessayre, D.

    1990-01-01

    The effects of the R-(-) and S-(+)ibuprofen enantiomers were first studied in vitro with mouse liver mitochondria incubated in the presence of various concentrations of exogenous coenzyme A. In the presence of a low concentration of coenzyme A (2.5 microM), the R-(-)enantiomer (which forms an acylcoenzyme A) inhibited stereoselectively the beta oxidation of [1- 14 C]palmitic acid but not that of [1- 14 C]palmitoyl-L-carnitine (which can directly enter the mitochondria). In the presence, however, of a concentration of coenzyme A (50 microM) reproducing that present in liver cell cytosol, both enantiomers (2 mM) slightly inhibited the beta oxidation of [1- 14 C]palmitic acid and markedly inhibited the beta oxidation of [1- 14 C]octanoic acid and [1- 14 C]butyric acid. In vivo, both enantiomers (1 mmol.kg-1) similarly inhibited the formation of [ 14 C]CO 2 from [1- 14 C]fatty acids. Both enantiomers similarly decreased plasma ketone bodies. Both similarly increased hepatic triglycerides, and both produced mild microvesicular steatosis of the liver. We conclude that both ibuprofen enantiomers inhibit beta oxidation of fatty acids in vitro and in vivo. In addition, the R-(-)enantiomer may stereoselectively sequester coenzyme A; at low concentrations of coenzyme A in vitro, this may stereoselectively inhibit the mitochondrial uptake and beta oxidation of long chain fatty acids

  3. A controlled release of ibuprofen by systematically tailoring the morphology of mesoporous silica materials

    International Nuclear Information System (INIS)

    Qu Fengyu; Zhu Guangshan; Lin Huiming; Zhang Weiwei; Sun Jinyu; Li Shougui; Qiu Shilun

    2006-01-01

    A series of mesoporous silica materials with similar pore sizes, different morphologies and variable pore geometries were prepared systematically. In order to control drug release, ibuprofen was employed as a model drug and the influence of morphology and pore geometry of mesoporous silica on drug release profiles was extensively studied. The mesoporous silica and drug-loaded samples were characterized by X-ray diffraction, Fourier transform IR spectroscopy, N 2 adsorption and desorption, scanning electron microscopy, and transmission electron microscopy. It was found that the drug-loading amount was directly correlated to the Brunauer-Emmett-Teller surface area, pore geometry, and pore volume; while the drug release profiles could be controlled by tailoring the morphologies of mesoporous silica carriers. - Graphical abstract: The release of ibuprofen is controlled by tailoring the morphologies of mesoporous silica. The mesoporous silica and drug-loaded samples are characterized by powder X-ray diffraction, Fourier transform IR spectroscopy, N 2 adsorption and desorption, scanning electron microscopy, and transmission electron microscopy. The drug-loading amount is directly correlated to the Brunauer-Emmett-Teller surface area, pore geometry, and pore volume; while the drug release profiles can be controlled by tailoring the morphologies of mesoporous silica carriers

  4. Safety of oral ibuprofen--analysis of data from the spontaneous reporting system in Poland.

    Science.gov (United States)

    Kuchari, Ernest; Han, Stanisław; Karłowicz-Bodalska, Katarzyna; Miśkiewicz, Katarzyna; Kutycka, Elzbieta

    2014-01-01

    Ibuprofen is a popular over-the-counter, non-steroidal anti-inflammatory medication, frequently used for the relief of fever, headaches, menstrual and other minor pains as well as a major active ingredient in numerous cold preparations. We analyzed sales volume and data obtained from the monitoring of spontaneous reports on the adverse effects of IBUM soft capsules, IBUM Forte soft capsules, and IBUM oral suspension 100 mg/5 mL collected by the manufacturer (PPF HASCO-LEK S.A. Wroclaw, Poland) and National Monitoring Center in Warszawa in the period between October 2002 and June 2012. A total of 19,644,797 units of IBUM soft capsules 200 mg, 5,678,164 units of IBUM Forte soft capsules 400 mg and 4,333,325 units of IBUM oral suspension 100 mg/5 mL (29,656,286 units altogether) produced by PPF HASCO-LEK S.A. Wrodcaw, P'oland were marketed during the period analyzed. There were 5 spontaneous reports regarding these medications registered in Poland in the period analyzed. Forms of oral ibuprofen are very safe medication rarely causing adverse effects; nevertheless, the existing spontaneous monitoring system of adverse effects in Poland is not sensitive enough to detect all adverse effects and needs improvement.

  5. Enteric coating of ibuprofen tablets (200 mg using an aqueous dispersion system

    Directory of Open Access Journals (Sweden)

    Rabia Bushra

    2010-03-01

    Full Text Available Ibuprofen is a propionic acid derivative that belongs to the class NSAIDs. Major adverse reactions associated with Ibuprofen are related to GIT and include peptic and mucosal ulcers, dyspepsia, severe gastric pain and bleeding, that results in excessive treatment failure. The goal of this study was to develop enteric coated ibuprofen tablets in order to avoid gastric mucosal irritation, diffusion of drug across mucosal lining and to let active ingredient be absorbed easily in small intestine. The formulation was developed and manufactured through the direct compression process, the simplest, easiest and most economical method of manufacturing. Enteric coating was done using an Opadry white subcoating and an aqueous coating dispersion of Acryl-Eze. Enteric coated formulation was subjected to disintegration and dissolution tests by placing in 0.1 M hydrochloric acid for 2 h and then 1 h in phosphate buffer with a pH of 6.8. About 0.04% of drug was released in the acidic phase and 99.05% in the basic medium. These results reflect that ibuprofen can be successfully enteric coated in order to prevent its release in the stomach and facilitate rapid release of the drug in the duodenum, due to the presence of superdisintegrant. Formulating this enteric coated tablets could increase patient compliance by decreasing adverse drug reactions (ADR S associated with Ibuprofen therapy.Ibuprofeno é um derivado do ácido propiônico, que pertence à classe dos fármacos não-esteróides (AINES. As principais reações adversas associadas com o ibuprofeno se referem àquelas do trato gastrintestinal (TGI, como úlceras pépticas e da mucosa, dispepsia, dor gástrica grave e sangramento, que resultam em muitas falhas de tratamento. O objetivo do estudo foi desenvolver comprimidos revestidos de ibuprofeno que impeçam a irritação da mucosa gástrica, difusão do fármaco através da mucosa e permitam, facilmente, a absorção do princípio ativo do intestino

  6. Capillary isotachophoresis with ESI-MS detection: Methodology for highly sensitive analysis of ibuprofen and diclofenac in waters

    Czech Academy of Sciences Publication Activity Database

    Malá, Zdeňka; Gebauer, Petr; Boček, Petr

    2016-01-01

    Roč. 907, FEB (2016), s. 1-6 ISSN 0003-2670 R&D Projects: GA ČR(CZ) GA13-05762S Institutional support: RVO:68081715 Keywords : isotachophoresis * mass spectrometric detection * Diclofenac * Ibuprofen Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 4.950, year: 2016

  7. Efficacy of nano- and microemulsion-based topical gels in delivery of ibuprofen: an in vivo study.

    Science.gov (United States)

    Azizi, Mosayeb; Esmaeili, Fariba; Partoazar, Alireza; Ejtemaei Mehr, Shahram; Amani, Amir

    2017-03-01

    Nanoemulsion has shown many advantages in drug delivery systems. In this study, for the first time, analgesic and anti-inflammatory properties of a nanomelusion of almond oil with and without ibuprofen was compared with corresponding microemulsion and commercial topical gel of the drug using formalin and carrageenan tests, respectively. Almond oil (oil phase) was mixed with Tween 80 and Span 80 (surfactants), and ethanol (co-surfactant) and them distilled water (aqueous phase) was then added to the mixture at once. Prepared nanoemulsions were pre-emulsified into a 100 ml beaker using magnet/stirrer (1000 rpm). Then, using a probe ultrasonicator (Hielscher UP400s, Hielscher, Ringwood, NJ) the nanoemulsions were formed. The optimised nanoemulsion formulation containing 2.5% ibuprofen, showed improved analgesic and anti-inflammatory effects compared with commercial product and corresponding microemulsion product containing 5% ibuprofen (i.e. twice the content of ibuprofen in the nanoemulsion) in vivo. The nanoemulsion preparation showed superior analgesic activities during chronic phase. Also, it decreased the inflammation from the first hour, while the microemulsion and the commercial product started to show their anti-inflammatory effects after 2 and 3 h, respectively. Our finding suggests that the size of the emulsion particles must be considered as an important factor in topical drug delivery systems.

  8. Simultaneous Estimation of Ibuprofen and Phenylephrine Hydrochloride in Bulk and Combined Dosage Form by First Derivative UV Spectrophotometry Method

    Directory of Open Access Journals (Sweden)

    Mehul Patel

    2013-01-01

    Full Text Available A simple, precise, rapid, and economic method was developed for the simultaneous determination of Ibuprofen and Phenylephrine HCl in bulk and combined dosage form. This method involves first-order derivative spectroscopy using 248 nm and 237 nm as zero crossing points for Ibuprofen and Phenylephrine HCl, respectively. For spectrophotometric method 0.1 N NaOH was used as a solvent. The linearity was established over the concentration range of 12–72 μg/mL and 1.5–22 μg/mL for Ibuprofen and Phenylephrine HCl with correlation coefficient (r2 of 0.9972 and 0.9981, respectively. The mean % recoveries were found to be in the range of 98.88% and 98.54% for Ibuprofen and Phenylephrine HCl, respectively. Interday and intraday studies showed repeatability of the method. The method was found to be specific and robust. The method was successfully applied to pharmaceutical formulation, with no interference from excipients as indicated by the recovery study. Results of analysis were validated statistically and by recovery studies.

  9. Effects of Subchronic Treatment with Ibuprofen and Nimesulide on Spatial Memory and NMDAR Subunits Expression in Aged Rats.

    Science.gov (United States)

    Ozturk Bilgin, Ozlem; Kumbul Doguc, Duygu; Altuntas, Irfan; Sutcu, Recep; Delibas, Namık

    2013-01-01

    Several studies point to an important function of cyclooxygenase (COX) and prostaglandin signaling in models of synaptic plasticity which is associated with N-methyl-D-aspartate receptors (NMDARs). Cyclooxygenase gene is suggested to be an immediate early gene that is tightly regulated in neurons by NMDA dependent synaptic activity. Nonsteroid Antiinflammatory Drugs (NSAIDs) exert their antiinflammatory effect by the inhibion of COX have controversial effects on learning and memory. We administered ibuprofen as a non-selective COX-2 inhibitor and nimesulide as a selective COX-2 inhibitor for 8 weeks for determining the cognitive impact of subchronic administration of NSAIDs to aged rats. Wistar albino rats (16 mo, n = 30) were separated into control (n = 10), ibuprofen (n = 10) and nimesulide (n = 10) treated groups. First we evaluated hippocampus-dependent spatial memory in the radial arm maze (RAM) and than we evaluated the expression of the NMDAR subunits, NR2A and NR2B by western blotting to see if their expressions are effected by subchronic administration with these drugs. Ibuprofen and nimesulide treated rats completed the task in a statistically significant shorter time when compared with control group (p RAM. Furthermore, no statistically significant difference was detected for the protein expressions of NR2A and NR2B of the subjects. Oral administration of ibuprofen and nimesulide for 8 weeks showed no impairment but partly improved spatial memory.

  10. The effect of food on gastrointestinal (GI) transit of sustained-release ibuprofen tablets as evaluated by gamma scintigraphy

    International Nuclear Information System (INIS)

    Borin, M.T.; Khare, S.; Beihn, R.M.; Jay, M.

    1990-01-01

    The GI transit of radiolabeled sustained-release ibuprofen 800-mg tablets in eight healthy, fed volunteers was monitored using external gamma scintigraphy. Ibuprofen serum concentrations were determined from blood samples drawn over 36 hr following dosing. Sustained-release ibuprofen tablets containing 0.18% of 170Er2O3 (greater than 96% 170Er) in the bulk formulation were manufactured under pilot-scale conditions and were radiolabeled utilizing a neutron activation procedure which converted stable 170Er to radioactive 171Er (t1/2 = 7.5 hr). At the time of dosing, each tablet contained 50 mu Ci of 171Er. Dosage form position were reported at various time intervals. In five subjects the sustained-release tablet remained in the stomach and eroded slowly over 7-12 hr, resulting in gradual increases in small bowel radioactivity. In the remaining three subjects, the intact tablet was ejected from the stomach and a gastric residence time of approximately 4 hr was measured. This is in marked contrast to a previous study conducted in fasted volunteers in which gastric retention time ranged from 10 to 60 min. Differences in GI transit between fed and fasted volunteers had little effect on ibuprofen bioavailability. AUC and Tmax were unaltered and Cmax was increased by 24%, which is in agreement with results from a previous, crossover-design food effect study

  11. Protective Effects of Ibuprofen and L-Carnitine Against Whole Body Gamma Irradiation-Induced Duodenal Mucosal Injury

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    Meryem Akpolat

    2011-03-01

    Full Text Available Objective: Ibuprofen and L-carnitine have been demonstrated to provide radioprotective activity to the hamster against whole body sublethal irradiation. The purpose of this study is to test those antioxidant drugs, each of which has the capacity of inhibiting mucosal injury, as topical radioprotectants for the intestine. Material and Methods: The male hamsters were divided into the following four groups (n=6: group 1: control group, received saline, 1 ml/100 g by gavage, as placebo. Group 2: irradiated-control group, received whole body irradiation of 8 Gy as a single dose plus physiological saline. The animals in groups 3 and 4 were given a daily dose of 10 mg/kg of ibuprofen and 50 mg/kg of L-carnitine for 15 days respectively, before irradiation with a single dose of 8 Gy. Twenty-four hours after radiation exposure, the hamsters were sacrificed and samples were taken from the duodenum, and the histopatological determinations were carried out. Results: Morphologically, examination of the gamma irradiated duodenum revealed the presence of shortening and thickening of villi and flattening of enterocytes, massive subepithelial lifting. Pretreatment of ibuprofen and L-carnitine with irradiation reduced these histopathological changes. Conclusion: Ibuprofen and L-carnitine administrated by the oral route may be a good radioprotector against small intestinal damage in patients undergoing radiotherapy.

  12. Acetaminophen Versus Liquefied Ibuprofen for Control of Pain During Separation in Orthodontic Patients: A Randomized Triple Blinded Clinical Trial

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    Tahereh Hosseinzadeh Nik

    2016-07-01

    Full Text Available The aim of this randomized clinical study was to investigate the effectiveness of acetaminophen 650 mg or liquefied ibuprofen 400 mg in pain control of orthodontic patients during separation with an elastic separator. A total of 101 patients with specific inclusion criteria were divided randomly into three groups (acetaminophen, liquefied ibuprofen, and placebo. They were instructed to take their drugs one hour before separator placement and every six hours afterward (five doses in total. They recorded their discomfort on visual analog scales immediately after separator placement, 2 hours later, 6 hours later, at bedtime, and 24 hours after separator placement. Repeated measure analysis of variance (ANOVA was used to compare the mean pain scores between the three groups. Data were collected from 89 patients. The pain increased with time in all groups. Pain scores were statistically lower in the analgesic groups compared with the placebo group (P.value<0.001, but no statistically significant difference was found in mean pain scores between the two drug groups (acetaminophen and liquefied ibuprofen (P.value=1. Acetaminophen and liquefied ibuprofen have similar potential in pain reduction during separation.

  13. Effects of selected pharmaceuticals (ibuprofen and amoxicillin on the demography of Brachionus calyciflorus and Brachionus havanaensis (Rotifera

    Directory of Open Access Journals (Sweden)

    Brenda Karen González-Pérez

    2016-09-01

    Full Text Available The levels of emerging chemicals have increased dramatically during the last two decades posing problems for human and environmental health. Pain-killers such as ibuprofen and antibiotics such as amoxicillin are generally consumed together and hence are discharged into waterbodies as effluents. The lack of a rigorous control of pharmaceutical discharges into natural waterbodies is a concern for limnologists and ecotoxicologists because of their possible effects on non-target organisms. Rotifers, due to their sensitivity, short generation time and high reproductive rates, are widely used as bioassay organisms in testing the effects of different substances including pharmaceuticals. Here we quantified the demographic responses of Brachionus calyciflorus and Brachionus havanaensis exposed to three sublethal concentrations of ibuprofen (25, 12.5 and 6.25 mg L−1 and amoxicillin (200, 100 and 50 μg L−1. Our data showed that both survivorship- and reproduction-related variables were negatively affected with increasing concentrations of both pharmaceuticals. The rate of population increase of B. calyciflorus (0.63–0.72 d−1 was not affected by amoxicillin or by ibuprofen but for B. havanaensis, it was decreased significantly (from 0.89 to 0.38 d−1. Compared to ibuprofen, amoxicillin had more adverse effects on both the rotifer species.

  14. Oral Ibuprofen versus Intravenous Indomethacin for Closure of Patent Ductus Arteriosus in Very Low Birth Weight Infants

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    Cheng Han Lee

    2012-12-01

    Conclusion: In infants with VLBW, oral ibuprofen is as effective as intravenous indomethacin for closure of PDA and is associated with significantly fewer cases of necrotizing enterocolitis among infants with birth body weights <1250 g and significantly lower rates of elevated creatinine levels among neonates with birth body weights ranging from 1000 to 1500 g.

  15. Resolution of ibuprofen: a project for an experimental organic chemistry course; Resolucao do ibuprofeno: um projeto para disciplina de quimica organica experimental

    Energy Technology Data Exchange (ETDEWEB)

    Romero, Adriano L.; Baptistella, Lucia H.B.; Coelho, Fernando; Imamura, Paulo M., E-mail: imam@iqm.unicamp.br [Universidade Estadual de Campinas, SP (Brazil). Inst. de Quimica

    2012-07-01

    A practical and didactic sequence of experiments was proposed to illustrate the stereochemistry concept, optically active compounds, resolution of racemates, and use of the NMR technique, including 2D-COSY for identification of organic compounds, on a laboratory course for undergraduate students. The sequence was: extractions of racemic ibuprofen and chiral naproxen from commercial tablets; syntheses of diastereoisomeric amides reacting chiral (S)-(-)-{alpha}-methylbenzylamine with (+-)-ibuprofen; separation and determination of absolute configuration of amides by {sup 1}H NMR spectroscopy and GC analysis, and hydrolysis of amides to obtain (+)- and (-)-ibuprofen. (author)

  16. Early and late effects of Ibuprofen on mouse sperm parameters, chromatin condensation, and DNA integrity in mice.

    Science.gov (United States)

    Roodbari, Fatemeh; Abedi, Nahid; Talebi, Ali Reza

    2015-11-01

    There are few studies indicating the detrimental effects of ibuprofen on sperm fertility potential and DNA integrity. To determine the effects of Ibuprofen on sperm parameters, chromatin condensation and DNA integrity of mice. In this experimental study, 36 adult male mice with average weight 37 gr were divided into three groups, including control (group I, n=12), normal dosage of ibuprofen (group II, n=12) and high dosage (group III, n=12). Ibuprofen with different doses was dissolved in daily water of animals. After 35, 70 and 105 days, the cauda epididymis of mice were cut and incubated in Ham's F10 media. Sperm samples were analyzed for parameters (motility, morphology and count), DNA integrity (SCD test) and chromatin condensation (chromomycin A3 and Aniline blue staining). After 35 days, in addition to above mentioned sperm parameters, all of the treated mice showed statistically significant increase in spermatozoa with immature chromatin (Psperm DNA fragmentation assessed by SCD was increased in group II (66.5±0.7) and the percentage of immature spermatozoa (AB(+) and CMA3(+)) was higher in group III (77.5±0.7 and 49.5±6.3 respectively) than other groups. After 105 days, the AB(+) spermatozoa were increased in both normal dose and high dose groups. Ibuprofen may cause a significant reduction in sperm parameters and sperm chromatin/DNA integrity in mice. It should be noted that these deleterious effects are dose-dependent and can be seen in early and late stage of drug treatments.

  17. Early and late effects of Ibuprofen on mouse sperm parameters, chromatin condensation, and DNA integrity in mice

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    Fatemeh Roodbari

    2015-11-01

    Full Text Available Background: There are few studies indicating the detrimental effects of ibuprofen on sperm fertility potential and DNA integrity. Objective: To determine the effects of Ibuprofen on sperm parameters, chromatin condensation and DNA integrity of mice. Materials and Methods: In this experimental study, 36 adult male mice with average weight 37 gr were divided into three groups, including control (group I, n=12, normal dosage of ibuprofen (group II, n=12 and high dosage (group III, n=12. Ibuprofen with different doses was dissolved in daily water of animals. After 35, 70 and 105 days, the cauda epididymis of mice were cut and incubated in Ham’s F10 media. Sperm samples were analyzed for parameters (motility, morphology and count, DNA integrity (SCD test and chromatin condensation (chromomycin A3 and Aniline blue staining. Results: After 35 days, in addition to above mentioned sperm parameters, all of the treated mice showed statistically significant increase in spermatozoa with immature chromatin (P<0.05. However, after 70 days, the rate of sperm DNA fragmentation assessed by SCD was increased in group II (66.5±0.7 and the percentage of immature spermatozoa (AB+ and CMA3+ was higher in group III (77.5±0.7 and 49.5±6.3 respectively than other groups. After 105 days, the AB+ spermatozoa were increased in both normal dose and high dose groups. Conclusion: Ibuprofen may cause a significant reduction in sperm parameters and sperm chromatin/DNA integrity in mice. It should be noted that these deleterious effects are dose-dependent and can be seen in early and late stage of drug treatments.

  18. Effects of lornoxicam and intravenous ibuprofen on erythrocyte deformability and hepatic and renal blood flow in rats.

    Science.gov (United States)

    Arpacı, Hande; Çomu, Faruk Metin; Küçük, Ayşegül; Kösem, Bahadır; Kartal, Seyfi; Şıvgın, Volkan; Turgut, Hüseyin Cihad; Aydın, Muhammed Enes; Koç, Derya Sebile; Arslan, Mustafa

    2016-01-01

    Change in blood supply is held responsible for anesthesia-related abnormal tissue and organ perfusion. Decreased erythrocyte deformability and increased aggregation may be detected after surgery performed under general anesthesia. It was shown that nonsteroidal anti-inflammatory drugs decrease erythrocyte deformability. Lornoxicam and/or intravenous (iv) ibuprofen are commonly preferred analgesic agents for postoperative pain management. In this study, we aimed to investigate the effects of lornoxicam (2 mg/kg, iv) and ibuprofen (30 mg/kg, iv) on erythrocyte deformability, as well as hepatic and renal blood flows, in male rats. Eighteen male Wistar albino rats were randomly divided into three groups as follows: iv lornoxicam-treated group (Group L), iv ibuprofen-treated group (Group İ), and control group (Group C). Drug administration was carried out by the iv route in all groups except Group C. Hepatic and renal blood flows were studied by laser Doppler, and euthanasia was performed via intra-abdominal blood uptake. Erythrocyte deformability was measured using a constant-flow filtrometry system. Lornoxicam and ibuprofen increased the relative resistance, which is an indicator of erythrocyte deformability, of rats (P=0.016). Comparison of the results from Group L and Group I revealed no statistically significant differences (P=0.694), although the erythrocyte deformability levels in Group L and Group I were statistically higher than the results observed in Group C (P=0.018 and P=0.008, respectively). Hepatic and renal blood flows were significantly lower than the same in Group C. We believe that lornoxicam and ibuprofen may lead to functional disorders related to renal and liver tissue perfusion secondary to both decreased blood flow and erythrocyte deformability. Further studies regarding these issues are thought to be essential.

  19. A preliminary pilot randomized crossover study of uzara (Xysmalobium undulatum versus ibuprofen in the treatment of primary dysmenorrhea.

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    Karim H I Abd-El-Maeboud

    Full Text Available Preliminary evaluation of efficacy and safety of uzara use in treatment of moderate and severe primary dysmenorrhea in comparison to ibuprofen.This randomized, comparative two way cross-over study comprised 60 single female students at Faculty of Medicine, Ain Shams University, Egypt, aged 19-28 years with moderate (n = 46 or severe (n = 14 primary dysmenorrhea. Participants were randomized to take either uzara (80 mg/8 hours for two doses, then 40 mg/8 hours then ibuprofen (400 mg/6 hours in two subsequent cycles or vice versa. The pain intensity, using VAS, was recorded immediately before taking the medication (0 hour and after 4, 12, 24, 48-60, 96-120 hours. Main outcome measures included effectiveness of pain relief defined as drop of VAS to 3 or less, patient's global evaluation of the drug, absence from school, the use of a rescue medication, and, in those who continued the treatment, the pain intensity difference (PID at different points after start of medication and its sum (SPID.Uzara was comparably effective to ibuprofen (78.3% vs. 86.7% of cycles; respectively, with comparable rates of effectiveness on global evaluation (being around 50% for either drug, and rates of school absences (11.7% vs. 13.3%; respectively. The need for rescue medication was different (18.3% and 10%; respectively, albeit with no statistical significance. The means of PID at different time points and SPID were comparable, with significantly lower average mean of VAS scores compared to that felt with no medication (1.6 vs. 6.8, p<0.001. Side effects were less with uzara than ibuprofen (0% vs. 8.3%, p<0.05.Uzara might be as effective as ibuprofen in management of primary dysmenorrhea but with less side effects. These findings need to be confirmed by a properly designed trial with a larger sample size.Current Controlled Trials ISRCTN25618258.

  20. Efficacy and safety of Curcuma domestica extracts compared with ibuprofen in patients with knee osteoarthritis: a multicenter study

    Science.gov (United States)

    Kuptniratsaikul, Vilai; Dajpratham, Piyapat; Taechaarpornkul, Wirat; Buntragulpoontawee, Montana; Lukkanapichonchut, Pranee; Chootip, Chirawan; Saengsuwan, Jittima; Tantayakom, Kesthamrong; Laongpech, Supphalak

    2014-01-01

    Objective To determine the efficacy and safety of Curcuma domestica extracts in pain reduction and functional improvement. Methods 367 primary knee osteoarthritis patients with a pain score of 5 or higher were randomized to receive ibuprofen 1,200 mg/day or C. domestica extracts 1,500 mg/day for 4 weeks. The main outcomes were Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) total, WOMAC pain, WOMAC stiffness, and WOMAC function scores. Adverse events (AEs) were also recorded. Results 185 and 182 patients were randomly assigned into C. domestica extracts and ibuprofen groups, respectively. The baseline characteristics were no different between groups. The mean of all WOMAC scores at weeks 0, 2, and 4 showed significant improvement when compared with the baseline in both groups. After using the noninferiority test, the mean difference (95% confidence interval) of WOMAC total, WOMAC pain, and WOMAC function scores at week 4 adjusted by values at week 0 of C. domestica extracts were noninferior to those for the ibuprofen group (P=0.010, P=0.018, and P=0.010, respectively), except for the WOMAC stiffness subscale, which showed a trend toward significance (P=0.060). The number of patients who developed AEs was no different between groups. However, the number of events of abdominal pain/discomfort was significantly higher in the ibuprofen group than that in the C. domestica extracts group (P=0.046). Most subjects (96%–97%) were satisfied with the treatment, and two-thirds rated themselves as improved in a global assessment. Conclusion C. domestica extracts are as effective as ibuprofen for the treatment of knee osteoarthritis. The side effect profile was similar but with fewer gastrointestinal AE reports in the C. domestica extracts group. PMID:24672232

  1. Thermodynamics of inclusion complexes of natural and modified cyclodextrins with acetylsalicylic acid and ibuprofen in aqueous solution at 298 K

    Energy Technology Data Exchange (ETDEWEB)

    Castronuovo, Giuseppina, E-mail: giuseppina.castronuovo@unina.it [Department of Chemistry, University Federico II of Naples, Complesso Universitario a Monte S. Angelo, via Cintia, 80126 Naples (Italy); Niccoli, Marcella [Department of Chemistry, University Federico II of Naples, Complesso Universitario a Monte S. Angelo, via Cintia, 80126 Naples (Italy)

    2013-04-10

    Graphical abstract: Complexation forces acting in the association between natural and modified α- and β-cyclodextrins and acetylsalicylic acid (aspirin) or ibuprofen are examined through the analysis of the thermodynamic parameters obtained by isothermal calorimetry. Highlights: ► A calorimetric method is reported to study the association of natural and substituted cyclodextrins with acetylsalicylic acid and ibuprofen. ► The study aims to propose a hypothesis about the forces involved in the interaction. That can be useful for designing new cyclodextrins having suitable characteristics to include specific drugs. ► Enthalpic and entropic contributions on the association are discussed. The differences in the cavity dimensions of the cyclodextrins determine the values of the thermodynamic properties to be very different. - Abstract: Thermodynamic parameters for the association of natural and substituted α-, β-, and γ-cyclodextrins with acetylsalicylic acid, salicylic acid and ibuprofen have been determined by isothermal titration calorimetry. Analysis of the data shows that complexes form, all having 1:1 stoichiometry. The shape-matching between the host and guest is the factor determining the values of the thermodynamic quantities. In the case of the smallest cyclodextrin interacting with acetylsalicylic acid and salicylic acid, the parameters indicate that hydrophobic interactions play the major role. Association occurs through the shallow inclusion of the benzene ring into the cavity. In the case of substituted β-cyclodextrins, instead, inclusion of the benzene ring is deeper and the tight fitting of the guest molecule to the cavity makes the enthalpy and entropy to be both negative. Ibuprofen interacts through its isobutyl group: the values of the association constants are very high for β-cyclodextrins as determined by the large and positive entropies due to the relaxation of water molecules from the cavity and the hydration spheres of the interacting

  2. Factors associated with efficacy of an ibuprofen/pseudoephedrine combination drug in pharmacy customers with common cold symptoms.

    Science.gov (United States)

    Klimek, Ludger; Schumacher, Helmut; Schütt, Tanja; Gräter, Heidemarie; Mueck, Tobias; Michel, Martin C

    2017-02-01

    The aim of this study was to explore factors affecting efficacy of treatment of common cold symptoms with an over-the-counter ibuprofen/pseudoephedrine combination product. Data from an anonymous survey among 1770 pharmacy customers purchasing the combination product for treatment of own common cold symptoms underwent post-hoc descriptive analysis. Scores of symptoms typically responsive to ibuprofen (headache, pharyngeal pain, joint pain and fever), typically responsive to pseudoephedrine (congested nose, congested sinus and runny nose), considered non-specific (sneezing, fatigue, dry cough, cough with expectoration) and comprising all 11 symptoms were analysed. Multiple regression analysis was applied to explore factors associated with greater reduction in symptom intensity or greater probability of experiencing a symptom reduction of at least 50%. After intake of first dose of medication, typically ibuprofen-sensitive, pseudoephedrine-responsive, non-specific and total symptoms were reduced by 60.0%, 46.3%, 45.4% and 52.8%, respectively. A symptom reduction of at least 50% was reported by 73.6%, 55.1%, 50.9% and 61.6% of participants, respectively. A high baseline score was associated with greater reductions in symptom scores but smaller probability of achieving an improvement of at least 50%. Across both multiple regression approaches, two tablets at first dosing were more effective than one and (except for ibuprofen-sensitive symptoms) starting treatment later than day 2 of the cold was generally less effective. Efficacy of an ibuprofen/pseudoephedrine combination in the treatment of common cold symptoms was dose-dependent and greatest when treatment started within the first 2 days after onset of symptoms. © 2016 The Authors. International Journal of Clinical Practice Published by John Wiley & Sons Ltd.

  3. A comparative study between the efficacy of tramadol, celecoxib and ibuprofen in pain control after root canal therapy of tooth

    Directory of Open Access Journals (Sweden)

    Eshagh A. Saberi

    2011-01-01

    Full Text Available Background: Root canal therapy of teeth can relief the endodontic pain, but post-endodontic pain and discomfort are its undesirable effects. There are many studies on various drugs for alleviation of post-endodontic pain. The aim of this study was to compare the analgesic effect of tramadol, celecoxib and ibuprofen in vital teeth.Materials & Method: In this double blind randomized clinical trial study, 104 patients with vital first mandibular molar tooth were selected. The patients were divided in to four groups, tramadol (A, celecoxib (B, ibuprofen (C and placebo (D. The similar capsules were filled with50mg tramadol HCL, 100mg celecoxib, 400mg ibuprofen and starch . Each patient received randomly one capsule one hour before treatment. If the pain persists, the patient received one tablet of 325 mg acetaminophen every 6 hours. The groups were controlled for 3 days. The data were collected one hour before and 6, 12, 24, 48, 72 hours after treatment. Results were analyzed using kruskal-wallis and Mann-Whitney U tests.Results: The results showed that after 12 (p=0.039 and 24(p=0.024 hours of treatment, tramadol was better in pain relief in comparison with other groups and there was one difference between tramadol and ibuprofen after treatment after 12 hours (p=0.013. But there was no significant deference between drug groups at 6, 48 and 72 hour after treatment.Conclusion: Tramadol prescription in comparison with celecoxib, ibuprofen and placebo has greater analgesic effect after root canal therapy in vital teeth. In addition tramadol may be a good medicine for post-endodontic pain control

  4. Biodegradation of ibuprofen, diclofenac and carbamazepine in nitrifying activated sludge under 12 °C temperature conditions

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    Kruglova, Antonina; Ahlgren, Pia; Korhonen, Nasti; Rantanen, Pirjo; Mikola, Anna; Vahala, Riku

    2014-11-15

    Pharmaceuticals constitute a well-known group of emerging contaminants with an increasing significance in water pollution. This study focuses on three pharmaceuticals extensively used in Finland and which can be found in environmental waters: ibuprofen, diclofenac and carbamazepine. Biodegradation experiments were conducted in a full-scale Wastewater Treatment Plant (WWTP) and in laboratory-scale Sequencing Batch Reactors (SBRs). The SBRs were operated at 12 °C, with a sludge retention time (SRT) 10–12 d and organic loading rates (OLRs) of 0.17, 0.27 and 0.33 kg BOD{sub 7} m{sup -3}d{sup -1}. Ibuprofen was found to biodegrade up to 99%. The biodegradation rate constants (k{sub biol}) for ibuprofen were calculated for full-scale and laboratory processes as well as under different laboratory conditions and found to differ from 0.9 up to 5.0 l g{sub SS}{sup −1} d{sup −1}. Diclofenac demonstrated an unexpected immediate drop of concentration in three SBRs and partial recovery of the initial concentration in one of the reactors. High fluctuating in diclofenac concentration was presumably caused by removal of this compound under different concentrations of nitrites during development of nitrifying activated sludge. Carbamazepine showed no biodegradation in all the experiments. - Highlights: • The biodegradation of three pharmaceuticals examined under 12 °C conditions. • k{sub biol} constants for ibuprofen proposed for full-scale and laboratory-scale processes. • Influence of OLR on ibuprofen biodegradation was studied. • Removal followed by recovery of diclofenac detected in nitrifying activated sludge.

  5. Biodegradation of ibuprofen, diclofenac and carbamazepine in nitrifying activated sludge under 12 °C temperature conditions

    International Nuclear Information System (INIS)

    Kruglova, Antonina; Ahlgren, Pia; Korhonen, Nasti; Rantanen, Pirjo; Mikola, Anna; Vahala, Riku

    2014-01-01

    Pharmaceuticals constitute a well-known group of emerging contaminants with an increasing significance in water pollution. This study focuses on three pharmaceuticals extensively used in Finland and which can be found in environmental waters: ibuprofen, diclofenac and carbamazepine. Biodegradation experiments were conducted in a full-scale Wastewater Treatment Plant (WWTP) and in laboratory-scale Sequencing Batch Reactors (SBRs). The SBRs were operated at 12 °C, with a sludge retention time (SRT) 10–12 d and organic loading rates (OLRs) of 0.17, 0.27 and 0.33 kg BOD 7 m -3 d -1 . Ibuprofen was found to biodegrade up to 99%. The biodegradation rate constants (k biol ) for ibuprofen were calculated for full-scale and laboratory processes as well as under different laboratory conditions and found to differ from 0.9 up to 5.0 l g SS −1 d −1 . Diclofenac demonstrated an unexpected immediate drop of concentration in three SBRs and partial recovery of the initial concentration in one of the reactors. High fluctuating in diclofenac concentration was presumably caused by removal of this compound under different concentrations of nitrites during development of nitrifying activated sludge. Carbamazepine showed no biodegradation in all the experiments. - Highlights: • The biodegradation of three pharmaceuticals examined under 12 °C conditions. • k biol constants for ibuprofen proposed for full-scale and laboratory-scale processes. • Influence of OLR on ibuprofen biodegradation was studied. • Removal followed by recovery of diclofenac detected in nitrifying activated sludge

  6. Comparison of the Effect of 800 mg Ibuprofen and 30 mg Predenisolone on Relief of Post Endodontic Pain

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    S.M. Jalalzadeh

    2009-04-01

    Full Text Available Introduction & Objective: One of the important problems in dentistry is post endodontic pains .The purpose of this study was comparison of the effect of prophylactic oral ibuprofen 800mg and oral predenisolone 30mg on prevention of post endodontic pain.Materials & Methods: The present study is a double-blind, randomized and controlled trial. It was conducted on 60 patient (16men and 44 women between the ages of 18-63 who needed endodontic treatment. Inclusive criteria for selecting of patients were: need for root canal therapy in one of the posterior teeth, having no systemic problem, no evidence of abscess; not taking analgesic or similar drug for at least 6 hours before treatment. Patients were divided into three experimental groups randomly taking one of the drugs before the treatment {ibuprofen 800 mg, prednisolone30mg and placebo (oral dextrose}. Patients completed VAS at 6,12 and 24 hours post root canal therapy and analyzed using the spss15 by chi-square, ANOVA test and Tukey test.Results: During 24 hours after treatment post endodontic pain is 95%- 100% in the placebo group. The prevalence of no-pain was not significant 6, 12 and 24 hours after treatment between the ibuprofen and predenisolone groups. The mean scale of pain in ibuprofen and predenisolone groups was significantly lower than placebo group 6, 12 and 24 hours after treatment. Differences between the drug groups are significant only on 6 and 12 hours after treatment.Conclusion: Post endodontic pains are present 24 hours after treatment. 6 and 12 hours after treatment 30 mg predenisolone are significantly better for pain relief than 800 mg ibuprofen. But after 24 hours it is not significant.

  7. Comparison of two dose regimens of ibuprofen for the closure of patent ductus arteriosus in preterm newborns.

    Science.gov (United States)

    Dornelles, Laura Vargas; Corso, Andréa Lúcia; Silveira, Rita de Cássia; Procianoy, Renato Soibelmann

    2016-01-01

    To compare the efficacy of intravenous ibuprofen at high (20-10-10mg/kg/dose) and low doses (10-5-5mg/kg/dose) the closure of patent ductus arteriosus in preterm newborns. A cohort study with historical control of newborns that received high- and low-dose intravenous ibuprofen, from 2010 to 2013 in a neonatal intensive care unit, for closure of the patent ductus arteriosus, documented by echocardiography. Secondary outcomes included the number of ibuprofen cycles, incidence of bronchopulmonary dysplasia, necrotizing enterocolitis, changes in renal function, and death. Seventy-seven patients received three doses of ibuprofen for the treatment of patent ductus arteriosus, with 33 receiving high-dose and 44 low-dose therapy. The ductus closed after the first cycle in 25 (56.8%) low-dose patients and in 17 (51.5%) high-dose patients (p>0.99). Sixteen patients received a second cycle of ibuprofen, and the ductus closed in 50% after low-dose and in 60% after high-dose therapy (p>0.99). Seven patients required surgery for ductus closure, 13.6% in the low-dose group and 3% in the high-dose group (p=0.22). Thirty-nine patients developed bronchopulmonary dysplasia, 50% in the low-dose group and 51.5% in the high-dose group (p>0.99). Twenty-two (50%) low-dose patients died vs. 15 (45.5%) high-dose patients (p=0.86). There was no difference in closure of the ductus arteriosus or occurrence of adverse effects between the two dose regimens. Copyright © 2016 Sociedade Brasileira de Pediatria. Published by Elsevier Editora Ltda. All rights reserved.

  8. Comparison of two dose regimens of ibuprofen for the closure of patent ductus arteriosus in preterm newborns,

    Directory of Open Access Journals (Sweden)

    Laura Vargas Dornelles

    2016-06-01

    Full Text Available Abstract Objective: To compare the efficacy of intravenous ibuprofen at high (20-10-10 mg/kg/dose and low doses (10-5-5 mg/kg/dose the closure of patent ductus arteriosus in preterm newborns. Methods: A cohort study with historical control of newborns that received high- and low-dose intravenous ibuprofen, from 2010 to 2013 in a neonatal intensive care unit, for closure of the patent ductus arteriosus, documented by echocardiography. Secondary outcomes included the number of ibuprofen cycles, incidence of bronchopulmonary dysplasia, necrotizing enterocolitis, changes in renal function, and death. Results: Seventy-seven patients received three doses of ibuprofen for the treatment of patent ductus arteriosus, with 33 receiving high-dose and 44 low-dose therapy. The ductus closed after the first cycle in 25 (56.8% low-dose patients and in 17 (51.5% high-dose patients (p > 0.99. Sixteen patients received a second cycle of ibuprofen, and the ductus closed in 50% after low-dose and in 60% after high-dose therapy (p > 0.99. Seven patients required surgery for ductus closure, 13.6% in the low-dose group and 3% in the high-dose group (p = 0.22. Thirty-nine patients developed bronchopulmonary dysplasia, 50% in the low-dose group and 51.5% in the high-dose group (p > 0.99. Twenty-two (50% low-dose patients died vs. 15 (45.5% high-dose patients (p = 0.86. Conclusions: There was no difference in closure of the ductus arteriosus or occurrence of adverse effects between the two dose regimens.

  9. Thermodynamics of inclusion complexes of natural and modified cyclodextrins with acetylsalicylic acid and ibuprofen in aqueous solution at 298 K

    International Nuclear Information System (INIS)

    Castronuovo, Giuseppina; Niccoli, Marcella

    2013-01-01

    Graphical abstract: Complexation forces acting in the association between natural and modified α- and β-cyclodextrins and acetylsalicylic acid (aspirin) or ibuprofen are examined through the analysis of the thermodynamic parameters obtained by isothermal calorimetry. Highlights: ► A calorimetric method is reported to study the association of natural and substituted cyclodextrins with acetylsalicylic acid and ibuprofen. ► The study aims to propose a hypothesis about the forces involved in the interaction. That can be useful for designing new cyclodextrins having suitable characteristics to include specific drugs. ► Enthalpic and entropic contributions on the association are discussed. The differences in the cavity dimensions of the cyclodextrins determine the values of the thermodynamic properties to be very different. - Abstract: Thermodynamic parameters for the association of natural and substituted α-, β-, and γ-cyclodextrins with acetylsalicylic acid, salicylic acid and ibuprofen have been determined by isothermal titration calorimetry. Analysis of the data shows that complexes form, all having 1:1 stoichiometry. The shape-matching between the host and guest is the factor determining the values of the thermodynamic quantities. In the case of the smallest cyclodextrin interacting with acetylsalicylic acid and salicylic acid, the parameters indicate that hydrophobic interactions play the major role. Association occurs through the shallow inclusion of the benzene ring into the cavity. In the case of substituted β-cyclodextrins, instead, inclusion of the benzene ring is deeper and the tight fitting of the guest molecule to the cavity makes the enthalpy and entropy to be both negative. Ibuprofen interacts through its isobutyl group: the values of the association constants are very high for β-cyclodextrins as determined by the large and positive entropies due to the relaxation of water molecules from the cavity and the hydration spheres of the interacting

  10. Therapeutical Administration of Peptide Pep19-2.5 and Ibuprofen Reduces Inflammation and Prevents Lethal Sepsis

    Science.gov (United States)

    Barcena Varela, Sergio; Ferrer-Espada, Raquel; Reiling, Norbert; Goldmann, Torsten; Gutsmann, Thomas; Mier, Walter; Schürholz, Tobias; Drömann, Daniel; Brandenburg, Klaus; Martinez de Tejada, Guillermo

    2015-01-01

    Sepsis is still a major cause of death and many efforts have been made to improve the physical condition of sepsis patients and to reduce the high mortality rate associated with this disease. While achievements were implemented in the intensive care treatment, all attempts within the field of novel therapeutics have failed. As a consequence new medications and improved patient stratification as well as a thoughtful management of the support therapies are urgently needed. In this study, we investigated the simultaneous administration of ibuprofen as a commonly used nonsteroidal anti-inflammatory drug (NSAID) and Pep19-2.5 (Aspidasept), a newly developed antimicrobial peptide. Here, we show a synergistic therapeutic effect of combined Pep19-2.5-ibuprofen treatment in an endotoxemia mouse model of sepsis. In vivo protection correlates with a reduction in plasma levels of both tumor necrosis factor α and prostaglandin E, as a likely consequence of Pep19-2.5 and ibuprofen-dependent blockade of TLR4 and COX pro-inflammatory cascades, respectively. This finding is further characterised and confirmed in a transcriptome analysis of LPS-stimulated human monocytes. The transcriptome analyses showed that Pep19-2.5 and ibuprofen exerted a synergistic global effect both on the number of regulated genes as well as on associated gene ontology and pathway expression. Overall, ibuprofen potentiated the anti-inflammatory activity of Pep19-2.5 both in vivo and in vitro, suggesting that NSAIDs could be useful to supplement future anti-sepsis therapies. PMID:26197109

  11. CHRISTIAN SYMBOLISM IN FYODOR DOSTOEVSKY'S NOVEL "THE POSSESSED" ("DEMONS"

    Directory of Open Access Journals (Sweden)

    Sergei Leonidovich Sharakov

    2013-11-01

    Full Text Available The article raises a question of Christian symbolism in Fyodor Dostoevsky’s novel The Possessed (Demons. The introductory part identifies the purpose of a symbol in Christian poetics through the parallel with ancient symbolism. The author makes a conclusion that the functional role of a symbol in the ancient world and Christian tradition is different. Therefore, the ancient symbol involves a number of interrelated categories, such as fate, intuition or conjecture, inspiration, and predictions. Christian symbolism is based on the idea of redemption and moral innocence. Methodologically, the article is based on a cultural and historical approach, as well as on the comparative academic tradition. The overview of Dostoyevsky’s pre-materials for The Possessed (Demons enables us to suggest the use of Christian symbolism in this novel. Hence, the objective of the study is to investigate a composition of images and symbols in this piece of writing, with a special focus on the image of a chronicler since the storyline of the novel is developed through his perception. We make a supposition that there are several levels of Gospel perception in the artistic vision or consciousness of the chronicler, that form the basis of the symbolical composition of the novel. The article sequentially examines the examples of Christian symbolism, including the connection of ideas, characters and storylines of the novel with the Gospel. Then it gives evidence and reasons for the thesis that the Gospel gives the characters of the novel the grounds for shaping their destiny.

  12. Adducin family proteins possess different nuclear export potentials.

    Science.gov (United States)

    Liu, Chia-Mei; Hsu, Wen-Hsin; Lin, Wan-Yi; Chen, Hong-Chen

    2017-05-10

    The adducin (ADD) family proteins, namely ADD1, ADD2, and ADD3, are actin-binding proteins that play important roles in the stabilization of membrane cytoskeleton and cell-cell junctions. All the ADD proteins contain a highly conserved bipartite nuclear localization signal (NLS) at the carboxyl termini, but only ADD1 can localize to the nucleus. The reason for this discrepancy is not clear. To avoid the potential effect of cell-cell junctions on the distribution of ADD proteins, HA epitope-tagged ADD proteins and mutants were transiently expressed in NIH3T3 fibroblasts and their distribution in the cytoplasm and nucleus was examined by immunofluorescence staining. Several nuclear proteins were identified to interact with ADD1 by mass spectrometry, which were further verified by co-immunoprecipitation. In this study, we found that ADD1 was detectable both in the cytoplasm and nucleus, whereas ADD2 and ADD3 were detected only in the cytoplasm. However, ADD2 and ADD3 were partially (~40%) sequestered in the nucleus by leptomycin B, a CRM1/exportin1 inhibitor. Upon the removal of leptomycin B, ADD2 and ADD3 re-distributed to the cytoplasm. These results indicate that ADD2 and ADD3 possess functional NLS and are quickly transported to the cytoplasm upon entering the nucleus. Indeed, we found that ADD2 and ADD3 possess much higher potential to counteract the activity of the NLS derived from Simian virus 40 large T-antigen than ADD1. All the ADD proteins appear to contain multiple nuclear export signals mainly in their head and neck domains. However, except for the leucine-rich motif ( 377 FEALMRMLDWLGYRT 391 ) in the neck domain of ADD1, no other classic nuclear export signal was identified in the ADD proteins. In addition, the nuclear retention of ADD1 facilitates its interaction with RNA polymerase II and zinc-finger protein 331. Our results suggest that ADD2 and ADD3 possess functional NLS and shuttle between the cytoplasm and nucleus. The discrepancy in the

  13. A comparative bioavailability study of two ibuprofen formulations after single-dose administration in healthy volunteers

    Directory of Open Access Journals (Sweden)

    Metta S.S. Wiria

    2007-09-01

    Full Text Available This study was aimed to investigate the bioequivalence of ibuprofen 125 mg suppository formulation (Ibukal®, test formulation from PT. Kalbe Farma, Tbk., Jakarta and the ibuprofen suppository comparative formulation (Proris®, from PT. Pharos Indonesia, Jakarta in 12 healthy volunteers. The pharmacokinetic parameters used in this study were the area under the concentration-time curve from time zero to hour 10 (AUC0-t, the area under the concentration-time curve from time zero to infinite (AUC0-inf, the maximum concentration (Cmax, and the time needed to reach the maximum concentration (tmax. The study was designed as a random cross-over fashion, single-blinded which included 12 healthy adult volunteers. The volunteers were fasted overnight and in the morning they received a suppository of the test drug (Ibukal® or a suppository of the comparative drug (Proris®. Blood samples were withdrawn on hour 0 (control, 20 min; 40 min; 1; 1.5; 2; 2.5; 3; 4; 6; 8; and 10 time points after the administration of the drug. Following a wash-out period of 1 week, this procedure was repeated using the other drug. The serum concentration of the drug was determined by means of high-performance liquid chromatography with ultraviolet detection. The results of the study showed that, the mean (SD of AUC0-t, AUC0-inf, Cmax and tmax of the test drug were, respectively, 28.59(3.37 μg.h.mL-1, 30.47(3.56 μg.h.mL-1, 8.24(1.44 μg/mL, and 1.33(0.44 h. The mean (SD of AUC0-t, AUC0-inf, Cmax and tmax of the comparative drug were, respectively, 28.13(8.14 μg.h.mL-1, 30.56(8.05 μg.h.mL-1, 8.27(2.88 μg/mL, and 1.79(0.33 h. The geometric means ratio of the test to the comparative drug were 104.38% (CI 90%: 90.38-120.54% for AUC0-t, 101.97% (CI 90%: 89.51-116.16% for AUC0-inf, and 104.02% (CI 90%: 85.73-126.16% for Cmax. There was no side effect of the drug detected in this study. From the results we can conclude that the 125 mg of ibuprofen suppository of PT Kalbe Farma

  14. Computational study of ibuprofen removal from water by adsorption in realistic activated carbons.

    Science.gov (United States)

    Bahamon, Daniel; Carro, Leticia; Guri, Sonia; Vega, Lourdes F

    2017-07-15

    Molecular simulations using the Grand Canonical Monte Carlo (GCMC) method have been performed in order to obtain physical insights on how the interaction between ibuprofen (IBP) and activated carbons (ACs) in aqueous mixtures affects IBP removal from water by ACs. A nanoporous carbon model based on units of polyaromatic molecules with different number of rings, defects and polar-oxygenated sites is described. Individual effects of factors such as porous features and chemical heterogeneities in the adsorbents are investigated and quantified. Results are in good agreement with experimental adsorption data, highlightening the ability of GCMC simulation to describe the macroscopic adsorption performance in drug removal applications, while also providing additional insights into the IBP/water adsorption mechanism. The simulation results allow finding the optimal type of activated carbon material for separating this pollutant in water treatment. Copyright © 2017 Elsevier Inc. All rights reserved.

  15. Early intravenous ibuprofen decreases narcotic requirement and length of stay after traumatic rib fracture.

    Science.gov (United States)

    Bayouth, Lilly; Safcsak, Karen; Cheatham, Michael L; Smith, Chadwick P; Birrer, Kara L; Promes, John T

    2013-11-01

    Pain control after traumatic rib fracture is essential to avoid respiratory complications and prolonged hospitalization. Narcotics are commonly used, but adjunctive medications such as nonsteroidal anti-inflammatory drugs may be beneficial. Twenty-one patients with traumatic rib fractures treated with both narcotics and intravenous ibuprofen (IVIb) (Treatment) were retrospectively compared with 21 age- and rib fracture-matched patients who received narcotics alone (Control). Pain medication requirements over the first 7 hospital days were evaluated. Mean daily IVIb dose was 2070 ± 880 mg. Daily intravenous morphine-equivalent requirement was 19 ± 16 vs 32 ± 24 mg (P pain scores were lower in the Treatment group (P rib fractures significantly decreases narcotic requirement and results in clinically significant decreases in hospital length of stay. IVIb therapy should be initiated in patients with traumatic rib fractures to improve patient comfort and reduce narcotic requirement.

  16. Ultrasound-Assisted Enantioselective Esterification of Ibuprofen Catalyzed by a Flower-Like Nanobioreactor

    Directory of Open Access Journals (Sweden)

    Baiyi An

    2016-04-01

    Full Text Available A flower-like nanobioreactor was prepared for resolution of ibuprofen in organic solvents. Ultrasound irradiation has been used to improve the enzyme performance of APE1547 (a thermophilic esterase from the archaeon Aeropyrum pernix K1 in the enantioselective esterification. Under optimum reaction conditions (ultrasound power, 225 W; temperature, 45 °C; water activity, 0.21, the immobilized APE1547 showed an excellent catalytic performance (enzyme activity, 13.26 μmol/h/mg; E value, 147.1. After ten repeated reaction batches, the nanobioreactor retained almost 100% of its initial enzyme activity and enantioselectivity. These results indicated that the combination of the immobilization method and ultrasound irradiation can enhance the enzyme performance dramatically.

  17. Estimation of ibuprofen and famotidine in tablets by second order derivative spectrophotometery method

    Directory of Open Access Journals (Sweden)

    Dimal A. Shah

    2017-02-01

    Full Text Available A simple and accurate method for the analysis of ibuprofen (IBU and famotidine (FAM in their combined dosage form was developed using second order derivative spectrophotometery. IBU and FAM were quantified using second derivative responses at 272.8 nm and 290 nm in the spectra of their solutions in methanol. The calibration curves were linear in the concentration range of 100–600 μg/mL for IBU and 5–25 μg/mL for FAM. The method was validated and found to be accurate and precise. Developed method was successfully applied for the estimation of IBU and FAM in their combined dosage form.

  18. Ibuprofen for acute treatment of episodic tension-type headache in adults

    DEFF Research Database (Denmark)

    Derry, Sheena; Wiffen, Philip J; Moore, R Andrew

    2015-01-01

    2015. We sought unpublished studies by asking personal contacts and searching on-line clinical trial registers and manufacturers' websites. SELECTION CRITERIA: We included randomised, placebo-controlled studies (parallel-group or cross-over) using oral ibuprofen for symptomatic relief of an acute...... episode of TTH. Studies had to be prospective and include at least 10 participants per treatment arm. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed studies for inclusion, and extracted data. Numbers of participants achieving each outcome were used to calculate risk ratio (RR...... studies, all of which enrolled adult participants with frequent episodic TTH. Nine used the IHS diagnostic criteria, but two used the older classification of the Ad Hoc Committee, and one did not describe diagnostic criteria but excluded participants with migraines. While 3094 people with TTH participated...

  19. Uncertainty and Sensitivity Analysis for an Ibuprofen Synthesis Model Based on Hoechst Path

    DEFF Research Database (Denmark)

    da Conceicao Do Carmo Montes, Frederico; Gernaey, Krist V.; Sin, Gürkan

    2017-01-01

    into consideration the effects of temperature, acidity, and the choice of the catalyst. Parameter estimation and uncertainty analysis were conducted on the kinetic model parameters using experimental data available in the literature. Finally, one factor at a time sensitivity analysis in the form of deviations......The pharmaceutical industry faces several challenges and barriers when implementing new or improving current pharmaceutical processes, such as competition from generic drug manufacturers and stricter regulations from the U.S. Food and Drug Administration and the European Medicine agency. The demand...... for efficient and reliable models to simulate and design/improve pharmaceutical processes is therefore increasing. For the case of ibuprofen, a well-known anti-inflammatory drug, the existing models do not include its complete synthesis path, usually referring only to one out of aset of different reactions...

  20. Immobilized cells of Candida rugosa possessing fumarase activity

    Energy Technology Data Exchange (ETDEWEB)

    Yang, L.; Zhone, L.

    1980-01-01

    Immobilized cells of C. rugosa that possessed fumarase activity were prepared by different methods; the most active immobilized cells were entrapped in polyacrylamide gels. The effects of pH temperature, and divalent cations on the fumarase activity of both immobilized and native cells were the same. Mn/sup 2 +/, Mg/sup 2 +/, Ca/sup 2 +/, and Fe/sup 2 +/ did not protect the immobilized enzyme against thermal inactivation. The activity of immobilized fumarase remained constant during 91 days of storage of 4-6 degrees. The immobilized cell column was used for the continuous production of L-malic acid from 1M fumarate at 30 degrees and pH 8.5. The immobilized column operated steadily for 2 months. Half life of the immobilized fumarase at 30 degrees was 95 days.

  1. Social forces for team coordination in ball possession game

    Science.gov (United States)

    Yokoyama, Keiko; Shima, Hiroyuki; Fujii, Keisuke; Tabuchi, Noriyuki; Yamamoto, Yuji

    2018-02-01

    Team coordination is a basic human behavioral trait observed in many real-life communities. To promote teamwork, it is important to cultivate social skills that elicit team coordination. In the present work, we consider which social skills are indispensable for individuals performing a ball possession game in soccer. We develop a simple social force model that describes the synchronized motion of offensive players. Comparing the simulation results with experimental observations, we uncovered that the cooperative social force, a measure of perception skill, has the most important role in reproducing the harmonized collective motion of experienced players in the task. We further developed an experimental tool that facilitates real players' perceptions of interpersonal distance, revealing that the tool improves novice players' motions as if the cooperative social force were imposed.

  2. Comparative assessment of chewing gum and ibuprofen in the management of orthodontic pain with fixed appliances: A pragmatic multicenter randomized controlled trial.

    Science.gov (United States)

    Ireland, Anthony J; Ellis, Pamela; Jordan, Abbie; Bradley, Rebecca; Ewings, Paul; Atack, Nikki E; Griffiths, Helen; House, Kate; Moore, Matthew; Deacon, Scott; Wenger, Nick; Worth, Victoria; Scaysbrook, Emma; Sandy, Jonathan R

    2016-08-01

    The aim of this randomized trial was to investigate the effect of the use of a sugar-free chewing gum vs ibuprofen on reported pain in orthodontic patients. This was a 2-arm parallel design randomized controlled trial in 9 sites in the southwest of England. Patients about to undergo orthodontic treatment with maxillary and mandibular fixed appliances were recruited and randomly allocated to an experimental chewing gum group or a control ibuprofen group. Eligibility criteria included patients undergoing fixed maxillary and mandibular appliance therapy, aged 11 to 17 years, and able to use ibuprofen and chewing gum. The primary outcome measure was pain experienced after appliance placement using a mean of 3 recordings on a scale of 0 to 10. Secondary outcome measures were pain experienced in the subsequent 3 days, pain after the first archwire change, ibuprofen use, and appliance breakages. Pain scores were recorded with a questionnaire and posted to a collection center by each patient. Randomization was by means of a central telephone service and comprised computer-generated random numbers used to generate a sequential allocation list, with permuted blocks of variable size (2 and 4) and stratified by center. Neither the clinicians nor the patients were blinded to the intervention. Patients in the control group were permitted to use ibuprofen only, and patients in the experimental group were allowed to use ibuprofen if they did not get sufficient analgesia from the chewing gum. Data were analyzed using the principle of intention to treat with multilevel modeling to reflect the structured nature of the data (scores within patient within site). One thousand patients were recruited and randomized in a ratio of 1:1 to the chewing gum and ibuprofen (control) groups. The male-to-female ratios were similar in the groups. The pain questionnaire response rates were good at approximately 84% and 83% after appliance placement (chewing gum group, 419; ibuprofen group, 407) and

  3. High Concentrations of Sodium Chloride Improve Microbicidal Activity of Ibuprofen against Common Cystic Fibrosis Pathogens

    Directory of Open Access Journals (Sweden)

    Adrián J. Muñoz

    2018-05-01

    Full Text Available Ibuprofen (IBU-H, a widely used anti-inflammatory, also shows a marked antimicrobial effect against several bacterial species, including those involved in cystic fibrosis such as Pseudomona aeruginosa, methicillin resistant Staphylococcus aureus and Burkholderia cepacia complex. Additionally, our results show significant synergy between water soluble Na-ibuprofen (IBU-Na and ionic strength. Salt concentrations above 0.5 M modify the zeta potential promoting the action of Na-IBU; thus, with 1 M sodium chloride, IBU-Na is ten times more efficient than in the absence of ionic strength, and the minimum effective contact time is reduced from hours to minutes. In short time periods, where neither IBU-Na nor controls with 1 M NaCl show activity, the combination of both leads to a reduction in the bacterial load. We also analyzed whether the changes caused by salt on the bacterial membrane also promoted the activity of other microbicide compounds used in cystic fibrosis like gentamicin, tobramycin and phosphomycin. The results show that the presence of ionic strength only enhanced the bactericidal activity of the amphipathic molecule of IBU-Na. In this respect, the effect of saline concentration was also reflected in the surface properties of IBU-Na, where, in addition to the clear differences observed between 145 mM and 1 M, singular behaviors were also found, different in each condition. The combination of anti-inflammatory activity and this improved bactericidal effect of Na-IBU in hypertonic solution provides a new alternative for the treatment of respiratory infections of fibrotic patients based on known and widely used compounds.

  4. Effects of hypoxia on epididymal sperm parameters and protective role of ibuprofen and melatonin

    Directory of Open Access Journals (Sweden)

    Álvaro Vargas

    2011-01-01

    Full Text Available Hypobaric hypoxia is of interest due to an increase of human populations working at high altitude. Testicular damage is related to the physiological response (neoangiogenesis to increased intrascrotal blood flow as temperature rises. Hypoxia is a stress factor with overproduction of reactive oxygen species (ROS. The effect of hypoxia in mice reproductive parameters is analyzed. Animals were exposed to simulated hypoxia of 4,200 meters above sea level (m.a.s.l. in a chamber for 33.2 days, both to continuous (HH or intermittent hypoxia (HI with an intermittency period of 4 days hypoxia /4 days normoxia (500 m.a.s.l.. The anti-inflammatory drug Ibuprofen was administered to a group of mice to control vasodilation and increased blood flow. Melatonin was administered to another group of mice as a potent ROS scavenger. Animals in both HH and HI exposure were compared to normoxic non-treated controls. There was a hematological response in hypoxia, with an increase in hematocrit and reticulocytosis. There was also increased teratozoospermia. This damage was more pronounced in HH than HI, suggesting that alternating normoxic periods permits compensation for the effects of hypoxia. In both hypoxia systems, the level of lipoperoxidation and the instability of DNA increased. In HH, there was a reduction of teratozoospermia in melatonin-treated mice. Ibuprofen presented a protective effect on the same parameters as melatonin with both HI and HH. The quality of sperm DNA, fragmentation, unpacking and DNA stability diminished. In conclusion, reproductive damage elicited by HH or HI was partially ameliorated by simultaneous treatment with antiflogistic and/or antioxidant agents.

  5. Ibuprofen Can Induce Syndrome of Inappropriate Diuresis in Healthy Young Patients

    Directory of Open Access Journals (Sweden)

    Céline Roche

    2013-01-01

    Full Text Available A 30-year-old caucasian woman, without past medical history or known drug use, was admitted to the emergency department for persistent fever and arthralgias. The laboratory analysis showed moderate hypoosmolar hyponatremia (Na: 132 mmol/L, osmolality: 239 mOsm/L, normal sodium excretion (<20 mmol/L, and a high urinary osmolality (415 mOsm/L. Later, she deteriorated with seizures and deeper hyponatremia (Na: 113 mmol/L and so was moved to the critical care unit. At first, no obvious aetiology was found, the patient was euvolemic, as she was well hydrated and lacked concerning findings of heart failure, renal disease, or liver cirrhosis. A syndrome of inappropriate diuresis (SIAD was proposed, and corrective measures were started immediately to reduce her hyponatremia, including restriction of fluid intake. The administration of intravenous hypertonic saline solution permitted normal neurological status to be restored and corrected the sodium concentration but induced reversible acute renal failure. Further investigation revealed that the patient had ingested 8 g ibuprofen two days before admission. After other aetiologies were ruled out, drug-induced SIAD due to ibuprofen was the most likely diagnosis for this patient. SIAD-associated hyponatremia and acute renal failure are rare side effects of nonsteroidal anti-inflammatory drugs, particularly in young people. Therefore, this case may represent a unique case of NSAID-induced SIAD and highlight the need to obtain thorough medication histories and exclude all other potential causes in hyponatremic patients.

  6. Ibuprofen-Amino Acids Co-Crystal Screening Via Co-Grinding Methods

    Directory of Open Access Journals (Sweden)

    Othman Muhamad Fitri

    2016-01-01

    Full Text Available The importance of pharmaceutical co-crystals now has been recognized in order to improve the research and development in pharmaceutical industries. Low solubility of active pharmaceutical ingredient (API has led to the growth of new pharmaceutical co-crystals formation as it enhances the physicochemical properties of the API. In this works, preparation of new co-crystal formation between ibuprofen (IBP with selected amino acid compounds were performed by using dry grinding and liquid assisted grinding (LAG techniques. Ibuprofen (IBP was selected as the API meanwhile glycine (GLY, L-alanine (ALA and L-proline (PRO were selected as co-crystal former (CCF agents. The products of IBP-co-former from grinding experiments for the formation of co-crystals were characterized and verified using X-Ray Powder Diffraction (XRPD, Differential Scanning Calorimetry (DSC and Fourier Transform Infra-Red Spectroscopy (FTIR. The finding reveals that the IBP-PRO co-crystals have successfully formed. For IBP-PRO system, new crystalline peaks from XRPD were recorded at 2θ values of 4.374°, 5.436° and 10.944° from dry grinding technique and 4.41°, 5.436° and 10.962° for liquid assisted grinding (LAG technique. A new melting point of 257.49 °C was discovered for IBP-ALA indicates the possibility of co-crystals formation. On the other hand, the analysis for IBP-GLY shows that no co-crystals formed in the system.

  7. Influence of different structured channels of mesoporous silicate on the controlled ibuprofen delivery

    International Nuclear Information System (INIS)

    Gao, Lin; Sun, Jihong; Zhang, Li; Wang, Jinpeng; Ren, Bo

    2012-01-01

    The bimodal mesoporous silicas with short random mesoporous channels and MCM-41 with long ordered mesopores were synthesised and modified with 3-(2-aminoethylamino) propyltrimethoxysilane as ibuprofen carriers to study the influence of mesoporous structure on drug delivery property. For further comparing the different mesoporous channels, modified SBA-15 with relative large and long ordered mesopores was also synthesized as drug carriers. The resultant samples were characterized with X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectra, N 2 adsorption–desorption isotherms, thermogravimetric analyses, solid-state 29 Si NMR spectra, elemental analysis, and UV–vis spectra. Meanwhile, the Korsmeyer–Peppas equation f t = kt n was employed to analyze the drug release profile and three release mediums including simulated fluid solution, distilled water and simulated gastric fluid were used. The results indicated that the modified BMMs with the bimodal mesopores leaded to the most drug loading amount of 25.0 mg/0.1 g, while the MCM-41 with the long and one-dimensional mesopores had the least loading amount around 20.3 mg/0.1 g. Meanwhile, the easier diffusion behavior of drug molecules in the bimodal mesopore channels of BMMs resulted in relatively faster drug release properties in comparison with MCM-41, while the release time maintained in SBF for about 12 h (release percent was about 90 wt%) and corresponding release constant k obtained from Korsmeyer–Peppas equation was around 4.10. Highlights: ► BMMs, MCM-41 and SBA-15 with different mesostructure channels were modified with amino groups via post-treatment procedure. ► Loading and release profiles of ibuprofen in modified BMMs, MCM-41 and SBA-15. ► BMMs presents more drug loading amount than MCM-41 as well as better controlled release than SBA-15.

  8. A combined experimental and computational study of the molecular interactions between anionic ibuprofen and water

    Energy Technology Data Exchange (ETDEWEB)

    Zapata-Escobar, Andy; Manrique-Moreno, Marcela; Guerra, Doris; Hadad, C. Z.; Restrepo, Albeiro, E-mail: albeiro@exactas.udea.edu.co [Instituto de Química, Universidad de Antioquia UdeA, Calle 70 No. 52–21, Medellín (Colombia)

    2014-05-14

    In this work, we report a detailed study of the microsolvation of anionic ibuprofen, Ibu{sup −}. Stochastic explorations of the configurational spaces for the interactions of Ibu{sup −} with up to three water molecules at the DFT level lead to very rich and complex potential energy surfaces. Our results suggest that instead of only one preponderant structure, a collection of isomers with very similar energies would have significant contributions to the properties of the solvated drug. One of these properties is the shift on the vibrational frequencies of the asymmetric stretching band of the carboxylate group in hydrated Ibu{sup −} with respect to the anhydrous drug, whose experimental values are nicely reproduced using the weighted contribution of the structures. We found at least three types of stabilizing interactions, including conventional CO {sub 2}{sup −}⋯H{sub 2}O, H{sub 2}O⋯H{sub 2}O charge assisted hydrogen bonds (HBs), and less common H{sub 2}O⋯H–C and H{sub 2}O⋯π interactions. Biological water molecules, those in direct contact with Ibu{sup −}, prefer to cluster around the carboxylate oxygen atoms via cyclic or bridged charge assisted hydrogen bonds. Many of those interactions are strongly affected by the formal carboxylate charge, resulting in “enhanced” HBs with increased strengths and degree of covalency. We found striking similarities between this case and the microsolvation of dymethylphosphate, which lead us to hypothesize that since microsolvation of phosphatidylcholine depends mainly on the formal charge of its ionic PO {sub 2}{sup −} group in the polar head, then microsolvation of anionic ibuprofen and interactions of water molecules with eukaryotic cell membranes are governed by the same types of physical interactions.

  9. Influence of different structured channels of mesoporous silicate on the controlled ibuprofen delivery

    Energy Technology Data Exchange (ETDEWEB)

    Gao, Lin [Department of Chemistry and Chemical Engineering, College of Environmental and Energy Engineering, Beijing University of Technology, 100 PingLeYuan, Chaoyang District, Beijing 100124 (China); Sun, Jihong, E-mail: jhsun@bjut.edu.cn [Department of Chemistry and Chemical Engineering, College of Environmental and Energy Engineering, Beijing University of Technology, 100 PingLeYuan, Chaoyang District, Beijing 100124 (China); Zhang, Li; Wang, Jinpeng; Ren, Bo [Department of Chemistry and Chemical Engineering, College of Environmental and Energy Engineering, Beijing University of Technology, 100 PingLeYuan, Chaoyang District, Beijing 100124 (China)

    2012-08-15

    The bimodal mesoporous silicas with short random mesoporous channels and MCM-41 with long ordered mesopores were synthesised and modified with 3-(2-aminoethylamino) propyltrimethoxysilane as ibuprofen carriers to study the influence of mesoporous structure on drug delivery property. For further comparing the different mesoporous channels, modified SBA-15 with relative large and long ordered mesopores was also synthesized as drug carriers. The resultant samples were characterized with X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectra, N{sub 2} adsorption-desorption isotherms, thermogravimetric analyses, solid-state {sup 29}Si NMR spectra, elemental analysis, and UV-vis spectra. Meanwhile, the Korsmeyer-Peppas equation f{sub t} = kt{sup n} was employed to analyze the drug release profile and three release mediums including simulated fluid solution, distilled water and simulated gastric fluid were used. The results indicated that the modified BMMs with the bimodal mesopores leaded to the most drug loading amount of 25.0 mg/0.1 g, while the MCM-41 with the long and one-dimensional mesopores had the least loading amount around 20.3 mg/0.1 g. Meanwhile, the easier diffusion behavior of drug molecules in the bimodal mesopore channels of BMMs resulted in relatively faster drug release properties in comparison with MCM-41, while the release time maintained in SBF for about 12 h (release percent was about 90 wt%) and corresponding release constant k obtained from Korsmeyer-Peppas equation was around 4.10. Highlights: Black-Right-Pointing-Pointer BMMs, MCM-41 and SBA-15 with different mesostructure channels were modified with amino groups via post-treatment procedure. Black-Right-Pointing-Pointer Loading and release profiles of ibuprofen in modified BMMs, MCM-41 and SBA-15. Black-Right-Pointing-Pointer BMMs presents more drug loading amount than MCM-41 as well as better controlled release than SBA-15.

  10. A combined experimental and computational study of the molecular interactions between anionic ibuprofen and water

    International Nuclear Information System (INIS)

    Zapata-Escobar, Andy; Manrique-Moreno, Marcela; Guerra, Doris; Hadad, C. Z.; Restrepo, Albeiro

    2014-01-01

    In this work, we report a detailed study of the microsolvation of anionic ibuprofen, Ibu − . Stochastic explorations of the configurational spaces for the interactions of Ibu − with up to three water molecules at the DFT level lead to very rich and complex potential energy surfaces. Our results suggest that instead of only one preponderant structure, a collection of isomers with very similar energies would have significant contributions to the properties of the solvated drug. One of these properties is the shift on the vibrational frequencies of the asymmetric stretching band of the carboxylate group in hydrated Ibu − with respect to the anhydrous drug, whose experimental values are nicely reproduced using the weighted contribution of the structures. We found at least three types of stabilizing interactions, including conventional CO 2 − ⋯H 2 O, H 2 O⋯H 2 O charge assisted hydrogen bonds (HBs), and less common H 2 O⋯H–C and H 2 O⋯π interactions. Biological water molecules, those in direct contact with Ibu − , prefer to cluster around the carboxylate oxygen atoms via cyclic or bridged charge assisted hydrogen bonds. Many of those interactions are strongly affected by the formal carboxylate charge, resulting in “enhanced” HBs with increased strengths and degree of covalency. We found striking similarities between this case and the microsolvation of dymethylphosphate, which lead us to hypothesize that since microsolvation of phosphatidylcholine depends mainly on the formal charge of its ionic PO 2 − group in the polar head, then microsolvation of anionic ibuprofen and interactions of water molecules with eukaryotic cell membranes are governed by the same types of physical interactions

  11. Studies on oxidative radiolysis of ibuprofen in presence of potassium persulfate

    International Nuclear Information System (INIS)

    Paul, Jhimli; Naik, D.B.; Bhardwaj, Y.K.; Varshney, Lalit

    2014-01-01

    The radiolysis of ibuprofen (IBP), a model pharmaceutical compound, was studied by gamma irradiation in an aqueous solution in the presence and absence of potassium persulfate (K 2 S 2 O 8 ). The extent of mineralization was investigated by measuring the UV–visible spectra, decrease in the chemical oxygen demand (COD) and the total organic carbon (TOC) content of aqueous IBP solution at different doses. The gamma radiolysis, in the presence of K 2 S 2 O 8 , required much lesser dose compared to in the absence of K 2 S 2 O 8 for the same extent of mineralization of aqueous IBP solution. The pulse radiolysis of IBP was carried out under different radiolytic conditions to understand the mechanism of efficient mineralization of IBP during gamma radiolysis in the presence of K 2 S 2 O 8 . It was found that unlike · OH radical, SO 4 ·− radical preferentially produces benzyl type of radicals via the formation of the benzene radical cation. The results concluded that the gamma radiolysis in presence of K 2 S 2 O 8 could be one of the efficient advanced oxidation processes for degradation of pharmaceutical compounds present in the aqueous solution. - Highlights: • The radiolysis of aqueous solution of Ibuprofen (IBP) was investigated. • The COD and TOC content decreased significantly in presence of K 2 S 2 O 8 . • Pulse radiolysis studies revealed the mechanism of mineralization of IBP. • The presence of K 2 S 2 O 8 increased the efficiency of gamma radiolysis

  12. Comparison of diclofenac-emulgel local application with oral ibuprofen administration for the treatment of active interphalangeal hand joints osteoarthritis (Heberden and/or Bushar nodules

    Directory of Open Access Journals (Sweden)

    J Zacher

    2007-01-01

    Full Text Available Objective. To assess efficacy and tolerability of diclofenac-emulgel local application in comparison with oral ibuprofen administration for the treatment of active interphalangeal hand joints osteoarthritis (Heberden and/or Bushar nodules. Material and methods. 321 pts were randomized into two groups. Diclofenac-emulgel (active drug and placebo ibuprofen tablets were administered in one of them, placebo diclofenac-emulgel and ibuprofen tablets (active drug — in the other. Diclofenac was administered as 10 cm strip locally 4 times a day and 400 mg of ibuprofen were given 3 times a day. Frequency of improvement was used as the main outcome measure. Improvement was registered if pain on 100 mm visual analog scale decreased at least by 40%. Disease activity, pain at rest, pain at movement, morning stiffness, grip strength and quality of life were used as additional outcome measures. Results. To the end of treatment according to 5% lower equivalency limit local therapy was at least as effective as oral administration of ibuprofen (p=0,007. Administration of both treatment methods provided also comparable improvement of all additional outcome measures. Both treatment methods showed good tolerability but more pts with receiving ibuprofen experienced serious adverse events than those using diclofenac (9 and 4 pts respectively. There was also similar proportion of pts prematurely withdrawn due to side effects (n=21: 5 (3% from them received diclofenac and 16 (10% - ibuprofen. Similar ratio of adverse events attributed to study treatment was revealed. Such events were present in 2 pts using diclofenac and in 13 (8,3% receiving ibuprofen. Most of these events applied to gastrointestinal tract (in 1 pt using diclofenac and in 8 pts receiving ibuprofen. Conclusion. Local treatment of active interphalangeal hand joints osteoarthritis (Heberden and/or Bushar nodules with diclofenac is at least as effective as systemic administration of ibuprofen

  13. The role of prophylactic ibuprofen and N-acetylcysteine on the level of cytokines in periapical exudates and the post-treatment pain

    Directory of Open Access Journals (Sweden)

    Ehsani Maryam

    2012-09-01

    Full Text Available Abstract Background Periapical lesions are inflammatory diseases that result in periapical bone destruction because of host defensive–microbial disturbances. Objective To evaluate the role of prophylactic ibuprofen and N-acetylcysteine (NAC on the levels of tumor necrosis factor alpha (TNF- α, interleukin- 6(IL-6 and IL-17 and post-treatment pain level in chronic periapical lesions. Materials and methods Eighty patients with chronic apical lesions less than 1 cm were randomly assigned to receive NAC tablets (400 mg, ibuprofen tablets (400 mg, NAC (400 mg/ibuprofen (200 mg combination and placebo 90 minutes prior to sampling. Periapical exudates were collected from root canals. TNF- α, IL-6 and IL-17 levels were determined by ELISA and post-treatment pain was assessed using a visual analog scale (VAS. Results There was a significant difference in IL-6 level between ibuprofen group and placebo (p = 0.019. Significant difference in IL-17 level was observed between NAC/ibuprofen combination group and placebo (p = 0.043. Four hours after treatment, a significant difference was observed in VAS pain score between ibuprofen group and placebo (p = 0.017. Eight hours post-treatment, VAS pain score for NAC group was statistically lower than placebo group (p = 0.033. After 12 hours VAS pain score showed a significant decrease in NAC group compared to placebo (p = 0.049. Conclusion The prophylactic ibuprofen and NAC failed to clearly reflect their effect on cytokines levels in exudates of chronic periapical lesions. On the other hand it seems that NAC can be a substitute for ibuprofen in the management of post endodontic pain.

  14. The Role of Prophylactic Ibuprofen and N-Acetylcysteine on the Level of Cytokines in Periapical Exudates and the Post-Treatment Pain

    Directory of Open Access Journals (Sweden)

    Seyyed Mohsen Aghajanpour Mir

    2012-09-01

    Full Text Available Background Periapical lesions are inflammatory diseases that result in periapical bone destruction because of host defensive-microbial disturbances. Objective:To evaluate the role of prophylactic ibuprofen and N-acetylcysteine (NAC on the levels of tumor necrosis factor alpha (TNF- alpha, interleukin- 6(IL-6 and IL-17 and post-treatment pain level in chronic periapical lesions. Materials and methods Eighty patients with chronic apical lesions less than 1 cm were randomly assigned to receive NAC tablets (400 mg, ibuprofen tablets (400 mg, NAC (400 mg/ibuprofen (200 mg combination and placebo 90 minutes prior to sampling. Periapical exudates were collected from root canals. TNF- alpha, IL-6 and IL-17 levels were determined by ELISA and posttreatment pain was assessed using a visual analog scale (VAS. Results:There was a significant difference in IL-6 level between ibuprofen group and placebo (p = 0.019. Significant difference in IL-17 level was observed between NAC/ibuprofen combination group and placebo (p = 0.043. Four hours after treatment, a significant difference was observed in VAS pain score between ibuprofen group and placebo (p = 0.017. Eight hours post-treatment, VAS pain score for NAC group was statistically lower than placebo group (p = 0.033. After 12 hours VAS pain score showed a significant decrease in NAC group compared to placebo (p = 0.049. Conclusion:The prophylactic ibuprofen and NAC failed to clearly reflect their effect on cytokines levels in exudates of chronic periapical lesions. On the other hand it seems that NAC can be a substitute for ibuprofen in the management of post endodontic pain

  15. Efficacy and safety assessment of acute sports-related traumatic soft tissue injuries using a new ibuprofen medicated plaster: results from a randomized controlled clinical trial.

    Science.gov (United States)

    Predel, Hans-Georg; Connolly, Mark P; Bhatt, Aomesh; Giannetti, Bruno

    2017-11-01

    To investigate the efficacy and safety of a recently developed ibuprofen medicated plaster in the treatment of acute sports impact injuries/contusions. In this double-blind, multi-center, placebo-controlled, parallel group, phase 3 study (EudraCT Number: 2012-003257-2) patients (n = 132; ages 18 to 60 years) diagnosed with acute sports-related traumatic blunt soft tissue injury/contusion to the upper or lower limbs were randomized to receive either ibuprofen 200 mg plaster (n = 64) or placebo plaster (n = 68). Plasters were administered once daily for five consecutive days. The primary assessment was the area under the curve (AUC) of the visual analogue scale (VAS) of pain on movement (POM) over 0 to 72 h (VAS 0-72 ). The ibuprofen medicated plaster was associated with a reduction in pain on movement (POM) based on lower VAS AUC 0-72h (2399.4 mm*h) compared with placebo (4078.9 mm*h) (least squares mean difference: - 1679.5 mm*h; P ibuprofen medicated plaster compared with placebo at 12, 48, 24, and 120 h (P ibuprofen medicated plaster was associated with greater reduction in tenderness/pain than placebo at each timepoint (P values ibuprofen plaster, and n = 6 [8.8%] for placebo). All drug-related AEs were administration site reactions and were mild in intensity. The results of this study indicate that ibuprofen medicated plaster results in rapid and clinically relevant reduction of pain in patients suffering from blunt musculoskeletal injuries or recurrent pain. The ibuprofen medicated plaster was well tolerated.

  16. Intravenous Ibuprofen for Treatment of Post-Operative Pain: A Multicenter, Double Blind, Placebo-Controlled, Randomized Clinical Trial.

    Directory of Open Access Journals (Sweden)

    Andrea Gago Martínez

    Full Text Available Non-steroidal anti-inflammatory drugs are often used as components of multimodal therapy for postoperative pain management, but their use is currently limited by its side effects. The specific objective of this study was to evaluate the efficacy and safety of a new formulation of intravenous (IV ibuprofen for the management of postoperative pain in a European population.A total of 206 patients from both abdominal and orthopedic surgery, were randomly assigned in 1:1 ratio to receive 800 mg IV-ibuprofen or placebo every 6 hours; all patients had morphine access through a patient controlled analgesia pump. The primary outcome measure was median morphine consumption within the first 24 hours following surgery. The mean±SEM of morphine requirements was reduced from 29,8±5,25 mg to 14,22±3,23 mg (p = 0,015 and resulted in a decrease in pain at rest (p = 0,02 measured by Visual Analog Scale (VAS from mean±SEM 3.34±0,35 to 0.86±0.24, and also in pain during movement (p = 0,02 from 4.32±0,36 to 1.90±0,30 in the ibuprofen treatment arm; while in the placebo group VAS score at rest ranged from 4.68±0,40 to 2.12±0,42 and during movement from 5.66±0,42 to 3.38±0,44. Similar treatment-emergent adverse events occurred across both study groups and there was no difference in the overall incidence of these events.Perioperative administration of IV-Ibuprofen 800 mg every 6 hours in abdominal surgery patient's decreases morphine requirements and pain score. Furthermore IV-Ibuprofen was safe and well tolerate. Consequently we consider appropriate that protocols for management of postoperative pain include IV-Ibuprofen 800 mg every 6 hours as an option to offer patients an analgesic benefit while reducing the potentially risks associated with morphine consumption.EU Clinical Trials Register 2011-005007-33.

  17. Intravenous Ibuprofen for Treatment of Post-Operative Pain: A Multicenter, Double Blind, Placebo-Controlled, Randomized Clinical Trial

    Science.gov (United States)

    Escontrela Rodriguez, Blanca; Planas Roca, Antonio; Martínez Ruiz, Alberto

    2016-01-01

    Background Non-steroidal anti-inflammatory drugs are often used as components of multimodal therapy for postoperative pain management, but their use is currently limited by its side effects. The specific objective of this study was to evaluate the efficacy and safety of a new formulation of intravenous (IV) ibuprofen for the management of postoperative pain in a European population. Methods and Findings A total of 206 patients from both abdominal and orthopedic surgery, were randomly assigned in 1:1 ratio to receive 800 mg IV-ibuprofen or placebo every 6 hours; all patients had morphine access through a patient controlled analgesia pump. The primary outcome measure was median morphine consumption within the first 24 hours following surgery. The mean±SEM of morphine requirements was reduced from 29,8±5,25 mg to 14,22±3,23 mg (p = 0,015) and resulted in a decrease in pain at rest (p = 0,02) measured by Visual Analog Scale (VAS) from mean±SEM 3.34±0,35 to 0.86±0.24, and also in pain during movement (p = 0,02) from 4.32±0,36 to 1.90±0,30 in the ibuprofen treatment arm; while in the placebo group VAS score at rest ranged from 4.68±0,40 to 2.12±0,42 and during movement from 5.66±0,42 to 3.38±0,44. Similar treatment-emergent adverse events occurred across both study groups and there was no difference in the overall incidence of these events. Conclusions Perioperative administration of IV-Ibuprofen 800 mg every 6 hours in abdominal surgery patient’s decreases morphine requirements and pain score. Furthermore IV-Ibuprofen was safe and well tolerate. Consequently we consider appropriate that protocols for management of postoperative pain include IV-Ibuprofen 800 mg every 6 hours as an option to offer patients an analgesic benefit while reducing the potentially risks associated with morphine consumption. Trial Registration EU Clinical Trials Register 2011-005007-33 PMID:27152748

  18. Radiation protective agents possessing anti-oxidative properties

    Energy Technology Data Exchange (ETDEWEB)

    Anzai, Kazunori; Ueno, Emi; Yoshida, Akira; Furuse, Masako; Ikota, Nobuo [National Inst. of Radiological Sciences, Research Center for Radiation Safety, Chiba, Chiba (Japan)

    2005-11-15

    The purpose of studies is to see mechanisms of radiation protection of agents possessing anti-oxidative properties because the initial step resulting in radiation hazard is the formation of radicals by water radiolysis. Agents were commercially available or synthesized proxyl derivatives (spin prove agents), commercially available spin-trapping agents, edaravone and TMG (a tocopherol glycoside). Mice and cultured cells were X-irradiated by Shimadzu Pantak HF-320 or 320S. Survivals of cells were determined by colony assay and of mice, to which the agents were given intraperitoneally before or after X-irradiation, within 30 days post irradiation. Plasma and marrow concentrations of proxyls were estimated by electron spin resonance (ESR) spectrometry. Mechanisms of their radiation protective effects were shown different from agent to agent. TMG was found effective even post irradiation, which suggests a possibility for a new drug development. Some (spin trapping agents and TMG), virtually ineffective at the cell level, were found effective in the whole body, suggesting the necessity of studies on their disposition and metabolism. (S.I.)

  19. Radiation protective agents possessing anti-oxidative properties

    International Nuclear Information System (INIS)

    Anzai, Kazunori; Ueno, Emi; Yoshida, Akira; Furuse, Masako; Ikota, Nobuo

    2005-01-01

    The purpose of studies is to see mechanisms of radiation protection of agents possessing anti-oxidative properties because the initial step resulting in radiation hazard is the formation of radicals by water radiolysis. Agents were commercially available or synthesized proxyl derivatives (spin prove agents), commercially available spin-trapping agents, edaravone and TMG (a tocopherol glycoside). Mice and cultured cells were X-irradiated by Shimadzu Pantak HF-320 or 320S. Survivals of cells were determined by colony assay and of mice, to which the agents were given intraperitoneally before or after X-irradiation, within 30 days post irradiation. Plasma and marrow concentrations of proxyls were estimated by electron spin resonance (ESR) spectrometry. Mechanisms of their radiation protective effects were shown different from agent to agent. TMG was found effective even post irradiation, which suggests a possibility for a new drug development. Some (spin trapping agents and TMG), virtually ineffective at the cell level, were found effective in the whole body, suggesting the necessity of studies on their disposition and metabolism. (S.I.)

  20. The possession law suit, caused by forbidden immissions

    Directory of Open Access Journals (Sweden)

    Popov Danica D.

    2015-01-01

    Full Text Available In the Serbian Law and in most of jurisdictions, there are limits on exercising the right of property. The real estate owner must refrain from activities by which the use of other real estate is being impoded through the immission of execive gasses, vapors, smoke, heat noise, tremors etc. The property ownership whose is affected by immission exceeding the set limits, has the right to request a stop of immisions which exceeded the allowed volume of immissions. In article author describes various kinds of immissions. The general feature of this law suit is that there is only discussion on the facts and not for a legal matters. Subject matter jurisdiction for the resolution of such disputes belongs to the court of general jurisdiction, while the disputes itself is a litigation. The special rule of proceedings of action of disturbance are: provisionality of the protection of possession; urgency in proceedings; initiation of proceedings; limiting of objection; prescribing temporary measures; rendering a ruling in the form of order; appeals which may be filed within a short deadline and which does not have suspensive effect (do not delay the execution of the order; revision is not allowed etc.

  1. Novel β-amyloid aggregation inhibitors possessing a turn mimic.

    Science.gov (United States)

    Hamada, Yoshio; Miyamoto, Naoko; Kiso, Yoshiaki

    2015-04-01

    Amyloid β peptide, the main component of senile plaques found in the brain of Alzheimer disease (AD) patients, is a molecular target for AD therapeutic intervention. A number of potential AD therapeutics have been reported, including inhibitors of β-secretase, γ-secretase, and Aβ aggregation, and anti-amyloid agents, such as neprilysin, insulin degrading enzyme (IDE), and Aβ antibodies. Recently, we reported potent small-sized β-secretase (BACE1) inhibitors, which could serve as anti-AD drugs. However AD is a progressive disorder, where dementia symptoms gradually worsen over several decades, and therefore may require many years to get cured. One possible way to achieve a greater therapeutic effect is through simultaneous administration of multiple drugs, similar to those used in Highly Active Anti-Retroviral Therapy (HAART) used to treat AIDS. In order to overcome AD, we took a drug discovery approach to evaluate, novel β-amyloid aggregation inhibitors. Previously, we reported that a tong-type compound possessing a turn mimic as the inhibitor of HIV-1 protease dimerization. Oligomerized amyloid β peptides contain a turn structure within the molecule. Here, we designed and synthesized novel β-amyloid aggregation inhibitors with a turn-mimic template, based on the turn conformer of the oligomerized amyloid β peptides. Copyright © 2015 Elsevier Ltd. All rights reserved.

  2. Influence of acetaminophen and ibuprofen on in vivo patellar tendon adaptations to knee extensor resistance exercise in older adults

    DEFF Research Database (Denmark)

    Carroll, C C; Dickinson, J M; LeMoine, J K

    2011-01-01

    adults induces modest changes in the mechanical properties of the patellar tendon. Over-the-counter doses of acetaminophen, but not ibuprofen, have a strong influence on tendon mechanical and material property adaptations to resistance training. These findings add to a growing body of evidence......Millions of older individuals consume acetaminophen or ibuprofen daily and these same individuals are encouraged to participate in resistance training. Several in vitro studies suggest that cyclooxygenase-inhibiting drugs can alter tendon metabolism and may influence adaptations to resistance...... tendon properties were assessed with MRI [cross-sectional area (CSA) and signal intensity] and ultrasonography of patellar tendon deformation coupled with force measurements to obtain stiffness, modulus, stress, and strain. Mean patellar tendon CSA was unchanged (P > 0.05) with training in the placebo...

  3. Optimization and design of ibuprofen-loaded nanostructured lipid carriers using a hybrid-design approach for ocular drug delivery

    Science.gov (United States)

    Rathod, Vishal

    The objective of the present project was to develop the Ibuprofen-loaded Nanostructured Lipid Carrier (IBU-NLCs) for topical ocular delivery based on substantial pre-formulation screening of the components and understanding the interplay between the formulation and process variables. The BCS Class II drug: Ibuprofen was selected as the model drug for the current study. IBU-NLCs were prepared by melt emulsification and ultrasonication technique. Extensive pre-formulation studies were performed to screen the lipid components (solid and liquid) based on drug's solubility and affinity as well as components compatibility. The results from DSC & XRD assisted in selecting the most suitable ratio to be utilized for future studies. DynasanRTM 114 was selected as the solid lipid & MiglyolRTM 840 was selected as the liquid lipid based on preliminary lipid screening. The ratio of 6:4 was predicted to be the best based on its crystallinity index and the thermal events. As there are many variables involved for further optimization of the formulation, a single design approach is not always adequate. A hybrid-design approach was applied by employing the Plackett Burman design (PBD) for preliminary screening of 7 critical variables, followed by Box-Behnken design (BBD), a sub-type of response surface methodology (RSM) design using 2 relatively significant variables from the former design and incorporating Surfactant/Co-surfactant ratio as the third variable. Comparatively, KolliphorRTM HS15 demonstrated lower Mean Particle Size (PS) & Polydispersity Index (PDI) and KolliphorRTM P188 resulted in Zeta Potential (ZP) ibuprofen thereafter over several hours. These values also confirm that the production method, and all other selected variables, effectively promoted the incorporation of ibuprofen in NLC. Quality by Design (QbD) approach was successfully implemented in developing a robust ophthalmic formulation with superior physicochemical and morphometric properties. NLCs as the

  4. Ibuprofen administration attenuates serum TNF-α levels, hepatic glutathione depletion, hepatic apoptosis and mouse mortality after Fas stimulation

    International Nuclear Information System (INIS)

    Cazanave, Sophie; Vadrot, Nathalie; Tinel, Marina; Berson, Alain; Letteron, Philippe; Larosche, Isabelle; Descatoire, Veronique; Feldmann, Gerard; Robin, Marie-Anne; Pessayre, Dominique

    2008-01-01

    Fas stimulation recruits neutrophils and activates macrophages that secrete tumor necrosis factor-α (TNF-α), which aggravates Fas-mediated liver injury. To determine whether nonsteroidal anti-inflammatory drugs modify these processes, we challenged 24-hour-fasted mice with the agonistic Jo2 anti-Fas antibody (4 μg/mouse), and treated the animals 1 h later with saline or ibuprofen (250 mg/kg), a dual cyclooxygenase (COX)-1 and COX-2 inhibitor. Ibuprofen attenuated the Jo2-mediated recruitment/activation of myeloperoxidase-secreting neutrophils/macrophages in the liver, and attenuated the surge in serum TNF-α. Ibuprofen also minimized hepatic glutathione depletion, Bid truncation, caspase activation, outer mitochondrial membrane rupture, hepatocyte apoptosis and the increase in serum alanine aminotransferase (ALT) activity 5 h after Jo2 administration, to finally decrease mouse mortality at later times. The concomitant administration of pentoxifylline (decreasing TNF-α secretion) and infliximab (trapping TNF-α) likewise attenuated the Jo2-mediated increase in TNF-α, the decrease in hepatic glutathione, and the increase in serum ALT activity 5 h after Jo2 administration. The concomitant administration of the COX-1 inhibitor, SC-560 (10 mg/kg) and the COX-2 inhibitor, celecoxib (40 mg/kg) 1 h after Jo2 administration, also decreased liver injury 5 h after Jo2 administration. In contrast, SC-560 (10 mg/kg) or celecoxib (40 or 160 mg/kg) given alone had no significant protective effects. In conclusion, secondary TNF-α secretion plays an important role in Jo2-mediated glutathione depletion and liver injury. The combined inhibition of COX-1 and COX-2 by ibuprofen attenuates TNF-α secretion, glutathione depletion, mitochondrial alterations, hepatic apoptosis and mortality in Jo2-treated fasted mice

  5. Actual use of and adherence to ibuprofen 400 mg tablet dosing instructions in a simulated OTC environment
.

    Science.gov (United States)

    Meeves, Suzanne; Leyva, Rina; Richardson, Clark; Wilson, Brenda; Savastano, David M

    2017-07-01

    Evaluate adherence of US consumers to proposed label directions for a new 400 mg ibuprofen formulation. In this single-arm, open-label, multicenter, 30-day study simulating an over-the-counter (OTC)-like environment, US analgesic consumers reviewed proposed product packaging for a new 400 mg ibuprofen formulation and made a purchase decision. Purchasers used the product as needed and recorded use over 30 days. Outcomes included the percentage of participants who exhibited correct or acceptable product use for the primary endpoint (not exceeding 1,200 mg/day > 2 times during the study) or secondary endpoint (not exceeding 400 mg/dose > 2 times during the study) and adherence to the labeled dosing interval of 6 - 8 hours. Primary endpoint success was met if the lower bound of the 95% confidence interval (CI) was ≥ 85%. Of 685 purchasers providing use data, correct or acceptable use behavior occurred in 95.2% (95% CI: 93.6%, 96.8%) regarding total daily dose and in 84.4% (95% CI: 81.7%, 87.1%) regarding the number of tablets taken per dosing occasion. Most participants (87.3%) never used > 1,200 mg/day or took > 1 tablet/dose (78.1%). Nearly 43% of subjects re-dosed within 6 hours of the previous dose; of these, ~ 82% re-dosed between the 4- and 6-hour time intervals. Adverse events were consistent with prior ibuprofen 200 mg experience. This study provides evidence that a majority of US consumers would be able to use OTC ibuprofen 400 mg tablets in a manner consistent with product labeling. Misuse rates were low and unlikely to generate an excess risk of clinically important adverse events.
.

  6. Comparative Studies on the Dissolution Profiles of Oral Ibuprofen Suspension and Commercial Tablets using Biopharmaceutical Classification System Criteria

    Science.gov (United States)

    Rivera-Leyva, J. C.; García-Flores, M.; Valladares-Méndez, A.; Orozco-Castellanos, L. M.; Martínez-Alfaro, M.

    2012-01-01

    In vitro dissolution studies for solid oral dosage forms have recently widened the scope to a variety of special dosage forms such as suspensions. For class II drugs, like Ibuprofen, it is very important to have discriminative methods for different formulations in physiological conditions of the gastrointestinal tract, which will identify different problems that compromise the drug bioavailability. In the present work, two agitation speeds have been performed in order to study ibuprofen suspension dissolution. The suspensions have been characterised relatively to particle size, density and solubility. The dissolution study was conducted using the following media: buffer pH 7.2, pH 6.8, 4.5 and 0.1 M HCl. For quantitative analysis, the UV/Vis spectrophotometry was used because this methodology had been adequately validated. The results show that 50 rpm was the adequate condition to discriminate the dissolution profile. The suspension kinetic release was found to be dependent on pH and was different compared to tablet release profile at the same experimental conditions. The ibuprofen release at pH 1.0 was the slowest. PMID:23626386

  7. Simultaneous Determination of Ibuprofen and Caffeine in Urine Samples by Combining MCR-ALS and Excitation-emission Data

    Directory of Open Access Journals (Sweden)

    Masoumeh Mohammadnejad

    2016-06-01

    Full Text Available Second order advantage of excitation-emission fluorescence matrix was applied for the simultaneous determination of ibuprofen and caffeine. The proposed method is based on the measurement of the native fluorescence and recording emission spectra of ibuprofen and caffeine in different excitation wavelengths. The mixture of these compounds was resolved by multivariate curve resolution coupled with alternative least squares (MCR-ALS on constructed matrix. The EEM spectra were recorded at excitation wavelengths from 250-275 nm; the emission wavelengths ranged from 275-400 nm. For each particular quantitative determination, an augmented matrix was defined. The resolution of each augmented-data matrix gave an estimation of the excitation and emission spectra of the species included in the model. Ibuprofen and caffeine were determined in concentration range from 0.10-8.00 and 0.50-15.00 mg ml-1, respectively. The minimal sample pretreatment and relatively low running cost, make this method a good alternative to existing methods for determination of the analytes in urine samples.

  8. Comparing the analgesic effect of heat patch containing iron chip and ibuprofen for primary dysmenorrhea: a randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Navvabi Rigi Shahindokht

    2012-08-01

    Full Text Available Abstract Background Primary dysmenorrhea is a common and sometimes disabling condition. In recent years, some studies aimed to improve the treatment of dysmenorrhea, and therefore, introduced several therapeutic measures. This study was designed to compare the analgesic effect of iron chip containing heat wrap with ibuprofen for the treatment of primary dysmenorrhea. Methods In this randomized (IRCT201107187038N2 controlled trial, 147 students (18–30 years old with the diagnosis of primary dysmenorrhea were enrolled considering the CONSORT guideline. Screening for primary dysmenorrhea was done by a two-question screening tool. The participants were randomly assigned into one of the intervention groups (heat Patch and ibuprofen. Data regarding the severity and emotional impact of the pain were recorded by a shortened version of McGill Pain Questionnaire (SF-MPQ. Student's t test was used for statistical analysis. Results The maximum and minimum pain severities were observed at 2 and 24 hours in both groups. The severity of sensual pain at 8, 12, and 24 hours was non-significantly less in the heat Patch group. There was also no significant difference between the groups regarding the emotional impact of pain at the first 2, 4, 8, 12 and 12 hours of menstruation. Conclusions Heat patch containing Iron chip has comparable analgesic effects to ibuprofen and can possibly be used for primary dysmenorrhea. Trial registration IRCT201107187038N2

  9. Ibuprofen and/or paracetamol (acetaminophen) for pain relief after surgical removal of lower wisdom teeth, a Cochrane systematic review.

    Science.gov (United States)

    Bailey, E; Worthington, H; Coulthard, P

    2014-04-01

    This paper compares the beneficial and harmful effects of paracetamol, ibuprofen and the novel combination of both in a single tablet for pain relief following the surgical removal of lower wisdom teeth. In this systematic review only randomised controlled double-blinded clinical trials were included. We calculated the proportion of patients with at least 50% pain relief at 2 and 6 hours post dosing, along with the proportion of participants using rescue medication at 6 and 8 hours. Adverse events were also analysed. Data was meta-analysed where possible. Seven studies were included with a total of 2,241 participants enrolled. Ibuprofen 400 mg is superior to 1,000 mg paracetamol with a risk ratio for at least 50% pain relief at 6 hours of 1.47 (95% confidence interval [CI] 1.28 to 1.69). For the combined drug, the risk ratio for at least 50% maximum pain relief over 6 hours is 1.77 (95% CI 1.32 to 2.39) based on total pain relief (TOTPAR) data. There is high quality evidence that ibuprofen is superior to paracetamol. The novel combination drug shows encouraging results when compared to the single drugs (based on two trials).

  10. Histological Study of the Effects of Ibuprofen on Acute Apical Inflammation Following Root Canal Therapy in Cats

    Directory of Open Access Journals (Sweden)

    Ghoddusi J

    2000-05-01

    Full Text Available Postoperative pain following Root Canal Therapy (RCT is the common problem for patients,"ndentist and dental staff. Regardless of cause it appears that postoperative pain and discomfort is related to"nperiapical inflammation. The purpose of this study was to investigate histologically the effect of"nIbuprofen on acute apical inflammation following RCT. on cat. Fifty-six cuspids teeth of 14 cats were"ndivided into three groups, 6 cats for experimental group, 6 cats for positive control group and 2 cats for"nnegative control group. In first group, to anesthesize the animals each cat received 10 mg/kg Ibuprofen"n36 hours before RCT and repeated every 24 hours. In second group RCT was performed in 24 cat teeth"nwithout any prescription. In negative control groups 2 cats, no RCT were done."nFollowing vital perfusion, in interval of 6, 12, 24 hours, samples were post fixed in 10% formalin and"nfive micron sections were prepared, and stained with H&E and studied under the Mann Whitney"nparameter test. Infilteration of inflamatory cells in 6 hours interval in experimental group was"nsignificantly less than two control groups. In 12 hours samples, however, inflammation in experimental"ngroup reduced, but it was not significant. In 24 hours samples there was no significant difference"nbetween experimental groups and controls. The result of this in-vivo study shows prescription of"nIbuprofen before root canal therapy can reduce inflammatory reaction.

  11. Comparison of paracetamol, ibuprofen, and diclofenac potassium for pain relief following dental extractions and deep cavity preparations

    Directory of Open Access Journals (Sweden)

    Giath Gazal

    2017-03-01

    Full Text Available Objectives: To compare the effectiveness of different oral analgesics for relieving pain and distress in adults following the extraction of teeth and deep cavity preparations under local anesthesia. Methods: This randomized controlled study was conducted between November 2015 and May 2016. One hundred and twenty patients were randomly allocated to 3 groups. Forty patients were in the paracetamol (1 gram group, 40 in the ibuprofen (400 mg group and 40 in the diclofenac potassium (50 mg group. Evaluation of the post extraction and deep cavity preparations pain was made by patients immediately postoperatively, 2, 4 and 6 hours postoperatively on standard 100 mm visual analogue scales (VAS. Furthermore, each patient was observed preoperatively and immediately postoperatively for signs of distress by using a 5 point face scale. Results: There were significant decreases in mean pain VAS scores for diclofenac potassium group compared to paracetamol and ibuprofen groups at 4 hours postoperatively (one-way Analysis of Variance: p=0.0001, p=0.001 and 6 hours postoperatively (p=0.04, p=0.005. Changes in distress scores from the preoperative score to the postoperative score were made using the paired sample t-test. There were significant decreases in distress scores between the preoperative and postoperative scores (p=0.0001. Conclusions: Diclofenac potassium was more effective than paracetamol or ibuprofen for reducing postoperative pain associated with tooth extraction and deep cavity preparation. Patients’ distress levels can be alleviated by using preemptive analgesics.

  12. Correlation of ibuprofen bioavailability with gastrointestinal transit by scintigraphic monitoring of 171Er-labeled sustained-release tablets

    International Nuclear Information System (INIS)

    Parr, A.F.; Beihn, R.M.; Franz, R.M.; Szpunar, G.J.; Jay, M.

    1987-01-01

    External gamma scintigraphy was used to monitor the gastrointestinal (GI) transit of radiolabeled sustained-release tablets containing 800 mg ibuprofen in eight fasted healthy volunteers. Ibuprofen serum concentrations were determined from blood samples drawn sequentially over a 24-hr period. Serum concentrations and related parameters were correlated to the position of the dosage form in the GI tract from the scintiphotos. The sustained-release tablets were radiolabeled intact utilizing a neutron activation procedure, by incorporating 0.18% of 170 Er2O3 (enriched to greater than 96% 170 Er) into the bulk formulation. After manufacture of the final dosage forms, the tablets were irradiated in a neutron flux (4.4 x 10(13) n/cm2.sec) for 2 min, converting the stable 170 Er to radioactive 171 Er (t1/2 = 7.5 hr). Each tablet contained 50 microCi of 171 Er at the time of administration. The scintigraphy studies suggested that the greatest proportion of ibuprofen was absorbed from this dosage form while the tablet was in the large bowel. The dosage forms eroded slowly in the small bowel and appeared to lose their integrity in the large bowel. In vitro studies showed only minimal effects of the neutron irradiation procedure on the dosage form performance

  13. Medication possession ratio predicts antiretroviral regimens persistence in Peru.

    Science.gov (United States)

    Salinas, Jorge L; Alave, Jorge L; Westfall, Andrew O; Paz, Jorge; Moran, Fiorella; Carbajal-Gonzalez, Danny; Callacondo, David; Avalos, Odalie; Rodriguez, Martin; Gotuzzo, Eduardo; Echevarria, Juan; Willig, James H

    2013-01-01

    In developing nations, the use of operational parameters (OPs) in the prediction of clinical care represents a missed opportunity to enhance the care process. We modeled the impact of multiple measurements of antiretroviral treatment (ART) adherence on antiretroviral treatment outcomes in Peru. Retrospective cohort study including ART naïve, non-pregnant, adults initiating therapy at Hospital Nacional Cayetano Heredia, Lima-Peru (2006-2010). Three OPs were defined: 1) Medication possession ratio (MPR): days with antiretrovirals dispensed/days on first-line therapy; 2) Laboratory monitory constancy (LMC): proportion of 6 months intervals with ≥1 viral load or CD4 reported; 3) Clinic visit constancy (CVC): proportion of 6 months intervals with ≥1 clinic visit. Three multi-variable Cox proportional hazard (PH) models (one per OP) were fit for (1) time of first-line ART persistence and (2) time to second-line virologic failure. All models were adjusted for socio-demographic, clinical and laboratory variables. 856 patients were included in first-line persistence analyses, median age was 35.6 years [29.4-42.9] and most were male (624; 73%). In multivariable PH models, MPR (per 10% increase HR=0.66; 95%CI=0.61-0.71) and LMC (per 10% increase 0.83; 0.71-0.96) were associated with prolonged time on first-line therapies. Among 79 individuals included in time to second-line virologic failure analyses, MPR was the only OP independently associated with prolonged time to second-line virologic failure (per 10% increase 0.88; 0.77-0.99). The capture and utilization of program level parameters such as MPR can provide valuable insight into patient-level treatment outcomes.

  14. A questionnaire based survey study for the evaluation of knowledge of Pakistani University teachers regarding their awareness about ibuprofen as an over the counter analgesic.

    Science.gov (United States)

    Chen, Jianxian; Murtaza, Ghulam; Nadeem, Nida; Shao, Xiaokuai; Siddiqi, Bushra G; Shafique, Zainab; Ahmad, Saeed; Amjad, Seyyeda T; Haroon, Saima; Tanoli, Mamoona; Zhou, Mei

    2014-01-01

    In recent time, due to convenient availability of number of over the counter (OTC) drugs, patients are able to treat minor ailments by themselves. The self-medicated regimen has lead to certain health problems in all age groups irrespective of their professions. People are usually unaware about the safe use of NSAIDs (non-steroidal anti-inflammatory drugs) and currently there is no study carried out in COMSATS Institute of Information Technology (CIIT), Abbottabad, regarding the choice of faculty members for NSAIDs to relieve pain and their knowledge about its safety and use. A questionnaire based survey was carried out to collectdata about the choice of CIIT faculty for a specific NSAID and their cognition related to ibuprofen. Two hundred fifty faculty members (comprising of 53 pharmacy faculty members and 197 faculty members who belonged to other departments) of which 87 were females, took part in this study. Average age of participants was 34.86 +/- 9.02 years. Ibuprofen was the drug of choice NSAID among the participants. Four percent participants experienced pain almost every day. Analgesia was the well known indication for ibuprofen (31%) by both the groups and in general more educated and younger participants showed better apprehension related to indications. Sixty one percent participants comprising of non-pharmacy faculty were unaware of any undesirable effects and 79% (comprising of 72% pharmacists and 5% non-pharmacists) were affirmative that ibuprofen had no adverse effects. Fifteen percent participants of department other than pharmacy were not aware of any interactions of ibuprofen. 34% of participants (comprising of 32% non-pharmacists and 2% pharmacists) entrusted their physician for an analgesic. Regardless that many participants suffered from pain almost every day and their drug of choice would be ibuprofen, they had inadequate information related to the safety and use of ibuprofen.

  15. Celecoxib and Ibuprofen Restore the ATP Content and the Gluconeogenesis Activity in the Liver of Walker-256 Tumor-Bearing Rats

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    Camila Oliveira de Souza

    2015-07-01

    Full Text Available Background/Aims: The main purpose of this study was to investigate the effects of celecoxib and ibuprofen, both non-steroidal anti-inflammatory drugs (NSAIDs, on the decreased gluconeogenesis observed in liver of Walker-256 tumor-bearing rats. Methods: Celecoxib and ibuprofen (both at 25 mg/Kg were orally administered for 12 days, beginning on the same day when the rats were inoculated with Walker-256 tumor cells. Results: Celecoxib and ibuprofen treatment reversed the reduced production of glucose, pyruvate, lactate and urea from alanine as well as the reduced production of glucose from pyruvate and lactate in perfused liver from tumor-bearing rats. Besides, celecoxib and ibuprofen treatment restored the decreased ATP content, increased triacylglycerol levels and reduced mRNA expression of carnitine palmitoyl transferase 1 (CPT1, while ibuprofen treatment restored the reduced mRNA expression of peroxisome proliferator-activated receptor alpha (PPARα in the liver of tumor-bearing rats. Both treatments tended to decrease TNFα, IL6 and IL10 in the liver of tumor-bearing rats. Finally, the treatment with celecoxib, but not with ibuprofen, reduced the growth of Walker-256 tumor. Conclusion: Celecoxib and ibuprofen restored the decreased gluconeogenesis in the liver of Walker-256 tumor-bearing rats. These effects did not involve changes in tumor growth and probably occurred by anti-inflammatory properties of these NSAIDs, which increased expression of genes associated with fatty acid oxidation (PPARα and CPT1 and consequently the ATP production, normalizing the energy status in the liver of tumor-bearing rats.

  16. Enantioselective skin permeation of ibuprofen enantiomers: mechanistic insights from ATR-FTIR and CLSM studies based on synthetic enantiomers as naphthalimide fluorescent probes.

    Science.gov (United States)

    Che, Qi-en; Quan, Peng; Mu, Mao; Zhang, Xinfu; Zhao, Hanqing; Zhang, Yu; You, Song; Xiao, Yi; Fang, Liang

    2014-10-01

    The aim of this study was to investigate the mechanisms of different skin permeability of ibuprofen racemate and enantiomers. The percutaneous permeation of ibuprofen racemate and enantiomers through rabbit normal skin and damaged skin (without stratum corneum [SC]) was investigated in vitro using side-by-side diffusion cells. With the melting temperature-membrane transport model, the flux ratio of enantiomer/racemate was calculated from their thermodynamic properties obtained by differential scanning calorimetry. Attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) study was performed to evaluate the interaction between the enantiomers and the SC. New fluorescent probes were designed and utilized in confocal laser scanning microscopy (CLSM) study for visualization of the enantioselective permeation of the enantiomers through the intact rabbit skin. The flux of (S)-ibuprofen through normal skin was significantly higher than that of (RS)-ibuprofen and (R)-ibuprofen (p skin, there was no significant difference (p > 0.05). The predicted flux ratio of (S)-ibuprofen/(RS)-ibuprofen (2.50) was in close agreement with the experimentally determined ratio (2.48). These results were supported by ATR-FTIR and CLSM studies that indicated that a chiral environment of the skin led to the enantioselective permeation of enantiomers. The chiral nature of the SC and the different physicochemical properties of the enantiomers should be taken into account in the assessment of different skin permeability of the racemate and enantiomers. The synthetic fluorescent probes used in this study could visualize the enantioselective permeation of the chiral compounds across the skin.

  17. Treatment with acetaminophen/paracetamol or ibuprofen alleviates post-dose symptoms related to intravenous infusion with zoledronic acid 5 mg.

    Science.gov (United States)

    Wark, J D; Bensen, W; Recknor, C; Ryabitseva, O; Chiodo, J; Mesenbrink, P; de Villiers, T J

    2012-02-01

    Patients treated with intravenous zoledronic acid 5 mg for osteoporosis may experience post-dose influenza-like symptoms. Oral acetaminophen/paracetamol or ibuprofen administered 4 h post-infusion reduced the proportion of patients with increased oral temperature and worsening post-infusion symptom scores vs. placebo, thus providing an effective strategy for the treatment of such symptoms. Once-yearly intravenous zoledronic acid 5 mg is a safe and effective treatment for postmenopausal osteoporosis. This study assessed whether transient influenza-like post-dose symptoms associated with intravenous infusion of zoledronic acid can be reduced by post-dose administration of acetaminophen/paracetamol or ibuprofen. In an international, multicenter, randomized, double-blind, double-dummy parallel-group study, bisphosphonate-naïve postmenopausal women with osteopenia (n = 481) were randomized to receive zoledronic acid 5 mg + acetaminophen/paracetamol (n = 135), ibuprofen (n = 137) or placebo (n = 137), or placebo + placebo (n = 72). Acetaminophen/paracetamol and ibuprofen were administered every 6 h for 3 days beginning 4 h post-infusion. The proportion of patients with increased oral temperature (≥1°C above 37.5°C) and with worsening post-infusion symptom scores over 3 days was significantly lower in patients receiving ibuprofen (36.8% and 48.5%) or acetaminophen/paracetamol (37.3% and 46.3%) vs. those receiving placebo (63.5% and 75.9%, respectively; all p paracetamol or ibuprofen. Oral acetaminophen/paracetamol or ibuprofen effectively managed the transient influenza-like symptoms associated with zoledronic acid 5 mg.

  18. Effects of low-dose ibuprofen supplementation and resistance training on bone and muscle in postmenopausal women: A randomized controlled trial

    Directory of Open Access Journals (Sweden)

    Whitney R.D. Duff

    2016-12-01

    Full Text Available Purpose: To compare the effects of nine months of exercise training and ibuprofen supplementation (given immeditately after exercise sessions on bone and muscle in postmenopausal women. Methods: In a double-blind randomized trial, participants (females: n = 90, mean age 64.8, SD 4.3 years were assigned (computer generated, double blind to receive supervised resistance training or stretching 3 days/week, and ibuprofen (400 mg, post-exercise or placebo (i.e. 4 groups for 9 months. In this proof-of-concept study the sample size was halved from required 200 identified via 90% power calculation. Baseline and post-intervention testing included: Dual energy x-ray absorptiometry (DXA for lumbar spine, femoral neck, and total body areal bone mineral density (aBMD; geometry of proximal femur; total body lean tissue and fat mass; predicted 1-repetition maximum muscle strength testing (1RM; biceps curl, hack squat. Results: Exercise training or ibuprofen supplementation had no effects on aBMD of the lumbar spine, femoral neck, and total body. There was a significant exercise × supplement × time interaction for aBMD of Ward's region of the femoral neck (p = 0.015 with post hoc comparison showing a 6% decrease for stretching with placebo vs. a 3% increase for stretching with ibuprofen (p = 0.017. Resistance training increased biceps curl and hack squat strength vs. stretching (22% vs. 4% and 114% vs. 12%, respectively (p < 0.01 and decreased percent body fat compared to stretching (2% vs. 0% (p < 0.05. Conclusions: Ibuprofen supplementation provided some benefits to bone when taken independent of exercise training in postmenopausal women. This study provides evidence towards a novel, easily accessible stimulus for enhancing bone health [i.e. ibuprofen]. Keywords: Aging, Osteoporosis, Sarcopenia, Ibuprofen

  19. Association of High-Dose Ibuprofen Use, Lung Function Decline, and Long-Term Survival in Children with Cystic Fibrosis.

    Science.gov (United States)

    Konstan, Michael W; VanDevanter, Donald R; Sawicki, Gregory S; Pasta, David J; Foreman, Aimee J; Neiman, Evgueni A; Morgan, Wayne J

    2018-04-01

    Cystic fibrosis deaths result primarily from lung function loss, so chronic respiratory therapies, intended to preserve lung function, are cornerstones of cystic fibrosis care. Although treatment-associated reduction in rate of lung function loss should ultimately improve cystic fibrosis survival, no such relationship has been described for any chronic cystic fibrosis therapy. In part, this is because the ages of most rapid lung function decline-early adolescence-precede the median age of cystic fibrosis deaths by more than a decade. To study associations of high-dose ibuprofen treatment with the rate of forced expiratory volume in 1 second decline and mortality among children followed in the Epidemiologic Study of Cystic Fibrosis and subsequently in the U.S. Cystic Fibrosis Foundation Patient Registry. We performed a matched cohort study using data from Epidemiologic Study of Cystic Fibrosis. Exposure was defined as high-dose ibuprofen use reported at ≥80% of encounters over 2 years. Unexposed children were matched to exposed children 5:1 using propensity scores on the basis of demographic, clinical, and treatment covariates. The rate of decline of percent predicted forced expiratory volume in 1 second during the 2-year follow-up period was estimated by mixed-effects modeling with random slopes and intercepts. Survival over 16 follow-up years in the U.S. Cystic Fibrosis Foundation Patient Registry was compared between treatment groups by using proportional hazards modeling controlling for matching and covariates. We included 775 high-dose ibuprofen users and 3,665 nonusers who were well matched on demographic, clinical, and treatment variables. High-dose ibuprofen users declined on average 1.10 percent predicted forced expiratory volume in 1 second/yr (95% confidence interval; 0.51, 1.69) during the 2-year treatment period, whereas nonusers declined at a rate of 1.76% percent predicted forced expiratory volume in 1 second/yr (95% confidence interval; 1.48, 2

  20. An upper and lower bound of the Medication Possession Ratio

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    Sperber CM

    2017-08-01

    Full Text Available Christian M Sperber, Suren R Samarasinghe, Grace P Lomax Patient Connect Limited, Guildford, UK Background: The Medication Possession Ratio (MPR is a ubiquitous and central measurement for adherence in the health care industry. However, attempts to standardize its calculation have failed, possibly due to the opacity of a single, static MPR, incapability of directly lending itself to a variety of studies, and challenges of comparing the value across studies. This work shows that the MPR strictly depends on the length of the time interval over which it is measured as well as on the dominant dispense quantity for short time intervals. Furthermore, removing a proportion of the patient cohort based on the number of acquisitions may also have a severe impact on the MPR. Therefore, it is suggested that the MPR is represented as a trend over a range of time intervals. To this end, an upper and lower bound of the MPR trend is developed with an upper bound acknowledging patients who change their treatment and the lower bound acknowledging patients who discontinue their treatment.Purpose: Introducing a representation of the MPR value as a trend rather than a static number by developing a quantitative description of an upper and lower bound of the MPR trend, while shedding light on the impacts on prefiltering the patient cohort.Patients and methods: Anonymized patient-level data was utilized as an example for a suggested calculation of an upper and lower bound of the MPR.Results: Representation of the MPR for a predefined time interval precludes a reliable MPR assessment. A quantitative approach is suggested to generate an upper and lower trend of the MPR while emphasizing the impact on removing patients with a limited number of acquisitions.Conclusion: An upper and lower trend makes the MPR more transparent and allows a better comparison across different studies. Removing patients with a limited number of acquisitions should be avoided. Keywords: MPR

  1. Are symptoms of spirit possessed patients covered by the DSM-IV or DSM-5 criteria for possession trance disorder? A mixed-method explorative study in Uganda

    NARCIS (Netherlands)

    van Duijl, M.; Kleyn, W.; de Jong, J.

    2013-01-01

    Introduction and aims As in many cultures, spirit possession is a common idiom of distress in Uganda. The DSM-IV contains experimental research criteria for dissociative and possession trance disorder (DTD and PTD), which are under review for the DSM-5. In the current proposed categories of the

  2. The Secret Prover : Proving Possession of Arbitrary Files While not Giving Them Away

    NARCIS (Netherlands)

    Teepe, Wouter

    2005-01-01

    The Secret Prover is a Java application which allows a user (A) to prove to another user (B), that A possesses a file. If B also possesses this file B will get convinced, and if B does not possess this file B will gain no information on (the contents of) this file. This is the first implementation

  3. Building a polysaccharide hydrogel capsule delivery system for control release of ibuprofen.

    Science.gov (United States)

    Chen, Zhi; Wang, Ting; Yan, Qing

    2018-02-01

    Development of a delivery system which can effectively carry hydrophobic drugs and have pH response is becoming necessary. Here we demonstrate that through preparation of β-cyclodextrin polymer (β-CDP), a hydrophobic drug molecule of ibuprofen (IBU) was incorporated into our prepared β-CDP inner cavities, aiming to improve the poor water solubility of IBU. A core-shell capsule structure has been designed for achieving the drug pH targeted and sustained release. This delivery system was built with polysaccharide polymer of Sodium alginate (SA), sodium carboxymethylcellulose (CMC) and hydroxyethyl cellulose (HEC) by physical cross-linking. The drug pH-response control release is this hydrogel system's chief merit, which has potential value for synthesizing enteric capsule. Besides, due to our simple preparing strategy, optimal conditions can be readily determined and the synthesis process can be accurately controlled, leading to consistent and reproducible hydrogel capsules. In addition, phase-solubility method was used to investigate the solubilization effect of IBU by β-CDP. SEM was used to prove the forming of core and shell structure. FT-IR and 1 H-NMR were also used to perform structural characteristics. By the technique of UV determination, the pH targeted and sustained release study were also performed. The results have proved that our prepared polysaccharide hydrogel capsule delivery system has potential applications as oral drugs delivery in the field of biomedical materials.

  4. Deposition of Ibuprofen Crystals on Hydroxypropyl Cellulose/Polyacrylamide Gel: Experimental and Mathematic Modeling Releasing

    Directory of Open Access Journals (Sweden)

    Claudia Alicia Castillo-Miranda

    2016-01-01

    Full Text Available The crystallization of nonsteroidal anti-inflammatory drug [2-(4-isobutyl-phenyl propionic acid] ibuprofen (IBP on a hydroxypropyl cellulose (HPC and polyacrylamide (PAAm gel was studied as well as the release kinetics of the drug. The IBP was crystallized on the gel surface of HPC/PAAm. It had a prismatic shape and the growth was made in an aqueous medium; the crystallinity grade of the gels HPC/PAAm and HPC/PAAm-IBU increased to 68% and to 58%, respectively. The release of IBP is performed by two means: by a non-Fickian diffusion process and by relaxation of the chains of the gel; without regard to temperature and the diffusion media, this correlates with the lower critical solution temperature (LCST of the proposed gel. This polymer matrix provides an option for releasing nonsteroidal anti-inflammatory drugs in a temperature range of 35–39°C. Korsmeyer and Peppas mathematical model was simulated for data releases, statistically significant at 95% confidence level.

  5. An Acute Ibuprofen Overdose Masking a Severe Staphylococcus aureus Meningitis: A Case Report

    Directory of Open Access Journals (Sweden)

    Matthew Smetana

    2013-01-01

    Full Text Available Acute bacterial meningitis has a low incidence (3/100,000 in the United States and yet high fatality rate (approximately 14–16% and classically presents as a triad of fever, neck stiffness, and altered mental status. However, less than half of patients with meningitis present with this classic triad. We present the clinical course of a patient who initially presented to the emergency department after overdosing on ibuprofen for what he described as back pain secondary to mechanical injury. However, the patient's condition quickly deteriorated: he developed tachycardia, mental status changes, was intubated due to respiratory distress, and then suffered an 8-minute PEA arrest before return of spontaneous circulation was achieved. After the patient was stabilized, in addition to the nonsteroidal anti-inflammatory drug (NSAID overdose Staphylococcus aureus meningitis, bacteremia, and pneumonia were diagnosed. We report this case to illustrate that the initial presentation of meningitis may be extremely unusual especially in the setting of NSAID overdose and the acutely decompensating patient. As the risk of adverse clinical outcomes increases with delays in appropriate antibiotic therapy, it is therefore crucial to recognize the many signs and symptoms of meningitis, typical and atypical, and quickly begin appropriate treatment.

  6. Ibuprofen removal in horizontal subsurface flow constructed wetlands: treatment performance and fungal community dynamics.

    Science.gov (United States)

    Zhang, Dongqing; Luo, Jinxue; Lee, Zarraz May Ping; Gersberg, Richard M; Liu, Yu; Tan, Soon Keat; Ng, Wun Jern

    2016-01-01

    The treatment performance of ibuprofen (IBP)-enriched wastewater by horizontal subsurface flow constructed wetlands planted with cattail (Typha angustifolia) and unplanted control mesocosms was investigated. Removal efficiencies of IBP were significantly (p fungal community in these wetland systems. The overall diversity of the fungal community was reduced under the IBP exposure. Taxonomic analysis revealed that 62.2% of the fungal sequences were affiliated with Basidiomycota, followed by Ascomycota (37.4%) at the phylum level. Uncultured fungus (48.2%), Chaetomium sp. (14.2%), Aspergillus sp. (12.4%), Trichoderma sp. (5.7%), Cladosporium sp. (5.4%), and Emericellopsis sp. (5.2%) were identified as dominant genera. At the genus level, a distinct profile of the fungal community in the IBP-enriched mesocosms was observed as compared to the control beds, and as well specific fungal genera were enhanced in the planted beds, regardless of IBP enrichment. However, despite these differences, the composition of the fungal community (as measured by Bray-Curtis similarity) was mostly unaffected by the significant IBP enrichment. On the other hand, a consistent similarity pattern of fungal community structure in the planted mesocosms suggests that the presence of higher macrophytes in the wetland systems may well help shape the fungal community structure.

  7. Effects of Polymeric Additives on the Crystallization and Release Behavior of Amorphous Ibuprofen

    Directory of Open Access Journals (Sweden)

    Su Yang Lee

    2013-01-01

    Full Text Available Some polymeric additives were studied to understand their effects on the amorphous phase of ibuprofen (IBU, used as a poorly water soluble pharmaceutical model compound. The amorphous IBU in bulk, as well as in nanopores (diameter ~24 nm of anodic aluminum oxide, was examined with the addition of poly(acrylic acid, poly(N-vinyl pyrrolidone, or poly(4-vinylphenol. Results of bulk crystallization showed that they were effective in limiting the crystal growth, while the nucleation of the crystalline phase in contact with water was nearly instantaneous in all cases. Poly(N-vinyl pyrrolidone, the most effective additive, was in specific interaction with IBU, as revealed by IR spectroscopy. The addition of the polymers was combined with the nanoscopic confinement to further stabilize the amorphous phase. Still, the IBU with addition of polymeric additives showed sustained release behavior. The current study suggested that the inhibition of the crystal nucleation was probably the most important factor to stabilize the amorphous phase and fully harness its high solubility.

  8. Dynamics and interactions of ibuprofen in cyclodextrin nanosponges by solid-state NMR spectroscopy

    Directory of Open Access Journals (Sweden)

    Monica Ferro

    2017-01-01

    Full Text Available Two different formulations of cyclodextrin nanosponges (CDNS, obtained by polycondensation of β-cyclodextrin with ethylenediaminetetraacetic acid dianhydride (EDTAn, were treated with aqueous solutions of ibuprofen sodium salt (IbuNa affording hydrogels that, after lyophilisation, gave two solid CDNS-drug formulations. 1H fast MAS NMR and 13C CP-MAS NMR spectra showed that IbuNa was converted in situ into its acidic and dimeric form (IbuH after freeze-drying. 13C CP-MAS NMR spectra also indicated that the structure of the nanosponge did not undergo changes upon drug loading compared to the unloaded system. However, the 13C NMR spectra collected under variable contact time cross-polarization (VCT-CP conditions showed that the polymeric scaffold CDNS changed significantly its dynamic regime on passing from the empty CDNS to the drug-loaded CDNS, thus showing that the drug encapsulation can be seen as the formation of a real supramolecular aggregate rather than a conglomerate of two solid components. Finally, the structural features obtained from the different solid-state NMR approaches reported matched the information from powder X-ray diffraction profiles.

  9. Does platelet mass influence the effectiveness of ibuprofen treatment for patent ductus arteriosus in preterm infants?

    Science.gov (United States)

    Akar, Selahattin; Karadag, Nilgun; Gokmen Yildirim, Tulin; Toptan, Handan Hakyemez; Dincer, Emre; Tuten, Abdulhamit; Yavuz, Taner; Topcuoglu, Sevilay; Karatepe, Hande Ozgun; Ozalkaya, Elif; Karatekin, Guner; Ovali, Fahri

    2016-12-01

    The aim of this study is to evaluate whether the platelet mass in the first 24 h of life is effective on closure of patent ductus arteriosus (PDA) or not. Preterm infants with a gestational age of gender and maternal risk factors between the study groups. The mean platelet count in the first postnatal blood count was in Group 1: 211.3 ± 89.2 × 10(3)/mm(3) and in Group 2: 216.5 ± 26 × 10(3)/mm(3), respectively (p = 0.783). The mean platelet volumes (MPV) were similar in both groups (p = 0.535). No statistically significant difference between platelet mass values was detected (Group 1: 1811 ± 884 fl/nl, Group 2: 1868 ± 717 fl/nl) (p = 0.753). Our data suggest that platelet count, MPV and platelet mass did not affect the closure of hsPDA with ibuprofen.

  10. Application of nanofiltration for the removal of carbamazepine, diclofenac and ibuprofen from drinking water sources.

    Science.gov (United States)

    Vergili, I

    2013-09-30

    Pharmaceutical active compounds (PhACs) are persistent during the process used to treat drinking water and, because drinking water treatment plants are not specifically designed to remove PhACs, these compounds are found in drinking water. Although there are currently no regulations or drinking water directives for PhACs, precautionary principles suggest ensuring maximal removal of PhACs through improved or existing treatment techniques. This study was designed to investigate the performance of a nanofiltration membrane in cross-flow filtration equipment for the removal of three PhACs [carbamazepine (CBZ), diclofenac (DIC) and ibuprofen (IBU)] that were spiked in water taken from a drinking water treatment plant using surface water. Because of their low solubilities, high log Kow values, low dipole moments and negative charges, higher rejection values were obtained for DIC and IBU. Low to moderate rejection values were most likely due to the small molecular sizes of the PhACs (i.e., MW water. Flux declines obtained from DIC studies was attributed to the adsorption of DIC ions inside the membrane pores, which decreases the flux. The most evident change in the FT-IR spectrum after nanofiltration was the appearance of new intense bands at 1072 cm(-1) and 1011 cm(-1), indicating the deposition of calcium salts on the membrane surface. Copyright © 2013 Elsevier Ltd. All rights reserved.

  11. Electrochemical degradation of Ibuprofen on Ti/Pt/PbO2 and Si/BDD electrodes

    International Nuclear Information System (INIS)

    Ciriaco, L.; Anjo, C.; Correia, J.; Pacheco, M.J.; Lopes, A.

    2009-01-01

    The electrochemical oxidation of Ibuprofen (Ibu) was performed using a Ti/Pt/PbO 2 electrode as the anode, prepared according to literature, and a boron doped diamond (BDD) electrode, commercially available at Adamant Technologies. Tests were performed with model solutions of Ibu, with concentrations ranging from 0.22 to 1.75 mM for the Ti/Pt/PbO 2 electrode and 1.75 mM for the BDD electrode, using 0.035 M Na 2 SO 4 as the electrolyte, in a batch cell, at different current densities (10, 20 and 30 mA cm -2 ). Absorbance measurements, Chemical Oxygen Demand (COD) and Total Organic Carbon (TOC) tests were conducted for all samples. The results have shown a very good degradation of Ibu, with COD removals between 60 and 95% and TOC removals varying from 48 to 92%, in 6 h experiments, with higher values obtained with the BDD electrode. General Current Efficiency and Mineralization Current Efficiency, determined for both electrodes, show a similar behaviour for 20 mA cm -2 but a very different one at 30 mA cm -2 . The combustion efficiency was also determined for both anodes, and found to be slightly higher with BDD at lower current density and equal to 100% for both anodes at 30 mA cm -2

  12. Nuclear magnetic resonance study of naproxen and ibuprofen interaction with β - cyclodextrin in solution

    International Nuclear Information System (INIS)

    Bogdan, M.; Farcas, S.I.; Bojita, M.

    1999-01-01

    Modern biomedical research leads to revealing insights into the molecular activity of many therapeutic molecules. An interesting activity at the organ or cellular level, however, is not sufficient to turn a molecule into an usable drug. Problems such as limited solubility or stability can make impossible to transpose interesting in vitro properties of an experimental compound to an in vivo situation. Various physico - chemical methods have been used to improve aqueous solubility of poorly soluble drugs and to increase the life of unstable drugs, such as adjustment of pH of the aqueous solution, the complexation of drugs with various cyclodextrins and the formation of gels or emulsions. In this paper, we report a 1 H NMR study of the complex formed between naproxen and ibuprofen with β - cyclodextrin in aqueous medium. Our results confirm that inclusion occurs. Analysis of our data by the continuous variation method shows that the complexes have 1 : 1 stoichiometry. The association constants for the 1 : 1 complexes were calculated at different temperatures by non - linear least squares regression analysis of the observed changes in the chemical shifts of the drugs and β - cyclodextrin 1 H NMR lines as a function of β - cyclodextrin concentration. Thermodynamic parameters were obtained by using the temperature dependence of the association constants. Finally, based on the experimentally obtained data, the most probable structure of the investigated complexes is discussed. (authors)

  13. Gene transcription and biomarker responses in the clam Ruditapes philippinarum after exposure to ibuprofen

    International Nuclear Information System (INIS)

    Milan, Massimo; Pauletto, Marianna; Patarnello, Tomaso; Bargelloni, Luca; Marin, Maria Gabriella; Matozzo, Valerio

    2013-01-01

    Pharmaceuticals are a class of emerging environmental contaminants that continuously enter aquatic environments. Presently, little information is available about the effects of these substances on non-target organisms, such as bivalves. We investigated the effects of ibuprofen (IBU) on the clam Ruditapes philippinarum. Clams were exposed for 1, 3, 5 and 7 days to 0, 100 and 1000 μg IBU/L, and established biomarker responses (haemolymph lysozyme, gill acetylcholinesterase and digestive gland superoxide dismutase activities) as well as digestive gland transcriptome were evaluated. A two-way ANOVA revealed significant effects of both “IBU concentration” and “exposure duration” on biomarker responses. Overall, the enzyme activities were generally lower in IBU-exposed clams than in controls. Although limited knowledge of the mollusc transcriptome makes it difficult to interpret the effects of IBU on clams, the gene transcription analysis using DNA microarrays enabled the identification of the putative molecular mode of action of the IBU. The functional analysis of differentially transcribed genes suggests that IBU can interfere with various signalling pathways in clams, such as arachidonic acid metabolism, apoptosis, peroxisomal proliferator-activated receptors, and nuclear factor-kappa B. In addition, several genes involved in the metabolism of xenobiotics (e.g., glutathione S-transferase, sulfotransferase, cytochrome P450) were also found to be significantly affected by IBU exposure. In summary, the integrated approach of gene transcription analysis and biomarker responses facilitated the elucidation of the putative mechanisms of action of IBU in non-target species.

  14. Growth, physiological response and phytoremoval capability of two willow clones exposed to ibuprofen under hydroponic culture.

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    Iori, Valentina; Zacchini, Massimo; Pietrini, Fabrizio

    2013-11-15

    Ibuprofen (IBU) is one of the most widespread pharmaceuticals in the aquatic ecosystem, despite the high removal rate that occurs in wastewater treatment plants. Phytoremediation represents a technology to improve the performance of existing wastewater treatment. This study was conducted under hydroponics to evaluate the ability of Salicaceae plants to tolerate and reduce IBU concentration in contaminated water. To this end, we combined growth, physiological and biochemical data to study the effects of different IBU concentrations on two clones of Salix alba L. Data demonstrated that clone SS5 was more tolerant and showed a higher ability to reduce IBU concentration in the solution than clone SP3. The high tolerance to IBU shown by SS5 was likely due to several mechanisms including the capacity to maintain an elevated photosynthetic activity and an efficient antioxidative defence. These results illustrate the remarkable potential of willow to phytoremediate IBU-contaminated waters in natural and constructed wetlands. Copyright © 2013 Elsevier B.V. All rights reserved.

  15. Efficacy and safety of oral paracetamol versus oral ibuprofen for closure of patent ductus arteriosus in preterm infants: a randomized controlled trial.

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    El-Farrash, Rania A; El Shimy, Mohammed S; El-Sakka, Abeer S; Ahmed, Manal G; Abdel-Moez, Dina G

    2018-05-09

    The objective of this study is to evaluate the efficacy and safety of oral paracetamol versus oral ibuprofen in the treatment of hemodynamically significant patent ductus arteriosus (hsPDA) in preterm infants. An interventional randomized case-control study, registered in ClinicalTrials.gov (NCT03265782), was conducted on 60 preterm infants with gestational age ≤34 weeks, postnatal age of 2-7 d and color Doppler echocardiographic evidence of hsPDA. Neonates were randomly assigned to two groups: 30 received oral ibuprofen and 30 received oral paracetamol. With failure of ductal closure, a second course of ibuprofen or paracetamol was given. The included newborns were subjected to detailed history, clinical examination, laboratory investigations that included complete blood count, renal, and liver function tests and echocardiographic evaluation. Oral paracetamol was as effective as ibuprofen for the closure of patent ductus arteriosus (PDA) with one course of treatment (p > .05). Moreover, oral paracetamol was superior to ibuprofen among neonates who needed second course of treatment with significant decrease in end diastolic flow velocity in the left pulmonary artery (0.35 ± 0.09 versus 0.19 ± 0.06, p = .014), right ventricular systolic pressure (40.50 ± 12.91 versus 20.50 ± 0.58, p = .016) and left atrium to aortic root ratio (1.23 ± 0.14 versus 1.07 ± 0.04, p = .046) when compared to ibuprofen group. Furthermore, the mean difference between pre- and post-treatment PDA size was significantly higher in the paracetamol group compared with ibuprofen group after the second course of treatment (1.07 ± 0.32 versus 0.73 ± 0.38, p = .024). Oral paracetamol was comparable with ibuprofen in terms of the rate of non-surgical ductal closure [28 (93.3%) versus 24 (80%), p = .591]. In addition, oral paracetamol was as safe as oral ibuprofen in terms of gastrointestinal perforation or bleeding, necrotizing

  16. Ibuprofen induces reduction of the proliferation-seeking radiotracer 99mTc-(V)DMSA uptake in severe epithelial breast hyperplasia without atypia.

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    Papantoniou, Vassilios; Tsaroucha, Angeliki; Valsamaki, Pipitsa; Tsiouris, Spyridon; Sotiropoulou, Evangelia; Karianos, Theodore; Marinopoulos, Spyridon; Fothiadaki, Athina; Sotiropoulou, Maria; Archontaki, Aikaterini; Syrgiannis, Konstantinos; Dimitrakakis, Konstantinos; Antsaklis, Aris

    2010-10-01

    The purpose of this study was to investigate if ibuprofen intake can influence mammary uptake of the proliferation-seeking radiotracer technetium 99m-pentavalent dimercaptosuccinic acid (99mTc-(V)DMSA) in women with severe epithelial and atypical epithelial breast hyperplasia. Eight patients with histologically confirmed severe epithelial breast hyperplasia with (n  =  4) and without atypia (n  =  4) were submitted prospectively to 99mTc-(V)DMSA scintimammography before and after a 4-week course of 400 mg ibuprofen daily oral intake. Lesion to background ratios 60 minutes postinjection were calculated and compared (t-test) before and after ibuprofen administration. Prior to ibuprofen, the patients with severe epithelial hyperplasia displayed a significantly higher 99mTc-(V)DMSA uptake ratio compared to those with atypical epithelial hyperplasia (2.40 ± 0.32 vs 1.67 ± 0.09, respectively; p  =  .003). They also exhibited a more substantial percent decline in tracer uptake postibuprofen compared to women with atypical epithelial hyperplasia (62.0 ± 7.1 vs 15.0 ± 0.2, respectively; p  =  .001). Ibuprofen induces significant uptake reduction of the proliferation-seeking radiotracer 99mTc-(V)DMSA in severe epithelial breast hyperplasia without atypia. This agent could therefore constitute a potential imaging tool for monitoring chemoprophylaxis effectiveness in women at the early stages of malignant transformation.

  17. Oral paracetamol and/or ibuprofen for treating pain after soft tissue injuries: Single centre double-blind, randomised controlled clinical trial.

    Science.gov (United States)

    Hung, Kevin K C; Graham, Colin A; Lo, Ronson S L; Leung, Yuk Ki; Leung, Ling Yan; Man, S Y; Woo, W K; Cattermole, Giles N; Rainer, Timothy H

    2018-01-01

    Soft tissue injuries commonly present to the emergency department (ED), often with acute pain. They cause significant suffering and morbidity if not adequately treated. Paracetamol and ibuprofen are commonly used analgesics, but it remains unknown if either one or the combination of both is superior for pain control. To investigate the analgesic effect of paracetamol, ibuprofen and the combination of both in the treatment of soft tissue injury in an ED, and the side effect profile of these drugs. Double-blind, double dummy, placebo-controlled randomised controlled trial. 782 adult patients presenting with soft tissue injury without obvious fractures attending the ED of a university hospital in the New Territories of Hong Kong were recruited. Patients were randomised using a random number table into three parallel arms of paracetamol only, ibuprofen only and a combination of paracetamol and ibuprofen in a 1:1:1 ratio. The primary outcome measure was pain score at rest and on activity in the first 2 hours and first 3 days. Data was analysed on an intention to treat basis. There was no statistically significant difference in pain score in the initial two hours between the three groups, and no clinically significant difference in pain score in the first three days. There was no difference in analgesic effects or side effects observed using oral paracetamol, ibuprofen or a combination of both in patients with mild to moderate pain after soft tissue injuries attending the ED. The study is registered with ClinicalTrials.gov (no. NCT00528658).

  18. Ibuprofen abates cypermethrin-induced expression of pro-inflammatory mediators and mitogen-activated protein kinases and averts the nigrostriatal dopaminergic neurodegeneration.

    Science.gov (United States)

    Singh, Ashish; Tripathi, Pratibha; Prakash, Om; Singh, Mahendra Pratap

    2016-12-01

    Cypermethrin induces oxidative stress, microglial activation, inflammation and apoptosis leading to Parkinsonism in rats. While ibuprofen, a non-steroidal anti-inflammatory drug, relieves from inflammation, its efficacy against cypermethrin-induced Parkinsonism has not yet been investigated. The study aimed to explore the protective role of ibuprofen in cypermethrin-induced Parkinsonism, an environmentally relevant model of Parkinson's disease (PD), along with its underlying mechanism. Animals were treated with/without cypermethrin in the presence/absence of ibuprofen. Behavioural, immunohistochemical and biochemical parameters of Parkinsonism and expression of pro-inflammatory and pro-apoptotic proteins along with mitogen-activated protein kinases (MAPKs) were determined. Ibuprofen resisted cypermethrin-induced behavioural impairments, striatal dopamine depletion, oxidative stress in the nigrostriatal tissues and loss of the nigral dopamine producing cells and increase in microglial activation along with atypical expression of pro-inflammatory and apoptotic proteins that include cyclooxygenase-2, tumour necrosis factor-α, MAPKs (c-Jun N-terminal kinase, p38 and extracellular signal-regulated kinase), B cell lymphoma 2-associated protein X, tumour suppressor protein p53, cytochrome c and caspase-3 in the nigrostriatal tissue. The results obtained thus demonstrate that ibuprofen lessens inflammation and regulates MAPKs expression thereby averts cypermethrin-induced Parkinsonism.

  19. LEGAL SIGNIFICANCE AND PROTECTION OF POSSESSION IN THE REPUBLIC OF MACEDONIA

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    Vojo Belovski

    2015-04-01

    Full Text Available In this paper it will be discussed the legal significance and protection of possession in the Republic of Macedonia. Below it will be listed the kinds of possession, and finally the rules for possession termination will be explained. The possession is an indicator that the person who rules one item is also a right holder of that item. The possession itself occurs in two types specially authorized by a law and pure factual power behind which stands no right. The possession enjoys legal protection. Below in the paper it is processed the judicial protection of the possession which is given based on complaint for disturbance of possession and action to recover the possession. The important thing at the judicial protection is that the rulers’ protection is given to the last actual possession of the item, but it is not disputed the right of possession. Further in this paper it is included the protection of indirect possession where a complaint can be made by the indirect holder of the item, the judicial protection of possessory, possession protection of the heirs and permitted self – help for unauthorized harassment and revoking of the possession. With respect to the termination of the actual power of the item, listed and processed are the ways when the item failed, when the item was lost, when it is obvious that it won’t be returned, when the ruler had freely left it and when the item is not taken from him and the ruler hasn’t realized the right to possession.

  20. From distress to disease: a critique of the medicalisation of possession in DSM-5.

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    Padmanabhan, Divya

    2017-12-01

    This paper critiques the category of possession-form dissociative identity disorder as defined in the Diagnostic and Statistical Manual of Mental Disorders 5 (DSM-5) published in 2013 by the American Psychiatric Association (APA). The DSM as an index of psychiatry pathologises possession by categorising it as a form of dissociative identity disorder. Drawing upon ethnographic fieldwork, this paper argues that such a pathologisation medicalises possession, which is understood as a non-pathological condition in other contexts such as by those individuals who manifest possession at a temple in Kerala, South India. Through medicalising and further by creating distinctions between acceptable and pathological possession, the DSM converts a form of distress into a disease. This has both conceptual and pragmatic implications. The temple therefore becomes reduced to a culturally acceptable site for the manifestation of a mental illness in a form that is culturally available and possession is explained solely through a biomedical framework, denying alternative conceptualisations and theories which inform possession. By focussing on the DSM-5 classification of possession and the limitations of such a classification, this paper seeks to posit an alternative conceptualisation of possession by engaging with three primary areas which are significant in the DSM categorisation of possession: the DSM's conceptualisation of self in the singular, the distinction between pathological and non-pathological forms of possession, and the limitations of the DSM's equation of the condition of possession with the manifestation of possession. Finally, the paper briefly highlights alternative conceptualisations of possession, which emerged from the perspective of those seeking to heal possession at the Chottanikkara temple.

  1. Efficacy and safety of Curcuma domestica extracts compared with ibuprofen in patients with knee osteoarthritis: a multicenter study

    Directory of Open Access Journals (Sweden)

    Kuptniratsaikul V

    2014-03-01

    Full Text Available Vilai Kuptniratsaikul,1 Piyapat Dajpratham,1 Wirat Taechaarpornkul,2 Montana Buntragulpoontawee,3 Pranee Lukkanapichonchut,4 Chirawan Chootip,5 Jittima Saengsuwan,6 Kesthamrong Tantayakom,7 Supphalak Laongpech8 1Department of Rehabilitation Medicine, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok, Thailand; 2Sirindhorn National Medical Rehabilitation Center, Ministry of Public Health, Nonthaburi, Thailand; 3Department of Rehabilitation Medicine, Faculty of Medicine, Chiang Mai University, Chiang Mai, Thailand; 4Department of Rehabilitation Medicine, Ratchaburi Hospital, Ministry of Public Health, Ratchaburi, Thailand; 5Department of Rehabilitation Medicine, Songkhla Hospital, Ministry of Public Health, Songkhla, Thailand; 6Department of Rehabilitation Medicine, Faculty of Medicine, Khon Kaen University, Khon Kaen, Thailand; 7Department of Rehabilitation Medicine, Rajvithi Hospital, Ministry of Public Health, Bangkok, Thailand; 8Department of Rehabilitation Medicine, Vachira Phuket Hospital, Ministry of Public Health, Phuket, Thailand Objective: To determine the efficacy and safety of Curcuma domestica extracts in pain reduction and functional improvement. Methods: 367 primary knee osteoarthritis patients with a pain score of 5 or higher were randomized to receive ibuprofen 1,200 mg/day or C. domestica extracts 1,500 mg/day for 4 weeks. The main outcomes were Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC total, WOMAC pain, WOMAC stiffness, and WOMAC function scores. Adverse events (AEs were also recorded. Results: 185 and 182 patients were randomly assigned into C. domestica extracts and ibuprofen groups, respectively. The baseline characteristics were no different between groups. The mean of all WOMAC scores at weeks 0, 2, and 4 showed significant improvement when compared with the baseline in both groups. After using the noninferiority test, the mean difference (95% confidence interval of WOMAC total

  2. Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions.

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    Djekic, Ljiljana; Primorac, Marija; Filipic, Slavica; Agbaba, Danica

    2012-08-20

    The current study investigates the performances of the multicomponent mixtures of nonionic surfactants regarding the microemulsion stabilisation, drug solubilization and in vitro drug release kinetic. The primary surfactant was PEG-8 caprylic/capric glycerides (Labrasol). The cosurfactants were commercially available mixtures of octoxynol-12 and polysorbate 20 without or with the addition of PEG-40 hydrogenated castor oil (Solubilisant gamma 2421 and Solubilisant gamma 2429, respectively). The oil phase of microemulsions was isopropyl myristate. Phase behaviour study of the pseudo-ternary systems Labrasol/cosurfactant/oil/water at surfactant-to-cosurfactant weight ratios (K(m)) 40:60, 50:50 and 60:40, revealed a strong synergism in the investigated tensides mixtures for stabilisation of microemulsions containing up to 80% (w/w) of water phase at surfactant +cosurfactant-to-oil weight ratio (SCoS/O) 90:10. Solubilization of a model drug ibuprofen in concentration common for topical application (5%, w/w) was achieved at the water contents below 50% (w/w). Drug free and ibuprofen-loaded microemulsions M1-M6, containing 45% (w/w) of water phase, were prepared and characterized by polarized light microscopy, conductivity, pH, rheological and droplet size measurements. In vitro ibuprofen release kinetics from the microemulsions was investigated using paddle-over-enhancer cell method and compared with the commercial 5% (w/w) ibuprofen hydrogel product (Deep Relief, Mentholatum Company Ltd., USA). The investigated microemulsions were isotropic, low viscous Bingham-type liquids with the pH value (4.70-6.61) suitable for topical application. The different efficiency of the tensides mixtures for microemulsion stabilisation was observed, depending on the cosurfactant type and K(m) value. Solubilisant gamma 2429 as well as higher K(m) (i.e., lower relative content of the cosurfactant) provided higher surfactant/cosurfactant synergism. The drug molecules were predominantly

  3. Effects of ibuprofen, diclofenac, naproxen, and piroxicam on the course of pregnancy and pregnancy outcome: a prospective cohort study

    Science.gov (United States)

    Nezvalová-Henriksen, K; Spigset, O; Nordeng, H

    2013-01-01

    Objective To investigate the individual effects of ibuprofen, diclofenac, naproxen, and piroxicam on pregnancy outcome. Design Cohort study. Setting Norwegian population. Population Total of 90 417 women and singleton child pairs. Methods Norwegian Mother and Child Cohort Study and Medical Birth Registry of Norway datasets were used. Main outcome measures Infant survival, congenital malformations, structural heart defects, neonatal complications, haemorrhage during pregnancy and postpartum, asthma at age of 18 months. Results One or more of the four NSAIDs were used by 6511 pregnant women, (7.2%). No effect on infant survival, congenital malformation, or structural heart defect rate was found. Second trimester ibuprofen use was significantly associated with low birth weight (adjusted OR 1.7, 95% CI 1.3 to 2.3) and second and third trimester use was significantly associated with asthma in the 18 month old child (adjusted OR 1.5, 95%CI 1.2 to 1.9 and adjusted OR 1.5, 95%CI 1.1 to 2.1). Second trimester diclofenac use was significantly associated with low birth weight (adjusted OR 3.1, 95% CI 1.1 to 9.0), whereas third trimester use was significantly associated with maternal vaginal bleeding (adjusted OR 1.8, 95% CI 1.1 to 3.0). No associations with other neonatal complications were found. Conclusions The lack of associations with congenital malformations is reassuring. The significant association between diclofenac and ibuprofen use late in pregnancy and maternal bleeding and asthma in the child respectively is consistent with their pharmacological effects. The increased risk of low birth weight may partly have been caused by underlying inflammatory conditions and was reassuringly similar to the expected baseline risk of low birth weight. PMID:23489333

  4. Comparison of Preemptive Effects of Celecoxib and Ibuprofen on Postoperative Pain in Addicted Patients Undergoing Lower Abdominal Surgery

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    A. Farhanchi

    2017-10-01

    Full Text Available Background and Objective: Pain is a common postoperative complaint, and the use of analgesics before surgical trauma can effectively prevent peripheral and central sensitization. We aimed to compare the preemptive effects of ibuprofen and celecoxib on post-operative pain after lower abdominal surgery in addicted patients. Materials and Methods: In this clinical trial, after obtaining informed consent, 114 addicted patients undergoing lower abdominal surgery were randomly divided into three groups of 38. The first group was given a 200 mg dose of oral celecoxib, 400 mg of ibuprofen was orally administered to patients in the second group, and the third group was given redsop hcrats as placebo by a nurse who prepared these drugs in the form of capsules. Postoperative pain was assessed by using a 10-cm ruler as the visual analogue scale at intervals of 1 and 6 hours after surgery. Postoperative opioid consumption was recorded in those periods. The obtained data were analyzed using the appropriate statistical tests in SPSS software. Results: Mean pain scores at 1 hour after surgery were not significantly different across the three groups, whereas at 6 hours after surgery, pain scores were significantly lower in the ibuprofen and celecoxib groups in comparison to the placebo group (P=0.001 and P=0.005, respectively. Postoperative nausea and vomiting was not significantly different among the three groups. Conclusion: Despite the significant difference in mean pain scores among the study groups, the opioid consumption doses were not significantly different among the groups. Thus, the preemptive prescription of nonsteroidal anti-inflammatory drugs in addicted patient does not have any noticeable effects.

  5. Impact of non-adherent Ibuprofen foam dressing in the lives of patients with venous ulcers.

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    Salomé, Geraldo Magela; Ferreira, Lydia Masako

    2017-01-01

    to evaluate pain in patients with lower limb venous ulcer who used non-adherent Ibuprofen foam dressing (IFD). we conducted a prospective study of patients with lower limb venous ulcers treated from April 2013 to August 2014. We used the Numerical Scale and McGill Pain Questionnaire, performing the assessments at the moment of inclusion of the patient in the study and every eight days thereafter, totaling five consultations. We divided the patients into two groups: 40 in the Study Group (SG), who were treated with IFD, and 40 in the Control Group (CG), treated with primary dressing, according to tissue type and exudate. at the first consultation, patients from both groups reported intense pain. On the fifth day, SG patients reported no pain and the majority of CG reported moderate pain. Regarding the McGill Pain Questionnaire, most patients of both groups reported sensations related to sensory, affective, evaluative and miscellaneous descriptors at the beginning of data collection; after the second assessment, there was slight improvement among the patients in the SG. After the third consultation, they no longer reported the mentioned descriptors. CG patients displayed all the sensations of these descriptors until the fifth visit. non-adherent Ibuprofen foam dressing is effective in reducing the pain of patients with venous ulcers. avaliar a dor em pacientes portadores de úlcera venosa de membros inferiores que utilizaram curativo de espuma não aderente com Ibuprofeno (CEI). estudo prospectivo de pacientes portadores de úlceras venosas de membros inferiores tratados no período de abril de 2013 a agosto de 2014. Foram utilizados os questionários Escala Numérica e Questionário de Dor de McGille, as avaliações eram feitas no momento da inclusão do paciente no estudo e a cada oito dias, totalizando cinco consultas. Os pacientes foram divididos em dois grupos: 40 no Grupo Estudo (GE), que foram tratados com CEI, e 40 no Grupo Controle (GC), tratados com

  6. Effect of playing tactics on achieving score-box possessions in a random series of team possessions from Norwegian professional soccer matches.

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    Tenga, Albin; Holme, Ingar; Ronglan, Lars Tore; Bahr, Roald

    2010-02-01

    Methods of analysis that include an assessment of opponent interactions are thought to provide a more valid means of team match performance. The purpose of this study was to examine the effect of playing tactics on achieving score-box possession by assessing opponent interactions in Norwegian elite soccer matches. We analysed a random series of 1703 team possessions from 163 of 182 (90%) matches played in the professional men's league during the 2004 season. Multidimensional qualitative data obtained from ten ordered categorical variables were used. Offensive tactics were more effective in producing score-box possessions when playing against an imbalanced defence (28.5%) than against a balanced defence (6.5%) (P tactics on producing score-box possessions, and improves the validity of team match-performance analysis in soccer.

  7. Administration of the non-steroidal anti-inflammatory drug ibuprofen increases macrophage concentrations but reduces necrosis during modified muscle use

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    Cheung, E. V.; Tidball, J. G.

    2003-01-01

    OBJECTIVE: To test the hypothesis that ibuprofen administration during modified muscle use reduces muscle necrosis and invasion by select myeloid cell populations. METHODS: Rats were subjected to hindlimb unloading for 10 days, after which they experienced muscle reloading by normal weight-bearing to induce muscle inflammation and necrosis. Some animals received ibuprofen by intraperitoneal injection 8 h prior to the onset of muscle reloading, and then again at 8 and 16 h following the onset of reloading. Other animals received buffer injection at 8 h prior to reloading and then ibuprofen at 8 and 16 h following the onset of reloading. Control animals received buffer only at each time point. Quantitative immunohistochemical analysis was used to assess the presence of necrotic muscle fibers, total inflammatory infiltrate, neutrophils, ED1+ macrophages and ED2+ macrophages at 24 h following the onset of reloading. RESULT: Administration of ibuprofen beginning 8 h prior to reloading caused significant reduction in the concentration of necrotic fibers, but increased the concentration of inflammatory cells in muscle. The increase in inflammatory cells was attributable to a 2.6-fold increase in the concentration of ED2+ macrophages. Animals treated with ibuprofen 8 h following the onset of reloading showed no decrease in muscle necrosis or increase in ED2+ macrophage concentrations. CONCLUSION: Administration of ibuprofen prior to increased muscle loading reduces muscle damage, but increases the concentration of macrophages that express the ED2 antigen. The increase in ED2+ macrophage concentration and decrease in necrosis may be mechanistically related because ED2+ macrophages have been associated with muscle regeneration and repair.

  8. Effect of preoperative ibuprofen in controlling postendodontic pain with and without low-level laser therapy in single visit endodontics: A randomized clinical study

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    Shahnaz Nabi

    2018-01-01

    Full Text Available Aim: The aim of this study is to evaluate the effect of low-level laser irradiation and ibuprofen in reducing the onset and severity of postoperative pain following single visit endodontics. Materials and Methods: One hundred and twenty patients were recruited for this study. Group A (n = 30 patients were administered 400 mg of ibuprofen orally 1 h before the institution of an endodontic procedure. Group B (n = 30 patients were given irradiation of a low-level laser at 50 Hz for 3 min after the standard endodontic procedure at the periapical region on both buccal and lingual aspect. Group C (n = 30 patients were given preoperative ibuprofen followed with a low-level laser at 50 Hz for 3 min after endodontic treatment. Group D (n = 30 patients were administered no preoperative ibuprofen nor low-level laser irradiation after the endodontic procedure. The patient immediately recorded his/her pain perception on the Heft Parker pain survey after completion of the appointment and at 4, 8, 12, 24, and 48 h postoperatively. Inter group analysis was carried out using the analysis of variances with “least significant difference” post hoc test. For intra group analysis, Student's t-test was used. Chi-square test was applied for nonparametric data. Results: Pain was significantly reduced in all the treatment groups postoperatively. Ibuprofen showed significant pain reduction at 4 h and 8 h period. The combination of low-level laser and ibuprofen showed the best results in terms of postoperative pain reduction. Conclusion: This study proved that low-level laser therapy can be an effective alternative for conventional use of nonsteroidal anti-inflammatory drugs in controlling postendodontic pain thereby eliminating the adverse effects of such drugs on the patients.

  9. Comparative study of the efficacy and safety of paracetamol, ibuprofen, and indomethacin in closure of patent ductus arteriosus in preterm neonates.

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    El-Mashad, Abd El-Rahman; El-Mahdy, Heba; El Amrousy, Doaa; Elgendy, Marwa

    2017-02-01

    In this prospective study, we compared the efficacy and side effects of indomethacin, ibuprofen, and paracetamol in patent ductus arteriosus (PDA) closure in preterm neonates. Three hundred preterm neonates with hemodynamically significant PDA (hs-PDA) admitted at our neonatal intensive care unit were enrolled in the study. They were randomized into three groups. Group I (paracetamol group) received 15 mg/kg/6 h IV paracetamol infusion for 3 days. Group II (ibuprofen group) received 10 mg/kg IV ibuprofen infusion followed by 5 mg/kg/day for 2 days. Group III (indomethacin group) received 0.2 mg/kg/12 h indomethacin IV infusion for three doses. Laboratory investigations such as renal function test, liver function test, complete blood count, and blood gases were conducted in addition to echocardiographic examinations. All investigations were done before and 3 days after treatment. There was no significant difference between all groups regarding efficacy of PDA closure (P = 0.868). There was a significant increase in serum creatinine levels and serum blood urea nitrogen (BUN) in the ibuprofen and indomethacin groups (P  0.05). Ventilatory settings improved significantly in patients with successful closure of PDA than those with failed PDA closure (P closure of PDA in preterm neonates and has less side effects mainly on renal function, platelet count, and GIT bleeding. What is Known: • Hemodynamically significant patent ductus arteriosus has many complications for preterm and low birth weight neonates and better to be closed. Many drugs were used for medical closure of PDA e.g. indomethacin, ibuprofen and recently paracetamol. Many studies compare safety and efficacy of paracetamol with either indomethacin or ibuprofen. What is New: • It is the first large study that compares the efficacy and side effects of the three drugs in one study.

  10. Traumatic Experience and Somatoform Dissociation Among Spirit Possession Practitioners in the Dominican Republic.

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    Schaffler, Yvonne; Cardeña, Etzel; Reijman, Sophie; Haluza, Daniela

    2016-03-01

    Recent studies in African contexts have revealed a strong association between spirit possession and severe trauma, with inclusion into a possession cult serving at times a therapeutic function. Research on spirit possession in the Dominican Republic has so far not included quantitative studies of trauma and dissociation. This study evaluated demographic variables, somatoform dissociative symptoms, and potentially traumatizing events in the Dominican Republic with a group of Vodou practitioners that either do or do not experience spirit possession. Inter-group comparisons revealed that in contrast to non-possessed participants (n = 38), those experiencing spirit possession (n = 47) reported greater somatoform dissociation, more problems with sleep, and previous exposure to mortal danger such as assaults, accidents, or diseases. The two groups did not differ significantly in other types of trauma. The best predictor variable for group classification was somatoform dissociation, although those items could also reflect the experience of followers during a possession episode. A factor analysis across variables resulted in three factors: having to take responsibility early on in life and taking on a professional spiritual role; traumatic events and pain; and distress/dissociation. In comparison with the non-possessed individuals, the possessed ones did not seem to overall have a remarkably more severe story of trauma and seemed to derive economic gains from possession practice.

  11. Single, simultaneous and sequential applications of ultrasonic frequencies for the elimination of ibuprofen in water.

    Science.gov (United States)

    Ziylan-Yavas, Asu; Ince, Nilsun H

    2018-01-01

    The study is about the assessment of single and multi-frequency operations for the overall degradation of a widely consumed analgesic pharmaceutical-ibuprofen (IBP). The selected frequencies were in the range of 20-1130kHz emissions coming from probes, baths and piezo-electric transducers attached to plate-type devices. Multi-frequency operations were applied either simultaneously as "duals", or sequentially at fixed time intervals; and the total reaction time in all operations was 30-min. The work also covers evaluation of the effect of zero-valent iron (ZVI) on the efficiency of the degradation process and the performance of the reaction systems. It was found that low-frequency probe type devices especially at 20kHz were ineffective when applied singly and without ZVI, and relatively more effective in combined-frequency operations in the presence of ZVI. The power efficiencies of the reactors and/or reaction systems showed that 20-kHz probe was considerably more energy intensive than all others, and was therefore not used in multi-frequency operations. The most efficient reactor in terms of power consumption was the bath (200kHz), which however provided insufficient mineralization of the test chemical. The highest percentage of TOC decay (37%) was obtained in a dual-frequency operation (40/572kHz) with ZVI, in which the energy consumption was neither low nor exceptionally too high. A sequential operation (40+200kHz) in that respect was more efficient, because it required much less energy for a similar TOC decay performance (30%). In general, the degradation of IBP increased with increased power consumption, which in turn reduced the sonochemical yield. The study also showed that advanced Fenton reactions with ZVI were faster in the presence of ultrasound, and the metal was very effective in improving the performance of low-frequency operations. Copyright © 2017 Elsevier B.V. All rights reserved.

  12. Photoelectrochemical oxidation of ibuprofen via Cu_2O-doped TiO_2 nanotube arrays

    International Nuclear Information System (INIS)

    Sun, Qiannan; Peng, Yen-Ping; Chen, Hanlin; Chang, Ken-Lin; Qiu, Yang-Neng; Lai, Shiau-Wu

    2016-01-01

    Highlights: • A p–n junction material was synthesized to enhance photocatalytic ability. • Cu_2O-doped TiO_2 nanotube arrays works as a photoanode in a PEC system. • Recombination of photo-generated holes and electrons were greatly reduced. • Synergetic effect was quantified in PEC degradation. • Recombination of photogenerated holes and electrons was greatly enhanced. - Abstract: A p–n junction based Cu_2O-doped TiO_2 nanotube arrays (Cu_2O-TNAs) were synthesized and used as a working anode in a photoelectrochemical (PEC) system. The results revealed that the Cu_2O-TNAs were dominated by the anatase phase and responded significantly to visible light. XPS analyses indicated that with an amount of 24.79% Cu doping into the structure, the band gap of Cu_2O-TNAs was greatly reduced. SEM images revealed that the supported TiO_2 nanotubes had diameters of approximately 80 nm and lengths of about 2.63 μm. Upon doping with Cu_2O, the TiO_2 nanotubes maintained their structural integrity, exhibiting no significant morphological change, favoring PEC applications. Under illumination, the photocurrent from Cu_2O/TNAs was 2.4 times larger than that from TNAs, implying that doping with Cu_2O significantly improved electron mobility by reducing the rate of recombination of electron-hole pairs. The EIS and Bode plot revealed that the estimated electron lifetimes, τ_e_l, of TNAs and Cu_2O/TNAs were 6.91 and 26.26 ms, respectively. The efficiencies of degradation of Ibuprofen by photoelectrochemical, photocatalytic (PC), electrochemical (EC) and photolytic (P) methods were measured.

  13. [Application of β-cyclodextrin in the formulation of ODT tablets containing ibuprofen].

    Science.gov (United States)

    Zimmer, Łukasz; Kasperek, Regina; Poleszak, Ewa

    2014-01-01

    Oral disintegrating tablet (ODT) dissolves or disintegrates in saliva and then it is swallowed. Diluent in direct compression formulation has a dual role: it increases bulk of the dosage form and it promotes binding of the constituent particles of the formulation. Hence, selection of diluent is important in tablets produced by direct compression method. The aim of this work was to exame feasibility of preparing and optimizing oral disintegrating tablet formulation using β-cyclodextrin as a diluent. 400 mg round tablets were prepared by direct compression method on single punch tablet press using flat plain-face. 60% β-CD and MCC (microcrystalline cellulose - MCC-Vivapur 102) were used at different proportions for all the formulations. 5% of Kollidon CL was added as superdisintegrant. The eight formulations prepared were assessed for weight variation, thickness, disintegration time, hardness and dissolution rate according to FP IX. A dissolution test was performed at 37ºC using the paddle method at 50 rpm with 900 mL phosphate buffer (pH 6.8) as a dissolution medium. The content of ibuprofen sodium was found inside the ± 5% of the theoretical value. Hardness values of presented tablets were in the range 0.11-0.15 kG/mm2. Friability of the tablets lower than 1% indicates that the developed formulations can be processed and handled without excessive care. Disintegration time was in the range of 86 to 161 s. The results confirm the good mechanical properties of tablets containing β-CD. A composition with 20% β-CD and 40% MCC fulfilled a maximum requisite of an optimum formulation. These properties were similar to Ludiflash, the formulation used for comparison purposes. In the present study, higher concentration of β cyclodextrin was found to improve the hardness of tablets without increasing the disintegration time.

  14. Synthesis and characterization of pH-sensitive drinkable nanoparticles for oral delivery of ibuprofen

    Science.gov (United States)

    Agostini, Azzurra; Capasso Palmiero, Umberto; Barbieri, Sara D. A.; Lupi, Monica; Moscatelli, Davide

    2018-06-01

    Ibuprofen (IBU) is a widespread drug used to treat both acute and chronic disorders. It is generally taken orally but the free drug can induce the irritation of the gastric mucosa due to its acid nature. In literature, different approaches have been adopted to prevent the release in the stomach, such as physical entrapment with film-coated tablets and drug-conjugates. Nevertheless, these solutions have many disadvantages, including the fast release of the drug and the difficulty to swallow the tablet, especially for children who may vomit or refuse the tablet. For this reason, in this work, novel formulations are proposed that do not require the encapsulation of the drug into a solid form and, in turn, their assumption as a pill. IBU has been linked to different types of methacrylates via ester bond in order to produce pH-responsive macromolecular monomers. The novelty is related to the use of these drug-conjugates macromonomer for the production of nanoparticles (NPs) via emulsion polymerization (EP), using water as solvent. The final emulsion is able to load up to 30 mg ml‑1 of IBU, so less than 10 ml is required to be assumed to reach the minimum therapeutic dose of the drug (200 mg). Finally, the release of IBU from these novel drinkable formulations has been investigated in the gastric and intestinal simulated fluids to show the preferential release of IBU from the NPs in basic conditions. A comparison with an existing oral suspension has been performed to highlight the slower release in acid environment of these new formulations. Afterwards, the IBU loaded NPs were tested in vitro showing lower toxicity compared to the free drug.

  15. Thermodynamic study of the solubility of ibuprofen in acetone and dichloromethane

    Directory of Open Access Journals (Sweden)

    Diana Marcela Aragón

    2010-06-01

    Full Text Available Thermodynamic functions, Gibbs energy, enthalpy and entropy for the solution processes of ibuprofen (IBP in acetone and dichloromethane (DCM were calculated from solubility values obtained at temperatures ranging from 293.15 K to 313.15 K. The respective thermodynamic functions for mixing and solvation processes as well as the activity coefficients for the solute were calculated. IBP solubility was high and proved similar in both solvents but was greater in DCM than acetone. In addition, the thermodynamic quantities for the transfer process of this drug from cyclohexane to the organic solvents were also calculated in order to estimate the contributions of hydrogen-bonds or of other dipolar interactions. The results were discussed in terms of solute-solvent interactions.As funções termodinâmicas, energia de Gibbs, entalpia e entropia dos processos de solução de ibuprofeno (IBP em acetona e em diclorometano (DCM foram calculadas a partir dos valores de solubilidade, obtidos em intervalos de temperatura de 293,15 K a 313,15 K. As funções termodinâmicas respectivas para os processos de mistura e solvatação e os coeficientes de atividade para o soluto também foram calculados. A solubilidade do IBP foi grande e semelhante em ambos os solventes, mas, maior em DCM do que em acetona. Em adição, as quantidades termodinâmicas relativas ao processo de transferência desse fármaco do cicloexano para os solventes orgânicos foram, também, calculadas com o objetivo de estimar as contribuições devidas às ligações de hidrogênio ou a outras interações dipolares. Os resultados foram discutidos nos termos das interações soluto-solvente.

  16. Active removal of ibuprofen by Money plant enhanced by ferrous ions.

    Science.gov (United States)

    Chehrenegar, Behdad; Hu, Jiangyong; Ong, Say Leong

    2016-02-01

    In this study, the removal of ibuprofen (IBP), a pharmaceutical compound, from aqueous media by Money plant (Epipremnum aureum) was investigated. The effect of ferrous iron (Fe(2+)) on enhancing the IBP removal rate was also analyzed. The first-order removal rate constants showed higher values for lower IBP initial concentrations in the range of 0.20-0.28 d(-1) for an initial concentration of 125 μg L(-1) to 0.03-0.13 d(-1) for an initial concentration of 1000 μg L(-1). Introducing ferrous iron to the aqueous media enhanced the first-order removal rate constant up to 6.5 times in a 3 d time period. Along with the removal of IBP from the media, the endogenous concentration of H2O2 also decreased presumably by the production of hydroxyl radical (·OH). Reduction in the endogenous H2O2 concentration was recorded to be 38% and 98% in the absence and presence of Fe(2+) respectively in the first day and the H2O2 level remained considerably low until day 7 which then gradually increased slightly. Simultaneous reduction of IBP and endogenous H2O2 concentration could be due to the reaction of IBP with ·OH and presumably ·OH production itself accelerated via Fenton reaction. In addition, presence of sodium bicarbonate (NaHCO3) as ·OH scavenger in the system showed reduction of first-order removal rate constant from 1.30 d(-1) to 0.07 d(-1) which could be a possible evidence of biological advanced oxidation process which is believed to play an important role in phytoremediation. Copyright © 2015 Elsevier Ltd. All rights reserved.

  17. Gene transcription and biomarker responses in the clam Ruditapes philippinarum after exposure to ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Milan, Massimo; Pauletto, Marianna; Patarnello, Tomaso; Bargelloni, Luca [Department of Comparative Biomedicine and Food Science, University of Padova, Viale dell' Universita 16, Legnaro (Padova) (Italy); Marin, Maria Gabriella [Department of Biology, University of Padova, Via Ugo Bassi 58/B, 35131 Padova (Italy); Matozzo, Valerio, E-mail: matozzo@bio.unipd.it [Department of Biology, University of Padova, Via Ugo Bassi 58/B, 35131 Padova (Italy)

    2013-01-15

    Pharmaceuticals are a class of emerging environmental contaminants that continuously enter aquatic environments. Presently, little information is available about the effects of these substances on non-target organisms, such as bivalves. We investigated the effects of ibuprofen (IBU) on the clam Ruditapes philippinarum. Clams were exposed for 1, 3, 5 and 7 days to 0, 100 and 1000 {mu}g IBU/L, and established biomarker responses (haemolymph lysozyme, gill acetylcholinesterase and digestive gland superoxide dismutase activities) as well as digestive gland transcriptome were evaluated. A two-way ANOVA revealed significant effects of both 'IBU concentration' and 'exposure duration' on biomarker responses. Overall, the enzyme activities were generally lower in IBU-exposed clams than in controls. Although limited knowledge of the mollusc transcriptome makes it difficult to interpret the effects of IBU on clams, the gene transcription analysis using DNA microarrays enabled the identification of the putative molecular mode of action of the IBU. The functional analysis of differentially transcribed genes suggests that IBU can interfere with various signalling pathways in clams, such as arachidonic acid metabolism, apoptosis, peroxisomal proliferator-activated receptors, and nuclear factor-kappa B. In addition, several genes involved in the metabolism of xenobiotics (e.g., glutathione S-transferase, sulfotransferase, cytochrome P450) were also found to be significantly affected by IBU exposure. In summary, the integrated approach of gene transcription analysis and biomarker responses facilitated the elucidation of the putative mechanisms of action of IBU in non-target species.

  18. Ibuprofen in mesopores of Mobil Crystalline Material 41 (MCM-41): a deeper understanding.

    Science.gov (United States)

    Skorupska, Ewa; Jeziorna, Agata; Paluch, Piotr; Potrzebowski, Marek J

    2014-05-05

    In this work, we compared two methods (incipient wetness and melting) for the encapsulation of ibuprofen in the pores of Mobil Crystalline Material 41 (MCM-41) through NMR (nuclear magnetic resonance) spectroscopy. (1)H NMR spectra were recorded under very fast MAS (sample spinning 60 kHz) conditions in both 1D and 2D mode (NOESY sequence). We also performed (13)C cross-polarization magic angle spinning (CP/MAS) experiments, (13)C single pulse experiments (SPE), and (1)H-(13)C HSQC HR/MAS (heteronuclear single quantum coherence high resolution) HR/MAS correlations. Evaluation of the encapsulation methods included an analysis of the filling factor of the drug into the pores. The stability of Ibu/MCM in an environment of ethanol or water vapor was tested. Our study showed that melting a mixture of Ibu and MCM is a much more efficient method of confining the drug in the pores compared to incipient wetness. The optimal experiments for the former method achieved a filling factor of approximately 60%. We concluded that the major limitation to the applicability of the incipient wetness method (filling factor ca. 20%) is the high affinity of solvent (typically ethanol) for MCM-41. We found that even ethanol vapor can remove Ibu from the pores. When a sample of Ibu/MCM was stored for a few hours in a closed vessel with ethanol vapor, Ibu was transported from the pores to the outer walls of MCM. We observed a similar phenomenon with water vapor, although this process is slower compared to the analogous procedure using ethanol. Our study clearly demonstrates that existing methods used to encapsulate drugs in mesoporous silica nanoparticles (MSNs) require reevaluation.

  19. Ion-exchange selectivity of diclofenac, ibuprofen, ketoprofen, and naproxen in ureolyzed human urine.

    Science.gov (United States)

    Landry, Kelly A; Sun, Peizhe; Huang, Ching-Hua; Boyer, Treavor H

    2015-01-01

    This research advances the knowledge of ion-exchange of four non-steroidal anti-inflammatory drugs (NSAIDs) - diclofenac (DCF), ibuprofen (IBP), ketoprofen (KTP), and naproxen (NPX) - and one analgesic drug-paracetamol (PCM) - by strong-base anion exchange resin (AER) in synthetic ureolyzed urine. Freundlich, Langmuir, Dubinin-Astakhov, and Dubinin-Radushkevich isotherm models were fit to experimental equilibrium data using nonlinear least squares method. Favorable ion-exchange was observed for DCF, KTP, and NPX, whereas unfavorable ion-exchange was observed for IBP and PCM. The ion-exchange selectivity of the AER was enhanced by van der Waals interactions between the pharmaceutical and AER as well as the hydrophobicity of the pharmaceutical. For instance, the high selectivity of the AER for DCF was due to the combination of Coulombic interactions between quaternary ammonium functional group of resin and carboxylate functional group of DCF, van der Waals interactions between polystyrene resin matrix and benzene rings of DCF, and possibly hydrogen bonding between dimethylethanol amine functional group side chain and carboxylate and amine functional groups of DCF. Based on analysis of covariance, the presence of multiple pharmaceuticals did not have a significant effect on ion-exchange removal when the NSAIDs were combined in solution. The AER reached saturation of the pharmaceuticals in a continuous-flow column at varying bed volumes following a decreasing order of DCF > NPX ≈ KTP > IBP. Complete regeneration of the column was achieved using a 5% (m/m) NaCl, equal-volume water-methanol solution. Results from multiple treatment and regeneration cycles provide insight into the practical application of pharmaceutical ion-exchange in ureolyzed urine using AER.

  20. Cumulative effects of ibuprofen and air emersion in zebra mussels Dreissena polymorpha.

    Science.gov (United States)

    André, C; Gagné, F

    2017-10-01

    Municipal effluents are major source of pharmaceutical products in the environment. The purpose of this study was to examine the toxicity of a largely used drug, ibuprofen (Ibu), in Dresseina polymorpha mussels and its impact on air survival time. The mussels were exposed to increasing concentration of Ibu (0, 1, 10 and 100μg/L) for 96 at 15°C and a sub-group of mussels was maintain in air for another 96h. Post-exposure mussels (Ibu and Ibu+Air) were analyzed for weight loss, total triglycerides, neutral lipids, lipid peroxidation (LPO), arachidonate-dependent cyclooxygenase (COX) and glutathione S-transferase activity. Lipid extracts of mussel tissues were also analyzed by 1 H-nuclear resonance spectroscopy. The data revealed that mussels exposed to Ibu had increased signs of lipid oxidation, neutral lipids and decreased triglycerides, LPO and GST activity. COX activity was significantly reduced by Ibu in keeping with mode of action of the drug. Following exposure to air, increased weight loss, neutral lipids (lipid degradation), were observed in mussels exposed to Ibu but no changes in COX activity were observed. Air stress limited the decrease in triglycerides and the increase in GST in mussels exposed to 100μg/L Ibu indicating decreased anti-oxidant response/phase II biotransformation and limited lipid metabolism. In conclusion, exposure to Ibu has some anti-inflammatory effects to mussels based on COX activity but resulted in increased oxidative damage and lipid catabolism. Exposure to air stress could enhance some of these responses and contribute to decreased resistance to air exposures. Crown Copyright © 2017. Published by Elsevier B.V. All rights reserved.

  1. Co-delivery of ibuprofen and gentamicin from nanoporous anodic titanium dioxide layers.

    Science.gov (United States)

    Pawlik, Anna; Jarosz, Magdalena; Syrek, Karolina; Sulka, Grzegorz D

    2017-04-01

    Although single-drug therapy may prove insufficient in treating bacterial infections or inflammation after orthopaedic surgeries, complex therapy (using both an antibiotic and an anti-inflammatory drug) is thought to address the problem. Among drug delivery systems (DDSs) with prolonged drug release profiles, nanoporous anodic titanium dioxide (ATO) layers on Ti foil are very promising. In the discussed research, ATO samples were synthesized via a three-step anodization process in an ethylene glycol-based electrolyte with fluoride ions. The third step lasted 2, 5 and 10min in order to obtain different thicknesses of nanoporous layers. Annealing the as-prepared amorphous layers at the temperature of 400°C led to obtaining the anatase phase. In this study, water-insoluble ibuprofen and water-soluble gentamicin were used as model drugs. Three different drug loading procedures were applied. The desorption-desorption-diffusion (DDD) model of the drug release was fitted to the experimental data. The effects of crystalline structure, depth of TiO 2 nanopores and loading procedure on the drug release profiles were examined. The duration of the drug release process can be easily altered by changing the drug loading sequence. Water-soluble gentamicin is released for a long period of time if gentamicin is loaded in ATO as the first drug. Additionally, deeper nanopores and anatase phase suppress the initial burst release of drugs. These results confirm that factors such as morphological and crystalline structure of ATO layers, and the procedure of drug loading inside nanopores, allow to alter the drug release performance of nanoporous ATO layers. Copyright © 2017 Elsevier B.V. All rights reserved.

  2. Comparison of the Effects of Acetaminophen Plus Ibuprofen to Treat Fever Than any of the Two Alone in Febrile Children

    Directory of Open Access Journals (Sweden)

    Noor Mohammad Noori

    2016-07-01

    Full Text Available Background Fever is a natural response of the host to infection and a normal part of children's infectious disease. Objectives The purpose of the study was comparison of the combined treatment of acetaminophen and ibuprofen compact with each treatment alone. Methods This Double-blind clinical trial study was done on 540 children with 38°C to 41°C as body temperature. Eligible children after considering inclusion criteria divided in three groups randomly. First group of 183 patients administrated with acetaminophen, the second and the third groups of 178 and 179 patients with ibuprofen and combination. The first dose of antipyretic drug was administered to the patient under the supervision of a physician or nurse. After explanation of benefits and marginal effects to the parents if they accepted the conditions their children were admitted to the study. Parents were free if they wish to withdraw the study before completing. Information of each patient was recorded on a form. The data were analyzed by descriptive statistic, one-way ANOVA and SPSS software version 16. Results Out of sample 60.6% were boy. The mean age of children treated with acetaminophen, ibuprofen and combination therapy was 2.21 ± 2.49, 3.00 ± 2.92 and 2.22 ± 2.33 years in the order given. The results showed statistical difference in two (F = 4.45 and P = 0.012 and four hours (F = 3.11 and P = 0.045 after taking drug. A significant difference not observed in the value of temperature decrease within 2 - 4 hours after drug intake, (F = 2.49, P=0.084 but in the time of 0-2 (P = 0.012 and 4-6 hours (P = 0.001 was observed. Conclusions The findings of this study showed that acetaminophen is more effective for a short time but the combination in the long time when ibuprofen placed in the middle position with the respect of time.

  3. Removal of ibuprofen, naproxen and carbamazepine in aqueous solution onto natural clay: equilibrium, kinetics, and thermodynamic study

    Science.gov (United States)

    Khazri, Hassen; Ghorbel-Abid, Ibtissem; Kalfat, Rafik; Trabelsi-Ayadi, Malika

    2017-10-01

    This study aimed to describe the adsorption of three pharmaceuticals compounds (ibuprofen, naproxen and carbamazepine) onto natural clay on the basis of equilibrium parameters such as a function of time, effect of pH, varying of the concentration and the temperature. Adsorption kinetic data were modeled using the Lagergren's first-order and the pseudo-second-order kinetic equations. The kinetic results of adsorption are described better using the pseudo-second order model. The isotherm results were tested in the Langmuir, Freundlich and Dubinin-Radushkevich models. The thermodynamic parameters obtained indicate that the adsorption of pharmaceuticals on the clay is a spontaneous and endothermic process.

  4. Ibuprofen therapy resulted in significantly decreased tissue bacillary loads and increased survival in a new murine experimental model of active tuberculosis.

    Science.gov (United States)

    Vilaplana, Cristina; Marzo, Elena; Tapia, Gustavo; Diaz, Jorge; Garcia, Vanesa; Cardona, Pere-Joan

    2013-07-15

    C3HeB/FeJ mice infected with Mycobacterium tuberculosis were used in an experimental animal model mimicking active tuberculosis in humans to evaluate the effect of antiinflammatory agents. No other treatment but ibuprofen was given, and it was administered when the animals' health started to deteriorate. Animals treated with ibuprofen had statistically significant decreases in the size and number of lung lesions, decreases in the bacillary load, and improvements in survival, compared with findings for untreated animals. Because antiinflammatory agents are already on the market, further clinical trials should be done to evaluate this effect in humans as soon as possible, to determine their suitability as coadjuvant tuberculosis treatment.

  5. A SynoviocyteModel for Osteoarthritis and Rheumatoid Arthritis: Response to Ibuprofen, Betamethasone, and Ginger Extract—A Cross-Sectional In Vitro Study

    DEFF Research Database (Denmark)

    Ribel-Madsen, Søren; Bartels, Else Marie; Stockmarr, Anders

    2012-01-01

    synovial membrane or joint fluid. Cells were cultivated and exposed to no or TNF-α stimulation without, or in the presence of, betamethasone, ibuprofen, or a standardized ginger extract. Concentrations of a panel of cytokines, growth factors, and chemokines were mapped for each culture and condition. Our......, and IL-8 release in all groups. Ibuprofen showed no effect on cytokine production, while ginger extract was similar to betamethasone. Ginger extract was as effective an anti-inflammatory agent as betamethasone in this in vitro model. Cultured fibroblast-like synoviocytes from OA and RA subjects promise...

  6. Alternating Acetaminophen and Ibuprofen versus Monotherapies in Improvements of Distress and Reducing Refractory Fever in Febrile Children: A Randomized Controlled Trial.

    Science.gov (United States)

    Luo, Shuanghong; Ran, Mengdong; Luo, Qiuhong; Shu, Min; Guo, Qin; Zhu, Yu; Xie, Xiaoping; Zhang, Chongfan; Wan, Chaomin

    2017-10-01

    No evidence can be found in the medical literature about the efficacy of alternating acetaminophen and ibuprofen treatment in children with refractory fever. Our objective was to assess the effect of alternating acetaminophen and ibuprofen therapy on distress and refractory fever compared with acetaminophen or ibuprofen as monotherapy in febrile children. A total of 474 febrile children with axillary temperature ≥38.5 °C and fever history ≤3 days in a tertiary hospital were randomly assigned to receive either (1) alternating acetaminophen and ibuprofen (acetaminophen 10 mg/kg per dose with shortest interval of 4 h and ibuprofen 10 mg/kg per dose with shortest interval of 6 h and the shortest interval between acetaminophen and ibuprofen ≥2 h; n = 158), (2) acetaminophen monotherapy (10 mg/kg per dose with shortest interval of 4 h; n = 158), or (3) ibuprofen monotherapy (10 mg/kg per dose with shortest interval of 6 h; n = 158). The mean Non-Communicating Children's Pain Checklist (NCCPC) score was measured every 4 h, and axillary temperatures were measured every 2 h. In total, 471 children were included in an intention-to-treat analysis. No significant clinical or statistical difference was found in mean NCCPC score or temperature during the 24-h treatment period in all febrile children across the three groups. Although the proportion of children with refractory fever for 4 h and 6 h was significantly lower in the alternating group than in the monotherapy groups (4 h: 11.54% vs. 26.58% vs. 21.66%, respectively [p = 0.003]; 6 h: 3.85% vs. 10.13% vs. 17.83%, respectively [p ibuprofen can reduce the proportion of children with refractory fever, but if one cycle of alternating therapy cannot reduce febrile distress as defined by NCCPC score, two or more cycles of alternating therapy may have minimal to no clinical efficacy in some cases. The trial was registered with the Chinese Clinical Trial Registry as ChiCTR-TRC-13003440 and the WHO

  7. Efficacy and tolerability of a new ibuprofen 200mg plaster in patients with acute sports-related traumatic blunt soft tissue injury/contusion.

    Science.gov (United States)

    Predel, Hans-Georg; Giannetti, Bruno; Connolly, Mark P; Lewis, Fraser; Bhatt, Aomesh

    2018-01-01

    Ibuprofen is used for the treatment of non-serious pain. This study assessed the efficacy and safety of a new ibuprofen plaster for the treatment of pain associated with acute sports impact injuries/contusions. In this randomised, double-blind, multi-centre, placebo controlled, parallel group study, adults (n = 130; 18-58 years of age) diagnosed with acute sports-related blunt soft tissue injury/contusion were randomized to receive either ibuprofen 200 mg plaster or placebo plaster. Plasters were administered once daily for five consecutive days. The primary assessment was area under the visual analogue scale (VAS) of pain on movement (POM) over 0 to three days (VAS AUC 0-3d ). Other endpoints included algometry AUC from 0 to three days (AUC 0-3d ) and 0 to five days (AUC 0-5d ), to evaluate improvement of sensitivity at the injured site, and patient and investigator global assessment of efficacy. Safety was monitored throughout the study. The ibuprofen plaster resulted in superior reduction in AUC 0-3d compared with placebo; the Least Squares (LS) mean difference was 662.82 mm*h in favour of the ibuprofen 200mg plaster (P = 0.0011). The greater improvement in VAS AUC of POM was also observed after 12 h, 24 h, and five days of therapy. Tenderness also significantly improved with the ibuprofen plaster compared with placebo; LS mean difference in algometry/tenderness AUC 0-3d was 1.87 N/cm 2 *d and AUC 0-5d was 1.87 N/cm 2 *d (P values ≤0.0004). At all study timepoints, a greater percentage of patients and investigators rated the effectiveness of the ibuprofen 200 mg plaster as good/excellent than the placebo plaster. Treatment-emergent adverse events for the ibuprofen plaster were few (≤1.5%) and were mild in severity. The results of this study indicate 200 mg plaster is effective and safe for the treatment of pain due to acute sports-related traumatic blunt soft tissue injury/contusion in adults.

  8. New families of conservative systems on $S^2$ possessing an integral of fourth degree in momenta

    OpenAIRE

    Selivanova, Elena N.

    1997-01-01

    There is a well-known example of integrable conservative system on $S^2$, the case of Kovalevskaya in the dynamics of a rigid body, possessing an integral of fourth degree in momenta. Goryachev proposed a one-parameter family of examples of conservative systems on $S^2$ possessing an integral of fourth degree in momenta which includes the case of Kovalevskaya. In this paper we proposed new examples of conservative systems on $S^2$ possessing an integral of fourth degree in momenta.

  9. Evaluation of local anesthetic effects of Lidocaine-Ibuprofen ionic liquid stabilized silver nanoparticles in Male Swiss mice.

    Science.gov (United States)

    Jiang, Qiliang; Yu, Shashuang; Li, Xingwang; Ma, Chuangen; Li, Aixiang

    2018-01-01

    A simple approach for the synthesis of Lidocaine-Ibuprofen ionic liquid stabilized silver nanoparticles (IL-AgNPs) was reported in this work. The shape, size and surface morphology of the Lidocaine-Ibuprofen ionic liquid stabilized AgNPs were characterized by using spectroscopic and microscopic techniques such as Ultraviolet-visible spectroscopy (UV-Visible), X-ray diffraction (XRD) analysis, Selected area electron diffraction (SAED), Transmission electron microscopy (TEM). TEM analysis showed the formation of 20-30nm size of IL-AgNPs with very clear lattice fringes. SAED pattern confirmed the highly crystalline nature of fabricated IL stabilized AgNPs. EDS results confirmed the formation of nanosilver. The fabricated IL-AgNPs were studied for their local anesthetic effect in rats. The results of local anesthetic effect showed that the time for onset of action by IL-AgNPs is 10min, which is significantly higher than that for EMLA. Further, tactile test results confirmed the stronger and faster local anesthetic effect of IL-AgNPs when compared to that of EMLA. Copyright © 2017. Published by Elsevier B.V.

  10. Evaluation of analgesic and anti-inflammatory activity of a combination of tramadol-ibuprofen in experimental animals.

    Science.gov (United States)

    Suthakaran, Chidambarann; Kayalvizhi, Muniyagounder K; Nithya, Karnam; Raja, Thozhudalangudy Ar

    2017-01-01

    Pain is the major concern of patients attending dental clinics, and satisfactory pain relief has always been difficult to achieve. Since the pathophysiology of pain is a complex, central and peripheral nervous system process, combined analgesic regimens with different mechanisms of action as a multimodal approach are becoming popular among the clinicians and dentists. The aim of the present study was to evaluate the analgesic and anti-inflammatory activity of ibuprofen and tramadol when used alone or in combination in animal models of pain and inflammation. The animals were divided into six groups with six animals in each group. Analgesic activity was assessed by hot plate method in rats and by acetic acid-induced writhing test in mice. Paw edema model in rats after induction with 0.1 mL of 1% carrageenan was used to assess the anti-inflammatory activity. Analysis of variance followed by Tukey's honestly significant difference post hoc test was used for statistical analysis. Combined use of tramadol and ibuprofen provided enhanced analgesic and anti-inflammatory effects in animal models of pain and inflammation.

  11. Evaluation of analgesic and anti-inflammatory activity of a combination of tramadol-ibuprofen in experimental animals

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    Chidambarann Suthakaran

    2017-01-01

    Full Text Available Background: Pain is the major concern of patients attending dental clinics, and satisfactory pain relief has always been difficult to achieve. Since the pathophysiology of pain is a complex, central and peripheral nervous system process, combined analgesic regimens with different mechanisms of action as a multimodal approach are becoming popular among the clinicians and dentists. Objectives: The aim of the present study was to evaluate the analgesic and anti-inflammatory activity of ibuprofen and tramadol when used alone or in combination in animal models of pain and inflammation. Animals and Methods: The animals were divided into six groups with six animals in each group. Analgesic activity was assessed by hot plate method in rats and by acetic acid-induced writhing test in mice. Paw edema model in rats after induction with 0.1 mL of 1% carrageenan was used to assess the anti-inflammatory activity. Statistical Analysis: Analysis of variance followed by Tukey's honestly significant difference post hoc test was used for statistical analysis. Results and Conclusion: Combined use of tramadol and ibuprofen provided enhanced analgesic and anti-inflammatory effects in animal models of pain and inflammation.

  12. Comparison of Oral Ibuprofen and Intravenous Indomethacin for the Treatment of Patent Ductus Arteriosus in Extremely Low Birth Weight Infants

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    Eun Mi Yang

    2013-01-01

    Full Text Available Objective: There are few published reports concerning the efficacy of oral ibuprofen for the treatment of patent ductus arteriosus (PDA in extremely low birth weight (ELBW infants. Oral ibuprofen was compared to intravenous indomethacin regarding efficacy and safety in the treatment of PDA in infants weighting less than 1,000 g at birth. Method: This was a retrospective study in a single center. Data on ELBW infants who had an echocardiographically confirmed PDA were collected. The infants were treated with either intravenous indomethacin or oral ibuprofen. Rate of ductal closure, need for additional treatment, drug-related side effects or complications, and mortality were compared between the two treatment groups. Result: 26 infants who received indomethacin and 22 infants who received ibuprofen were studied. The overall rate of ductal closure was similar between the two treatments: it occurred in 23 of 26 infants (88.5% treated with indomethacin, and in 18 of 22 infants (81.8% treated with ibuprofen (p = 0.40. The rate of surgical ligation (11.5% versus 18.2%; p = 0.40 did not differ significantly between the two treatment groups. No significant difference was found in post-treatment serum creatinine concentrations between the two groups. There were no significant differences regarding additional side effects or complications. Conclusion: In ELBW infants, oral ibuprofen is as efficacious as intravenous indomethacin for the treatment of PDA. There were no differences between the two drugs with respect to safety. Oral ibuprofen could be used as an alternative agent for the treatment of PDA in ELBW infants. Resumo: Objetivo: Existem poucos relatórios publicados com relação à eficácia do ibuprofeno via oral no tratamento da persistência do canal arterial (PCA em neonatos com extremo baixo peso ao nascer (EBPN. Comparamos o ibuprofeno via oral à indometacina intrave- nosa no que diz respeito à eficácia e segurança no tratamento de

  13. Possession Zone as a Performance Indicator in Football. The Game of the Best Teams

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    Claudio A. Casal

    2017-07-01

    Full Text Available Possession time in football has been widely discussed in research but few studies have analyzed the importance of the field area in which possession occurs. The objective of this study was to identify the existence of significant differences in the field zone of ball possession between successful and unsuccessful teams and to acknowledge if the match status modulates the possession model. To this end, 2,284 attacks were analyzed corresponding to the matches in the final phase of the UEFA Euro 2016 France, recording possession time and field zone in which possession occurred. Video recordings of matches were analyzed and coded post-event using notational analysis. We have found that successful offensive game patterns are different from unsuccessful ones. Specifically, field zone in which major possession occurs changes significantly between successful and unsuccessful teams (x2 = 15.72, p < 0.05 and through Welch’s T significant differences were detected in possession time between successful and unsuccessful teams (H = 24.289, p < 0.001. The former are characterized by longer possession times, preferably in the middle offensive zone, on the other hand, unsuccessful teams have shorter possession times and preferably on the middle defensive zone. Logistic regression also allowed us to identify that greater possession in the middle offensive zone is a good indicator of success in the offensive game, allowing us to predict a greater chance of victory in the match. Specifically, every time the teams achieve possession in the middle offensive zone, the chance of winning the match will increase 1.72 times and, the probability of winning the match making longer possessions in the middle offensive zone is 44.25%. Applying the Kruskal–Wallis test we have also been able to verify how match status modulates the teams possession time, specifically, when teams are winning they have longer possessions x2 = 92.628, p = 0.011. Results obtained are expected to

  14. Sorption, Photodegradation, and Chemical Transformation of Naproxen and Ibuprofen in Soils and Water

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    Vulava, V. M.; Cory, W. C.; Murphey, V.; Ulmer, C.

    2015-12-01

    Trace levels of pharmaceutically active compounds (PhACs) are increasingly being found in municipal drinking water and natural streams around the world. PhACs enter natural water systems after passing through wastewater treatment plants that have proven to be relatively inefficient at removing them. Once they are released into the environment, they can undergo (1) soil sorption, (2) photodegradation, and/or (3) chemical transformation into structurally similar compounds. The overarching goal of this study is to understand the geochemical fate of common PhACs in the environment. Here we report on our studies with naproxen (NAP) and ibuprofen (IBP) in soils and water. Both compounds are complex nonpolar (aromatic) organic molecules with polar (carboxylic acid) functional groups. The carboxylic functional groups are likely to be deprotonated at environmentally relevant pHs (~4-8). Sorption studies of both compounds were conducted in clean and relatively acidic (soil pH ~4.5-6.5) natural soils that contained varying levels of organic matter (OM), clay minerals, and Fe oxides. OM was observed to play an important role in each of the above three processes. Sorption was observed to be stronger and nonlinear in higher OM soils, while weaker but still significant in lower OM, higher clay soils; the amphiphilic nature of NAP and IBP combined with the complex charged and nonpolar surfaces available in the soil was observed to control the sorption behavior. Both NAP and IBP underwent rapid photodegradation in aqueous suspensions when exposed to simulated sunlight. The degradation rates were observed to change in the presence of humic acid or fulvic acid. During sorption and photodegradation experiments, common transformation products were observed for both NAP and IBP. The transformation products produced were indicative of chemical transformation and not biological factors. Concentrations of the transformation products were significantly higher in the photoexposed aqueous

  15. 19 CFR 7.2 - Insular possessions of the United States other than Puerto Rico.

    Science.gov (United States)

    2010-04-01

    ... than Puerto Rico. 7.2 Section 7.2 Customs Duties U.S. CUSTOMS AND BORDER PROTECTION, DEPARTMENT OF... NAVAL STATION § 7.2 Insular possessions of the United States other than Puerto Rico. (a) Insular possessions of the United States other than Puerto Rico are also American territory but, because those insular...