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Sample records for subcutaneous controlled-release amoxicillin

  1. Amoxicillin

    Science.gov (United States)

    Amoxicillin is used to treat certain infections caused by bacteria, such as pneumonia; bronchitis; gonorrhea; and infections ... eliminate H. pylori, a bacteria that causes ulcers. Amoxicillin is in a class of medications called penicillin- ...

  2. Lansoprazole, Clarithromycin, and Amoxicillin

    Science.gov (United States)

    Lansoprazole, clarithromycin, and amoxicillin are used to treat and prevent the return of ulcers (sores in the lining of the stomach or intestine) ... of medications called proton pump inhibitors. Clarithromycin and amoxicillin are in a class of medications called antibiotics. ...

  3. Controlled release from recombinant polymers.

    Science.gov (United States)

    Price, Robert; Poursaid, Azadeh; Ghandehari, Hamidreza

    2014-09-28

    Recombinant polymers provide a high degree of molecular definition for correlating structure with function in controlled release. The wide array of amino acids available as building blocks for these materials lend many advantages including biorecognition, biodegradability, potential biocompatibility, and control over mechanical properties among other attributes. Genetic engineering and DNA manipulation techniques enable the optimization of structure for precise control over spatial and temporal release. Unlike the majority of chemical synthetic strategies used, recombinant DNA technology has allowed for the production of monodisperse polymers with specifically defined sequences. Several classes of recombinant polymers have been used for controlled drug delivery. These include, but are not limited to, elastin-like, silk-like, and silk-elastinlike proteins, as well as emerging cationic polymers for gene delivery. In this article, progress and prospects of recombinant polymers used in controlled release will be reviewed. Copyright © 2014 Elsevier B.V. All rights reserved.

  4. Controlled Release from Recombinant Polymers

    Science.gov (United States)

    Price, Robert; Poursaid, Azadeh; Ghandehari, Hamidreza

    2014-01-01

    Recombinant polymers provide a high degree of molecular definition for correlating structure with function in controlled release. The wide array of amino acids available as building blocks for these materials lend many advantages including biorecognition, biodegradability, potential biocompatibility, and control over mechanical properties among other attributes. Genetic engineering and DNA manipulation techniques enable the optimization of structure for precise control over spatial and temporal release. Unlike the majority of chemical synthetic strategies used, recombinant DNA technology has allowed for the production of monodisperse polymers with specifically defined sequences. Several classes of recombinant polymers have been used for controlled drug delivery. These include, but are not limited to, elastin-like, silk-like, and silk-elastinlike proteins, as well as emerging cationic polymers for gene delivery. In this article, progress and prospects of recombinant polymers used in controlled release will be reviewed. PMID:24956486

  5. Susceptibilities of 540 anaerobic gram-negative bacilli to amoxicillin, amoxicillin-BRL 42715, amoxicillin-clavulanate, temafloxacin, and clindamycin.

    OpenAIRE

    Appelbaum, P C; Spangler, S K; Shiman, R; Jacobs, M R

    1992-01-01

    Agar dilution MIC testing of amoxicillin, amoxicillin-BRL 42715, amoxicillin-clavulanate, temafloxacin, and clindamycin against 496 beta-lactamase-producing anaerobic gram-negative rods revealed MICs for 90% of the strains tested of 256.0 (amoxicillin), 2.0 (amoxicillin-BRL 42715 and amoxicillin-clavulanate), and 4.0 (temafloxacin and clindamycin) microgram/ml. Amoxicillin, temafloxacin, and clindamycin inhibited all 44 beta-lactamase-negative strains (MICs for 90% of the strains tested, less...

  6. Modelling and simulations of controlled release fertilizer

    Science.gov (United States)

    Irfan, Sayed Ameenuddin; Razali, Radzuan; Shaari, Ku Zilati Ku; Mansor, Nurlidia

    2016-11-01

    The recent advancement in controlled release fertilizer has provided an alternative solution to the conventional urea, controlled release fertilizer has a good plant nutrient uptake they are environment friendly. To have an optimum plant intake of nutrients from controlled release fertilizer it is very essential to understand the release characteristics. A mathematical model is developed to predict the release characteristics from polymer coated granule. Numerical simulations are performed by varying the parameters radius of granule, soil water content and soil porosity to study their effect on fertilizer release. Understanding these parameters helps in the better design and improve the efficiency of controlled release fertilizer.

  7. Subcutaneous Injections

    DEFF Research Database (Denmark)

    Thomsen, Maria

    This thesis is about visualization and characterization of the tissue-device interaction during subcutaneous injection. The tissue pressure build-up during subcutaneous injections was measured in humans. The insulin pen FlexTouchr (Novo Nordisk A/S) was used for the measurements and the pressure...... build-up was evaluated indirectly from the changes in the flow rate between subcutaneous injections and air injections. This method enabled the tissue counter pressure to be evaluated without a formal clinical study approval. The measurements were coupled to a model for the pressure evolution...... in subcutaneous tissue, based on mass conservation and flow in a porous medium. From the measurements the flow permeability and bulk modulus of the tissue were determined. In the adipose tissue the drug forms a bolus from where it is absorbed by the blood capillaries. The spatial distribution of the injected...

  8. Stimuli responsive nanomaterials for controlled release applications

    KAUST Repository

    Li, Song

    2012-01-01

    The controlled release of therapeutics has been one of the major challenges for scientists and engineers during the past three decades. Coupled with excellent biocompatibility profiles, various nanomaterials have showed great promise for biomedical applications. Stimuli-responsive nanomaterials guarantee the controlled release of cargo to a given location, at a specific time, and with an accurate amount. In this review, we have combined the major stimuli that are currently used to achieve the ultimate goal of controlled and targeted release by "smart" nanomaterials. The most heavily explored strategies include (1) pH, (2) enzymes, (3) redox, (4) magnetic, and (5) light-triggered release.

  9. Amoxicillin Pulsatile MiddleBrook: APC 111, APC-111, PULSYS-Enhanced Amoxicillin

    National Research Council Canada - National Science Library

    Adis International Limited

    2007-01-01

    MiddleBrook Pharmaceuticals (formerly Advancis Pharmaceutical) is developing an improved version of amoxicillin using its pulsatile oral drug delivery technology, called PULSYS™. Amoxicillin PULSYS...

  10. Amoxicillin-induced aseptic meningoencephalitis

    Directory of Open Access Journals (Sweden)

    Radi Shahien

    2010-06-01

    Full Text Available Radi Shahien1, Vetaly Vieksler1, Abdalla Bowirrat11Department of Neurology and Neurophysiology, Ziv Medical Center, Safed, IsraelAbstract: Meningitis is usually produced by an infectious agent, but there are multiple noninfectious causes. Drug-induced aseptic meningitis (DIAM is an important entity and has been reported as an uncommon adverse reaction with numerous agents. Thus, DIAM constitutes a diagnostic and patient management challenge. We present a patient with three episodes of aseptic meningitis due to amoxicillin, and then review the literature on this rare idiosyncratic event which may occur after local or systemic drug administration. A 77-year-old man was admitted to our hospital with fever, headache, and neck stiffness. Seven days before admission he had a dental and gingival inflammation. He was treated with two oral doses of 500 mg daily of amoxicillin for one week. The seventh day he awoke with the complaints that prompted hospital admittance. Amoxicillin was stopped 1 day before his admission. From his history we knew of two similar episodes: The first episode was after a dental procedure 3 months before this incident. He had received a 1-week course of postprocedure amoxicillin of 500 mg daily and had similar headache, fever, and chills during the entire course of treatment. He wasn’t admitted to the hospital, because he stopped taking amoxicillin and he felt spontaneous pain relief after taking symptomatic pain treatment. The second episodes was 6 months after his first admission, he had been admitted to our hospital with the same symptoms. Amoxicillin was stopped and changed with intravenous (IV ceftriaxone (CTRX for 10 days due to suspected partial untreated meningitis. The patient improved rapidly within 2 days and was discharged from the hospital. On the basis of these three confirmed episodes of meningitis after recurrent exposure to amoxicillin, with repetitive negative testing for viral, bacterial, and mycobacterial

  11. Dental enamel, fluorosis and amoxicillin

    Directory of Open Access Journals (Sweden)

    I. Ciarrocchi

    2012-06-01

    Full Text Available Introduction: Amoxicillin is one of the most used antibiotics among pediatric patients for the treatment of upper respiratory tract infections and specially for acute otitis media (AOM, a common diseases of infants and childhood. It has been speculated that the use of amoxicillin during early childhood could be associated with dental enamel fluorosis, also described in literature with the term Molar Incisor Hypomineralization (MIH, because they are generally situated in one or more 1st permanent molars and less frequently in the incisors. The effect of Amoxicillin seems to be independent of other risk factors such as fluoride intake, prematurity, hypoxia, hypocalcaemia, exposure to dioxins, chikenpox, otitis media, high fever and could have a significant impact on oral health for the wide use of this drug in that period of life. Objective: The aim of this work was to review the current literature about the association between amoxicillin and fluorosis. Methods and Results: A literature survey was done by applying the Medline database (Entrez PubMed; the Cochrane Library database of the Cochrane Collaboration (CENTRAL. The databases were searched using the following strategy and keywords: amoxicillin* AND (dental fluorosis* OR dental enamel* AND MIH*. After selecting the studies, only three relevant articles published between 1966 and 2011 were included in the review. Conclusion: The presence of several methodological issues does not allow to draw any evidence-based conclusions. No evidence of association was detected, therefore, there is a need of further well-designed studies to assess the scientific evidence of the relationship between amoxicillin and fluorosis and to restrict the prescription of this drug for recurrent upper respiratory tract infections especially acute otitis media (AOM during the first two years of life. When it is possible can be opportune to use an alternative antibiotic treatment.

  12. Controlled release fertilizer workshop, 1991: Proceedings

    Energy Technology Data Exchange (ETDEWEB)

    Scheib, R.M. (ed.)

    1991-11-01

    Over the last 20 years the Tennessee Valley Authority's National Fertilizer and Environmental Research Center (NFERC) has carried out a number of programs to develop controlled release fertilizers. They pioneered the development and commercialization of sulfur coated urea and conducted extensive research in an attempt to develop an economical synthesis for oxamide. In recent years there has developed an increasing interest in the environmental impact of fertilizers, particularly on the potential for ground water contamination by nitrate derived from fertilizer materials. In response to this interest NFERC's Chemical Research Department organized a five member Controlled Release Fertilizer (CRF) Team to reassess the potential for controlled release materials in agriculture with a view to minimizing any adverse environmental impact and increasing the efficiency of nutrient utilization by the crop. This workshop was part of that reassessment program. The workshop goals were: To determine the present status of CRF research, production and use; to assess the future needs of CRF producers and consumers; and to promote communication and exchange of information. To accomplish these goals the team invited speakers from across' the United States representing academics, experimental station researchers, fertilizer producers, environmentalists, and marketing experts to present papers.

  13. Controlled release fertilizer workshop, 1991: Proceedings

    Energy Technology Data Exchange (ETDEWEB)

    Scheib, R.M. [ed.

    1991-11-01

    Over the last 20 years the Tennessee Valley Authority`s National Fertilizer and Environmental Research Center (NFERC) has carried out a number of programs to develop controlled release fertilizers. They pioneered the development and commercialization of sulfur coated urea and conducted extensive research in an attempt to develop an economical synthesis for oxamide. In recent years there has developed an increasing interest in the environmental impact of fertilizers, particularly on the potential for ground water contamination by nitrate derived from fertilizer materials. In response to this interest NFERC`s Chemical Research Department organized a five member Controlled Release Fertilizer (CRF) Team to reassess the potential for controlled release materials in agriculture with a view to minimizing any adverse environmental impact and increasing the efficiency of nutrient utilization by the crop. This workshop was part of that reassessment program. The workshop goals were: To determine the present status of CRF research, production and use; to assess the future needs of CRF producers and consumers; and to promote communication and exchange of information. To accomplish these goals the team invited speakers from across` the United States representing academics, experimental station researchers, fertilizer producers, environmentalists, and marketing experts to present papers.

  14. Electrosprayed nanoparticle delivery system for controlled release

    Energy Technology Data Exchange (ETDEWEB)

    Eltayeb, Megdi, E-mail: megdi.eltayeb@sustech.edu [Department of Biomedical Engineering, Sudan University of Science and Technology, PO Box 407, Khartoum (Sudan); Stride, Eleanor, E-mail: eleanor.stride@eng.ox.ac.uk [Institute of Biomedical Engineering, Department of Engineering Science, University of Oxford, Old Road Campus Research Building, Headington OX3 7DQ (United Kingdom); Edirisinghe, Mohan, E-mail: m.edirisinghe@ucl.ac.uk [Department of Mechanical Engineering, University College London, Torrington Place, London WC1E 7JE (United Kingdom); Harker, Anthony, E-mail: a.harker@ucl.ac.uk [London Centre for Nanotechnology, Gordon Street, London WC1H 0AH (United Kingdom); Department of Physics & Astronomy, University College London, Gower Street, London WC1E 6BT (United Kingdom)

    2016-09-01

    This study utilises an electrohydrodynamic technique to prepare core-shell lipid nanoparticles with a tunable size and high active ingredient loading capacity, encapsulation efficiency and controlled release. Using stearic acid and ethylvanillin as model shell and active ingredients respectively, we identify the processing conditions and ratios of lipid:ethylvanillin required to form nanoparticles. Nanoparticles with a mean size ranging from 60 to 70 nm at the rate of 1.37 × 10{sup 9} nanoparticles per minute were prepared with different lipid:ethylvanillin ratios. The polydispersity index was ≈ 21% and the encapsulation efficiency ≈ 70%. It was found that the rate of ethylvanillin release was a function of the nanoparticle size, and lipid:ethylvanillin ratio. The internal structure of the lipid nanoparticles was studied by transmission electron microscopy which confirmed that the ethylvanillin was encapsulated within a stearic acid shell. Fourier transform infrared spectroscopy analysis indicated that the ethylvanillin had not been affected. Extensive analysis of the release of ethylvanillin was performed using several existing models and a new diffusive release model incorporating a tanh function. The results were consistent with a core-shell structure. - Highlights: • Electrohydrodynamic spraying is used to produce lipid-coated nanoparticles. • A new model is proposed for the release rates of active components from nanoparticles. • The technique has potential applications in food science and medicine. • Electrohydrodynamic processing controlled release lipid nanoparticles.

  15. Amoxicillin, a potential epileptogenic drug.

    Science.gov (United States)

    Raposo, João; Teotónio, Rute; Bento, Conceição; Sales, Francisco

    2016-12-01

    Beta-lactams are known to cause a wide spectrum of neurotoxic manifestations including epileptic seizures. The neurotoxicity of penicillin was first reported in 1945 by Johnson and Walker and is believed to exert an inhibitory effect on gamma-aminobutyric acid transmission of cortical pyramidal cells, due to its beta-lactam ring structure. Epileptogenicity is also a feature of the semisynthetic beta-lactams including aminopenicillins. In this report, we present a patient with a recurrent history of discrete body twitching/jerks of epileptic nature in the context of amoxicillin exposure. The EEG revealed intermittent generalized short bursts of beta-frequency polyspikes. This electro-clinical picture was reversed by amoxicillin discontinuation.

  16. Meltable magnetic biocomposites for controlled release

    Science.gov (United States)

    Müller, R.; Zhou, M.; Dellith, A.; Liebert, T.; Heinze, T.

    2017-06-01

    New biocompatible composites with adjustable melting point in the range of 30-140 °C, consisting of magnetite nanoparticles embedded into a matrix of meltable dextran fatty acid ester are presented which can be softened under an induced alternating magnetic field (AMF). The chosen thermoplastic magnetic composites have a melting range close to human body temperature and can be easily shaped into disk or coating film under melting. The composite disks were loaded with green fluorescent protein (GFP) as a model protein. Controlled release of the protein was realized with high frequent alternating magnetic field of 20 kA/m at 400 kHz. These results showed that under an AMF the release of GFP from magnetic composite was accelerated compared to the control sample without exposure to AMF. Furthermore a texturing of particles in the polymer matrix by a static magnetic field was investigated.

  17. Convergence palsy secondary to amoxicillin.

    Science.gov (United States)

    Pérez-Roca, F; Alfaro Juárez, A; Sánchez Merino, C; Navarro Mingorance, A

    2016-12-01

    We present the case of an 11-year-old boy with acute diplopia in near vision secondary to transient convergence palsy, possibly in relation to amoxicillin. Convergence palsy is an uncommon eye disorder. The causes are reviewed, and amoxicilin is identified as presumptive etiologic agent. This is the first case reported. Copyright © 2016 Sociedad Española de Oftalmología. Publicado por Elsevier España, S.L.U. All rights reserved.

  18. Controlled Release Formulations of Auxinic Herbicides

    Science.gov (United States)

    Kowalski, Witold J.; Siłowiecki, Andrzej.; Romanowska, Iwona; Glazek, Mariola; Bajor, Justyna; Cieciwa, Katarzyna; Rychter, Piotr

    2013-04-01

    Controlled release formulations are applied extensively for the release of active ingredients such as plant protection agents and fertilizers in response to growing concern for ecological problems associated with increased use of plant protection chemicals required for intensive agricultural practices [1]. We synthesized oligomeric mixtures of (R,S)-3-hydroxy butyric acid chemically bonded with 2,4-D, Dicamba and MCPA herbicides (HBA) respectively, and determined their molecular structure and molecular weight dispersion by the size exclusion chromatography, proton magnetic resonance spectrometry and electro-spray ionization mass spectrometry. Further we carried out bioassays of herbicidal effectiveness of the HBA herbicides vs. series of dicotyledonous weeds and crop injury tests [2, 3, 4]. Field bioassays were accomplished according to the EPPO standards [5]. Groups of representative weeds (the development stages in the BCCH scale: 10 - 30) were selected as targets. Statistical variabilities were assessed by the Fisher LSD test for plants treated with the studied herbicides in form of HBA oligomers, the reference herbicides in form of dimethyl ammonium salts (DMA), and untreated plants. No statistically significant differences in the crop injuries caused by the HBA vs. the DMA reference formulation were observed. The effectiveness of the HBA herbicides was lower through the initial period (ca. 2 weeks) relative to the DMA salts, but a significant increase in the effectiveness of the HBA systems followed during the remaining fraction of each assay. After 6 weeks all observed efficiencies approached 100%. The death of weeds treated with the HBA herbicides was delayed when compared with the DMA reference herbicides. The delayed uptake observed for the HBA oligomers relative to the DMA salts was due to controlled release phenomena. In case of the DMA salts the total amount of active ingredients was available at the target site. By contrast, the amount of an active

  19. 21 CFR 556.38 - Amoxicillin.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin. 556.38 Section 556.38 Food and Drugs... Residues of New Animal Drugs § 556.38 Amoxicillin. A tolerance of 0.01 part per million is established for negligible residues of amoxicillin in milk and in the uncooked edible tissues of cattle. [49 FR 45422, Nov...

  20. Meltable magnetic biocomposites for controlled release

    Energy Technology Data Exchange (ETDEWEB)

    Müller, R., E-mail: robert.mueller@ipht-jena.de [Leibniz Institute of Photonic Technology (IPHT), P.O.B. 100239, Jena, D-07702 Germany (Germany); Zhou, M. [Institute of Organic Chemistry and Macromolecular Chemistry, Friedrich Schiller University of Jena, Humboldtstrasse 10, Jena, D-07743 Germany (Germany); Dellith, A. [Leibniz Institute of Photonic Technology (IPHT), P.O.B. 100239, Jena, D-07702 Germany (Germany); Liebert, T.; Heinze, T. [Institute of Organic Chemistry and Macromolecular Chemistry, Friedrich Schiller University of Jena, Humboldtstrasse 10, Jena, D-07743 Germany (Germany)

    2017-06-01

    New biocompatible composites with adjustable melting point in the range of 30–140 °C, consisting of magnetite nanoparticles embedded into a matrix of meltable dextran fatty acid ester are presented which can be softened under an induced alternating magnetic field (AMF). The chosen thermoplastic magnetic composites have a melting range close to human body temperature and can be easily shaped into disk or coating film under melting. The composite disks were loaded with green fluorescent protein (GFP) as a model protein. Controlled release of the protein was realized with high frequent alternating magnetic field of 20 kA/m at 400 kHz. These results showed that under an AMF the release of GFP from magnetic composite was accelerated compared to the control sample without exposure to AMF. Furthermore a texturing of particles in the polymer matrix by a static magnetic field was investigated. - Highlights: • Thermoplastic biocomposite are prepared from dextran ester and magnetite particles. • The composite can be heated by an AC magnetic field above the melting temperature. • In molten state texturing of particles is possible and improves the heating ability. • The biopolymer could be used as a remote controlled matrix for protein release.

  1. Meticulous Overview on the Controlled Release Fertilizers

    Directory of Open Access Journals (Sweden)

    Siafu Ibahati Sempeho

    2014-01-01

    Full Text Available Owing to the high demand for fertilizer formulations that will exhaust the possibilities of nutrient use efficiency (NUE, regulate fertilizer consumption, and lessen agrophysicochemical properties and environmental adverse effects instigated by conventional nutrient supply to crops, this review recapitulates controlled release fertilizers (CRFs as a cutting-edge and safe way to supply crops’ nutrients over the conventional ways. Essentially, CRFs entail fertilizer particles intercalated within excipients aiming at reducing the frequency of fertilizer application thereby abating potential adverse effects linked with conventional fertilizer use. Application of nanotechnology and materials engineering in agriculture particularly in the design of CRFs, the distinctions and classification of CRFs, and the economical, agronomical, and environmental aspects of CRFs has been revised putting into account the development and synthesis of CRFs, laboratory CRFs syntheses and testing, and both linear and sigmoid release features of CRF formulations. Methodical account on the mechanism of nutrient release centring on the empirical and mechanistic approaches of predicting nutrient release is given in view of selected mathematical models. Compositions and laboratory preparations of CRFs basing on in situ and graft polymerization are provided alongside the physical methods used in CRFs encapsulation, with an emphasis on the natural polymers, modified clays, and superabsorbent nanocomposite excipients.

  2. Sustained Release of Amoxicillin from Ethyl Cellulose-Coated Amoxicillin/Chitosan–Cyclodextrin-Based Tablets

    OpenAIRE

    Songsurang, Kultida; Pakdeebumrung, Jatuporn; Praphairaksit, Narong; Muangsin, Nongnuj

    2010-01-01

    Sustained release mucoadhesive amoxicillin tablets with tolerance to acid degradation in the stomach were studied. The sustained-release tablets of amoxicillin were prepared from amoxicillin coated with ethyl cellulose (EC) and then formulated into tablets using chitosan (CS) or a mixture of CS and beta-cyclodextrin (CD) as the retard polymer. The effects of various (w/w) ratios of EC/amoxicillin, the particle sized of EC coated amoxicillin and the different (w/w) ratios of CS/CD for the reta...

  3. Once-Daily Amoxicillin for Pharyngitis

    Science.gov (United States)

    Andrews, Megan; Condren, Michelle

    2010-01-01

    A once-daily antibiotic regimen for group A β-hemolytic streptococcal pharyngitis (GABHS) could improve compliance and be effective in the prevention of rheumatic fever, a dangerous complication of untreated or poorly treated GABHS. Amoxicillin is ideal for once-daily dosing due to its low cost. Azithromycin, cefadroxil, ceftibuten, cefixime and extended release amoxicillin are also FDA approved to treat GABHS once daily; however, even when taken for short courses, these antibiotics are more expensive compared with a oncedaily dosing of conventional amoxicillin for 10 days. The American Heart Association recently recommended once-daily amoxicillin dosing when treating GABHS, and amoxicillin has been proven to be effective when dosed once daily, with no obvious disadvantage compared with twice-daily dosing or with conventional penicillin treatment 3 to 4 times daily. PMID:22477812

  4. Design of Salecan-containing semi-IPN hydrogel for amoxicillin delivery.

    Science.gov (United States)

    Qi, Xiaoliang; Wei, Wei; Li, Junjian; Su, Ting; Pan, Xihao; Zuo, Gancheng; Zhang, Jianfa; Dong, Wei

    2017-06-01

    Salecan is a new linear extracellular β-glucan. The unique structure and beneficial properties of Salecan makes it an appealing material in biomedical applications. In this work, novel drug devices based on Salecan in a hydrogel matrix of poly(N-(3-dimethylaminopropyl)acrylamide-co-acrylamide) (Salecan/PDA) were fabricated via free radical polymerization for controlled release of amoxicillin. It was demonstrated that amoxicillin was efficiently encapsulated into the developed hydrogels and released in a Salecan dose-dependent and pH-sensitive manner. Furthermore, cell toxicity and adhesion assays confirmed that these drug carriers were biocompatible. Altogether, this study opens a new avenue to fabricate hydrogel devices for controlled delivery of drug. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. [Preparation of Shuxiong pulsatile controlled-release dropping pill].

    Science.gov (United States)

    Chen, Hui; Chen, Yan-Zhong; Xie, Qing-Chun; Lin, Shi-Yuan; Lin, Jia-Cheng; Jianc, Wei-Ning

    2013-07-01

    To prepare Shuxiong pulsatile controlled-release dropping pill and study the influencing factors in vitro. Dropping pills with suitable size (10 - 15 mg) were coated with swelling layer containing croscarmellose sodium and controlled-release layer containing ethylcellulos aqueous dispersion respectively to prepare Shuxiong pulsatile controlled-release dropping pill. The effects of the materials of swelling layer, the weight of swelling layer and controlled-release layer on the release of drugs were investigated to optimize the process technology and validate formula. The release behavior was influenced strikingly by the types and weight of coating layer. The optimal formula was as follows: Shuxiong pulsatile controlled-release dropping pills were prepared using croscarmellose sodium as inner layer with 15% (weight) coating level and ethylcellulose aqueous dispersion (Surelease) as outer controlled-release layer with 7% (weight) coating level. The lag time of prepared pulsatile controlled-release dropping pills was about 4 h and accumulative release rate reached 80% within 4 h. The drug release of Shuxiong pulsatile controlled-release dropping pill is shown in pulsatile way in vitro.

  6. Effect of Bioenhancers on Amoxicillin bioavailability

    Directory of Open Access Journals (Sweden)

    Kalyani Barve

    2015-03-01

    Full Text Available Amoxicillin, which inspite of being effective is losing its importance due to less bioavailability. Bioavailability could be enhanced by combining the antibiotics with bioenhancers like Piperine and Ginger resin. The present abstract deals with the use of piperine and ginger resin in increasing the bioavailability of amoxicillin using the insitu SPIP method. Piperine, isolated was found to be 99 % pure and ginger resin contained 4.36 % w/w of gingerol. The absorption of amoxicillin increased with addition of Piperine (1.2, 1.5, 1.8 % w/w of amoxicillin in a dose dependant manner reaching saturation after 45 minutes wheras Ginger resin (6, 7, 8 % w/w of amoxicillin failed to show this effect in the invitro studies. Piperine enhanced the permeation of Amoxicillin but ginger resin failed to show this effect using the insitu SPIP method. The method used may be appropriate for bioenhancers acting on transporters, metabolizing enzymes or modulators of diffusivity but not for those acting on gut motility. The combination of Piperine and Amoxicillin trihydarte may have a potential in reducing the dose, shortening the treatment period thus reducing drug-resistance problems of the antibiotic.

  7. Bioavailability enhancement studies of amoxicillin with Nigella

    Science.gov (United States)

    Ali, Babar; Amin, Saima; Ahmad, Javed; Ali, Abuzer; Ali, Mohd; Mir, Showkat R.

    2012-01-01

    Background & objectives: Nigella sativa Linn. is extensively used in the Indian diasporas as spice, which may interact with co-administered drugs and affect their intestinal availability. The purpose of this study was to investigate the effect of Nigella on bioavailability of amoxicillin in animal model. Methods: Everted rat intestinal sacs were used for in vitro experiment to study the transfer of amoxicillin across the gut. Amoxicillin (6 mg/ml) was co-infused with 3 and 6 mg of methanol and hexane extract of Nigella seeds separately. The amount of amoxicillin that traversed the gut was followed spectrophotometrically at 273 nm. For in vivo studies Wistar albino rats were used. Amoxicillin (25 mg/kg, po) was co-administered with hexane extract of Nigella seeds (25 mg/kg, po). The amount of amoxicillin in rat plasma was determined by UPLC-MS/MS method. Results: The in vitro studies both with methanol and hexane extracts of Nigella increased the permeation of amoxicillin significantly (Pamoxicillin in rat plasma when administered orally alone and in combination with hexane extract increased correspondingly from 4138.251 ± 156.93 to 5995.045 ± 196.28 ng/ml while as AUC0→t increased from 8890.40 ± 143.33 to 13483.46 ± 152.45 ng/ml.h. Interpretation & conclusions: Nigella enhanced amoxicillin availability in both in vivo and in vitro studies. As the increase in bioavailability is attributed, in part, to enhanced diffusivity across intestine, our study indicated that Nigella increased intestinal absorption of amoxicillin. PMID:22664507

  8. 21 CFR 526.88 - Amoxicillin trihydrate for intramammary infusion.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin trihydrate for intramammary infusion... Amoxicillin trihydrate for intramammary infusion. (a) Specifications. Each single dose syringe contains amoxicillin trihydrate equivalent to 62.5 milligrams of amoxicillin. (b) Sponsor. See No. 000061 in § 510.600...

  9. Progress of nano-controlled releasing system on ophthalmologic administration

    Directory of Open Access Journals (Sweden)

    Shu-Rong Wang

    2015-12-01

    Full Text Available The ophthalmic application of nanometer materials are mainly concentrated on controlled releasing systems. Due to the unique properties of nanometer materials,it has great advantages in carrying ophthalmic drugs compared with the conventional method, mainly in higher bioavailability and fewer side effects. As a result, nano-controlled releasing system has good application prospect in ophthalmology. At present, a variety of different types of nano-controlled releasing systems have been used to enhance the efficiency of the ophthalmic drugs, including nanomicelle, nanoparticles, nanosuspensions, liposomes,dendrimers, etc. In this paper, the research progress as well as the application of nano-controlled releasing system on ophthalmologic administration is reviewed.

  10. Encapsulated Urea-Kaolinite Nanocomposite for Controlled Release Fertilizer Formulations

    National Research Council Canada - National Science Library

    Sempeho, Siafu Ibahati; Kim, Hee Taik; Mubofu, Egid; Pogrebnoi, Alexander; Shao, Godlisten; Hilonga, Askwar

    2015-01-01

    Urea controlled release fertilizer (CRF) was prepared via kaolinite intercalation followed by gum arabic encapsulation in an attempt to reduce its severe losses associated with dissolution, hydrolysis, and diffusion...

  11. Dual drug delivery system for targeting H. pylori in the stomach: preparation and in vitro characterization of amoxicillin-loaded Carbopol® nanospheres

    Science.gov (United States)

    Harsha, Sree

    2012-01-01

    Background and methods: A dual (immediate/sustained-release) oral amoxicillin suspension was developed as a new dosage form to eradicate Helicobacter pylori. Carbopol®-loaded amoxi-cillin nanospheres could bind with the mucosa after delivery to the stomach and could increase the efficiency of the drug, providing both an immediate and a sustained action. Results: The objective of this research was to develop amoxicillin nanospheres using a spray-drying technique and to investigate such features as their particle size, drug content, percentage yield, surface morphology, in vitro release, and stability. The nanospheres had a particle size range of 280–320 nm after optimizing the preparation method using a central composite design. The drug content and percentage yield was 85.3% ± 0.7% and 92.8% ± 0.9%, respectively. The in vitro release profile of the amoxicillin nanospheres was consistent with a Korsmeyer-Peppas pattern, and the release after one hour was 19%, while for the original drug, amoxicillin, under the same conditions, 90% was released in the first 30 minutes. Conclusion: The nanospheres used in this study enabled controlled release of amoxicillin over an extended period of time for up to 12 hours and the formulation was stable for 12 months. PMID:22969298

  12. Dual drug delivery system for targeting H. pylori in the stomach: preparation and in vitro characterization of amoxicillin-loaded Carbopol® nanospheres.

    Science.gov (United States)

    Harsha, Sree

    2012-01-01

    A dual (immediate/sustained-release) oral amoxicillin suspension was developed as a new dosage form to eradicate Helicobacter pylori. Carbopol®-loaded amoxicillin nanospheres could bind with the mucosa after delivery to the stomach and could increase the efficiency of the drug, providing both an immediate and a sustained action. The objective of this research was to develop amoxicillin nanospheres using a spray-drying technique and to investigate such features as their particle size, drug content, percentage yield, surface morphology, in vitro release, and stability. The nanospheres had a particle size range of 280-320 nm after optimizing the preparation method using a central composite design. The drug content and percentage yield was 85.3% ± 0.7% and 92.8% ± 0.9%, respectively. The in vitro release profile of the amoxicillin nanospheres was consistent with a Korsmeyer-Peppas pattern, and the release after one hour was 19%, while for the original drug, amoxicillin, under the same conditions, 90% was released in the first 30 minutes. The nanospheres used in this study enabled controlled release of amoxicillin over an extended period of time for up to 12 hours and the formulation was stable for 12 months.

  13. Susceptibility of Porphyromonas gingivalis in biofilms to amoxicillin, doxycycline and metronidazole

    DEFF Research Database (Denmark)

    Larsen, T.

    2002-01-01

    Biofilm, Porphyromonas gingivalis, susceptibility testing, amoxicillin, doxycycline, metronidazole......Biofilm, Porphyromonas gingivalis, susceptibility testing, amoxicillin, doxycycline, metronidazole...

  14. Comparative trial between the use of amoxicillin and amoxicillin clavulanate in the removal of third molars.

    Science.gov (United States)

    Iglesias-Martín, Fernando; García-Perla-García, Alberto; Yañez-Vico, Rosa; Aced-Jiménez, Elena; Arjona-Gerveno, Esther; González-Padilla, Juan-David; Gutierrez-Pérez, Jose-Luis; Torres-Lagares, Daniel

    2014-11-01

    The purpose of this study was to compare the use of amoxicillin (1g) vs amoxicillin and clavulanate (875/125mg) after extraction of retained third molars for prevention of infectious complications. The study involved 546 patients attending for removal a retained third molar and divided in to two groups: Group 1 - amoxicillin and clavunate (875/125mg) group (n=257) and Group 2 - amoxicillin (1g) group (n=289). All patients were recalled for investigating the possibility of infection, presence of diarrhea and further analgesic intake. From a total of 546 patients, the frequency of infection was 1.4%, without no statistically differences between the two groups. Group 1 showed statistically higher presence of patients with gastrointestinal complications (p>0.05). In 546 patients, 2.7% of patients reported severe pain that would not relieve with medication. The results of our study show that the use of amoxicillin (1g) and amoxicillin and clavunate (875/125mg) is similar efficacious in preventing infection after retained third molar extraction but amoxicillin and clavunate (875/125mg) produces more gastrointestinal discomfort.

  15. Toxic Epidermal Necrolysis Caused by Amoxicillin

    Directory of Open Access Journals (Sweden)

    Celalettin Sever

    2011-09-01

    Full Text Available Toxic epidermal necrolysis (TEN is a severe skin reaction related to drugs and infections, characterized by fever, stomatitis and conjunctivitis. Many drug related TEN cases have been reported in literature but amoxicillin related TEN cases are rare. In this article, a case of amoxicillin related severe TEN in a female patient during treatment of tonsillitis has been reported. The increased use of amoxicillin, especially for control of infection, may be the reason for the increased incidence TEN due to the same drug. The identification of a drug as the cause for the immune related cytotoxic reaction may be difficult if the molecule is not generally known to be a classical cause of this reaction.

  16. Subcutaneous granuloma annulare

    Directory of Open Access Journals (Sweden)

    Dhar Sandipan

    1993-01-01

    Full Text Available Two cases of subcutaneous granuloma annulare are reported. Clinical presentation was in the form of hard subcutaneous nodules, histopathology confirmed the clinical diagnosis. The cases were unique because of onset in adult age, occurrence over unusual sites and absence of classical lesions of granuloma annulare elsewhere.

  17. Amoxicillin functionalized gold nanoparticles reverts MRSA resistance

    Energy Technology Data Exchange (ETDEWEB)

    Kalita, Sanjeeb; Kandimalla, Raghuram; Sharma, Kaustav Kalyan [Drug Discovery Lab, Life Science Division, Institute of Advanced Study in Science and Technology (IASST), Paschim Boragaon, Garchuk, Guwahati 781035, Assam (India); Kataki, Amal Chandra [Dr. B. Borooah Cancer Institute, Guwahati, Assam (India); Department of Applied Sciences, Gopinath Bordoloi Nagar, Jalukbari, Gauhati University, Guwahati 781014, Assam (India); Deka, Manab [Department of Applied Sciences, Gopinath Bordoloi Nagar, Jalukbari, Gauhati University, Guwahati 781014, Assam (India); Kotoky, Jibon, E-mail: jkotoky@gmail.com [Drug Discovery Lab, Life Science Division, Institute of Advanced Study in Science and Technology (IASST), Paschim Boragaon, Garchuk, Guwahati 781035, Assam (India)

    2016-04-01

    In this study, we have described the biosynthesis of biocompatible gold nanoparticles (GNPs) from aqueous extract of the aerial parts of a pteridophyte, “Adiantum philippense” by microwave irradiation and its surface functionalization with broad spectrum beta lactam antibiotic, amoxicillin (Amox). The functionalization of amoxicillin on GNPs (GNP-Amox) was carried out via electrostatic interaction of protonated amino group and thioether moiety mediated attractive forces. The synthesized GNPs and GNP-Amox were physicochemically characterized. UV–Vis spectroscopy, Zeta potential, XRD, FTIR and SERS (surface enhanced raman spectra) results confirmed the loading of Amox into GNPs. Loading of Amox to GNPs reduce amoxicillin cytotoxicity, whereas GNPs were found to be nontoxic to mouse fibroblast cell line (L929) as evident from MTT and acridine orange/ethidium bromide (AO/EtBr) live/dead cell assays. The GNP-Amox conjugates demonstrated enhanced broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Furthermore, in-vitro and in-vivo assays of GNP-Amox revealed potent anti-MRSA activity and improved the survival rate. This indicates the subversion of antibiotic resistance mechanism by overcoming the effect of high levels of β-lactamase produced by methicillin resistant Staphylococcus aureus (MRSA). Taken together, this study demonstrates the positive attributes from GNP-Amox conjugates as a promising antibacterial therapeutic agent against MRSA as well as other pathogens. - Highlights: • Aqueous extract of A. phillippens was used as a reducing and capping agent for synthesis of microwave irradiated gold nanoparticles. • GNPs were loaded with amoxicillin for restoration in antibacterial activity of amoxicillin against MRSA strains. • Gold nanoparticles and GNP-Amox were found biocompitable as tested on L929 cell line. • The nanoparticle antibiotic conjugates exhibited restoration of amoxicillin activity against MRSA in

  18. 21 CFR 520.88e - Amoxicillin trihydrate boluses.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin trihydrate boluses. 520.88e Section... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.88e Amoxicillin trihydrate boluses. (a) Specifications. Each bolus contains the equivalent of 400 milligrams of amoxicillin...

  19. 21 CFR 520.88c - Amoxicillin trihydrate oral suspension.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin trihydrate oral suspension. 520.88c... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.88c Amoxicillin trihydrate oral suspension. (a) Specifications. Each 0.8-milliliter dose contains amoxicillin trihydrate...

  20. Controlled release of diclofenac sodium from pH-responsive ...

    Indian Academy of Sciences (India)

    In this paper, controlled release of diclofenac sodium (DS) from pH-sensitive carrageenan-gpoly(acrylic acid) superabsorbent hydrogels was investigated. The hydrogels were prepared by graft copolymerization of acrylic acid (AA) onto kappa-carrageenan, using ammonium persulfate (APS) as a free radical initiator in the ...

  1. Rectal absorption of morphine from controlled release suppositories

    NARCIS (Netherlands)

    Moolenaar, Frits; Meyler, Pim; Frijlink, Erik; Jauw, Tjoe Hang; Visser, Jan; Proost, Johannes

    1995-01-01

    The absorption profiles and bioavailability of morphine in human volunteers (n = 13) were described after oral administration of MS Contin tablets and rectal administration of a newly developed controlled release suppository. By manipulating the viscosity of fatty suppository base an entirely

  2. Controlled release of 5-flurouracil from biomedical polyurethanes

    Indian Academy of Sciences (India)

    Administrator

    kles on their surfaces. The release of 5-FU through the microspheres was investigated in pH 7⋅4- phosphate buffer. An increase in release rate was observed with increasing molar ratio of PLF68 with respect to castor oil. Keywords. Biomedical polyurethane; controlled release; 5-flurouracil; drug delivery. 1. Introduction.

  3. Biopolymers in controlled release devices for agricultural applications.

    Science.gov (United States)

    The use of biopolymers such as starch for agricultural applications including controlled release devices is growing due the environmental benefits. Recently, concerns have grown about the worldwide spread of parasitic mites (Varroa destructor) that infect colonies of honey bees (Apis mellifera L.). ...

  4. Chemical analysis of substrates with controlled release fertilizer

    NARCIS (Netherlands)

    Kreij, de C.

    2004-01-01

    Water-soluble fertilizer added to media containing controlled release fertilizer cannot be analysed with the 1:1.5 volume water extract, because the latter increases the element content in the extract. During storage and stirring or mixing the substrate with the extractant, part of the controlled

  5. Controlled release fertilizer improves quality of container longleaf pine seedlings

    Science.gov (United States)

    R. Kasten Dumroese; Jeff Parkhurst; James P. Barnett

    2005-01-01

    In an operational trial, increasing the amount of nitrogen (N) applied to container longleaf pine seedlings by incorporating controlled release fertilizer (CRF) into the media improved seedling growth and quality. Compared with control seedlings that received 40 mg N, seedlings receiving 66 mg N through CRF supplemented with liquid fertilizer had needles that were 4 in...

  6. Formulation and Pharmacokinetic Evaluation of Controlled-Release ...

    African Journals Online (AJOL)

    Controlled-Release Oxybutynin Tablets in Dogs. Joonho Bae1 and Jin Woo Park2*. 1Amorepacific Corporation R&D Center, 314-1, Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do, 446-729, 2College of. Pharmacy and Natural Medicine Research Institute, Mokpo National University, 1666 Youngsan-ro, Muan-gun, ...

  7. Effects of azithromycin versus metronidazole– amoxicillin ...

    African Journals Online (AJOL)

    This healing tendency was observed in the AZT group despite the baseline plaque scores. Therefore, AZT might be active against the bacteria in dental biofilms. Keywords: Azithromycin, generalized aggressive periodontitis, metronidazole and amoxicillin, nonsurgical periodontal therapy, scaling and root planning ...

  8. Effect of Amoxicillin Use on Oral Microbiota in Young Children

    OpenAIRE

    Ready, D.; Lancaster, H.; Qureshi, F; Bedi, R.; Mullany, P; Wilson, M

    2004-01-01

    Dental plaque samples from 40 children were screened for the presence of bacteria resistant to amoxicillin. Fifteen children had used amoxicillin and 25 had not used any antibiotic in the 3 months prior to sample collection. All (100%) of the children harbored amoxicillin-resistant oral bacteria. The median percentage of the total cultivable oral microbiota resistant to amoxicillin was 2.4% (range, 0.1 to 14.3%) in children without amoxicillin use and 10.9% (range, 0.8 to 97.3%) in children w...

  9. Effect of dosing schemes of amoxicillin on eradication rates of Helicobacter pylori with amoxicillin-based triple therapy.

    Science.gov (United States)

    Furuta, Takahisa; Sugimoto, Mitsushige; Yamade, Mihoko; Uotani, Takahiro; Sahara, Shu; Ichikawa, Hitomi; Yamada, Takanori; Osawa, Satoshi; Sugimoto, Ken; Watanabe, Hiroshi; Umemura, Kazuo

    2014-03-01

    In standard regimens for Helicobacter pylori infection, amoxicillin is dosed twice daily, although the bactericidal effect of amoxicillin depends on the %time-above-MIC. We aimed to examine whether dosing schemes of amoxicillin influenced eradication rates of amoxicillin-based regimens. One hundred eighty-seven patients infected with clarithromycin-sensitive strains of H. pylori were treated with PPI, clarithromycin 200 mg bid and amoxicillin 750 mg bid, 500 mg tid or 500 mg qid for 1 week and 125 infected with clarithromycin-resistant strains were treated with PPI, metronidazole 250 mg bid and amoxicillin 750 mg bid, 500 mg tid or 500 mg qid for 1 week. Eradication rates (ITT) of the triple PPI/amoxicillin/clarithromycin therapy with bid, tid and qid dosings of amoxicillin were 77.8% (49/63), 93.5% (58/62), and 91.9% (57/62), respectively. Those of the triple PPI/amoxicillin/metronidazole therapy were 80.5% (33/41), 90.5% (38/42), and 95.2% (40/42), respectively. Eradication rates in regimens with tid and qid dosing of amoxicillin were higher than those of regimens with the bid dosing of amoxicillin. The dosing scheme of amoxicillin significantly influenced eradication rates of triple therapies. Although amoxicillin is empirically dosed twice daily, amoxicillin should be dosed at least three times daily in amoxicillin-based triple therapies. © 2013, The American College of Clinical Pharmacology.

  10. Decomposition and mineralization of amoxicillin by high ionizing energy

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Dong Kyu; Yu, Seung Ho; Lee, Myun Joo [Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup (Korea, Republic of); Jeong, Seung Woo [Dept. of Environmental Engineering, Kunsan National University, Kunsan (Korea, Republic of)

    2007-05-15

    The presence of antibiotics in aquatic environment has been concerning as a new environment pollutant problem. The aim of this study was to evaluate the degradation of antibiotics by gamma irradiation. Amoxicillin as one of β-lactam antibiotics is widely used for both human and animals. To compare the removal efficiencies of amoxicillin, amoxicillin solutions were saturated or purged with three difference gases; N{sub 2}O, O{sub 2} and N{sub 2} separately. The amoxicillin solutions were irradiated at up to 100 kGy. Amoxicillin was completely degraded between 20 and 40 kGy. Especially, amoxicillin saturated with N2O showed the highest degradation rate, and 90% TOC removal efficiency. The enhanced radiolytic decomposition of amoxicillin can be explained by the reactions with oxidizing radicals such as ∙OH and O{sub 2}∙{sup -}/HO{sub 2}∙ radicals.

  11. The synergy and mode of action of quercetin plus amoxicillin against amoxicillin-resistant Staphylococcus epidermidis.

    Science.gov (United States)

    Siriwong, Supatcharee; Teethaisong, Yothin; Thumanu, Kanjana; Dunkhunthod, Benjawan; Eumkeb, Griangsak

    2016-08-04

    Staphylococcus epidermidis is one of the most multiple resistances to antibiotics in the recent years. Therefore, practically-prescribed antibiotics in the treatment of these strains are not effective. Plant-derived antibacterial is one of the most interesting sources of new therapeutics. The present study was to investigate antibacterial, synergy and modes of action of quercetin and amoxicillin against amoxicillin-resistant Staphylococcus epidermidis (ARSE). The MICs, checkerboard assay, viability curves, cytoplasmic membrane (CM) permeability, enzyme assay, transmission electron microscopy, confocal microscopy and FT-IR microspectroscopy measurement was performed. The MICs of amoxicillin, penicillin, quercetin and kaempferol against all ARSE strains were 16, 200, 256-384 and >1024 μg/mL respectively. Synergistic effects were exhibited on amoxicillin plus quercetin and penicillin plus kaempferol against these strains at FIC index 0.50 and <0.38 respectively. The synergistic activity of quercetin plus amoxicillin was confirmed by the viable count. This combination increased CM permeability, caused marked morphological, peptidoglycan and cytoplasmic membrane damage, increased protein amide I and II, but decreased fatty acid in bacterial cells. The quercetin had an inhibitory activity against β-lactamase. So, these findings are the first report that quercetin has the synergistic effect with amoxicillin against ARSE via four modes of actions, inhibit peptidoglycan synthesis and β-lactamases activity, increase CM permeability and protein amide I and II but decrease fatty acid in bacterial cells. Of course, this flavonol has the dominant potential to develop a brand-new collateral phytochemical agent plus amoxicillin to treat ARSE. Future work should focus on the bioavailability, efficacy and toxicity in animal and human studies, as well as, the synergistic effect on blood and tissue should be evaluated and achieved.

  12. Magnetic molecularly imprinted polymer for aspirin recognition and controlled release

    Science.gov (United States)

    Kan, Xianwen; Geng, Zhirong; Zhao, Yao; Wang, Zhilin; Zhu, Jun-Jie

    2009-04-01

    Core-shell structural magnetic molecularly imprinted polymers (magnetic MIPs) with combined properties of molecular recognition and controlled release were prepared and characterized. Magnetic MIPs were synthesized by the co-polymerization of methacrylic acid (MAA) and trimethylolpropane trimethacrylate (TRIM) around aspirin (ASP) at the surface of double-bond-functionalized Fe3O4 nanoparticles in chloroform. The obtained spherical magnetic MIPs with diameters of about 500 nm had obvious superparamagnetism and could be separated quickly by an external magnetic field. Binding experiments were carried out to evaluate the properties of magnetic MIPs and magnetic non-molecularly imprinted polymers (magnetic NIPs). The results demonstrated that the magnetic MIPs had high adsorption capacity and selectivity to ASP. Moreover, release profiles and release rate of ASP from the ASP-loaded magnetic MIPs indicated that the magnetic MIPs also had potential applications in drug controlled release.

  13. Magnetic molecularly imprinted polymer for aspirin recognition and controlled release

    Energy Technology Data Exchange (ETDEWEB)

    Kan Xianwen; Geng Zhirong; Zhao Yao; Wang Zhilin; Zhu Junjie [State Key Laboratory of Coordination Chemistry, MOE Key Lab of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, 22 Hankou Road, Nanjing 210093 (China)], E-mail: wangzl@nju.edu.cn, E-mail: jjzhu@nju.edu.cn

    2009-04-22

    Core-shell structural magnetic molecularly imprinted polymers (magnetic MIPs) with combined properties of molecular recognition and controlled release were prepared and characterized. Magnetic MIPs were synthesized by the co-polymerization of methacrylic acid (MAA) and trimethylolpropane trimethacrylate (TRIM) around aspirin (ASP) at the surface of double-bond-functionalized Fe{sub 3}O{sub 4} nanoparticles in chloroform. The obtained spherical magnetic MIPs with diameters of about 500 nm had obvious superparamagnetism and could be separated quickly by an external magnetic field. Binding experiments were carried out to evaluate the properties of magnetic MIPs and magnetic non-molecularly imprinted polymers (magnetic NIPs). The results demonstrated that the magnetic MIPs had high adsorption capacity and selectivity to ASP. Moreover, release profiles and release rate of ASP from the ASP-loaded magnetic MIPs indicated that the magnetic MIPs also had potential applications in drug controlled release.

  14. Nutritional effects of folic acid controlled release from mesoporous materials

    OpenAIRE

    Barat, José; Pérez-Esteve, Édgar; Bernardos,Andrea; Martínez-Mañez, Ramón

    2011-01-01

    [EN] Folic acid deficiency causes serious disorders in humans and supplementation has numerous health benefits. However, there is initial evidence that suggest a negative impact of an increased exposure to folic with respect to certain developmental and degenerative disorders. In this line, controlled release of folic acid by using mesoporous silica materials, MCM-41, has been studied as an alternative to direct supplementation. For this purpose, various mesoporous solids MCM-41 loaded with f...

  15. Encapsulation and Controlled Release of Pharmaceuticals with Biodegradable Hyperbranched Polyesters

    OpenAIRE

    Mallepally, Rajendar Reddy

    2009-01-01

    The main aim of this work is to prepare enzyme triggered controlled release systems based on hyperbranched polyesters. Attempts to encapsulate drugs with the synthetic polymers often require the use of organic solvents, which is an obstacle for pharmaceutical applications. In this work a solvent free method, called melt dispersion, is used for this purpose. This method is based on the emulsification of the polymer melt and is firstly applied to hyperbranched polymers. The investigated drug su...

  16. Encapsulated Urea-Kaolinite Nanocomposite for Controlled Release Fertilizer Formulations

    OpenAIRE

    Siafu Ibahati Sempeho; Hee Taik Kim; Egid Mubofu; Alexander Pogrebnoi; Godlisten Shao; Askwar Hilonga

    2015-01-01

    Urea controlled release fertilizer (CRF) was prepared via kaolinite intercalation followed by gum arabic encapsulation in an attempt to reduce its severe losses associated with dissolution, hydrolysis, and diffusion. Following the beneficiation, the nonkaolinite fraction decreased from 39.58% to 0.36% whereas the kaolinite fraction increased from 60.42% to 99.64%. The X-ray diffractions showed that kaolinite was a major phase with FCC Bravais crystal lattice with particle sizes ranging betwee...

  17. Stimuli-Responsive Materials for Controlled Release Applications

    KAUST Repository

    Li, Song

    2015-04-01

    The controlled release of therapeutics has been one of the major challenges for scientists and engineers during the past three decades. To address this outstanding problem, the design and fabrication of stimuli-responsive materials are pursued to guarantee the controlled release of cargo at a specific time and with an accurate amount. Upon applying different stimuli such as light, magnetic field, heat, pH change, enzymes or redox, functional materials change their physicochemical properties through physical transformation or chemical reactions, allowing the release of payload agents on demand. This dissertation studied three stimuli-responsive membrane systems for controlled release from films of macro sizes to microcapsules of nano sizes. The first membrane system is a polymeric composite film which can decrease and sustain diffusion upon light irradiation. The photo-response of membranes is based on the photoreaction of cinnamic derivatives. The second one is composite membrane which can improve diffusion upon heating. The thermo-response of membranes comes from the volume phase transition ability of hydrogels. The third one is microcapsule which can release encapsulated agents upon light irradiation. The photo-response of capsules results from the photoreaction of nitrobenzyl derivatives. The study on these membrane systems reveals that stimuli-responsive release can be achieved by utilizing different functional materials on either macro or micro level. Based on the abundant family of smart materials, designing and fabricating stimuli-responsive systems shall lead to various advanced release processes on demand for biomedical applications.

  18. Controlled release for local delivery of drugs: barriers and models.

    Science.gov (United States)

    Weiser, Jennifer R; Saltzman, W Mark

    2014-09-28

    Controlled release systems are an effective means for local drug delivery. In local drug delivery, the major goal is to supply therapeutic levels of a drug agent at a physical site in the body for a prolonged period. A second goal is to reduce systemic toxicities, by avoiding the delivery of agents to non-target tissues remote from the site. Understanding the dynamics of drug transport in the vicinity of a local drug delivery device is helpful in achieving both of these goals. Here, we provide an overview of controlled release systems for local delivery and we review mathematical models of drug transport in tissue, which describe the local penetration of drugs into tissue and illustrate the factors - such as diffusion, convection, and elimination - that control drug dispersion and its ultimate fate. This review highlights the important role of controlled release science in development of reliable methods for local delivery, as well as the barriers to accomplishing effective delivery in the brain, blood vessels, mucosal epithelia, and the skin. Copyright © 2014 Elsevier B.V. All rights reserved.

  19. Amoxicillin in a biological water recovery system

    Energy Technology Data Exchange (ETDEWEB)

    Morse, A.; Jackson, A.; Rainwater, K. [Texas Tech Univ., Water Resources Center, Lubbock, Texas (United States); Pickering, K. [Johnson Space Center, NASA, Houston, Texas (United States)

    2002-06-15

    Pharmaceuticals are new contaminants of concern in the aquatic environment, having been identified in groundwater, surface water, and residential tap water. Possible sources of pharmaceuticals include household wastewaters, runoff from feedlots, or waste discharges from pharmaceutical manufacturing plants. When surface water or groundwater supplies impacted by pharmaceuticals are used in drinking water production, the contaminants may reduce drinking water quality. Many pharmaceuticals, such as amoxicillin, pass through the body largely unmetabolized and directly enter wastewater collection systems. Pharmaceuticals are designed to persist in the body long enough to have the desired therapeutic effect. Therefore, they may also have the ability to persist in the environment (Seiler et al, 1999). The purpose of this work is to determine the overall transformation potential of a candidate pharmaceutical in wastewater treatment with specific emphasis on recycle systems. Amoxicillin is the selected pharmaceutical agent, an orally absorbed broad-spectrum antibiotic with a variety of clinical uses including ear, nose, and throat infections and lower respiratory tract infections. Experiments were conducted using an anaerobic reactor (with NO{sub 3}{sup -} and NO{sub 2}{sup -} as the e{sup -} acceptors) followed by a two-phase nitrifying tubular reactor. Influent composed of water, urine and surfactant was spiked with amoxicillin and fed into the wastewater recycle system. The concentration of amoxicillin in the feed and effluent was quantified using an HPLC. Results from this study include potential for long-term buildup in recycled systems, accumulation of breakdown products and possible transfer of antibiotic resistance to microorganisms in the system effluent. In addition, the results of this study may provide information on contamination potential for communities that are considering supplementing drinking water supplies with recovered wastewater or for entities

  20. Amoxicillin functionalized gold nanoparticles reverts MRSA resistance.

    Science.gov (United States)

    Kalita, Sanjeeb; Kandimalla, Raghuram; Sharma, Kaustav Kalyan; Kataki, Amal Chandra; Deka, Manab; Kotoky, Jibon

    2016-04-01

    In this study, we have described the biosynthesis of biocompatible gold nanoparticles (GNPs) from aqueous extract of the aerial parts of a pteridophyte, "Adiantum philippense" by microwave irradiation and its surface functionalization with broad spectrum beta lactam antibiotic, amoxicillin (Amox). The functionalization of amoxicillin on GNPs (GNP-Amox) was carried out via electrostatic interaction of protonated amino group and thioether moiety mediated attractive forces. The synthesized GNPs and GNP-Amox were physicochemically characterized. UV-Vis spectroscopy, Zeta potential, XRD, FTIR and SERS (surface enhanced raman spectra) results confirmed the loading of Amox into GNPs. Loading of Amox to GNPs reduce amoxicillin cytotoxicity, whereas GNPs were found to be nontoxic to mouse fibroblast cell line (L929) as evident from MTT and acridine orange/ethidium bromide (AO/EtBr) live/dead cell assays. The GNP-Amox conjugates demonstrated enhanced broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Furthermore, in-vitro and in-vivo assays of GNP-Amox revealed potent anti-MRSA activity and improved the survival rate. This indicates the subversion of antibiotic resistance mechanism by overcoming the effect of high levels of β-lactamase produced by methicillin resistant Staphylococcus aureus (MRSA). Taken together, this study demonstrates the positive attributes from GNP-Amox conjugates as a promising antibacterial therapeutic agent against MRSA as well as other pathogens. Copyright © 2016 Elsevier B.V. All rights reserved.

  1. Subcutaneous Zygomycosis Basidiobolomycosis

    Directory of Open Access Journals (Sweden)

    Sethuraman G

    2001-01-01

    Full Text Available Subcutaneous zygomycosis, also known as basidiobolomycosis, is a rare disease caused by the fungus Basidiobolus ranarum. Since its first description in 1954, may cases have been reported. In India, so far only few cases have been described. We report this entity in a 3 year- old female child who had firm to hard swelling of the right upper extremely and chest. Histopathology showed short aseptate hyphae surrounded by eosinophilic material within the granulomatous tissue response, in the subcutaneous tissue. She responded dramatically to saturated solution of potassium iodide.

  2. Amoxicillin pulsatile - MiddleBrook: APC 111, APC-111, PULSYS-enhanced amoxicillin.

    Science.gov (United States)

    2007-01-01

    MiddleBrook Pharmaceuticals (formerly Advancis Pharmaceutical) is developing an improved version of amoxicillin using its pulsatile oral drug delivery technology, called PULSYS. Amoxicillin PULSYS is intended to provide a lower treatment dose, once-daily alternative to currently approved amoxicillin and penicillin regimens for the treatment of adolescents/adults with pharyngitis and/or tonsillitis. If amoxicillin PULSYS is approved, it will be the first and only once-daily amoxicillin therapy approved for use in the US. Regulatory submissions for the treatment of pharyngitis/tonsillitis have been made in the US. Amoxicillin PULSYS is in clinical development for the treatment of pharyngitis and/or tonsillitis due to group A streptococcal infections in adolescents/adults as a tablet formulation. MiddleBrook was conducting clinical development of a sprinkle formulation for children. However, this has been put on hold for financial reasons. MiddleBrook is seeking regulatory approval for this product as a 505(b)(2) product, which is one that is not considered to be a completely new product, but is also not a generic product. It is a product with some differences from a previously approved product and clinical data to support such differences are required; however, the basic safety and efficacy studies may have been conducted by other organisations. In June 2007, Advancis Pharmaceutical was renamed as MiddleBrook Pharmaceuticals, Inc. MiddleBrook and Par Pharmaceuticals entered a co-promotion agreement for this product in June 2004. Par was to fund future development in exchange for co-exclusive marketing rights and exclusive rights to sell amoxicillin PULSYS. MiddleBrook retained responsibility for the manufacturing programme and also retained all patents and brand names and was responsible for their enforcement. However, this collaboration was subsequently terminated in August 2005 by Par Pharmaceutical. MiddleBrook received the US $4.75 million R&D reimbursement

  3. Formulation, characterization and physicochemical evaluation of amoxicillin effervescent tablets

    OpenAIRE

    Abolfazl Aslani; Tahereh Sharifian

    2014-01-01

    Background: Amoxicillin is a semisynthetic antibiotic, which is used as an antimicrobial drug. This study was designed to formulate amoxicillin effervescent tablets, aimed at improved patient compliance and increased drug stability. Materials and Methods: In this study, nine effervescent tablet formulations were prepared from amoxicillin trihydrate. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Powders and granules were evaluated for their p...

  4. Subcutaneous encapsulated fat necrosis

    DEFF Research Database (Denmark)

    Aydin, Dogu; Berg, Jais O

    2016-01-01

    We have described subcutaneous encapsulated fat necrosis, which is benign, usually asymptomatic and underreported. Images have only been published on two earlier occasions, in which the necrotic nodules appear "pearly" than the cloudy yellow surface in present case. The presented image may help...

  5. Subcutaneous granuloma annulare

    Directory of Open Access Journals (Sweden)

    Dhar Sandipan

    1994-01-01

    Full Text Available Two cases of subcutaneos granuloma annulare are reported. Clinical presentation was in the form of hard subcutaneous nodules; histopathology confirmed the clinical diagnosis. The cases were unique because of onset in adult hood, occurrence over unusual sites and absence of classical lesions of granuloma annulare elsewhere.

  6. FERLENT - a controlled release fertilizer produced from a polymer material

    Energy Technology Data Exchange (ETDEWEB)

    NONE

    2011-07-01

    The possibility to use release controlled fertilizers in the agriculture of the tropical countries is more important than in the agriculture of the countries of the template regions. In this context, this work purpose the development of a new Fertilizer of Controlled Release named FERLENT, which was obtained starting from a polymeric material, under controlled conditions which allowed to corroborate the adjustment of the synthesis parameters under the modulate of nutrients liberation. It was characterized by, Scanning Microscopy Electron (SEM), Thermogravimetric analysis (TGA), Nuclear Magnetic Resonance (NMR) and infrared spectroscopy (FTIR). (author)

  7. 75 FR 76016 - Determination That AUGMENTIN `125' (Amoxicillin; Clavulanate Potassium) Chewable Tablet and Six...

    Science.gov (United States)

    2010-12-07

    ... HUMAN SERVICES Food and Drug Administration Determination That AUGMENTIN `125' (Amoxicillin; Clavulanate Potassium) Chewable Tablet and Six Other AUGMENTIN (Amoxicillin; Clavulanate Potassium) Drug Products Were... (amoxicillin; clavulanate potassium) drug products listed in this notice were not withdrawn from sale for...

  8. Controlled Release of Imidacloprid from Poly Styrene-Diacetone - Nanoformulation

    Science.gov (United States)

    Qian, Kun; Guo, Yanzhen; He, Lin

    2012-01-01

    Imidacloprid is a neonicotinoids insecticide, which is important for the cash crops such as tomato, rape and so on. The conventional formulation does not only increase the loss of pesticide but also leads to environmental pollution. Controlled-release formulations of pesticide are highly desirable not only for attaining the most effective utilization of the pesticide, but also for reducing environmental pollution. Pesticide imidacloprid was incorporated in poly (styrene-diacetone crylamide)-based formulation to obtain controlled release properties, and the imidacloprid nanocontrolled release formulation was characterized by infrared (IR) and field emission scanning electron microscope (FESEM). Factors related to loading efficiency, swelling and release behaviors of the formulation were investigated. It showed that the loading efficiency could reach about 40% (w/w). The values for the diffusion exponent "n" were in the range of 0.31-0.58, which indicated that the release of imidacloprid was diffusion-controlled. The time taken for 50% of the active ingredient to be released into water, T50, was also calculated for the comparison of formulations in different conditions. The results showed that the formulation with higher temperature and more diacetone crylamide had lower value of T50, which means a quicker release of the active ingredient. This study highlighted some pieces of evidence that improved pesticide incorporation and slower release were linked to potential interactions between the pesticide and the polymer.

  9. Controlled Release of Agrochemicals Intercalated into Montmorillonite Interlayer Space

    Science.gov (United States)

    2014-01-01

    Periodic application of agrochemicals has led to high cost of production and serious environmental pollution. In this study, the ability of montmorillonite (MMT) clay to act as a controlled release carrier for model agrochemical molecules has been investigated. Urea was loaded into MMT by a simple immersion technique while loading of metalaxyl was achieved by a rotary evaporation method. The successful incorporation of the agrochemicals into the interlayer space of MMT was confirmed by several techniques, such as, significant expansion of the interlayer space, reduction of Barrett-Joyner-Halenda (BJH) pore volumes and Brunauer-Emmett-Teller (BET) surface areas, and appearance of urea and metalaxyl characteristic bands on the Fourier-transform infrared spectra of the urea loaded montmorillonite (UMMT) and metalaxyl loaded montmorillonite (RMMT) complexes. Controlled release of the trapped molecules from the matrix was done in water and in the soil. The results reveal slow and sustained release behaviour for UMMT for a period of 10 days in soil. For a period of 30 days, MMT delayed the release of metalaxyl in soil by more than 6 times. It is evident that MMT could be used to improve the efficiency of urea and metalaxyl delivery in the soil. PMID:24696655

  10. Controlled Release of Agrochemicals Intercalated into Montmorillonite Interlayer Space

    Directory of Open Access Journals (Sweden)

    Harrison Wanyika

    2014-01-01

    Full Text Available Periodic application of agrochemicals has led to high cost of production and serious environmental pollution. In this study, the ability of montmorillonite (MMT clay to act as a controlled release carrier for model agrochemical molecules has been investigated. Urea was loaded into MMT by a simple immersion technique while loading of metalaxyl was achieved by a rotary evaporation method. The successful incorporation of the agrochemicals into the interlayer space of MMT was confirmed by several techniques, such as, significant expansion of the interlayer space, reduction of Barrett-Joyner-Halenda (BJH pore volumes and Brunauer-Emmett-Teller (BET surface areas, and appearance of urea and metalaxyl characteristic bands on the Fourier-transform infrared spectra of the urea loaded montmorillonite (UMMT and metalaxyl loaded montmorillonite (RMMT complexes. Controlled release of the trapped molecules from the matrix was done in water and in the soil. The results reveal slow and sustained release behaviour for UMMT for a period of 10 days in soil. For a period of 30 days, MMT delayed the release of metalaxyl in soil by more than 6 times. It is evident that MMT could be used to improve the efficiency of urea and metalaxyl delivery in the soil.

  11. Study on acute toxicity of amoxicillin wastewater to Zebrafish

    Science.gov (United States)

    Xie, Weifang; Shen, Hongyan

    2017-12-01

    The main research in this paper is to obtain the effect of pharmaceutical wastewater on the acute toxicity of Zebrafish. The experimental method of exposure is used in this research. Experiments were carried out with different groups of pharmaceutical wastewater. Zebrafish was cultivated in a five liter fish tank. In the experiment, according to mortality, initially a 96h preliminary test was carried out at exposure concentrations to determine if the amoxicillin wastewater was toxic and to define the concentration range (24h LC100, 96h LC0) to be employed in the definitive tests. Based on the half lethal concentration of Zebrafish, the acute toxicity of amoxicillin wastewater to Zebrafish was calculated and the toxicity grade of wastewater was determined. In the experiment, the Zebrafish was exposed with amoxicillin wastewater during 96h. The 24h, 48h, 72h and 96h LC50 of amoxicillin wastewater on the Zebrafish were 63.10%, 53.70%, 41.69% and 40.74%, respectively. At 96h, the test time is the longest, and the value of LC50 is the smallest. In the observation period of 96 hours, the LC50 of amoxicillin wastewater were in the range of 40% ~ 60% and the value of Tua is 1 ~ 2. It indicates amoxicillin wastewater is low toxic wastewater when the experimental time is shorter than 48h, amoxicillin wastewater is moderate toxicity wastewater when the experimental time is higher than 48h. According to the experimental data, with the exposure time and the volume percentage of amoxicillin wastewater increases, the mortality rate of Zebrafish is gradually increased and the toxicity of amoxicillin wastewater increases. It indicates that the toxicity of amoxicillin wastewater is the biggest and the effect of wastewater on Zebrafish is greatest. In some ways, the toxicity of amoxicillin wastewater can be affected by the test time.

  12. Massive subcutaneous emphysema with pneumoscrotopenis ...

    African Journals Online (AJOL)

    Chest injury commonly leads to subcutaneous emphysema of the chest, neck and face. It is usually non-life threatening. Massive subcutaneous emphysema may occur and very rarely may spread to involve the scrotal sac and subcutaneous tissue planes of the penis to cause pneumoscrotopenis. This case report presents ...

  13. Subcutaneous bronchogenic cyst

    Directory of Open Access Journals (Sweden)

    Vivek Manchanda

    2010-01-01

    Full Text Available Bronchogenic cysts occur due to the anomalous development of the primitive tracheobronchial tree early in fetal life. They are usually present in middle mediastinum. Rarely, they have been found in other locations. We describe two patients with subcutaneous bronchogenic cysts located over manubrium sterni with special emphasis on the difficulties in pre-operative diagnosis. The two boys were managed by complete excision of the cysts. The children are well on follow-up.

  14. Relative bioequivalence of amoxicillin dissolved in breast milk.

    Science.gov (United States)

    Yazdani-Brojeni, Parvaneh; Garcia-Bournissen, Facundo; Fujii, Hisaki; Tanoshima, Reo; Ito, Shinya

    2014-03-01

    Oral antibiotics use in infants in developing countries is challenging because liquid formulations are often unavailable. However, dissolving solid formulation of drugs in water poses a risk of gastrointestinal infection. Although mother's milk may be a potential vehicle, no evidence exists to indicate that antibiotics dissolved in human milk are bioequivalent to those dissolved in water. Therefore, we compared pharmacokinetic parameters of an orally administered antibiotic, amoxicillin, dissolved in human milk, to those of water-dissolved amoxicillin. A pharmacokinetic study was conducted in 16 healthy adult volunteers in a randomised crossover design. Marketed amoxicillin powder for suspension was dissolved in either human milk or water at a final concentration of 50 mg/mL, and 10 mL was given orally in a fasting state. Timed blood samples were obtained and plasma amoxicillin was quantified using liquid chromatography-mass spectrometry. Results showed that pharmacokinetic parameters, including area-under-the-curve, Cmax and half-life of the water-based and milk-based amoxicillin administration were not significantly different. 90% CIs of the ratios of these parameters in concomitant breast milk administration to those of water were within 89% and 116%, suggesting they are bioequivalent (defined as a range between 80% and 125%). We conclude that oral administration of amoxicillin dissolved in human milk at 50 mg/mL results in pharmacokinetics profiles comparable to amoxicillin dissolved in water. Pharmaceutical interactions between amoxicillin and breast milk are unlikely, suggesting no need to modify dosing schedules.

  15. Impact of oral and intramuscular administration amoxicillin on the ...

    African Journals Online (AJOL)

    Objective: The aim of this study was to evaluate the level of selection of amoxicillin-resistant Enterobacteriaceae in the digestive microbiota of piglets during oral and intramuscular administration of amoxicillin. Methodology and Results: Enumeration of Enterobacteriaceae was carried out on MacConkey agar with and ...

  16. 21 CFR 520.88 - Amoxicillin oral dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin oral dosage forms. 520.88 Section 520...) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.88 Amoxicillin oral dosage forms. ...

  17. Preparation and in vitro evaluation of amoxicillin encapsulated in ...

    African Journals Online (AJOL)

    Purpose: To optimize and characterize amoxicillin encapsulated in mucoadhesive alginate-coated ... microparticles protects acid-labile drugs better from degradation in acidic solution (pH 1.5) than the chitosan microparticles alone. The coating also acts as a barrier from ..... the amoxicillin-loaded nanoparticles in the gastric.

  18. Reversible and competitive inhibitory kinetics of amoxicillin on mushroom tyrosinase.

    Science.gov (United States)

    Chen, Xiao-Xin; Zhang, Jian; Chai, Wei-Ming; Feng, Hui-Ling; Xiang, Zhi-Hao; Shen, Dong-Yan; Chen, Qing-Xi

    2013-11-01

    In the present work, we investigated the inhibitory effects of amoxicillin, a bacteriolytic β-lactam antibiotic drug, on the rate of monophenol hydroxylation and o-diphenol oxidation catalyzed by mushroom tyrosinase. The results showed that amoxicillin could inhibit both monophenolase and diphenolase activities. For monophenolase activity, the inhibition on reaction rate was dose-dependent, while the influence on lag period was not obvious. For diphenolase activity, amoxicillin was found to be a reversible inhibitor, with an IC50 value of 9.0 ± 1.8 mM. Kinetics analysis showed that amoxicillin was a mixed type inhibitor of the enzyme with KI and KIS values of 8.30 mM and 44.79 mM, respectively. Further, the molecular mechanism underlying the inhibition of tyrosinse by amoxicillin was investigated by means of fluorescence quenching and molecular docking techniques. The results showed that amoxicillin could form static interaction with the catalytic pocket of the enzyme through the interaction of amoxicillin with the dicopper irons and amino acid residues in the enzyme active center. Our results contributed to the usage of amoxicillin as a potential tyrosinase inhibitor in the field of medicinal industry and could also provide guidance in the design of novel tyrosinase inhibitors. Copyright © 2013. Published by Elsevier B.V.

  19. In vivo Evaluation of Amoxicillin Trihydrate and Clarithromycin ...

    African Journals Online (AJOL)

    Purpose: To evaluate in vivo H. pylori clearance efficacy of formulated mucoadhesive microspheres of amoxicillin trihydrate and clarithromycin. Methods: Amoxicillin trihydrate and clarithromycin mucoadhesive microspheres were prepared by solvent evaporation method using Carbopol 974P, HPMC K4M and Eudragit RS ...

  20. Evaluation of drug Quality II: Determination of Amoxicillin ...

    African Journals Online (AJOL)

    Statistical analysis of data showed that there was no significant difference between the two methods used in this study and the amoxicillin samples studied were not significantly different from one another. Keywords: Amoxicillin concentration, capsules, spectrophotometric/titrimetric methods. International Journal of Natural ...

  1. Post-marketing stability surveillance: Amoxicillin | Naidoo | South ...

    African Journals Online (AJOL)

    The mini-survey identified four types of packaging in which amoxicillin capsules are dispensed – plastic packets, flip-top amber bottles, flip-top amber bottles with cotton wool and flip-top transparent bottles with cotton wool. The laboratory analyses showed that only those amoxicillin capsules stored between 20 and 25 0C ...

  2. 21 CFR 520.88d - Amoxicillin trihydrate soluble powder.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin trihydrate soluble powder. 520.88d Section 520.88d Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... trihydrate soluble powder. (a) Specifications. Each gram contains amoxicillin trihydrate equivalent to 115.4...

  3. Design and characterization of controlled release tablet of metoprolol

    Directory of Open Access Journals (Sweden)

    Gautam Singhvi

    2012-01-01

    Full Text Available Metoprolol succinate is a selective beta-adrenergic receptor blocker useful in treatment of hypertension, angina and heart failure. The purpose of the present work was to design and evaluate controlled release matrix type tablet of Metoprolo succinate using HPMC K15M and Eudragit (RLPO and RSPO as a matrix forming agents. Effect of various polymer alone and combinations were studied in pH 1.2 buffer using USP type II paddle at 50 rpm. HPMC was used to form firm gel with Eudragit polymer. Formulation with Equal proportion (1:1 of Eudragit RSPO and RLPO showed optimum drug release t50 =7 hrs and t100 =16 hrs indicate optimum permeability for drug release from matrix. The drug release mechanism was predominantly found to be Non-Fickian diffusion controlled.

  4. Chitosan Hydrogels for Chondroitin Sulphate Controlled Release: An Analytical Characterization

    Directory of Open Access Journals (Sweden)

    Annalisa Bianchera

    2014-01-01

    Full Text Available This paper provides an analytical characterization of chitosan scaffolds obtained by freeze-gelation toward the uptake and the controlled release of chondroitin sulphate (CS, as cartilage repair agent, under different pH conditions. Scanning electron microscopy (SEM, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR, and liquid chromatography-UV spectrophotometry (LC-UV techniques were exploited to obtain qualitative and quantitative descriptions of polymer and drug behaviour in the biomaterial. As for morphology, SEM analysis allowed the evaluation of scaffold porosity in terms of pore size and distribution both at the surface (Feret diameter 58±19 μm and on the cross section (Feret diameter 106±51 μm. LC and ATR-FTIR evidenced a pH-dependent CS loading and release behaviour, strongly highlighting the role of electrostatic forces on chitosan/chondroitin sulphate interactions.

  5. Controlled Release System for Localized and Sustained Drug Delivery Applications

    Science.gov (United States)

    Rodriguez, Lidia Betsabe

    Current controlled release formulations has many drawbacks such as excess of initial burst release, low drug efficiency, non-degradability of the system and low reproducibility. The present project aims to offer an alternative by developing a technique to prepare uniform, biodegradable particles ( ˜19 mum ) that can sustainably release a drug for a specific period of time. Chitosan is a natural polysaccharide that has many characteristics to be used for biomedical applications. In the last two decades, there have been a considerable number of studies affirming that chitosan could be used for pharmaceutical applications. However, chitosan suffers from inherent weaknesses such as low mechanical stability and dissolution of the system in acidic media. In the present study, chitosan microparticles were prepared by emulsification process. The model drug chosen was acetylsalicylic acid as it is a small and challenging molecule. The maximum loading capacity obtained for the microparticles was approximately 96%. The parameters for the preparation of uniform particles with a narrow size distribution were identified in a triangular phase diagram. Moreover, chitosan particles were successfully coated with thin layers of poly lactic-coglycolic acid (PLGA) and poly lactic acid (PLA). The performance of different layerswas tested for in vitro drug release and degradation studies. Additionally, the degradability of the system was evaluated by measuring the weight loss of the system when exposed to enzyme and without enzyme. Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), atomic force microscopy (AFM) and inductively coupled plasma optical emission spectrometry (ICP-OES) were used to characterize the controlled release system. Additionally, the in vitro drug release was monitored by ultraviolet-visible spectrophotometry (UV-Vis) and liquid chromatography mass spectrometry (LC-MS). The results obtained from this project showed that it is

  6. Serum concentrations of amoxicillin in neonates during continuous intravenous infusion.

    Science.gov (United States)

    van Boekholt, A; Fleuren, H; Mouton, J; Kramers, C; Sprong, T; Gerrits, P; Semmekrot, B

    2016-06-01

    Amoxicillin is commonly used for the treatment of neonatal bacterial infection with intermittent dosing (ID) regimens. However, increasing bacterial resistance, in addition to a lack of new antimicrobial agents, urges the optimization of current therapeutic options. Clinical studies in adults suggest continuous infusion (CI) regimens of beta-lactam antibiotics to be superior to ID. There are as yet no guidelines concerning the CI dosing of amoxicillin. The present study was developed to describe the CI pharmacokinetics and -dynamics of amoxicillin during the first 3 days of life in search of the optimal dosing regimen. Neonates with a gestational age above 34 weeks, at risk of neonatal infection and requiring amoxicillin therapy, were included. Serum concentrations of amoxicillin were measured during CI on days 1 and 3 in the steady state. Twenty-two serum samples of 11 patients were collected. All patients reached and retained serum concentrations of amoxicillin within the therapeutic range without exceeding the toxic concentration (serum concentrations on day 1 mean 55.4 mg/l, range 30.9-69.5, SD 10.5, and on day 3 48.8 mg/l, range 25.5-92.4, SD 18.4). There was no significant decrease in concentration from day 1 to day 3 (p = 0.38). This study showed therapeutic, nontoxic concentrations of amoxicillin in neonates on CI of amoxicillin in the first 3 days of life. Randomized controlled trials should reveal whether the clinical benefits of the CI of amoxicillin exceed those of ID regimens.

  7. 21 CFR 520.88a - Amoxicillin trihydrate film-coated tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Amoxicillin trihydrate film-coated tablets. 520... Amoxicillin trihydrate film-coated tablets. (a) Specifications. Each tablet contains amoxicillin trihydrate equivalent to 50, 100, 150, 200, or 400 milligrams of amoxicillin. (b) Sponsor. See No. 000069 in § 510.600(c...

  8. Subcutaneous Phycomycosis in a Child

    Directory of Open Access Journals (Sweden)

    Manjiri R. Naniwadekar

    2009-11-01

    Full Text Available Subcutaneous phycomycosis is a rare entity. We hereby report a case of subcutaneous phycomycosis in 18 months old female child who presented with a painless, non-tender swelling on the thigh. Skin biopsy showed eosinophilic granuloma lying deep in the subcutaneous tissue, with sparse hyphae. Culture on Sabouraud's dextrose agar showed characteristic colonies. Patient was started on oral potassium iodide. The swelling was completely resolved after one month of treatment.

  9. Controlled release of vancomycin from poloxamer 407 gels.

    Science.gov (United States)

    Veyries, M L; Couarraze, G; Geiger, S; Agnely, F; Massias, L; Kunzli, B; Faurisson, F; Rouveix, B

    1999-12-10

    The purpose of this study was to investigate Poloxamer 407 25% (w/w) formulations aimed at prolonging the residence time of vancomycin, a time-dependent antibiotic, in a body site with a high infectious risk. Reversible thermal gelation of the formulations permitted their local injection in liquid form and in situ gelation as they warmed to body temperature. Neither the rheological properties of the Poloxamer matrices nor the antibacterial activity of vancomycin was altered by their combination. In vitro, the dispersed form exhibited prolonged release, with a lower diffusion coefficient of vancomycin compared to the solubilized form (4.7x10(-8) vs 2. 1x10(-7) cm(2) s(-1)131 mg l(-1) for the solubilized form), followed by lower but effective antibacterial levels for at least 8 days. Controlled-release profiles, good preservation of vancomycin activity, good tolerability in rats, and ease of administration suggest that Poloxamer 407 may be useful as a vancomycin delivery vehicle for local prophylaxis of infections, especially in prosthetic surgery.

  10. Encapsulated Urea-Kaolinite Nanocomposite for Controlled Release Fertilizer Formulations

    Directory of Open Access Journals (Sweden)

    Siafu Ibahati Sempeho

    2015-01-01

    Full Text Available Urea controlled release fertilizer (CRF was prepared via kaolinite intercalation followed by gum arabic encapsulation in an attempt to reduce its severe losses associated with dissolution, hydrolysis, and diffusion. Following the beneficiation, the nonkaolinite fraction decreased from 39.58% to 0.36% whereas the kaolinite fraction increased from 60.42% to 99.64%. The X-ray diffractions showed that kaolinite was a major phase with FCC Bravais crystal lattice with particle sizes ranging between 14.6 nm and 92.5 nm. The particle size varied with intercalation ratios with methanol intercalated kaolinite > DMSO-kaolinite > urea-kaolinite (KPDMU. Following intercalation, SEM analysis revealed a change of order from thick compact overlapping euhedral pseudohexagonal platelets to irregular booklets which later transformed to vermiform morphology and dispersed euhedral pseudohexagonal platelets. Besides, dispersed euhedral pseudohexagonal platelets were seen to coexist with blocky-vermicular booklets. In addition, a unique brain-form agglomeration which transformed into roundish particles mart was observed after encapsulation. The nanocomposites decomposed between 48 and 600°C. Release profiles showed that 100% of urea was released in 97 hours from KPDMU while 87% was released in 150 hours from the encapsulated nanocomposite. The findings established that it is possible to use Pugu kaolinite and gum arabic biopolymer to prepare urea CRF formulations.

  11. Controlled release tablet formulation containing natural Δ(9)-tetrahydrocannabinol.

    Science.gov (United States)

    Punyamurthula, Nagendra S; Hingorani, Tushar; Adelli, Goutham; Gul, Waseem; ElSohly, Mahmoud A; Repka, Michael A; Majumdar, Soumyajit

    2016-01-01

    Cannabinoids are increasingly being used in the treatment of chemotherapy-induced nausea and vomiting (CINV) because of their action on the cannabinoid receptors, CB1 and CB2. The currently marketed capsule formulations (sesame oil based and crystalline powder) are required to be administered frequently to maintain therapeutic levels, which leads to non-compliance. In the present study, oral controlled release tablet formulations of Δ(9)-tetrahydrocannabinol (THC) were prepared using the lipids Precirol® and Compritol®. Release profiles using THC-lipid matrices and/or with the lipids in the external phase (blend) were evaluated. The effect of directly compressible diluents lactose mixture (Ludipress®), dicalcium phosphate anhydrous (Emcompress®) and microcrystalline cellulose (Avicel® 102) on tablet characteristics and in vitro drug release was also investigated. Further, in vitro THC release in the presence of a lipase inhibitor, Pluronic® F68, was also studied. A 24 h zero-order THC release profile was obtained with a combination of Precirol® and Compritol® in the compression blend. Addition of Pluronic® F68 did not alter THC release in vitro. These optimized tablets were chemically and physically stable for 3 months, the last time point tested, at 25 °C/60% RH. The overall results demonstrate the feasibility of preparing oral THC tablets for once a day administration which can improve CINV management.

  12. Controlled release of 5-fluorouracil from microporous zeolites.

    Science.gov (United States)

    Spanakis, Marios; Bouropoulos, Nikolaos; Theodoropoulos, Dimitrios; Sygellou, Lamprini; Ewart, Sinead; Moschovi, Anastasia Maria; Siokou, Angeliki; Niopas, Ioannis; Kachrimanis, Kyriakos; Nikolakis, Vladimiros; Cox, Paul A; Vizirianakis, Ioannis S; Fatouros, Dimitrios G

    2014-01-01

    Zeolite particles with different pore diameter and particle size were loaded with the model anticancer drug 5-fluorouracil. The loaded zeolites were characterized by means of SEM, XRD, DSC, XPS, N2 physisorption and FT-IR. Higher loading of 5-FU was observed for NaX-FAU than BEA. Release studies were carried out in HCl 0.1N. Release of 5-FU from NaX-FAU showed exponential-type behaviour with the drug fully released within 10 min. In the case of BEA, the kinetics of 5-FU shows a multi-step profile with prolonged release over time. Molecular dynamics simulations showed that diffusion of the drug molecule through the BEA framework is lower than for NaX-FAU due to increased van der Waals interaction between the drug and the framework. The effect of zeolitic particles on the viability of Caco-2 monolayers showed that the NaX-FAU particles cause a reduction of cell viability in a more pronounced way compared with the BEA particles. This article describes zeolite-based nanoparticles in generating time-controlled release of 5-FU from zeolite preparations for anti-cancer therapy. © 2013.

  13. Modifying sorbents in controlled release formulations to prevent herbicides pollution

    Energy Technology Data Exchange (ETDEWEB)

    Cespedes, F.F.; Sanchez, M.V.; Garcia, S.P.; Perez, M.F. [University of Almeria, Almeria (Spain). Dept. of Inorganic Chemistry

    2007-10-15

    The herbicides chloridazon and metribuzin, identified as groundwater pollutants, were incorporated in alginate-based granules to obtain controlled release properties. In this research the effect of incorporation of sorbents such as bentonite, anthracite and activated carbon in alginate basic formulation were not only studied on encapsulation efficiency but also on the release rate of herbicides which was studied using water release kinetic tests. In addition, sorption studies of herbicides with bentonite, anthracite and activated carbon were made. The kinetic experiments of chloridazon and metribuzin release in water have shown that the release rate is higher in metribuzin systems than in those prepared with chloridazon, which has lower water solubility. Besides, it can be deduced that the use of sorbents reduces the release rate of the chloridazon and metribuzin in comparison to the technical product and to the alginate formulation without sorbents. The highest decrease in release rate corresponds to the formulations prepared with activated carbon as a sorbent. The water uptake, permeability, and time taken for 50% of the active ingredient to be released into water, were calculated to compare the formulations. On the basis of a parameter of an empirical equation used to fit the herbicide release data, the release of chloridazon and metribuzin from the various formulations into water is controlled by a diffusion mechanism.

  14. Subcutaneous adipose tissue classification

    Directory of Open Access Journals (Sweden)

    A. Sbarbati

    2010-11-01

    Full Text Available The developments in the technologies based on the use of autologous adipose tissue attracted attention to minor depots as possible sampling areas. Some of those depots have never been studied in detail. The present study was performed on subcutaneous adipose depots sampled in different areas with the aim of explaining their morphology, particularly as far as regards stem niches. The results demonstrated that three different types of white adipose tissue (WAT can be differentiated on the basis of structural and ultrastructural features: deposit WAT (dWAT, structural WAT (sWAT and fibrous WAT (fWAT. dWAT can be found essentially in large fatty depots in the abdominal area (periumbilical. In the dWAT, cells are tightly packed and linked by a weak net of isolated collagen fibers. Collagenic components are very poor, cells are large and few blood vessels are present. The deep portion appears more fibrous then the superficial one. The microcirculation is formed by thin walled capillaries with rare stem niches. Reinforcement pericyte elements are rarely evident. The sWAT is more stromal; it is located in some areas in the limbs and in the hips. The stroma is fairly well represented, with a good vascularity and adequate staminality. Cells are wrapped by a basket of collagen fibers. The fatty depots of the knees and of the trochanteric areas have quite loose meshes. The fWAT has a noteworthy fibrous component and can be found in areas where a severe mechanic stress occurs. Adipocytes have an individual thick fibrous shell. In conclusion, the present study demonstrates evident differences among subcutaneous WAT deposits, thus suggesting that in regenerative procedures based on autologous adipose tissues the sampling area should not be randomly chosen, but it should be oriented by evidence based evaluations. The structural peculiarities of the sWAT, and particularly of its microcirculation, suggest that it could represent a privileged source for

  15. Preparation and in vitro evaluation of amoxicillin encapsulated in ...

    African Journals Online (AJOL)

    Conclusion: The mucoadhesive amoxicillin microparticles may improve the treatment of gastric ulcer caused by H. ... Sodium alginate is also a hydrophilic polymer and comprises ..... microparticles for gastroretentive delivery. Preparation,.

  16. Serum concentrations of amoxicillin in neonates during continuous intravenous infusion

    NARCIS (Netherlands)

    Boekholt, A. van; Fleuren, H.; Mouton, J.; Kramers, C.; Sprong, T.; Gerrits, P.; Semmekrot, B.

    2016-01-01

    Amoxicillin is commonly used for the treatment of neonatal bacterial infection with intermittent dosing (ID) regimens. However, increasing bacterial resistance, in addition to a lack of new antimicrobial agents, urges the optimization of current therapeutic options. Clinical studies in adults

  17. Organoclays for controlled release of the herbicide fenuron.

    Science.gov (United States)

    Hermosin, M C; Calderón, M J; Aguer, J P; Cornejo, J

    2001-09-01

    Organoclays were assayed as matrices in which to associate herbicides, with the aim of decreasing product losses that could give rise to water contamination from agricultural activities. Fenuron was selected as model of a very mobile and highly water-soluble herbicide. Two different organoclays of high (A-HDT) and low (H-C18) reversible fenuron sorption were selected. Herbicide-organoclay complexes were prepared from the two organoclays and with two different fenuron contents (20 and 40 g AI kg-1) and two different mixing times, so as to form a series of weak and strong complexes. The release of fenuron from those complexes into water and water/soil suspensions gave values of T50 (time to release 50% of the fenuron content) ranging from 0.3 min to 2400 h. The total fenuron released in these closed systems ranged from 48 to 80% of the fenuron in the complex. The organoclay type (high or low sorptivity) had the greatest influence on fenuron release, followed by the strong or weak complex, suggesting that herbicide-organoclay interactions are the main factors controlling release. Soil column leaching experiments showed fenuron-organoclay complexes to be effective in reducing the peak herbicide concentration in the leachate to a half (6 microns) or a quarter (3 microns) of that obtained from the free technical compound (12 microns). Herbicide lost through leaching was reduced from 78% for the free technical fenuron to 50-30%, depending on the organoclay used as carrier and the strength of the complex. Bioassay with ryegrass showed that the weak fenuron/H-C18 complex (40 g AI kg-1) gave the same herbicidal activity as technical fenuron. The potential suitability of low-sorptive organoclays for conferring slow-release properties on the fenuron complex has been demonstrated.

  18. Antimicrobial beeswax coated polylactide films with silver control release capacity.

    Science.gov (United States)

    Martínez-Abad, Antonio; Lagarón, Jose Maria; Ocio, María Jose

    2014-03-17

    Although the application of silver based antimicrobial systems is a widespread technology, its implementation in areas such as food packaging is still challenging. The present paper describes the fabrication of poly(lactic acid) (PLA) coated with beeswax with controlled release properties for sustained antimicrobial performance. Release of silver ions from the polymers was monitored voltammetrically under various conditions (surface contact, immersion in various liquid media and at different pH values) throughout at least 7days. A higher release was noted with decreasing pH while surface release was much slower than the release when immersed in liquid medium. While uncoated films demonstrated a high burst release which in some instances implied surpassing some current migration restrictions (<0.05mg/kg food), the addition of a beeswax layer allowed a sustained release of the antimicrobial compound. Increasing the thickness of the beeswax layer resulted in an increase in the water barrier properties of the films while reducing the relatively constant values of sustained release. Antimicrobial performance was correlated with the release of silver ions, indicating threshold concentrations for biocide action of <6μg/L and 9-14μg/L for surface contact and in liquid media, respectively. Either by surface contact or by immersion in growth medium or vegetable soup, the coated films displayed a strong bactericidal effect against Salmonella enterica. The application of this functional barrier thus offers the possibility of tuning the release profiles of the films to suit a specific application and puts forth the possible suitability of these materials for food packaging or other migration sensitive applications. Copyright © 2013 Elsevier B.V. All rights reserved.

  19. Kounis syndrome associated with amoxicillin/clavulanic acid

    Directory of Open Access Journals (Sweden)

    A Shimi

    2016-01-01

    Full Text Available Kounis syndrome (KS is a life-threatening medical condition that causes severes allergic reaction and acute coronary syndrome (ACS. We describe the case of 56-year-old woman who developed ACS following an anaphylactic reaction to amoxicillin/clavulanic acid. Immediately after the administration of amoxicillin/clavulanic acid, she presented a chest pain, cutaneous allergic, hypotension, and ST depression on the electrocardiogram. After the necessary diagnostic test, the final diagnosis was variant I of KS.

  20. Effects of Controlled Release Fertilizer on the Flag Leaves Senescence in Dry-land Wheat

    OpenAIRE

    Dandan Liu; Yan Shi

    2013-01-01

    In order to select a reasonable controlled release fertilizer application method to slow down the senescence of flag leaf in dry-land wheat. The effects of controlled release fertilizer on soluble protein content, MDA content, the Catalase (CAT) activity, the Superoxide Dismutase (SOD) activity on the flag leaves senescence in dry-land wheat had been studied in the open field with the variety wheat Jimai22. The results indicated that, the combination application of controlled release fertiliz...

  1. Maternal Exposure to Amoxicillin and the Risk of Oral Clefts

    Science.gov (United States)

    Lin, Kueiyu Joshua; Mitchell, Allen A.; Yau, Wai-Ping; Louik, Carol; Hernández-Díaz, Sonia

    2013-01-01

    Background Prior studies have suggested an increased risk of oral clefts after exposure to amoxicillin in early pregnancy, but findings have been inconsistent. Methods Among participants in the Slone Epidemiology Center Birth Defects Study from 1994 to 2008, we identified 877 infants with cleft lip with/without cleft palate (CL/P) and 471 with cleft palate alone (CP). Controls included 6952 non-malformed infants. Mothers were interviewed about demographic, reproductive and medical factors, and details of medication use. We estimated odds ratios (ORs) and 95% confidence intervals (CIs) associated with use of amoxicillin in the first trimester using conditional logistic regression and adjusting for known risk factors for oral clefts, as well as for infections, fever, and concomitant treatments. Results In the control group, 3% of women had used amoxicillin in the first trimester. Maternal use of amoxicillin was associated with an increased risk of CL/P (adjusted OR= 2.0 [95% CI= 1.0–4.1]), with an OR of 4.3 (1.4–13.0) for third-gestational-month use. Risks were not elevated for use of other penicillins or cephalosporins. For CP, the OR for first-trimester amoxicillin was 1.0 (0.4–2.3), with an OR of 7.1 (1.4–36.4) for third-gestational-month use. Conclusions Amoxicillin use in early pregnancy may be associated with an increased risk of oral clefts. PMID:22766750

  2. The removal of amoxicillin from wastewater using organobentonite.

    Science.gov (United States)

    Zha, Shuang xing; Zhou, Yan; Jin, Xiaoying; Chen, Zuliang

    2013-11-15

    Organobentonites used as absorbents to remove amoxicillin from wastewater have been investigated here because they are effective in removing organic pollutants. It is evident that bentonite modified with hexadecyl trimethyl ammonium (DK1) can effectively remove amoxicillin from aqueous solution. Batch experiments showed that the adsorption of amoxicillin onto DK1 fitted well to a pseudo second-order kinetic model with corresponding rate constants (0.0187 g/mg min at 20 °C). The Langmuir isotherm provided the highest adsorption capacity (26.18 mg/g at 20 °C). Our thermodynamic study suggested that the adsorption of amoxicillin onto DK1 was physisorptive and endothermic in nature. Furthermore DK1 was characterized by scanning electronic microscopy (SEM), Specific Surface Area (SSA), X-ray powder diffraction (XRD) and Fourier Transform Infrared (FTIR) spectrometer. These characterizations provided evidence of the morphological properties and how well the adsorption process performed. An adsorption mechanism including both ion-exchange and partition was proposed. Finally, DK1 was used to remove amoxicillin from wastewaters and the results showed 81.9% and 87.5% of amoxicillin was removed at 19.0 mg/L and 2.0 mg/L, respectively. Copyright © 2013 Elsevier Ltd. All rights reserved.

  3. Controlled release of tocopherols from polymer blend films

    Science.gov (United States)

    Obinata, Noe

    Controlled release packaging has great potential to increase storage stability of foods by releasing active compounds into foods continuously over time. However, a major limitation in development of this technology is the inability to control the release and provide rates useful for long term storage of foods. Better understanding of the factors affecting active compound release is needed to overcome this limitation. The objective of this research was to investigate the relationship between polymer composition, polymer processing method, polymer morphology, and release properties of active compounds, and to provide proof of principle that compound release is controlled by film morphology. A natural antioxidant, tocopherol was used as a model active compound because it is natural, effective, heat stable, and soluble in most packaging polymers. Polymer blend films were produced from combination of linear low density polyethylene (LLDPE) and high density polyethylene (HDPE), polypropylene (PP), or polystyrene (PS) with 3000 ppm mixed tocopherols using conventional blending method and innovative blending method, smart blending with a novel mixer using chaotic advection. Film morphologies were visualized with scanning electron microscopy (SEM). Release of tocopherols into 95% ethanol as a food simulant was measured by UV/Visible spectrophotometry or HPLC, and diffusivity of tocopherols in the polymers was estimated from this data. Polymer composition (blend proportions) and processing methods have major effects on film morphology. Four different types of morphologies, dispersed, co-continuous, fiber, and multilayer structures were developed by either conventional extrusion or smart blending. With smart blending of fixed polymer compositions, different morphologies were progressively developed with fixed polymer composition as the number of rod rotations increased, providing a way to separate effects of polymer composition and morphology. The different morphologies

  4. Controlled release of estradiol solubilized in carbopol/surfactant aggregates.

    Science.gov (United States)

    Barreiro-Iglesias, Rafael; Alvarez-Lorenzo, Carmen; Concheiro, Angel

    2003-12-12

    The potential of carbopol/surfactant dispersions as solubilizing and controlled release systems of estradiol (a poorly water-soluble drug) was evaluated. The solubilization of estradiol in the dispersions of Carbopol 934 (0.25%) and Pluronic F-127, Tween 80, sodium dodecylsulfate (SDS), or benzalkonium chloride (BkCl) was assessed, by differential scanning calorimetry (DSC) of films obtained by desiccation, as a decrease in estradiol melting temperature and enthalpy. The amounts of estradiol solubilized in carbopol/SDS and carbopol/Tween 80 aqueous dispersions were considerably greater (solubilization capacity: 1.3 and 9 times greater) than in the surfactant alone solutions and up to 100 times greater than in water. High aggregates/water equilibrium partition coefficients of estradiol in carbopol/SDS (1768 M(-1)) and carbopol/Tween 80 (14114 M(-1)) dispersions were found. Carbopol/(1%) SDS/(25 mg/dl) estradiol and carbopol/(0.1%) Tween 80/(5 mg/dl) estradiol dispersions had a pH of around 4, were easy flowing, and showed sustained release for at least 1 week. Estradiol diffusion coefficients were greater when the receptor medium was 0.3-1.0% SDS solution than when it was iso-osmotic NaCl solution or pH 7.5 phosphate buffer. At this pH, a viscoelastic gel is formed on the donor side of the membrane and the drug diffusion slowed down. When the receptor medium contains a surfactant, estradiol release seems to happen as a direct exchange between the carbopol/surfactant aggregates and the receptor surfactant micelles. If no surfactant is in the receptor fluid, estradiol/surfactant complexes migrate towards the receptor. Despite the low viscosity of these dispersions, estradiol diffusion coefficients were in the same order of magnitude as those obtained with a commercially available neutralized ethanol/water carbopol gel of estradiol (60 mg/dl). When the receptor medium had no surfactant, the low affinity of estradiol for water prevented drug diffusion from the

  5. ESTIMATION OF AMOXICILLIN RESIDUES IN COMMERCIAL MEAT AND MILK SAMPLES

    Directory of Open Access Journals (Sweden)

    Ainee Irum

    2014-08-01

    Full Text Available The present study was conducted to evaluate the extent of ß - lactam antibiotic, amoxicillin residues in market milk and meat. Samples were randomly collected from Faisalabad city, Pakistan. High Performance Liquid Chromatography (HPLC method with inflorescent detector was used to detect, identify and quantify the amoxicillin residues in milk and meat samples. The milk samples were purified by performing a protein precipitation step, followed by derivatization. To clean up tissue samples, a liquid extraction, followed by a solid-phase extraction procedure C18 (4.0X4.6mm, 5μm was performed. A 50% meat and 90% milk samples were found contaminated with residues. The residues of amoxicillin in milk were in range of 28 to 46μg/kg and in meat were 9 to 84μg/kg. All of the contaminated milk and 40 out of 50% meat samples fall in maximum residue limits.

  6. Preparation of Controlled-Release Fine Particles Using a Dry Coating Method.

    Science.gov (United States)

    Nakamura, Shohei; Sakamoto, Takatoshi; Ito, Tomonori; Kabasawa, Kazuhiro; Yuasa, Hiroshi

    2016-12-01

    Wet coating methods use organic solvents to prepare layered particles that provide controlled-release medications. However, this approach has disadvantages in that it can cause particle agglomeration, reduce pharmaceutical stability, and leave residual organic solvents. We used a dry coating method to overcome these issues. Fine particles (less than 50 μm in diameter) of controlled-release theophylline were created using theophylline (TP; model drug), polyethylene glycol 20,000 (PEG; drug fixative), hydrogenated castor oil (HCO; controlled-release material), hydrogenated rapeseed oil (HRSO; controlled-release material), and cornstarch (CS; core particle). An ultrahigh-speed mixer was employed to mix TP and CS for 5 min at 28,000 rpm. Subsequent addition of PEG produced single-core particles with a drug reservoir coating. Addition of HCO and HRSO to these particles produced a controlled-release layer on their surface, resulting in less than 10% TP dissolution after 8 h. We successfully demonstrated that this dry coating method could be used to coat 16-μm CS particles with a drug reservoir layer and a controlled-release layer, producing multi-layer coated single-core particles that were less than 50 μm in diameter. These can be used to prepare controlled-release tablets, capsules, and orally disintegrating tablets.

  7. The influence of labour on the pharmacokinetics of intravenously administered amoxicillin in pregnant women

    NARCIS (Netherlands)

    A.F. Muller (Alex); P.J. Dörr (Joep); J.W. Mouton (Johan); J. de Jongh (Joost); P.M. Oostvogel (Paul); E.A.P. Steegers (Eric); R.A. Voskuyl (Robert); M. Danhof (Meindert)

    2008-01-01

    textabstractAIMS: Many physiological changes take place during pregnancy and labour. These might change the pharmacokinetics of amoxicillin, necessitating adjustment of the dose for prevention of neonatal infections. We investigated the influence of labour on the pharmacokinetics of amoxicillin.

  8. Subcutaneous granuloma annulare: radiologic appearance

    Energy Technology Data Exchange (ETDEWEB)

    Kransdorf, M.J. [Saint Mary`s Hospital, Richmond, VA (United States). Dept. of Radiol.]|[Department of Radiologic Pathology, Armed Forces Institute of Pathology, Washington, DC (United States); Murphey, M.D. [Department of Radiologic Pathology, Armed Forces Institute of Pathology, Washington, DC (United States)]|[Department of Radiology and Nuclear Medicine, Uniformed Services University of the Health Sciences, Bethesda, Maryland (United States)]|[Department of Radiology, School of Medicine, University of Maryland, Baltimore, Maryland (United States); Temple, H.T. [Department of Orthopedic Surgery, University of Virginia Health Sciences Center, Charlottesville, Virginia (United States)]|[Department of Orthopedic Pathology, Armed Forces Institute of Pathology, Washington, DC (United States)

    1998-05-01

    Objective. Granuloma annulare is an uncommon benign inflammatory dermatosis characterized by the formation of dermal papules with a tendency to form rings. There are several clinically distinct forms. The subcutaneous form is the most frequently encountered by radiologists, with the lesion presenting as a superficial mass. There are only a few scattered reports of the imaging appearance of this entity in the literature. We report the radiologic appearance of five cases of subcutaneous granuloma annulare. Design and patients. The radiologic images of five patients (three male, two female) with subcutaneous granuloma annulare were retrospectively studied. Mean patient age was 6.4 years (range, 2-13 years). The lesions occurred in the lower leg (two), foot, forearm, and hand. MR images were available for all lesions, gadolinium-enhanced imaging in three cases, radiographs in four, and bone scintigraphy in one. Results. Radiographs showed unmineralized nodular masses localized to the subcutaneous adipose tissue. The size range, in greatest dimension on imaging studies, was 1-4 cm. MR images show a mass with relatively decreased signal intensity on all pulse sequences, with variable but generally relatively well defined margins. There was extensive diffuse enhancement following gadolinium administration. Conclusion. The radiologic appearance of subcutaneous granuloma annulare is characteristic, typically demonstrating a nodular soft-tissue mass involving the subcutaneous adipose tissue. MR images show a mass with relatively decreased signal intensity on all pulse sequences and variable but generally well defined margins. There is extensive diffuse enhancement following gadolinium administration. Radiographs show a soft-tissue mass or soft-tissue swelling without evidence of bone involvement or mineralization. This radiologic appearance in a young individual is highly suggestive of subcutaneous granuloma annulare. (orig.) With 3 figs., 17 refs.

  9. Relation Between Amoxicillin Concentration in Sputum of COPD Patients and Length of Hospitalization

    NARCIS (Netherlands)

    Brusse-Keizer, Marjolein; ten Bokum, Leonore; Movig, Kris; van der Valk, Paul; Kerstjens, Huib; van der Palen, Job; Hendrix, Ron

    Amoxicillin is a widely used antibiotic in COPD. Little is known about the transfer of amoxicillin into sputum of COPD patients. The objective was to investigate the relationship between the concentration of amoxicillin in sputum in hospitalized COPD patients and length of hospitalization. To be

  10. Characterization of amoxicillin- and clavulanic acid-specific T cells in patients with amoxicillin-clavulanate-induced liver injury.

    Science.gov (United States)

    Kim, Seung-Hyun; Saide, Katy; Farrell, John; Faulkner, Lee; Tailor, Arun; Ogese, Monday; Daly, Ann K; Pirmohamed, Munir; Park, B Kevin; Naisbitt, Dean J

    2015-09-01

    Drug-induced liver injury (DILI) frequently has a delayed onset with several human leukocyte antigen (HLA) genotypes affecting susceptibility, indicating a potential role for the adaptive immune system in the disease. The aim of this study was to investigate whether drug-responsive T lymphocytes are detectable in patients who developed DILI with the combination, antimicrobial amoxicillin-clavulanate. Lymphocytes from 6 of 7 patients were found to proliferate and/or secrete interferon-gamma (IFN-γ) when cultured with amoxicillin and/or clavulanic acid. Amoxicillin (n = 105) and clavulanic acid (n = 16) responsive CD4(+) and CD8(+) T-cell clones expressing CCR, chemokine (C-C motif) receptor 4, CCR9, and chemokine (C-X-C motif) receptor 3 were generated from patients with and without HLA risk alleles; no cross-reactivity was observed between the two drug antigens. Amoxicillin clones were found to secrete a heterogeneous panel of mediators, including IFN-γ, interleukin-22 and cytolytic molecules. In contrast, cytokine secretion by the clavulanic acid clones was more restricted. CD4(+) and CD8(+) clones were major histocompatability complex class II and I restricted, respectively, with the drug antigen being presented to CD4(+) clones in the context of HLA-DR molecules. Several pieces of evidence indicate that the clones were activated by a hapten mechanism: First, professional antigen-presenting cells (APCs) were required for optimal activation; second, pulsing APCs for 4-16 hours activated the clones; and third, inhibition of processing abrogated the proliferative response and cytokine release. Both amoxicillin- and clavulanic acid-specific T cells participate in the liver injury that develops in certain patients exposed to amoxicillin-clavulanate. © 2015 by the American Association for the Study of Liver Diseases.

  11. Self-assembled nanoparticles of glycol chitosan – Ergocalciferol succinate conjugate, for controlled release

    DEFF Research Database (Denmark)

    Quinones, Javier Perez; Gothelf, Kurt Vesterager; Kjems, Jørgen

    2012-01-01

    Glycol chitosan was linked to vitamin D2 hemisuccinate (ergocalciferol hemisuccinate) for controlled release through water-soluble carbodiimide activation. The resulting conjugate formed self-assembled nanoparticles in aqueous solution with particle size of 279 nm and ergocalciferol hemisuccinate...

  12. Controlled-release fertilizer composition substantially coated with an impermeable layer

    Energy Technology Data Exchange (ETDEWEB)

    Ankeny, Mark

    2016-03-29

    A controlled-release fertilizer composition is provided that is substantially coated with an impermeable layer. The fertilizer composition may further include one or more hollow sections to allow for root penetration and efficient delivery of nutrients.

  13. Materials for Pharmaceutical Dosage Forms: Molecular Pharmaceutics and Controlled Release Drug Delivery Aspects

    Directory of Open Access Journals (Sweden)

    Patrick P. DeLuca

    2010-09-01

    Full Text Available Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles over immediate release delivery. These advantages include reduced dosing frequency, better therapeutic control, fewer side effects, and, consequently, these dosage forms are well accepted by patients. Advances in polymer material science, particle engineering design, manufacture, and nanotechnology have led the way to the introduction of several marketed controlled release products and several more are in pre-clinical and clinical development.

  14. Materials for pharmaceutical dosage forms: molecular pharmaceutics and controlled release drug delivery aspects.

    Science.gov (United States)

    Mansour, Heidi M; Sohn, Minji; Al-Ghananeem, Abeer; Deluca, Patrick P

    2010-09-15

    Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles) over immediate release delivery. These advantages include reduced dosing frequency, better therapeutic control, fewer side effects, and, consequently, these dosage forms are well accepted by patients. Advances in polymer material science, particle engineering design, manufacture, and nanotechnology have led the way to the introduction of several marketed controlled release products and several more are in pre-clinical and clinical development.

  15. [Research advances on controlled-release mechanisms of nutrients in coated fertilizers].

    Science.gov (United States)

    Zhang, Haijun; Wu, Zhijie; Liang, Wenju; Xie, Hongtu

    2003-12-01

    Using encapsulation techniques to coat easily soluble fertilizers is an important way to improve fertilizer use efficiency while reduce environmental hazards. Based on a wide range of literature collection on coated fertilizer research, the theories, processes, and characters of nutrient controlled-release from coated fertilizer were discussed, and the factors affecting nutrient controlled-release and the mathematical simulations on it were reviewed. The main tendencies related to this research in China were also put forward.

  16. Post-marketing stability surveillance: Amoxicillin | Naidoo | South ...

    African Journals Online (AJOL)

    Thus, the aims of this study were to determine whether the types of packaging in which amoxicillin preparations are dispensed and the temperature and humidity conditions under which they are stored by patients are adequate and appropriate to ensure drug stability. Methods A mini-survey of pharmacies and patients was ...

  17. Influence of Chloramphenicol and Amoxicillin on Rat Liver ...

    African Journals Online (AJOL)

    This study examined the effect of chloramphenicol and amoxicillin on liver microsomal enzymes Ca2+-ATPase and Glucose-6-Phosphatase (G-6-P) and lipid peroxidation in rats. Male Wistar strain rats weighing 120 – 195 g were divided into four groups. Group one, the control group, received physiological saline, group ...

  18. Amoxicillin photodegradation by nanocrystalline TiO2

    Directory of Open Access Journals (Sweden)

    Radosavljević K D.

    2017-01-01

    Full Text Available Nanocrystalline TiO2, synthesized by sol-gel route and characterized by XRPD, BET and SEM measurements, was applied in the photocatalytic degradation of amoxicillin, using an Osram Ultra-Vitalux® lamp as the light source. Amoxicillin is a semi-synthetic penicillin type antibiotic active against a wide range of grampositive and a limited range of gram-negative organisms. The continuous release of antibiotics and their persistence in the environment may result in serious irreversible effects on aquatic and terrestrial organisms. Heterogeneous catalysis, which uses catalysts like TiO2, is a promising route for the degradation of organic pollutants including antibiotics. The effects of initial concentration of catalyst, initial salt concentration (NaCl and Na2SO4, ethanol and pH on the photocatalytic degradation of amoxicillin were studied. The mineralization of amoxicillin was analyzed by ion chromatography as well as by total organic analysis. The catalytic properties of nanocrystalline TiO2 were compared to Evonik P25 catalyst.

  19. Preparation and in vitro evaluation of amoxicillin encapsulated in ...

    African Journals Online (AJOL)

    Purpose: To optimize and characterize amoxicillin encapsulated in mucoadhesive alginate-coated chitosan microparticles for the treatment of gastric and duodenal ulcers caused by Helicobacter pylori. Methods: Eighteen batches of various ratios of chitosan, sodium alginate and calcium chloride were prepared by ...

  20. Routine Amoxicillin for Uncomplicated Severe Acute Malnutrition in Children.

    Science.gov (United States)

    Isanaka, Sheila; Langendorf, Céline; Berthé, Fatou; Gnegne, Smaila; Li, Nan; Ousmane, Nassirou; Harouna, Souley; Hassane, Hamidine; Schaefer, Myrto; Adehossi, Eric; Grais, Rebecca F

    2016-02-04

    High-quality evidence supporting a community-based treatment protocol for children with severe acute malnutrition, including routine antibiotic use at admission to a nutritional treatment program, remains limited. In view of the costs and consequences of emerging resistance associated with routine antibiotic use, more evidence is required to support this practice. In a double-blind, placebo-controlled trial in Niger, we randomly assigned children who were 6 to 59 months of age and had uncomplicated severe acute malnutrition to receive amoxicillin or placebo for 7 days. The primary outcome was nutritional recovery at or before week 8. A total of 2412 children underwent randomization, and 2399 children were included in the analysis. Nutritional recovery occurred in 65.9% of children in the amoxicillin group (790 of 1199) and in 62.7% of children in the placebo group (752 of 1200). There was no significant difference in the likelihood of nutritional recovery (risk ratio for amoxicillin vs. placebo, 1.05; 95% confidence interval [CI], 0.99 to 1.12; P=0.10). In secondary analyses, amoxicillin decreased the risk of transfer to inpatient care by 14% (26.4% in the amoxicillin group vs. 30.7% in the placebo group; risk ratio, 0.86; 95% CI, 0.76 to 0.98; P=0.02). We found no benefit of routine antibiotic use with respect to nutritional recovery from uncomplicated severe acute malnutrition in Niger. In regions with adequate infrastructure for surveillance and management of complications, health care facilities could consider eliminating the routine use of antibiotics in protocols for the treatment of uncomplicated severe acute malnutrition. (Funded by Médecins sans Frontières Operational Center Paris; ClinicalTrials.gov number, NCT01613547.).

  1. Deteksi Resistensi Amoxicillin Helicobacter pylori pada Pasien Dispepsia

    Directory of Open Access Journals (Sweden)

    Indah Sulistiyawati

    2017-08-01

    Full Text Available Amoxicillin is one of the antibiotics that commonly used on treatment of H. pylori infection. pbp1A gene mutation in H. pylori is a dominant cause of amoxicillin resistance. This study was aimed to evaluate the presence of H. pylori in patients with dyspepsia by using non-invasive method i.e. H. pylori stool antigen (HPSA and invasive method i.e. pbp1A gene amplification, and also evaluate the amoxicillin resistance of H. pylori by assessing the pbp1A gene mutations. The samples were  26 faeces and 26 gastric biopsies of patients with dyspepsia from the Internal Disease of Prof. Dr. Margono Soekardjo Hospital in Purwokerto. DNA amplification performed by using polymerase chain reaction (PCR to detect the presence of amoxicillin resistance encoding gene i.e. penicillin binding protein (pbp1A. Sequencing of the DNA sample was performed at the First Base Malaysian Company, to analyze the existence of a point mutation. DNA sequencing analysis of 12 samples showed the presence of a mutations in pbp1A gene from 2 samples, in the third motive of pbp i.e. amino acid changes, Alanine 599 substituted to Threonin and Threonin 592 to Alanine. Those mutations become a dominant risk factor for resistance of H. pylori, toward the bacterial peptidoglycan synthesis. In this research, it was known that the detection of H. pylori infection by using PCR remains more accurate and specific method. The presence of H. pylori mutant strains in this study may becomes the risk factors of resistance to amoxicillin treatment.

  2. SUBCUTANEOUS BASIDIOBOLOMYCOSIS: A CASE REPORT

    African Journals Online (AJOL)

    2013-07-09

    Jul 9, 2013 ... E-mail: sackey@sky.com. Conflict of interest: None declared. SUMMARY. Basidiobolomycosis is an uncommon chronic deep fungal infection in which gradually enlarging granulomas form, usually in the subcutaneous fat tissues of the limbs, chest or trunk of immunocompetent hosts, primarily children.

  3. Pneumomediastinum and subcutaneous cervical emphysema ...

    African Journals Online (AJOL)

    PROF. EZECHUKWU

    2012-09-08

    Sep 8, 2012 ... department with a history of increasing difficulty with breathing and ... ward and commenced on intravenous antibiotics and high flow oxygen. He made remarkable improvement with complete resolution of subcutaneous emphysema on the 4th day ... the left lateral decubitus position.18 Our patient met most.

  4. Pyrexial therapy in subcutaneous phycomycosis

    Directory of Open Access Journals (Sweden)

    Reddy BSN

    1992-01-01

    Full Text Available A case of subcutaneous phycomycosis occurring in a 2 ½ year old child is reported for its rarity, clinical interest and paucity of literature. The condition failed to resolve with conventional antimycotics but improved with the administration of concomitant pyrexial therapy.

  5. Pneumomediastinum and subcutaneous cervical emphysema ...

    African Journals Online (AJOL)

    PROF. EZECHUKWU

    2012-09-08

    Sep 8, 2012 ... to trauma or pathological disease state3, with gastroin- testinal and respiratory diseases most commonly impli- cated.4,5. The respiratory disease commonly associated with pneu- momediastinum and subcutaneous cervical emphysema is bronchial asthma.6 Pneumonia, though a very com- mon childhood ...

  6. WE-AB-BRA-03: Non-Invasive Controlled Release from Implantable Hydrogel Scaffolds Using Ultrasound

    Energy Technology Data Exchange (ETDEWEB)

    Moncion, A; Kripfgans, O.D; Putnam, A.J; Frances chi, R.T; Fabiilli, M.L [University of Michigan, Ann Arbor, MI (United States)

    2016-06-15

    Purpose: To control release of a model payload in acoustically responsive scaffolds (ARSs) using focused ultrasound (FUS). Methods: Fluorescently-labeled dextran (10 kDa) was encapsulated in sonosensitive perfluorocarbon (C{sub 6}F{sub 14} or C{sub 5}F{sub 12}) double emulsions (mean diameter: 2.9±0.1 µm). For in vitro release studies, 0.5 mL ARSs (10 mg/mL fibrin, 1% (v/v) emulsion) were polymerized in 24 well plates and covered with 0.5 mL medium. Starting one day after polymerization, ARSs were exposed to FUS (2.5 MHz, Pr = 8 MPa, 13 cycles, 100 Hz PRF) for 2 min daily. The amount of dextran released into the media was quantified. For in vivo studies, 0.25 mL ARSs were prepared as described previously and injected subcutaneously in the lower back of BALB/c mice. After polymerization, a subset of the implanted ARSs were exposed to FUS (as previously described). Animals were imaged longitudinally using a fluorescence imaging system to quantify the amount of dextran released from the ARSs. Results: In vitro: Over 6 days, +FUS displayed an 8.2-fold increase in dextran release compared to −FUS (−FUS: 2.7±0.6%; +FUS: 22.2±3.0%) for C{sub 6}F{sub 14} ARSs, and a 6.7-fold increase (−FUS: 5.0±0.8%; +FUS: 38.5±1.6%) for C{sub 5}F{sub 12}:C{sub 6}F{sub 14} ARSs. In vivo: +FUS displayed statistically greater dextran release compared to −FUS one day after implantation for C{sub 5}F{sub 12}:C{sub 6}F{sub 14} ARSs (−FUS: 55.1±1.5%; +FUS: 74.1±2.2%) and three days after implantation for C{sub 6}F{sub 14} ARSs (−FUS: 1.4±6.5%; +FUS: 30.4±5.4%). Conclusion: FUS enables non-invasive control of payload release from an ARS, which could benefit growth factor delivery for tissue regeneration. ARS are versatile due to their tunability (i.e. stiffness, emulsion composition, FUS pressure, FUS frequency, etc.) and can be modified to for optimal payload release. Future work will optimize ARS formulations for in vivo use to minimize payload release in the absence of

  7. Calcium modified edible Canna (Canna edulis L) starch for controlled released matrix

    Science.gov (United States)

    Putri, A. P.; Ridwan, M.; Darmawan, T. A.; Darusman, F.; Gadri, A.

    2017-07-01

    Canna edulis L starch was modified with calcium chloride in order to form controlled released matrix. Present study aim to analyze modified starch characteristic. Four different formulation of ondansetron granules was used to provide dissolution profile of controlled released, two formula consisted of 15% and 30% modified starch, one formula utilized matrix reference standards and the last granules was negative control. Methocel-hydroxypropyl methyl cellulose was used as controlled released matrix reference standards in the third formula. Calcium starch was synthesized in the presence of sodium hydroxide to form gelatinized mass and calcium chloride as the cross linking agent. Physicochemical and dissolution properties of modified starch for controlled released application were investigated. Modified starch has higher swelling index, water solubility and compressibility index. Three of four different formulation of granules provide dissolution profile of controlled released. The profiles indicate granules which employed calcium Canna edulis L starch as matrix are able to resemble controlled drug released profile of matrix reference, however their bigger detain ability lead to lower bioavailability.

  8. [Effects of slow/controlled release fertilizers on the growth and nutrient use efficiency of pepper].

    Science.gov (United States)

    Tang, Shuan-Hu; Zhang, Fa-Bao; Huang, Xu; Chen, Jian-Sheng; Xu, Pei-Zhi

    2008-05-01

    Pot trails were conducted from 2003 to 2005 to study the effects of slow/controlled release fertilizers on the growth and nutrient use efficiency of pepper. The results indicated that in comparison with conventional splitting fertilization (T1), basal application of polymer-coated controlled release fertilizer (T2) enhanced the single fruit mass and vitamin C concentration, improved the root activity, and increased the fruit yield by 8.4%, but no significant effect was observed on the dissoluble sugar concentration in fruit. NH4MgPO4-coated controlled release fertilizer (T3) increased the dissoluble sugar concentration by 5.67%, but had less effect on single fruit mass and vitamin C concentration. Under the application of T3, the root system had a vigorous growth at early stages but became infirm at later stages, resulting in a lower yield. Comparing with T1, the application of 3 slow release fertilizers increased the dissoluble sugar concentration in fruit, enhanced the root activity, but had less effect on the yield. All test slow/controlled release fertilizers increased the use efficiency of N, P, and K significantly, with an exception for T2 which increased the use efficiency of N and K but decreased that of P. It was demonstrated that an appropriate application of slow/controlled release fertilizers could enhance pepper' s root activity and improve nutrient use efficiency.

  9. A novel controlled-release system for antibacterial enzyme lysostaphin delivery using hydroxyapatite/chitosan composite bone cement.

    Directory of Open Access Journals (Sweden)

    Bai Xue

    Full Text Available In this work, a lysostaphin-loaded, control-released, self-setting and injectable porous bone cement with efficient protein delivery was prepared by a novel setting method using hydroxyapatite/chitosan (HA/CS composite scaffold. The cement samples were made through cementitious reactions by mixing solid powder, a mixture of HA/CS composite particles, lysostaphin, Ca(OH2, CaCO3 and NaHCO3, with setting liquid containing citric acid, acetic acid, NaH2PO4, CaCl2 and poloxamer. The setting parameters of the cement samples were determined. The results showed that the final setting time was 96.6±5.2 min and the pH value increased from approximately 6.2 to nearly 10 during the setting process and the porosity was 34% at the end. And the microstructure and composition were detected by scanning electron microscopy (SEM, x-ray diffraction and Fourier transform-infrared spectroscopy. For the release behavior of lysostaphin loaded in the cement sample, the in vitro cement extract experiment indicated that about 94.2±10.9% of the loaded protein was released before day 8 and the in vivo Qdot 625 fluorescence tracking experiment showed that the loaded protein released slower than the free one. Then the biocompatibility of the cement samples was evaluated using the methylthiazol tetrazolium assay, SEM and hematoxylin-eosin staining, which suggested good biocompatibility of cement samples with MC 3T3-E1 cells and subcutaneous tissues of mice. Finally the antibacterial activity assay indicated that the loaded lysostaphin had good release ability and strong antibacterial enzymatic activity against methicillin-resistant Staphylococcus aureus. Collectively, all the results suggested that the lysostaphin-loaded self-setting injectable porous bone cement released the protein in a controlled and effective way and the protein activity was well retained during the setting and releasing process. Thus this bone cement can be potentially applied as a combination of

  10. Injectable agents affecting subcutaneous fats.

    Science.gov (United States)

    Chen, David Lk; Cohen, Joel L; Green, Jeremy B

    2015-09-01

    Mesotherapy is an intradermal or subcutaneous injection of therapeutic agents to induce local effects, and was pioneered in Europe during the 1950s. For the past 2 decades, there has been significant interest in the use of mesotherapy for minimally invasive local fat contouring. Based on the theorized lipolytic effects of the agent phosphatidylcholine, initial attempts involved its injection into subcutaneous tissue. With further studies, however, it became apparent that the activity attributed to phosphatidylcholine mesotherapy was due to the adipolytic effects of deoxycholate, a detergent used to solubilize phosphatidylcholine. Since then, clinical trials have surfaced that demonstrate the efficacy of a proprietary formulation of deoxycholate for local fat contouring. Current trials on mesotherapy with salmeterol, a b-adrenergic agonist and lipolysis stimulator, are underway-with promising preliminary results as well. ©2015 Frontline Medical Communications.

  11. Principles of subcutaneous port placement.

    Science.gov (United States)

    Gonda, Shaun J; Li, Ruizong

    2011-12-01

    The introduction of totally implantable subcutaneous devices in the early 1980s provided patients with secure, reliable venous access and also gave them the ability to move more freely and have a more normal lifestyle with these devices in place. The most common totally implantable device used today is the subcutaneous port. These ports consist of an injection port connected to a catheter. Ports provide a number of advantages compared with other venous catheters; the most important is the reduced risk of infection. These devices have significantly lower rates of infection than nontunneled and tunneled catheters. Additional advantages include less frequent irrigation and minimal home care, and they are less prone to environmental or cutaneous contamination when not being accessed. This article will focus on the placement of these ports. Copyright © 2011 Elsevier Inc. All rights reserved.

  12. Concentration of amoxicillin in maternal serum, cord blood, amniotic fluid and the placenta after vaginal administration.

    Science.gov (United States)

    Zaręba-Szczudlik, Julia; Romejko-Wolniewicz, Ewa; Lewandowski, Zbigniew; Różańska, Hanna; Czajkowski, Krzysztof

    2015-01-01

    The aim of this study was to assess the amoxicillin concentration in maternal serum, cord blood, amniotic fluid and the placenta, 2 h following vaginal administration and the factors influencing the drug level. Twenty-eight full-term pregnant women who qualified for elective cesarean delivery were included in the study. Vaginal suppositories containing 250 mg of amoxicillin were administered 2 h prior to the operation. Amoxicillin levels were determined using the diffusion microbial assay. The amoxicillin level in amniotic fluid was significantly higher in comparison to that of maternal serum, cord blood or the placenta. Maternal age positively and gestational weight gain negatively correlated with the amoxicillin concentration in maternal serum. The maternal serum hemoglobin level and red blood cell count were positively correlated with amoxicillin concentration in the amniotic fluid. Neonatal birth weight was positively correlated with maternal serum and cord blood amoxicillin levels. Hypertensive women had significantly higher amoxicillin concentrations in amniotic fluid, and women with thrombocytopenia presented significantly higher cord blood amoxicillin concentrations. Amoxicillin presented poor concentration in maternal-fetal compartments after vaginal administration, but the factors influencing the drug level in different compartments require further investigation.

  13. Cellular responses and biodegradation of amoxicillin in Microcystis aeruginosa at different nitrogen levels.

    Science.gov (United States)

    Liu, Ying; Wang, Feng; Chen, Xiao; Zhang, Jian; Gao, Baoyu

    2015-01-01

    The influence of nitrogen on the interactions between amoxicillin and Microcystis aeruginosa was investigated using a 7-day exposure test. Growth of M. aeruginosa was not significantly (p>0.05) affected by amoxicillin at the lowest nitrogen level of 0.05 mg L(-1), stimulated by 500 ng L(-1) of amoxicillin at a moderate nitrogen level of 0.5 mg L(-1) and enhanced by 200-500 ng L(-1) of amoxicillin at the highest nitrogen level of 5 mg L(-1). The generation of reactive oxygen species (ROS) and the synthesis of glutathione S-transferases (GST) and glutathione (GSH) were more sensitive to amoxicillin and were stimulated at all nitrogen levels. At the lowest nitrogen level of 0.05 mg L(-1), superoxide dismutase and peroxidase were not effective at eliminating amoxicillin-induced ROS, resulting in the highest malondialdehyde content in M. aeruginosa. The biodegradation of 18.5-30.5% of amoxicillin by M. aeruginosa was coupled to increasing GST activity and GSH content. Elevated nitrogen concentrations significantly enhanced (pamoxicillin on the growth of M. aeruginosa, the antioxidant responses to amoxicillin and the biodegradation of amoxicillin in M. aeruginosa. The nitrogen-dependent hormesis effect of the coexisting amoxicillin contaminant on the M. aeruginosa bloom should be fully considered during the control of M. aeruginosa bloom. Copyright © 2014 Elsevier Inc. All rights reserved.

  14. Application of photoremovable protecting group for controlled release of plant growth regulators by sunlight.

    Science.gov (United States)

    Atta, Sanghamitra; Ikbal, Mohammed; Kumar, Ashutosh; Pradeep Singh, N D

    2012-06-04

    We report a novel technique for controlled release of plant growth regulators (PGRs) by sunlight using photoremovable protecting group (PRPG) as a delivery device. In the present work, carboxyl-containing PGRs of the auxin group [indoleacetic acid (IAA) and naphthoxyacetic acid (NOAA)] were chemically caged using PRPGs of coumarin derivatives. Photophysical studies showed that caged PGRs exhibited good fluorescence properties. Irradiation of caged PGRs by sunlight in both aqueous ethanol and soil media resulted in controlled release of PGRs. The results of the bioactivity experiments indicated that caged PGRs showed better enhancement in the root and shoot length growth of Cicer arietinum compared to PGRs after 10days of sunlight exposure. Our results indicated that use of PRPG as a delivery device for controlled release of PGRs by sunlight in soil holds great interest for field application since it can overcome the rapid loss of PGRs in environmental conditions. Copyright © 2012 Elsevier B.V. All rights reserved.

  15. Analytical solution of diffusion model for nutrient release from controlled release fertilizer

    Science.gov (United States)

    Ameenuddin Irfan, Sayed; Razali, Radzuan; KuShaari, KuZilati; Mansor, Nurlidia; Azeem, Babar

    2017-09-01

    An analytical method has been developed to solve the initial value problem which arises from Fick’s diffusion equation encountered in the modelling of the Controlled Release Fertilizers. The proposed analytical solution is developed using the modified Adomian decomposition method. This method does not require the discretization method, reliability and efficiency of this method is more and it also reduces the calculation time. The model has predicted the effect of granule radius and diffusion coefficient on the nutrient release and total release time of Controlled Release Fertilizer. Model has predicted that increase in the radius of granule reduces the release and vice versa in case of diffusion coefficient. Detailed understanding of these parameters helps in improved designing of Controlled Release Fertilizer.

  16. Subcutaneous emphysema during status astmaticus

    Energy Technology Data Exchange (ETDEWEB)

    Schwarz, E.

    1985-09-01

    Spontaneous subcutaneous accumulations of air in the soft parts of the thorax during an asthmatic crisis (status asthmaticus) are rarely seen. The pathomechanism of the phenomenon, which may lead to the formation of an emphysema of the soft parts via the pneumomediastinum, is discussed, and the possible complications which must be taken into account are pointed out. The value of radiological examination of the thorax in children suffering from asthma bronchiale, is explained briefly. (orig.).

  17. Epidural, paraspinal, and subcutaneous lipomatosis

    Energy Technology Data Exchange (ETDEWEB)

    Sener, R. Nuri [Department of Radiology, Ege University Hospital, Bornova, Izmir (Turkey)

    2003-09-01

    A unique case of idiopathic diffuse lipomatosis is reported. The patient was an 11-year-old boy with diffuse lipomatosis in the epidural space, paraspinal muscles, and thoracolumbar subcutaneous regions. Epidural lipomatosis involved the entire thoracolumbar spine and was associated with filar thickening and lipoma. In addition, paraspinal muscles, especially the erector spinae group, had diffuse fatty infiltration. The ultimate clinical effect of this fatty tissue was urinary dysfunction, radicular pain and hypoesthesia in both legs and difficulty walking. (orig.)

  18. Rash, fever and proteinuria after amoxicillin in a SLE patient.

    Science.gov (United States)

    Couto, M; Duarte, C; Geraldes, A; Medeiros, Colleen; Inês, L; Malcata, A

    2009-01-01

    We report a case of severe type IV hypersensitivity reaction to amoxicillin, which occurred in a person with a 12-year history of SLE. The present case illustrates the wide differential diagnosis in a SLE patient who presents with an allergic drug reaction. The attribution of the presenting symptoms to the underlying SLE and/or to the drugs used to treat SLE and coexisting conditions is a major challenge.

  19. Quality of amoxicillin formulations in some Arab countries.

    Science.gov (United States)

    Kyriacos, S; Mroueh, M; Chahine, R P; Khouzam, O

    2008-08-01

    The problem of counterfeit and substandard drugs is recurrent in developing countries where antibiotics account for the majority of such products. The aim of this study was to investigate the quality of locally produced and imported amoxicillin products on the Lebanese, Jordanian, Egyptian and Saudi markets. One hundred and eleven samples of amoxicillin capsules and suspensions purchased from retail pharmacies were analysed for their drug content by a validated chromatographic method in order to verify if they complied with pharmacopeial requirements. Suspensions were analysed for their drug content immediately after reconstitution as well as 7 or 14 days later according to the expiry date. Fifty-six per cent of amoxicillin capsules did not meet the United State Pharmacopeia (USP) requirements and most had amounts bordering the lower limit. Individual average values as low as 59% of the label claim were detected. Eight per cent of the samples of suspensions gave measurements outside pharmacopeial limits. Furthermore, after 7 or 14 days, 38% of the samples were outside the pharmacopeial limits. All the European brands met the pharmacopeial limits except for one. Our results reveal the high incidence of substandard drugs on some Arab market where several factors might jeopardize the quality status of medicines: lack of effective quality assurance system during manufacture in both Arab and export countries, and uncontrolled storage conditions, especially unsuitable pharmacy premises. Use of substandard antibiotic preparations increases the risk of therapeutic failure and the emergence of drug-resistant microorganisms.

  20. Research of amoxicillin microcapsules preparation playing micro-jetting technology.

    Science.gov (United States)

    Sun, Huaiyuan; Gu, Qingqing; Liao, Yuehua; Sun, Chenjie

    2015-01-01

    With polylactic-co-glycolic acid(PLGA) as shell material of microcapsule, amoxicillin as the model, poly(vinyl alcohol) and twain as surfactant, amoxicillin-PLGA microcapsules were manufactured using digital micro-jetting technology and a glass nozzle of 40μm diameter. The influences of the parameters of micro-jetting system on the mean grain size and size distribution of amoxicillin-PLGA microcapsules were studied with single factor analysis and orthogonal experiment method, namely, PLGA solution concentration, driving voltage, jetting frequency, stirrer speed, etc. The optimal result was obtained; the form representation of microcapsule was analyzed as well. The results show that, under certain conditions of experimental drug prescription, driving voltage was proportional to the particle size; jetting frequency and stirrer speed were inversely proportional. When the PLGA concentration for 3%, driving voltage for 80V, the jetting frequency for 10000Hz and the stirrer speed for 750rpm, the particles were in an ideal state with the mean grain size of 60.246μm, the encapsulation efficiency reached 62.39% and 2.1% for drug loading.

  1. Floating Gastroretentive of Amoxicillin Using Hard Alginate Capsules and Its Antibacterial Activities

    OpenAIRE

    Arianto, Anayanti; Bangun, Hakim; Yohana, Ade; Silalahi, Jansen

    2017-01-01

    Anayanti Haryanto Objective: The aim of this study was to formulate the floating gastroretentive of amoxicillin using hard alginate capsules shell and evaluate the antibacterial activities of floating gastroretentive of amoxicillin. Methods: Amoxicillin was prepared in the solid dispersion form, it was prepared by a solvent method using polyvinylpyrrolidone (PVP) K30. The solid dispersion was characterized by X-ray diffraction and Fourier transformed infra-red analysis. The drug w...

  2. Dynamics of controlled release systems based on water-in-water emulsions: A general theory

    NARCIS (Netherlands)

    Sagis, L.M.C.

    2008-01-01

    Phase-separated biopolymer solutions, and aqueous dispersions of hydrogel beads, liposomes, polymersomes, aqueous polymer microcapsules, and colloidosomes are all examples of water-in-water emulsions. These systems can be used for encapsulation and controlled release purposes, in for example food or

  3. Computer-aided and predictive models for design of controlled release of pesticides

    DEFF Research Database (Denmark)

    Suné, Nuria Muro; Gani, Rafiqul

    2004-01-01

    In the field of pesticide controlled release technology, a computer based model that can predict the delivery of the Active Ingredient (AI) from fabricated units is important for purposes of product design and marketing. A model for the release of an M from a microcapsule device is presented...

  4. Hydrogel based drug carriers for controlled release of hydrophobic drugs and proteins

    NARCIS (Netherlands)

    Ke Peng,

    2011-01-01

    The aim of this study is to prepare in situ forming hydrogels based on biocompatible polymers for the controlled release of hydrophobic drug and proteins. In order to load hydrophobic drug to the hydrophilic hydrogel matrix, beta-cyclodextrin and human serum albumin was introduced to the hydrogel

  5. Evaluation of Dosing Guidelines for Use of Controlled-Release Codeine in Chronic Noncancer Plan

    Directory of Open Access Journals (Sweden)

    Alan Russell

    2003-01-01

    Full Text Available OBJECTIVE: The clinical utility of guidelines for conversion of patients from a combination analgesic preparation of acetaminophen 300 mg plus codeine 30 mg every 4 h to 6h as needed to scheduled controlled-release (CR codeine every 12 h was evaluated.

  6. Innovative application of metal-organic frameworks for encapsulation and controlled release of allyl isothiocyanate

    Science.gov (United States)

    This research investigated the technical feasibility of metal-organic frameworks (MOFs) as novel delivery systems for encapsulation and controlled release of volatile allyl isothiocyanate (AITC) molecules. We hypothesized that water vapor molecules could act as an external stimulus to trigger the re...

  7. Using polymer-coated controlled-release fertilizers in the nursery and after outplanting

    Science.gov (United States)

    Thomas D. Landis; R. Kasten Dumroese

    2009-01-01

    Controlled-release fertilizers (CRF) are the newest and most technically advanced way of supplying mineral nutrients to nursery crops. Compared to conventional fertilizers, their gradual pattern of nutrient release better meets plant needs, minimizes leaching, and therefore improves fertilizer use efficiency. In our review of the literature, we found many terms used...

  8. Reducing Runoff Loss of Applied Nutrients in Oil Palm Cultivation Using Controlled-Release Fertilizers

    Directory of Open Access Journals (Sweden)

    A. Bah

    2014-01-01

    Full Text Available Controlled-release fertilizers are expected to minimize nutrient loss from crop fields due to their potential to supply plant-available nutrients in synchrony with crop requirements. The evaluation of the efficiency of these fertilizers in tropical oil palm agroecological conditions is not yet fully explored. In this study, a one-year field trial was conducted to determine the impact of fertilization with water soluble conventional mixture and controlled-release fertilizers on runoff loss of nutrients from an immature oil palm field. Soil and nutrient loss were monitored for one year in 2012/2013 under erosion plots of 16 m2 on 10% slope gradient. Mean sediments concentration in runoff amounted to about 6.41 t ha−1. Conventional mixture fertilizer posed the greatest risk of nutrient loss in runoff following fertilization due to elevated nitrogen (6.97%, potassium (13.37%, and magnesium (14.76% as percentage of applied nutrients. In contrast, this risk decreased with the application of controlled-release fertilizers, representing 0.75–2.44% N, 3.55–5.09% K, and 4.35–5.43% Mg loss. Meanwhile, nutrient loss via eroded sediments was minimal compared with loss through runoff. This research demonstrates that the addition of controlled-release fertilizers reduced the runoff risks of nutrient loss possibly due to their slow-release properties.

  9. Substrates and controlled-release fertilizations on the quality of eucalyptus cuttings

    Directory of Open Access Journals (Sweden)

    Richardson B. G. da Silva

    2014-11-01

    Full Text Available To produce cuttings with quality, the most appropriate nutritional management strategies should be sought to reduce wastage of fertilizer, while accounting for the characteristics of each substrate. This study evaluated the effect of substrates and doses of controlled-release fertilizer on the quality of Eucalyptus grandis Hill ex Maiden x Eucalyptus urophylla S. T. Blake cuttings. The substrates consisted of several mixtures: vermiculite+carbonized rice chaff+coconut fibre (1:1:1; vermiculite+coconut fibre (1:1; and vermiculite+carbonized rice chaff (1:1. These mixtures were added to 2, 4, 6 and 8 kg of controlled-release fertilizer per cubic meter of substrate. The substrates that do not support root development and have lower water retention, independently of the dose of controlled-release fertilizer, reduce the quality of the root system. For substrates with proper values of water retention, such as vermiculite+coconut fibre (1:1 and vermiculite+carbonised rice chaff+coconut fibre (1:1:1, the utilization of dose 2 kg of controlled-release fertilizer to each cubic meter is enough to promote cuttings with greater quality of the root systems and proper heights and stem diameters.

  10. Effects of Controlled Release Fertilizer on the Post-Production Performance of Impatiens Wallerana

    Science.gov (United States)

    Controlled release fertilizers (CRF) in production systems have been known to reduce environmental contamination. However, there is a lot to be explored as per its use in bedding plant production. Bedding plant growers have not adapted CRF use because there is little information about its use and ...

  11. Longevity of controlled release fertilizer influences the growth of bedding Impatiens

    Science.gov (United States)

    Controlled-release fertilizers (CRF) have not been extensively used in floriculture production, perhaps due to lack of grower experience and research-based information with their use in herbaceous plant production. Any information about the correct use of CRF should increase growers’ confidence in ...

  12. Series elasticity of the human triceps surae muscle : Measurement by controlled-release vs. resonance methods.

    NARCIS (Netherlands)

    Hof, AL; Boom, H; Robinson, C; Rutten, W; Neuman, M; Wijkstra, H

    1997-01-01

    With a newly developed Controlled-Release Ergometer the complete characteristic of the series elastic component can be measured in human muscles. Previous estimates were based on the resonance method: muscle elasticity was assessed from the resonance frequency of the muscle elasticity connected to a

  13. CONTROLLED-RELEASE OF PARACETAMOL FROM AMYLODEXTRIN TABLETS - IN-VITRO AND IN-VIVO RESULTS

    NARCIS (Netherlands)

    VANDERVEEN, J; EISSENS, AC; LERK, CF

    Amylodextrin is a suitable excipient for the design of solid controlled-release systems. The release of paracetamol from tablets containing 30% drug and 70% amylodextrin was studied in vitro and in vivo. In vitro dissolution profiles showed almost-constant drug release rates during 8 hr, when

  14. A case of amoxicillin-induced hepatocellular liver injury with bile-duct damage

    Science.gov (United States)

    Kim, Ju Seung; Jang, Young Rock; Lee, Ji Won; Kim, Jin Yong; Chung, Dong Hae; Kwon, Oh Sang; Kim, Yun Soo; Choi, Duck Joo; Kim, Ju Hyun

    2011-01-01

    Amoxicillin, an antibiotic that is widely prescribed for various infections, is associated with a very low rate of drug-induced liver injury; hepatitis and cholestasis are rare complications. Here we present a case of a 39-year-old woman who was diagnosed with abdominal actinomycosis and received amoxicillin treatment. The patient displayed hepatocellular and bile-duct injury, in addition to elevated levels of liver enzymes. The patient was diagnosed with amoxicillin-induced cholestatic hepatitis. When amoxicillin was discontinued, the patient's symptoms improved and her liver enzyme levels reduced to near to the normal range. PMID:22102391

  15. Effects of Amoxicillin and Clavulanic Acid on the Spontaneous Mechanical Activity of Juvenile Rat Duodenum.

    Science.gov (United States)

    Ciciora, Steven L; Williams, Kent C; Gariepy, Cheryl E

    2015-09-01

    There are a limited number of medications for the treatment of foregut dysmotility. Enteral amoxicillin/clavulanic acid induces phase III duodenal contractions in a fasting pediatric patient. The mechanism by which this occurs is unknown. We examined the individual contributions of amoxicillin and clavulanic acid on the spontaneous mechanical activity of juvenile rat duodenum to better understand this phenomenon. Duodenal segments from juvenile rats were longitudinally attached to force transducers in organ baths. Samples were cumulatively exposed to amoxicillin or clavulanic acid. Separate samples were exposed to carbachol alone to assess response in both the presence and absence of amoxicillin or clavulanic acid. Basal tone, frequency, and amplitude of contractions were digitized and recorded. The amplitude of the spontaneous contractions increased with amoxicillin. Inhibition of neuronal activity prevented this effect. Clavulanic acid did not affect the spontaneous contractions. Basal tone and the rate of contractions did not differ with either drug. Stimulation with carbachol in the presence of amoxicillin caused a statistically significant increase in the contractility compared with carbachol alone. Amoxicillin alters the spontaneous longitudinal mechanical activity of juvenile rat duodenum. Our results suggest that amoxicillin modulates the spontaneous pattern of cyclic mechanical activity of duodenal smooth muscle through noncholinergic, neurally mediated mechanisms. Our work provides an initial physiologic basis for the therapeutic use of amoxicillin in patients with gastrointestinal dysmotility.

  16. Postantibiotic effects and postantibiotic sub-MIC effects of amoxicillin on Streptococcus gordonii and Streptococcus sanguis.

    Science.gov (United States)

    Lee, S Y

    2000-10-01

    Amoxicillin is one of the most frequently recommended antibiotics for prophylaxis of infective endocarditis in dental/oral procedures. In this study, the postantibiotic effect (PAE), postantibiotic sub-MIC (PASME) and sub-MIC effect (SME) of amoxicillin on oral streptococci, Streptococcus gordonii and Streptococcus sanguis, which are two of the major etiological agents in infective endocarditis, were investigated. The PAE was induced by 10 x MIC of amoxicillin for 2 h and the antibiotic was eliminated by washing. The PASMEs were studied by addition of 0.1, 0.2 and 0.3 x MICs during the postantibiotic phase of the bacteria, and the SMEs were studied by exposing bacteria to amoxicillin at the sub-MICs only. The PAE of amoxicillin was 2.0 h with S. gordonii DL1 and 0.7 h with S. sanguis MPC1. The PASME and SME of amoxicillin were observed both for S. gordonii DL1 and for S. sanguis MPC1. However, the durations of effects for S. sanguis MPC1 were shorter than those for S. gordonii DL1. The PASME values for both strains increased as the concentration of amoxicillin increased. The PASME values for both strains were substantially longer than the SME values. The present study illustrates the existence of PAE, PASME and SME for amoxicillin against S. gordonii and S. sanguis, thereby extending the pharmacodynamic advantages of amoxicillin for these bacteria in the prophylaxis procedures of infective endocarditis.

  17. Subcutaneous Leiomyosarcoma of the Frenulum

    Directory of Open Access Journals (Sweden)

    D. Mendis

    2005-01-01

    Full Text Available Leiomyosarcomas of the penis are rare, with only 29 reported cases to date. We record the case of a patient who presented with a 2-year history of a seemingly indolent penile skin lesion. On histopathology of the local resection, a diagnosis of subcutaneous leiomyosarcoma was made. Specifically, leiomyosarcoma of the penile frenulum has not been clearly reported previously. The patient underwent a further excision to ensure an adequate resection margin and has had no disease recurrence at subsequent follow-up. Our case was of a lesion that, although clinically benign, was malignant and this possibility should be borne in mind when assessing patients.

  18. Effects of Control Release Fertilizers on Nutrient Leaching, Palm Growth and Production Cost

    Directory of Open Access Journals (Sweden)

    Pushpa Soti

    2015-11-01

    Full Text Available Objective of this study was to evaluate the effect of different controlled release fertilizer technologies on nutrient leaching and plant growth parameters of two palm species, Chinese Fan (Livistona chinensis and Queen (Syagrus romanzoffiana. We compared Nutri-Pak (12-4-12 controlled release packet and Harrell’s (12-4-12 controlled release polymer coated urea against Atlantic (8-4-12 controlled release polymer coated urea, coated sulfate of potash, the most commonly used palm fertilizer in South Florida. Plants were grown in 25 cm (11 L pots under 70% shade, watered weekly, with pest and weed control done as required. Plant growth parameters: number of leaves, leaf length and width, and basal diameter, were measured every two months. Leachate was collected weekly after irrigation and a two-month composite sample was analyzed for nutrient concentrations. There was no difference in the growth parameters among the three fertilizers for Chinese Fan plants. However for Queen, Atlantic and Harrell’s had significantly thicker basal diameter than Nutri-Pak. Significant difference in the concentration of nutrients in the leachate was observed among the fertilizer types. Throughout the study period, Nutri-Pak had a lower concentration of nutrients in the leachate than Atlantic and Harrell’s. Our research indicates that Nutri-Pak control release fertilizer is comparable to other commercial fertilizers in Chinese Fan growth, but the larger Queen palms likely require an additional packet. Nutri-Pak fertilizer resulted in less nutrient leaching and could be a better environmental choice.

  19. Effects of Controlled Release Urea on Wheat Yield and Nitrogen Utilization Efficiency Under Different Applied Conditions

    Directory of Open Access Journals (Sweden)

    XIA Wei-guang

    2014-02-01

    Full Text Available The field trial was conducted to study the effects of different nitrogen fertilizer applications on winter wheat yield, nitrogen utilization efficiency and economic benefit. 7 treatments were designed as CK(no nitrogen fertilizer applied, 100%PU10/0(conventional urea applied before sowing, N rate was 240 kg·hm-2, 100%PU6/4(conventional urea applied before sowing and at jointing with the ratio of 6∶4, N rate was 240 kg·hm-2, 80%PU6/4(conventional urea applied before sowing and at jointing with the ratio of 6∶4, N rate was 192 kg·hm-2, 100%CRU(resin coated controlled release urea applied before sowing, N rate was 240 kg·hm-2, 80%CRU(resin coated controlled release urea applied before sowing, N rate was 192 kg·hm-2, and 40%CRU+40%PU(resin coated controlled release urea and conventional urea applied before sowing, N rate was 192 kg·hm-2. The results showed that no matter on the efficiency of yield or that of nitrogen, resin coated controlled-release urea(CRU was better when compared with conventional urea(PU. Especially, the combined application treatment(40%CRU+40%PUwas the best with achieving the highest wheat yield of 7 709 kg·hm-2, the highest N fertilizer utilization efficiency of 36.44% and the maximum net income of 15 946 yuan·hm-2. And it could not only increase winter wheat yield with reducing the nitrogen fertilizer application, but also improve N fertilizer utilization efficiency and owe the highest ratio of output to input. Therefore, the combined application of the resin coated controlled-release urea and conventional urea(40%CRU+40%PUwas the optimal nitrogen fertilizer treatment under the conditions of this experiment.

  20. The Effects of Different Amounts of Controlled Release Fertilizer on the Root Growth and the Filling Rate in Winter Wheat

    OpenAIRE

    Meng Li; Jingtian Yang; Liyuan Yan; Yan Shi

    2014-01-01

    In order to increase the fertilizer use efficiency and yield in winter wheat, the effects of controlled release fertilizer on the root growth and the filling rate in winter wheat by applying different amounts of controlled release fertilizer had been studied in open field. The results indicated that conventional complex fertilizer and controlled release fertilizer could cause corresponding changes of the wheat root activity, dry root weight, root-shoot ratio and filling rate, but the fertiliz...

  1. Presternal subcutaneous bronchogenic cyst in adolescence

    Science.gov (United States)

    Moon, Sung Mo; Lee, Sang Min; Kang, Haeyoun; Choi, Hye Jeong

    2017-01-01

    Abstract Subcutaneous bronchogenic cysts have been described rarely, particularly among adolescents. Only a few reports have described the ultrasonographic features of bronchogenic cysts, characterizing them as nonspecific cystic masses with or without internal echogenic foci or debris. Therefore, it is hard to differentiate subcutaneous bronchogenic cysts from other subcutaneous cystic tumors ultrasonographically. We report a case of presternal subcutaneous bronchogenic cyst in an 18-year-old man with unusual ultrasonographic findings. Ultrasonography revealed a small, oval, cystic mass containing a well-circumscribed, heterogeneously hypoechoic, egg-shaped lesion in the dependent portion of the mass within the subcutaneous fat layer overlying the sternum. Surgical excision was performed, and the cystic mass was diagnosed as a bronchogenic cyst. On pathological examination, the internal, heterogeneously hypoechoic, ball-like lesion was found to be mucous material within the cyst. To our knowledge, this is the first reported case of a presternal subcutaneous bronchogenic cyst presenting with a ball-like lesion inside of the cyst. This unusual ultrasonographic feature can be a clue to the diagnosis of subcutaneous bronchogenic cyst. In conclusion, if an anechoic cyst containing an internal, well-circumscribed, hypoechoic ball-like lesion is seen in the presternal subcutaneous fat layer, subcutaneous bronchogenic cyst should be considered in the differential diagnosis of subcutaneous cystic masses. PMID:28151916

  2. Biocompatible Fe3O4 Increases the Efficacy of Amoxicillin Delivery against Gram-Positive and Gram-Negative Bacteria

    Directory of Open Access Journals (Sweden)

    Alexandru Mihai Grumezescu

    2014-04-01

    Full Text Available This paper reports the synthesis and characterization of amoxicillin- functionalized magnetite nanostructures (Fe3O4@AMO, revealing and discussing several biomedical applications of these nanomaterials. Our results proved that 10 nm Fe3O4@AMO nanoparticles does not alter the normal cell cycle progression of cultured diploid cells, and an in vivo murine model confirms that the nanostructures disperse through the host body and tend to localize in particular sites and organs. The nanoparticles were found clustered especially in the lungs, kidneys and spleen, next to the blood vessels at this level, while being totally absent in the brain and liver, suggesting that they are circulated through the blood flow and have low toxicity. Fe3O4@AMO has the ability to be easily circulated through the body and optimizations may be done so these nanostructures cluster to a specific target region. Functionalized magnetite nanostructures proved a great antimicrobial effect, being active against both the Gram positive pathogen S. aureus and the Gram negative pathogen E. coli. The fabricated nanostructures significantly reduced the minimum inhibitory concentration (MIC of the active drug. This result has a great practical relevance, since the functionalized nanostructures may be used for decreasing the therapeutic doses which usually manifest great severe side effects, when administrated in high doses. Fe3O4@AMO represents also a suitable approach for the development of new alternative strategies for improving the activity of therapeutic agents by targeted delivery and controlled release.

  3. [Subcutaneous teicoplanin for children with infectious endocarditis].

    Science.gov (United States)

    Carpentier, E; Roméo, B; El Samad, Y; Geslin-Lichtenberger, L; Maingourd, Y; Tourneux, P

    2013-07-01

    Infectious endocarditis in children requires prolonged antibiotic therapy. In adults, antibiotics administrated subcutaneously such as teicoplanin are an alternative to intravenous treatment. We report the use of subcutaneous teicoplanin, after an initial antibiotic treatment administrated intravenously, for 2 children treated for infectious endocarditis following an initial cardiac surgery. Serum concentrations of teicoplanin were within the target range after the adaptation in the teicoplanin subcutaneous dosages. The treatment was effective for both cases. No specific side effects related to the treatment were reported. Subcutaneous administration could be used for prolonged antibiotic therapy for the treatment of infectious endocarditis in children, after an initial intravenous treatment. Variability of the bioavailability of antibiotics administrated subcutaneously requires regular testing. Prospective, randomized trials comparing intravenous and subcutaneous administration of teicoplanin should be conducted to assess the efficacy and safety of this treatment. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

  4. Functional changes of dendritic cells in hypersensivity reactions to amoxicillin

    Directory of Open Access Journals (Sweden)

    C.M.F. Lima

    2010-10-01

    Full Text Available A better understanding of dendritic cell (DC involvement in responses to haptenic drugs is needed, because it represents a possible approach to the development of an in vitro test, which could identify patients prone to drug allergies. There are two main DC subsets: plasmacytoid DC (pDC and myeloid DC (mDC. β-lactams form hapten-carrier conjugates and may provide a suitable model to study DC behavior in drug allergy reactions. It has been demonstrated that drugs interact differently with DC in drug allergic and non-allergic patients, but there are no studies regarding these subsets. Our aim was to assess the functional changes of mDC and pDC harvested from an amoxicillin-hypersensitive 32-year-old woman who experienced a severe maculopapular exanthema as reflected in interleukin-6 (IL-6 production after stimulation with this drug and penicillin. We also aim to demonstrate, for the first time, the feasibility of this method for dendritic cell isolation followed by in vitro stimulation for studies of drug allergy physiopathology. DC were harvested using a double Percoll density gradient, which generates a basophil-depleted cell (BDC suspension. Further, pDC were isolated by blood DC antigen 4-positive magnetic selection and gravity filtration through magnetized columns. After stimulation with amoxicillin, penicillin and positive and negative controls, IL-6 production was measured by ELISA. A positive dose-response curve for IL-6 after stimulation with amoxicillin and penicillin was observed for pDC, but not for mDC or BDC suspension. These preliminary results demonstrate the feasibility of this methodology to expand the knowledge of the effect of dendritic cell activation by drug allergens.

  5. Formulation, characterization and physicochemical evaluation of amoxicillin effervescent tablets.

    Science.gov (United States)

    Aslani, Abolfazl; Sharifian, Tahereh

    2014-01-01

    Amoxicillin is a semisynthetic antibiotic, which is used as an antimicrobial drug. This study was designed to formulate amoxicillin effervescent tablets, aimed at improved patient compliance and increased drug stability. In this study, nine effervescent tablet formulations were prepared from amoxicillin trihydrate. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Powders and granules were evaluated for their particle size, bulk density, tapped density, compressibility index, Hausner's ratio and angle of repose. The effervescent tablets were then prepared from powders and granules of acceptable quality by direct compression and fusion methods. The tablets were evaluated for weight variation, friability, pH of solution, carbon dioxide (CO2) content, hardness, effervescence time, thickness, assay, content uniformity, water content and equilibrium moisture content. The results indicated better flowability of granules prepared by fusion method as compared with the direct compression. The percent weight variations of tablets were within the acceptable limit of 0.5%. The friability was less than 1% in all formulations. The solution pH of tablets prepared by direct compression and fusion methods ranged from 4.55 to 5.74 and 4.74-5.84, respectively. The CO2 amounts generated by of fusion method tablets were smaller as compared to the direct compression method. The hardness of tablets was 40.66-56 for direct compression method and 60.6-74.6 for fusion method. The tablets produced by the fusion method had a larger thickness and lower water content than tablets produced by direct compression method. Tablets prepared by the fusion method exhibited superior pre- and post-compression characteristics as compared to tablets prepared by direct compression method.

  6. Formulation, characterization and physicochemical evaluation of amoxicillin effervescent tablets

    Directory of Open Access Journals (Sweden)

    Abolfazl Aslani

    2014-01-01

    Full Text Available Background: Amoxicillin is a semisynthetic antibiotic, which is used as an antimicrobial drug. This study was designed to formulate amoxicillin effervescent tablets, aimed at improved patient compliance and increased drug stability. Materials and Methods: In this study, nine effervescent tablet formulations were prepared from amoxicillin trihydrate. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Powders and granules were evaluated for their particle size, bulk density, tapped density, compressibility index, Hausner′s ratio and angle of repose. The effervescent tablets were then prepared from powders and granules of acceptable quality by direct compression and fusion methods. The tablets were evaluated for weight variation, friability, pH of solution, carbon dioxide (CO 2 content, hardness, effervescence time, thickness, assay, content uniformity, water content and equilibrium moisture content. Results: The results indicated better flowability of granules prepared by fusion method as compared with the direct compression. The percent weight variations of tablets were within the acceptable limit of 0.5%. The friability was less than 1% in all formulations. The solution pH of tablets prepared by direct compression and fusion methods ranged from 4.55 to 5.74 and 4.74-5.84, respectively. The CO 2 amounts generated by of fusion method tablets were smaller as compared to the direct compression method. The hardness of tablets was 40.66-56 for direct compression method and 60.6-74.6 for fusion method. The tablets produced by the fusion method had a larger thickness and lower water content than tablets produced by direct compression method. Conclusion: Tablets prepared by the fusion method exhibited superior pre- and post-compression characteristics as compared to tablets prepared by direct compression method.

  7. Subcutaneous Emphysema—Beyond the Pneumoperitoneum

    OpenAIRE

    Ott, Douglas E.

    2014-01-01

    Background: Subcutaneous emphysema and gas extravasation outside of the peritoneal cavity during laparoscopy has consequences. Knowledge of the circumstances that increase the potential for subcutaneous emphysema is necessary for safe laparoscopy. Methods: A literature review and a PubMed search are the basis for this review. Conclusions: The known risk factors leading to subcutaneous emphysema during laparoscopy are multiple attempts at abdominal entry, improper cannula placement, loose fitt...

  8. Pillar[6]arene-valved mesoporous silica nanovehicles for multiresponsive controlled release.

    Science.gov (United States)

    Huang, Xuan; Du, Xuezhong

    2014-11-26

    The synthesis and host-guest chemistry of pillararene (PA) derivatives are a hot research topic, and the applications of PAs in relevant research fields are essential to explore. Carboxylate-substituted pillar[6]arene (CPA[6])-valved mesoporous silica nanoparticles (MSNs) functionalized with dimethylbenzimidazolium (DMBI) and bipyridinium (BP) stalks were constructed, respectively, for multiresponsive controlled release. CPA[6] encircled the DMBI or BP stalks to develop supramolecular nanovalves for encapsulation of cargo within the MSN pores. The release of cargo was triggered by acidic pH or competitive binding for the dethreading of CPA[6] and the opening of the nanovalves; moreover, coordination chemistry is the first strategy to activate CPA nanovalves by metal chelating with the carboxylate groups of CPA for cargo release. The controlled release of the CPA[6]-valved MSN delivery systems can meet diverse requirements and has promising biological applications in targeted drug therapy.

  9. Chitosan/TPP microparticles obtained by microemulsion method applied in controlled release of heparin.

    Science.gov (United States)

    Martins, Alessandro F; de Oliveira, Daiane M; Pereira, Antonio G B; Rubira, Adley F; Muniz, Edvani C

    2012-12-01

    This work deals with the preparation of chitosan/tripolyphosphate microparticles (CHT/TPP) using microemulsion system based on water/benzyl alcohol. The morphology of the microparticles was evaluated by scanning electron microscopy (SEM). The microparticles were also characterized through infrared spectroscopy (FTIR) and wide-angle X-ray scattering (WAXS). The morphology and crystallinity of microparticles depended mainly on CHT/TPP ratio. Studies of controlled release of HP were evaluated in distilled water and in simulated gastric fluid. Besides, the profile of HP releasing could be tailored by tuning the CHT/TPP molar ratio. Finally, these prospective results allow the particles to be employed as site-specific HP controlled release system. Copyright © 2012 Elsevier B.V. All rights reserved.

  10. Model-based computer-aided design for controlled release of pesticides

    DEFF Research Database (Denmark)

    Muro Sunè, Nuria; Gani, Rafiqul; Bell, G.

    2005-01-01

    In the field of controlled release technology for pesticides or active ingredients (AI), models that can predict its delivery during application are important for purposes of design and marketing of the pesticide product. Appropriate models for the controlled release of pesticides, if available......, can be used to study and analyze some of the important issues related to the design/application of the pesticide. This paper highlights the needs for predictive models and proposes the use of a computer aided modelling framework through which a collection of reliable and predictive constitutive...... extended models have been developed and implemented into a computer-aided system. The total model consisting of the property models embedded into the release models are then employed to study the release of different combinations of AIs and polymer-based microcapsules....

  11. Controlled release of small molecules from silica xerogel with limited nanoporosity.

    Science.gov (United States)

    Chen, Rong; Qu, Haibo; Agrawal, Ashwin; Guo, Shaoyun; Ducheyne, Paul

    2013-01-01

    Conventional sol-gel processing requires several distinct steps involving hydrolysis, condensation and drying to obtain a highly porous, glassy solid material. With the goal of achieving controlled release of small molecules, herein we focus on the acceleration of the condensation and drying steps by casting the hydrolyzed sol on a large open surface to achieve a denser 100 % silica xerogel structure. Thus, cast xerogel with a more limited porosity was prepared. The effect of synthesis parameters during sol-gel synthesis on the release kinetics of bupivacaine, vancomycin and cephalexin was investigated. The release kinetics fitted well with the Higuchi model, suggesting a diffusional release mechanism. Combining the release and nanostructure data, the formation mechanism of cast xerogel is described. Without introducing additional precursors or additives into sol-gel systems, sol-gel casting is an easy technique that further expands the applicability of sol-gel materials as excellent carriers for the controlled release of a variety of drugs.

  12. Photo-controlled release of fipronil from a coumarin triggered precursor.

    Science.gov (United States)

    Gao, Zhenhong; Yuan, Pengtao; Wang, Donghui; Xu, Zhiping; Li, Zhong; Shao, Xusheng

    2017-06-01

    Developing efficient controlled release system of insecticide can facilitate the better use of insecticide. We described here a first example of photo-controlled release of an insecticide by linking fipronil with photoresponsive coumarin covalently. The generated coumarin-fipronil (CF) precursor could undergo cleavage to release free fipronil in the presence of blue light (420nm) or sunlight. Photophysical studies of CF showed that it exhibited strong fluorescence properties. The CF had no obvious activity against mosquito larvae under dark, but it can be activated by light inside the mosquito larvae. The released Fip from CF by blue light irradiation in vitro retained its activity to armyworm (Mythimna separate) with LC50 value of 24.64μmolL-1. This photocaged molecule provided an alternative delivery method for fipronil. Copyright © 2017. Published by Elsevier Ltd.

  13. Formulation optimization of hydrodynamically balanced oral controlled release bioadhesive tablets of tramadol hydrochloride.

    Science.gov (United States)

    Singh, Bhupinder; Rani, Ashu; Babita; Ahuja, Naveen; Kapil, Rishi

    2010-01-01

    The directly compressible floating-bioadhesive tablets of tramadol were formulated using varying amounts Carbopol 971P (CP) and hydroxy-propylmethyl cellulose (HPMC), along with other requisite excipients. In vitro drug release profile, floatational characteristics and ex vivo bioadhesive strength using texture analyzer were determined, and systematically optimized using a 3(2) central composite design (CCD). The studies indicated successful formulation of gastroretentive compressed matrices with excellent controlled release, mucoadhesion and hydrodynamic balance. Comparison of the dissolution profiles of the optimized formulation, with optimal composition of CP:HPMC :: 80.0:125.0, with that of the marketed controlled release formulation other indicated analogy of drug release performance with each other. Validation of optimization study using eight confirmatory experimental runs indicated very high degree of prognostic ability of CCD with mean  SEM of â0.06%  0.37. Further, the study successfully unravels the effect of the polymers on the selected response variables.

  14. Cell microenvironment stimuli-responsive controlled-release delivery systems based on mesoporous silica nanoparticles

    Directory of Open Access Journals (Sweden)

    Chun-Ling Zhu

    2014-03-01

    Full Text Available To develop novel tumor cell microenvironment stimuli-responsive smart controlled-release delivery systems is one of the current common interests of materials science and clinical medicine. Meanwhile, mesoporous silica nanoparticles as a promising drug carrier have become the new area of interest in the field of biomedical application in recent years because of their unique characteristics and abilities to efficiently and specifically entrap cargo molecules. This review describes the more recent developments and achievements of mesoporous silica nanoparticles in drug delivery. In particular, we focus on the stimuli-responsive controlled-release systems that are able to respond to tumor cell environmental changes, such as pH, glucose, adenosine-5′-triphosphate (ATP, glutathione (GSH, and H2O2.

  15. Veiligheid en verdraagbaarheid van verneveling van amoxicilline + clavulaanzuur bij stabiele coPD-pati??nten

    NARCIS (Netherlands)

    Nijdam, Lars C.; Kuijvenhoven, J.C.; van der Valk, P.D.L.P.M.; Brusse-Keizer, M.G.J.; Van Der Palen, J.; Movig, K.L.L.

    2015-01-01

    OBJECTIVE: To study the safety and tolerability of nebulized amoxicillin + clavulanic acid in patients with stable COPD. Acute exacerbations in COPD are often treated with antibiotics. Previous studies showed ineffective amoxicillin concentrations in sputum in two thirds of the patients treated with

  16. Antimicrobial Effect of a Single Dose of Amoxicillin on the Oral Microbiota

    NARCIS (Netherlands)

    Wexell, Cecilia Larsson; Ryberg, Henrik; Andersson, Wivi-Anne Sjoberg; Blomqvist, Susanne; Colin, Pieter; Van Bocxlaer, Jan; Dahlen, Gunnar

    Purpose: Amoxicillin is commonly used in oral surgery for antimicrobial prophylaxis against surgical-site infection and bacteremia because of its effect on oral streptococci. The aim of this study was to determine whether amoxicillin reaches the break-point concentrations in saliva and has any

  17. Veiligheid en verdraagbaarheid van verneveling van amoxicilline + clavulaanzuur bij stabiele coPD-patienten

    NARCIS (Netherlands)

    Nijdam, Lars C.; Kuijvenhoven, J.C.; van der Valk, P.D.L.P.M.; Brusse-Keizer, Marjolein G.J.; Van Der Palen, J.; Movig, K.L.L.

    2015-01-01

    OBJECTIVE: To study the safety and tolerability of nebulized amoxicillin + clavulanic acid in patients with stable COPD. Acute exacerbations in COPD are often treated with antibiotics. Previous studies showed ineffective amoxicillin concentrations in sputum in two thirds of the patients treated with

  18. Interactions between Microcystis aeruginosa and coexisting amoxicillin contaminant at different phosphorus levels.

    Science.gov (United States)

    Liu, Ying; Chen, Shi; Chen, Xiao; Zhang, Jian; Gao, Baoyu

    2015-10-30

    Microcystis aeruginosa was cultured with 0.05-5 mg L(-1) of phosphorus and exposed to 200-500 ng L(-1) of amoxicillin for seven days. Amoxicillin presented no significant effect (p>0.05) on the growth of M. aeruginosa at phosphorus levels of 0.05 and 0.2 mg L(-1), but stimulated algal growth as a hormesis effect at phosphorus levels of 1 and 5 mg L(-1). Phosphorus and amoxicillin affected the contents of chlorophyll-a, adenosine triphosphate (ATP) and malondialdehyde, the expression of psbA and rbcL, as well as the activities of adenosinetriphosphatase and glutathione S-transferase in similar manners, but regulated the production and release of microcystins and the activities of superoxide dismutase and peroxidase in different ways. Increased photosynthesis activity was related with the ATP consumption for the stress response to amoxicillin, and the stress response was enhanced as the phosphorus concentration increased. The biodegradation of amoxicillin by M. aeruginosa increased from 11.5% to 28.2% as the phosphorus concentration increased. Coexisting amoxicillin aggravated M. aeruginosa pollution by increasing cell density and concentration of microcystins, while M. aeruginosa alleviated amoxicillin pollution via biodegradation. The interactions between M. aeruginosa and amoxicillin were significantly regulated by phosphorus (p<0.05) and led to a complicated situation of combined pollution. Copyright © 2015 Elsevier B.V. All rights reserved.

  19. Evolution of amoxicillin resistance of Helicobacter pylori in vitro: characterization of resistance mechanisms.

    Science.gov (United States)

    Qureshi, Nadia N; Gallaher, Brandon; Schiller, Neal L

    2014-12-01

    Helicobacter pylori is the major cause of peptic ulcers and gastric cancer in humans. Treatment involves a two or three drug cocktail, typically including amoxicillin. Increasing levels of resistance to amoxicillin contribute to treatment failures, and higher levels of resistance are believed to be due to multiple genetic mutations. In this study, we examined the progression of spontaneous genetic mutations that contribute to amoxicillin resistance in H. pylori when exposed to increasing concentrations of amoxicillin in vitro. During the selection process, we isolated five strains each of which had progressively higher levels of resistance. Using a whole genome sequencing approach, we identified mutations in a number of genes, notably pbp1, pbp2, hefC, hopC, and hofH, and by sequencing these genes in each isolate we were able to map the order and gradual accumulation of mutations in these isolates. These five isolates, each expressing multiple mutated genes and four transformed strains expressing individually mutated pbp1, hefC, or hofH, were characterized using minimum inhibitory concentrations, amoxicillin uptake, and efflux studies. Our results indicate that mutations in pbp1, hefC, hopC, hofH, and possibly pbp2 contribute to H. pylori high-level amoxicillin resistance. The data also provide evidence for the complexity of the evolution of amoxicillin resistance in H. pylori and indicate that certain families of genes might be more susceptible to amoxicillin resistance mutations than others.

  20. Amoxicillin and Ceftriaxone as Treatment Alternatives to Penicillin for Maternal Syphilis.

    Science.gov (United States)

    Katanami, Yuichi; Hashimoto, Takehiro; Takaya, Saho; Yamamoto, Kei; Kutsuna, Satoshi; Takeshita, Nozomi; Hayakawa, Kayoko; Kanagawa, Shuzo; Ohmagari, Norio

    2017-05-01

    There is no proven alternative to penicillin for treatment of maternal syphilis. We report 2 case-patients with maternal syphilis who were successfully treated without penicillin. We used amoxicillin and probenecid for the first case-patient and amoxicillin, probenecid, and ceftriaxone for the second case-patient.

  1. MMC controlled-release membranes attenuate epidural scar formation in rat models after laminectomy

    OpenAIRE

    Xie, Hao; Wang, Binbin; Shen, Xun; Qin, Jian; Jiang, Longhai; Yu, Chen; Geng, Dawei; Yuan, Tangbo; Wu, Tao; Cao, Xiaojian; Liu, Jun

    2017-01-01

    Epidural scar formation after laminectomy impede surgical outcomes of decompression. Mitomycin C (MMC) has been demonstrated to have significant inhibitory effects on epidural scar. This study was undertaken to develop an effective MMC controlled-release membrane and to investigate its effects on epidural scar in rat models of laminectomy. A total of 72 rats that underwent laminectomy were divided into three groups. Among them, 24 were treated with mitomycin C-polylactic acid (MMC-PLA) contro...

  2. Design of a gastroretentive mucoadhesive dosage form of furosemide for controlled release

    OpenAIRE

    Sharad S. Darandale; VAVIA, PRADEEP R.

    2012-01-01

    The aim of the present study was to develop and characterize a gastroretentive dosage form suitable for controlled drug release. It consists of a drug loaded polymeric film made up of a bilayer of immediate (IR) and controlled release (CR) layers folded into a hard gelatin capsule. Gastroretention results from unfolding and swelling of the film and its bioadhesion to the gastric mucosa. Furosemide, a drug with a narrow absorption window, was selected as the model drug. Inclusion of hydroxypro...

  3. Nutrients Release from a Novel Gel-Based Slow/Controlled Release Fertilizer

    OpenAIRE

    Ding, H.; Zhang, Y. S.; Li, W. H.; Zheng, X. Z.; Wang, M. K.; Tang, L. N.; Chen, D. L.

    2016-01-01

    A novel gel-based slow/controlled release fertilizer (G-CRF) was developed, which was produced by combining various natural, seminatural, and/or synthetic organic macromolecule materials and natural inorganic mineral with conventional NPK fertilizers. Its nutrient release characteristics were studied to compare with conventional fertilizers through the soil column leaching method. The influences of soil factors, including temperature, pH, water, and nutrient contents in the G-CRF on nutrient ...

  4. Silicone Doped Chitosan-Acrylamide Coencapsulated Urea Fertilizer: An Approach to Controlled Release Fertilizers

    OpenAIRE

    Siafu, Sempeho Ibahati

    2017-01-01

    In the absence of special management practices, urea is known to undergo chemical transformations resulting in severe losses (≈60–70%) of total fertilizer applied. In an attempt to design urea controlled release fertilizers in order to counterbalance the 60–70% loss, urea was cross-linked with chitosan and acrylamide under refluxed in situ copolymerization technique; the procedures were repeated with silicone doping prior cross-linking with MBA. The particles were characterized with FTIR/ATR,...

  5. Intercalation of urea into kaolinite for preparation of controlled release fertilizer

    OpenAIRE

    Mahdavi Fariba; Abdul Rashid Suraya; Khanif Yusop Mohd

    2014-01-01

    In this study urea was intercalated between layers of kaolinite by dry grinding technique to be used for preparing controlled release fertilizer. X-ray powder diffraction (XRPD) patterns confirmed the intercalation of urea into kaolinite by the significant expansion of the basal spacing of kaolinite layers from 0.710 nm to 1.090 nm. Fourier transform infrared spectroscopy (FT-IR) also confirmed the hydrogen bonding between urea and kaolinite. Based on CHNS ...

  6. Preparation and characterization of controlled-release fertilizers coated with marine polysaccharide derivatives

    Science.gov (United States)

    Wang, Jing; Liu, Song; Qin, Yukun; Chen, Xiaolin; Xing, Rong'e.; Yu, Huahua; Li, Kecheng; Li, Pengcheng

    2017-09-01

    Encapsulation of water-soluble nitrogen fertilizers by membranes can be used to control the release of nutrients to maximize the fertilization effect and reduce environmental pollution. In this research, we formulated a new double-coated controlled-release fertilizer (CRF) by using food-grade microcrystalline wax (MW) and marine polysaccharide derivatives (calcium alginate and chitosan-glutaraldehyde copolymer). The pellets of water-soluble nitrogen fertilizer were coated with the marine polysaccharide derivatives and MW. A convenient and eco-friendly method was used to prepare the CRF. Scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) were used to characterize the morphology and composition of the products. The nitrogen-release properties were determined in water using UV-Vis spectrophotometry. The controlled-release properties of the fertilizer were improved dramatically after coating with MW and the marine polysaccharide derivatives. The results show that the double-coated CRFs can release nitrogen in a controlled manner, have excellent controlled-release features, and meet the European Standard for CRFs.

  7. Alginate/quaternized carboxymethyl chitosan/clay nanocomposite microspheres: preparation and drug-controlled release behavior.

    Science.gov (United States)

    Liu, Bo; Luo, Jiwen; Wang, Xiaoying; Lu, Junxiang; Deng, Hongbing; Sun, Runcang

    2013-01-01

    Drug-delivery systems, using natural drug carriers, have become increasingly important because of their nontoxicity and biodegradability. In this study, firstly, quaternized carboxymethyl chitosan (QCMC) was intercalated into the interlayer of organic montmorillonite (OMMT) to obtain the QCMC/OMMT nanocomposites, their structure, morphology, and thermal stability were investigated. Next, crosslinked alginate/QCMC/OMMT (AQCOM) microsphere was obtained by crosslinking with CaCl2, and the drug-controlled release behavior was evaluated with bovine serum albumin (BSA) as model drug. The results suggested that, carboxyl groups in alginate and QCMC crosslinked with Ca(2+), quaternary ammonium groups in QCMC or OMMT electrostatically interacted with carboxyl groups in alginate, and there was stable three-dimensional network in AQCOM microsphere. The swelling ratio of AQCOM microspheres decreased with the increase of OMMT content, the lowest one was only about 45% compared to the microsphere without OMMT of 197%. Besides, the in vitro release results for BSA indicated that the AQCOM microsphere displayed more excellent encapsulation and controlled release capacities than the microsphere without OMMT. The in vitro active cutaneous anaphylaxis test was carried out on Guinea pigs, which revealed that AQCOM microsphere did not cause anaphylaxis. Therefore, QCMC/OMMT nanocomposites from natural materials are considerably suitable to apply as drug-controlled release carriers.

  8. Intercalation of urea into kaolinite for preparation of controlled release fertilizer

    Directory of Open Access Journals (Sweden)

    Mahdavi Fariba

    2014-01-01

    Full Text Available In this study urea was intercalated between layers of kaolinite by dry grinding technique to be used for preparing controlled release fertilizer. X-ray powder diffraction (XRPD patterns confirmed the intercalation of urea into kaolinite by the significant expansion of the basal spacing of kaolinite layers from 0.710 nm to 1.090 nm. Fourier transform infrared spectroscopy (FT-IR also confirmed the hydrogen bonding between urea and kaolinite. Based on CHNS elemental analysis, 20% (wt. urea was intercalated between kaolinite layers. The urea-intercalated kaolinite was mixed with hydroxypropyl methylcellulose (HPMC binder and was granulated to prepare the nitrogen-based controlled release fertilizer. To study the nitrogen release behavior of granules, ultraviolet/visible (UV-Vis spectroscopy was used through the diacetyl monoxime (DAM colorimetric method. The result of UV-Vis spectroscopy showed that intercalation of urea into kaolinite decreased the nitrogen release from 25.50 to 13.66 % after 24 hours and from 98.15 to 70.01% after 30 days incubation in water. According to the results, the prepared controlled release fertilizer (CRF behaved according to the standard for CRFs.

  9. [Fate and balance of bulk blending controlled release fertilizer nitrogen under continuous cropping of mustard].

    Science.gov (United States)

    Zhang, Pan-Pan; Fan, Xiao-Lin

    2012-10-01

    Under the conditions of applying water soluble fertilizer and its bulk blending with controlled release fertilizer (BB-CRF), and by using micro-lysimeter, this paper quantitatively studied the nitrogen (N) uptake by mustard, the soil N losses from N2O emission, leaching and others, and the N residual in soil in three rotations of continuously cropped mustard. In the treatment of BB-CRF with 25% of controlled release nitrogen, the N uptake by mustard increased with rotations, and the yield by the end of the experiment was significantly higher than that in the treatment of water soluble fertilizer. The cumulated N2O emission loss and the N leaching loss were obviously higher in treatment water soluble fertilizer than in treatment BB-CRF. NO3(-)-N was the primary form of N in the leachate. In relative to water soluble fertilizer, BB-CRF altered the fates of fertilizer nitrogen, i.e., the N uptake by mustard and the N residual in soil increased by 75.4% and 76.0%, and the N leaching loss and other apparent N losses decreased by 27.1% and 66.3%, respectively. The application of BB-CRF could be an effective way to reduce the various losses of fertilizer N while increase the fertilizer N use efficiency, and the controlled release fertilizer is the environmentally friendly fertilizer with the property of high N use efficiency.

  10. Fabrication and Evaluation of Multilayer Nanofiber-Hydrogel Meshes with a Controlled Release Property

    Directory of Open Access Journals (Sweden)

    Rigumula Wu

    2015-07-01

    Full Text Available Controlled release drug delivery systems enable the sustained release of bioactive molecules, and increase bioavailability over an extended length of time. Biocompatible and biodegradable materials such as polycaprolactone (PCL nanofibers and alginate hydrogel play a significant role in designing controlled release systems. Prolonged release of bioactive molecules is observed when these polymer materials are used as matrices independently. However, there has not been a report in the literature that shows how different molecules are released at various rates over time. The goal of this study is to demonstrate a novel drug delivery system that has a property of releasing designated drugs at various rates over a defined length of time. We fabricated multilayer nanofiber-hydrogel meshes using electrospun PCL nanofiber and alginate hydrogel, and evaluated their controlled release properties. The multilayer meshes are composed of sandwiched layers of alternating PCL nanofibers and alginate hydrogel. Adenosine triphosphate (ATP, encapsulated in the designated hydrogel layers, is used as a mock drug for the release study. The exposed top layer of the meshes demonstrates a dramatically higher burst release and shorter release time compared to the deeper layers. Such properties of the different layers within the meshes can be employed to achieve the release of multiple drugs at different rates over a specified length of time.

  11. Controlled release formulations of metribuzin: release kinetics in water and soil.

    Science.gov (United States)

    Kumar, Jitendra; Nisar, Keyath; Shakil, N A; Walia, Suresh; Parsad, Rajender

    2010-05-01

    Controlled release (CR) formulations of metribuzin in Polyvinyl chloride [(PVC) (emulsion)], carboxy methyl cellulose (CMC), and carboxy methyl cellulose-kaolinite composite (CMC-KAO), are reported. Kinetics of its release in water and soil was studied in comparison with the commercial formulation (75 DF). Metribuzin from the commercial formulation became non-detectable after 35 days whereas it attained maxima between 35-49 days and became non-detectable after 63 days in the developed products. Amongst the CR formulations, the release in both water and soil was the fastest in CMC and slowest in PVC. The CMC-KAO composite reduced the rate of release as compared to CMC alone. The diffusion exponent (n value) of metribuzin in water and soil ranged from 0.515 to 0.745 and 0.662 to 1.296, respectively in the various formulations. The release was diffusion controlled with half release time (t(1/2)) from different controlled release matrices of 12.98 to 47.63 days in water and 16.90 to 51.79 days in soil. It was 3.25 and 4.66 days, respectively in the commercial formulation. The period of optimum availability of metribuzin in water and soil from controlled released formulations ranged from 15.09 to 31.68 and 17.99 to 34.72 days as against 5.03 and 8.80 days in the commercial formulation.

  12. Self-assembled polyelectrolyte complexes films as efficient compression coating layers for controlled-releasing tablets.

    Science.gov (United States)

    Li, Wenyan; Huo, Mengmeng; Sen Chaudhuri, Arka; Yang, Chen; Cao, Dazhong; Wu, Zhenghong; Qi, Xiaole

    2017-05-01

    Currently, polysaccharide-based hydrogels are widely studied macromolecular networks to modify drug dissolution from controlled-releasing matrix tablets. Among them, polyelectrolyte complexes (PEC) films consisted of chitosan (CS) and sodium alginate (SA) could be obtained via spontaneously assembling under physiological gastrointestinal environment. Here, we utilized these self-assembled PEC films as an efficient coating materials to develop controlled-released matrix tablets through compression coating process, with paracetamol (APAP) as model drug. The constitutive and morphology characteristic studies on these PEC films illustrated that the mixture of CS and SA with the weight ratio of 1:1 would be an promising outer layer for compression-coating tablets. In addition, the in vitro drug releasing behavior experiments demonstrated that the optimized compression coating tablets displayed satisfied zero-order drug releasing profits. Furthermore, the in vivo pharmacokinetic studies of these APAP loaded compression-coated tablets in New Zealand rabbits gave that the T max (12.32 ± 1.05 h) was significantly prolonged (p tablets (Jinfuning ® ) after oral administration. These studies suggest that the compression-coated tablets with self-assembled PEC film as coating outer layer may be a promising strategy for peroral controlled release delivery system of water soluble drugs.

  13. Amoxicillin-loaded electrospun nanocomposite membranes for dental applications.

    Science.gov (United States)

    Furtos, Gabriel; Rivero, Guadalupe; Rapuntean, Sorin; Abraham, Gustavo A

    2017-07-01

    Electrospun nanocomposite matrices based on poly(ε-caprolactone) (PCL), nano-hydroxyapatite (nHAp) and amoxicillin (AMX) were designed and investigated for dental applications. nHAp provides good biocompatibility, bioactivity, osteoconductivity, and osteoinductivity properties, and AMX, as antibiotic model, controls and/or reduces bacterial contamination of periodontal defects while enhancing tissue regeneration. A series of polymeric nanocomposites was obtained by varying both the antibiotic and nHAp contents. Fibrous membranes of different compositions were obtained by electrospinning technique, and morphological, thermal, mechanical and surface properties were characterized. The incorporation of AMX seemed to alter the nHAp distribution within the microfibrous matrix. The interaction between AMX and nHAp affected the mechanical performance and modulated the antibiotic release behavior. AMX release profiles presented a burst release that depended on nHAp content, followed by a slow release stage where the drug content (85-100%) was released in 3 weeks. The antimicrobial activity of the AMX-loaded membranes was tested with four bacterial strains depended on both the drug and nHAp contents. Extensive mineralization in simulated body fluid (SBF) was evidenced by SEM/EDX analysis after 21 days. The studied electrospun nanocomposite amoxicillin-loaded membranes could be a promising fibrous-based antibiotic carrier system for dental and tissue engineering applications. © 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 105B: 966-976, 2017. © 2016 Wiley Periodicals, Inc.

  14. Allergy to cloxacillin with normal tolerance to amoxicillin and cefuroxime.

    Science.gov (United States)

    Domínguez-Ortega, J; Martínez-Alonso, J C; Marcos-Pérez, M C; Kindelan, C; Frades, A

    2006-01-01

    Cloxacillin is a semisynthetic penicillin widely used in nonmethicillin resistant Staphylococcus aureus infections. Several hypersensitivity reactions to cloxacillin have been reported, although IgE-mediated allergic reactions to the drug are rare and there is little information about possible tolerance to other semisynthetic penicillins or cephalosporins in patients with cloxacillin allergy. We present 2 patients with demonstrated IgE-mediated allergy to cloxacillin and tolerance to amoxicillin and cefuroxime. Case 1. A 47-year-old woman began treatment with cloxacillin due to acute cellulitis. After ingesting 500 mg of the drug, she experience generalized maculopapular eruption and facial angioedema. Case 2. A 55-year-old woman presented an episode of acute urticaria and labial angioedema 60 minutes after ingesting 500 mg of cloxacillin for a skin abscess. Skin prick tests were positive to cloxacillin in case 1 and negative in case 2. However, an intradermal test was positive to cloxacillin (2 mg/ml) in case 2. Simple-blind oral challenge tests with amoxicillin (1 g) and cefuroxime (500 mg) were well-tolerated by both patients. We present 2 patients allergic to cloxacillin with normal tolerance to other betalactam antibiotics, confirming that cross-reactivity among these antibiotics seems to be uncommon. Complete allergy study, including an oral challenge test, should be considered in these patients.

  15. One-pot, two-step enzymatic synthesis of amoxicillin by complexing with Zn2+.

    Science.gov (United States)

    Zhang, Ye-Wang; Liu, Rui-Jiang; Xu, Xi-Ming

    2010-09-01

    A one-pot, two-step enzymatic synthesis of amoxicillin from penicillin G, using penicillin acylase, is presented. Immobilized penicillin acylase from Kluyvera citrophila was selected as the biocatalyst for its good pH stability and selectivity. Hydrolysis of penicillin G and synthesis of amoxicillin from the 6-aminopenicillanic acid formed and D-p-hydroxyphenylglycine methyl ester were catalyzed in situ by a single enzyme. Zinc ions can react with amoxicillin to form complexes, and the yield of 76.5% was obtained after optimization. In the combined one-pot synthesis process, zinc sulfate was added to remove produced amoxicillin as complex for shifting the equilibrium to the product in the second step. By controlling the conditions in two separated steps, the conversion of the first and second step was 93.8% and 76.2%, respectively. With one-pot continuous procedure, a 71.5% amoxicillin yield using penicillin G was obtained.

  16. Pharmacokinetics and tissue distribution of amoxicillin in healthy and Salmonella Typhimurium-inoculated pigs

    DEFF Research Database (Denmark)

    Agerso, H.; Friis, C.; Nielsen, Jens

    2000-01-01

    Objective--To determine pharmacokinetics and tissue distribution of amoxicillin in healthy and Salmonella Typhimurium-inoculated pigs. Animals--12 healthy pigs and 12 S Typhimurium-inoculated pigs. Procedure-Concentration of amoxicillin in tissue was measured by use of high-performance liquid...... chromatography 4, 8, 12, and 24 hours after IM administration. Pharmacokinetic values of amoxicillin in plasma were assessed by use of a l-compartment model with first-order absorption. Results--Inoculation caused diarrhea and increased rectal temperature and WBC count. Absorption half-life was shorter...... pigs and from 0.22 to 0.36 in inoculated pigs. Conclusions and Clinical Relevance-Salmonella Typhimurium inoculation altered absorption of amoxicillin from the injection sire and prolonged elimination half-life. However, distribution of amoxicillin to intestinal tract tissue was only affected...

  17. Frontal subcutaneous blood flow, and epi- and subcutaneous temperatures during scalp cooling in normal man

    DEFF Research Database (Denmark)

    Bülow, J; Friberg, L; Gaardsting, O

    1985-01-01

    during cooling and rewarming and to measure the effect of scalp cooling on subcutaneous scalp blood flow, subcutaneous blood flow and epi- and subcutaneous temperatures were measured in the frontal region at the hairline border before and during cooling with a cooling helmet, during spontaneous rewarming...

  18. Hormesis effects of amoxicillin on growth and cellular biosynthesis of Microcystis aeruginosa at different nitrogen levels.

    Science.gov (United States)

    Liu, Ying; Chen, Xiao; Zhang, Jian; Gao, Baoyu

    2015-04-01

    Coexisting antibiotic contaminants have potential to regulate cyanobacterial bloom, and the regulation is likely affected by nitrogen supply. A typical cyanobaterium Microcystis aeruginosa was cultured with 0.05-50 mg L(-1) of nitrogen and exposed to 100-600 ng L(-1) of amoxicillin for 7 days. Algal growth was not significantly (p > 0.05) affected by amoxicillin at the lowest nitrogen level of 0.05 mg L(-1), stimulated by 600 ng L(-1) of amoxicillin at a moderate nitrogen level of 0.5 mg L(-1) and enhanced by 100-600 ng L(-1) of amoxicillin at higher nitrogen levels of 5-50 mg L(-1). Amoxicillin affected chlorophyll-a, psbA gene, and rbcL gene in a similar manner as algal growth, suggesting a regulation of algal growth via the photosynthesis system. At each nitrogen level, synthesis of protein and polysaccharides as well as production and release of microcystins (MCs) increased in response to environmental stress caused by amoxicillin. Expression of ntcA and mcyB showed a positive correlation with the total content of MCs under exposure to amoxicillin at nitrogen levels of 0.05-50 mg L(-1). Nitrogen and amoxicillin significantly (p amoxicillin contaminant on M. aeruginosa bloom should be fully considered during the combined pollution control of M. aeruginosa and amoxicillin.

  19. Gentamicin concentrations in human subcutaneous tissue

    DEFF Research Database (Denmark)

    Lorentzen, Hanne; Kallehave, Finn Lasse; Kolmos, Hans Jørn Jepsen

    1996-01-01

    in human subcutaneous adipose tissue by a microdialysis technique. Seven healthy young volunteers each had four microdialysis probes placed in the fat (subcutaneous) layer of the abdominal skin. After the administration of a 240-mg gentamicin intravenous bolus, consecutive measurements of the drug...

  20. Facilitated subcutaneous immunoglobulin administration (fSCIg)

    DEFF Research Database (Denmark)

    Blau, Igor-Wolfgang; Conlon, Niall; Petermann, Robert

    2016-01-01

    and diverse medical needs that treatments for SID management should strive to meet. In this special report, we study the opportunities provided by facilitated subcutaneous immunoglobulin administration (fSCIg) to treat patients for whom the conventional routes (intravenous and subcutaneous) are sub...

  1. Gentamicin concentrations in human subcutaneous tissue

    DEFF Research Database (Denmark)

    Lorentzen, Hanne; Kallehave, Finn Lasse; Kolmos, Hans Jørn Jepsen

    1996-01-01

    Wound infections frequently originate from the subcutaneous tissue. The effect of gentamicin in subcutaneous tissue has, however, normally been evaluated from concentrations in blood or wound fluid. The aim of the present study was to investigate the pharmacokinetic properties of gentamicin in hu...... the presence of sufficient concentrations in the adipose tissue to be effective against common bacteria....

  2. Stimulation of vascularization of a subcutaneous scaffold applicable for pancreatic islet-transplantation enhances immediate post-transplant islet graft function but not long-term normoglycemia

    OpenAIRE

    Smink, Alexandra M.; Shiri, Li; Swart, Daniël H; Hertsig, Don T; de Haan, Bart J.; Kamps, Jan A A M; Schwab, Leendert; van Apeldoorn, Aart A.; de Koning, Eelco; Faas, Marijke M.; Lakey, Jonathan R.T.; Vos, Paul

    2017-01-01

    Abstract The liver as transplantation site for pancreatic islets is associated with significant loss of islets, which can be prevented by grafting in a prevascularized, subcutaneous scaffold. Supporting vascularization of a scaffold to limit the period of ischemia is challenging and was developed here by applying liposomes for controlled release of angiogenic factors. The angiogenic capacity of platelet?derived growth factor, vascular endothelial growth factor, acidic fibroblast growth factor...

  3. Subcutaneous Emphysema—Beyond the Pneumoperitoneum

    Science.gov (United States)

    2014-01-01

    Background: Subcutaneous emphysema and gas extravasation outside of the peritoneal cavity during laparoscopy has consequences. Knowledge of the circumstances that increase the potential for subcutaneous emphysema is necessary for safe laparoscopy. Methods: A literature review and a PubMed search are the basis for this review. Conclusions: The known risk factors leading to subcutaneous emphysema during laparoscopy are multiple attempts at abdominal entry, improper cannula placement, loose fitting cannula/skin and fascial entry points, use of >5 cannulas, use of cannulas as fulcrums, torque of the laparoscope, increased intra-abdominal pressure, procedures lasting >3.5 hours, and attention to details. New additional risk factors acting as direct factors leading to subcutaneous emphysema risk and occurrence are total gas volume, gas flow rate, valveless trocar systems, and robotic fulcrum forces. Recognizing this spectrum of factors that leads to subcutaneous emphysema will yield greater patient safety during laparoscopic procedures. PMID:24680136

  4. Effect of single-dose amoxicillin on rat incisor odontogenesis: a morphological study.

    Science.gov (United States)

    Kumazawa, Kaido; Sawada, Takashi; Yanagisawa, Takaaki; Shintani, Seikou

    2012-06-01

    The effect of exposure to amoxicillin on tooth development remains to be elucidated. The purpose of this study was to investigate the effect of amoxicillin on rat incisor odontogenesis. Male Wistar rats weighing approximately 100 g were given a single intraperitoneal injection of 3.0 g/kg body weight amoxicillin. One week after injection, the rats were fixed, and the lower incisors were demineralized and prepared into paraffin sections for light microscopy (LM) and immunohistochemistry. Undemineralized samples were embedded in resin and ground for processing for contact microradiography (CMR) and scanning electron microscopy (SEM). Serum calcium, phosphate, and magnesium concentrations were measured. At 1 week after amoxicillin administration, LM, CMR, and SEM revealed a clear increase in the area of interglobular dentin, representing disruption of mineralization by odontoblasts. Immunohistochemistry demonstrated moderate levels of the small integrin-binding ligand N-linked glycoprotein family dentin matrix protein 1 in large areas of interglobular dentin. On the other hand, no morphological alteration or hypomineralization was observed in the enamel. Serum calcium values showed no significant differences between the control and experimental rats during the experimental period although both serum phosphate and magnesium levels increased at day 1 after amoxicillin injection. The results suggest that a single dose of amoxicillin specifically affects normal tooth dentin mineralization, but not enamel mineralization in rat incisor odontogenesis. The present results further our understanding of the clinical association between dentin abnormality and amoxicillin exposure during tooth development.

  5. Effect of chronic lead intoxication on the distribution and elimination of amoxicillin in goats

    Science.gov (United States)

    Soliman, Ahmed M.; Abu-Basha, Ehab A.; Youssef, Salah A. H.; Amer, Aziza M.; Murphy, Patricia A.; Hauck, Catherine C.; Gehring, Ronette

    2013-01-01

    A study of amoxicillin pharmacokinetics was conducted in healthy goats and goats with chronic lead intoxication. The intoxicated goats had increased serum concentrations of liver enzymes (alanine aminotransferase and γ-glutamyl transferase), blood urea nitrogen, and reactivated δ-aminolevulinic acid dehydratase compared to the controls. Following intravenous amoxicillin (10 mg/kg bw) in control and lead-intoxicated goats, elimination half-lives were 4.14 and 1.26 h, respectively. The volumes of distribution based on the terminal phase were 1.19 and 0.38 L/kg, respectively, and those at steady-state were 0.54 and 0.18 L/kg, respectively. After intramuscular (IM) amoxicillin (10 mg/kg bw) in lead-intoxicated goats and control animals, the absorption, distribution, and elimination of the drug were more rapid in lead-intoxicated goats than the controls. Peak serum concentrations of 21.89 and 12.19 µg/mL were achieved at 1 h and 2 h, respectively, in lead-intoxicated and control goats. Amoxicillin bioavailability in the lead-intoxicated goats decreased 20% compared to the controls. After amoxicillin, more of the drug was excreted in the urine from lead-intoxicated goats than the controls. Our results suggested that lead intoxication in goats increases the rate of amoxicillin absorption after IM administration and distribution and elimination. Thus, lead intoxication may impair the therapeutic effectiveness of amoxicillin. PMID:23820209

  6. Pharmacokinetics and relative bioavailability of an oral amoxicillin-apramycin combination in pigs.

    Science.gov (United States)

    Dai, Chongshan; Zhao, Tingting; Yang, Xing; Xiao, Xilong; Velkov, Tony; Tang, Shusheng

    2017-01-01

    A new compound granular premix of amoxicillin (20% w/w dry mass)/apramycin (5% w/w dry mass) was developed, and its pharmacokinetics and relative bioavailability were determined in pigs following oral administration following a cross-over study design. The pharmacokinetic parameters of amoxicillin (t1/2λ = 6.43 ± 4.85h, Cmax = 3.2 ± 1.35 μg·mL-1, Tmax = 1.92 ± 0.58, AUCINF = 8.98 ± 2.11 h·μg·mL-1) and apramycin (t1/2λ = 8.67±4.4h, Cmax = 0.23 ± 0.12 μg·mL-1, Tmax = 2.25 ± 0.82 h, AUCINF = 12.37 ± 8.64h·μg·mL-1) when administered as the amoxicillin-apramycin granular premix did not significantly differ from those for the single-ingredient powder form of each component. The relative bioavailability of amoxicillin following oral administration of the amoxicillin-apramycin granular premix was 22.62% when compared to the intramuscular administration of commercial amoxicillin sodium-powder. This is the first report of a new amoxicillin-apramycin combination which has a potential veterinary application the for prevention and treatment digestive tract infections in pigs.

  7. Hydrophilic magnetic nanoclusters with thermo-responsive properties and their drug controlled release

    Energy Technology Data Exchange (ETDEWEB)

    Meerod, Siraprapa [Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Naresuan University, Phitsanulok 65000 (Thailand); Rutnakornpituk, Boonjira; Wichai, Uthai [Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Naresuan University, Phitsanulok 65000 (Thailand); Center of Excellence in Biomaterials, Faculty of Science, Naresuan University, Phitsanulok 65000 Thailand (Thailand); Rutnakornpituk, Metha, E-mail: methar@nu.ac.th [Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Naresuan University, Phitsanulok 65000 (Thailand); Center of Excellence in Biomaterials, Faculty of Science, Naresuan University, Phitsanulok 65000 Thailand (Thailand)

    2015-10-15

    Synthesis and drug controlled release properties of thermo-responsive magnetic nanoclusters grafted with poly(N-isopropylacrylamide) (poly(NIPAAm)) and poly(NIPAAm-co-poly(ethylene glycol) methyl ether methacrylate) (PEGMA) copolymers were described. These magnetic nanoclusters were synthesized via an in situ radical polymerization in the presence of acrylamide-grafted magnetic nanoparticles (MNPs). Poly(NIPAAm) provided thermo-responsive properties, while PEGMA played a role in good water dispersibility to the nanoclusters. The ratios of PEGMA to NIPAAm in the (co)polymerization in the presence of the MNPs were fine-tuned such that the nanoclusters with good water dispersibility, good magnetic sensitivity and thermo responsiveness were obtained. The size of the nanoclusters was in the range of 50–100 nm in diameter with about 100–200 particles/cluster. The nanoclusters were well dispersible in water at room temperature and can be suddenly agglomerated when temperature was increased beyond the lower critical solution temperature (LCST) (32 °C). The release behavior of an indomethacin model drug from the nanoclusters was also investigated. These novel magnetic nanoclusters with good dispersibility in water and reversible thermo-responsive properties might be good candidates for the targeting drug controlled release applications. - Highlights: • Nanoclusters with good water dispersibility and magnetic response were prepared. • They were grafted with thermo-responsive poly(NIPAAm) and/or poly(PEGMA). • Poly(NIPAAm) provided thermo-responsive properties to the nanoclusters. • Poly(PEGMA) provided good water dispersibilityto the nanoclusters. • Accelerated and controllable releases of a drug from the nanoclusters were shown.

  8. Doses of controlled-release fertilizer for production of rubber tree rootstocks

    Directory of Open Access Journals (Sweden)

    Renato Luis Grisi Macedo

    2012-06-01

    Full Text Available This experimental study aimed to evaluate the effects of doses of controlled-release fertilizer (ALL on the development of rubber tree rootstocks. The fertilizer used was Osmocote®, scheduled to be released for 8-9 months and with the following composition: N (15%, P2O5 (9%, K2O (12%, Mg (1%, S (2.3%, B (0.02%, Cu (0.05%, Fe (1%, Mn (0.06%, Mo (0.02% and Zn (0.05%. A randomized block design was used, with four treatments and eight replicates of 20 plants per plot. The controlled-release fertilizer was added to Rendimax Floreira® substrate at doses of 0, 3, 6 and 9 g per liter, and rootstocks were produced in plastic containers with a capacity of two liters of substrate. Three seeds of clone GT 1 were scattered in each container and thinning was performed on day 60, leaving the most vigorous plant only. After the fourth leaf shot from each rootstock, the containers of each treatment were topped, due to compaction, with 300 mL of the relevant fertilizer and substrate mixture. The rootstocks were evaluated at eight months of age as to height, stem diameter (DC 5 cm above root collar, total dry matter, shoot and root dry matter, leaf nutrient levels and percentage of plants suitable for grafting (DC≥1.0 cm. Results revealed that adequate development and nutrition of rootstocks was achieved by using 6 g of controlled-release fertilizer per liter of substrate.

  9. Synthesis and Characterization of Chitosan- Alginate for Controlled Release of Isoniazid Drug

    Directory of Open Access Journals (Sweden)

    Sari Edi Cahyaningrum

    2015-03-01

    Full Text Available The aim of this research was to synthesize and characterize chitosan-calcium alginate as matrix isoniazid encapsulation to produce controlled release isoniazid drug. The microparticles were evaluated for surface morphology, functional groups, size particles, drug content and swelling index. The drug release kinetic was investigated at gastric and intestinal artificial pH. The results showed that isoniazid-calcium alginate-chitosan has majority particle diameter of 1001-1500 nm. The release mechanism of isoniazid was through combination of erosion and diffusion.

  10. Predictive property models for use in design of controlled release of pesticides

    DEFF Research Database (Denmark)

    Suné, Nuria Muro; Gani, Rafiqul; Bell, G.

    2005-01-01

    A model capable of predicting the release of an Active Ingredient (AI) from a specific device would be very useful in the field of pesticide controlled release technology for design purposes. For the release of an AI from a microcapsule a mathematical model is briefly presented here......-contribution model for polymers (GC-Flory EoS). Therefore, this model (GC-Flory EoS) is extended in order to suit the needs of the complex pesticide molecules. The results of the extension of the GC-Flory EoS model, together with a case study dealing with the release of a pesticide from a microcapsule as well...

  11. Building Adjustable Pre-storm Reservoir Flood-control Release Rules

    Science.gov (United States)

    Yang, Shun-Nien; Chang, Li-Chiu; Chang, Fi-John; Hsieh, Cheng-Daw

    2017-04-01

    Typhoons hit Taiwan several times every year, which could cause serious flood disasters. Because mountainous terrains and steep landforms can rapidly accelerate the speed of flood flow during typhoon events, rivers cannot be a stable source of water supply. Reservoirs become the most effective floodwater storage facilities for alleviating flood damages in Taiwan. The pre-storm flood-control release can significantly increase reservoir storage capacity available to store floodwaters for reducing downstream flood damage, while the uncertainties of total forecasted rainfalls are very high in different stages of an oncoming typhoon, which may cause the risk of water shortage in the future. This study proposes adjustable pre-storm reservoir flood-control release rules in three designed operating stages with various hydrological conditions in the Feitsui Reservoir, a pivot reservoir for water supply to Taipei metropolitan in Taiwan, not only to reduce the risk of reservoir flood control and downstream flooding but also to consider water supply. The three operating stages before an oncoming typhoon are defined upon the timings when: (1) typhoon news is issued (3-7days before typhoon hit); (2) the sea warning is issued (2-4 days before typhoon hit); and (3) the land warning is issued (1-2 days before typhoon hit). We simulate 95 historical typhoon events with 3000 initial water levels and build some pre-storm flood-control release rules to adjust the amount of pre-release based on the total forecasted rainfalls at different operating stages. A great number of simulations (68.4 millions) are conducted to extract their major consequences and then build the adjustable pre-storm reservoir flood-control release rules. Accordingly, given a total forecasted rainfall and a water level, reservoir decision makers can easily identify the corresponding rule to tell the amount of pre-release in any stage. The results show that the proposed adjustable pre-release rules can effectively

  12. Productivity of irrigated beans due to sources of stabilized nitrogen fertilizer and controlled release

    OpenAIRE

    Tatiely Gomes Bernardes; Pedro Marques da Silveira; Marcia Thaís de Melo Carvalho; Beáta Emöke Madari; Maria da Conceição Santana Carvalho

    2015-01-01

    ABSTRACT New nitrogen fertilizers are available in the market actually, however, does not have results on the efficiency of the Cerrado conditions. With that objective of this study was to evaluate the effect of urea including stabilized and controlled release urea on yield of irrigated common beans (Phaseolus vulgaris L) in no-tillage system. The experiment was conducted in the winter crop, at Embrapa Arroz e Feijão, in Santo Antônio de Goiás, State of Goiás, Brazil. The experimental design ...

  13. Asthma, Family History of Drug Allergy, and Age Predict Amoxicillin Allergy in Children.

    Science.gov (United States)

    Faitelson, Yoram; Boaz, Mona; Dalal, Ilan

    2017-12-06

    Suspected adverse reactions to amoxicillin are common, but there are no known factors that can predict amoxicillin allergy in children. In addition, methods used for the diagnosis of amoxicillin allergy are not standardized and their role in diagnosis is not clear. To identify predictive factors and to assess the role of skin test in the diagnosis of amoxicillin allergy in children. Children with a history of immediate (excluding anaphylaxis) or nonimmediate reactions to amoxicillin were tested by skin prick test, followed by oral graded challenge with amoxicillin. Clinical characteristics of the reaction before and after the challenge were recorded, and data of personal and relatives' drug allergies and atopy were collected for statistical analysis. Skin prick tests followed by an oral graded challenge with amoxicillin were performed on 133 children. The skin test result was not of clinical value because it was negative in all children. Three children (2%) had an immediate reaction and 7 children (5%) had a nonimmediate reaction. Asthma (odds ratio [OR], 0.12; 95% CI, 0.017-0.869; P = .03), family history of drug allergy (OR, 0.12; 95% CI, 0.026-0.613; P = .01), older age at reaction (OR, 0.837; 95% CI, 0.699-1; P = .05), and angioedema (OR, 0.22; 95% CI, 0.043-1.12; marginally significant at P = .069) were associated with reduced chance to pass the oral challenge. Skin prick test did not contribute to the diagnosis of amoxicillin allergy. The presence of asthma, family history of drug allergy, and older age at reaction can be used as predictive factors for true amoxicillin allergy in children. Copyright © 2017 American Academy of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  14. Amoxicillin Oxidative Degradation Synthesized by Nano Zero Valent Iron

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    AR Yazdanbakhsh

    2016-03-01

    Full Text Available Introduction: Amoxicillin is one of the most important groups of pharmaceuticals that benefits humans and animals. However, antibiotics excertion in wastewaters and environment have emerged as a serious risk to the biotic environment, and their toxic effects can harm the organisms. Iron-based metallic nanoparticles have received special attention in regard with remediation of groundwater contaminants. In the typical nZVI-based bimetallic particle system, Fe acts as the reducing agent. Thus, the present study aimed to evaluate the synthesis and characteristics of nZVI in regard with degrading AMX. Methods: In this study, nZVI nanoparticles were synthesized using the liquid-phase reduction method by EDTA as a stabilizer material. Structure and properties of nanoparticles were characterized by BET, SEM, XRD and EDX analysis. A multi-variate analysis was applied using a response surface methodology (RSM in order to develop a quadratic model as a functional relationship between AMX removal efficiency and independent variables ( initial pH values, dosage of nZVI, contact time and amoxicillin concentration. The four independent variables of solution pH (2–10, AMX concentration (5-45mg/l, contact time (5-85 min and nanoparticles dose (0.25 – 1.25 g were transformed to the coded values. Results: The study results demonstrated that more than 69 % of AMX was removed by nZVI. The optimal AMX removal conditions using nZVI were found as 1.25 g of nZVI, pH 4, contact time of 80 min and concentration of 30 mg/l. Conclusions: The ability of nZVI in degradation of AMX revealed that these materials can serve as a potential nano material with respect to the environmental remediation.

  15. Amoxicillin-induced exanthema in young adults with infectious mononucleosis: demonstration of drug-specific lymphocyte reactivity.

    Science.gov (United States)

    Renn, C N; Straff, W; Dorfmüller, A; Al-Masaoudi, T; Merk, H F; Sachs, B

    2002-12-01

    Teenagers and young adults frequently develop maculopapular exanthema following amoxicillin intake within infectious mononucleosis. The underlying pathomechanisms are still largely unknown. To investigate whether amoxicillin-induced exanthema in florid infectious mononucleosis is a disease-associated phenomenon or results from specific sensitization to the drug. Four patients with amoxicillin-induced exanthema within infectious mononucleosis were analysed in vivo by prick, intradermal and patch tests and in vitro by means of the lymphocyte transformation test (LTT) employing amoxicillin, ampicillin, benzylpenicillin and phenoxymethylpenicillin. Drug-specific sensitization to amoxicillin in the LTT was observed in three patients, two of whom showed a side-chain-specific sensitization to amoxicillin and ampicillin. The in vitro results were confirmed in vivo by skin tests. These data suggest that real sensitization to amoxicillin and ampicillin may occur within infectious mononucleosis and may be detected in vivo and in vitro by means of skin tests and the LTT.

  16. Acute dermatomyositis associated with generalized subcutaneous edema.

    Science.gov (United States)

    Lee, Ki-Hong; Lim, Sung-Ryoun; Kim, Yeon-Joo; Lee, Kyung-Ju; Myung, Dae-Seong; Jeong, Hae-Chang; Yoon, Woong; Lee, Shin-Seok; Park, Yong-Wook

    2008-06-01

    Generalized subcutaneous edema is an uncommon manifestation of inflammatory myopathy. We report a 48-year-old female patient who presented with severe generalized edema, an erythematous skin rash, dysphagia and proximal muscle weakness. She was diagnosed with dermatomyositis from the clinical signs, increased muscle enzymes, electromyographic findings and a muscle biopsy. Magnetic resonance imaging revealed increased signal intensity in the muscular and subcutaneous layers. The conditions causing generalized edema were excluded. It was concluded that the generalized edema was secondary to dermatomyositis. Aggressive treatments with high-dose glucocorticoids and immunosuppressive agents were used to control the severe subcutaneous edema.

  17. Estonian and Russian Federation amoxicillin formulations: a comparative study of in vitro dissolution.

    Science.gov (United States)

    Bronnikova, O; Matto, V; Meos, A

    2008-06-01

    The in vitro dissolution properties were compared for four different formulations from the Estonian drug market and four from the Russian Federation drug market. Seven of the eight formulations tested released at least 75% or 80% amoxicillin during 30- or 90-min dissolution tests (37 degrees C, purified water, 75 rpm), respectively. One marketed Russian Federation formulation released 74% amoxicillin over a 90-min period. The present study shows that, in general, the in vitro dissolution properties of the Russian Federation amoxicillin formulations are, with some minor exceptions, comparable to those of the Estonian formulations. Copyright 2008 Prous Science, S.A.U. or its licensors. All rights reserved.

  18. Efficacy of amoxicillin and amoxicillin/clavulanic acid in the prevention of infection and dry socket after third molar extraction. A systematic review and meta-analysis.

    Science.gov (United States)

    Arteagoitia, M-I; Barbier, L; Santamaría, J; Santamaría, G; Ramos, E

    2016-07-01

    Prophylactic use of amoxicillin and amoxicillin/clavulanic acid, although controversial, is common in routine clinical practice in third molar surgery. Our objective was to assess the efficacy of prophylactic amoxicillin with or without clavulanic acid in reducing the incidence of dry socket and/or infection after third molar extraction. We conducted a systematic review and meta-analysis consulting electronic databases and references in retrieved articles. We included double-blind placebo-controlled randomized clinical trials published up to June 2015 investigating the efficacy of amoxicillin with or without clavulanic acid on the incidence of the aforementioned conditions after third molar extraction. Relative risks (RRs) were estimated with a generic inverse-variance approach and a random effect model using Stata/IC 13 and Review Manager Version 5.2. Stratified analysis was performed by antibiotic type. We included 10 papers in the qualitative review and in the quantitative synthesis (1997 extractions: 1072 in experimental groups and 925 in controls, with 27 and 74 events of dry socket and/or infection, respectively). The overall RR was 0.350 (p<0.001; 95% CI 0.214 to 0.574). We found no evidence of heterogeneity (I2=0%, p=0.470). The number needed to treat was 18 (95% CI 13 to 29). Five studies reported adverse reactions (RR=1.188, 95% CI 0.658 to 2.146, p =0.567). The RRs were 0.563 for amoxicillin (95% CI 0.295 to 1.08, p=0.082) and 0.215 for amoxicillin/clavulanic acid (95% CI 0.117 to 0.395, p<0.001). Prophylactic use of amoxicillin does not significantly reduce the risk of infection and/or dry socket after third molar extraction. With amoxicillin/clavulanic acid, the risk decreases significantly. Nevertheless, considering the number needed to treat, low prevalence of infection, potential adverse reactions to antibiotics and lack of serious complications in placebo groups, the routine prescription of amoxicillin with or without clavulanic acid is not

  19. Effect of Control-released Basic Fibroblast Growth Factor Incorporated in β-Tricalcium Phosphate for Murine Cranial Model

    Directory of Open Access Journals (Sweden)

    Azusa Shimizu, MD

    2014-03-01

    Conclusions: These findings suggest that control-released bFGF incorporated in β-TCP can accelerate bone regeneration in the murine cranial defect model and may be promising for the clinical treatment of cranial defects.

  20. Controlled-Release Oxycodone and Naloxone in the Treatment of Chronic Low Back Pain: A Placebo-Controlled, Randomized Study

    Directory of Open Access Journals (Sweden)

    C Cloutier

    2013-01-01

    Full Text Available BACKGROUND: For Canadian regulatory purposes, an analgesic study was required to complement previously completed, pivotal studies on bowel effects and analgesia associated with controlled-release (CR oxycodone/CR naloxone.

  1. In vitro characterization of a controlled-release ocular insert for delivery of brimonidine tartrate.

    Science.gov (United States)

    Mealy, J E; Fedorchak, M V; Little, S R

    2014-01-01

    Glaucoma is the second leading cause of blindness in the US. Brimonidine tartrate (BT) is a modern anti-glaucoma agent that is currently administered as frequently as a thrice-daily topical eye drop medication. Accordingly, compliance with BT regimens is low, limiting overall effectiveness. One attempt that has previously proved effective in addressing non-adherence is the formation of ocular inserts, such as the Ocusert(®), whose diffusion-based control released an older drug (pilocarpine) for a week-long period. Modern controlled drug-release technology provides an avenue for extending the release of practically any drug (including new drugs such as BT) for as long as 1 month from a singular insert. Currently, no controlled-release formulations for BT exist. This work outlines the development and characterization of a BT-releasing ocular insert designed from poly(lactic co-glycolic) acid/polyethylene glycol (PEG). It was found that a formulation containing 15% PEG can be created that produces a linear BT-release profile corresponding to BT eye drop delivery estimates. Additionally, these inserts were shown, through the use of atomic force microscopy and scanning electron microscopy, to have smooth surfaces and physical properties suitable for ophthalmic use. Copyright © 2013 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.

  2. Controlled Release of Doxorubicin from Doxorubicin/γ-Polyglutamic Acid Ionic Complex

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    Bhavik Manocha

    2010-01-01

    Full Text Available Formation of drug/polymer complexes through ionic interactions has proven to be very effective for the controlled release of drugs. The stability of such drug/polymer ionic complexes can be greatly influenced by solution pH and ionic strength. The aim of the current work was to evaluate the potential of γ-polyglutamic acid (γ-PGA as a carrier for the anticancer drug, Doxorubicin (DOX. We investigated the formation of ionic complexes between γ-PGA and DOX using scanning electron microscopy, spectroscopy, thermal analysis, and X-ray diffraction. Our studies demonstrate that DOX specifically interacts with γ-PGA forming random colloidal aggregates and results in almost 100% complexation efficiency. In vitro drug release studies illustrated that these complexes were relatively stable at neutral pH but dissociates slowly under acidic pH environments, facilitating a pH-triggered release of DOX from the complex. Hydrolytic degradation of γ-PGA and DOX/γ-PGA complex was also evaluated in physiological buffer. In conclusion, these studies clearly showed the feasibility of γ-PGA to associate cationic drug such as DOX and that is may serve as a new drug carrier for the controlled release of DOX in malignant tissues.

  3. Application of controlled release glass in the production of French marigold (Tagetes patula L.

    Directory of Open Access Journals (Sweden)

    Vujošević Ana

    2012-01-01

    Full Text Available This paper investigates the possibility and justification of controlled release glass application as a new ecological material in the production of plants-seedlings of French marigold (Tagetes patula L.. During the investigation its influence on the development of the produced plants-seedlings was monitored. The seedlings were produced in poly-propylene containers (speedling system and poly-propylene pots (pot system. The trial was conducted in the greenhouse at the Faculty of Agriculture in Belgrade during 2011. In the course of seedling production the glass granulation of < 0.5 mm was added in the following doses: 0, 1, 2, 3, and 4 g/l. The results of the research show a positive effect of controlled release glass application in the production of French marigold seedlings, since high quality seedlings were produced justifying its application. The best effect on the analyzed parameters of plant-seedling development was found when substrate was applied in the dose of 1 g/l.

  4. Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion.

    Science.gov (United States)

    Malode, Vilas N; Paradkar, Anant; Devarajan, Padma V

    2015-08-01

    We present hot melt extrusion (HME) for the design of floating multiparticulates. Metoprolol succinate was selected as the model drug. Our foremost objective was to optimize the components Eudragit(®) RS PO, polyethylene oxide (PEO) and hydroxypropyl methylcellulose (HPMC) to balance both buoyancy and controlled release. Gas generated by sodium bicarbonate in acidic medium was trapped in the polymer matrix to enable floating. Eudragit(®) RS PO and PEO with sodium bicarbonate resulted in multiparticulates which exhibited rapid flotation within 3 min but inadequate total floating time (TFT) of 3h. Addition of HPMC to the matrix did not affect floating lag time (FLT), moreover TFT increased to more than 12h with controlled release of metoprolol succinate. Floating multiparticulates exhibited t50% of 5.24h and t90% of 10.12h. XRD and DSC analysis revealed crystalline state of drug while FTIR suggested nonexistence of chemical interaction between the drug and the other excipients. The assay, FLT, TFT and the drug release of the multiparticulates were unchanged when stored at 40°C/75%RH for 3 months confirming stability. We present floating multiparticulates by HME which could be extrapolated to a range of other drugs. Our approach hence presents platform technology for floating multiparticulates. Copyright © 2015 Elsevier B.V. All rights reserved.

  5. Modified tamarind kernel polysaccharide: a novel matrix for control release of aspirin.

    Science.gov (United States)

    Ghosh, Sandipta; Pal, Sagar

    2013-07-01

    pH dependent hydrogels of modified tamarind kernel polysaccharide (TKP) were synthesized by grafting with polyacrylamide chains on TKP backbone in presence of microwave irradiation and initiator. The present study is carried out to design oral controlled drug delivery systems for aspirin using synthesized hydrogels as carrier in form of tablets. TKP-g-PAM based hydrogels show significant enhancement for control release of aspirin. Release behavior of aspirin has been evaluated using USP type I apparatus in 900 mL of buffer solutions (pH 1.2, 6.8, 7.4), maintained at 37°C at 100 rpm. It is observed that with increase in percentage of grafting (% G), swelling of matrices increases whereas erosion and rate of drug release decrease. The effect of % G onto t50 value (time taken for release of 50% drug) has also been discussed. The release characteristics from the matrices under study show non-Fickian diffusion mechanism, suggesting the controlled release of aspirin. Copyright © 2013 Elsevier B.V. All rights reserved.

  6. Zinc polycarboxylate dental cement for the controlled release of an active organic substance: proof of concept.

    Science.gov (United States)

    Ali, Mohammad Naseem; Edwards, Mark; Nicholson, John W

    2010-04-01

    The potential of employing zinc polycarboxylate dental cement as a controlled release material has been studied. Benzalkonium chloride was used as the active ingredient, and incorporated at concentrations of 1, 2 and 3% by mass within the cement. At these levels, there was no observable effect on the speed of setting. Release was followed using an ion-selective electrode to determine changes in chloride ion concentration with time. This technique showed that the additive was released when the cured cement was placed in water, with release occurring by a diffusion mechanism for the first 3 h, but continuing beyond that for up to 1 week. Diffusion coefficients were in the range 5.62 x 10(-6) cm(2) s(-1) (for 1% concentration) to 10.90 x 10(-6) cm(2) s(-1) (for 3% concentration). Up to 3% of the total loading of benzalkonium chloride was released from the zinc polycarboxylate after a week, which is similar to that found in previous studies with glass-ionomer cement. It is concluded that zinc polycarboxylate cement is capable of acting as a useful material for the controlled release of active organic compounds.

  7. Evaluation of microwave assisted grafted sago starch as controlled release polymeric carrier.

    Science.gov (United States)

    Singh, Akhilesh Vikram; Nath, Lila Kanta

    2013-09-01

    In the present investigation an attempt has been made to develop a new co-polymeric material for controlled release tablet formulations. The acrylamide grafting was successfully performed on the backbone of sago starch. The modified starch was tested for acute toxicity and drug-excipient compatibility study. The grafted material was used in making of controlled release tablets of lamivudine. The formulations were evaluated for physical characteristics such as hardness, friability, %drug content and weight variations. The in vitro release study showed that the optimized formulation exhibited highest correlation (R) value in case of Higuchi model and the release mechanism of the optimized formulation predominantly exhibited combination of diffusion and erosion process. There was a significant difference in the pharmacokinetic parameters (T(max), C(max), AUC, V(d), T(1/2) and MDT) of the optimized formulation as compared to the marketed conventional tablet Lamivir(®) was observed. The pharmacokinetics parameters were showed controlled pattern and better bioavailability. The optimized formulation exhibited good stability and release profile at the accelerated stability conditions. Copyright © 2013 Elsevier B.V. All rights reserved.

  8. Promising applications of cyclodextrins in food: Improvement of essential oils retention, controlled release and antiradical activity.

    Science.gov (United States)

    Kfoury, Miriana; Auezova, Lizette; Greige-Gerges, Hélène; Fourmentin, Sophie

    2015-10-20

    Essential oils (EOs) are gaining great interest as alternatives for harmful synthetic food preservatives. Due to their volatile nature, they could be applied in food packaging to improve food quality and extend shelf-life. To provide long-term effects of EOs by increasing their retention and ensuring controlled release of their components, they could be encapsulated in cyclodextrins (CDs). Herein, the ability of six CDs to retain nine EOs and to bind their individual components was investigated. Retention capacities and binding abilities of CDs were assessed by static headspace-gas chromatography (SH-GC) using a new validated "rapid method". The ability of CDs to generate controlled release systems was examined by multiple headspace extraction (MHE). Finally, radical scavenging activity of free and encapsulated EOs was evaluated. The highest retention capacity toward the studied EOs was obtained for β-CD and its derivatives (69-78%). Also, β-CD and its derivatives showed, with one exception, the highest Kf values for all the studied guests. In addition, encapsulation in CDs reduced the releasing rate of EO components (from 1.43 to 2.43-fold for β-CD/Satureja montana EO used as a model). Furthermore, the inclusion complexes showed higher ABTS(+) scavenging capacity than the free EOs. Results confirmed the usefulness of CDs as encapsulant for EOs and should encourage their application in food and as part of active packaging systems. Copyright © 2015 Elsevier Ltd. All rights reserved.

  9. Preparation and investigation of controlled-release glipizide novel oral device with three-dimensional printing.

    Science.gov (United States)

    Li, Qijun; Wen, Haoyang; Jia, Danyang; Guan, Xiaoying; Pan, Hao; Yang, Yue; Yu, Shihui; Zhu, Zhihong; Xiang, Rongwu; Pan, Weisan

    2017-06-15

    The purpose of this study was to explore the feasibility of combining fused deposition modeling (FDM) 3D printing technology with hot melt extrusion (HME) to fabricate a novel controlled-release drug delivery device. Glipizide used in the treatment of diabetes was selected as model drug, and was successfully loaded into commercial polyvinyl alcohol (PVA) filaments by HME method. The drug-loaded filaments were printed through a dual-nozzle 3D printer, and finally formed a double-chamber device composed by a tablet embedded within a larger tablet (DuoTablet), each chamber contains different contents of glipizide. The drug-loaded 3D printed device was evaluated for drug release under in vitro dissolution condition, and we found the release profile fit Korsmeyer-Peppas release kinetics. With the double-chamber design, it is feasible to design either controlled drug release or delayed drug release behavior by reasonably arranging the concentration distribution of the drug in the device. The characteristics of the external layer performed main influence on the release profile of the internal compartment such as lag-time or rate of release. The results of this study suggest the potential of 3D printing to fabricate controlled-release drug delivery system containing multiple drug concentration distributions via hot melt extrusion method and specialized design configurations. Copyright © 2017 Elsevier B.V. All rights reserved.

  10. Biodegradable soy wound dressings with controlled release of antibiotics: Results from a guinea pig burn model.

    Science.gov (United States)

    Egozi, Dana; Baranes-Zeevi, Maya; Ullmann, Yehuda; Gilhar, Amos; Keren, Aviad; Matanes, Elias; Berdicevsky, Israela; Krivoy, Norberto; Zilberman, Meital

    2015-11-01

    There is growing interest in the development of biodegradable materials from renewable biopolymers, such as soy protein, for biomedical applications. Soy protein is a major fraction of natural soybean and has the advantages of being economically competitive, biodegradable and biocompatible. It presents good water resistance as well as storage stability. In the current study, homogenous antibiotic-loaded soy protein films were cast from aqueous solutions. The antibiotic drug gentamicin was incorporated into the films in order to inhibit bacterial growth, and thus prevent or combat infection, upon its controlled release to the surrounding tissue. The current in vivo study of the dressing material in contaminated deep second-degree burn wounds in guinea pigs (n=20) demonstrated its ability to accelerate epithelialization with 71% epithelial coverage compared to an unloaded format of the soy material (62%) and a significant improved epithelial coverage as compared to the conventional dressing material (55%). Our new platform of antibiotic-eluting wound dressings is advantageous over currently used popular dressing materials that provide controlled release of silver ions, due to its gentamicin release profile, which is safer. Another advantage of our novel concept is that it is based on a biodegradable natural polymer and therefore does not require bandage changes and offers a potentially valuable and economic approach for treating burn-related infections. Copyright © 2015 Elsevier Ltd and ISBI. All rights reserved.

  11. Improving the controlled release of water-insoluble emodin from amino-functionalized mesoporous silica

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    Xu Yunqiang; Wang Chunfeng [Shandong Provincial Key Laboratory of Fine Chemicals, School of Chemistry, Shandong Polytechnic University, Jinan 250353, Shandong (China); Zhou Guowei, E-mail: guoweizhou@hotmail.com [Shandong Provincial Key Laboratory of Fine Chemicals, School of Chemistry, Shandong Polytechnic University, Jinan 250353, Shandong (China); Wu Yue; Chen Jing [Shandong Provincial Key Laboratory of Fine Chemicals, School of Chemistry, Shandong Polytechnic University, Jinan 250353, Shandong (China)

    2012-06-15

    Several types of amino-functionalized mesoporous silica, including F5-SBA-15, F10-SBA-15, and F15-SBA-15 were prepared through co-condensation of tetraethoxysilane (TEOS) and (3-aminopropyl)triethoxysilane (APTES) in varying molar ratios (5 mol%, 10 mol%, and 15 mol%) via a hydrothermal process. The materials obtained were characterized by means of small-angle X-ray powder diffraction, scanning electron microscopy, transmission electron microscopy, N{sub 2} adsorption-desorption, Fourier transformed infrared spectra, and X-ray photoelectron spectroscopy. Increasing APTES molar ratios decreased the degree of orderliness of the functionalized mesoporous silica. Pure and amino-functionalized SBA-15 samples were employed as supports for the controlled release of water-insoluble drug emodin. Loading experiments showed that drug loading capacities mainly depended on the surface areas and pore diameters of the carriers. Controlled release profiles of emodin-loaded samples were studied in phosphate buffered saline (PBS, pH 7.4), and results indicated that the emodin release rate could be controlled by surface amino-functionalized carriers. Emodin loaded on functionalized mesoporous supports exhibited a lower release rate than that of loaded on pure SBA-15, emodin loaded on F10-SBA-15 showed the smallest release amount (71.74 wt%) after stirring in PBS for 60 h. Findings suggest that functionalized mesoporous SBA-15 is a promising carrier for achieving prolonged release time periods.

  12. Controlled release of doxorubicin from electrospun PEO/chitosan/graphene oxide nanocomposite nanofibrous scaffolds.

    Science.gov (United States)

    Ardeshirzadeh, Behnaz; Anaraki, Nadia Aboutalebi; Irani, Mohammad; Rad, Leila Roshanfekr; Shamshiri, Soodeh

    2015-03-01

    Polyethylene oxide (PEO)/chitosan (CS)/graphene oxide (GO) electrospun nanofibrous scaffolds were successfully developed via electrospinning process for controlled release of doxorubicin (DOX). The SEM analysis of nanofibrous scaffolds with different contents of GO (0.1, 0.2, 0.5 and 0.7wt.%) indicated that the minimum diameter of nanofibers was found to be 85nm for PEO/CS/GO 0.5% nanofibers. The π-π stacking interaction between DOX and GO with fine pores of nanofibrous scaffolds exhibited higher drug loading (98%) and controlled release of the DOX loaded PEO/CS/GO nanofibers. The results of DOX release from nanofibrous scaffolds at pH5.3 and 7.4 indicated strong pH dependence. The hydrogen bonding interaction between GO and DOX could be unstable under acidic conditions which resulted in faster drug release rate in pH5.3. The cell viability results indicated that DOX loaded PEO/CS/GO/DOX nanofibrous scaffold could be used as an alternative source of DOX compared with free DOX to avoid the side effects of free DOX. Thus, the prepared nanofibrous scaffold offers as a novel formulation for treatment of lung cancer. Copyright © 2014 Elsevier B.V. All rights reserved.

  13. Starch-based hydrogel loading with carbendazim for controlled-release and water absorption.

    Science.gov (United States)

    Bai, Chan; Zhang, Sufen; Huang, Lei; Wang, Haiyan; Wang, Wei; Ye, Qingfu

    2015-07-10

    Starch, with properties of eco-friendliness and abundance, is one of the most important natural polymers. Starch-based hydrogels were investigated as carriers of carbendazim to combine controlled-release and water absorption (WA). Three carbendazim-loaded hydrogels (CLHs) with different WA capacities were prepared by solution polymerization. The CLHs were characterized by Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and liquid-chromatography mass-spectrometry (LC-MS/MS). Release kinetics of CLHs was investigated using (14)C-labeling method. The diffusion parameters of CLHs were 0.47, 0.57 and 0.81 in deionized H2O (ddH2O). WA affected release profile significantly, the release longevity reaching 240 h when WA was 800 g/g in ddH2O. Solution pH influenced release profiles and the lowest release rate occurred in the lowest pH. Addition of CLH (1.3g/kg soil) markedly increased water-holding capacity (WHC) of soil by 8.2%. The study indicated that starch-based CLH was a good controlled-release agent for carbendazim and water absorbent for soil. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. Composite microsphere-functionalized scaffold for the controlled release of small molecules in tissue engineering

    Directory of Open Access Journals (Sweden)

    Laura Pandolfi

    2016-01-01

    Full Text Available Current tissue engineering strategies focus on restoring damaged tissue architectures using biologically active scaffolds. The ideal scaffold would mimic the extracellular matrix of any tissue of interest, promoting cell proliferation and de novo extracellular matrix deposition. A plethora of techniques have been evaluated to engineer scaffolds for the controlled and targeted release of bioactive molecules to provide a functional structure for tissue growth and remodeling, as well as enhance recruitment and proliferation of autologous cells within the implant. Recently, novel approaches using small molecules, instead of growth factors, have been exploited to regulate tissue regeneration. The use of small synthetic molecules could be very advantageous because of their stability, tunability, and low cost. Herein, we propose a chitosan–gelatin scaffold functionalized with composite microspheres consisting of mesoporous silicon microparticles and poly(dl-lactic-co-glycolic acid for the controlled release of sphingosine-1-phospate, a small molecule of interest. We characterized the platform with scanning electron microscopy, Fourier transform infrared spectroscopy, and confocal microscopy. Finally, the biocompatibility of this multiscale system was analyzed by culturing human mesenchymal stem cells onto the scaffold. The presented strategy establishes the basis of a versatile scaffold for the controlled release of small molecules and for culturing mesenchymal stem cells for regenerative medicine applications.

  15. Hydrophobic Drug-Loaded PEGylated Magnetic Liposomes for Drug-Controlled Release

    Science.gov (United States)

    Hardiansyah, Andri; Yang, Ming-Chien; Liu, Ting-Yu; Kuo, Chih-Yu; Huang, Li-Ying; Chan, Tzu-Yi

    2017-05-01

    Less targeted and limited solubility of hydrophobic-based drug are one of the serious obstacles in drug delivery system. Thus, new strategies to enhance the solubility of hydrophobic drug and controlled release behaviors would be developed. Herein, curcumin, a model of hydrophobic drug, has been loaded into PEGylated magnetic liposomes as a drug carrier platform for drug controlled release system. Inductive magnetic heating (hyperthermia)-stimulated drug release, in vitro cellular cytotoxicity assay of curcumin-loaded PEGylated magnetic liposomes and cellular internalization-induced by magnetic guidance would be investigated. The resultant of drug carriers could disperse homogeneously in aqueous solution, showing a superparamagnetic characteristic and could inductive magnetic heating with external high-frequency magnetic field (HFMF). In vitro curcumin release studies confirmed that the drug carriers exhibited no significant release at 37 °C, whereas exhibited rapid releasing at 45 °C. However, it would display enormous (three times higher) curcumin releasing under the HFMF exposure, compared with that without HFMF exposure at 45 °C. In vitro cytotoxicity test shows that curcumin-loaded PEGylated magnetic liposomes could efficiently kill MCF-7 cells in parallel with increasing curcumin concentration. Fluorescence microscopy observed that these drug carriers could internalize efficiently into the cellular compartment of MCF-7 cells. Thus, it would be anticipated that the novel hydrophobic drug-loaded PEGylated magnetic liposomes in combination with inductive magnetic heating are promising to apply in the combination of chemotherapy and thermotherapy for cancer therapy.

  16. Controlled Release of Lysozyme from Double-Walled Poly(Lactide-Co-Glycolide (PLGA Microspheres

    Directory of Open Access Journals (Sweden)

    Rezaul H. Ansary

    2017-10-01

    Full Text Available Double-walled microspheres based on poly(lactide-co-glycolide (PLGA are potential delivery systems for reducing a very high initial burst release of encapsulated protein and peptide drugs. In this study, double-walled microspheres made of glucose core, hydroxyl-terminated poly(lactide-co-glycolide (Glu-PLGA, and carboxyl-terminated PLGA were fabricated using a modified water-in-oil-in-oil-in-water (w1/o/o/w2 emulsion solvent evaporation technique for the controlled release of a model protein, lysozyme. Microspheres size, morphology, encapsulation efficiency, lysozyme in vitro release profiles, bioactivity, and structural integrity, were evaluated. Scanning electron microscopy (SEM images revealed that double-walled microspheres comprising of Glu-PLGA and PLGA with a mass ratio of 1:1 have a spherical shape and smooth surfaces. A statistically significant increase in the encapsulation efficiency (82.52% ± 3.28% was achieved when 1% (w/v polyvinyl alcohol (PVA and 2.5% (w/v trehalose were incorporated in the internal and external aqueous phase, respectively, during emulsification. Double-walled microspheres prepared together with excipients (PVA and trehalose showed a better control release of lysozyme. The released lysozyme was fully bioactive, and its structural integrity was slightly affected during microspheres fabrication and in vitro release studies. Therefore, double-walled microspheres made of Glu-PLGA and PLGA together with excipients (PVA and trehalose provide a controlled and sustained release for lysozyme.

  17. Ammonia and carbon dioxide emissions by stabilized conventional nitrogen fertilizers and controlled release in corn crop

    Directory of Open Access Journals (Sweden)

    Taylor Lima de Souza

    Full Text Available ABSTRACT The market of stabilized, slow and controlled release nitrogen (N fertilizers represents 1% of the world fertilizer consumption. On the other hand, the increase in availability, innovation and application of these technologies could lead to the improvement of N use efficiency in agroecossystems and to the reduction of environmental impacts. The objective of this study was to quantify agronomic efficiency relative index, ammonia volatilization, and CO2 emissions from conventional, stabilized and controlled release N fertilizers in corn summer crop. The experiment was carried out in a corn crop area located in Lavras, state of Minas Gerais, Brazil, without irrigation. All treatments were applied in topdressing at rate of 150 kg ha-1 N. N-NH3 losses from N fertilizers were: Granular urea (39% of the applied N = prilled urea (38% > urea coated with 16% S0 (32% = blend of urea + 7.9% S0 + polymers + conventional urea (32% > prilled urea incorporated at 0.02 m depth (24% > urea + 530 mg kg-1 of NBPT (8% = Hydrolyzed leather (9% > urea + thermoplastic resin (3% = ammonium sulfate (1% = ammonium nitrate (0.7%. Thermoplastic resin coated urea, ammonium nitrate and ammonium sulfate presented low values of cumulative CO2 emissions in corn crop. On the other hand, hydrolyzed leather promoted greater C-CO2 emission, when compared with other nitrogen fertilizers.

  18. Bionanocomposite systems based on montmorillonite and biopolymers for the controlled release of olanzapine.

    Science.gov (United States)

    Oliveira, Artur S; Alcântara, Ana C S; Pergher, Sibele B C

    2017-06-01

    Olanzapine (OLZ) is a drug that is used in the treatment of schizophrenia and other psychoses, and it belongs to the thienobenzodiazepine class. The OLZ molecule has low solubility decreasing bioavailability, but has high permeability in membrane biological being classified as a Class II drug substance according to the Biopharmaceutics Classification System. It was reported many side effects of administering OLZ orally. So, in order to increase the bioavailability of drug and possibly reducing some of side effects, this paper proposes a new material able to controllably release the drug in the body. To control the dissolution rate, this work proposes a system that incorporates the drug into montmorillonite (MMT) dispersed in a mixture of alginate (ALG) and xanthan gum (XG) biopolymers. The proposed hybrids and bionanocomposites were characterized by several physicochemical techniques, including XRD, IR-ATR, TG DTA, SEM-EDS and HPLC. The characterization data confirmed the intercalation of the OLZ into the MMT by the ion exchange process, as well as the interaction of the MMT-OLZ with the biopolymers. The release test, conducted under various pH conditions, showed that the proposed system exhibited a more controlled drug release than commercial tablets, indicating that the ALG-XG/MMT-OLZ bionanocomposite can act as a controlled release system for OLZ. Copyright © 2017 Elsevier B.V. All rights reserved.

  19. Nutrients Release from a Novel Gel-Based Slow/Controlled Release Fertilizer

    Directory of Open Access Journals (Sweden)

    H. Ding

    2016-01-01

    Full Text Available A novel gel-based slow/controlled release fertilizer (G-CRF was developed, which was produced by combining various natural, seminatural, and/or synthetic organic macromolecule materials and natural inorganic mineral with conventional NPK fertilizers. Its nutrient release characteristics were studied to compare with conventional fertilizers through the soil column leaching method. The influences of soil factors, including temperature, pH, water, and nutrient contents in the G-CRF on nutrient release, were also investigated through soil-water incubation method. These results indicated that the G-CRF had better effect on controlling release of N, P, and K nutrients, and the effect was more efficient when soil-water content was lower than 45% (w/w, temperature was below 35°C, and soil pH was in the range from weak acid to neutral. In addition, considering the effect of controlling nutrient release and cost of the materials in the G-CRF, it is recommended that the most feasible NPK nutrient contents in the G-CRF ranged from 30 to 35%.

  20. Review on materials & methods to produce controlled release coated urea fertilizer.

    Science.gov (United States)

    Azeem, Babar; KuShaari, KuZilati; Man, Zakaria B; Basit, Abdul; Thanh, Trinh H

    2014-05-10

    With the exponential growth of the global population, the agricultural sector is bound to use ever larger quantities of fertilizers to augment the food supply, which consequently increases food production costs. Urea, when applied to crops is vulnerable to losses from volatilization and leaching. Current methods also reduce nitrogen use efficiency (NUE) by plants which limits crop yields and, moreover, contributes towards environmental pollution in terms of hazardous gaseous emissions and water eutrophication. An approach that offsets this pollution while also enhancing NUE is the use of controlled release urea (CRU) for which several methods and materials have been reported. The physical intromission of urea granules in an appropriate coating material is one such technique that produces controlled release coated urea (CRCU). The development of CRCU is a green technology that not only reduces nitrogen loss caused by volatilization and leaching, but also alters the kinetics of nitrogen release, which, in turn, provides nutrients to plants at a pace that is more compatible with their metabolic needs. This review covers the research quantum regarding the physical coating of original urea granules. Special emphasis is placed on the latest coating methods as well as release experiments and mechanisms with an integrated critical analyses followed by suggestions for future research. Copyright © 2014 Elsevier B.V. All rights reserved.

  1. A review of mathematical modeling and simulation of controlled-release fertilizers.

    Science.gov (United States)

    Irfan, Sayed Ameenuddin; Razali, Radzuan; KuShaari, KuZilati; Mansor, Nurlidia; Azeem, Babar; Ford Versypt, Ashlee N

    2018-02-10

    Nutrients released into soils from uncoated fertilizer granules are lost continuously due to volatilization, leaching, denitrification, and surface run-off. These issues have caused economic loss due to low nutrient absorption efficiency and environmental pollution due to hazardous emissions and water eutrophication. Controlled-release fertilizers (CRFs) can change the release kinetics of the fertilizer nutrients through an abatement strategy to offset these issues by providing the fertilizer content in synchrony with the metabolic needs of the plants. Parametric analysis of release characteristics of CRFs is of paramount importance for the design and development of new CRFs. However, the experimental approaches are not only time consuming, but they are also cumbersome and expensive. Scientists have introduced mathematical modeling techniques to predict the release of nutrients from the CRFs to elucidate fundamental understanding of the dynamics of the release processes and to design new CRFs in a shorter time and with relatively lower cost. This paper reviews and critically analyzes the latest developments in the mathematical modeling and simulation techniques that have been reported for the characteristics and mechanisms of nutrient release from CRFs. The scope of this review includes the modeling and simulations techniques used for coated, controlled-release fertilizers. Copyright © 2017 Elsevier B.V. All rights reserved.

  2. Enhanced legumain-recognition and NIR controlled released of cisplatin-indocyanine nanosphere against gastric carcinoma.

    Science.gov (United States)

    Shi, Tianyi; Gu, Lianshuai; Sun, Yu; Wang, Senlin; You, Chaoqun; Zhang, Xiangyang; Zhu, Jin; Sun, Baiwang

    2017-01-05

    Cisplatin-therapy has faced limitations in the gastric cancer therapy. To settle the bottleneck, enhanced specificity and controlled-release property are choosen. We synthesize cisplatin and indocyanine green (ICG) loaded PLGA-(DSPE-PEG2000) nanoparticles, which is abbreviated as CINPs. And we conjugate the Gly-Cys-Gly-Ala-Ala-Asn-Leu (GCGAANL) heptapeptide upon the surface of CINPs, the product is abbreviated as ACINPs. ACINPs with nearly 110nm exhibit good monodispersity and size stability. The EE (efficiency of encapsulation) and LE (loading of encapsulation) of cisplatin loaded into ACINPs are optimized as 29.81% and 3.88%. MGC803 cells overexpressing the legumain and MKN28 cells, which negatively express the legumain as well as the normal stomach cells, are selected. In vitro studies have suggested ACINPs, compared with CINPs, could be recognized by MGC803 cells and efficiently killed the cancer cells, while be harmless to MKN28 cells, which indicates the specificity and safety of ACINPs. Under irradiation of 808nm NIR irradiation, ICG loaded in ACINPs could rapidly transform the light to heat up to 60℃. Nanoparticles compared with non-irraditaion group could be quickly disrupted and release the cisplatin which could enhance the controlled-release ability. Hence, the ACINPs exhibit great potential in avoiding the side effects and enhancing the therapy ability of cisplatin. Copyright © 2016 Elsevier B.V. All rights reserved.

  3. Design of a gastroretentive mucoadhesive dosage form of furosemide for controlled release

    Directory of Open Access Journals (Sweden)

    Sharad S. Darandale

    2012-10-01

    Full Text Available The aim of the present study was to develop and characterize a gastroretentive dosage form suitable for controlled drug release. It consists of a drug loaded polymeric film made up of a bilayer of immediate (IR and controlled release (CR layers folded into a hard gelatin capsule. Gastroretention results from unfolding and swelling of the film and its bioadhesion to the gastric mucosa. Furosemide, a drug with a narrow absorption window, was selected as the model drug. Inclusion of hydroxypropyl β-cyclodextrin in both layers and Carbopol® 971P NF in the CR layer of the bilayer film resulted in optimum drug release, bioadhesion and mechanical properties. The film with zig-zag folding in the capsule was shown to unfold and swell under acidic conditions and provide IR of drug over 1 h and CR for up to 12 h in acidic medium. X-ray diffraction, differential scanning calorimetry and scanning electron microscopy revealed uniform dispersion of furosemide in the polymeric matrices. The results indicate the dosage form is gastroretentive and can provide controlled release of drugs with narrow therapeutic windows.

  4. Development of controlled-release cisplatin dry powders for inhalation against lung cancers.

    Science.gov (United States)

    Levet, Vincent; Rosière, Rémi; Merlos, Romain; Fusaro, Luca; Berger, Gilles; Amighi, Karim; Wauthoz, Nathalie

    2016-12-30

    The present study focuses on the development of dry powders for inhalation as adjuvant chemotherapy in lung cancer treatment. Cisplatin was chosen as a potential candidate for a local treatment as it remains the main platinum component used in conventional chemotherapies, despite its high and cumulative systemic toxicities. Bulk cisplatin was reduced to submicron sizes using high-pressure homogenization, mixed with a solubilized lipid and/or PEGylated component and then spray-dried to produce controlled-release dry powder formulations. The obtained formulations were characterized for their physicochemical properties (particle size and morphology), aerodynamic performance and release profiles. Cisplatin content and integrity were assessed by electrothermal atomic absorption spectrometry and (195)Pt nuclear magnetic resonance spectroscopy. DPI formulations with cisplatin contents ranging from 48.5 to 101.0% w/w exhibited high fine particle fractions ranging from 37.3% to 51.5% of the nominal dose. Formulations containing cisplatin microcrystals dispersed in solid lipid microparticles based on acceptable triglycerides for inhalation and PEGylated excipients showed a controlled-release for more than 24h and a limited burst effect. These new formulations could provide an interesting approach to increasing and prolonging drug exposure in the lung while minimizing systemic toxicities. Copyright © 2016 Elsevier B.V. All rights reserved.

  5. Oral controlled release formulation of diclofenac sodium by microencapsulation with ethyl cellulose.

    Science.gov (United States)

    Sajeev, C; Vinay, G; Archna, R; Saha, R N

    2002-01-01

    The aim of this study was to formulate and evaluate microencapsulated controlled release preparations of diclofenac sodium (DFS) using different proportions of ethyl cellulose (EC) as the retardant material to extend the release. The formulated microcapsules were then compressed into tablets to obtain controlled release oral formulations. Phase separation-coacervation technique was employed to prepare microcapsules of DFS using different proportions of EC in cyclohexane. Physical characteristics of microcapsules and their tablets, in vitro release pattern of the designed microcapsules and their tablets prepared from them were studied using USP dissolution apparatus (USP 2000) type 2 (paddle method) in triple distilled water. The prepared microcapsules were white, free flowing and spherical in shape, with the particle size varying from 49.94-52.72 microm. The duration of DFS release from microcapsules was found to be directly proportional to the proportion of EC and, thus, coat thickness. All tablets were of good quality with respect to appearance, drug content uniformity, hardness, weight variation, friability and thickness uniformity. In vitro release study of the tabletted microcapsules in triple distilled water showed a zero order release kinetics and extended release beyond 24 h. A good correlation was obtained between drug release (t(60)) and proportion of EC in the microcapsules. In the case of tabletted microcapsules, very good correlation could be established between t(60), proportion of EC, weight of the tablets and between release rate constant (K) and proportion of EC. All the formulations were highly stable and possessed reproducible release kinetics across the batches.

  6. Massive Subcutaneous Emphysema in Robotic Sacrocolpopexy

    Science.gov (United States)

    Celik, Hatice; Cremins, Angela; Jones, Keisha A.

    2013-01-01

    The advent of robotic surgery has increased the popularity of laparoscopic sacrocolpopexy. Carbon dioxide insufflation, an essential component of laparoscopy, may rarely cause massive subcutaneous emphysema, which may be coincident with life-threatening situations such as hypercarbia, pneumothorax, and pneumomediastinum. Although the literature contains several reports of massive subcutaneous emphysema after a variety of laparoscopic procedures, we were not able to identify any report of this complication associated with laparoscopic or robotic sacrocolpopexy. Massive subcutaneous emphysema occurred in 3 women after robotic sacrocolpopexy in our practice. The patients had remarkable but reversible physical deformities lasting up to 1 week. A valveless endoscopic dynamic pressure system was used in all 3 of our cases. Our objective is to define the risk of massive subcutaneous emphysema during robotic sacrocolpopexy in light of these cases and discuss probable predisposing factors including the use of valveless endoscopic dynamic pressure trocars. PMID:23925018

  7. Effects of Controlled-Release Urea on Grain Yield of Spring Maize, Nitrogen Use Efficiency and Nitrogen Balance

    OpenAIRE

    JI Jing-hong; LI Yu-ying; LIU Shuang-quan; TONG Yu-xin; REN Gui-lin; LI Jie; LIU Ying; ZHANG Ming-yi

    2017-01-01

    The effects of mixing controlled-released urea (CRU) (release period of resin coated urea is 90 days) and urea (U) on maize yield, nitrogen use efficiency and nitrogen balance were studied by 4 plot experiments (site:Shuangcheng, Binxian, Harbin and Zhaoyuan) in two years (from year 2011 to 2012) to clarify the effect of controlled release urea on spring maize and soil nitrogen balance. Results were as follow:Spring maize yield and nitrogen absorption were increased with the increasing nitrog...

  8. Recurrent, giant subcutaneous leiomyosarcoma of the thigh

    Directory of Open Access Journals (Sweden)

    Gao Chuanping, MD

    2015-10-01

    Full Text Available We present a case of recurrent, massive subcutaneous leiomyosarcoma involving the left thigh in a 29-year-old male from Madagascar. The patient had earlier undergone local resection of subcutaneous leiomyosarcoma a half year before. After surgical intervention, local recurrence developed at this site and was rapidly growing. The patient was surgically treated with a 2-cm-wide margin local excision in our hospital. The patient has remained recurrence free at 1-year follow-up.

  9. Poly(Propylene Imine Dendrimers and Amoxicillin as Dual-Action Antibacterial Agents

    Directory of Open Access Journals (Sweden)

    Natalia Wrońska

    2015-10-01

    Full Text Available Besides acting as antimicrobial compounds, dendrimers can be considered as agents that improve the therapeutic effectiveness of existing antibiotics. In this work we present a new approach to using amoxicillin (AMX against reference strains of common Gram-negative pathogens, alone and in combination with poly(propylene imine (PPI dendrimers, or derivatives thereof, in which 100% of the available hydrogen atoms are substituted with maltose (PPI 100%malG3. The concentrations of dendrimers used remained in the range non-toxic to eukaryotic cells. The results indicate that PPI dendrimers significantly enhance the antibacterial effect of amoxicillin alone, allowing antibiotic doses to be reduced. It is important to reduce doses of amoxicillin because its widespread use in medicine could lead to the development of bacterial resistance and environmental pollution. This is the first report on the combined antibacterial activity of PPI surface-modified maltose dendrimers and amoxicillin.

  10. Amoxicillin loaded chitosan-alginate polyelectrolyte complex nanoparticles as mucopenetrating delivery system for h. Pylori

    National Research Council Canada - National Science Library

    Arora, Saahil; Gupta, Sankalp; Narang, Raj K; Budhiraja, Ramji D

    2011-01-01

    ...) nanoparticles of amoxicillin have been designed and optimized for various variables such as pH and mixing ratio of polymers, concentrations of polymers, drug and surfactant, using 3(3) Box-Behnken design...

  11. Novel fluorene-based supramolecular sensor for selective detection of amoxicillin in water and blood.

    Science.gov (United States)

    Shah, Kiramat; Hassan, Erum; Ahmed, Farid; Anis, Itrat; Rabnawaz, Muhammad; Shah, Muhammad Raza

    2017-07-01

    Synthesis, characterization and molecular recognition properties of fluorene based supramolecular cleft 1 is reported. The cleft molecule 1 was prepared in a single-step with good yield (85% yield), by linking Fluorene with 1-ethyl piperazine. The cleft molecule 1 was carefully characterized using various spectroscopic techniques such as NMR and mass spectrometry. The supramolecular interaction of cleft 1 with amoxicillin, 6APA, aspirin, captopril, cefotaxime, ceftriaxone, cefuroxime, diclofenac, penicillin, and cephradine was evaluated by fluorescent spectroscopy. The molecular recognition studies showed that amoxicillin selectively binds with cleft 1 in the presence of other drugs. The analytical method developed for the supramolecular interaction of molecular cleft 1 and amoxicillin was validated at varying pH, concentration and temperature during recognition process. Job's plots indicated that the stochiometry of the interactions between the cleft 1 and the amoxicillin was 1:1. Copyright © 2017. Published by Elsevier Inc.

  12. Poly(Propylene Imine) Dendrimers and Amoxicillin as Dual-Action Antibacterial Agents.

    Science.gov (United States)

    Wrońska, Natalia; Felczak, Aleksandra; Zawadzka, Katarzyna; Poszepczyńska, Martyna; Różalska, Sylwia; Bryszewska, Maria; Appelhans, Dietmar; Lisowska, Katarzyna

    2015-10-23

    Besides acting as antimicrobial compounds, dendrimers can be considered as agents that improve the therapeutic effectiveness of existing antibiotics. In this work we present a new approach to using amoxicillin (AMX) against reference strains of common Gram-negative pathogens, alone and in combination with poly(propylene imine) (PPI) dendrimers, or derivatives thereof, in which 100% of the available hydrogen atoms are substituted with maltose (PPI 100%malG3). The concentrations of dendrimers used remained in the range non-toxic to eukaryotic cells. The results indicate that PPI dendrimers significantly enhance the antibacterial effect of amoxicillin alone, allowing antibiotic doses to be reduced. It is important to reduce doses of amoxicillin because its widespread use in medicine could lead to the development of bacterial resistance and environmental pollution. This is the first report on the combined antibacterial activity of PPI surface-modified maltose dendrimers and amoxicillin.

  13. Frontal subcutaneous blood flow, and epi- and subcutaneous temperatures during scalp cooling in normal man

    DEFF Research Database (Denmark)

    Bülow, J; Friberg, L; Gaardsting, O

    1985-01-01

    Cooling of the scalp has been found to prevent hair loss following cytostatic treatment, but in order to obtain the hair preserving effect the subcutaneous temperature has to be reduced below 22 degrees C. In order to establish the relationship between epicutaneous and subcutaneous temperatures...... epicutaneous and subcutaneous temperatures could be demonstrated with the regression equation: s = 0.9 c + 4.9 (r = 0.99). In eight of the 10 subjects the subcutaneous temperature could be reduced below 22 degrees C with the applied technique. It is concluded that the hair preserving effect of scalp cooling...

  14. Amoxicillin allergy in children: five-day drug provocation test in the diagnosis of nonimmediate reactions.

    Science.gov (United States)

    Mori, Francesca; Cianferoni, Antonella; Barni, Simona; Pucci, Neri; Rossi, Maria Elisabetta; Novembre, Elio

    2015-01-01

    The drug provocation test (DPT) is the gold standard to rule out drug hypersensitivity. There are standardized DPT protocols to diagnose immediate reactions to drugs, but not for nonimmediate reactions. The aim of this study was to show the sensitivity and specificity of an allergy work-up that included a 5-day DPT in children with histories of nonimmediate reactions to amoxicillin through focusing on a pediatric population with histories of immediate and nonimmediate reactions to amoxicillin. Two hundred consecutive patients with histories of amoxicillin reactions referred to the Allergy Unit of Anna Meyer Children's Hospital for suspected drug allergy from 2008 to 2011 underwent in vivo tests with the culprit drug according to European Academy of Allergy and Clinical Immunology guidelines. Moreover, most of those children, regardless of the skin tests results, were challenged with amoxicillin for a total of 5 days. In 4 years, 200 patients were evaluated for a history of drug hypersensitivity to amoxicillin. The majority of patients (76%) had a history of mild nonimmediate reactions. All 200 patients underwent skin tests, and 9 of 200 tested positive. A total of 177 DPTs were performed with amoxicillin for 5 days in each child. Diagnosis of amoxicillin allergy was confirmed by a DPT in 17 patients (9.6%); 14/17 had history of nonimmediate reactions; 4/14 (26.6%) reacted on day 5. According to our results, a long-term DPT protocol increases the sensitivity of the allergy work-up, and it should be recommended for patients with a history of amoxicillin nonimmediate reaction. Copyright © 2015 American Academy of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  15. Prenatal effects by exposing to amoxicillin on dental enamel in Wistar rats

    Science.gov (United States)

    Gottberg, Beatriz; Berné, Jeanily; Quiñónez, Belkis

    2014-01-01

    Amoxicillin is an antibiotic widely prescribed; its most frequent side effects are gastrointestinal disorders and hypersensitivity reactions. Over the last 10 years studies have been published which suggest that amoxicillin may cause dental alterations similar to dental fluorosis. Never the less, the results are not conclusive, this is why it was planned the need to make controlled studies on test animals. Objectives: The purpose of this study was to determine the effect produced by amoxicillin prenatal administration on dental enamel in Wistar rats. Study Design: 12 pregnant adult rats were used distributed into five different groups: witness control (n=2) didn’t get any treatment; negative control (n=2) they were prescribed with saline solution; positive control (n=3) they were prescribed with tetracycline 130 mg/kg, and two groups (n=3 and n=2) treated with amoxicillin doses of 50 and 100 mg/kg respectively. The treatments were daily administered by mouth, from the 6th gestation day to the end of gestation. Twenty five days after they were born, the offspring were sacrificed with a sodium pentobarbital overdose, the mandible was dissected and the first lower molars were gotten. The samples were fixed in 10% formaldehyde solution and clinically and histologically observed to determine any enamel disorders. Results: hypomineralization was observed in every single sample of the tetracyclic and amoxicillin treated group 100 mg/kg, meanwhile only 50% from the group administered with 50 mg/kg amoxicillin showed this histological disorder. Conclusions: the side effect caused by amoxicillin on dental enamel was doses dependent. Key words:Amoxicillin, dental enamel, hypomineralization, Wistar rats. PMID:24121904

  16. Comparative pharmacokinetics of amoxicillin/clavulanic acid combination after intravenous administration to sheep and goats.

    Science.gov (United States)

    Carceles, C M; Escudero, E; Baggot, J D

    1995-04-01

    The pharmacokinetic behaviour of an amoxicillin/clavulanic acid combination was studied after intravenous administration of single doses (20 mg/kg per kg body weight) to five sheep and six goats. The objective was to determine whether there are differences between sheep and goats in the disposition of amoxicillin and clavulanic acid. The plasma concentration-time data were analysed by compartmental pharmacokinetic and non-compartmental methods. The disposition curves for both drugs were best described by a biexponential equation (two-compartment open model) in sheep and goats. The elimination half-lives of amoxicillin were 1.43 +/- 0.16 h in sheep and 1.13 +/- 0.19 h in goats, and of clavulanic acid were 1.16 +/- 0.01 h and 0.85 +/- 0.09 h in sheep and goats respectively. The apparent volumes of distribution of amoxicillin and clavulanic acid were similar in the two species. Body clearances of amoxicillin were 0.09 +/- 0.01 L/h kg in sheep and 0.11 +/- 0.01 L/h kg in goats, and of clavulanic acid were 0.07 +/- 0.01 L/h kg and 0.12 +/- 0.01 L/h kg in sheep and goats respectively. The half-lives and body clearances of amoxicillin and clavulanic acid differed significantly between sheep and goats. It was concluded that the disposition of amoxicillin and clavulanic acid administered intravenously as an amoxicillin/clavulanic acid combination to sheep and goats differed between the two ruminant species. Even though the differences in disposition kinetics of both drugs were statistically significant, the same intravenous dosing rate of this antimicrobial combination can generally be used in sheep and goats.

  17. Transfer and distribution of amoxicillin in the rat gastric mucosa and gastric juice and the effects of rabeprazole

    Science.gov (United States)

    Zheng, Hai-lun; Hu, Yong-mei; Bao, Jun-jun; Xu, Jian-ming

    2010-01-01

    Aim: To investigate the distribution of amoxicillin in the gastric juice and gastric mucosa of rats and to investigate the effects of proton pump inhibitor rabeprazole on amoxicillin concentrations in various compartments. Methods: One hundred and sixty anesthetized rats were divided into five groups, and given intravenously different doses of amoxicillin or amoxicillin and rabeprazole. The pH value and volume of gastric juice was aspirated were measured and separated gastric mucosa was homogenized. The concentrations of amoxicillin in the plasma, gastric juice and gastric mucosa were measured by high performance liquid chromatography (HPLC). Results: The maximum concentrations of amoxicillin in gastric juice and gastric mucosa were significantly lower than those in plasma (Pamoxicillin in the plasma and did not alter gastric antibiotic clearance or the gastric transfer fraction of amoxicillin in gastric juice. However, rabeprazole did increase the amoxicillin concentration and pH value in gastric juice and reduced the volume of the gastric juice. Conclusion: Amoxicillin could penetrate the gastric mucosa and achieve therapeutic concentrations at the target site after transfer from the blood to the stomach. Rabeprazole increased the amoxicillin concentration in gastric juice by decreasing the gastric juice volume but did not affect its concentration in blood or gastric mucosa. PMID:20305682

  18. Incorporation of amoxicillin-loaded organic montmorillonite into poly(ester-urethane) urea nanofibers as a functional tissue engineering scaffold.

    Science.gov (United States)

    Yu, Kui; Zhu, Tonghe; Wu, Yu; Zhou, Xiangxiang; Yang, Xingxing; Wang, Juan; Fang, Jun; El-Hamshary, Hany; Al-Deyab, Salem S; Mo, Xiumei

    2017-03-01

    A dual drug-loaded system is a promising alternative for the sustained drug release system and skin tissue engineering. In this study, a natural sodium montmorillonite (Na-MMT) modified by cetyl trimethyl ammonium bromide (CTAB) was prepared as a carrier to load a model drug - amoxicillin (AMX), the modified organic montmorillonite (CTAB-OMMT) loaded with AMX was marked as AMX@CTAB-OMMT and was subsequently incorporated into poly(ester-urethane) urea (PEUU) and gelatin hybrid nanofibers via electrospinning, resulting in a new drug-loaded nanofibrous scaffold (AMX@CTAB-OMMT-PU75). The scanning electron microscopy (SEM) result showed that the fiber morphology did not change after the embedding of AMX@CTAB-OMMT. Meanwhile, there was a significant increase of mechanical properties for PEUU/Gelatin hybrid nanofibers (PU75) after the incorporation of AMX@CTAB-OMMT and CTAB-OMMT. Importantly, AMX@CTAB-OMMT-PU75 nanofibers showed a kind of sustained drug release property which could be justified reasonably for the controlled release of AMX depending on the various application. The sustained release property could be identified roughly by the result of antibacterial test. The anaphylactic reaction test proved that there was no any anaphylactic reaction or inflammation on the back of rat for AMX@CTAB-OMMT-PU75 nanofibers. Consequently, the prepared drug-loaded AMX@CTAB-OMMT-PU75 nanofibrous scaffold is a promising candidate for application in the skin tissue engineering field and controlled drug release system. Copyright © 2016 Elsevier B.V. All rights reserved.

  19. Reformulation of controlled-release oxycodone and pharmacy dispensing patterns near the US–Canada border

    Science.gov (United States)

    Gomes, Tara; Paterson, J Michael; Juurlink, David N; Dhalla, Irfan A; Mamdani, Muhammad M

    2012-01-01

    Background In August 2010, a tamper-resistant formulation of controlled-release oxycodone (OxyContin-OP) was introduced in the United States but not in Canada. Our objective was to determine whether introduction of OxyContin-OP in the United States influenced prescription volumes for the original controlled-release oxycodone formulation (OxyContin) at Canadian pharmacies near the international border. Methods We conducted a population-based, serial, cross-sectional study of prescriptions dispensed from pharmacies in the 3 cities with the highest volume of US–Canada border crossings in Ontario: Niagara Falls, Windsor and Sarnia. We analyzed data on all outpatient prescriptions for OxyContin dispensed by Canadian pharmacies near each border crossing between 2010 Apr. 1 and 2012 Feb. 29. We calculated and compared monthly prescription rates, adjusted per 1000 population and stratified by tablet strength. Results The number of tablets dispensed near 4 border crossings in the 3 Canadian cities remained stable over the study period. However, the rate of dispensing at pharmacies near the Detroit–Windsor Tunnel increased roughly 4-fold between August 2010 and February 2011, from 505 to 1969 tablets per 1000 population. By April 2011, following warnings to prescribers and pharmacies regarding drug-seeking behaviour, the dispensing rate declined to 1683 tablets per 1000 population in this area. By November 2011, the rate had returned to levels observed in early 2010. Our analyses suggest that 242 075 excess OxyContin tablets were dispensed near the Detroit–Windsor Tunnel between August 2010 and October 2011. Conclusions Prescribing of the original formulation of controlled-release oxycodone rose substantially near a major international border crossing following the introduction of a tamper-resistant formulation in the United States. It is possible that the restriction of this finding to the area surrounding the Detroit–Windsor Tunnel reflects specific

  20. Reformulation of controlled-release oxycodone and pharmacy dispensing patterns near the US-Canada border.

    Science.gov (United States)

    Gomes, Tara; Paterson, J Michael; Juurlink, David N; Dhalla, Irfan A; Mamdani, Muhammad M

    2012-01-01

    In August 2010, a tamper-resistant formulation of controlled-release oxycodone (OxyContin-OP) was introduced in the United States but not in Canada. Our objective was to determine whether introduction of OxyContin-OP in the United States influenced prescription volumes for the original controlled-release oxycodone formulation (OxyContin) at Canadian pharmacies near the international border. We conducted a population-based, serial, cross-sectional study of prescriptions dispensed from pharmacies in the 3 cities with the highest volume of US-Canada border crossings in Ontario: Niagara Falls, Windsor and Sarnia. We analyzed data on all outpatient prescriptions for OxyContin dispensed by Canadian pharmacies near each border crossing between 2010 Apr. 1 and 2012 Feb. 29. We calculated and compared monthly prescription rates, adjusted per 1000 population and stratified by tablet strength. The number of tablets dispensed near 4 border crossings in the 3 Canadian cities remained stable over the study period. However, the rate of dispensing at pharmacies near the Detroit-Windsor Tunnel increased roughly 4-fold between August 2010 and February 2011, from 505 to 1969 tablets per 1000 population. By April 2011, following warnings to prescribers and pharmacies regarding drug-seeking behaviour, the dispensing rate declined to 1683 tablets per 1000 population in this area. By November 2011, the rate had returned to levels observed in early 2010. Our analyses suggest that 242 075 excess OxyContin tablets were dispensed near the Detroit-Windsor Tunnel between August 2010 and October 2011. Prescribing of the original formulation of controlled-release oxycodone rose substantially near a major international border crossing following the introduction of a tamper-resistant formulation in the United States. It is possible that the restriction of this finding to the area surrounding the Detroit-Windsor Tunnel reflects specific characteristics of this border crossing, including its high

  1. Conductive polymers for controlled release and treatment of central nervous system injury

    Science.gov (United States)

    Saigal, Rajiv

    As one of the most devastating forms of neurotrauma, spinal cord injury remains a challenging clinical problem. The difficulties in treatment could potentially be resolved by better technologies for therapeutic delivery. In order to develop new approaches to treating central nervous system injury, this dissertation focused on using electrically-conductive polymers, controlled drug release, and stem cell transplantation. We first sought to enhance the therapeutic potential of neural stem cells by electrically increasing their production of neurotrophic factors (NTFs), important molecules for neuronal cell survival, differentiation, synaptic development, plasticity, and growth. We fabricated a new cell culture device for growing neural stem cells on a biocompatible, conductive polymer. Electrical stimulation via the polymer led to upregulation of NTF production by neural stem cells. This approach has the potential to enhance stem cell function while avoiding the pitfalls of genetic manipulation, possibly making stem cells more viable as a clinical therapy. Seeing the therapeutic potential of conductive polymers, we extended our studies to an in vivo model of spinal cord injury (SCI). Using a novel fabrication and extraction technique, a conductive polymer was fabricated to fit to the characteristic pathology that follows contusive SCI. Assessed via quantitative analysis of MR images, the conductive polymer significantly reduced compression of the injured spinal cord. Further characterizing astroglial and neuronal response of injured host tissue, we found significant neuronal sparing as a result of this treatment. The in vivo studies also demonstrated improved locomotor recovery mediated by a conductive polymer scaffold over a non-conductive control. We next sought to take advantage of conductive polymers for local, electronically-controlled release of drugs. Seeking to overcome reported limitations in drug delivery via polypyrrole, we first embedded drugs in poly

  2. Contribution of Specific Amino Acid Changes in Penicillin Binding Protein 1 to Amoxicillin Resistance in Clinical Helicobacter pylori isolates ▿

    Science.gov (United States)

    Qureshi, Nadia N.; Morikis, Dimitrios; Schiller, Neal L.

    2011-01-01

    Amoxicillin is commonly used to treat Helicobacter pylori, a major cause of peptic ulcers, stomach cancer, and B-cell mucosa-associated lymphoid tissue lymphoma. Amoxicillin resistance in H. pylori is increasing steadily, especially in developing countries, leading to treatment failures. In this study, we characterize the mechanism of amoxicillin resistance in the U.S. clinical isolate B258. Transformation of amoxicillin-susceptible strain 26695 with the penicillin binding protein 1 gene (pbp1) from B258 increased the amoxicillin resistance of 26695 to equal that of B258, while studies using biotinylated amoxicillin showed a decrease in the binding of amoxicillin to the PBP1 of B258. Transformation with 4 pbp1 fragments, each encompassing several amino acid substitutions, combined with site-directed mutagenesis studies, identified 3 amino acid substitutions in PBP1 of B258 which affected amoxicillin susceptibility (Val 469 Met, Phe 473 Leu, and Ser 543 Arg). Homology modeling showed the spatial orientation of these specific amino acid changes in PBP1 from 26695 and B258. The results of these studies demonstrate that amoxicillin resistance in the clinical U.S. isolate B258 is due solely to an altered PBP1 protein with a lower binding affinity for amoxicillin. Homology modeling analyses using previously identified amino acid substitutions of amoxicillin-resistant PBP1s demonstrate the importance of specific amino acid substitutions in PBP1 that affect the binding of amoxicillin in the putative binding cleft, defining those substitutions deemed most important in amoxicillin resistance. PMID:20956585

  3. Common harms from amoxicillin: a systematic review and meta-analysis of randomized placebo-controlled trials for any indication.

    Science.gov (United States)

    Gillies, Malcolm; Ranakusuma, Anggi; Hoffmann, Tammy; Thorning, Sarah; McGuire, Treasure; Glasziou, Paul; Del Mar, Christopher

    2015-01-06

    When prescribing antibiotics for common indications, clinicians need information about both harms and benefits, information that is currently available only from observational studies. We quantified the common harms of the most frequently prescribed antibiotic, amoxicillin, from randomized placebo-controlled trials. For this systematic review, we searched MEDLINE, Embase and the Cochrane Central Register of Controlled Trials, without language restriction, for any randomized, participant-blinded, placebo-controlled trials of amoxicillin or amoxicillin-clavulanic acid for any indication, in any setting. Our main outcome was any reported adverse event. Of 730 studies identified, we included 45 trials: 27 involving amoxicillin, 17 involving amoxicillin-clavulanic acid and 1 involving both. The indications for antibiotic therapy were variable. The risk of bias was low, although only 25 trials provided data suitable for assessment of harms, which suggested under-reporting. Diarrhea was attributed to amoxicillin only in the form of amoxicillin-clavulanic acid (Peto odds ratio [OR] 3.30, 95% confidence interval [CI] 2.23-4.87). The OR for candidiasis (3 trials) was significantly higher (OR 7.77, 95% CI 2.23-27.11). Rashes, nausea, itching, vomiting and abnormal results on liver function tests were not significantly increased. The results were not altered by sensitivity analyses, nor did funnel plots suggest publication bias. The number of courses of antibiotics needed to harm was 10 (95% CI 6-17) for diarrhea with amoxicillin-clavulanic acid and 27 (95% CI 24-42) for candidiasis with amoxicillin (with or without clavulanic acid). Diarrhea was caused by use of amoxicillin-clavulanic acid, and candidiasis was caused by both amoxicillin and amoxicillin-clavulanic acid. Harms were poorly reported in most trials, and their true incidence may have been higher than reported. Nevertheless, these rates of common harms associated with amoxicillin therapy may inform decisions by

  4. Pharmacokinetics and oral bioavailability of amoxicillin in chicken infected with caecal coccidiosis.

    Science.gov (United States)

    Kandeel, M

    2015-10-01

    Chicken infected with caecal coccidiosis (Eimeria tenella) was used to evaluate the effect of coccidiosis on the pharmacokinetic and bioavailability of amoxicillin. The level of amoxicillin was estimated by high-performance chromatography (HPLC) to calculate the pharmacokinetic parameters and oral bioavailability. For i.v. injection of amoxicillin, Vd and CL were 0.29 and 0.27 (mg/kg)/(μg/mL)/h, respectively. Compared with healthy chicken, intravenous injection of amoxicillin in the infected chicken showed higher distribution and elimination constants, delayed clearance and statistically significant higher AUC and MRT. Oral administration in healthy chicken was accompanied by rapid absorption and high bioavailability with Tmax , Cmax and F about 1.03 h, 3.26 μg/mL and 40.2, respectively. Furthermore, oral administration in the infected chicken produced higher mean absorption time, delayed Tmax, lower Cmax, smaller AUC value and lower bioavailability (16.76). Based on these results, monitoring and adjustment of amoxicillin dosing could be practiced during the presence of coccidiosis. The measured Cmax values suggest the administration of 1.3-folds of the normal dose to maintain the normal maximal serum concentrations of amoxicillin in chicken infected with caecal coccidiosis. © 2015 John Wiley & Sons Ltd.

  5. Comparing performance of amoxicillin and intramuscular benzathine penicillin in relieving manifestations of streptococcal pharyngitis in children.

    Science.gov (United States)

    Eslami, S T; Nassirian, A; Nassirian, H; Hatami, E; Sobhani, E; Najibpour, R

    2014-12-01

    To compare clinical and bacteriologic responses to intramuscular benzathine penicillin G (BPG) and single dose of amoxicillin in Group A streptococcal (GAS) pharyngitis. This study included 571 children from 6 to 15 years old age, with pharyngitis, who were admitted to 45 elementary and guidance schools from 7 regions of Education Organization in North-East of Iran, Mashhad. They were screened for enrollment and if he/she presented pharyngitis with clinical criteria of sore throat, erythema, exudate and tender or enlarged anterior cervical lymph nodes. Exclusion criteria included reports of antibiotic use, negative throat culture for GAS and history of allergy to the drugs. Clinical and bacteriologic responses to BPG and once daily orally amoxicillin were considered and compared. In the amoxicillin group, treatment failure was more than the penicillin group (18.9% vs. 6.4%, respectively) but the difference was not statistically significant (p amoxicillin. Our study was in line with studies comparing the two drugs. The results show that once-daily therapy with amoxicillin is as effective as intramuscular benzathine penicillin G for the treatment of GAS pharyngitis, but penicillin was significantly more effective in reducing exudate and concurrent signs vs. amoxicillin.

  6. Amoxicillin Use during Early Childhood and Fluorosis of Later Developing Tooth Zones

    Science.gov (United States)

    Levy, Steven M.; Warren, John J.; Broffitt, Barbara

    2015-01-01

    Objectives Amoxicillin use has been reported to be associated with developmental defects on enamel surfaces. This analysis assessed the association between amoxicillin use and fluorosis on late-erupting permanent teeth. Methods As part of the Iowa Fluoride Study, subjects were followed from birth to 32 months with questionnaires every 3-4 months to gather information on fluoride intake and amoxicillin use (n=357 subjects for this analysis). Permanent tooth fluorosis on late-erupting zones was assessed by three trained dentists using the Fluorosis Risk Index (FRI) at approximately age 13. A case was defined as fluorosis if a subject had at least two FRI classification II zone scores of 2 or 3. Chi-square tests and logistic regression were used and relative risks and odds ratios were calculated. Results There were 113 cases and 244 controls. In bivariate analyses, amoxicillin use from 20-24 months significantly increased the risk of fluorosis on FRI classification II zones (44.2% vs 30.4%, RR=1.45, 95% CI 1.05-2.04), but other individual time periods did not. Multivariable logistic regression confirmed the increased risk of fluorosis for amoxicillin use from 20-24 months (OR=2.92, 95% CI=1.34-6.40), after controlling for otitis media, breast-feeding, and fluoride intake. Conclusions Amoxicillin use during early childhood could be a risk factor in the etiology of fluorosis on late-erupting permanent tooth zones, but further research is needed. PMID:21972463

  7. Pharmacokinetics of amoxicillin/clavulanic acid combination after intravenous and oral administration in goats.

    Science.gov (United States)

    Carceles, C M; Escudero, E; Vicente, M S; Serrano, J M; Carli, S

    1995-12-01

    The intravenous and oral pharmacokinetics of an amoxicillin and clavulanic acid combination (20 mg/kg of sodium amoxicillin and 5 mg/kg of potassium clavulanate) were studied in six goats. After intravenous administration the pharmacokinetics of both drugs could be described by an open two-compartment model. Amoxicillin had a greater distribution volume (0.19 +/- 0.01 l/kg) than clavulanic acid (0.15 +/- 0.01 l/kg), whereas the distribution and elimination constants were higher for the latter, which was eliminated more quickly than amoxicillin. After oral administration of both drugs their pharmacokinetic behaviour was best described by an open one-compartment model with first-order absorption. Elimination half-lives were twice as long after oral (2.15 +/- 0.20 h and 1.94 +/- 0.16 h for amoxicillin and clavulanic acid respectively) than after intravenous administration (1.20 +/- 0.16 h and 0.86 +/- 0.09, respectively). An apparent 'flip-flop' situation was evident in this study. Bioavailability was 27% for amoxicillin and 50% for clavulanic acid.

  8. Development and application of a Controlled Release Facility (CRF) to validate flux quantifying methodologies.

    Science.gov (United States)

    Helmore, Jonathan

    2017-04-01

    The National Physical Laboratory, the UK's National Measurement Institute, has developed a novel facility capable of replicating the gaseous emission flux characteristics of a variety of real-word scenarios as may be found in small to medium scale industry and agriculture. The Controlled Release Facility (CRF) can be used to challenge conventional remote sensing techniques, as well as validate new Unmanned Aerial Vehicle (UAV) and distributed sensor network based methods, for source identification and flux calculation. The CRF method will be described and the results from three case studies will be discussed: The replication of an operational on-shore shale gas well using emissions of natural gas to atmosphere and measurements using Differential Absorption LIDAR (DIAL); the replication of fugitive volatile organic compounds emissions from a petrochemical unit and measurements using DIAL; and the replication of methane and carbon dioxide emissions from landfill and measurements using both fixed wing and multi-rotor UAVs.

  9. Effect of crosslinking agents on chitosan microspheres in controlled release of diclofenac sodium

    Directory of Open Access Journals (Sweden)

    Vanessa L. Gonçalves

    2005-03-01

    Full Text Available In this work chitosan microspheres were prepared by the simple coacervation method and crosslinked using epichlorhydrin or glutaraldehyde for the controlled release of diclofenac sodium. The effects of the crosslinking agents on chitosan microspheres over a 12-hour period were assessed with regard to swelling, hydrolysis, porosity, crosslinking, impregnation of diclofenac sodium (DS, and consequently to the release of DS in buffer solutions, simulating the gastrointestinal tract. The degree of swelling varied with the pH for glutaraldehyde chitosan microspheres (GCM and epichlorhydrin chitosan microspheres (ECM. Partial acid and basic hydrolysis affected the swelling behavior of the GCM matrix. Release kinetics of diclofenac sodium from these matrices were investigated at pH 1.2, 6.8 and 9.0, simulating the gastrointestinal tract conditions. The results indicated that the release mechanism deviated slightly from Fickian transport.

  10. Bovine serum albumin nanoparticles as controlled release carrier for local drug delivery to the inner ear

    Science.gov (United States)

    Yu, Zhan; Yu, Min; Zhang, Zhibao; Hong, Ge; Xiong, Qingqing

    2014-07-01

    Nanoparticles have attracted increasing attention for local drug delivery to the inner ear recently. Bovine serum albumin (BSA) nanoparticles were prepared by desolvation method followed by glutaraldehyde fixation or heat denaturation. The nanoparticles were spherical in shape with an average diameter of 492 nm. The heat-denatured nanoparticles had good cytocompatibility. The nanoparticles could adhere on and penetrate through the round window membrane of guinea pigs. The nanoparticles were analyzed as drug carriers to investigate the loading capacity and release behaviors. Rhodamine B was used as a model drug in this paper. Rhodamine B-loaded nanoparticles showed a controlled release profile and could be deposited on the osseous spiral lamina. We considered that the bovine serum albumin nanoparticles may have potential applications in the field of local drug delivery in the treatment of inner ear disorders.

  11. Sustained and controlled release of lipophilic drugs from a self-assembling amphiphilic peptide hydrogel

    DEFF Research Database (Denmark)

    Briuglia, Maria-Lucia; Urquhart, Andrew; Lamprou, Dimitrios A.

    2014-01-01

    Materials which undergo self-assembly to form supramolecular structures can provide alternative strategies to drug loading problems in controlled release application. RADA 16 is a simple and versatile self-assembling peptide with a designed structure formed of two distinct surfaces, one hydrophilic...... and one hydrophobic that are positioned in such a well-ordered fashion allowing precise assembly into a predetermined organization. A "smart" architecture in nanostructures can represent a good opportunity to use RADA16 as a carrier system for hydrophobic drugs solving problems of drugs delivery....... In this work, we have investigated the diffusion properties of Pindolol, Quinine and Timolol maleate from RADA16 in PBS and in BSS-PLUS at 37°C. A sustained, controlled, reproducible and efficient drug release has been detected for all the systems, which allows to understand the dependence of release kinetics...

  12. Controlled Release Kinetics in Hydroxy Double Salts: Effect of Host Anion Structure

    Directory of Open Access Journals (Sweden)

    Stephen Majoni

    2014-01-01

    Full Text Available Nanodimensional layered metal hydroxides such as layered double hydroxides (LDHs and hydroxy double salts (HDSs can undergo anion exchange reactions releasing intercalated anions. Because of this, these metal hydroxides have found applications in controlled release delivery of bioactive species such as drugs and pesticides. In this work, isomers of hydroxycinnamate were used as model compounds to systematically explore the effects of anion structure on the rate and extent of anion release in HDSs. Following intercalation and subsequent release of the isomers, it has been demonstrated that the nature and position of substituent groups on intercalated anions have profound effects on the rate and extent of release. The extent of release was correlated with the magnitude of dipole moments while the rate of reaction showed strong dependence on the extent of hydrogen bonding within the layers. The orthoisomer showed a more sustained and complete release as compared to the other isomers.

  13. Bioinspired Heparin Nanosponge Prepared by Photo-crosslinking for Controlled Release of Growth Factors

    DEFF Research Database (Denmark)

    Choi, Won Il; Sahu, Abhishek; Vilos, Cristian

    2017-01-01

    Growth factors have great therapeutic potential for various disease therapy and tissue engineering applications. However, their clinical efficacy is hampered by low bioavailability, rapid degradation in vivo and non-specific biodistribution. Nanoparticle based delivery systems are being evaluated...... factor binding ability. Four different growth factors, bFGF, VEGF, BMP-2, and HGF were successfully encapsulated into Hep-NS. In vitro studies showed sustained release of all the growth factors for almost 60 days and the rate of release was directly dependent on the amount of heparin in Hep......-NS. The released growth factors retained their bioactivity as assessed by a cell proliferation assay. This heparin nanosponge is therefore a promising nanocarrier for the loading and controlled release of growth factors....

  14. Photoresponsive Conjugated Microporous Polymer Films Fabricated by Electrochemical Deposition for Controlled Release.

    Science.gov (United States)

    Zhao, Ruiyang; Han, Jishu; Huang, Mei; Liu, Fusheng; Wang, Lei; Ma, Yuguang

    2017-09-01

    Stable controlled release system, conjugated microporous polymers (CMPs) with stimuli-responsive properties can be ideal structures because their 3D microporous matrix structure and possible stimulated response provide inherent switchable acceptor sites to capture and release guest molecules. Herein, the in situ electrochemical deposition of precursors (DTCzAzo) is utilized to construct highly crosslinked photoresponsive CMP films, which can reversibly undergo the trans-to-cis isomerization alternately with irradiation by 355 and 480 nm laser beams. The size of pores in CMP films changes tremendously during the process of trans-cis photoisomerization, to controllably capture, conserve, and release the guest molecules. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  15. pH-Sensitive Amphiphilic Block-Copolymers for Transport and Controlled Release of Oxygen

    KAUST Repository

    Patil, Yogesh Raghunath

    2017-05-31

    Saturated fluorocarbons, their derivatives and emulsions are capable of dissolving anomalously high amounts of oxygen and other gases. The mechanistic aspects of this remarkable effect remain to be explored experimentally. Here, the synthesis of a library of amphiphilic fluorous block-copolymers incorporating different fluorinated monomers is described, and the capacity of these copolymers for oxygen transport in water is systematically investigated. The structure of the fluorous monomer employed was found to have a profound effect on both the oxygen-carrying capacity and the gas release kinetics of the polymer emulsions. Furthermore, the release of O2 from the polymer dispersions could be triggered by changing the pH of the solution. This is the first example of a polymer-based system for controlled release of a non-polar, non-covalently entrapped respiratory gas.

  16. Residue and bio-efficacy evaluation of controlled release formulations of metribuzin against weeds in wheat.

    Science.gov (United States)

    Kumar, Jitendra; Nisar, Keyath; Shakil, N A; Sharma, Rajvir

    2010-09-01

    Controlled release formulations of metribuzin in polyvinyl chloride, (emulsion); carboxy methyl cellulose, CMC and carboxy methyl cellulose- kaolinite composite, CMC-KAO are reported. The MET-CMC-KAO-3 (T(9)) formulation provided a superior control (76.1%) of weeds in field grown wheat in comparison to metribuzin 75 DF (57.14%) at the dose (350 g a.i. ha(-1)) after 90 days of sowing. The treatment (T(9)) reduced the dry weight of the weed flora after 30 days of sowing (4.0 g m(-2)) and significantly superior over metribuzin 75 DF (6.0 g m(-2)) and control (17.72 g m(-2)). There were nil to negligible metribuzin residue in soil at harvest of wheat crop and were within prescribed limit of 10 mg L(-1) in drinking water (EPA).

  17. Subcutaneous Fat Necrosis of the Newborn: A Case Report

    Energy Technology Data Exchange (ETDEWEB)

    Yi, Kyung Sik; Cho, Bum Sang; Bae, Il Hun; Lee, Seung Young; Jeon, Min Hee; Lee, Ok Jun; Kim, Mi Jung [Chungbuk National University College of Medicine, Cheongju (Korea, Republic of)

    2007-09-15

    Subcutaneous fat necrosis in the newborn is an uncommon transient disorder of the subcutaneous adipose tissue that develops after birth. We describe the characteristic ultrasonography and CT findings of a case of pathologically confirmed subcutaneous fat necrosis located at the subcutaneous fat layer of the neck, back, and shoulders with a review of the literature

  18. MMC controlled-release membranes attenuate epidural scar formation in rat models after laminectomy.

    Science.gov (United States)

    Xie, Hao; Wang, Binbin; Shen, Xun; Qin, Jian; Jiang, Longhai; Yu, Chen; Geng, Dawei; Yuan, Tangbo; Wu, Tao; Cao, Xiaojian; Liu, Jun

    2017-06-01

    Epidural scar formation after laminectomy impede surgical outcomes of decompression. Mitomycin C (MMC) has been demonstrated to have significant inhibitory effects on epidural scar. This study was undertaken to develop an effective MMC controlled‑release membrane and to investigate its effects on epidural scar in rat models of laminectomy. A total of 72 rats that underwent laminectomy were divided into three groups. Among them, 24 were treated with mitomycin C‑polylactic acid (MMC-PLA) controlled‑release membrane, 24 with mitomycin C-polyethylene glycol (MMC-PEG) controlled-release membrane, and no treatment was performed for the remaining 24 rats (control group). In the following 4 weeks, magnetic resonance image (MRI), macroscopic observation, histology and hydroxyproline (Hyp) concentration analysis were performed to explore the effects of these three therapies on epidural scar. MRI revealed a significant reduction of epidural fibrosis in MMC-PLA and MMC-PEG treatment groups, compared with the control group. Histological results also showed that collagen deposition was significantly reduced after being treated with MMC-PLA or MMC-PEG membranes. Likewise, Hyp concentrations of the epidural scar tissue in MMC-PLA and MMC-PEG groups were markedly lower than those in the control group. However, regarding the effects on reducing epidural scar, no significant difference was found between the MMC-PLA and MMC-PEG groups. In conclusion, MMC-PLA and MMC-PEG membranes are safe and effective in reducing fibrosis. Thus, MMC-controlled-release membranes promises to be a potential therapeutic in preventing epidural scar formation after laminectomy.

  19. Investigation of excipient type and level on drug release from controlled release tablets containing HPMC.

    Science.gov (United States)

    Williams, Robert O; Reynolds, Thomas D; Cabelka, Tim D; Sykora, Matthew A; Mahaguna, Vorapann

    2002-05-01

    The purpose of this study was to investigate the influence of excipient type and level on the release of alprazolam formulated in controlled release matrix tablets containing hydroxypropyl methylcellulose (HPMC). Each tablet formulation contained alprazolam, HPMC (Methocel K4MP), excipients, and magnesium stearate. The soluble excipients investigated were lactose monohydrate, sucrose, and dextrose, and the insoluble excipients included dicalcium phosphate dihydrate, dicalcium phosphate anhydrous, and calcium sulfate dihydrate. The similarity factor (f2 factor) was used to compare the dissolution profile of each formulation. The insoluble excipients, especially dicalcium phosphate dihydrate, caused the drug to be released at a slower rate and to a lesser extent than the soluble excipients. Soluble excipients created a more permeable hydrated gel layer for drug release, increased the porosity resulting in faster diffusion of drug, and increased the rate of tablet erosion. Use of binary mixtures of lactose monohydrate and dicalcium phosphate dihydrate produced release profiles of intermediate duration. Rapid drug dissolution was obtained when only 9.1% w/w of lactose monohydrate was present in the tablet formulation. Only when the dicalcium phosphate dihydrate level was sufficiently high (36.5% w/w) was the release rate and extent decreased. It was demonstrated that the type and level of excipient influenced the rate and extent of drug release from controlled release tablets containing HPMC. The release mechanism of alprazolam from each tablet formulation was described by either the Hixson-Crowell cube root kinetics equation or Peppas's equation. However, the different excipient types investigated did not influence the release mechanism of alprazolam from the final tablets.

  20. Qualitative analysis of controlled release ciprofloxacin/carbopol 934 mucoadhesive suspension

    Science.gov (United States)

    Sahoo, Subhashree; Chakraborti, Chandra Kanti; Mishra, Subash Chandra

    2011-01-01

    Mucoadhesive polymeric (carbopol 934) suspension of ciprofloxacin was prepared by ultrasonication and optimized with the aim of developing an oral controlled release gastro-retentive dosage form. The qualitative analysis of the formulation was performed by fourier transform infrared spectroscopy (FTIR), Raman spectroscopy, X-ray powder diffraction (XRD), and scanning electron microscopy (SEM) analyses. FTIR (400 cm-1 to 4000 cm-1 region) and Raman (140 to 2400 cm-1 region) Spectroscopic studies were carried out and the spectra were used for interpretation. XRD data of pure drug, polymer and the formulation were obtained using a powder diffractometer scanned from a Bragg's angle (2θ) of 10° to 70°. The dispersion of the particle was observed using SEM techniques. The particle size distribution and aspect ratio of particles in the polymeric suspension were obtained from SEM image analysis. The results from FTIR and Raman spectroscopic analyses suggested that, in formulation, the carboxylic groups of ciprofloxacin and hydroxyl groups of C934 undergo a chemical interaction leading to esterification and hydrogen bonding. The XRD data suggested that the retention of crystalline nature of ciprofloxacin in the formulation would lead to increase in stability and drug loading; decrease in solubility; and delay in release of the drug from polymeric suspension with better bioavailability and penetration capacity. The SEM image analysis indicated that, in the formulation maximum particles were having aspect ratio from 2 to 4 and standard deviation was very less which provided supporting evidences for homogeneous, uniformly dispersed, stable controlled release ciprofloxacin suspension which would be pharmaceutically acceptable. PMID:22171318

  1. Silicone Doped Chitosan-Acrylamide Coencapsulated Urea Fertilizer: An Approach to Controlled Release Fertilizers

    Directory of Open Access Journals (Sweden)

    Sempeho Ibahati Siafu

    2017-01-01

    Full Text Available In the absence of special management practices, urea is known to undergo chemical transformations resulting in severe losses (≈60–70% of total fertilizer applied. In an attempt to design urea controlled release fertilizers in order to counterbalance the 60–70% loss, urea was cross-linked with chitosan and acrylamide under refluxed in situ copolymerization technique; the procedures were repeated with silicone doping prior cross-linking with MBA. The particles were characterized with FTIR/ATR, EDX, XRD, and SEM. The IR bands observed within 3426–409 cm−1 revealed the formation of new bands after coencapsulation for the νγN-H, νβN-H, νOH, νsNH2, νCH2, νC=O, δ′NH2, νC=C, δNH2, νC-N, βCH3, $C-N, γNH2, νC=O, and $CH2. Crystallinity indices for urea with and without silicone doping were found to be 50.9% and 72.1%, respectively, with a distinctive split peak at (d 12.30°. The formation of Microdunes and Microballs 3D network sized 0.64 μm was noted. Release profiles demonstrated that 80% N was released in a period of 30 days at RT and pH 7. The release patterns exhibited linear and deformed sigmoid release models. Empirically, the findings demonstrated that it is possible to design urea controlled release fertilizers with varying particle sizes and morphologies by using chitosan-acrylamide coencapsulation.

  2. Qualitative analysis of controlled release ciprofloxacin/carbopol 934 mucoadhesive suspension

    Directory of Open Access Journals (Sweden)

    Subhashree Sahoo

    2011-01-01

    Full Text Available Mucoadhesive polymeric (carbopol 934 suspension of ciprofloxacin was prepared by ultrasonication and optimized with the aim of developing an oral controlled release gastro-retentive dosage form. The qualitative analysis of the formulation was performed by fourier transform infrared spectroscopy (FTIR, Raman spectroscopy, X-ray powder diffraction (XRD, and scanning electron microscopy (SEM analyses. FTIR (400 cm-1 to 4000 cm-1 region and Raman (140 to 2400 cm-1 region Spectroscopic studies were carried out and the spectra were used for interpretation. XRD data of pure drug, polymer and the formulation were obtained using a powder diffractometer scanned from a Bragg′s angle (2q of 10° to 70°. The dispersion of the particle was observed using SEM techniques. The particle size distribution and aspect ratio of particles in the polymeric suspension were obtained from SEM image analysis. The results from FTIR and Raman spectroscopic analyses suggested that, in formulation, the carboxylic groups of ciprofloxacin and hydroxyl groups of C934 undergo a chemical interaction leading to esterification and hydrogen bonding. The XRD data suggested that the retention of crystalline nature of ciprofloxacin in the formulation would lead to increase in stability and drug loading; decrease in solubility; and delay in release of the drug from polymeric suspension with better bioavailability and penetration capacity. The SEM image analysis indicated that, in the formulation maximum particles were having aspect ratio from 2 to 4 and standard deviation was very less which provided supporting evidences for homogeneous, uniformly dispersed, stable controlled release ciprofloxacin suspension which would be pharmaceutically acceptable.

  3. Preparation and Physicochemical Evaluation of Controlled-release Carbon Source Tablet for Groundwater in situ Denitrification

    Science.gov (United States)

    Kim, Y.; Kang, J. H.; Yeum, Y.; Han, K. J.; Kim, D. W.; Park, C. W.

    2015-12-01

    Nitric nitrogen could be the one of typical pollution source such asNO3-through domestic sewage, livestock and agricultural wastewater. Resident microflorain aquifer has known to remove the nitric nitrogen spontaneously following the denitration process with the carbon source (CS) as reactant. However, it could be reacted very slowly with the rack of CS and there have been some studies for controlled addition of CS (Ref #1-3). The aim of this study was to prepare the controlled-release carbon source (CR-CS) tablet and to evaluate in vitro release profile for groundwater in situ denitrification. CR-CS tablet could be manufactured by direct compression method using hydraulic laboratory press (Caver® 3850) with 8 mm rounded concave punch/ die.Seven kinds of CR-CS tablet were prepared to determine the nature of the additives and their ratio such as sodium silicate, dicalcium phosphate, bentonite and sand#8.For each formulation, the LOD% and flowability of pre-mixed powders and the hardness of compressed tablets were analyzed. In vitro release study was performed to confirm the dissolution profiles following the USP Apparatus 2 method with Distilled water of 900mL, 20 °C. As a result, for each lubricated powders, they were compared in terms of ability to give an acceptable dry pre-mixed powder for tableting process. The hardness of the compressed tablets is acceptable whatever the formulations tested. After in vitro release study, it could confirm that the different formulations of CR-CS tablet have a various release rate patterns, which could release 100% at 3 hrs, 6 hrs and 12 hrs. The in vitro dissolution profiles were in good correlation of Higuchi release kinetic model. In conclusion, this study could be used as a background for development and evaluation of the controlled-release carbon source (CR-CS) tablet for the purification of groundwater following the in situ denitrification.

  4. Frontal subcutaneous blood flow, and epi- and subcutaneous temperatures during scalp cooling in normal man

    DEFF Research Database (Denmark)

    Bülow, J; Friberg, L; Gaardsting, O

    1985-01-01

    Cooling of the scalp has been found to prevent hair loss following cytostatic treatment, but in order to obtain the hair preserving effect the subcutaneous temperature has to be reduced below 22 degrees C. In order to establish the relationship between epicutaneous and subcutaneous temperatures d...

  5. Trends in controlled-release oxycodone (OxyContin) prescribing among Medicaid recipients in Kentucky, 1998-2002.

    Science.gov (United States)

    Havens, Jennifer R; Talbert, Jeffrey C; Walker, Robert; Leedham, Cynthia; Leukefeld, Carl G

    2006-01-01

    Prescription opioid abuse has emerged as a public health problem, particularly in rural America. To examine temporal and geographic trends in rates of controlled-release oxycodone (OxyContin) prescribing for Kentucky Medicaid recipients. A cross-sectional analysis was completed in which the state was divided into 3 regions (distressed Appalachia, Appalachia, and other Kentucky), and data from Medicaid pharmacy claims from 1998 to 2002 were analyzed. Claims were further stratified by disability status. Temporary Assistance for Needy Families Medicaid recipients in distressed Appalachia were more likely than those in other Kentucky regions to file controlled-release oxycodone claims in 1999, 2001, and 2002. Even after adjusting for the proportion of Temporary Assistance for Needy Families recipients in each region, the distressed region still had significantly higher rates (P< .05) than the non-Appalachian region of controlled-release oxycodone prescription claims among Temporary Assistance for Needy Families recipients. Similar findings were observed for disabled Medicaid recipients in 2002. Higher rates of claims for controlled-release oxycodone in the distressed Appalachian region of Kentucky suggest that economic and health factors unique to this area may be contributing to increased use of this product. The increased availability of controlled-release oxycodone in distressed Appalachian regions may facilitate abuse.

  6. Subcutaneous epinephrine vs nebulized salbutamol in asthma.

    Science.gov (United States)

    Sharma, A; Madan, A

    2001-12-01

    This study was conducted to compare the efficacy of the subcutaneous epinephrine with nebulized salbutamol. Fifty asthmatic children in the age range of 6-14 years were divided into two equal groups. Group I children were given subcutaneous epinephrine and Group II were nebulized with salbutamol. Patients were observed at 15, 20, 30, 60, 120, 180 and 240 minute intervals. Both the groups had comparable mean increase in peak expiratory flow rate (PEFR %) (Group I 27.7 +/- 0.7; Group II 28.8 +/- 0.06, p >0.05). In Group I there was significant increase in systolic blood pressure, 30 minutes after the start of treatment, however it settled on its own by 60 minutes. Both the groups had satisfactory improvement in clinical parameters which continued upto 4 hours after start of treatment. Subcutaneous epinephrine can be safely used if nebulizers are not available.

  7. Hypertrophic Obesity and Subcutaneous Adipose Tissue Dysfunction

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    Anna Meiliana

    2014-08-01

    Full Text Available BACKGROUND: Over the past 50 years, scientists have recognized that not all adipose tissue is alike, and that health risk is associated with the location as well as the amount of body fat. Different depots are sufficiently distinct with respect to fatty-acid storage and release as to probably play unique roles in human physiology. Whether fat redistribution causes metabolic disease or whether it is a marker of underlying processes that are primarily responsible is an open question. CONTENT: The limited expandability of the subcutaneous adipose tissue leads to inappropriate adipose cell expansion (hypertrophic obesity with local inflammation and a dysregulated and insulin-resistant adipose tissue. The inability to store excess fat in the subcutaneous adipose tissue is a likely key mechanism for promoting ectopic fat accumulation in tissues and areas where fat can be stored, including the intra-abdominal and visceral areas, in the liver, epi/pericardial area, around vessels, in the myocardium, and in the skeletal muscles. Many studies have implicated ectopic fat accumulation and the associated lipotoxicity as the major determinant of the metabolic complications of obesity driving systemic insulin resistance, inflammation, hepatic glucose production, and dyslipidemia. SUMMARY: In summary, hypertrophic obesity is due to an impaired ability to recruit and differentiate available adipose precursor cells in the subcutaneous adipose tissue. Thus, the subcutaneous adipose tissue may be particular in its limited ability in certain individuals to undergo adipogenesis during weight increase. Inability to promote subcutaneous adipogenesis under periods of affluence would favor lipid overlow and ectopic fat accumulation with negative metabolic consequences. KEYWORDS: obesity, adipogenesis, subcutaneous adipose tissue, visceral adipose tissue, adipocyte dysfunction.

  8. Electrochemical oxidation of amoxicillin in its pharmaceutical formulation at boron doped diamond (BDD electrode

    Directory of Open Access Journals (Sweden)

    Corneil Quand-Meme Gnamba

    2015-08-01

    Full Text Available In this work, voltammetric andelectrolysis experiments have been carried out on a conductive boron dopeddiamond (BDD electrode in solution containing amoxicillin in itspharmaceutical formulation. The physical characterization of the BDD surface byscanning electron microscopy (SEM reveals a polycrystalline structure withgrain sizes ranging between 0.3 and 0.6 µm. With Raman spectroscopy, BDDsurface is composed of diamons (Csp3 type carbon (Csp3and graphitic type carbon (Csp2. The electrochemical characterization of the BDD electrode in sulfuric acid electrolyte showed a wide potential window worthing 2.74 V. The oxidation of Amoxicillin showed an irreversible anodic wave on the voltammogram in the domain of water stability indicating a direct oxidation of amoxicillin at BDD surface. The treatment of Amoxicillin in the synthetic wastewaters under various constant current densities 20, 50, 100, 135 mA cm-2 on BDD showed that Amoxicillin is highly reducedunder 100 mA cm-2 reaching 92% of the Chemical Oxygen Demand (CODremoval after 5 h of electrolysis. Investigation performed in perchloric acidas supporting electrolyte led to 87% of COD removal after 5 h of electrolysis.Mineralization of amoxicillin occurs on BDD and the chemical oxygen demandremoval was higher in sulfuric acid than in perchloric acid owing to theinvolvement of the in-situ formed persulfate and perchlorate  to the degradation process mainly in the bulkof the solution. The instantaneous current efficiency (ICE presents anexponential decay indicating that the process was limited by diffusion. Thespecific energy consumed after 5h of the amoxicillin electrolysis was 0.096 kWh COD-1and 0.035 kWh COD-1 in sulfuric acid and in perchloric acidrespectively.

  9. Meta-analysis: is combination of tetracycline and amoxicillin suitable for Helicobacter pylori infection?

    Science.gov (United States)

    Lv, Zhi-Fa; Wang, Fu-Cai; Zheng, Hui-Lie; Wang, Ben; Xie, Yong; Zhou, Xiao-Jiang; Lv, Nong-Hua

    2015-02-28

    To access the efficacy of combination with amoxicillin and tetracycline for eradication of Helicobacter pylori (H. pylori), thus providing clinical practice guidelines. PubMed, EMBASE, Cochrane Central Register of Controlled Trials, Science Citation Index, China National Knowledge Infrastructure, Wanfang, and Chinese Biomedical Literature databases and abstract books of major European, American, and Asian gastroenterological meetings were searched. All clinical trials that examined the efficacy of H. pylori eradication therapies and included both tetracycline and amoxicillin in one study arm were selected for this systematic review and meta-analysis. Statistical analysis was performed with Comprehensive Meta-Analysis Software (Version 2). Subgroup, meta-regression, and sensitivity analyses were also carried out. Thirty-three studies met the inclusion criteria. The pooled odds ratio (OR) was 0.90 (95%CI: 0.42-1.78) for quadruple therapy with amoxicillin and tetracycline vs other quadruple regimens, and total eradication rates were 78.1% by intention-to-treat (ITT) and 84.5% by per-protocol (PP) analyses in the experimental groups. The pooled eradication rates of 14-d quadruple regimens with a combination of amoxicillin and tetracycline were 82.3% by ITT and 89.0% by PP, and those of 10-d regimens were 84.6% by ITT and 93.7% by PP. The OR by ITT were 1.21 (95%CI: 0.64-2.28) for triple regimens with amoxicillin and tetracycline vs other regimens and 1.81 (95%CI: 1.37-2.41) for sequential treatment with amoxicillin and tetracycline vs other regimens, respectively. The effectiveness of regimens employing amoxicillin and tetracycline for H. pylori eradication may be not inferior to other regimens, but further study should be necessary.

  10. Effects of Low-Dose Amoxicillin on Staphylococcus aureus USA300 Biofilms.

    Science.gov (United States)

    Mlynek, Kevin D; Callahan, Mary T; Shimkevitch, Anton V; Farmer, Jackson T; Endres, Jennifer L; Marchand, Mélodie; Bayles, Kenneth W; Horswill, Alexander R; Kaplan, Jeffrey B

    2016-05-01

    Previous studies showed that sub-MIC levels of β-lactam antibiotics stimulate biofilm formation in most methicillin-resistant Staphylococcus aureus (MRSA) strains. Here, we investigated this process by measuring the effects of sub-MIC amoxicillin on biofilm formation by the epidemic community-associated MRSA strain USA300. We found that sub-MIC amoxicillin increased the ability of USA300 cells to attach to surfaces and form biofilms under both static and flow conditions. We also found that USA300 biofilms cultured in sub-MIC amoxicillin were thicker, contained more pillar and channel structures, and were less porous than biofilms cultured without antibiotic. Biofilm formation in sub-MIC amoxicillin correlated with the production of extracellular DNA (eDNA). However, eDNA released by amoxicillin-induced cell lysis alone was evidently not sufficient to stimulate biofilm. Sub-MIC levels of two other cell wall-active agents with different mechanisms of action-d-cycloserine and fosfomycin-also stimulated eDNA-dependent biofilm, suggesting that biofilm formation may be a mechanistic adaptation to cell wall stress. Screening a USA300 mariner transposon library for mutants deficient in biofilm formation in sub-MIC amoxicillin identified numerous known mediators of S. aureus β-lactam resistance and biofilm formation, as well as novel genes not previously associated with these phenotypes. Our results link cell wall stress and biofilm formation in MRSA and suggest that eDNA-dependent biofilm formation by strain USA300 in low-dose amoxicillin is an inducible phenotype that can be used to identify novel genes impacting MRSA β-lactam resistance and biofilm formation. Copyright © 2016, American Society for Microbiology. All Rights Reserved.

  11. Efficacy of ceftibuten compared with amoxicillin for otitis media with effusion in infants and children.

    Science.gov (United States)

    Mandel, E M; Casselbrant, M L; Kurs-Lasky, M; Bluestone, C D

    1996-05-01

    This trial compared the efficacy of ceftibuten with that of amoxicillin in resolving otitis media with effusion. Two hundred ten children with otitis media with effusion were randomly assigned to receive either ceftibuten (9 mg/kg/day in one daily dose) or amoxicillin (40 mg/kg/day divided into 3 daily doses) for 14 days. Outcome was assessed at 2 and 4 weeks in all subjects; those without middle ear effusion at the 4-week visit were examined at 8, 12 and 16 weeks. Middle ear status was determined by pneumatic otoscopy and by an algorithm combining pneumatic otoscopy with tympanometry. The percentages of subjects who were effusion-free in the ceftibuten and amoxicillin groups at 2 weeks by otoscopy were 29.8 and 27.2%, respectively (P = 0.59), and by the algorithm, 23.4 and 20.4%, respectively (P = 0.47). In children who were effusion-free at 2 weeks, recurrence of effusion by 16 weeks was noted in approximately 60% of the ceftibuten group and 67% of the amoxicillin group. No medication side effects were reported by 88% of subjects in the ceftibuten group and by 93% of subjects in the amoxicillin group. We found no significant differences between the ceftibuten and amoxicillin groups with respect to resolution of middle ear effusion, rate of recurrence or side effects. Amoxicillin remains the drug of first choice for treatment of otitis media with effusion when treatment is deemed advisable, but ceftibuten may be an alternative drug in selected situations.

  12. Amoxicillin effects on functional microbial community and spread of antibiotic resistance genes in amoxicillin manufacture wastewater treatment system.

    Science.gov (United States)

    Meng, Lingwei; Li, Xiangkun; Wang, Xinran; Ma, Kaili; Liu, Gaige; Zhang, Jie

    2017-11-01

    This study aimed to reveal how amoxicillin (AMX) affected the microbial community and the spread mechanism of antibiotic resistance genes (ARGs) in the AMX manufacture wastewater treatment system. For this purpose, a 1.47 L expanded granular sludge bed (EGSB) reactor was designed and run for 241days treating artificial AMX manufacture wastewater. 454 pyrosequencing was applied to analyze functional microorganisms in the system. The antibiotic genes OXA- 1 , OXA -2 , OXA -10 , TEM -1 , CTX-M -1 , class I integrons (intI1) and 16S rRNA genes were also examined in sludge samples. The results showed that the genera Ignavibacterium, Phocoenobacter, Spirochaeta, Aminobacterium and Cloacibacillus contributed to the degradation of different organic compounds (such as various sugars and amines). And the relative quantification of each β-lactam resistance gene in the study was changed with the increasing of AMX concentration. Furthermore the vertical gene transfer was the main driver for the spread of ARGs rather than horizontal transfer pathways in the system. Copyright © 2017. Published by Elsevier B.V.

  13. Combined subcutaneous, intrathoracic and abdominal splenosis.

    Science.gov (United States)

    Javadrashid, Reza; Paak, Neda; Salehi, Ahad

    2010-09-01

    We report a case of combined subcutaneous, intrathoracic, and abdominal splenosis who presented with attacks of flushing, tachycardia and vague abdominal pain. The patient's past medical history included a splenectomy due to abdominal trauma and years later, a lung lobectomy due to recurrent pneumonia. An enhancing solid mass adjacent to the upper pole of the left kidney and nodular pleural based lesions in the left hemi-thorax along with nodular lesions in subcutaneous tissue of the left chest wall suggested possible adrenal malignancy with multiple metastases. Histopathologic examination demonstrated benign lesions of ectopic splenic tissue.

  14. Simultaneous Intercalation of 1-Naphthylacetic Acid and Indole-3-butyric Acid into Layered Double Hydroxides and Controlled Release Properties

    Directory of Open Access Journals (Sweden)

    Shifeng Li

    2014-01-01

    Full Text Available Controlled release formulations have been shown to have potential in overcoming the drawbacks of conventional plant growth regulators formulations. A controlled-release formulation of 1-naphthylacetic acid (NAA and indole-3-butyric acid (IBA simultaneous intercalated MgAl-layered double hydroxides (LDHs was prepared. The synthetic nanohybrid material was characterized by various techniques, and release kinetics was studied. NAA and IBA anions located in the gallery of MgAl-LDHs with bilayer arrangement, and the nanohybrids particles were of typical plate-like shape with the lateral size of 50–100 nm. The results revealed that NAA and IBA have been intercalated into the interlayer spaces of MgAl-LDHs. The release of NAA and IBA fits pseudo-second-order model and is dependent on temperature, pH value, and release medium. The nanohybrids of NAA and IBA simultaneously intercalated in LDHs possessed good controlled release properties.

  15. Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

    Directory of Open Access Journals (Sweden)

    Tariq Ali

    2014-12-01

    Full Text Available The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2 results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.

  16. New cellulose-lignin hydrogels and their application in controlled release of polyphenols

    Energy Technology Data Exchange (ETDEWEB)

    Ciolacu, Diana, E-mail: dciolacu@icmpp.ro; Oprea, Ana Maria; Anghel, Narcis; Cazacu, Georgeta; Cazacu, Maria

    2012-04-01

    Novel superabsorbant cellulose-lignin hydrogels (CL) were prepared by a new two-step procedure consisting in dissolving cellulose in an alkaline solution with further mixing with lignin, followed by the chemical crosslinking with epichlorohydrin. The crosslinking occurrence was verified by Fourier Transform Infrared spectroscopy (FT-IR). The effect of the structure features of cellulose-lignin hydrogels on their dehydration heat was evaluated by Differential Scanning Calorimetry (DSC). The Scanning Electron Microscopy (SEM) images reveal some morphological aspects of the hydrogels. The degree as well as the rate of swelling in a mixture of water:ethanol = 19:1 were estimated. The possible application of these hydrogels as controlled release systems was tested. Polyphenols known as having a wide range of biological effects were selected to be incorporated in such hydrogels by an optimal procedure. The extract of grapes seeds from the Chambourcin type was used as a source of polyphenols (PF). The amount of the incorporated polyphenols was estimated by UV-VIS measurements. Characterization of the hydrogels containing polyphenols was performed by FTIR spectroscopy. Some parameters were estimated based on the registered spectra, as H-bond energy (E{sub H}), the asymmetric index (a/b) and the enthalpy of H-bond formation ({Delta}H). The modifications of the thermal behavior and morphology induced by the presence of the polyphenols in hydrogels were highlighted by DSC and SEM, respectively. The release of polyphenols from CL hydrogels depended on the lignin content from matrices, as assessed by spectral studies. Both loading with polyphenols and their release can be controlled by the composition of the hydrogels. The kinetic of polyphenols release was studied. - Highlights: Black-Right-Pointing-Pointer A unique method to obtain cellulose-lignin hydrogels. Black-Right-Pointing-Pointer The application of these hydrogels as controlled release systems was tested. Black

  17. Ammonia volatilization from blends with stabilized and controlled-released urea in the coffee system

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    Wantuir Filipe Teixeira Chagas

    Full Text Available ABSTRACT Application of stabilized and controlled-release urea blends can reduce the losses of N-NH3 as compared to conventional urea. The aim of this study was to quantify ammonia volatilization from conventional nitrogen fertilizers and blends of urea + (urea + NBPT + controlled release urea applied in drip irrigated coffee system. The experiment was conducted under field conditions in in a Red Latosol located in Lavras-MG, Brazil. The randomized complete block design with six treatments: Urea = 450 kg ha-1 yr-1 N (100% of the recommended dose divided in three splittings equal to 150 kg ha-1 N with an interval of 50 days; ammonium nitrate = 450 kg ha-1 yr-1 N (100% of the recommended dose in three splittings equal to 150 kg ha-1 N with an interval of 50 days; Polyblen Extend(r-100%= 450 kg ha-1 yr-1 (100% of the recommended dose applied in two splittings, 315 kg ha-1 N in the 1º split and 135 kg ha-1 N in the 2º split; Polyblen Extend(r-70% = 315 kg ha-1 yr-1 N (70% of the recommended dose in two splittings, 220.5 kg ha-1 N in the 1º split and 94.5 kg ha-1 N in the 2º split; Polyblen Montanha(r-100% = 450 kg ha-1 yr-1 (100% of the recommended dose in an unique application in the 1º split and Polyblen Montanha(r-70% = 315 kg ha-1 yr-1 N (70% of the recommended dose at an unique application in the 1º split, with three repetitions. Total accumulated N-NH3 losses followed the decreasing order: Urea (83.2 kg ha-1 N > Polyblen Extend(r - 100% (60.3 kg ha-1 N > Polyblen Montanha(r - 100% (46.8 kg ha-1 N > Polyblen Extend(r - 70% (35.1 kg ha-1 N > Polyblen Montanha(r - 70% (24.2 kg ha-1 N > nitrate ammonium (2.0 kg ha-1 N . The use of Polyblen Montanha(r decreases two splittings compared to conventional sources such as urea and ammonium nitrate, by applying only 70% of the recommended dose without affecting yield and coffee crop nutrition.

  18. Impact of controlled release urea on maize yield and nitrogen use efficiency under different water conditions.

    Directory of Open Access Journals (Sweden)

    Guanghao Li

    Full Text Available Controlled release urea (CRU has been widely adopted to increase nitrogen (N use efficiency and maize production, but the impacts can range widely depending on water availability in the soil. In an experiment using Zhengdan 958 (a popular summer maize hybrid, three levels of water treatments (adequate water condition [W3], which maintained soil moisture at about 75% ± 5% of the soil's field capacity; mild water stress [W2], which maintained moisture content at 55% ± 5% of field capacity; and severe water stress [W1], which had a moisture content of 35% ± 5% of field capacity and four levels of controlled release urea fertilizer (N0, N1, N2 and N3 were 0, 105, 210 and 315 kg N ha-1, respectively were compared in a rainout shelter system with soil. The results revealed that CRU had significant effects on maize yields and N use efficiencies under different water conditions. The mean yields increased with increasing water levels and showed significant differences. Under W1, the accumulation of dry matter and N were limited, and N internal efficiency (NIE and the apparent recovery efficiency of applied N (REN decreased with N increases; yields of N1, N2, and N3 were similar. Under W2, the dry matter and N accumulation, as well as the yield, showed an increasing trend with an increase in N application, and the NIE and REN of N3 showed no difference from N2. Under W3, yields of N2 and N3 were similar and they were significantly higher than that of N1, but the agronomic N use efficiency (ANUE, REN, and the physiological NUE (PNUE of N2 were 54.2, 34.9, and 14.4% higher, respectively, than those of N3. N application beyond the optimal N rate did not consistently increase maize yield, and caused a decrease in N use efficiencies. Highest overall dry matter, N accumulation, and yields were observed with N3 under W2, and those showed no differences with N2 and N3 under W3. Under this experimental condition, the CRU of 210 kg ha-1 was optimized when soil

  19. Diels-Alder hydrogels with enhanced stability: First step toward controlled release of bevacizumab.

    Science.gov (United States)

    Kirchhof, Susanne; Gregoritza, Manuel; Messmann, Viktoria; Hammer, Nadine; Goepferich, Achim M; Brandl, Ferdinand P

    2015-10-01

    Eight-armed PEG was functionalized with furyl and maleimide groups (8armPEG20k-Fur and 8armPEG20k-Mal); degradable hydrogels were obtained by cross-linking via Diels-Alder chemistry. To increase the stability to degradation, the macromonomers were modified by introducing a hydrophobic 6-aminohexanoic acid spacer between PEG and the reactive end-groups (8armPEG20k-Ahx-Fur and 8armPEG20k-Ahx-Mal). In an alternative approach, the number of reactive groups per macromonomer was increased by branching the terminal ends of eight-armed PEG with lysine (Lys) and Ahx residues (8armPEG20k-Lys-Ahx-Fur2 and 8armPEG20k-Lys-Ahx-Mal2). The hydrolytic resistance of the synthesized macromonomers was determined by UV spectroscopy; the obtained hydrogels were characterized by rheology and degradation studies. The degradation time of 5% (w/v) 8armPEG20k-Ahx hydrogels (28days) was twice as long as the degradation time of 5% (w/v) 8armPEG20k hydrogels (14days); this is explained by increased hydrolytic resistance of the maleimide group. Using dendritic 8armPEG20k-Lys-Ahx macromonomers substantially increased the stability of the resulting hydrogels; degradation of 5% (w/v) 8armPEG20k-Lys-Ahx hydrogels occurred after 34 weeks. 8armPEG20k hydrogels had the largest mesh size of all tested hydrogels, while hydrogels made from dendritic 8armPEG20k-Lys-Ahx macromonomers showed the smallest value. To evaluate their potential for the controlled release of therapeutic antibodies, the hydrogels were loaded with bevacizumab. The incorporated bevacizumab was released over 10 days (8armPEG20k) and 42days (8armPEG20k-Ahx), respectively; release from 8armPEG20k-Lys-Ahx hydrogels was not completed after 105 days. In summary, we believe that 8armPEG20k-Ahx or 8armPEG20k-Lys-Ahx hydrogels could serve as controlled release system for therapeutic antibodies such as bevacizumab. Copyright © 2015 Elsevier B.V. All rights reserved.

  20. Thermal post-treatment alters nutrient release from a controlled-release fertilizer coated with a waterborne polymer

    OpenAIRE

    Zhou, Zijun; Du, Changwen; Li, Ting; Shen, Yazhen; Zhou, Jianmin

    2015-01-01

    Controlled-release fertilizers (CRF) use a controlled-release technology to enhance the nutrient use efficiency of crops. Many factors affect the release of nutrients from the waterborne polymer-coated CRF, but the effects of thermal post-treatments remain unclear. In this study, a waterborne polyacrylate-coated CRF was post-treated at different temperatures (30 °C, 60 °C, and 80 °C) and durations (2, 4, 8, 12, and 24 h) after being developed in the Wurster fluidized bed. To characterize the ...

  1. The influence of labour on the pharmacokinetics of intravenously administered amoxicillin in pregnant women

    Science.gov (United States)

    Muller, Anouk E; Dörr, P Joep; Mouton, Johan W; De Jongh, Joost; Oostvogel, Paul M; Steegers, Eric A P; Voskuyl, Rob A; Danhof, Meindert

    2008-01-01

    WHAT IS ALREADY KNOWN ABOUT THIS SUBJECTExamples exist that pharmacokinetics of drugs in pregnant women can differ from that in non-pregnant individuals.In pregnant women before the onset of labour, the pharmacokinetics of amoxicillin is similar to that in non-pregnant individuals, but for women during labour this is unknown. WHAT THIS STUDY ADDSLabour influences the pharmacokinetics of amoxicillin.During labour and even more in the immediate postpartum period, the peripheral volume of distribution was decreased compared with pregnant women before the onset of labour.The volume of distribution increases with an increasing amount of oedema. AIMS Many physiological changes take place during pregnancy and labour. These might change the pharmacokinetics of amoxicillin, necessitating adjustment of the dose for prevention of neonatal infections. We investigated the influence of labour on the pharmacokinetics of amoxicillin. METHODS Pregnant women before and during labour were recruited and treated with amoxicillin intravenously. A postpartum dose was offered. Blood samples were obtained and amoxicillin concentrations were determined using high-pressure liquid chromatography. The pharmacokinetics were characterized by nonlinear mixed-effects modelling using NONMEM. RESULTS The pharmacokinetics of amoxicillin in 34 patients was best described by a three-compartment model. Moderate interindividual variability was identified in CL, central and peripheral volumes of distribution. The volume of distribution (V) increased with an increasing amount of oedema. Labour influenced the parameter estimate of peripheral volume of distribution (V2). V2 was decreased during labour, and even more in the immediate postpartum period. For all patients the population estimates (mean ± SE) for CL and V were 21.1 ± 4.1 l h−1 (CL), 8.7 ± 6.6 l (V1), 11.8 ± 7.7 l (V2) and 20.5 ± 15.4 l (V3) respectively. CONCLUSIONS The peripheral distribution volume of amoxicillin in pregnant women during

  2. A combination of amoxicillin and clavulanic acid in the treatment of pyoderma in children

    Directory of Open Access Journals (Sweden)

    Kar P

    1996-01-01

    Full Text Available The efficacy and safety of amoxicillin plus clavulanic acid was compared with that of amoxicillin, erythromycin and co-trimoxazole in an open label, randomized trial in 50 children in each group (total 200 with mild to severe pyodermas. Majority (47% had impetigo. Fifty (25% children had mild pyoderma, 56 (28% had moderate and 94 (47% children had severe pyoderma. Pure growth of S aureus was isolated in 130 (65% children, S pyogenes in 42 (21% and both organisms in 28 (14% children. In mild to moderate pyoderma either of the drug tried was equally effective. In severe pyoderma, 24 of twenty five (96% children receiving amoxicillin plus clavulanic acid, 18 of twenty (90% children in amoxicillin group, 20 of twenty four (83.3% children in erythromycin group and 13 of twenty five (52% children in co-trimoxazole group showed clinical cure of therapy. Amoxicillin combined with clavulanic acid was well tolerated in children and there was no significant side effect except mild diarrhoea in two cases (4% which was well controlled by taking the drug with meals.

  3. Signal Detection of Adverse Drug Reaction of Amoxicillin Using the Korea Adverse Event Reporting System Database.

    Science.gov (United States)

    Soukavong, Mick; Kim, Jungmee; Park, Kyounghoon; Yang, Bo Ram; Lee, Joongyub; Jin, Xue Mei; Park, Byung Joo

    2016-09-01

    We conducted pharmacovigilance data mining for a β-lactam antibiotics, amoxicillin, and compare the adverse events (AEs) with the drug labels of 9 countries including Korea, USA, UK, Japan, Germany, Swiss, Italy, France, and Laos. We used the Korea Adverse Event Reporting System (KAERS) database, a nationwide database of AE reports, between December 1988 and June 2014. Frequentist and Bayesian methods were used to calculate disproportionality distribution of drug-AE pairs. The AE which was detected by all the three indices of proportional reporting ratio (PRR), reporting odds ratio (ROR), and information component (IC) was defined as a signal. The KAERS database contained a total of 807,582 AE reports, among which 1,722 reports were attributed to amoxicillin. Among the 192,510 antibiotics-AE pairs, the number of amoxicillin-AE pairs was 2,913. Among 241 AEs, 52 adverse events were detected as amoxicillin signals. Comparing the drug labels of 9 countries, 12 adverse events including ineffective medicine, bronchitis, rhinitis, sinusitis, dry mouth, gastroesophageal reflux, hypercholesterolemia, gastric carcinoma, abnormal crying, induration, pulmonary carcinoma, and influenza-like symptoms were not listed on any of the labels of nine countries. In conclusion, we detected 12 new signals of amoxicillin which were not listed on the labels of 9 countries. Therefore, it should be followed by signal evaluation including causal association, clinical significance, and preventability.

  4. Treatment of amoxicillin by O3/Fenton process in a rotating packed bed.

    Science.gov (United States)

    Li, Mo; Zeng, Zequan; Li, Yingwen; Arowo, Moses; Chen, Jianfeng; Meng, Hong; Shao, Lei

    2015-03-01

    In this study, simulated amoxicillin wastewater was treated by the O3/Fenton process in a rotating packed bed (RPB) and the results were compared with the Fenton process and the O3 followed by Fenton (O3 + Fenton) process. The chemical oxygen demand (COD) removal rate and the ratio of 5-day biological oxygen demand to chemical oxygen demand (BOD5/COD) in the O3/Fenton process were approximately 17% and 26%, respectively, higher than those in the O3 + Fenton process with an initial pH of 3. The COD removal rate of the amoxicillin solution reached maximum at the Fe(II) concentration of 0.6 mM, temperature of 25 °C, rotation speed of 800 rpm and initial pH of 3. The BOD5/COD of the amoxicillin solution increased from 0 to 0.38 after the solution was treated by the O3/Fenton process. Analysis of the intermediates indicated that the pathway of amoxicillin degradation in the O3/Fenton process was similar to that in the O3 + Fenton process. Contrast experiment results showed that amoxicillin degradation was significantly intensified in the RPB. Copyright © 2014 Elsevier Ltd. All rights reserved.

  5. Combinatorial effects of amoxicillin and metronidazole on selected periodontal bacteria and whole plaque samples.

    Science.gov (United States)

    Kulik Kunz, Eva M; Lenkeit, Krystyna; Waltimo, Tuomas; Weiger, Roland; Walter, Clemens

    2014-06-01

    The aim of the present study was to analyze in vitro the combinatorial effects of the antibiotic combination of amoxicillin plus metronidazole on subgingival bacterial isolates. Aggregatibacter (Actinobacillus) actinomycetemcomitans, Prevotella intermedia/nigrescens, Fusobacterium nucleatum and Eikenella corrodens from our strain collection and subgingival bacteria isolated from patients with periodontitis were tested for their susceptibility to amoxicillin and metronidazole using the Etest. The fractional inhibitory concentration index (FICI), which is commonly used to describe drug interactions, was calculated. Synergy, i.e. FICI values ≤ 0.5, between amoxicillin and metronidazole was shown for two A. actinomycetemcomitans (FICI: 0.3), two F. nucleatum (FICI: 0.3 and 0.5, respectively) and one E. corrodens (FICI: 0.4) isolates. Indifference, i.e. FIC indices of >0.5 but ≤4, occurred for other isolates and the 14 P. intermedia/nigrescens strains tested. Microorganisms resistant to either amoxicillin or metronidazole were detected in all samples by Etest. Combinatorial effects occur between amoxicillin and metronidazole on some strains of A. actinomycetemcomitans, F. nucleatum and E. corrodens. Synergy was shown for a few strains only. Copyright © 2014 Elsevier Ltd. All rights reserved.

  6. Oral microflora and selection of resistance after a single dose of amoxicillin.

    Science.gov (United States)

    Khalil, D; Hultin, M; Rashid, M U; Lund, B

    2016-11-01

    The study aimed to determine the effects of a single-dose antibiotic prophylaxis on normal oral microflora. A single dose of 2 g amoxicillin was given to 29 healthy volunteers. Saliva was collected before antibiotic administration (day 1), and again on days 2, 5, 10, 17 and 24 and subjected to culturing and antibiotic sensitivity analysis. Twenty-one per cent (6/29) of the individuals carried penicillin-V- and amoxicillin-resistant viridans streptococci before antibiotic administration. After a single dose of amoxicillin there was a significant reduction in Streptococcus salivarius on days 2 and 5, a significant reduction in other viridans streptococci on day 2 and the proportion of viridans streptococci with reduced susceptibility to amoxicillin was significantly increased on days 2 and 5. A single dose of amoxicillin can cause an ecological disturbance and induce selection of resistant strains in the oral microflora. Copyright © 2016 European Society of Clinical Microbiology and Infectious Diseases. Published by Elsevier Ltd. All rights reserved.

  7. The degradation of antibiotic amoxicillin in the Fenton-activated sludge combined system.

    Science.gov (United States)

    Guo, Ruixin; Xie, Xiaodan; Chen, Jianqiu

    2015-01-01

    The present study investigated the removal efficiency of amoxicillin by the Fenton process, individual activated sludge process and Fenton-activated sludge combined system. For the antibiotic at 1 g L(-1), the optimal conditions of the Fenton process included: 4 mL FeSO4·7H2O solution (20.43 g  L(-1)), 6 mL H2O2 solution (3%) and 40°C. Under the optimal conditions, the removal rate of amoxicillin achieved up to 80% in 70 min. In addition, the impact of amoxicillin on microorganism limited the removal capacity of the activated sludge process. When the concentration of amoxicillin was less than 350 mg L(-1), 69.04-88.79% of the antibiotic was removed. However, the antibiotic could not be treated by the activated sludge when the concentration increased up to 650 mg L(-1). On the other hand, ifamoxicillin was pretreated partly by the Fenton process it was then degraded completely by the same activated sludge. Thus, the combined system included two steps: 80% amoxicillin was degraded in step I and was removed completely in the cheaper biological treatment (step II). Our result showed that compared with the individual activated sludge process, the Fenton process improved the removal capacity of the subsequent activated sludge process in the combined system.

  8. Optimization of Fenton process for treatment of amoxicillin, ampicillin and cloxacillin antibiotics in aqueous solution.

    Science.gov (United States)

    Elmolla, Emad; Chaudhuri, Malay

    2009-10-30

    The study examined the effect of operating conditions of the Fenton process on biodegradability improvement and mineralization of amoxicillin, ampicillin and cloxacillin antibiotics in aqueous solution. In addition, degradation of amoxicillin, ampicillin and cloxacillin under optimum operating conditions were evaluated. The optimum operating conditions for an aqueous solution containing 104, 105 and 103 mg/L amoxicillin, ampicillin, and cloxacillin, respectively were observed to be COD/H2O2/Fe2+ molar ratio 1:3:0.30 and pH 3. Under optimum operating conditions, complete degradation of amoxicillin, ampicillin and cloxacillin occurred in 2 min. In addition, biodegradability improved from approximately 0 to 0.37 in 10 min, and COD and DOC degradation were 81.4% and 54.3%, respectively in 60 min. Maximum biodegradability (BOD5/COD ratio) improvement was achieved in 10, 20 and 40 min at antibiotics concentration 100, 250 and 500 mg/L, respectively for each antibiotic in aqueous solution. Increase in nitrate and ammonia concentration were observed due to mineralization of organic nitrogen, concentration of nitrate increased from 0.3 to 10 mg/L and concentration of ammonia increased from 8 to 13 mg/L in 60 min. The study indicated that Fenton process can be used for pretreatment of amoxicillin, ampicillin and cloxacillin wastewater for biological treatment.

  9. Pharmacokinetics of amoxicillin-clavulanic acid combination after intravenous and intramuscular administration to turkeys and chickens.

    Science.gov (United States)

    Carceles, C M; Vicente, M S; Escudero, E

    1995-12-01

    The pharmacokinetic behaviour of amoxicillin/clavulanic acid (4:1) combination was studied after intravenous and intramuscular administration of single doses (25 mg/kg body weight) to 15 turkeys and 15 chickens. The objective was to determine whether there are differences between turkeys and chickens in the disposition kinetics of amoxicillin and clavulanic acid. The plasma concentrations-time data were analysed by compartmental pharmacokinetic and non-compartmental methods. The disposition curves for both drugs after intravenous administration were best described by a two-compartment open model in turkeys and chickens. The apparent volumes of distribution of amoxicillin and clavulanic acid were similar in the two species. The body clearances of amoxicillin and clavulanic acid in turkeys were significantly slower than in chickens. The elimination half-life of amoxicillin was similar in turkeys (1.12 +/-0.09 h) and chickens (1.03 +/-0.11 h) after intravenous administration, but that of clavulanic acid differed significantly (P<0.05) between turkeys (1.12 +/-0.03 h) and chickens (0.98 +/- 0.05 h). After intramuscular administration both drugs had a significantly longer half-life (P<0.05) in turkeys and chickens than that after the intravenous treatment. The bioavailability after the intramuscular injection was high and similar with both drugs, but higher values were obtained for chickens than turkeys.

  10. Evaluation of Amoxicillin & Cephalexin concentrations in dental alveolar sockets after tooth extraction

    Directory of Open Access Journals (Sweden)

    Fakhraei AH.

    2005-06-01

    Full Text Available Statement of Problem: One of the most important complications after tooth extraction and oral and maxillofacial surgery is transient bacteraemia and prescription of prophylactic antibiotic is necessary to prevent postoperative infections in immunocompromised patients. Purpose: The aim of this study was the evaluation of cephalexin and amoxicillin concentrations in dental alveolar sockets following tooth extraction. Materials and Methods: In this interventional study, 80 healthy patients subjected to tooth extraction were divided into two groups. Each group received 1 gr amoxicillin or cephalexin and teeth were extracted 30-60-90-120-180 minutes after antibiotic intake. Blood sampling was performed immediately after extraction and concentrations of two antibiotics were measured in microbiology laboratory. ANOVA test and Post-hoc (Duncan test were used for statistical analysis with P<0.05 as the limit of significance. Results: The maximum serum concentration was 10.1006 μg/ml for amoxicillin at 120 minutes and 41.5467 μg/ml for cephalexin at 90 minutes after drug intake. The minimum inhibitory concentration (MIC of cephalexin and amoxicillin for Streptococcus sanguis was 2 μg/ml and 1 μg/ml respectively. Conclusion: The mean concentration for amoxicillin was 10 times and for cephalexin was 20 times higher than MIC.

  11. Transmissible Venereal Tumor with Subcutaneous and Bone ...

    African Journals Online (AJOL)

    A five year old entire mixed breed dog was admitted to the University of Nairobi's small animal clinic with a 5-months history of subcutaneous masses. Physical examination revealed firm and mobile masses in the subcuticular tissues, on the mandible and the transverse processes of the lumbar vertebrae. Visual inspection ...

  12. Radiological case: subcutaneous and mediastinal enfisema

    OpenAIRE

    Nascimento, J.; Gomes, M.; Moreira, C.; Macedo, F.

    2012-01-01

    ABSTRACT We present the case of a 5 year old asmathic girl admitted to the hospital for acute non traumatic edema and crepitus of the face, neck and upper thorax. Thoracic x-ray (not shown) and thoracic and neck CT were performed, showing extensive subcutaneous and mediastinal enfisema. These are rare complications of asthma. The imaging features are described.

  13. Case Report Pneumomediastinum and Subcutaneous Emphysema ...

    African Journals Online (AJOL)

    wheezing and neck pain. He was diagnosed asthmatic at the age of eleven and had been admitted on a few occasions for acute exacerbations in the prior ten years. He had salbutamol tablets regularly. At this index presentation, he was noted to have subcutaneous swelling and crepitus over the neck and upper anterior ...

  14. Thoracic duct lymphography by subcutaneous contrast agent ...

    African Journals Online (AJOL)

    A 4-year-old male Japanese Shiba Inu presented with recurrent chylothorax. The thoracic duct was successfully imaged using computed tomography after the injection of an iodine contrast agent into the subcutaneous tissue surrounding the anus. The thoracic duct was successfully ligated and pericardectomy performed via ...

  15. Anthropometrical Profile, Skinfold Tickness and Subcutaneous Fat ...

    African Journals Online (AJOL)

    Background: The threatening health problems resulting from excess subcutaneous fat depositions have been reported by the world Health Organization. Also noteworthy is that childhood obesity is a pointer to adult obesity. This necessitated a study on the anthropometrical profiles of adolescents of Southeast Nigeria using ...

  16. Case Report: Pneumomediastinum and subcutaneous cervical ...

    African Journals Online (AJOL)

    The occurrence of pneumomediastinum and subcutaneous cervical emphysema as complications of childhood pneumonia is very unusual. They results most often from respiratory manoeuvres that produce high intrathoracic pressure. Although they are largely benign, pneumomediastinum can cause compression of major ...

  17. Iron/dextran sulfate multilayered microcapsules for controlled release of 10-hydroxycamptothecin.

    Science.gov (United States)

    Guo, Shenglei; Zheng, Jian; Dong, Jing; Guo, Na; Jing, Lijia; Yue, Xiuli; Yan, Xiufeng; Wang, Yang; Dai, Zhifei

    2011-10-01

    Stable 10-hydroxycamptothecin (HCPT) microcrystals with a length of about 5-10μm and a ζ-potential of -38.5mV were produced by pH-induced reprecipitation in presence of a stabilizer hydroxypropylmethylcellulose. Sequential layer growth was achieved by the layer-by-layer (LbL) assembly of Fe(3+) and dextran sulfate (DS) on the surface of HCPT microcrystals via both electrostatic interaction and chemical complexation process. The satisfactory drug loading content (67.2±0.82%) as well as high encapsulation efficiency (60.56±0.82%) for four bilayers of Fe(3+)/DS coating was achieved. Both in vitro and in vivo release study revealed that the release time increased as the number of deposited Fe(3+)/DS bilayers increased. These results indicated that such iron-polysaccharide multilayered microcapsules can be a promising approach for the construction of an effective controlled release delivery system of HCPT as well as other drugs with potential cytotoxicity or short half-life time. Copyright © 2011 Elsevier B.V. All rights reserved.

  18. Alginate/chitosan nanoparticles for encapsulation and controlled release of vitamin B2.

    Science.gov (United States)

    Azevedo, Maria A; Bourbon, Ana I; Vicente, António A; Cerqueira, Miguel A

    2014-11-01

    This work aims at evaluating encapsulation and controlled release of vitamin B2 from alginate/chitosan nanoparticles. Ionotropic polyelectrolyte pre-gelation was used as production method being chitosan and alginate used as main materials. Nanoparticles were characterized in terms of average size, polydispersity index (PDI), zeta potential and vitamin entrapment efficiency. The average size for alginate/chitosan nanoparticles was 119.5±49.9nm for samples without vitamin B2 and 104.0±67.2nm with the encapsulation of vitamin B2, presenting a PDI of 0.454±0.066 and 0.319±0.068, respectively. The nanoparticles showed encapsulation efficiency and loading capacity values of 55.9±5.6% and 2.2±0.6%, respectively. Release profiles were evaluated at different conditions showing that the polymeric relaxation was the most influent phenomenon in vitamin B2 release. In order to study their stability nanoparticles were stored at 4°C being particles sizes and PDI evaluated during 5 months showing the results that vitamin B2-loaded nanoparticles are more stable (in terms of size and PDI) than nanoparticles without vitamin B2. Copyright © 2014 Elsevier B.V. All rights reserved.

  19. Blend Hydrogel Microspheres of Carboxymethyl Chitosan and Gelatin for the Controlled Release of 5-Fluorouracil

    Directory of Open Access Journals (Sweden)

    Vanarchi Rajini Kanth

    2017-03-01

    Full Text Available Carboxymethyl chitosan (CMCS was synthesized and blended with gelatin (GE to prepare hydrogel microspheres by w/o emulsion cross-linking in the presence of glutaraldehyde (GA, which acted as a cross-linker. 5-Fluorouracil (5-FU was encapsulated to investigate its controlled release (CR characteristics in acidic (pH 1.2 and alkaline (pH 7.4 buffer media. The microspheres which formed were spherical in nature, with smooth surfaces, as judged by the scanning electron microscopy (SEM. Fourier transform infrared spectroscopy (FTIR confirmed the carboxymethylation of CS and the chemical stability of 5-FU in the formulations. Differential scanning calorimetry (DSC and X-ray diffraction (XRD confirmed the physical state and molecular level dispersion of 5-FU. Equilibrium swelling of microspheres was performed in water, in order to understand the water uptake properties. The in vitro release of 5-FU was extended up to 12 h in pH 7.4 phosphate buffer, revealing an encapsulation efficiency of 72%. The effects of blend composition, the extent of cross-linking, and initial drug loading on the in vitro release properties, were investigated. When analyzed through empirical equations, the release data suggested a non-Fickian transport mechanism.

  20. Enhancement of the controlled-release properties of chitosan membranes by crosslinking with suberoyl chloride.

    Science.gov (United States)

    Chen, Chao; Gao, Zideng; Qiu, Xiaoyun; Hu, Shuwen

    2013-06-19

    A novel crosslinking agent, suberoyl chloride, was used to crosslink N-phthaloyl acylated chitosan and improves the properties of chitosan membranes. Membranes with different crosslinking degrees were synthesized. The derivatives were characterized by Fourier transform infrared spectroscopy and ¹³C solid state nuclear magnetic resonance spectroscopy, which indicated that the crosslinking degrees ranged from 0 to 7.4%. The permeabilities of various plant nutrients, including macroelements (N, P, K), microelements (Zn²⁺ and Cu²⁺), and a plant growth regulator (naphthylacetic acid), were varied by moderate changes in crosslinking degree, indicating that the controlled-release properties can be regulated in this way. The film-forming ability of native chitosan was maintained, whilst mechanical properties, hydrophobicity and controlled permeability were improved. These dramatic improvements occurred with a small amount of added suberoyl chloride; excessive crosslinking led to membranes with unwanted poor permeability. Thus, both the mechanical properties and permeability of the crosslinked membrane can be optimized.

  1. Potential application of thermo-sensitive hydrogels for controlled release of phenacetin

    Directory of Open Access Journals (Sweden)

    Ilić-Stojanović Snežana S.

    2012-01-01

    Full Text Available Over the past years, many scientific researches have been focused on thermo-sensitive hydrogels containing N-isopropylacrylamide (NIPAM as a monomer. The NIPAM based hydrogels with 20 mol% 2-hydroxypropyl methacrylate (HPMet were synthesized using ethylene glycol dimethacrylate as a cross-linker. The characterization of xerogel and phenacetin using FTIR spectra and SEM micrographs confirm the performed synthesis with satisfactory purity as well as loading of phenacetin into hydrogel. The swelling transport mechanism at simulated physiological conditions (pH 2.20 and 7.40 at 37°C is described by the time-independent kinetics. The potential application of synthesized hydrogels for the controlled release of phenacetin as a model drug was investigated at simulated physiological conditions by HPLC method. [Acknowledgement. This work is part of the project MNTR TR-34012 financed by the Ministry of Education and Science of the Republic of Serbia. The authors are grateful for the support provided by the Ministry.

  2. Controlled release of anti-diabetic drug Gliclazide from poly(caprolactone)/poly(acrylic acid) hydrogels.

    Science.gov (United States)

    Bajpai, S K; Chand, Navin; Soni, Shweta

    2015-01-01

    Drug Gliclazide (Glz) has limited solubility and low bioavailability. In order to obtain a controlled release of this drug and to improve its bioavailability, the drug has been loaded into poly(caprolactone) (PCL)/poly(acrylic acid) (PAAc) hydrogels, prepared by free radical polymerization of acrylic acid in the presence of poly(caprolactone) in acetone medium using azo-isobutyronitrile as initiator and N,N' methylene bisacrylamide as cross-linking agent. The swelling behaviour of these hydrogels has been investigated in the physiological gastric and intestinal fluids to obtain an optimum composition suitable for delivery of a biologically active compound. The gels were loaded with anti-diabetic drug Glz and a detailed investigation of release of drug has been carried out. Various kinetic models have been applied on the release data. Finally, the Albino wistar rats were treated for Streptozotocin plus nicotinamide - induced diabetes using a Glz-loaded PCL/PAAc hydrogel. The results indicated a fair reduction in the glucose level of rats.

  3. Encapsulated eucalyptus oil in ionically cross-linked alginate microcapsules and its controlled release.

    Science.gov (United States)

    Noppakundilograt, Supaporn; Piboon, Phianghathai; Graisuwan, Wilaiporn; Nuisin, Roongkan; Kiatkamjornwong, Suda

    2015-10-20

    Sodium alginate microcapsules containing eucalyptus oil were prepared by oil-in-water emulsification via Shirasu porous glass (SPG) membrane and cross-linked by calcium chloride (CaCl2). SPG membrane pore size of 5.2μm was used to control the size of eucalyptus oil microdroplets. Effects of sodium alginate, having a mannuronic acid/guluronic acid (M/G) ratio of 1.13, eucalyptus oil and CaCl2 amounts on microdroplet sizes and size distribution were elucidated. Increasing sodium alginate amounts from 0.1 to 0.5% (wv(-1)) sodium alginate, the average droplets size increased from 42.2±2.0 to 48.5±0.6μm, with CVs of 16.5±2.2 and 30.2±4.5%, respectively. CaCl2 successfully gave narrower size distribution of cross-linked eucalyptus oil microcapsules. The optimum conditions for preparing the microcapsules, oil loading efficiency, and controlled release of the encapsulated eucalyptus oil from the microcapsules as a function of time at 40°C were investigated. Release model for the oil from microcapsules fitted Ritger-Peppas model with non-Fickian transport mechanism. Copyright © 2015 Elsevier Ltd. All rights reserved.

  4. Characterizing and designing polycation-clay nanocomposites as a basis for imazapyr controlled release formulations.

    Science.gov (United States)

    Radian, Adi; Mishael, Yael G

    2008-03-01

    A novel controlled release formulation (CRF) of the herbicide imazapyr (IMP) was designed to reduce its leaching,which causes soil and water contamination. The anionic herbicide IMP was bound to polydiallyldimethylammonium-chloride (PDADMAC)-montmorillonite composites. PDADMAC adsorption reached a high loading of polymer, which resulted in charge reversal of the clay and promoted IMP binding. The composites were characterized by Fourier transform infrared, zeta potential, and X-ray diffraction measurements, indicating electrostatic interactions of the polycation with the surface, polycation intercalation in the clay and suggesting a configuration as loops and tails on the surface at high loadings. IMP binding to the composites is affected by polycation loading and flocculation. Upon adding high concentrations of IMP to a composite of 0.16 g/g, we obtained high herbicide loadings (66% active ingredient). IMP release from the CRFs applied on a thin layer of soil was substantially slower than its release from the commercial formulation (Arsenal). Accordingly, soil column bioassays indicated reduced herbicide leaching (nearly 2-fold) upon applying the CRFs while maintaining good herbicidal activity. The new PDADMAC-clay formulations are promising from the environmental and weed control management points of view.

  5. A new formulation of controlled release amitriptyline pellets and its in vivo/in vitro assessments.

    Science.gov (United States)

    Park, Eun-Seok; Lee, Dong-Soo; Kwon, Seok-Young; Chi, Sang-Cheol

    2003-07-01

    Controlled-release amitriptyline pellets (ATP) were formulated and its oral bioavailability was assessed in human volunteers after oral administration under fasting conditions. Core pellets were prepared using a CF granulator by two different methods (powder layering and solvent spraying) and coated with Eudragit RS or RL 100. Physical characteristics and dissolution rates of core pellets and coated pellets were evaluated to optimize the formulation. Powder layering method resulted in a better surface morphology than solvent spraying method. However, physical properties of the products were poorer when prepared by powder layering method with respect to hardness, friability and density. The dissolution profile of amitriptyline coated with Eudragit RS 100 was comparable to that of commercially available amitriptyline enteric-coated pellets (Saroten retard). After the oral administration of both products at the dose of 50 mg, the mean maximum concentrations (Cmax) were 36.4 and 29.7 ng/mL, and the mean areas under the concentration-time curve (AUC(0-96)) were 1180.2 and 1010.7 ng.h/mL for ATP and Saroten retard, respectively. The time to reach the maximum concentrations (Tmax) was 6 h for both formulations. Statistical evaluation suggested that ATP was bioequivalent to Saroten retard.

  6. Controlled release for crop and wood protection: Recent progress toward sustainable and safe nanostructured biocidal systems.

    Science.gov (United States)

    Mattos, Bruno D; Tardy, Blaise L; Magalhães, Washington L E; Rojas, Orlando J

    2017-09-28

    We review biocide delivery systems (BDS), which are designed to deter or control harmful organisms that damage agricultural crops, forests and forest products. This is a timely topic, given the growing socio-economical concerns that have motivated major developments in sustainable BDS. Associated designs aim at improving or replacing traditional systems, which often consist of biocides with extreme behavior as far as their solubility in water. This includes those that compromise or pollute soil and water (highly soluble or volatile biocides) or those that present low bioavailability (poorly soluble biocides). Major breakthroughs are sought to mitigate or eliminate consequential environmental and health impacts in agriculture and silviculture. Here, we consider the most important BDS vehicles or carriers, their synthesis, the environmental impact of their constituents and interactions with the active components together with the factors that affect their rates of release such as environmental factors and interaction of BDS with the crops or forest products. We put in perspective the state-of-the-art nanostructured carriers for controlled release, which need to address many of the challenges that exist in the application of BDS. Copyright © 2017 Elsevier B.V. All rights reserved.

  7. The Controlled Release of Drugs and Bioactive Compounds from Mesoporous Silica Nanoparticles.

    Science.gov (United States)

    Chowdhury, Mohammad A

    2016-01-01

    In recent period of time the mesoporous silica nanoparticles (MSNs) have been extensively utilised in controlled release (CR) applications. This burgeoning research is favoured because of the unique characteristics of the MSNs such as, ordered and homogenous pore network, high surface area and pore volumes, silanol-containing surfaces, and relatively low toxic in nature. However, for an effective targeted drug delivery, these materials offer numerous challenges such as, to reduce the complications and toxicity and avoid any undesired interactions of the MSNs with the untargeted healthy cells and membranes. A range of concepts and techniques have been implied to overcome these challenges. This article presents an overview on the recent research advancements in CR of drugs and bioactive compounds from the MSNs. Based on the past researches that took place over the last 15 years, the article illustrates three particular areas: 1) unmodified MSNs, 2) modified MSNs, and 3) biocompatibility, bio-toxicity, tissue responses and cellular uptakes of the MSNs. The three encompassed areas of research describe enormous diversities and complexities which span the aspects of complex designs and syntheses, types of silica materials being used, drug loadings, types of drug used, and ranges of biological evaluations of the MSNs. Perspectives and insights are presented into a range of aspects such as, syntheses, characterisations, functionalisation and incorporations of biomacromolecules into the MSNs; drug loadings and drug release kinetics; biological evaluations such as, biocompatibility, bio-toxicity and intracellular drug delivery; and, the effects of size, shape, morphology, structural and textural properties of the MSNs.

  8. Formulation development and evaluation of lamivudine controlled release tablets using cross-linked sago starch.

    Science.gov (United States)

    Singh, Akhilesh Vikram; Nath, Lila Kanta

    2013-02-01

    Modified starches based polymeric substances find utmost applicability in pharmaceutical formulation development. Cross-linked starches showed very promising results in drug delivery application. The present investigation concerns with the development of controlled release tablets of lamivudine using cross-linked sago starch. The cross-linked derivative was synthesized with phosphorous oxychloride and native sago starch in basic pH medium. The cross-linked sago starch was tested for acute toxicity and drug-excipient compatibility study. The formulated tablets were evaluated for various physical characteristics, in vitro dissolution release study and in vivo pharmacokinetic study in rabbit model. In vitro release study showed that the optimized formulation exhibited highest correlation (R) in case of zero order kinetic model and the release mechanism followed a combination of diffusion and erosion process. There was a significant difference in the pharmacokinetic parameters (T(max), C(max), AUC, V(d), T(1/2), and MDT) of the optimized formulation as compared to the marketed conventional tablet Lamivir®. The cross-linked starch showed promising results in terms of controlling the release behavior of the active drug from the matrix. The hydrophilic matrix synthesized by cross-linking could be used with a variety of active pharmaceutical ingredients for making their controlled/sustained release formulations.

  9. Controlled release from aspirin based linear biodegradable poly(anhydride esters) for anti-inflammatory activity.

    Science.gov (United States)

    Dasgupta, Queeny; Movva, Sahitya; Chatterjee, Kaushik; Madras, Giridhar

    2017-08-07

    This work reports the synthesis of a novel, aspirin-loaded, linear poly (anhydride ester) and provides mechanistic insights into the release of aspirin from this polymer for anti-inflammatory activity. As compared to conventional drug delivery systems that rely on diffusion based release, incorporation of bioactives in the polymer backbone is challenging and high loading is difficult to achieve. In the present study, we exploit the pentafunctional sugar alcohol (xylitol) to provide sites for drug (aspirin) attachment at its non-terminal OH groups. The terminal OH groups are polymerized with a diacid anhydride. The hydrolysis of the anhydride and ester bonds under physiological conditions release aspirin from the matrix. The resulting poly(anhydride ester) has high drug loading (53%) and displays controlled release kinetics of aspirin. The polymer releases 8.5 % and 20%, of the loaded drug in one and four weeks, respectively and has a release rate constant of 0.0035h -0.61 . The release rate is suitable for its use as an anti-inflammatory agent without being cytotoxic. The polymer exhibits good cytocompatibility and anti-inflammatory properties and may find applications as injectable or as an implantable bioactive material. The physical insights into the release mechanism can provide development of other drug loaded polymers. Copyright © 2017 Elsevier B.V. All rights reserved.

  10. Multilayer laminar co-extrudate as a novel controlled release dosage form.

    Science.gov (United States)

    Müllers, Katrin C; Wahl, Martin A; Pinto, João F

    2013-07-16

    Design of a new dosage form manufactured by laminar extrusion for oral administration of drugs. Different mixtures of materials (microcrystalline cellulose [MCC], hydroxypropyl methylcellulose [HPMC], lactose [LAC], dicalcium phosphate [DCP], coumarin [COU], propranolol hydrochloride [PRO], water [W]) were prepared prior to laminar extrusion. Mono, bi and tri layer extrudates were manufactured and evaluated for extrudability, drying, water uptake and swelling ability and in vitro characterization of the drug release. Good quality extrudates were manufactured with higher HPMC molecular weight and fraction in formulation at an extrusion rate of 400 mm/min and slow drying (forced air stream), otherwise surface roughness, thickness in-homogeneity, bending and shark skin were present in the extrudates. Swelling of extrudates was dependent on HPMC fraction and molecular weight (60% up to 90% weight gain for low and high polymer chains, respectively) and the presence of either MCC or DCP. The release of drug was dependent on its solubility (PRO>COU), the fraction of HPMC (low>high fractions), the type of diluent (DCP>MCC) and number of layers (1>2>3 layers). By designing the number and type of layers, dosage forms with well-defined release-kinetics can be tailored. The study has shown the ability of the technology of extrusion to manufacture a controlled release dosage form in a continuous fashion. Copyright © 2013 Elsevier B.V. All rights reserved.

  11. Design, in vitro release characterization and pharmacokinetics of novel controlled release pellets containing levodropropizine.

    Science.gov (United States)

    Cao, Qing-Ri; Piao, Yong-Nan; Choi, Jae-Seung; Liu, Yan; Yang, Mingshi; Cui, Jing-Hao

    2014-05-01

    This study was performed to investigate the in vitro release characteristics of levodropropizine (LDP) from novel dual-coated sustained release (SR) pellets, and evaluate the pharmacokinetics of a novel controlled release (CR) preparation composed of the dual-coated SR pellets and immediate release (IR) LDP pellets. The dual-coated SR pellets composed of a drug-loaded nonpareil core, a sub-coating layer (HPMC 6cps) and an SR-coating layer (Aquacoat® ECD, Eudragit® RS 30D or Kollicoat® SR 30D) were prepared by a bottom-spray fluidized bed-coating method. The drug release from the dual-coated SR pellets coated with Aquacoat® ECD followed a zero-order profile in water, and the drug release was not affected by the coating level of the sub-coating layer and stable under the accelerated storage condition (40 °C, 75% RH) for 6 months. The CR preparation showed significantly decreased values of maximum drug concentration (Cmax) and elimination rate (K) than the reference product (LEVOTUS® SYR) but the similar bioavailability (F = 95.43%). The novel CR preparation presents promising delivery of LDP with an immediate and sustained release manner, with similar clinical effect as the commercial IR product.

  12. Statistical optimization of controlled release microspheres containing cetirizine hydrochloride as a model for water soluble drugs.

    Science.gov (United States)

    El-Say, Khalid M; El-Helw, Abdel-Rahim M; Ahmed, Osama A A; Hosny, Khaled M; Ahmed, Tarek A; Kharshoum, Rasha M; Fahmy, Usama A; Alsawahli, Majed

    2015-01-01

    The purpose was to improve the encapsulation efficiency of cetirizine hydrochloride (CTZ) microspheres as a model for water soluble drugs and control its release by applying response surface methodology. A 3(3) Box-Behnken design was used to determine the effect of drug/polymer ratio (X1), surfactant concentration (X2) and stirring speed (X3), on the mean particle size (Y1), percentage encapsulation efficiency (Y2) and cumulative percent drug released for 12 h (Y3). Emulsion solvent evaporation (ESE) technique was applied utilizing Eudragit RS100 as coating polymer and span 80 as surfactant. All formulations were evaluated for micromeritic properties and morphologically characterized by scanning electron microscopy (SEM). The relative bioavailability of the optimized microspheres was compared with CTZ marketed product after oral administration on healthy human volunteers using a double blind, randomized, cross-over design. The results revealed that the mean particle sizes of the microspheres ranged from 62 to 348 µm and the efficiency of entrapment ranged from 36.3% to 70.1%. The optimized CTZ microspheres exhibited a slow and controlled release over 12 h. The pharmacokinetic data of optimized CTZ microspheres showed prolonged tmax, decreased Cmax and AUC0-∞ value of 3309 ± 211 ng h/ml indicating improved relative bioavailability by 169.4% compared with marketed tablets.

  13. A novel drug carrier based on functional modified nanofiber cellulose and the control release behavior

    Science.gov (United States)

    Shi, Xiangning; Zheng, Yudong; Zhang, Wei; Zhang, Zeyu; Peng, Yunling

    2013-08-01

    This study developed a novel drug carrier based on functional modified bacterial cellulose(BC) which was conjugated with Ibuprofen(IBU) by esterification. BC-Ibuprofen as the macro- molecular prodrugs and drug carrier used to improve the short half-life of the drug, and was able to control release through the hydrolysis of ester bond between the hydroxyl groups of BC with Ibuprofen under different condition. Fourier transform infrared analysis revealed that Ibuprofen had been successfully grafted onto the bacterial cellulose (BC). Thermal and morphological characterization indicated the formation of the BC-Ibuprofen system incompletely reacted maintained the bulk structure of the pristine material such as crystallinity, 3-dimentional network and so on. The drug release behaviours were affected by the ester bond hydrolysis as well as the microstructure characteristics of the modified nanofiber. The release of BC-IBU showed an apparent pH-dependent, fast in alkaline and acid solution but slow relatively in neutral. Such pH-responsiveness, in addition to its morphological characteristics, in this paper suggested a great potential of BC-IBU as a more effective, safe, and stable prodrug candidate.

  14. Rheological behaviour and physical properties of controlled-release gluten-based bioplastics.

    Science.gov (United States)

    Gómez-Martínez, D; Partal, P; Martínez, I; Gallegos, C

    2009-03-01

    Bioplastics based on glycerol, water and wheat gluten have been manufactured in order to determine the effect that mechanical processing and further thermal treatments exert on different thermo-mechanical properties of the biomaterials obtained. An "active agent", KCl was incorporated in these matrices to develop controlled-release formulations. Oscillatory shear, dynamic mechanical thermal analysis (DMTA), diffusion and water absorption tests were carried out in order to study the influence of the above-mentioned treatments on the physico-chemical characteristics and rheological behaviour of these bioplastic samples. Wheat gluten protein-based bioplastics studied in this work present a high ability for thermosetting modification, due to protein denaturation, which may favour the development of a wide variety of biomaterials. Bioplastic hygroscopic properties depend on plasticizer nature and processing procedure, and may be a key factor for industrial applications where water absorption is required. On the other hand, high water absorption and slow KCl release from bioplastic samples (both of them suitable properties in agricultural applications) may be obtained by adding citric acid to a given formulation, at selected processing conditions.

  15. Diffusion characteristics and controlled release of bacterial fertilizers from modified calcium alginate capsules.

    Science.gov (United States)

    Liu, Chien-Hung; Wu, Jane-Yii; Chang, Jo-Shu

    2008-04-01

    An indigenous Cellulosimicrobium cellulans GS6 isolate able to solubilize insoluble phosphate complexes in soil is a potential bacterial fertilizer. Enclosure of the phosphate-solubilizing bacterium (PSB) in biodegradable capsules may protect the PSB cells inoculated into soil and, in the meantime, enable the control of cell release that confers long-term fertilizing effects. In this study, calcium alginate (CA) was used as the core matrix to encapsulate cells of C. cellulans GS6. The cell-liberating properties of the CA-based capsules were modified by blending with a variety of supplemental materials (SM), including chitin, cellulose, olive oil, and gelatin. The experimental results showed that the maximum cell-release percentage (MCR%) of the capsules decreased in the order of CA-cellulose>CA-olive oil>CA-chitin>CA-gelatin>CA. Furthermore, a mass transport model was developed to accurately describe the kinetics of cell release results for each capsule. The diffusion coefficient (D(e)) of each capsule was also determined from the model simulation. We found that the estimated D(e) values are positively correlated to the release rate with rare exceptions. Lastly, as our results underscored the crucial roles that the type of capsules plays in the rate and amount of cell release, controlled release of the bacterial fertilizer (C. cellulans GS6 cells) may be achieved via the design of capsule materials.

  16. Development of biopolymer nanocomposite for silver nanoparticles and Ciprofloxacin controlled release.

    Science.gov (United States)

    Islan, German A; Mukherjee, Arup; Castro, Guillermo R

    2015-01-01

    Screening of biopolymeric gel beads containing Silver NanoParticles (Ag-NPs) stabilized in Guar Gum Alkyl Amine (GGAA) and Ciprofloxacin (Cip) was carried out in order to obtain a novel nanocomposite with controlled release profile of both antimicrobians. The selected matrix composed of Alginate/High Methoxyl Pectin (HMP)/GGAA (4:4:1) was able to co-incorporate Ag-NPs and Cip with encapsulation efficiency higher than 70%. SEM images revealed good cohesivity and compatibility between the biopolymers and the cargos. Beads provided protection against Ag-NPs degradation at acidic pHs and HMP would played a key role providing hydrophobic regions. While Cip release profile showed a pH independent diffusional process, Ag-NPs release was restricted to matrix erodability. Calcium quelating agents and/or alginate degrading enzymes could modulate the release profile. The bactericidal activity of beads was tested in liquid medium, showing cooperative effects between the antimicrobials against Pseudomonas aeruginosa, Escherichia coli, Bacillus cereus and Staphylococcus aureus. TEM images confirmed interaction of Ag-NPs with bacterial surfaces followed by membrane damage. Results suggested the nanocomposite matrix as a promising system for oral treatment of intestinal infectious diseases caused by multidrug resistant and unknown microorganisms, since both Cip and Ag-NPs would be able to reach intestine in the active form. Copyright © 2014 Elsevier B.V. All rights reserved.

  17. Controlled release of astaxanthin from nanoporous silicified-phospholipids assembled boron nitride complex for cosmetic applications

    Science.gov (United States)

    Lee, Hye Sun; Sung, Dae Kyung; Kim, Sung Hyun; Choi, Won Il; Hwang, Ee Tag; Choi, Doo Jin; Chang, Jeong Ho

    2017-12-01

    Nanoporous silicified-phospholipids assembled boron nitride (nSPLs@BN) powder was prepared and demonstrated for use in controlled release of anti-oxidant astaxanthin (AX) as a cosmetic application. The nanoporous silicified phospholipids (nSPLs) were obtained by the silicification with tetraethyl orthosilicate (TEOS) of the hydrophilic region of phospholipid bilayers. This process involved the co-assembly of chemically active phospholipid bilayers within the porous silica matrix. In addition, nSPLs@BN was characterized using several analytical techniques and tested to assess their efficiency as drug delivery systems. We calculated the maximum release amounts as a function of time and various pH. The release rate of AX from the nSPLs@BN for the initial 24 h was 10.7 μmol/(h mg) at pH 7.4. Furthermore, we determined the antioxidant activity (KD) for the released AX with DPPH (1,1-diphenyl-2-picryl-hydrazyl) radical and the result was 34.6%.

  18. [Oxidation of mercury by CuBr2 decomposition under controlled-release membrane catalysis condition].

    Science.gov (United States)

    Hu, Lin-Gang; Qu, Zan; Yan, Nai-Qiang; Guo, Yong-Fu; Xie, Jiang-Kun; Jia, Jin-Ping

    2014-02-01

    CuBr2 in the multi-porous ceramic membrane can release Br2 at high temperature, which was employed as the oxidant for Hg0 oxidation. Hg0 oxidation efficiency was studied by a membrane catalysis device. Meanwhile, a reaction and in situ monitoring device was designed to avoid the impact of Br2 on the downstream pipe. The result showed that the MnO(x)/alpha-Al2O3 catalysis membrane had a considerable "controlled-release" effect on Br2 produced by CuBr2 decomposition. The adsorption and reaction of Hg0 and Br2 on the surface of catalysis membrane obeyed the Langmuir-Hinshelwood mechanism. The removal efficiency of Hg0 increased with the rising of Br2 concentration. However, when Br2 reached a certain concentration, the removal efficiency was limited by adsorption rate and reaction rate of Hg0 and Br2 on the catalysis membrane. From 473 K to 573 K, the variation of Hg0 oxidation efficiency was relatively stable. SO2 in flue gas inhibited the oxidation of Hg0 while NO displayed no obvious effect.

  19. β-Cyclodextrin grafted polypyrrole magnetic nanocomposites toward the targeted delivery and controlled release of doxorubicin

    Science.gov (United States)

    Hong, Shasha; Li, Zengbo; Li, Chenzhong; Dong, Chuan; Shuang, Shaomin

    2018-01-01

    The Fe3O4@PPy-HA-β-CD nanocomposites as the novel nanocarrier were prepared by grafting ethylenediamine derivative of​ β-​CD to the surface of polypyrrole-coated magnetic nanoparticles (Fe3O4@PPy) via using hyaluronan (HA) as the intermediate linker. HA was also the efficient target ligand for CD44. The as-prepared drug carrier was characterized by TEM, TGA, XRD, and VSM and used for the delivery of doxorubicin hydrochloride (DOX) with the high loading content of 447 mg/g. The multilayer Freundlich isotherm model was found to be a good fit for the loading of the drug carrier for DOX. Significant NIR-triggered release of DOX was observed in a weak acidic pH. And the release data in vitro was well described using the Retiger-Pepper kinetic model. Furthermore, MTT assay and confocal microscopy against Hep-G2 cells clearly illustrated that the drug carrier had no associated cytotoxicity and could easily enter the cells. The release and accumulation of DOX were observed in the cell nuclei. Thus, the DOX-loaded drug carrier killed the cancer cells efficaciously and minimized adverse side effects due to its target effect. These results suggested the as-prepared drug carrier would be of great potential for the controlled release and targeted delivery of DOX.

  20. An oral controlled release system for ambroxol hydrochloride containing a wax and a water insoluble polymer.

    Science.gov (United States)

    Chi, Na; Guo, Ju Hong; Zhang, Yu; Zhang, Wei; Tang, Xing

    2010-01-01

    This study was carried out to develop and optimize oral sustained-release formulations for Ambroxol hydrochloride matrix pellets using a combination of wax and water-insoluble polymer, glyceryl behenate (Compritol 888 ATO) and Ethylcellulose (EC(7 FP)). It involved three factors: the content of Compritol 888 ATO (X(1)), EC(7 FP) (X(2)), and the matrix formation methods (X(3)), as independent variables. The drug release percentages at 1, 2 and 4 h were the target responses and were restricted to 15-45% (Y(1)), 45-80% (Y(2)) and 80-100% (Y(3)), respectively. The final blend formulation prepared by extrusion spheronization, was achieved with 27.00% (w/w) Ambroxol hydrochloride, 48.70% (w/w) Compritol 888 ATO, and 24.30% (w/w) EC(7 Fp) with 40 degrees C for 12 h. Comparing the single matrix materials consisting of just the wax or water-insoluble in the complex matrix system containing wax and water-insoluble polymer, the release of the drug can be far more retarded, when the formulations have undergone the process of heat treatment. Furthermore, the combination of the two polymers, with flexible matrix formation methods, will offer a very promising way of producing matrix pellets instead of coated controlled-release pellets to meet various demands of drug release.

  1. Dynamics of controlled release systems based on water-in-water emulsions: a general theory.

    Science.gov (United States)

    Sagis, Leonard M C

    2008-10-06

    Phase-separated biopolymer solutions, and aqueous dispersions of hydrogel beads, liposomes, polymersomes, aqueous polymer microcapsules, and colloidosomes are all examples of water-in-water emulsions. These systems can be used for encapsulation and controlled release purposes, in for example food or pharmaceutical applications. The stress-deformation behavior of the droplets in these systems is very complex, and affected by mass transfer across the interface. The relaxation time of a deformation of a droplet may depend on interfacial properties such as surface tension, bending rigidity, spontaneous curvature, permeability, and interfacial viscoelasticity. It also depends on bulk viscoelasticity and composition. A non-equilibrium thermodynamic model is developed for the dynamic behavior of these systems, which incorporates all these parameters, and is based on the interfacial transport phenomena (ITP) formalism. The ITP formalism allows us to describe all water-in-water emulsions with one general theory. Phase-separated biopolymer solutions, and dispersions of hydrogel beads, liposomes, polymersomes, polymer microcapsules, and colloidosomes are basically limiting cases of this general theory with respect to bulk and interfacial rheological behavior.

  2. Studies on controlled release effervescent osmotic pump tablets from Traditional Chinese Medicine Compound Recipe.

    Science.gov (United States)

    Li, Xiao-Dong; Pan, Wei-San; Nie, Shu-Fang; Wu, Li-Jun

    2004-05-18

    A controlled release effervescent osmotic pump tablet (EOPT) of Traditional Chinese Medicine Compound Recipe (TCMCR), named Fuzilizhong prescription which includes acidic drugs consisted of many known and unknown effective components and has been used for several thousands years, was successfully prepared with sodium chloride, sodium hydrogen carbonate and hydroxypropylmethylcellulose(HPMC) as osmotic agents. Since the osmotic pressure in EOPT with sodium chloride and sodium hydrogen carbonate increased greatly, which was induced mostly by gas carbon dioxide generating from the reaction of sodium hydrogen carbonate and the acidic drugs in TCMCR after the fluid being imbibed into the compartment through the semipermeable membrane and the in vitro accumulative dissolution percent from prescription 3 was up to 96.6% at 14 hour, the problem that water insoluble drugs can not to be elementary osmotic pump tablet for its low dissolution rate was solved in the paper. On the basis of prescription 3, the drug in effervescent osmotic pump tablet was released controllably after HPMC was selected as retarder and has a good in-vitro-in-vivo correlation(IVIVC, r=0.9550). Threrfore, it could be concluded that the formulation of TCMCR is appropriate to being made into EOPT, which improves acidic drugs composed of soluble and poorly soluble components release more greatly and controllably. From the point of this, water insoluble drugs can be designed to elementary osmotic pump tablet for more complete dissolution release.

  3. Application of Graphene-Oxide-Modified Polyacrylate Polymer for Controlled-Release Coated Urea

    Directory of Open Access Journals (Sweden)

    Wenjun Yuan

    2018-02-01

    Full Text Available Polyacrylate polymer (PA was modified with graphene oxide (GO and the obtained composites were applied as coatings for controlled-release coated urea (CRU. The physicochemical properties of the different PA/GO coatings were characterized in detail and the nitrogen-release characteristics of the obtained CRU samples were determined in water at 25 °C. The experimental results revealed that addition of GO to PA reduced the swelling degree from 83.01% to 46.35% and improved its mechanical properties (the Young’s modulus was improved from 31.52 to 34.97 MPa and the glass transition temperature was increased from 4.21 to 6.11 °C, thus dramatically slowing down the cumulative nutrient release from the CRU fertilizer from 87.25% to 59.71%. These results suggest that GO enhances the properties of PA for CRU applications, which shows that GO-modified PA is a good coating material.

  4. Controlled release fertilizer and container volumes in the production of Parapiptadenia rigida (Benth. Brenan seedlings

    Directory of Open Access Journals (Sweden)

    Ezequiel Gasparin

    2015-10-01

    Full Text Available Growing demand for native tree seedlings will require improvements in quality standards of production processes through the use of more efficient cultivation techniques. This study evaluated the effects of different doses of controlled release fertilizer (CRF and different container volumes in the production of Parapiptadenia rigida seedlings. We examined the effects of five different concentrations (0, 3, 6, 9 and 12 g L-1 substrate of CRF (18-5-9 NPK and three different container volumes (50, 110 and 180 cm3 on seedling height (H and collar diameter (CD measured monthly for seven months and then calculated H/CD ratios. After 210 days of growth, the dry masses of the aerial portions, root systems, and total masses were determined, as well as the concentrations of macro- and micronutrients in the aerial portions of the seedlings. In general, the dose 9 g L-1 substrate combined with the 180 cm3 cultivation tubes demonstrated the best results in terms of the morphological variables analyzed, resulting in consistent quality seedlings for field planting.

  5. [Effects of controlled release fertilizers on N2O emission from paddy field].

    Science.gov (United States)

    Li, Fangmin; Fan, Xiaolin; Liu, Fang; Wang, Qiang

    2004-11-01

    With close chamber method, this paper studied the effects of controlled release fertilizer (CRF), non-coated compound fertilizer (Com) and conventional urea (CK) on N2O emission from paddy field. The results showed that within 10 days after transplanting, the ammonium and nitrate concentrations in the surface water of the plot treated with CRF were significantly different from those treated with Com. The partial coefficient between N2O emission rates and corresponding nitrate concentrations in the water was significantly high (r = 0.6834). Compared with Com, CRF was able to reduce N2O emission from the paddy field. Within 100 days after basal application, the N2O emission rate of treatment CRF was only 13.45%-21.26% of Corn and 71.17%-112.47% of CK. The N2O emission of Com was mainly concentrated in 1-25 d after basal fertilization and mid-aeration period, but that of CRF was remarkably lower during same period, while the peak of N2O emission of CK was postponed and reduced. It was concluded that both one-time fertilization of CRF and several-time fertilizations of conventional urea were able to reduce N2O emission from the paddy field.

  6. Controlled release fertilizer increased phytoremediation of petroleum-contaminated sandy soil.

    Science.gov (United States)

    Cartmill, Andrew D; Cartmill, Donita L; Alarcón, Alejandro

    2014-01-01

    A greenhouse experiment was conducted to determine the effect of the application of controlled release fertilizer [(CRF) 0, 4,6, or 8 kg m(-3)] on Lolium multiflorum Lam. survival and potential biodegradation of petroleum hydrocarbons (0, 3000, 6000, or 15000 mg kg(-1)) in sandy soil. Plant adaptation, growth, photosynthesis, total chlorophyll, and proline content as well as rhizosphere microbial population (culturable heterotrophic fungal and bacterial populations) and total petroleum hydrocarbon (TPH)-degradation were determined. Petroleum induced-toxicity resulted in reduced plant growth, photosynthesis, and nutrient status. Plant adaptation, growth, photosynthesis, and chlorophyll content were enhanced by the application of CRF in contaminated soil. Proline content showed limited use as a physiological indicator of petroleum induced-stress in plants. Bacterial and filamentous fungi populations were stimulated by the petroleum concentrations. Bacterial populations were stimulated by CRF application. At low petroleum contamination, CRF did not enhance TPH-degradation. However, petroleum degradation in the rhizosphere was enhanced by the application of medium rates of CRF, especially when plants were exposed to intermediate and high petroleum contamination. Application of CRF allowed plants to overcome the growth impairment induced by the presence of petroleum hydrocarbons in soils.

  7. Preparation of hydroxypropyl cyclosophoraose/dextran microspheres for the controlled release of ciprofloxacin

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Benel; Jeong, Da Ham; Joo, Sang Woo; Choi, Jae Min; Jung, Seung Ho; Cho, Eun Na [Center for Biotechnology Research in UBITA (CBRU), Konkuk University, Seoul (Korea, Republic of); Lee, Jae Yung [Dept. Biological Science, Mokpo National University, Mokpo (Korea, Republic of); Park, Se Yeon [Dept. Applied Chemistry, Dongduk Women' s University, Seoul (Korea, Republic of)

    2016-12-15

    Hydroxypropyl cyclosophoraose/dextran (HPCys/dextran) microspheres were prepared using an emulsion polymerization method for use as drug carriers to achieve the controlled release of a poorly water-soluble antibacterial drug, ciprofloxacin (CFX). Cyclosophoraoses are cyclic (1 → 2)-β-d-glucans isolated from the Rhizobium species. Characteristics of HPCys/dextran microspheres were investigated using Fourier transform infrared analysis, solid-state 13C nuclear magnetic resonance spectroscopy, and field emission scanning electron microscopy. The amount of CFX released from these microspheres at pH 7.4 (intestinal phase pH) was about two times higher than that released at pH 1.2 (gastric phase pH). Furthermore, HPCys/dextran microspheres did not show any toxicity in human embryonic kidney cells. We propose that HPCys/dextran microspheres could be used as an effective pH-dependent release system for poorly water-soluble drugs such as CFX.

  8. Controlled release drug delivery systems to improve post-operative pharmacotherapy.

    Science.gov (United States)

    Bhusal, Prabhat; Harrison, Jeff; Sharma, Manisha; Jones, David S; Hill, Andrew G; Svirskis, Darren

    2016-10-01

    Over 230 million surgical procedures are conducted worldwide each year with numbers increasing. Pain, undesirable inflammation and infection are common complications experienced by patients following surgery. Opioids, non-steroidal anti-inflammatory drugs (NSAIDs), local anaesthetics (LAs) and antibiotics are the commonly administered drugs peri-operatively to manage these complications. Post-operative pharmacotherapy is typically achieved using immediate-release dosage forms of drugs, which lead to issues around fluctuating plasma concentrations, systemic adverse effects and poor patient adherence. Controlled release (CR) systems for certain medicines including opioids, NSAIDs and antibiotics have demonstrably enhanced treatment efficacy in the post-surgical setting. However, challenges remain to ensure patient safety while achieving individual therapeutic needs. Newer CR systems in the research and development pipeline have a high level of control over medicine release, which can be initiated, tuned or stopped on-demand. Future systems will self-regulate drug release in response to biological markers providing precise individualized therapy. In this review, we cover currently adopted CR systems in post-operative pharmacotherapy, including drug eluting medical devices, and highlight a series of examples of novel CR technologies that have the potential for translation into post-surgical settings to improve medication efficacy and enhance post-surgical recovery.

  9. Potent removal of cyanobacteria with controlled release of toxic secondary metabolites by a titanium xerogel coagulant.

    Science.gov (United States)

    Wang, Xiaomeng; Wang, Xin; Wei, Zhongbo; Zhang, Shujuan

    2018-01-01

    Cyanobacteria blooming is a serious environmental issue throughout the world. Removal of cyanobacterial cells from surface water with controlled release of cyanobacterial organic matter (COM), especially toxic microcystins (MCs), would potentially reduce the processing burden in follow-up water treatment. Coagulation is a key technique in water treatment. Herein, the potential application of a novel titanium xerogel coagulant (TXC) was evaluated for the treatment of cyanobacteria-laden water in terms of cyanobacteria removal efficiency, variation of cell viability, the release and evolution of COM in the floc accumulation and storage process. Under acidic to neutral conditions, TXC showed a higher removal efficiency of approximately 99% for cyanobacteria and a lower residual Ti concentration than the widely-used commercial polyferric sulfate (PFS) and polyaluminum chloride (PAC). Another advantage of TXC was the reduced MCs concentration caused by the released acetylacetone (AcAc) from the hydrolysis of TXC. Under solar irradiation, AcAc degraded the extracellular MCs from an initial concentration of 40 μg/L to a residual concentration of 7 μg/L during a 16-day floc storage process. The low residual Ti concentration (coagulation reduced the toxicity to photobacteria. The results demonstrate that TXC is a promising dual-effect coagulant for treatment of cyanobacteria-laden water. Copyright © 2017 Elsevier Ltd. All rights reserved.

  10. Polymeric macroporous formulations for the control release of mosquitocidal Bacillus sphaericus ISPC-8.

    Science.gov (United States)

    Tripathi, Anuj; Hadapad, Ashok B; Hire, Ramesh S; Melo, Jose S; D'Souza, Stanislaus F

    2013-12-10

    Bio-polymeric mosquitocidal formulations were developed for the control release of Bacillus sphaericus ISPC-8 by the immobilization of its spore-crystal complex onto the macroporous polymeric matrices. The biodegradable formulations were synthesized at sub-zero temperature using natural polymeric substrates like agarose, alginate, cellulose, non-adsorbent cotton, wooden cork powder and also magnetite nanoparticles. The obtained polymeric matrices were morphologically characterized, which showed 85-90% porosity, uniform pores distribution, high permeability and controlled degradation (19-30%) in 4 weeks depending upon the composition of formulations. Further, the polymeric macroporous formulations were tested for persistence of mosquitocidal activity against Culex quinquefasciatus larvae. Unformulated B. sphaericus ISPC-8 spores retained 54% of larvicidal activity after 7 days, which completely reduced after 35 days of treatment. However, the immobilized B. sphaericus spores in agarose-alginate formulations showed high larvicidal activity on day 7 and retained about 45% activity even after 35 days of treatments. Studies on UV-B and pH dependent inactivation of toxins and spore viability showed that these formulations were significantly protecting the spores as compared to the unformulated spores, which suggest its potential application for the mosquito control program. Copyright © 2013 Elsevier Inc. All rights reserved.

  11. Blend Hydrogel Microspheres of Carboxymethyl Chitosan and Gelatin for the Controlled Release of 5-Fluorouracil.

    Science.gov (United States)

    Kanth, Vanarchi Rajini; Kajjari, Praveen B; Madalageri, Priya M; Ravindra, Sakey; Manjeshwar, Lata S; Aminabhavi, Tejraj M

    2017-03-27

    Carboxymethyl chitosan (CMCS) was synthesized and blended with gelatin (GE) to prepare hydrogel microspheres by w/o emulsion cross-linking in the presence of glutaraldehyde (GA), which acted as a cross-linker. 5-Fluorouracil (5-FU) was encapsulated to investigate its controlled release (CR) characteristics in acidic (pH 1.2) and alkaline (pH 7.4) buffer media. The microspheres which formed were spherical in nature, with smooth surfaces, as judged by the scanning electron microscopy (SEM). Fourier transform infrared spectroscopy (FTIR) confirmed the carboxymethylation of CS and the chemical stability of 5-FU in the formulations. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) confirmed the physical state and molecular level dispersion of 5-FU. Equilibrium swelling of microspheres was performed in water, in order to understand the water uptake properties. The in vitro release of 5-FU was extended up to 12 h in pH 7.4 phosphate buffer, revealing an encapsulation efficiency of 72%. The effects of blend composition, the extent of cross-linking, and initial drug loading on the in vitro release properties, were investigated. When analyzed through empirical equations, the release data suggested a non-Fickian transport mechanism.

  12. Controlled release of insulin from folic acid-insulin complex nanoparticles.

    Science.gov (United States)

    Gupta, Rajat; Mohanty, Sanat

    2017-06-01

    Associative interactions between folic acid and proteins are well known. This work leverages these interactions to engineer folic acid nanoparticles for controlled release of insulin during diabetes therapy. The insulin-loaded folic acid nanoformulation is synthesized during this study to achieve better insulin loading and encapsulation than previous strategies. The maximum insulin loading in the FA particles was kept at 6mg with less than 10% insulin loss during the synthesis process which is significantly better compare to previous strategies. The folic acid nanoparticles of 50-150nm size are further characterized in the present study. The release behaviour of insulin from the nanoparticles has been studied to quantify released insulin and folic acid with time using high performance liquid chromatography. Insulin release results suggest that more than 90% of the insulin is encapsulated and released within 24h from folic acid nanoparticles. The analysis of folic acid release along with insulin release indicates that the particles are formed by folic acid-insulin complexation at the molecular level. The release of insulin from nanoparticles is controllable with the change in the crosslinking salt concentration as well as the amount of folic acid loaded during particle synthesis. These results prove that folic acid nanocarriers are capable to control the release of therapeutic proteins. Copyright © 2017 Elsevier B.V. All rights reserved.

  13. Comparative evaluation of polymersome versus micelle structures as vehicles for the controlled release of drugs

    Energy Technology Data Exchange (ETDEWEB)

    Alibolandi, Mona [Mashhad University of Medical Sciences, Biotechnology Research Center, School of Pharmacy (Iran, Islamic Republic of); Ramezani, Mohammad; Abnous, Khalil [Mashhad University of Medical Sciences, Pharmaceutical Research Center, School of Pharmacy (Iran, Islamic Republic of); Sadeghi, Fatemeh, E-mail: sadeghif@mums.ac.ir [Mashhad University of Medical Sciences, Targeted Drug Delivery Research Center, School of Pharmacy (Iran, Islamic Republic of); Hadizadeh, Farzin, E-mail: hadizadehf@mums.ac.ir [Mashhad University of Medical Sciences, Biotechnology Research Center, School of Pharmacy (Iran, Islamic Republic of)

    2015-02-15

    Di-block copolymers composed of two biocompatible polymers, poly(ethylene glycol) and poly(d,l-lactide), were synthesized by ring-opening polymerization for the preparation of doxorubicin-loaded self-assembled nanostructures, including polymeric vesicles (polymersomes) and micelles. The capability and stability of the nanostructures prepared for the controlled release of DOX are discussed in this paper. The in vitro drug release at 37 °C was evaluated up to 6 days at pH 7.4 and 5.5 and in the presence of 50 % FBS. The cellular uptake and cytotoxicity effect of both formulations were also evaluated in the MCF-7 cell line. The SEM and AFM images confirmed the hollow spherical structure of the polymersomes and the solid round structures of the micelles. The TEM results also revealed the uniformity in size and shape of the drug-loaded micelle and polymersome nanostructures. The DOX-loaded micelles and polymersomes presented efficient anticancer performance, as verified by flow cytometry and MTT assay tests. The most important finding of this study is that the prepared nanopolymersomes presented significant increases in the doxorubicin encapsulation efficiency and the stability of the formulation in comparison with the micelle formulation. In vitro studies revealed that polymersomes may be stable in the blood circulation and meet the requirements for an effective drug delivery system.

  14. The Importance of Amoxicillin and Amoxicillin-Clavulanate Determinants in the Diagnosis of Immediate Allergic Reactions to β-Lactams.

    Science.gov (United States)

    Confino-Cohen, Ronit; Rosman, Yossi; Lachover, Idit; Meir Shafrir, Keren; Goldberg, Arnon

    2016-01-01

    Immediate allergic reactions to β-lactam antibiotics are considered to be one of the most important drug hypersensitivities. A positive skin test (ST) with a combination of major and minor penicillin determinants is usually sufficient to recommend avoidance of the culprit drug, whereas a negative ST is usually followed by an oral challenge test (OCT). Recently, concern has been raised regarding the role of amoxicillin (AMX) ST in the diagnosis of AMX allergy. The aim of this study was to examine the additive value of AMX determinants in STs of patients with immediate hypersensitivity reactions to AMX or AMX-clavulanate (AMX-C). Patients with a history of immediate AMX or AMX-C allergy underwent an ST using a combination of penicilloyl-polylysine (PPL) and minor determinants as well as AMX. An ST with AMX-C was added when appropriate. Thirty-one patients were evaluated. Eight patients, all of them with a history of AMX allergy, had positive reactions only to the AMX component. Two patients with AMX-C allergy had a positive ST reaction only to the AMX-C component. Moreover, only 14 patients (13 with AMX and 1 with AMX-C allergy) had a positive reaction to PPL, whereas most patients (54.8%) had positive reactions to other determinants. One patient, who was positive for AMX, developed several urticarial lesions after the test. Skin testing with AMX and AMX-C is mandatory in patients with immediate allergy to these drugs. Failure to perform it may result in a false-negative ST jeopardizing these patients with anaphylactic reactions during a hazardous OCT. © 2016 S. Karger AG, Basel.

  15. Solid-liquid equilibrium data of amoxicillin and hydroxyphenylglycine in aqueous media

    Directory of Open Access Journals (Sweden)

    I. M. Bezerra

    2013-03-01

    Full Text Available The enzymatic synthesis of amoxicillin is catalyzed by Penicillin G Acylase (PGA. As byproducts, hydroxyphenylglycine and alcohol are also formed from hydrolytic reactions and antibiotic synthesis, respectively. The design of this process should be directed to promote the synthesis reaction. At the same time, it is necessary to reduce the hydrolytic reaction of amoxicillin through its crystallization or separation from the reaction medium. This work presents measurements of solid-liquid equilibrium data for amoxicillin and hydroxyphenylglycine in water at different temperatures (283.15 - 298.15 K, pH (5.5 - 7.5 and ethanol composition (0 - 70 wt.%. This information is relevant to determine the conditions that offer the lowest solubility for the antibiotic, favoring its separation and purification. All solubility data were obtained using an analytical method with indirect determination by UV spectroscopy. Ideal thermodynamic modeling was applied to describe the experimental solubility data sets.

  16. Patterns of Helicobacter pylori isolate resistance to fluoroquinolones, amoxicillin, clarithromycin and metronidazoles.

    Science.gov (United States)

    Kumala, Widyasari; Rani, Aziz

    2006-09-01

    Helicobacter pylori eradication using the three antibiotic regimen of amoxicillin, clarithromycin and metronidazole often fails, making it imperative to find substitutes. The following study made use of 72 H. pylori isolates derived from pyloric antrum mucosa biopsies of gastritis and chronic dyspepsia patients treated at the Cipto Mangunkusumo National General Hospital and three private hospitals in Jakarta. Testing for H. pylori sensitivity to various antimicrobials was conducted using the disk diffusion method (Kirby Bauer) and procedures determined by the Clinical and Laboratory Standards Intitute (CLSI)/NCCLS. The resistance rates of the isolates were 100% for metronodazole, 27.8% for clarithromycin, 19.4% for amoxicillin, 6.9% for ciprofloxacin, norfloxacin and ofloxacin, 2.8% for sparfloxacin and gatifloxacin, and 1.4% for levofloxacin and moxifloxacin. Fluoroquinolons have the lowest resistance compared to amoxicillin, clarithromycin and metronidazole.

  17. Controlled Release of Plectasin NZ2114 from a Hybrid Silicone-Hydrogel Material for Inhibition of Staphylococcus aureus Biofilm

    DEFF Research Database (Denmark)

    Klein, Kasper; Grønnemose, Rasmus Birkholm; Alm, Martin

    2017-01-01

    Staphylococcus aureus is a major human pathogen in catheter-related infections. Modifying catheter material with interpenetrating polymer networks is a novel material technology that allows for impregnation with drugs and subsequent controlled release. Here, we evaluated the potential for combini...

  18. N,O6-partially acetylated chitosan nanoparticles hydrophobically-modified for controlled release of steroids and vitamin E

    DEFF Research Database (Denmark)

    Quinones, Javier Perez; Gothelf, Kurt Vesterager; Kjems, Jørgen

    2013-01-01

    Diosgenin, two synthetic analogs of brassinosteroids, testosterone and dl-α-tocopherol were covalently linked to synthetic water-soluble N,O6-partially acetylated chitosan, for their controlled release. Drug linking was confirmed by FTIR spectroscopy and proton NMR. Conjugates were also character...

  19. The Effect of Control-released Basic Fibroblast Growth Factor in Wound Healing: Histological Analyses and Clinical Application

    Directory of Open Access Journals (Sweden)

    Shigeru Matsumoto, MD

    2013-09-01

    Conclusions: These findings suggest that control-released bFGF using gelatin sheet is effective for promoting wound healing. Such therapeutic strategy was considered to offer several clinical advantages including rapid healing and reduction of the dressing change with less patient discomfort.

  20. Trends in Controlled-Release Oxycodone (Oxycontin[R]) Prescribing among Medicaid Recipients in Kentucky, 1998-2002. Research Note

    Science.gov (United States)

    Havens, Jennifer R.; Talbert, Jeffrey C.; Walker, Robert; Leedham, Cynthia; Leukefeld, Carl G.

    2006-01-01

    Context: Prescription opioid abuse has emerged as a public health problem, particularly in rural America. Purpose: To examine temporal and geographic trends in rates of controlled-release oxycodone (OxyContin) prescribing for Kentucky Medicaid recipients. Methods: A cross-sectional analysis was completed in which the state was divided into 3…

  1. 77 FR 33389 - ArborGen, LLC; Availability of an Environmental Assessment for Controlled Release of a...

    Science.gov (United States)

    2012-06-06

    ..., interstate movement, or release into the environment) of organisms and products altered or produced through..., interstate movement, or release in the environment of a regulated article. On February 21, 2011, the Animal... Controlled Release of a Genetically Engineered Eucalyptus Hybrid AGENCY: Animal and Plant Health Inspection...

  2. 77 FR 7123 - ArborGen, LLC; Availability of an Environmental Assessment for Controlled Release of a...

    Science.gov (United States)

    2012-02-10

    ..., interstate movement, or release into the environment) of organisms and products altered or produced through..., interstate movement, or release in the environment of a regulated article. On February 21, 2011, the Animal... Controlled Release of a Genetically Engineered Eucalyptus Hybrid AGENCY: Animal and Plant Health Inspection...

  3. An Open-Label Study of Controlled-Release Melatonin in Treatment of Sleep Disorders in Children with Autism

    Science.gov (United States)

    Giannotti, F.; Cortesi, F.; Cerquiglini, A.; Bernabei, P.

    2006-01-01

    Long-term effectiveness of controlled-release melatonin in 25 children, aged 2.6-9.6 years with autism without other coexistent pathologies was evaluated openly. Sleep patterns were studied using Children's Sleep Habits Questionnaire (CSHQ) and sleep diaries at baseline, after 1-3-6 months melatonin treatment and 1 month after discontinuation.…

  4. A double-blind placebo-controlled study of controlled release fluvoxamine for the treatment of generalized social anxiety disorder

    NARCIS (Netherlands)

    Westenberg, HGM; Stein, DJ; Yang, HC; Li, D; Barbato, LM

    This was a randomized double-blind placebo-controlled multicenter study to assess the efficacy, safety, and tolerability of fluvoxamine in a controlled release (CR) formulation for treatment of generalized social anxiety disorder (GSAD). A total of 300 subjects with GSAD were randomly assigned to

  5. Greenhouse production of Impatiens wallerana using a controlled-release fertiliser produces quality finished plants with enhanced garden performance

    Science.gov (United States)

    Nutrient management during production can greatly influence post-production quality of plants. The objective of this research was to evaluate the effect of controlled release fertilizer (CRF) applied at the time of plug planting on the garden performance (post-production) of impatiens (Impatiens wal...

  6. Clinical efficacy, safety and pharmacokinetics of a newly developed controlled release morphine sulphate suppository in patients with cancer pain

    NARCIS (Netherlands)

    Moolenaar, F.; Meijler, W.J.; Frijlink, H.W.; Visser, Jan; Proost, J.H.

    Objective: To compare the efficacy, safety and pharmacokinetics of a newly developed controlled-release suppository (MSR) with MS Contin tablets (MSC) in cancer patients with pain. Methods: In a double-blind, randomised, two-way crossover trial, 25 patients with cancer pain were selected with a

  7. Azithromycin Is Equally Effective as Amoxicillin in Children with Solitary Erythema Migrans.

    Science.gov (United States)

    Arnež, Maja; Ružić-Sabljić, Eva

    2015-10-01

    Comparison of clinical efficacy and adverse effects of treatment with azithromycin and amoxicillin in children with solitary erythema migrans (EM). Consecutive patients younger than 15 years with untreated solitary EM referred to our institution 2002-2003 were included in this unblinded prospective clinical study in which patients were alternatively treated with either azithromycin for 5 days or amoxicillin for 14 days. The efficacy of treatment of acute disease, development of minor and major manifestations of Lyme borreliosis and adverse effects of treatment were surveyed by follow-up visits during the first year after inclusion. Eighty-four patients received azithromycin and 84 amoxicillin. Pretreatment characteristics in the 2 groups were comparable with the exception that patients in azithromycin group more often reported a tick bite at the site of later EM (69% versus 52%; P = 0.0400), had more often EM on the trunk (50% versus 26%; P = 0.0025) and reported longer duration of symptoms (median 3 versus 2 days; P = 0.0283). The posttreatment period revealed no significant differences between azithromycin and amoxicillin groups including the duration of EM (median 3 days; P = 0.8984) and the appearance of minor (12% versus 21%; P = 0.2146) and major manifestations (2.6% in each group) of Lyme borreliosis. Adverse effects of treatment were observed in 21% of patients treated with azithromycin and in 16% treated with amoxicillin, and the appearance of Jarisch-Herxheimer reaction was recorded in 7% and 15%, respectively (P = 0.1438). Comparison of azithromycin and amoxicillin for the treatment of children with solitary EM revealed comparable efficacy and adverse effects of treatment.

  8. Penicillin allergy: value of including amoxicillin as a determinant in penicillin skin testing.

    Science.gov (United States)

    Lin, Erina; Saxon, Andrew; Riedl, Marc

    2010-01-01

    Allergy to penicillins remains an important issue. Penicillin skin testing (PST) with major and minor determinants has been shown to be a highly valuable tool for identifying IgE-mediated penicillin allergy. The value of additional testing with side-chain-specific moieties from semisynthetic penicillins such as amoxicillin is not well-established in spite of the widespread use of these medications. A retrospective review of all consecutive inpatient PST results from 1995 to 2007 comprising 1,068 patients was performed in our institution on individuals with a self-reported history of beta-lactam allergy to assess the importance of including the amoxicillin determinant in a previously validated PST panel. Descriptive statistics were performed. The PST panel included penicilloyl-polylysine, penicillin G, penicilloate, penilloate and amoxicillin. Of 1,068 patients, 243 (23%) had a positive skin test reaction on the PST panel. Testing with amoxicillin was positive in 30.9% of patients, the majority of whom (81%) were also positive to 1 or more standard penicillin reagents. Fourteen of the 243 positive patients (5.8%) had a positive skin test reaction only to amoxicillin. Additionally, the use of penicilloate and penilloate minor determinants in combination with penicillin G identified a greater percentage of penicillin-allergic individuals compared to using only penicillin G (22.6 vs. 6.6%), demonstrating their importance in the PST panel. These data indicate that the inclusion of the amoxicillin determinant appears to identify a small but important group of allergic individuals who may otherwise test negative on a PST panel. Copyright 2010 S. Karger AG, Basel.

  9. Treatment of Enterococcal Peritonitis in Peritoneal Dialysis Patients by Oral Amoxicillin or Intra-Peritoneal Vancomcyin: a Retrospective Study

    Directory of Open Access Journals (Sweden)

    Cheuk Chun Szeto

    2017-10-01

    Full Text Available Background/Aims: Enterococcal peritonitis in peritoneal dialysis (PD patients is associated with a high complication rate. The optimal treatment regimen of PD-related enterococcal peritonitis is controversial. The latest international guideline recommends intra-peritoneal (IP vancomycin. Although ampicillin is often effective for systemic enterococcal infections, they have little in vitro activity when added to common PD solutions. Since oral amoxicillin achieves therapeutic drug level in the peritoneal cavity, we explore the efficacy of oral amoxicillin for enterococcal peritonitis. Methods: We studied 105 episodes of enterococcal peritonitis over 20 years in our unit; 43 (41.0% were treated with oral amoxicillin, and 62 (59.0% with IP vancomycin. Their clinical outcome was reviewed. Result: The overall primary response rate to oral amoxicillin and IP vancomycin was 76.4% and 85.5%, respectively (p = 0.3. The complete cure rate of oral amoxicillin and IP vancomycin was 55.8% and 54.8%, respectively (p = 0.8. When the 5 episodes of ampicillin-resistant Enterococcus episodes were excluded, the primary response rate and complete cure rate of oral amoxicillin were 86.8% and 63.2%, respectively. Conclusion: Oral amoxicillin has an excellent primary response rate and complete cure rate for PD-related peritonitis episodes caused by Enterococcus species, indicating that oral amoxicillin is a valid and convenient therapeutic option for enterococcal peritonitis episodes.

  10. Safety and Tolerability of Nebulized Amoxicillin-Clavulanic Acid in Patients with COPD (STONAC 1 and STONAC 2)

    NARCIS (Netherlands)

    Nijdam, L.C.; Assink, M.D.M.; Kuijvenhoven, J.C.; de Saegher, M.E.A.; van der Valk, P.D.L.P.M.; van der Palen, Jacobus Adrianus Maria; Brusse-Keizer, M.G.J.; Movig, K.L.L.

    2016-01-01

    The safety and tolerability of nebulized amoxicillin clavulanic acid were determined in patients with stable COPD and during severe exacerbations of COPD. Nine stable COPD patients received doses ranging from 50:10 mg up to 300:60 mg amoxicillin clavulanic acid and eight patients hospitalised for a

  11. Effects of Controlled-Release Urea on Grain Yield of Spring Maize, Nitrogen Use Efficiency and Nitrogen Balance

    Directory of Open Access Journals (Sweden)

    JI Jing-hong

    2017-03-01

    Full Text Available The effects of mixing controlled-released urea (CRU (release period of resin coated urea is 90 days and urea (U on maize yield, nitrogen use efficiency and nitrogen balance were studied by 4 plot experiments (site:Shuangcheng, Binxian, Harbin and Zhaoyuan in two years (from year 2011 to 2012 to clarify the effect of controlled release urea on spring maize and soil nitrogen balance. Results were as follow:Spring maize yield and nitrogen absorption were increased with the increasing nitrogen fertilizer. Compared with applying urea treatment, applying CRU could increase yield, nitrogen absorption, nitrogen use efficiency, agriculture efficiency of nitrogen and nitrogen contribution rate. Under the same amount of nitrogen (100%, 75%, 50%, compared with 100% U as basic fertilizer treatment, maize yield of 100% CRU treatment increased 391, 427, 291 kg·hm-2, nitrogen use efficiency increased by 5.9%,4.9% and 5.1%, agriculture efficiency of nitrogen increased 2.0, 2.6, 2.6 kg·kg-1, and nitrogen contribution rate increased 2.7%, 3.1% and 2.4%, respectively. The value of maize yield, nitrogen absorption, nitrogen use efficiency and agriculture efficiency of nitrogen between the treatment four (40% urea as basic fertilizer+60% urea as topdressing and treatment five (40% urea plus 60% controlled release urea as basic fertilizer were similar. Apparent profit and loss of nitrogen decreased with the increase of nitrogen nitrogen fertilizer. Nitrogen apparent loss by applying 100% controlled release urea was reduced of 15.0 kg·hm-2 than applying 100% U treatment;Nitrogen apparent loss amount was decreased of 23.9 kg·hm-2 under treatment five. The method of mixing 40% urea and 60% controlled release urea should be applied in maize production in Heilongjiang Province.

  12. [Study on self-microemulsifying membrane controlled-release drop pill of hawthorn leaves flavonoids].

    Science.gov (United States)

    Wang, Jin-Xuan; Huang, Hong-Zhang; Li, Ning; Gao, Chong-Kai

    2014-03-01

    To prepare the hawthorn leaves flavonoids self-microemulsifying membrane controlled-release coated drop pill, and to study its release rate in vitro and pharmacokinetics study in vivo. In order to improve the dissolution of hawthorn leaves flavonoids, self-microemulsifying technology was used to prepare the hawthorn leaves flavonoids self-microemulsion. Hawthorn leaves flavonoids self-microemulsifying drop pill was prepared with the PEG 6000. Studies were made on the in vitro release of flavonoids from hawthorn leaves self-micro-emulsifying membrane-moderated coated drop pills and the in vivo pharmacokinetic in rats. The prescription of flavonoids from hawthorn leaves self-micro-emulsifying drop pills was 0.25 g of flavonoids from hawthorn leaves, 0.25 g of iodophenyl maleimide, 0.375 g of polyethylene glycol 400, 0.375 g of cremophor RH 40 and 2 g of polyethylene glycol 6000. The optimized prescription was 4 g of ethyl cellulose 20, 0.64 g of polyethylene glycol 400, 1.8 g of diethyl phthalate, and the weight of coating materials increased by 3.5%. Flavonoids from hawthorn leaves self-micro-emulsifying membrane-moderated coated drop pills complied with the design of sustained-release in 12 h in terms of in vitro release and in vivo pharmacokinetic parameters in rats, and its bioavailability was 2.47 times of quick-release drop pills. Slightly soluble flavonoids from hawthorn leaves could be made into sustained-release preparations by the self-micro-emulsifying and coating technology.

  13. In situ generation of sodium alginate/hydroxyapatite nanocomposite beads as drug-controlled release matrices.

    Science.gov (United States)

    Zhang, J; Wang, Q; Wang, A

    2010-02-01

    In order to find a new way to slow down the release of drugs and to solve the burst release problem of drugs from traditionally used hydrogel matrices, a series of novel pH-sensitive sodium alginate/hydroxyapatite (SA/HA) nanocomposite beads was prepared by the in situ generation of HA micro-particles in the beads during the sol-gel transition process of SA. The SA/HA nanocomposites were characterized by Fourier transform IR spectroscopy, X-ray fluorescence spectrometry, scanning electron microscopy and field emission SEM in order to reveal their composition and surface morphology as well as the role that the in situ generated HA micro-particles play. The factors influencing the swelling behavior, drug loading and controlled release behavior of the SA/HA nanocomposite beads were also investigated using diclofenac sodium (DS) as the model drug. The HA micro-particles act as inorganic crosslinkers in the nanocomposites, which could contract and restrict the movability of the SA polymer chains, and then change the surface morphology and decrease the swell ratio. Meanwhile, the entrapment efficiency of DS was improved, and the burst release of DS was overcome. The factors (including concentration of Ca(2+), reaction time and temperature) affecting the growth of HA micro-particles have a clear influence on the entrapment efficiency and release rate of DS. In this work, the nanocomposite beads prepared under optimum condition could prolong the release of DS for 8h more compared with the pristine SA hydrogel beads.

  14. Effects of aprepitant on the pharmacokinetics of controlled-release oral oxycodone in cancer patients.

    Directory of Open Access Journals (Sweden)

    Yutaka Fujiwara

    Full Text Available PURPOSE: Oxycodone is a µ-opioid receptor agonist widely used in the treatment of cancer pain. The predominant metabolic pathway of oxycodone is CYP3A4-mediated N-demethylation to noroxycodone, while a minor proportion undergoes 3-O-demethylation to oxymorphone by CYP2D6. The aim of this study was to investigate the effects of the mild CYP3A4 inhibitor aprepitant on the pharmacokinetics of orally administered controlled-release (CR oxycodone. METHOD: This study design was an open-label, single-sequence with two phases in cancer patients with pain who continued to be administered orally with multiple doses of CR oxycodone every 8 or 12 hours. Plasma concentration of oxycodone and its metabolites were measured up to 8 hours after administration as follows: on day 1, CR oxycodone was administered alone; on day 2, CR oxycodone was administered with aprepitant (125 mg, at the same time of oxycodone dosing in the morning. The steady-state trough concentrations (Css were measured from day 1 to day 3. RESULTS: Aprepitant increased the area under the plasma concentration-time curve (AUC0-8 of oxycodone by 25% (p<0.001 and of oxymorphone by 34% (p<0.001, as well as decreased the AUC0-8 of noroxycodone by 14% (p<0.001. Moreover, aprepitant increased Css of oxycodone by 57% (p = 0.001 and of oxymorphone by 36% (p<0.001 and decreased Css of noroxycodone by 24% (p = 0.02 at day 3 compared to day 1. CONCLUSIONS: The clinical use of aprepitant in patients receiving multiple doses of CR oxycodone for cancer pain significantly altered plasma concentration levels, but would not appear to need modification of the CR oxycodone dose. TRIAL REGISTRATION: UMIN.ac.jp UMIN000003580.

  15. Electrospun Gelatin/poly(Glycerol Sebacate Membrane with Controlled Release of Antibiotics for Wound Dressing

    Directory of Open Access Journals (Sweden)

    Parisa Shirazaki

    2017-01-01

    Full Text Available Background: The most important risk that threatens the skin wounds is infections. Therefore, fabrication of a membrane as a wound dressing with the ability of antibiotic delivery in a proper delivery rate is especially important. Materials and Methods: Poly(glycerol sebacate (PGS was prepared from sebacic acid and glycerol with 1:1 ratio; then, it was added to gelatin in the 1:3 ratio and was dissolved in 80% (v/v acetic acid, and finally, ciprofloxacin was added in 10% (w/v of polymer solution. The gelatin/PGS membrane was fabricated using an electrospinning method. The membrane was cross-linked using ethyl-3-(3-dimethylaminopropyl carbodiimide ethyl-3-(3-dimethylaminopropylcarbodiim (EDC and N-hydroxysuccinimide (NHS in different time periods to achieve a proper drug release rate. Fourier-transform infrared (FTIR spectroscopy was being used to manifest the peaks of polymers and drug in the membrane. Scanning electron microscopy (SEM was used to evaluate the morphology, fibers diameter, pore size, and porosity before and after crosslinking process. Ultraviolet (UV-visible spectrophotometry was used to show the ciprofloxacin release from the cross-linked membrane. Results: FTIR analysis showed the characteristic peaks of gelatin, PGS, and ciprofloxacin without any added peaks after the crosslinking process. SEM images revealed that nanofibers' size increased during the crosslinking process and porosity was higher than 80% before and after crosslinking process. UV-visible spectrophotometry showed the proper rate of ciprofloxacin release occurred from cross-linked membrane that remaining in EDC/NHS ethanol solution for 120 min. Conclusion: The obtained results suggest that this recently developed gelatin/PGS membrane with controlled release of ciprofloxacin could be a promising biodegradable membrane for wound dressing.

  16. Productivity of irrigated beans due to sources of stabilized nitrogen fertilizer and controlled release

    Directory of Open Access Journals (Sweden)

    Tatiely Gomes Bernardes

    2015-12-01

    Full Text Available ABSTRACT New nitrogen fertilizers are available in the market actually, however, does not have results on the efficiency of the Cerrado conditions. With that objective of this study was to evaluate the effect of urea including stabilized and controlled release urea on yield of irrigated common beans (Phaseolus vulgaris L in no-tillage system. The experiment was conducted in the winter crop, at Embrapa Arroz e Feijão, in Santo Antônio de Goiás, State of Goiás, Brazil. The experimental design was randomized blocks, with five replicates. Treatments consisted of five N sources (urea, urea + NBPT, urea + polymer, ammonium sulphate, and ammonium nitrate and a control (without N being applied 20 kg ha-1 of N at sowing and 80 kg ha-1 onf N in topdressing. We evaluated the chlorophyll content in leaves of common beans, the leaf N content and dry mass weight (MSPA in the flowering of common beans, the number of pods per plant, number of grains per pod, mass of 100 grains, grain yield and final stand of the common beans. The sources of nitrogen fertilizer did not influence, leaf N content, the mass of MSPA and the relative chlorophyll index of common beans. The use of polymerized urea and urea with urease inhibitor, did not produce increases in the number of grains per pod, number of pods per plant, mass of 100 grains and common beans yield compared to traditional sources of N, urea, ammonium sulfate and ammonium nitrate.

  17. Controlled release of NELL-1 protein from chitosan/hydroxyapatite-modified TCP particles.

    Science.gov (United States)

    Zhang, Yulong; Dong, Rui; Park, Yujin; Bohner, Marc; Zhang, Xinli; Ting, Kang; Soo, Chia; Wu, Benjamin M

    2016-09-10

    NEL-like molecule-1 (NELL-1) is a novel osteogenic protein that showing high specificity to osteochondral cells. It was widely used in bone regeneration research by loading onto carriers such as tricalcium phosphate (TCP) particles. However, there has been little research on protein controlled release from this material and its potential application. In this study, TCP was first modified with a hydroxyapatite coating followed by a chitosan coating to prepare chitosan/hydroxyapatite-coated TCP particles (Chi/HA-TCP). The preparation was characterized by SEM, EDX, FTIR, XRD, FM and Zeta potential measurements. The NELL-1 loaded Chi/HA-TCP particles and the release kinetics were investigated in vitro. It was observed that the Chi/HA-TCP particles prepared with the 0.3% (wt/wt) chitosan solution were able to successfully control the release of NELL-1 and maintain a slow, steady release for up to 28 days. Furthermore, more than 78% of the loaded protein's bioactivity was preserved in Chi/HA-TCP particles over the period of the investigation, which was significantly higher than that of the protein released from hydroxyapatite coated TCP (HA-TCP) particles. Collectively, this study suggests that the osteogenic protein NELL-1 showed a sustained release pattern after being encapsulated into the modified Chi/HA-TCP particles, and the NELL-1 integrated composite of Chi/HA-TCP showed a potential to function as a protein delivery carrier and as an improved bone matrix for use in bone regeneration research. Copyright © 2016 Elsevier B.V. All rights reserved.

  18. Development of time and pH dependent controlled release colon specific delivery of tinidazole

    Directory of Open Access Journals (Sweden)

    2008-08-01

    Full Text Available Purpose: Tinidazole is used in treatment of amoebiasis and other protozoal infections in doses of 2.0 g/ day (60 mg/kg for three days. In the present paper, controlled release formulation of tinidazole was developed with an objective to achieve colon specific drug delivery with reduced frequency of dosing, to minimize gastric side effects and thus to increase patient compliance. Methods: Matrix systems of tinidazole (500 mg were prepared by using swellable and pH dependent polymers like hydroxypropyl methylcellulose (HPMC K4M and K15M and eudragit (eudragit L-100 and S-100. Prepared tablets were enteric coated in order to overcome variability in gastric emptying time and delay in the release, to reduce gastric side effects and to provide prolonged localized action in colon. Process of manufacture was optimized during the scale up studies. Bioavailability study (using parallel group design was carried of on conventional marketed, developed uncoated and enteric coated tablets in healthy human volunteers. Results: Bioavailability study showed that greater portion of tinidazole was released in the large intestine and drug level in plasma was above 4 mg/mL in blood for 24 hours. Conclusion: From the results of this study it appears that, the proposed single enteric coated tinidazole (500 mg tablet per day could be used in place of 3-4 doses of 500 mg tinidazole conventional tablet with better control of drug release for targeted drug delivery. In addition developed colon-specific drug delivery system (CDDS was relatively inexpensive and easy to manufacture using conventional pharmaceutical coating technique.

  19. Self-Emulsifying Granules and Pellets: Composition and Formation Mechanisms for Instant or Controlled Release

    Directory of Open Access Journals (Sweden)

    Ioannis Nikolakakis

    2017-11-01

    Full Text Available Many articles have been published in the last two decades demonstrating improvement in the dissolution and absorption of low solubility drugs when formulated into self-emulsifying drug delivery systems (SEDDS. Several such pharmaceutical products have appeared in the market for medium dose (Neoral® for Cyclsoprin A, Kaletra® for Lopinavir and Ritonavir, or low dose medications (Rocaltrol® for Calcitriol and Avodart® for Dutasteride. However, these are in the form of viscous liquids or semisolid presentations, characterized by the disadvantages of high production cost, stability problems and the requirement of large quantities of surfactants. Solid SEDDS (S-SEDDS, as coarse powders, granules or pellets, besides solubility improvement, can be filled easily into capsules or processed into tablets providing a handy dosage form with instant release, which can be further developed into controlled release by mixing with suitable polymers or coating with polymeric films. In this review, the materials used for the preparation of S-SEDDS, their properties and role in the formulations are detailed. Factors affecting the physical characteristics, mechanical properties of S-SEDDS as well as their in vitro release and in vivo absorption are discussed. The mechanisms involved in the formation of instant and sustained release self-emulsifying granules or pellets are elucidated. Relationships are demonstrated between the characteristics of S-SEDDS units (size, shape, mechanical properties, re-emulsification ability, drug migration and drug release and the properties of the submicron emulsions used as massing liquids, with the aim to further elucidate the formation mechanisms. The influence of the composition of the powdered ingredients forming the granule or pellet on the properties of S-SEDDS is also examined. Examples of formulations of S-SEDDS that have been reported in the literature in the last thirteen years (2004–2017 are presented.

  20. Biomimetic synthesized chiral mesoporous silica: Structures and controlled release functions as drug carrier

    Energy Technology Data Exchange (ETDEWEB)

    Li, Jing; Xu, Lu, E-mail: xl2013109@163.com; Yang, Baixue; Bao, Zhihong; Pan, Weisan; Li, Sanming, E-mail: li_sanming2013@163.com

    2015-10-01

    This work initially illustrated the formation mechanism of chiral mesoporous silica (CMS) in a brand new insight named biomimetic synthesis. Three kinds of biomimetic synthesized CMS (B-CMS, including B-CMS1, B-CMS2 and B-CMS3) were prepared using different pH or stirring rate condition, and their characteristics were tested with transmission electron microscope and small angle X-ray diffraction. The model drug indomethacin was loaded into B-CMS and drug loading content was measured using ultraviolet spectroscopy. The result suggested that pH condition influenced energetics of self-assembly process, mainly packing energetics of the surfactant, while stirring rate was the more dominant factor to determine particle length. In application, indomethacin loading content was measured to be 35.3%, 34.8% and 35.1% for indomethacin loaded B-CMS1, indomethacin loaded B-CMS2 and indomethacin loaded B-CMS3. After loading indomethacin into B-CMS carriers, surface area, pore volume and pore diameter of B-CMS carriers were reduced. B-CMS converted crystalline state of indomethacin to amorphous state, leading to the improved indomethacin dissolution. B-CMS1 controlled drug release without burst-release, while B-CMS2 and B-CMS3 released indomethacin faster than B-CMS1, demonstrating that the particle length, the ordered lever of multiple helixes, the curvature degree of helical channels and pore diameter greatly contributed to the release behavior of indomethacin loaded B-CMS. - Highlights: • Chiral mesoporous silica was synthesized using biomimetic method. • pH influenced energetics of self-assembly process of chiral mesoporous silica. • Stirring rate determined the particle length of chiral mesoporous silica. • Controlled release behaviors of chiral mesoporous silica varied based on structures.

  1. Formulation and evaluation of controlled release matrix mucoadhesive tablets of domperidone using Salvia plebeian gum

    Directory of Open Access Journals (Sweden)

    Gurpreet Arora

    2011-01-01

    Full Text Available The aim of study was to prepare controlled release matrix mucoadhesive tablets of domperidone using Salvia plebeian gum as natural polymer. Tablets were formulated by direct compression technology employing the natural polymer in different concentrations (5, 10, 15 and 20% w/w. The prepared batches were evaluated for drug assay, diameter, thickness, hardness and tensile strength, swelling index, mucoadhesive strength (using texture analyzer and subjected to in vitro drug release studies. Real-time stability studies were also conducted on prepared batches. In vitro drug release data were fitted in various release kinetic models for studying the mechanism of drug release. Tensile strength was found to increase from 0.808 ± 0.098 to 1.527 ± 0.10 mN/cm 2 and mucoadhesive strength increased from 13.673 ± 1.542 to 40.378 ± 2.345 N, with an increase in the polymer concentration from 5 to 20% (A1 to A4. Swelling index was reported to increase with both increase in the concentration of gum and the time duration. The in vitro drug release decreased from 97.76 to 83.4% (A1 to A4 with the increase in polymer concentration. The drug release from the matrix tablets was found to follow zero-order and Higuchi models, indicating the matrix-forming potential of natural polymer. The value of n was found to be between 0.5221 and 0.8992, indicating the involvement of more than one drug release mechanism from the formulation and possibly the combination of both diffusion and erosion. These research findings clearly indicate the potential of S. plebeian gum to be used as binder, release retardant and mucoadhesive natural material in tablet formulations.

  2. Tuneable semi-synthetic network alginate for absorptive encapsulation and controlled release of protein therapeutics.

    Science.gov (United States)

    Chan, Ariel W; Neufeld, Ronald J

    2010-12-01

    Stimuli-responsive hydrogels swell or contract in response to external pH, ionic strength or temperature, and are of considerable interest as pharmaceutical controlled release devices. Alginate, a mucoadhesive biopolymer, was used as building block in the semi-synthesis of a tetra-functional acetal-linked networked polymer (SNAP) with carboxylate moieties preserved as stimuli-responsive sensors and tuneable pore sizes larger than the hydrodynamic radius of model molecules ranging between 1 and 540 kDa. Based on the diffusion coefficients calculated from protein uptake experiments, the networked polymer with pre-designed pore size of 80 nm can allow vitamin B(12), lysozyme, subtilisin, insulin, albumin, and urease to diffuse freely into the hydrogel with diffusivity ratio of D(gel)/D(water) (diffusion coefficients in hydrogel to water) between 0.60 and 0.95. Drying was applied as post-fabrication modification to alter/control the diffusional properties of the gel matrix. Together with the pH-responsive swelling properties, SNAP granules containing acid-labile protein therapeutics such as insulin showed protective characteristics by retaining collapsed/compact state in gastric environment (pH˜1.2) while swelling in neutral pH to release the bioactives at near zero-order kinetics. SNAP, a new class of tuneable biomaterial, can be semi-synthesized with desired pore properties, which when applied with the absorptive encapsulation technique, can serve as a technology platform for oral delivery of biomolecules with wide range of molecular sizes. Copyright © 2010 Elsevier Ltd. All rights reserved.

  3. Subcutaneous implantable defibrillator: State-of-the art 2013

    OpenAIRE

    Akerström, Finn; Arias, Miguel A; Pachón, Marta; Puchol, Alberto; Jiménez-López, Jesús

    2013-01-01

    The subcutaneous implantable cardioverter-defibrillator (S-ICD) has recently been approved for commercial use in Europe, New Zealand and the United States. It is comprised of a pulse generator, placed subcutaneously in a left lateral position, and a parasternal subcutaneous lead-electrode with two sensing electrodes separated by a shocking coil. Being an entirely subcutaneous system it avoids important periprocedural and long-term complications associated with transvenous implantable cardiove...

  4. Subcutaneous filariasis: An unusual case report

    Directory of Open Access Journals (Sweden)

    Valand Arvindbhai

    2007-01-01

    Full Text Available Wuchereria bancrofti presented in subcutaneous nodule is a very rare presentation. Wuchereria bancrofti first reported by Bancrofti in Brisbane in 1876 and the name filaria Bancrofti was given in 1877 and the generic name was given in 1878. A 15-year-old male patient′s known case of pulmonary Koch′s with incidentally detected subcutaneous nodule on right arm pit, cytology from the nodule shows many sheathed microfilaria along with segment of an adult female worm. Wet mount peripheral blood smear shows nocturnal motile microfilaria. The Wuchereria bancrofti is known to be associated with pulmonary Koch′s. Nocturnal motility and cytomorphological features differentiate Wuchereria bancrofti from Wuchereria loa loa . After giving diethyl carbamazine (DEC 6 mg/kg for 21 days without disturbing anti Koch′s treatment schedule and microfilaria disappeared from peripheral blood.

  5. A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling

    Science.gov (United States)

    Li, Jin; Chai, Hongyu; Li, Yang; Chai, Xuyu; Zhao, Yan; Zhao, Yunfan; Tao, Tao; Xiang, Xiaoqiang

    2016-01-01

    Background Amoxicillin is a commonly used antibiotic which has a short half-life in human. The frequent administration of amoxicillin is often required to keep the plasma drug level in an effective range. The short dosing interval of amoxicillin could also cause some side effects and drug resistance, and impair its therapeutic efficacy and patients’ compliance. Therefore, a three-pulse release tablet of amoxicillin is desired to generate sustained release in vivo, and thus to avoid the above mentioned disadvantages. Methods The pulsatile release tablet consists of three pulsatile components: one immediate-release granule and two delayed release pellets, all containing amoxicillin. The preparation of a pulsatile release tablet of amoxicillin mainly includes wet granulation craft, extrusion/spheronization craft, pellet coating craft, mixing craft, tablet compression craft and film coating craft. Box–Behnken design, Scanning Electron Microscope and in vitro drug release test were used to help the optimization of formulations. A crossover pharmacokinetic study was performed to compare the pharmacokinetic profile of our in-house pulsatile tablet with that of commercial immediate release tablet. The pharmacokinetic profile of this pulse formulation was simulated by physiologically based pharmacokinetic (PBPK) model with the help of Simcyp®. Results and Discussion Single factor experiments identify four important factors of the formulation, namely, coating weight of Eudragit L30 D-55 (X1), coating weight of AQOAT AS-HF (X2), the extrusion screen aperture (X3) and compression forces (X4). The interrelations of the four factors were uncovered by a Box–Behnken design to help to determine the optimal formulation. The immediate-release granule, two delayed release pellets, together with other excipients, namely, Avicel PH 102, colloidal silicon dioxide, polyplasdone and magnesium stearate were mixed, and compressed into tablets, which was subsequently coated with Opadry

  6. A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling.

    Science.gov (United States)

    Li, Jin; Chai, Hongyu; Li, Yang; Chai, Xuyu; Zhao, Yan; Zhao, Yunfan; Tao, Tao; Xiang, Xiaoqiang

    2016-01-01

    Amoxicillin is a commonly used antibiotic which has a short half-life in human. The frequent administration of amoxicillin is often required to keep the plasma drug level in an effective range. The short dosing interval of amoxicillin could also cause some side effects and drug resistance, and impair its therapeutic efficacy and patients' compliance. Therefore, a three-pulse release tablet of amoxicillin is desired to generate sustained release in vivo, and thus to avoid the above mentioned disadvantages. The pulsatile release tablet consists of three pulsatile components: one immediate-release granule and two delayed release pellets, all containing amoxicillin. The preparation of a pulsatile release tablet of amoxicillin mainly includes wet granulation craft, extrusion/spheronization craft, pellet coating craft, mixing craft, tablet compression craft and film coating craft. Box-Behnken design, Scanning Electron Microscope and in vitro drug release test were used to help the optimization of formulations. A crossover pharmacokinetic study was performed to compare the pharmacokinetic profile of our in-house pulsatile tablet with that of commercial immediate release tablet. The pharmacokinetic profile of this pulse formulation was simulated by physiologically based pharmacokinetic (PBPK) model with the help of Simcyp®. Single factor experiments identify four important factors of the formulation, namely, coating weight of Eudragit L30 D-55 (X1), coating weight of AQOAT AS-HF (X2), the extrusion screen aperture (X3) and compression forces (X4). The interrelations of the four factors were uncovered by a Box-Behnken design to help to determine the optimal formulation. The immediate-release granule, two delayed release pellets, together with other excipients, namely, Avicel PH 102, colloidal silicon dioxide, polyplasdone and magnesium stearate were mixed, and compressed into tablets, which was subsequently coated with Opadry® film to produce pulsatile tablet of

  7. Primary Sonographic Diagnosis of Subcutaneous Cysticercosis

    Directory of Open Access Journals (Sweden)

    M E Shivu

    2011-01-01

    Full Text Available We present the case of a 40-year-old woman with a small diffuse swelling on the left side of her face. She was diagnosed with intramuscular cysticercosis in the masseter muscle (case of disseminated cysticercosis involving the muscular system and subcutaneous tissues with surrounding phlegmon on high-resolution ultrasound and managed conservatively. To our knowledge, the imaging findings of disseminated muscular cysUcercosis have been reported before only a few numbers of times. In this case, the correct diagnosis was made on the basis of high-resolution sonography of the subcutaneous tissue and muscles. It showed multiple oval to circular, predominantly anechoic lesions, which were around 1 cm in diameter. Most of these cystic lesions showed a hyperechoic focus within suggestive of a scolex. There was no increased vascularity surrounding the lesions. Thus, sonography can primarily make the correct diagnosis of disseminated muscular cysticercosis if such lesions are seen. In endemic areas, cysticercosis should be considered one of the differential diagnosis of the subcutaneous swellings.

  8. Macromolecular confinement of therapeutic protein in polymeric particles for controlled release: insulin as a case study

    Directory of Open Access Journals (Sweden)

    Luiz Henrique Guerreiro

    2017-06-01

    Full Text Available ABSTRACT Sustained release systems for therapeutic proteins have been widely studied targeting to improve the action of these drugs. Molecular entrapping of proteins is particularly challenging due to their conformational instability. We have developed a micro-structured poly-epsilon-caprolactone (PCL particle system loaded with human insulin using a simple double-emulsion w/o/w method followed by solvent evaporation method. This formulation is comprised by spheric-shaped microparticles with average size of 10 micrometers. In vitro release showed a biphasic behavior such as a rapid release with about 50% of drug delivered within 2 hours and a sustained phase for up to 48 h. The subcutaneous administration of microencapsulated insulin showed a biphasic effect on glycemia in streptozotocin-induced diabetic mice, compatible with short and intermediate-acting behaviors, with first transition peak at about 2 h and the second phase exerting effect for up to 48h after s.c. administration. This study reveals that a simplified double-emulsion system results in biocompatible human-insulin-loaded PCL microparticles that might be used for further development of optimized sustained release formulations of insulin to be used in the restoration of hormonal levels.

  9. Controlled release of dutasteride from biodegradable microspheres: in vitro and in vivo studies.

    Directory of Open Access Journals (Sweden)

    Xiangyang Xie

    Full Text Available The aim of the present work was to study the in vitro/in vivo characteristics of dutasteride loaded biodegradable microspheres designed for sustained release of dutasteride over four weeks. An O/W emulsion-solvent evaporation method was used to incorporate dutasteride, which is of interest in the treatment of benign prostatic hyperplasia (BPH, into poly(lactide-co-glycolide (PLGA. A response surface method (RSM with central composite design (CCD was employed to optimize the formulation variables. A prolonged in vitro drug release profile was observed, with a complete release of the entrapped drug within 28 days. The pharmacokinetics study showed sustained plasma drug concentration-time profile of dutasteride loaded microspheres after subcutaneous injection into rats. The in vitro drug release in rats correlated well with the in vivo pharmacokinetics profile. The pharmacodynamics evaluated by determination of the BPH inhibition in the rat models also showed a prolonged pharmacological response. These results suggest the potential use of dutasteride loaded biodegradable microspheres for the management of BPH over long periods.

  10. Controlled release of bioactive PDGF-AA from a hydrogel/nanoparticle composite.

    Science.gov (United States)

    Elliott Donaghue, Irja; Shoichet, Molly S

    2015-10-01

    Polymer excipients, such as low molar mass poly(ethylene glycol) (PEG), have shown contradictory effects on protein stability when co-encapsulated in polymeric nanoparticles. To gain further insight into these effects, platelet-derived growth factor (PDGF-AA) was encapsulated in polymeric nanoparticles with vs. without PEG. PDGF-AA is a particularly compelling protein, as it has been demonstrated to promote cell survival and induce the oligodendrocyte differentiation of neural stem/progenitor cells (NSPCs) both in vitro and in vivo. Here we show, for the first time, the controlled release of bioactive PDGF-AA from an injectable nanoparticle/hydrogel drug delivery system (DDS). PDGF-AA was encapsulated, with high efficiency, in poly(lactide-co-glycolide) nanoparticles, and its release from the drug delivery system was followed over 21 d. Interestingly, the co-encapsulation of low molecular weight poly(ethylene glycol) increased the PDGF-AA loading but, unexpectedly, accelerated the aggregation of PDGF-AA, resulting in reduced activity and detection by enzyme-linked immunosorbent assay (ELISA). In the absence of PEG, released PDGF-AA remained bioactive as demonstrated with NSPC oligodendrocyte differentiation, similar to positive controls, and significantly different from untreated controls. This work presents a novel delivery method for differentiation factors, such as PDGF-AA, and provides insights into the contradictory effects reported in the literature of excipients, such as PEG, on the loading and release of proteins from polymeric nanoparticles. Previously, the polymer poly(ethylene glycol) (PEG) has been used in many biomaterials applications, from surface coatings to the encapsulation of proteins. In this work, we demonstrate that, unexpectedly, low molecular weight PEG has a deleterious effect on the release of the encapsulated protein platelet-derived growth factor AA (PDGF-AA). We also demonstrate release of bioactive PDGF-AA (in the absence of PEG

  11. Development and evaluation of controlled-release buccoadhesive verapamil hydrochloride tablets

    Directory of Open Access Journals (Sweden)

    Emami J.

    2008-05-01

    Full Text Available Background and purpose of the study: Verapamil hydrochloride is a calcium channel blocker which is used in the control of supraventricular arrhythmia, hypertension and myocardial infraction. There are considerable inter-individual variations in serum concencentration of verpamil due to variation in the extent of hepatic metabolism. In this study controlled-release buccoadhesive tablets of verapamil hydrochloride (VPH were prepared in order to achieve constant plasma concentrations, to improve the bioavailability by the avoidance of hepatic first-pass metabolism, and to prevent frequent administration. Materials and methods: Tablets containing fixed amount of VPH were prepared by direct compression method using polymers like carbomer (CP, hydroxypropylmethyl cellulose (HPMC and sodium carboxymethyl cellulose (NaCMC in various combination and ratios and evaluated for thickness, weight variation, hardness, drug content uniformity, swelling, mucoadhesive strength, drug release and possible interaction between ingredients. Results: All tablets were acceptable with regard to thickness, weight variation, hardness, and drug content. The maximum bioadhesive strength was observed in tablets formulated with a combination of CP-NaCMC followed by CP-HPMC and NaCMC-HPMC.  Decreasing the content of CP in CP-HPMC tablets or NaCMC in CP-NaCMC or NaCMC-HPMC systems resulted in decrease in detachment forces. Lower release rates were observed by lowering the content of CP in CP-HPMC containing formulations or NaCMC in tablets which contained CP-NaCMC or NaCMC-HPMC. The release behavior was non-Fickian controlled by a combination of diffusion and chain relaxation mechanisms and best fitted zero-order kinetics. Conclusion: The buccoadhesive VPH tablets containing 53% CP and 13.3% HPMC showed suitable release kinetics (n = 0.78, K0 zero order release = 4.11 mg/h, MDT = 5.66 h and adhesive properties and did not show any interaction between polymers and drug based on

  12. Controlled-release oxycodone relieves neuropathic pain: a randomized controlled trial in painful diabetic neuropathy.

    Science.gov (United States)

    Watson, C Peter N; Moulin, Dwight; Watt-Watson, Judith; Gordon, Allan; Eisenhoffer, John

    2003-09-01

    Painful neuropathy is one of the most common long-term complications of diabetes mellitus and often proves difficult to relieve. Patients with diabetic neuropathy with moderate or greater pain for at least 3 months, were evaluated for efficacy, safety and health-related quality of life (QOL) while receiving controlled-release (CR) oxycodone (OxyContin) or active placebo. Patients underwent washout from all opioids 2-7 days before randomization to 10 mg CR oxycodone or active placebo (0.25 mg benztropine) q12h. The dose was increased, approximately weekly, to a maximum of 40 mg q12h CR oxycodone or 1 mg q12h benztropine, with crossover to the alternate treatment after a maximum of 4 weeks. Acetaminophen, 325-650 mg q4-6h prn was provided as rescue. Thirty-six patients were evaluable for efficacy (21 men, 15 women, mean age 63.0+/-9.4 years). CR oxycodone resulted in significantly lower (P=0.0001) mean daily pain (21.8+/-20.7 vs. 48.6+/-26.6 mm VAS), steady pain (23.5+/-23.0 vs. 47.6+/-30.7 mm VAS), brief pain (21.8+/-23.5 vs. 46.7+/-30.8 mm VAS), skin pain (14.3+/-20.4 vs. 43.2+/-31.3 mm VAS), and total pain and disability (16.8+/-15.6 vs. 25.2+/-16.7; P=0.004). Scores from 6 of the 8 SF-36 domains and both summary scales, Standardized Physical Component (P=0.0002) and Standardized Mental Component (P=0.0338) were significantly better during CR oxycodone treatment. The number needed to treat to obtain one patient with at least 50% pain relief is 2.6 and clinical effectiveness scores favoured treatment with CR oxycodone over placebo (P=0.0001). CR oxycodone is effective and safe for the management of painful diabetic neuropathy and improves QOL.

  13. Amoxicillin removal from aqueous solution using activated carbon prepared by chemical activation of olive stone.

    Science.gov (United States)

    Limousy, Lionel; Ghouma, Imen; Ouederni, Abdelmottaleb; Jeguirim, Mejdi

    2017-04-01

    A chemical-activated carbon (CAC) was prepared by phosphoric acid activation of olive stone. The CAC was characterized using various analytical techniques and evaluated for the removal of amoxicillin from aqueous solutions under different operating conditions (initial concentration, 12.5-100 mg L -1 , temperature, 20-25 °C, contact time, 0-7000 min). The CAC characterization indicates that it is a microporous carbon with a specific surface area of 1174 m 2 /g and a pore volume of 0.46 cm 3 /g and contains essentially acidic functional groups. The adsorption tests indicated that 93 % of amoxicillin was removed at 20 °C for 25 mg L -1 initial concentration. Moreover, it was found that adsorption capacity increased with contact time and temperature. Kinetic study shows that the highest correlation was obtained for the pseudo-second-order kinetic model, which confirms that the process of adsorption of amoxicillin is mainly chemisorption. Using the intraparticle diffusion model, the mechanism of the adsorption process was determined. The equilibrium data analysis showed that the Sips and Langmuir models fitted well the experimental data with maximal adsorption capacities of 67.7 and 57 mg/g, respectively, at 25 °C. The chemical-activated carbon of olive stones could be considered as an efficient adsorbent for amoxicillin removal from aqueous solutions.

  14. Additional clinical and microbiological effects of amoxicillin and metronidazole after initial periodontal therapy

    NARCIS (Netherlands)

    Winkel, EG; van Winkelhoff, AJ; van der Velden, U

    1998-01-01

    The aims of this study were to evaluate the clinical and microbiological effects of initial periodontal therapy (IT) and to determine the additional effects of systemic amoxicillin (Flemoxin Solutab(R)) 375 mg TID plus metronidazole 250 mg TID therapy, in patients with adult Actinobacillus

  15. Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Amoxicillin Trihydrate.

    NARCIS (Netherlands)

    Thambavita, Dhanusha; Galappatthy, Priyadarshani; Mannapperuma, Uthpali; Jayakody, Lal; Cristofoletti, Rodrigo; Abrahamsson, Bertil; Groot, Dirk W; Langguth, Peter; Mehta, Mehul; Parr, Alan; Polli, James E; Shah, Vinod P; Dressman, Jennifer

    2017-01-01

    Literature and experimental data relevant to waiver of in vivo bioequivalence (BE) testing for the approval of immediate-release solid oral dosage forms containing amoxicillin trihydrate are reviewed. Solubility and permeability characteristics according to the Biopharmaceutics Classification System

  16. Preparation and characterization of poly (ethersulfone) nanofiltration membranes for amoxicillin removal from contaminated water.

    Science.gov (United States)

    Omidvar, Maryam; Mousavi, Seyed Mahmoud; Soltanieh, Mohammad; Safekordi, Ali Akbar

    2014-01-08

    Nowadays, antibiotics such as amoxicillin have been entered in water bodies. Nanofiltration has been proposed as an attractive technology for removal of antibiotics from aquatic environment instead of conventional wastewater treatment. In this paper, novel asymmetric flat sheet nanofiltration membranes were prepared via immersion precipitation technique and by using the poly(ethersulfone)/Brij®S100/Poly(vinylpirrolidone)/1-methyl-2-pyrolidone casting solutions. The effect of addition of Brij®S100 as a non-ionic surfactant additive as well as concentration of poly (ethersulfone) on morphology, wettability, pure water flux and rejection of amoxicillin were studied using the scanning electron microscopy, water contact angle apparatus and experimental set-up. The results indicated that the addition of Brij®S100 to the casting solutions resulted in the formation of membranes with higher hydrophilicity and relatively noticeable rejection of amoxicillin up to 99% in comparison with unmodified poly(ethersulfone) membrane. Contrary to amoxicillin rejection, pure water flux was decreased when higher poly(ethersulfone) concentration was employed.

  17. Normal boundary intersection applied as multivariate and multiobjective optimization in the treatment of amoxicillin synthetic solution.

    Science.gov (United States)

    Moura, Deberton; Barcelos, Vithor; Samanamud, Gisella Rossana Lamas; França, Alexandre Boscaro; Lofrano, Renata; Loures, Carla Cristina Almeida; Naves, Luzia Lima Rezende; Amaral, Mateus Souza; Naves, Fabiano Luiz

    2018-02-14

    Amoxicillin is a useful antibiotic to combat bacterial infections. However, this drug can cause serious problems when discarded in waterways due to its great bioaccumulation potential. This compound can be treated via advanced oxidation processes (AOPs), which are capable of converting amoxicillin into carbon dioxide and water. In this context, the use of ozone as an oxidizer has excelled in amoxicillin degradation. This paper aims at treating a synthetic solution of amoxicillin (0.1 g L -1 ) in a reactor with ozone bubbling. A Design of Experiment (DoE) with a response surface known as Central Composite Design (CCD) was used to optimize the treatment process. In addition, a Normal Boundary Intersection (NBI) method was used in the construction of a Pareto boundary chart. Results after 1-h treatment showed a reduction of 53% of the initial organic matter from a designed model using factors, such as pH, ozone generator power, and O 3 flow. A model was built from the CCD with score of 0.9929. Thus, the model was able to represent the real scenario with confidence.

  18. Targeted Delivery of Amoxicillin to C. trachomatis by the Transferrin Iron Acquisition Pathway.

    Science.gov (United States)

    Hai, Jun; Serradji, Nawal; Mouton, Ludovic; Redeker, Virginie; Cornu, David; El Hage Chahine, Jean-Michel; Verbeke, Philippe; Hémadi, Miryana

    2016-01-01

    Weak intracellular penetration of antibiotics makes some infections difficult to treat. The Trojan horse strategy for targeted drug delivery is among the interesting routes being explored to overcome this therapeutic difficulty. Chlamydia trachomatis, as an obligate intracellular human pathogen, is responsible for both trachoma and sexually transmitted diseases. Chlamydia develops in a vacuole and is therefore protected by four membranes (plasma membrane, bacterial inclusion membrane, and bacterial membranes). In this work, the iron-transport protein, human serum-transferrin, was used as a Trojan horse for antibiotic delivery into the bacterial vacuole. Amoxicillin was grafted onto transferrin. The transferrin-amoxicillin construct was characterized by mass spectrometry and absorption spectroscopy. Its affinity for transferrin receptor 1, determined by fluorescence emission titration [KaffTf-amox = (1.3 ± 1.0) x 108], is very close to that of transferrin [4.3 x 108]. Transmission electron and confocal microscopies showed a co-localization of transferrin with the bacteria in the vacuole and were also used to evaluate the antibiotic capability of the construct. It is significantly more effective than amoxicillin alone. These promising results demonstrate targeted delivery of amoxicillin to suppress Chlamydia and are of interest for Chlamydiaceae and maybe other intracellular bacteria therapies.

  19. Amoxicillin rash in patients with infectious mononucleosis: evidence of true drug sensitization.

    Science.gov (United States)

    Ónodi-Nagy, Katinka; Kinyó, Ágnes; Meszes, Angéla; Garaczi, Edina; Kemény, Lajos; Bata-Csörgő, Zsuzsanna

    2015-01-01

    It hasn't been clearly understood yet whether sensitization to antibiotics, the virus itself or transient loss of drug tolerance due to the virus, is responsible for the development of maculopapular exanthems following amoxicillin intake in patients with infectious mononucleosis. We aimed to examine whether sensitization to penicillin developed among patients with skin rash following amoxicillin treatment within infectious mononucleosis. Ten patients were investigated for drug sensitization by lymphocyte transformation test and six patients were further tested by prick-, intradermal and patch tests employing the penicillin's main antigens. Lymphocyte transformation test showed negative results with amoxicillin, while one patient had positive reaction to cefixime. Six patients with suspected sensitization to amoxicillin were then investigated by in vivo tests. Prick tests were negative in all six patients, but the intradermal tests showed positive reactions in four patients. Our data demonstrate that in vitro testing is not sensitive enough in determining drug sensitization to penicillin. In vivo tests should be performed to detect sensitization and indeed with skin tests our results confirmed that sensitization to aminopenicillin may develop within infectious mononucleosis.

  20. Pharmacokinetics of amoxicillin/clavulanic acid combination after intravenous and intramuscular administration to pigeons.

    Science.gov (United States)

    Escudero, E; Vicente, M S; Carceles, C M

    1998-01-01

    The pharmacokinetics of amoxicillin/clavulanic acid (4:1) combination were studied after intravenous and intramuscular administration of single doses (25 mg kg(-1) bodyweight) to 50 pigeons. The plasma concentrations-time data were analysed by compartmental pharmacokinetics and non-compartmental methods. The disposition curves for both drugs after intravenous administration were best described by a two-compartment open model. The apparent volumes of distribution of amoxicillin and clavulanic acid were 1.77 litres kg(-1) and 1.30 litres kg(-1) respectively. The body clearances of amoxicillin and clavulanic acid were not significantly different. The elimination half-lives of amoxicillin after intravenous and intramuscular administration were 1.22 (0.09) hour and 1.52 (0.09) hour respectively, and those of clavulanic acid were 1.15 (0.08) hour and 1.49 (0.08) hour. After intramuscular administration both drugs had a significantly longer half-life (P or =0.5 mg litre(-1) (minimum inhibitory concentration of most susceptible pathogens).

  1. Sonographic Appearance of Dermal and Subcutaneous Sarcoidosis: A Case Report

    Energy Technology Data Exchange (ETDEWEB)

    Jang, Ja Yoon; Bae, Young A; Hong, Hyeok Jin; Kwon, Kye Won [Dept. of Radiology, Bundang Jesaeng General Hospital, Seongnam (Korea, Republic of)

    2012-08-15

    Sarcoidosis is a systemic granulomatous disease of unknown origin that mainly involves lung and skin, but rarely involves subcutaneous tissue. While some studies have reported on CT or MR imaging findings of subcutaneous sarcoidosis, there is only one report on sonographic findings of subcutaneous sarcoidosis, recently published in the US. Familiarity with ultrasonographic findings of subcutaneous sarcoidosis might be helpful for the early diagnosis in patient with palpable nodules and image follow-up for subcutaneous sarcoidosis. Here we report on the sonographic appearance of subcutaneous sarcoidosis involving dermal and subcutaneous tissue over axilla and sole, a case diagnosed as sarcoidosis and improved by steroid treatment, along with a review of the relevant literature.

  2. Design of Controlled Release Non-erodible Polymeric Matrix Tablet Using Microwave Oven-assisted Sintering Technique.

    Science.gov (United States)

    Patel, Dm; Patel, Bk; Patel, Ha; Patel, Cn

    2011-07-01

    The objective of the present study was to evaluate the effect of sintering condition on matrix formation and subsequent drug release from polymer matrix tablet for controlled release. The present study highlights the use of a microwave oven for the sintering process in order to achieve more uniform heat distribution with reduction in time required for sintering. We could achieve effective sintering within 8 min which is very less compared to conventional hot air oven sintering. The tablets containing the drug (propranolol hydrochloride) and sintering polymer (eudragit S-100) were prepared and kept in a microwave oven at 540 watt, 720 watt and 900 watt power for different time periods for sintering. The sintered tablets were evaluated for various tablet characteristics including dissolution study. Tablets sintered at 900 watt power for 8 min gave better dissolution profile compared to others. We conclude that microwave oven sintering is better than conventional hot air oven sintering process in preparation of controlled release tablets.

  3. Reaction-Multi Diffusion Model for Nutrient Release and Autocatalytic Degradation of PLA-Coated Controlled-Release Fertilizer

    Directory of Open Access Journals (Sweden)

    Sayed Ameenuddin Irfan

    2017-03-01

    Full Text Available A mathematical model for the reaction-diffusion equation is developed to describe the nutrient release profiles and degradation of poly(lactic acid (PLA-coated controlled-release fertilizer. A multi-diffusion model that consists of coupled partial differential equations is used to study the diffusion and chemical reaction (autocatalytic degradation simultaneously. The model is solved using an analytical-numerical method. Firstly, the model equation is transformed using the Laplace transformation as the Laplace transform cannot be inverted analytically. Numerical inversion of the Laplace transform is used by employing the Zakian method. The solution is useful in predicting the nutrient release profiles at various diffusivity, concentration of extraction medium, and reaction rates. It also helps in explaining the transformation of autocatalytic concentration in the coating material for various reaction rates, times of reaction, and reaction-multi diffusion. The solution is also applicable to the other biodegradable polymer-coated controlled-release fertilizers.

  4. Long-term and controlled release of chlorhexidine-copper(II) from organically modified montmorillonite (OMMT) nanocomposites

    Energy Technology Data Exchange (ETDEWEB)

    Wu, Yue [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210097 (China); Jiangsu Engineering Research Center for Biomedical Function Materials, Nanjing Normal University, Nanjing 210097 (China); Zhou, Ninglin, E-mail: zhouninglin@njnu.edu.cn [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210097 (China); Jiangsu Engineering Research Center for Biomedical Function Materials, Nanjing Normal University, Nanjing 210097 (China); Jiangsu Technological Research Center for Interfacial Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093 (China); Li, Wenhao; Gu, Hao; Fan, Yunting [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210097 (China); Jiangsu Engineering Research Center for Biomedical Function Materials, Nanjing Normal University, Nanjing 210097 (China); Yuan, Jiang, E-mail: bioalchem@yahoo.com [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210097 (China); Jiangsu Engineering Research Center for Biomedical Function Materials, Nanjing Normal University, Nanjing 210097 (China); Jiangsu Technological Research Center for Interfacial Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093 (China)

    2013-03-01

    Drug/metal ion complexes exhibit improved antimicrobial activity and intercalating the above complexes into the interlayer of clay endows a long-term and controlled-release behavior. In this study, chlorhexidine was first complexed with copper (II) ion and then intercalated into the interlayer of MMT to form chlorhexidine-copper (II)/montmorillonite (CHX-Cu/MMT) nanocomposites. The nanocomposites were characterized with Fourier transform infrared (FT-IR), X-ray diffraction (XRD) and thermogravimetric analysis (TGA). A nearly lateral-monolayer arrangement of CHX-Cu was supposed for the intercalation. Release kinetics indicated that the release process satisfied a pseudo-second-order mode. The antibacterial results showed that the CHX-Cu/MMT composites had long-term and controlled-release behavior. - Graphical abstract: The antibacterial agent of chlorhexidine was first complexed with copper(II) chloride and then intercalated into the interlayer of MMT to form nanocomposites. The CHX-Cu/MMT composites exhibited long-term antibacterial activity and controlled release behaviors. Highlights: Black-Right-Pointing-Pointer Chlorhexidine-copper (II)/montmorillonite (CHX-Cu/MMT) complex exhibits improved antimicrobial activity. Black-Right-Pointing-Pointer Intercalating chlorhexidine-copper (II) complex into the interlayer of clay endows a long-term and controlled-release. Black-Right-Pointing-Pointer Release kinetics indicated that the release process satisfied a pseudo-second-order mode. Black-Right-Pointing-Pointer A nearly lateral-monolayer arrangement of CHX-Cu was supposed for the intercalation.

  5. Photodegradation of amoxicillin by catalyzed Fe3+/H2O2 process.

    Science.gov (United States)

    Li, Xiaoming; Shen, Tingting; Wang, Dongbo; Yue, Xiu; Liu, Xian; Yang, Qi; Cao, Jianbin; Zheng, Wei; Zeng, Guangming

    2012-01-01

    Three oxidation processes of UV-Fe3+(EDTA)/H2O2 (UV: ultraviolet light; EDTA: ethylenediaminetetraacetic acid), UV-Fe3+/H2O2 and Fe3+/H2O2 were simultaneously investigated for the degradation of amoxicillin at pH 7.0. The results indicated that, 100% amoxicillin degradation and 81.9% chemical oxygen demand (COD(Cr)) removal could be achieved in the UV-Fe3+ (EDTA)/H2O2 process. The treatment efficiency of amoxicillin and COD(Cr) removal were found to decrease to 59.0% and 43.0% in the UV-Fe3+/H2O2 process; 39.6% and 31.3% in the Fe3+/H2O2 process. Moreover, the results of biodegradability (biological oxygen demand (BOD5)/COD(Cr) ratio) revealed that the UV-Fe3+ (EDTA)/H2O2 process was a promising strategy to degrade amoxicillin as the biodegradability of the effluent was improved to 0.45, compared with the cases of UV-Fe3+/H2O2 (0.25) and Fe3+/H2O2 (0.10) processes. Therefore, it could be deduced that EDTA and UV light performed synergetic catalytic effect on the Fe3+/H2O2 process, enhancing the treatment efficiency. The degradation mechanisms were also investigated via UV-Vis spectra, and high performance liquid chromatography-mass spectra. The degradation pathway of amoxicillin was further proposed.

  6. The efficacy of amoxicillin sodium against streptococcosis in cultured olive flounder Paralichthys olivaceus and its pharmacokinetics.

    Science.gov (United States)

    Lim, J-W; Jung, M-H; Jung, S-J; Kim, D-H; Park, K H; Kang, S Y

    2017-01-01

    The efficacy of amoxicillin sodium for controlling field and experimental Streptococcus iniae and S. parauberis infections in olive flounder (Paralichthys olivaceus) was evaluated after a single intramuscular administration. Furthermore, the minimal inhibitory concentrations (MIC) against 21 Streptococcus strains were determined. In addition, the pharmacokinetics and residue depletion in olive flounder were investigated. Single intramuscular doses of amoxicillin sodium at 20, 40, 80, and 160 mg/kg b.w. fish significantly reduced cumulative mortality rates to 18.8-31.3% (P amoxicillin sodium reduced the cumulative mortality rate to 7.5% and 4.8% at 20 and 40 mg/kg b.w. fish, respectively, whereas that of the untreated control group was 35.2%. Peak plasma concentrations (Cmax ) following a single intramuscular dose of 40 and 80 mg/kg b.w. fish were 62.64 (Tmax , 1.59 h) and 87.61 (Tmax , 3.02 h) μg/mL, respectively, with large AUC0-t /MIC and Cmax /MIC ratios, and sufficient T > MIC (time for maintaining plasma drug concentration greater than MICs) for S. iniae and S. parauberis. The estimated withdrawal period of amoxicillin sodium from muscle of olive flounder was about 8 days at 40 mg/kg b.w. fish (at 22 ± 1 °C). These results demonstrated a single intramuscular administration of amoxicillin sodium to be effective against streptococcosis in olive flounder. © 2016 John Wiley & Sons Ltd.

  7. Clarithromycin vs. amoxicillin suspensions in the treatment of pediatric patients with acute otitis media.

    Science.gov (United States)

    Pukander, J S; Jero, J P; Kaprio, E A; Sorri, M J

    1993-12-01

    Clarithromycin is a new macrolide antibiotic that is active in vitro against a variety of organisms that are responsible for acute otitis media in children. The parent compound is metabolized to microbiologically active 14-hydroxy clarithromycin, which is especially active against Haemophilus influenzae. The safety and efficacy of clarithromycin and amoxicillin suspensions were compared in the treatment of acute otitis media in children 1 to 12 years of age inclusive. This was a Phase III, single blind (investigator-blind), randomized, multicenter clinical trial. Clarithromycin oral suspension was given in a dose of 7.5 mg/kg (maximum, 500 mg) twice daily, and amoxicillin suspension in a dose of 20 mg/kg (maximum, 750 mg) was given twice daily for 7 to 10 days in a 1:1 ratio. Clinical evaluations were performed pretreatment, within 48 hours posttreatment and 10 to 14 days posttreatment. Myringotomy was performed in every child to obtain a microbiologic sample pretreatment and at subsequent visits as clinically indicated. A total of 79 children were enrolled, 39 in the clarithromycin and 40 in the amoxicillin treatment group. Thirty-two children were excluded from the efficacy analysis for various reasons. Clinical success (cure and improvement) rates at 0 to 4 days posttreatment were 93% for clarithromycin and 90% for amoxicillin (P > 0.999). Altogether 17 children (10 receiving clarithromycin, 7 receiving amoxicillin) experienced some adverse event, with gastrointestinal disorders being the most common complaint. No clinically significant differences in laboratory tests were found between the groups.(ABSTRACT TRUNCATED AT 250 WORDS)

  8. Biochar Production from Domestic Sludge: A Cost-effective, Recycled Product for Removal of Amoxicillin in Wastewater

    Science.gov (United States)

    Arun, Sija; Kothari, Kaushal; Mazumdar, Debayan; Mukhopadhyay, Moitraiyee; Chakraborty, Paromita

    2017-08-01

    Due to the broad spectrum, antimicrobial activity, Amoxicillin is one of the extensively used antibiotics. Amoxicillin ends up in the wastewater stream by direct or indirect disposal pathways which ultimately affect the aquatic ecosystem. Conventional wastewater treatment plant cannot remove it completely. Hence our objective was to produce sludge derived biochar and use it as an adsorbent for removal of amoxicillin. Effective biochar was obtained at 300°C produced from the sludge of the domestic wastewater treatment plant. 100 ppm amoxicillin solution spiked in biochar was kept for 180 mins in an orbital shaker and every 30 minutes the filtrate was checked in UV spectrophotometer. A steady decreasing gradient was obtained for absorbance of amoxicillin after 30 minutes. Further scanning electron microscopy showed significant morphological change in biochar obtained before and after spiking amoxicillin. Our preliminary assessment suggests that biochar can be exploited as an effective treatment technique to remove amoxicillin from wastewater. Moreover, we suggest that utilization of domestic sludge for commercial application in treatment plants can reduce the load of domestic waste in the open dumpsites.

  9. Growth, microcystin-production and proteomic responses of Microcystis aeruginosa under long-term exposure to amoxicillin.

    Science.gov (United States)

    Liu, Ying; Chen, Shi; Zhang, Jian; Gao, Baoyu

    2016-04-15

    Ecological risk of antibiotics due to the induction of antibiotic-resistant bacteria has been widely investigated, while studies on the hazard of antibiotic contaminants via the regulation of cyanobacteria were still limited. This study focused on the long-term action effect and mechanism of amoxicillin (a broadly used antibiotic) in Microcystis aeruginosa at environmentally relevant concentrations through 30 days of semi-continuous culture. Amoxicillin stimulated the photosynthesis activity and the production of microcystins, and interaction of differential proteins under amoxicillin exposure further manifested the close correlation between the two processes. D1 protein, ATP synthase subunits alpha and beta, enolase, triosephosphate isomerase and phosphoglycerate kinase were candidate target positions of amoxicillin in M. aeruginosa under long-term exposure. Amoxicillin affected the cellular biosynthesis process and the metabolism of carbohydrate and nucleoside phosphate according to the proteomic responses. Under exposure to amoxicillin, stimulated growth rate at the beginning phase and increased production and release of microcystins during the whole exposure period would lead to a higher contamination of M. aeruginosa cells and microcystins, indicating that amoxicillin was harmful to aquatic environments through the promotion of cyanobacterial bloom. Copyright © 2016 Elsevier Ltd. All rights reserved.

  10. Substitutions in penicillin-binding protein 1 in amoxicillin-resistant Helicobacter pylori strains isolated from Korean patients.

    Science.gov (United States)

    Kim, Beom Jin; Kim, Jae G

    2013-11-01

    A worldwide increase in amoxicillin resistance in Helicobacter pylori is having an adverse effect on eradication therapy. In this study, we investigated the mechanism of the amoxicillin resistance of H. pylori in terms of amino acid substitutions in penicillin-binding protein 1 (PBP1). In total, 150 H. pylori strains were isolated from 144 patients with chronic gastritis, peptic ulcers, or stomach cancer. The minimum inhibitory concentrations (MICs) of the strains were determined with a serial 2-fold agar dilution method. The resistance breakpoint for amoxicillin was defined as >0.5 µg/mL. Nine of 150 H. pylori strains showed amoxicillin resistance (6%). The MIC values of the resistant strains ranged from 1 to 4 µg/mL. A PBP1 sequence analysis of the resistant strains revealed multiple amino acid substitutions: Val16→Ile, Val45→Ile, Ser414→Arg, Asn562→Tyr, Thr593→Ala, Gly595→Ser, and Ala599→Thr. The natural transformation of these mutated genes into amoxicillin-sensitive strains was performed in two separate pbp1 gene segments. A moderate increase in the amoxicillin MIC was observed in the segment that contained the penicillin-binding motif of the C-terminal portion, the transpeptidase domain. pbp1 mutation affects the amoxicillin resistance of H. pylori through the transfer of the penicillin-binding motif.

  11. A biodegradable device for the controlled release of Piper nigrum (Piperaceae) standardized extract to control Aedes aegypti (Diptera, Culicidae) larvae.

    Science.gov (United States)

    Custódio, Kauê Muller; Oliveira, Joice Guilherme de; Moterle, Diego; Zepon, Karine Modolon; Prophiro, Josiane Somariva; Kanis, Luiz Alberto

    2016-01-01

    The significant increase in dengue, Zika, and chikungunya and the resistance of the Aedes aegypti mosquito to major insecticides emphasize the importance of studying alternatives to control this vector. The aim of this study was to develop a controlled-release device containing Piper nigrum extract and to study its larvicidal activity against Aedes aegypti. Piper nigrum extract was produced by maceration, standardized in piperine, and incorporated into cotton threads, which were inserted into hydrogel cylinders manufactured by the extrusion of carrageenan and carob. The piperine content of the extract and thread reservoirs was quantified by chromatography. The release profile from the device was assessed in aqueous medium and the larvicidal and residual activities of the standardized extract as well as of the controlled-release device were examined in Aedes aegypti larvae. The standardized extract contained 580mg/g of piperine and an LC50 value of 5.35ppm (24h) and the 3 cm thread reservoirs contained 13.83 ± 1.81mg of piperine. The device showed zero-order release of piperine for 16 days. The P. nigrum extract (25ppm) showed maximum residual larvicidal activity for 10 days, decreasing progressively thereafter. The device had a residual larvicidal activity for up to 37 days. The device provided controlled release of Piper nigrum extract with residual activity for 37 days. The device is easy to manufacture and may represent an effective alternative for the control of Aedes aegypti larvae in small water containers.

  12. The biopharmaceutics of successful controlled release drug product: Segmental-dependent permeability of glipizide vs. metoprolol throughout the intestinal tract.

    Science.gov (United States)

    Zur, Moran; Cohen, Noa; Agbaria, Riad; Dahan, Arik

    2015-07-15

    The purpose of this work was to study the challenges and prospects of regional-dependent absorption in a controlled-release scenario, through the oral biopharmaceutics of the sulfonylurea antidiabetic drug glipizide. The BCS solubility class of glipizide was determined, and its physicochemical properties and intestinal permeability were thoroughly investigated, both in-vitro (PAMPA and Caco-2) and in-vivo in rats. Metoprolol was used as the low/high permeability class boundary marker. Glipizide was found to be a low-solubility compound. All intestinal permeability experimental methods revealed similar trend; a mirror image small intestinal permeability with opposite regional/pH-dependency was obtained, a downward trend for glipizide, and an upward trend for metoprolol. Yet the lowest permeability of glipizide (terminal Ileum) was comparable to the lowest permeability of metoprolol (proximal jejunum). At the colon, similar permeability was evident for glipizide and metoprolol, that was higher than metoprolol's jejunal permeability. We present an analysis that identifies metoprolol's jejunal permeability as the low/high permeability class benchmark anywhere throughout the intestinal tract; we show that the permeability of both glipizide and metoprolol matches/exceeds this threshold throughout the entire intestinal tract, accounting for their success as controlled-release dosage form. This represents a key biopharmaceutical characteristic for a successful controlled-release dosage form. Copyright © 2015 Elsevier B.V. All rights reserved.

  13. Water-based polyurethane 3D printed scaffolds with controlled release function for customized cartilage tissue engineering.

    Science.gov (United States)

    Hung, Kun-Che; Tseng, Ching-Shiow; Dai, Lien-Guo; Hsu, Shan-hui

    2016-03-01

    Conventional 3D printing may not readily incorporate bioactive ingredients for controlled release because the process often involves the use of heat, organic solvent, or crosslinkers that reduce the bioactivity of the ingredients. Water-based 3D printing materials with controlled bioactivity for customized cartilage tissue engineering is developed in this study. The printing ink contains the water dispersion of synthetic biodegradable polyurethane (PU) elastic nanoparticles, hyaluronan, and bioactive ingredients TGFβ3 or a small molecule drug Y27632 to replace TGFβ3. Compliant scaffolds are printed from the ink at low temperature. These scaffolds promote the self-aggregation of mesenchymal stem cells (MSCs) and, with timely release of the bioactive ingredients, induce the chondrogenic differentiation of MSCs and produce matrix for cartilage repair. Moreover, the growth factor-free controlled release design may prevent cartilage hypertrophy. Rabbit knee implantation supports the potential of the novel 3D printing scaffolds in cartilage regeneration. We consider that the 3D printing composite scaffolds with controlled release bioactivity may have potential in customized tissue engineering. Copyright © 2016 Elsevier Ltd. All rights reserved.

  14. Biomimetic synthesized nanoporous silica@poly(ethyleneimine)s xerogel as drug carrier: characteristics and controlled release effect.

    Science.gov (United States)

    Li, Jing; Xu, Lu; Liu, Hongzhuo; Wang, Yan; Wang, Qifang; Chen, Hongtao; Pan, Weisan; Li, Sanming

    2014-06-05

    The purpose of this study was to prepare and characterize nanoporous silica@poly(ethyleneimine)s (NS@P) xerogel and methanol modified NS@P xerogel synthesized with biomimetic method, and investigate controlled release behavior of propranolol hydrochloride (PNH) loaded carrier materials in vitro and in vivo. Preparation was conducted at ambient conditions, and NS@P xerogel as well as PNH loaded NS@P xerogel were characterized using Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD) and differential scanning calorimeter (DSC). Investigations on morphology and porous characteristics of NS@P xerogel and methanol modified NS@P xerogel were evaluated with scanning electron microscopy (SEM), transmission electron microscopy (TEM) and nitrogen adsorption. The results showed that the order of morphology compactness was NS@P xerogel>25%NS@P xerogel>75%NS@P xerogel because PEIs scaffold ability for silica condensation and forming hydrogen bond weakened with increasing volume ratio of methanol modification. Moreover, SBET decreased and uniformity of pore size distribution was interrupted after methanol modification. PNH loaded carrier materials displayed controlled release, and release effect was related with pore size of materials and PEIs scaffold ability. In vivo pharmacokinetic study demonstrated that release of PNH was delayed due to the PNH incorporated inside carrier materials and controlled release effect was in accordance with in vitro results. Copyright © 2014 Elsevier B.V. All rights reserved.

  15. FORMULATION AND IN VITRO STUDY OF PROPRANOLOL HYDROCHLORIDE CONTROLLED RELEASE FROM CARBOXYMETHYL CHITOSAN-BASED MATRIX TABLETS

    Directory of Open Access Journals (Sweden)

    Hernawan Hernawan

    2013-12-01

    Full Text Available Formulation and in vitro study of propranolol hydrochloride controlled release from carboxymethyl chitosan-based matrix tablets have been conducted. Formulations with various concentrations of carboxymethyl chitosan 2% (F1, 4% (F2, 6% (F3 were done by wet granulation method. Compatibility test was conducted by XRD and FTIR spectroscopy to determine interaction between propranolol hydrochloride and polymer excipients. Dissolution profiles was obtained through in vitro tests release using simulated gastric fluid (without enzymes, pH 1.2 for the first 2 h and followed by simulated intestinal fluid (phosphate buffer solution without enzyme, pH 7.2 for 2 h remaining. The dissolution profile of each formulation was fitted with five kinetics modeling of drug release (zero order, first order, Higuchi, Peppas-Korsmeyer, and Hixson-Crowell. The compatibility test results showed that formulation caused physical interactions between propranolol hydrochloride and polymer excipient but doesn't make crystallinity nature of propranolol hydrochloride disturbed even after formulation. Dissolution profiles of each formulation showed that controlled release of propranolol hydrochloride from the tablet followed Peppas-Korsmeyer model. It is concluded that carboxymethyl chitosan in appropriate proportions is suitable for formulating propranolol hydrochloride controlled release tablets which exhibit Peppas-Korsmeyer release kinetics.

  16. Controlled release matrix tablets of glipizide: Influence of different grades of ethocel and Co-excipient on drug release.

    Science.gov (United States)

    Mehsud, Saif Ullah; Khan, Gul Majid; Hussain, Abid; Akram, Muhammad; Akhlaq, Muhammad; Khan, Kamran Ahmad; Shakoor, Abdul

    2016-05-01

    The aim of the current study was to formulate and evaluate glipizide controlled release matrix tablets by means of different grades of polymer Ethoceland different co-excipients in order to evaluate their effect on drug release profiles during in vitro dissolution studies. Type II diabetes mellitus is usually treated with Glipizide. Glipizide belongs to sulfonylurea group. Gastric disturbance and severe hypoglycemia has been observed after taking glipizide orally. To overcome these problems, controlled release matrices were developed using different grades of ethyl cellulose polymer with a drug-polymer ratio of 1:3by the direct compression method. The effect on drug release of partial replacement of lactose by different co-excipients, HPMC K100M, starch and CMC, were also studied. Diameter, thickness, hardness, friability, weight variations, drug contents of formulations were tested, these properties were within prescribed limits. Co-excipients and polymer containing formulations were compared to the without co-excipients and polymer containing formulations with respect to their release profile. After a 24-hour release study, ethyl cellulose polymer containing formulation exhibited prolonged release for 5-16 hours; however the polymer Ethocel (R) standard FP 7 Premium without co-excipient containing formulation exhibited controlled release for 24 hours. Incompatibility was investigated between drugs, co-excipient DSC and polymer study was performed and any type of interaction was not found. Different kinetic models were used to study the release mechanism. An enhanced release rate was observed in case of excipients containing formulations.

  17. [Effect of controlled release fertilizer on nitrous oxide emission from paddy field under plastic film mulching cultivation].

    Science.gov (United States)

    Zhang, Yi; Lü, Shi-Hua; Ma, Jing; Xu, Hua; Yuan, Jiang; Dong, Yu-Jiao

    2014-03-01

    A field experiment was conducted to assess the effect of controlled release fertilizer on N2O emission in paddy field under plastic film mulching cultivation (PM) with water-saving irrigation. Results showed that in the rice growing season, cumulative N2O emissions from the plots applied with urea (PM+U) and with controlled release fertilizer (PM+CRF) were (38.2 +/- 4.4) and (21.5 +/- 5.2) mg N x m(-2), respectively. The N2O emission factors were 0.25% and 0.14% in the treatments PM+U and PM+CRF, respectively. The controlled release fertilizer decreased the total N2O emission by 43.6% compared with urea, of which 49.6% was reduced before the drying period. It also reduced the peak of N2O emission by 52.6%. However, it did not affect soil microbial biomass N and soil NH(4+)-N content at any rice growing stage, and grain yield either. No significant correlation was observed between N2O flux and soil Eh or soil temperature at the depth of 5 cm.

  18. Lack of pharmacokinetic bioequivalence between generic and branded amoxicillin formulations. A post-marketing clinical study on healthy volunteers

    Science.gov (United States)

    Del Tacca, Mario; Pasqualetti, Giuseppe; Di Paolo, Antonello; Virdis, Agostino; Massimetti, Gabriele; Gori, Giovanni; Versari, Daniele; Taddei, Stefano; Blandizzi, Corrado

    2009-01-01

    AIMS There are concerns about the quality of generic drugs in the postmarketing setting. The aim was to establish whether two generic formulations of amoxicillin, available on the Italian market, fulfil the criteria for clinical pharmacokinetic bioequivalence vs. the branded drug. METHODS Two generic amoxicillin products (generic A and B) were selected among four fast-release tablet formulations available on the Italian market. Twenty-four healthy adult volunteers of either sex participated to a single-dose, randomized, three-treatment, crossover, single-blind bioequivalence study designed to compare generic A and B with branded amoxicillin. Plasma samples were collected at preset times for 24 h after dosing, and assayed for amoxicillin levels by high-performance liquid chromatography. RESULTS Ninety percent confidence intervals of AUC ratios were 0.8238, 1.0502 (ratio 0.9302) and 0.8116, 1.1007 (ratio 0.9452) for generic A and B vs. branded amoxicillin, respectively. Ninety percent confidence intervals of Cmax ratios were 0.7921, 1.0134 (ratio 0.8960) and 0.8246, 1.1199 (ratio 0.9610) for generic A and B vs. branded amoxicillin, respectively. The mean pharmacokinetic profiles showed that the AUC value of branded amoxicillin was 8.5 and 5.4% greater than that estimated for generic A and B, respectively. Few adverse events were recorded; these were not serious and occurred without apparent relationship to any specific amoxicillin formulation. CONCLUSIONS These results indicate that one of the two marketed amoxicillin generics analysed in the present study is not bioequivalent to the brand leader product for Cmax on the basis of single-dose pharmacokinetic assessment. PMID:19660001

  19. Evaluation of the amoxicillin concentrations in amniotic fluid, placenta, umbilical cord blood and maternal serum two hours after intravenous administration.

    Science.gov (United States)

    Zareba-Szczudlik, Julia; Romejko-Wolniewicz, Ewa; Lewandowski, Zbigniew; Rozanska, Hanna; Malinowska-Polubiec, Aneta; Dobrowolska-Redo, Agnieszka; Wilczynski, Jan; Czajkowski, Krzysztof

    2016-10-01

    The aims of this study were to evaluate amoxicillin concentrations in amniotic fluid, placenta, umbilical cord blood and maternal blood two hours after intravenous administration to assess obstetric and non-obstetric factors that could have influences on the penetration of the antibiotic into the examined tissues and to analyze the sensitivity to amoxicillin of the most common pathogens isolated from the genital tract. A total of 35 full-term pregnant women who qualified for elective Caesarean delivery were included in the study. Amoxicillin at a dose of 1000 mg was administered prior to surgery. Amoxicillin levels were determined by diffusion microbial assay. The drug concentration was highest in umbilical cord blood compared with amniotic fluid, maternal blood and placenta (4.20±1.06 µg/g versus 3.96±0.79 µg/g, 3.22±0.64 µg/g and 2.81±0.64 µg/g, respectively). Obstetric and non-obstetric factors had no influence on the amoxicillin concentration. The most common bacteria isolated from the genital tracts of pregnant women (Streptococcus agalactiae, Enterococcus faecalis, Escherichia coli) were sensitive to amoxicillin. The MIC for the sensitive strain of Streptococcus agalactiae was seen in the majority of tissues of all of the patients; however, the MICs for E. faecalis and E. coli were not observed in any compartment. Amoxicillin proved to have good penetration into the fetal tissues and placenta after intravenous administration. The most common bacteria isolated from the genital tracts of pregnant women were sensitive to amoxicillin. Pregnancy complications were not found to have an influence on the amoxicillin concentrations in the examined tissues.

  20. Lack of pharmacokinetic bioequivalence between generic and branded amoxicillin formulations. A post-marketing clinical study on healthy volunteers.

    Science.gov (United States)

    Del Tacca, Mario; Pasqualetti, Giuseppe; Di Paolo, Antonello; Virdis, Agostino; Massimetti, Gabriele; Gori, Giovanni; Versari, Daniele; Taddei, Stefano; Blandizzi, Corrado

    2009-07-01

    There are concerns about the quality of generic drugs in the postmarketing setting. The aim was to establish whether two generic formulations of amoxicillin, available on the Italian market, fulfil the criteria for clinical pharmacokinetic bioequivalence vs. the branded drug. Two generic amoxicillin products (generic A and B) were selected among four fast-release tablet formulations available on the Italian market. Twenty-four healthy adult volunteers of either sex participated to a single-dose, randomized, three-treatment, crossover, single-blind bioequivalence study designed to compare generic A and B with branded amoxicillin. Plasma samples were collected at preset times for 24 h after dosing, and assayed for amoxicillin levels by high-performance liquid chromatography. Ninety percent confidence intervals of AUC ratios were 0.8238, 1.0502 (ratio 0.9302) and 0.8116, 1.1007 (ratio 0.9452) for generic A and B vs. branded amoxicillin, respectively. Ninety percent confidence intervals of C(max) ratios were 0.7921, 1.0134 (ratio 0.8960) and 0.8246, 1.1199 (ratio 0.9610) for generic A and B vs. branded amoxicillin, respectively. The mean pharmacokinetic profiles showed that the AUC value of branded amoxicillin was 8.5 and 5.4% greater than that estimated for generic A and B, respectively. Few adverse events were recorded; these were not serious and occurred without apparent relationship to any specific amoxicillin formulation. These results indicate that one of the two marketed amoxicillin generics analysed in the present study is not bioequivalent to the brand leader product for C(max) on the basis of single-dose pharmacokinetic assessment.

  1. Surgical management of subcutaneous Colletotrichum gloeosporioides

    Science.gov (United States)

    Allton, David R; Parvez, Najma; Ranganath, Sangeetha; Jinadatha, Chetan

    2015-01-01

    A 52-year-old male patient with a history of sarcoidosis and over 10 years of chronic low-dose glucocorticoid use, cirrhosis and type 2 diabetes mellitus presented with two painful, enlarging subcutaneous nodules ultimately identified as Colletotrichum gloeosporioides. Two attempts at needle aspiration of the larger nodule resulted in rapid reaccumulation. Complete surgical excision of both nodules resulted in complete resolution without the use of any concomitant antifungals. Patient had no recurrence at 2 years of follow-up. PMID:25737220

  2. Subcutaneous myiasis caused by Dermatobia hominis.

    Science.gov (United States)

    Logar, J; Beović, B; Triller, C; Rakovec, S

    2001-01-01

    A case of subcutaneous myiasis caused by the larvae of the Dermatobia hominis fly is described, involving the ankle region of a 25-y-old man who had returned from Peru. After removal of 4 larvae from the affected sites, the lesions healed in 2 weeks without further treatment. Because of the increasing number of people travelling to tropical America, physicians in Slovenia will have to consider Dermatobia myiasis in the differential diagnosis of furuncular lesions in patients with a relevant travel history.

  3. Switching between intravenous and subcutaneous trastuzumab

    DEFF Research Database (Denmark)

    Gligorov, Joseph; Curigliano, Giuseppe; Müller, Volkmar

    2017-01-01

    AIM: To assess the safety and tolerability of switching between subcutaneous (SC) and intravenous (IV) trastuzumab in the PrefHer study (NCT01401166). PATIENTS AND METHODS: Patients with HER2-positive early breast cancer completed (neo)adjuvant chemotherapy and were randomised to receive four....... Rates of clinically important events, including grade ≥3 AEs, serious AEs, AEs leading to study drug discontinuation and cardiac AEs, were low and similar between treatment arms (safety signals for trastuzumab were observed. CONCLUSIONS: PrefHer revealed...... that switching from IV to SC trastuzumab (hand-held syringe or SID) or vice versa did not impact the known safety profile of trastuzumab....

  4. Antifouling composites with self-adaptive controlled release based on an active compound intercalated into layered double hydroxides

    Science.gov (United States)

    Yang, Miaosen; Gu, Lianghua; Yang, Bin; Wang, Li; Sun, Zhiyong; Zheng, Jiyong; Zhang, Jinwei; Hou, Jian; Lin, Cunguo

    2017-12-01

    This paper reports a novel method to prepare the antifouling composites with properties of self-adaptive controlled release (defined as control the release rate autonomously and adaptively according to the change of environmental conditions) by intercalation of sodium paeonolsilate (PAS) into MgAl and ZnAl layered double hydroxide (LDH) with the molar ratio (M2+/M3+) of 2:1 and 3:1, respectively. The powder X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) confirm the intercalation of PAS into the galleries of LDH. The controlled release behavior triggered by temperature for the PAS-LDH composites has been investigated, and the results show that the release rate of all PAS-LDH composites increases as the increase of temperature. However, the MgAl-PAS-LDH composites (Mg2Al-PAS-LDH and Mg3Al-PAS-LDH) exhibit the increased release rate of 0.21 ppm/°C from 15 to 30 °C in 3.5% NaCl solution, more than three times of the ZnAl-PAS-LDH composites (0.06 ppm/°C), owing to the confined microenvironment influenced by metal types in LDH layers. In addition, a possible diffusion-controlled process with surface diffusion, bulk diffusion and heterogeneous flat surface diffusion has been revealed via fitting four kinetic equations. Moreover, to verify the practical application of the PAS-LDH composites, a model coating denoted as Mg2Al-PAS-LDH coating was fabricated. The release result displays that the release rate increases or decreases as temperature altered at 15 and 25 °C alternately, indicating its self-adaptive controlled release behavior with temperature. Moreover, the superior resistance to the settlement of Ulva spores at 15 and 25 °C was observed for the Mg2Al-PAS-LDH coating, as a result of the controllable release of antifoulant. Therefore, this work provides a facile and effective method for the fabrication of antifouling composites with self-adaptive controlled release behavior in response to temperature, which can be used to prolong

  5. Enhancing Vascularization through the Controlled Release of Platelet-Derived Growth Factor-BB.

    Science.gov (United States)

    Minardi, Silvia; Pandolfi, Laura; Taraballi, Francesca; Wang, Xin; De Rosa, Enrica; Mills, Zachary D; Liu, Xuewu; Ferrari, Mauro; Tasciotti, Ennio

    2017-05-03

    Using delivery systems to control the in vivo release of growth factors (GFs) for tissue engineering applications is extremely desirable as the clinical use of GFs is limited by their fast in vivo turnover. Hence, the development of effective platforms that are able to finely control the release of GFs in vivo remains a challenge. Herein, we investigated the ability of multiscale microspheres, composed by a nanostructured silicon multistage vector (MSV) core and a poly(dl-lactide-co-glycolide) acid (PLGA) forming outer shell (PLGA-MSV), to release functional platelet-derived growth factor-BB (PDGF-BB) to induce in vivo localized neovascularization. The in vitro release of PDGF-BB was assessed by enzyme-linked immunosorbent assay (ELISA) over 2 weeks and showed a sustained, zero-order release kinetics. The ability to promote in vivo localized neovascularization was investigated in a subcutaneous injection model in BALB/c mice and followed by intravital microscopy up to 2 weeks. Fully functional newly formed vessels were found within the area where PLGA-MSVs were localized and covered 3.0 ± 0.9 and 19 ± 5.1% at 7 and 14 days, respectively, showing a 6-fold increase in 1 week. The distribution of CD31 + and α-SMA + cells was detected by immunofluorescence on harvested tissues. CD31 was significantly more expressed (4-fold increase) compared to the untreated control. Finally, the level of up-regulation of angiogenesis-associated genes (Vegfa, Vwf, and Col3a1) was assessed by q-PCR, resulting in a significantly higher expression where PLGA-MSVs were localized (Vegfa: 2.32 ± 0.50 at 7 days and 4.37 ± 0.75 at 14 days; Vwf: 4.13 ± 0.82 and 7.74 ± 0.91; Col3a1: 5.43 ± 0.37 and 6.66 ± 0.89). Altogether, our data supported the conclusion that the localized delivery of PDGF-BB from PLGA-MSVs induced the localized de novo formation of fully functional vessels in vivo. With this study, we demonstrated that PLGA-MSV holds promise for accomplishing the controlled

  6. Evaluation and comparison of in-vitro dissolution profiles for different brands of amoxicillin capsules.

    Science.gov (United States)

    Kassaye, L; Genete, G

    2013-06-01

    Amoxicillin is an oral semi-synthetic, β-lactam antibiotic used to treat bacterial infections caused by susceptible micro organisms. It is usually prepared in capsule, tablet and powder for oral suspension form. Solid dosage forms for oral administration pose bioavailability problems related to the absorption process The World Health Organization (WHO) has promoted the use of generic brands in order to make the cost of medicines affordable. Generic substitution could be considered when a generic copy of a reference drug contains identical amounts of the same active ingredient in the same dose formulation and route of administration. However, the presences of generic products those are not interchangeable with that of the innovator and/or with each others have been reported. To evaluate and compare the in-vitro dissolution profiles of different generic brands of amoxicillin capsules with the innovator that are available in Ethiopian market. Dissolution profiles for nine brands of amoxicillin capsules contained amoxicillin 500 mg which are available in Ethiopian market were determined using a method from the United States Pharmacopoeia (USP, 2009). The obtained dissolution profile data of the eight brands were evaluated and compared with the innovator brand (Amoxil™) using two different statistical methods: the fit factors (f1 & f2) and the dissolution efficiency (D.E.) model. Most generic brands of amoxicillin capsules (62.5% of the tested brands) are not interchangeable with the innovator brand. The calculated f1 factor for Brand A and Brand G are 10.1 and 1.1 respectively. However, for the rest six brands the f1 factors are greater than 15. The f2 factor for Brand G is 74.1 and for Brand A is 48.5 which is near to 50. Similarly, the f2 factors for the six brands are less than 50 which support the result of the f1 factors for the dissimilarity of these brands with the innovator brand. The mean dissolution efficiencies as well as the 95% confidence intervals are

  7. Synthesis of bio-based nanocomposites for controlled release of antimicrobial agents in food packaging

    Science.gov (United States)

    DeGruson, Min Liu

    The utilization of bio-based polymers as packaging materials has attracted great attention in both scientific and industrial areas due to the non-renewable and nondegradable nature of synthetic plastic packaging. Polyhydroxyalkanoate (PHA) is a biobased polymer with excellent film-forming and coating properties, but exhibits brittleness, insufficient gas barrier properties, and poor thermal stability. The overall goal of the project was to develop the polyhydroxyalkanoate-based bio-nanocomposite films modified by antimicrobial agents with improved mechanical and gas barrier properties, along with a controlled release rate of antimicrobial agents for the inhibition of foodborne pathogens and fungi in food. The ability for antimicrobial agents to intercalate into layered double hydroxides depended on the nature of the antimicrobial agents, such as size, spatial structure, and polarity, etc. Benzoate and gallate anions were successfully intercalated into LDH in the present study and different amounts of benzoate anion were loaded into LDH under different reaction conditions. Incorporation of nanoparticles showed no significant effect on mechanical properties of polyhydroxybutyrate (PHB) films, however, significantly increased the tensile strength and elongation at break of polyhydroxybutyrate-co-valerate (PHBV) films. The effects of type and concentration of LDH nanoparticles (unmodified LDH and LDH modified by sodium benzoate and sodium gallate) on structure and properties of PHBV films were then studied. The arrangement of LDH in the bio-nanocomposite matrices ranged from exfoliated to phase-separated depending on the type and concentration of LDH nanoparticles. Intercalated or partially exfoliated structures were obtained using modified LDH, however, only phase-separated structures were formed using unmodified LDH. The mechanical (tensile strength and elongation at break) and thermo-mechanical (storage modulus) properties were significantly improved with low

  8. The pharmacodynamic effect of amoxicillin and danofloxacin against Salmonella typhimurium in an in-vitro pharmacodynamic model

    DEFF Research Database (Denmark)

    Lindecrona, R.H.; Friis, C.; Aarestrup, Frank Møller

    2000-01-01

    The pharmacodynamic effect of amoxicillin and danofloxacin against two strains of Salmonella typhimurium was examined in an in-vitro pharmacodynamic model. For amoxicillin, peak concentrations of 1, 2 and 4 mu g ml(-1) and half-lives (t(1/2) of 3 and 15 hours were evaluated. For danofloxacin peak...... concentrations of 0.25, 0.50 and 1.50 mu g ml(-1) and half-lives of 7 and 15 hours were examined. For amoxicillin both the peak concentration and the half-life influenced the pharmacodynamic effect (P ... inhibitory concentration for 79 per cent or more of the dosing interval. The hires of the isolates increased when the amoxicillin concentrations were close to the nac during the first hours of exposure. For danofloxacin the pharmacodynamic effect was dependent on the peak concentration only (P

  9. Pharmacokinetics of amoxicillin/clavulanic acid combination and of both drugs alone after intravenous administration to goats.

    Science.gov (United States)

    Escudero, E; Carceles, C M; Vicente, S

    1996-09-01

    The pharmacokinetic behaviour of an amoxicillin/clavulanic acid combination (25 mg kg-1), and both drugs alone (amoxicillin 20 mg kg-1), clavulanic acid 5 mg kg-1), was studied after intravenous (i.v.) administration of single doses of 10 goats. The objective was to determine whether there were differences in the plasma kinetics of these drugs when administered in combination or alone. The plasma concentration-time data were analysed by compartmental pharmacokinetics and non-compartmental methods. The disposition curves for both drugs alone and in combination were best described by a biexponential equation (two-compartment open model). The elimination half-lives of amoxicillin were 1.05 +/- 0.09 h alone and 1.13 +/- 0.19 h in combination, and those of clavulanic acid were 0.87 +/- 0.07 h and 0.85 +/- 0.09 h, respectively. The apparent volumes of distribution of amoxicillin and clavulanic acid were similar in the two treatments. Body clearances of amoxicillin were 0.12 +/- 0.01 l h-1.kg alone and 0.11 +/- 0.01 l h-1.kg in combination, and of clavulanic acid were 0.12 +/- 0.02 l h-1.kg alone and 0.12 +/- 0.01 l h-1.kg in combination with amoxicillin. The half-lives and body clearances of amoxicillin and clavulanic acid did not differ significantly when administered alone and in combination. It was concluded that the i.v. administration of amoxicillin and clavulanic acid as a combination product did not alter the disposition kinetics of either drug.

  10. A biodegradable device for the controlled release of Piper nigrum (Piperaceae standardized extract to control Aedes aegypti (Diptera, Culicidae larvae

    Directory of Open Access Journals (Sweden)

    Kauê Muller Custódio

    Full Text Available Abstract: INTRODUCTION: The significant increase in dengue, Zika, and chikungunya and the resistance of the Aedes aegypti mosquito to major insecticides emphasize the importance of studying alternatives to control this vector. The aim of this study was to develop a controlled-release device containing Piper nigrum extract and to study its larvicidal activity against Aedes aegypti. METHODS: Piper nigrum extract was produced by maceration, standardized in piperine, and incorporated into cotton threads, which were inserted into hydrogel cylinders manufactured by the extrusion of carrageenan and carob. The piperine content of the extract and thread reservoirs was quantified by chromatography. The release profile from the device was assessed in aqueous medium and the larvicidal and residual activities of the standardized extract as well as of the controlled-release device were examined in Aedes aegypti larvae. RESULTS The standardized extract contained 580mg/g of piperine and an LC50 value of 5.35ppm (24h and the 3 cm thread reservoirs contained 13.83 ± 1.81mg of piperine. The device showed zero-order release of piperine for 16 days. The P. nigrum extract (25ppm showed maximum residual larvicidal activity for 10 days, decreasing progressively thereafter. The device had a residual larvicidal activity for up to 37 days. CONCLUSIONS: The device provided controlled release of Piper nigrum extract with residual activity for 37 days. The device is easy to manufacture and may represent an effective alternative for the control of Aedes aegypti larvae in small water containers.

  11. Effects of oxytetracycline, tylosin, and amoxicillin antibiotics on specific methanogenic activity of anaerobic biomass

    Directory of Open Access Journals (Sweden)

    Mohammad Mehdi Amin

    2012-01-01

    Materials and Methods: To evaluate the inhibitory antibiotics amoxicillin, tetracycline, and tylosin on biomass activity, specific methanogenic activity (SMA using anerobic biomass batch; into 120 ml vials: 30 ml biomass and 70 ml substrate including volatile fatty acids, mainly acetic acid and various concentrations of antibiotics were added. Methane gas production replacement through solution of KOH (2 N as an absorber of CO 2 and bromine thymol blue as indicator was measured. Each batch was tested for 10 days. Results: Based on the findings, inhibitory concentration of oxytetracycline, amoxicillin, and tylosin were 8000, 9000, and 9000 mg/L, respectively. Conclusions: This study showed that with increasing concentrations of antibiotics, the produced biogas volume from biomass per unit weight is decreased. COD removal was 42-82 % due to long retention time and adsorption to flocks.

  12. Impact of amoxicillin therapy on resistance selection in patients with community-acquired lower respiratory tract infections

    DEFF Research Database (Denmark)

    Malhotra-Kumar, Surbhi; Van Heirstraeten, Liesbet; Coenen, Samuel

    2016-01-01

    OBJECTIVES: To determine the effect of amoxicillin treatment on resistance selection in patients with community-acquired lower respiratory tract infections in a randomized, placebo-controlled trial. METHODS: Patients were prescribed amoxicillin 1 g, three times daily (n = 52) or placebo (n = 50......) for 7 days. Oropharyngeal swabs obtained before, within 48 h post-treatment and at 28-35 days were assessed for proportions of amoxicillin-resistant (ARS; amoxicillin MIC ≥2 mg/L) and -non-susceptible (ANS; MIC ≥0.5 mg/L) streptococci. Alterations in amoxicillin MICs and in penicillin......-binding-proteins were also investigated. ITT and PP analyses were conducted. RESULTS: ARS and ANS proportions increased 11- and 2.5-fold, respectively, within 48 h post-amoxicillin treatment compared with placebo [ARS mean increase (MI) 9.46, 95% CI 5.57-13.35; ANS MI 39.87, 95% CI 30.96-48.78; P 

  13. High dose amoxicillin-based first line regimen is equivalent to sequential therapy in the eradication of H. pylori infection.

    Science.gov (United States)

    Franceschi, F; Ojetti, V; Gabrielli, M; Petruzziello, C; Tortora, A; Gasbarrini, G; Lopetuso, L R; Scaldaferri, F; Gasbarrini, A

    2016-01-01

    Helicobater (H.) pylori eradication rates with standard first-line triple therapy have declined to unacceptable levels. To date, amoxicillin-resistant H. pylori strains have rarely been detected. Whether increasing the dosage of amoxicillin in a standard 7 days eradicating regimen may enhance its efficacy is not known. The aim of this paper is to compare the efficacy of a 7 days high-dose amoxicillin based first-line regimen with sequential therapy. We have retrospectively analyzed data from 300 sex and age matched patients, who underwent 3 different therapeutic schemes: (1) standard LCA, lansoprazole 30 mg bid, clarithromycin 500 mg bid and amoxicillin 1000 mg bid for 7 days; (2) high dose LCA (HD-LCA), lansoprazole 30 mg bid, clarithromycin 500 mg bid and amoxicillin 1000 mg tid for 7 days; (3) sequential LACT, lansoprazole 30 mg bid plus amoxicillin 1000 mg bid for 5 days, followed by lansoprazole 30 mg bid, clarithromycin 500 mg bid and tinidazole 500 mg bid for 5 days. Eradication was confirmed by 13C-urea breath test. Compliance and occurrence of adverse effects were also assessed. Eradication rates were: 55% for LCA, 75% for HD-LCA and 73% for LACT. Eradication rates were higher in HD-LCA group compared to LCA (pamoxicillin based eradicating treatment is superior to standard triple therapy and equivalent to sequential therapy; compared to the latter, the shorter duration may represent an advantage.

  14. Degradation of amoxicillin, ampicillin and cloxacillin antibiotics in aqueous solution by the UV/ZnO photocatalytic process

    Energy Technology Data Exchange (ETDEWEB)

    Elmolla, Emad S., E-mail: em_civil@yahoo.com [Dept. of Civil Engineering, Universiti Teknologi PETRONAS, Bandar Seri Iskandar, 31750 Tronoh, Perak (Malaysia); Chaudhuri, Malay [Dept. of Civil Engineering, Universiti Teknologi PETRONAS, Bandar Seri Iskandar, 31750 Tronoh, Perak (Malaysia)

    2010-01-15

    The study examined the effect of operating conditions (zinc oxide concentration, pH and irradiation time) of the UV/ZnO photocatalytic process on degradation of amoxicillin, ampicillin and cloxacillin in aqueous solution. pH has a great effect on amoxicillin, ampicillin and cloxacillin degradation. The optimum operating conditions for complete degradation of antibiotics in an aqueous solution containing 104, 105 and 103 mg/L amoxicillin, ampicillin and cloxacillin, respectively were: zinc oxide 0.5 g/L, irradiation time 180 min and pH 11. Under optimum operating conditions, complete degradation of amoxicillin, ampicillin and cloxacillin occurred and COD and DOC removal were 23.9 and 9.7%, respectively. The photocatalytic reactions under optimum conditions approximately followed a pseudo-first order kinetics with rate constant (k) 0.018, 0.015 and 0.029 min{sup -1} for amoxicillin, ampicillin and cloxacillin, respectively. UV/ZnO photocatalysis can be used for amoxicillin, ampicillin and cloxacillin degradation in aqueous solution.

  15. Impact of Sub-Inhibitory Concentrations of Amoxicillin on Streptococcus suis Capsule Gene Expression and Inflammatory Potential

    Directory of Open Access Journals (Sweden)

    Bruno Haas

    2016-04-01

    Full Text Available Streptococcus suis is an important swine pathogen and emerging zoonotic agent worldwide causing meningitis, endocarditis, arthritis and septicemia. Among the 29 serotypes identified to date, serotype 2 is mostly isolated from diseased pigs. Although several virulence mechanisms have been characterized in S. suis, the pathogenesis of S. suis infections remains only partially understood. This study focuses on the response of S. suis P1/7 to sub-inhibitory concentrations of amoxicillin. First, capsule expression was monitored by qRT-PCR when S. suis was cultivated in the presence of amoxicillin. Then, the pro-inflammatory potential of S. suis P1/7 culture supernatants or whole cells conditioned with amoxicillin was evaluated by monitoring the activation of the NF-κB pathway in monocytes and quantifying pro-inflammatory cytokines secreted by macrophages. It was found that amoxicillin decreased capsule expression in S. suis. Moreover, conditioning the bacterium with sub-inhibitory concentrations of amoxicillin caused an increased activation of the NF-κB pathway in monocytes following exposure to bacterial culture supernatants and to a lesser extent to whole bacterial cells. This was associated with an increased secretion of pro-inflammatory cytokines (CXCL8, IL-6, IL-1β by macrophages. This study identified a new mechanism by which S. suis may increase its inflammatory potential in the presence of sub-inhibitory concentrations of amoxicillin, a cell wall-active antibiotic, thus challenging its use for preventive treatments or as growth factor.

  16. Degradation of amoxicillin, ampicillin and cloxacillin antibiotics in aqueous solution by the UV/ZnO photocatalytic process.

    Science.gov (United States)

    Elmolla, Emad S; Chaudhuri, Malay

    2010-01-15

    The study examined the effect of operating conditions (zinc oxide concentration, pH and irradiation time) of the UV/ZnO photocatalytic process on degradation of amoxicillin, ampicillin and cloxacillin in aqueous solution. pH has a great effect on amoxicillin, ampicillin and cloxacillin degradation. The optimum operating conditions for complete degradation of antibiotics in an aqueous solution containing 104, 105 and 103 mg/L amoxicillin, ampicillin and cloxacillin, respectively were: zinc oxide 0.5 g/L, irradiation time 180 min and pH 11. Under optimum operating conditions, complete degradation of amoxicillin, ampicillin and cloxacillin occurred and COD and DOC removal were 23.9 and 9.7%, respectively. The photocatalytic reactions under optimum conditions approximately followed a pseudo-first order kinetics with rate constant (k) 0.018, 0.015 and 0.029 min(-1) for amoxicillin, ampicillin and cloxacillin, respectively. UV/ZnO photocatalysis can be used for amoxicillin, ampicillin and cloxacillin degradation in aqueous solution.

  17. [ANSYS simulation of subcutaneous pustule electrical characteristics].

    Science.gov (United States)

    Liu, Baohua; Wang, Xuan; Zhu, Honglian; Wang, Guoyong

    2011-12-01

    With the growing number of clinical surgery, post-operative surgical wound infection has become a very difficult clinical problem. In the treatments of it, non-invasive test of wound infection and healing status has a significance in clinical medicine practice. In this paper, beginning with the electrical properties of skin tissue structure and on the basis of the electromagnetism and the human anatomy, using the finite element analysis software, we applied safe voltage on the 3D skin model, performed the subcutaneous pustule simulation study and gained the relational curve between depth and radius of the pustule model. The simulation results suggested that the method we put forward could be feasible, and it could provide basis for non-invasive detection of wound healing and wound infection status.

  18. Relationship between the level of acquired resistance to gentamicin and synergism with amoxicillin in Enterococcus faecalis.

    Science.gov (United States)

    Aslangul, Elisabeth; Ruimy, Raymond; Chau, Françoise; Garry, Louis; Andremont, Antoine; Fantin, Bruno

    2005-10-01

    In enterococci, intrinsic low-level resistance to gentamicin does not abolish synergism with a cell wall-active antibiotic while high-level resistance due to acquired aminoglycoside-modifying enzymes does. To study the impact of intermediate levels of resistance to gentamicin (64 gentamicin at 128 microg/ml for G1-1477, 256 microg/ml for G2-1573, and 512 microg/ml for G3-1688. E. faecalis 102, which is highly resistant to gentamicin by enzymatic inactivation was used as control. In in vitro killing curves experiments, gentamicin concentrations allowing bactericidal activity and synergism in combination with amoxicillin increased from 4 microg/ml (1/16th the MIC), 16 microg/ml (one-eighth the MIC), 64 microg/ml (one-quarter the MIC), and 256 microg/ml (one-half the MIC) for strains JH2-2, G1-1477, G2-1573 and G3-1688, respectively. As expected, no bactericidal effect of the combination or synergism could be obtained with strain 102. In rabbits with aortic endocarditis caused by strain G1-1477 or G2-1573, combination therapy with amoxicillin and gentamicin was significantly more active than amoxicillin alone (P resistance to gentamicin was not associated with a loss of a beneficial effect of the gentamicin-amoxicillin combination in vivo even though higher concentrations of gentamicin were necessary to achieve in vitro synergism. Therefore, the use of an MIC of 500 microg/ml as a clinical cutoff limit to predict in vivo benefit of the combination remains a simple and effective tool.

  19. Epidemiological and Clinical Complexity of Amoxicillin-Clavulanate-Resistant Escherichia coli

    Science.gov (United States)

    Oteo, Jesús; Ortega, Adriana; Villar, Macarena; Conejo, M. Carmen; Bou, Germán; Aranzamendi-Zaldumbide, Maitane; Cercenado, Emilia; Gurguí, Mercè; Martínez-Martínez, Luis; Merino, María; Rivera, Alba; Oliver, Antonio; Weber, Irene; Pascual, Alvaro; Bartolomé, Rosa M.; Gónzalez-López, Juan José; Campos, José

    2013-01-01

    Two hundred twelve patients with colonization/infection due to amoxicillin-clavulanate (AMC)-resistant Escherichia coli were studied. OXA-1- and inhibitor-resistant TEM (IRT)-producing strains were associated with urinary tract infections, while OXA-1 producers and chromosomal AmpC hyperproducers were associated with bacteremic infections. AMC resistance in E. coli is a complex phenomenon with heterogeneous clinical implications. PMID:23637303

  20. Safely diagnosing clinically significant penicillin allergy using only penicilloyl-poly-lysine, penicillin, and oral amoxicillin.

    Science.gov (United States)

    Macy, Eric; Ngor, Eunis W

    2013-01-01

    Penicillin skin testing is rarely used to undiagnose penicillin "allergy" in the United States, partially because of concern that commercially available materials are inadequate. We determined whether skin testing with only commercially available penicilloyl-poly-lysine and penicillin followed by an oral amoxicillin challenge, if skin test-negative, can safely identify clinically significant penicillin allergy. Five hundred sequential persons with positive history of penicillin "allergy" were evaluated by skin testing with penicilloyl-poly-lysine and penicillin between June 8, 2010, and March 29, 2012. All persons with negative skin tests were given an oral amoxicillin challenge and observed for 1 hour. Persons undergoing penicillin allergy testing were representative of all health plan members with penicillin allergy. Only 4 persons (0.8%; 95% CI, 0.32%-2.03%) had a positive skin test result. Only 4 persons (0.8%; 95% CI, 0.32%-2.03%) had an acute objective oral amoxicillin challenge reaction. Fifteen persons (3.0%; 95% CI, 1.83%-4.98%) had subjective oral challenge reactions, either acute transient itching or dizziness. All were women and 11 (73.3%) had multiple drug intolerance syndrome. None had severe reactions or objective signs. These were not considered to be positive challenge reactions. Sixty-eight subjects (13.6%) who were negative on testing were exposed to 88 courses of penicillins during 90 days of follow-up. New reactions were reported after 4 courses (4.5%), 3 (75%) occurring in subjects with multiple drug intolerance syndrome. Penicillin skin testing, using only penicilloyl-poly-lysine and penicillin, followed by oral amoxicillin challenge, if negative, can safely identify clinically significant IgE-mediated penicillin allergy in patients who use health care in the United States at this time. Copyright © 2013 American Academy of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  1. Simulation of amoxicillin pharmacokinetics in humans for the prevention of streptococcal endocarditis in rats.

    OpenAIRE

    Fluckiger, U.; Moreillon, P.; Blaser, J.; Bickle, M.; Glauser, M P; Francioli, P.

    1994-01-01

    The pharmacokinetic determinants of successful antibiotic prophylaxis of endocarditis are not precisely known. Differences in half-lives of antibiotics between animals and humans preclude extrapolation of animal results to human situations. To overcome this limitation, we have mimicked in rats the amoxicillin kinetics in humans following a 3-g oral dose (as often used for prophylaxis of endocarditis) by delivering the drug through a computerized pump. Rats with catheter-induced vegetations we...

  2. High-dose extended-release lansoprazole (dexlansoprazole) and amoxicillin dual therapy for Helicobacter pylori infections.

    Science.gov (United States)

    Attumi, Taraq A; Graham, David Y

    2014-08-01

    Helicobacter pylori infections have become increasingly difficult to treat. To examine whether amoxicillin and high-dose dexlansoprazole would reliably achieve an H. pylori eradication rate of ≥90%. An open-label prospective pilot study of H. pylori eradication in treatment-naïve subjects with active H. pylori infection (positive by two tests). amoxicillin 1 g and dexlansoprazole 120 mg each twice a day at approximately 12-hour intervals for 14 days. Success was accessed by urea breath test. An effective therapy was defined as a per-protocol treatment success of 90% or greater; treatment success of 80% or less was prespecified as an unacceptable result. After 13 subjects were entered (12 men, one woman; average age of 54 years), the prespecified stopping rule of six treatment failures was achieved (i.e., the 95% confidence interval excluded achieving the required 90% success rate even if the proposed study of 50 completed patients were entered) and enrollment was stopped. Per-protocol and intention-to-treat treatment success were both 53.8%; (7/13); 95% CI = 25-80%. Compliance was 100%. Three patients (23%) reported side effects, all of which were mild and none interrupted therapy. Theoretically, dual PPI plus amoxicillin should reliably eradicate H. pylori provided nearly neutral intragastric pH can be maintained. Clearly, dexlansoprazole, despite being administered at high dose and twice a day (i.e., total daily dose 240 mg), failed to achieve an intragastric milieu consistent with dual PPI plus amoxicillin therapy being an effective anti-H. pylori regimen. © 2014 John Wiley & Sons Ltd.

  3. Purification and functionalization of nanodiamond to serve as a platform for amoxicillin delivery.

    Science.gov (United States)

    Rouhani, Parvaneh; Govindaraju, Nirmal; Iyer, Janaki K; Kaul, Rashmi; Kaul, Anil; Singh, Raj N

    2016-06-01

    Urinary tract infections (UTIs) cost $0.4-0.5 billion a year in the US and is the second most common disease affecting millions of people. As resistance to antibiotics becomes more common, a greater need for alternative treatments is needed. Nanodiamond particles (NDPs) are actively researched as drug delivery platforms due to their biocompatibility, particle size, and stable inert core. This research is aimed at developing NDPs as antibiotic drug delivery platforms for treating UTIs. To this end, 100 nm, 75 nm, 25 nm and 6 nm size NDPs are purified with acid and heat treatment techniques. Raman spectra of the NDPs showed that the acid treatment method resulted in higher diamond yield. Fourier transform infrared spectroscopy (FTIR) studies showed that both purification techniques result in oxygen terminated surface groups. Efficiency of loading amoxicillin on 25 nm NDPs based on electrostatic interaction of NDPs, functionalizing surfaces of NDPs with hydrogen, and polyethylenimine (PEI) are investigated. It is found that the electrostatic and surface hydrogenation approaches are not efficient in loading amoxicillin on the NDPs. On the other hand, PEI functionalized NDPs produced successful loading with amoxicillin as indicated by the presence of the β-lactam peak at 1770 cm(-1), amide peak at 1680 cm(-1), and bond between PEI NH stretching and amoxicillin -COOH group at 3650 cm(-1) by the FTIR spectra. These results are expected to lay the foundation for developing NDP based targeted drug delivery treatment techniques for treating UTIs and other infectious diseases. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. Specific mutations of penicillin-binding protein 1A in 77 clinically acquired amoxicillin-resistant Helicobacter pylori strains in comparison with 77 amoxicillin-susceptible strains.

    Science.gov (United States)

    Kwon, Yong Hwan; Kim, Ji Yeon; Kim, Nayoung; Park, Ji Hyun; Nam, Ryoung Hee; Lee, Sun Min; Kim, Jin-Wook; Kim, Jung Mogg; Park, Jong Youn; Lee, Dong Ho

    2017-08-25

    Amoxicillin (Amx) is one of the most important antibiotics for eradication of Helicobacter pylori (H. pylori). Main determinants of genetically stable Amx resistance are mutations in the C-terminus of penicillin-binding protein 1A (pbp1A). However, contribution of individual mutation remains unclear. 77 Amx-resistant (Amx(R) ) and 77 Amx-susceptible (Amx(S) ) H. pylori strains were isolated from gastric tissues, and DNA sequencing was performed to compare C-terminus sequences of pbp1A gene between Amx(R) and Amx(S) strains. Natural transformation of these mutated genes into amoxicillin-susceptible strains was performed. Among many mutations in pbp1A, D479E (OR: 37.4, 95% CI: 5.53-252.49, P < .001), and T593 mutation (OR: 32.0, 95% CI: 4.04-252.86, P < .001) independently contributed to Amx resistance in H. pylori strains. In the transformation experiment, T593 mutations were identified in their transformants showing Amx resistance. However, PCR product of D479E was not inserted into recipient (ATCC 43504) resulting in transformation failure. Amx resistance is associated with various substitutions in pbp1A and T593 mutation contributes to Amx resistance of H. pylori. © 2017 John Wiley & Sons Ltd.

  5. Basophil histamine release to Amoxicilloyl-poly-L-lysine compared to amoxicillin in patients with IgE-mediated allergic reactions to amoxicillin

    DEFF Research Database (Denmark)

    Arribas, F; Falkencrone, S; Sola, J

    2017-01-01

    BACKGROUND: Amoxicillin (AX) is the betalactam most often involved in IgE-mediated reactions and the diagnosis is mainly based on skin testing (ST) although without optimal sensitivity. We have produced a newly AX derivative, amoxicilloyl-poly-L-lysine (APL), and have analysed its IgE recognition...... can improve in vitro diagnostic accuracy of AX allergic reactions. Further use for ST needs to be done.......BACKGROUND: Amoxicillin (AX) is the betalactam most often involved in IgE-mediated reactions and the diagnosis is mainly based on skin testing (ST) although without optimal sensitivity. We have produced a newly AX derivative, amoxicilloyl-poly-L-lysine (APL), and have analysed its IgE recognition...... with AX or APL. Histamine released was determined and expressed as ng of histamine release/mL blood. RESULTS: Patients clinical symptoms were anaphylaxis (N=9), urticaria (N=7), erythema (N=2) and not defined immediate reactions (N=1). The median time interval between reaction and study was 90 days (IQR...

  6. Hyaluronidase facilitated subcutaneous immunoglobulin in primary immunodeficiency

    Directory of Open Access Journals (Sweden)

    Jolles S

    2013-09-01

    Full Text Available Stephen Jolles Department of Immunology, University Hospital of Wales, Cardiff, UK Abstract: Immunoglobulin (Ig-replacement therapy represents the mainstay of treatment for patients with primary antibody deficiency and is administered either intravenously (IVIg or subcutaneously (SCIg. While hyaluronidase has been used in clinical practice for over 50 years, the development of a high-purity recombinant form of this enzyme (recombinant human hyaluronidase PH20 has recently enabled the study of repeated and more prolonged use of hyaluronidase in facilitating the delivery of SC medicines. It has been used in a wide range of clinical settings to give antibiotics, local anesthetics, insulin, morphine, fluid replacement, and larger molecules, such as antibodies. Hyaluronidase has been used to help overcome the limitations on the maximum volume that can be delivered into the SC space by enabling dispersion of SCIg and its absorption into lymphatics. The rate of facilitated SCIg (fSCIg infusion is equivalent to that of IVIg, and the volume administered at a single site can be greater than 700 mL, a huge increase over conventional SCIg, at 20–40 mL. The use of fSCIg avoids the higher incidence of systemic side effects of IVIg, and it has higher bioavailability than SCIg. Data on the long-term safety of this approach are currently lacking, as fSCIg has only recently become available. fSCIg may help several areas of patient management in primary antibody deficiency, and the extent to which it may be used in future will depend on long-term safety data and cost–benefit analysis. Keywords: enzyme facilitated IgG infusion, recombinant human hyaluronidase PH20, subcutaneous immunoglobulin, intravenous immunoglobulin, primary immunodeficiency disease

  7. Amoxicillin / Clavulanic Acid and Cefotaxime Resistance in Salmonella Minnesota and Salmonella Heidelberg from Broiler Chickens

    Directory of Open Access Journals (Sweden)

    Rodrigues IBBE

    2017-10-01

    Full Text Available This study investigated the resistance of various Salmonella strains to beta-lactam antibiotics. Salmonella Minnesota (36 strains and Salmonella Heidelberg (24 strains were isolated from broiler chickens and carcasses by the Disk Diffusion Test and resistance genes blaCTX-M-8, blaACC-1 and blaCMY-2 were detected by PCR. Of the 60 strains tested, 80% were resistant to at least one antibiotic. Specifically, 66.7% were resistant to amoxicillin/clavulanic acid and 75% were resistant to cefotaxime. Among the amoxicillin/clavulanic acid resistant strains, the blaCMY-2 gene was detected in 40%, blaACC-1 in 37.5% and blaCTX-M-8 in 7.5%. Among the cefotaxime resistant strains, we detected the genes blaCTX-M-8 in 13.3%, blaACC-1 in 33.3%, and blaCMY-2 in 31.1%. The presence of cefotaxime- and amoxicillin/clavulanic acid-resistant Salmonella in poultry, and the prevalence of extended spectrum betalactamases and AmpC-betalactamases in these strains are of huge concern to public health and economy.

  8. Resistance pattern of Helicobacter pylori strains to clarithromycin, metronidazole, and amoxicillin in Isfahan, Iran

    Directory of Open Access Journals (Sweden)

    Farzad Khademi

    2013-01-01

    Full Text Available Background: Helicobacter pylori (H. pylori resistance to antibiotics has become a global problem and is an important factor in determining the outcome of treatment of infected patients. The purpose of this study was to determine the H. pylori resistance to clarithromycin, metronidazole, and amoxicillin in gastrointestinal disorders patients. Materials and Methods: In this study, a total of 260 gastric antrum biopsy specimens were collected from patients with gastrointestinal disorders who referred to Endoscopy Section of the Isfahan Hospitals. The E-test and Modified Disk Diffusion Method (MDDM were used to verify the prevalence of antibiotic resistance in 78 H. pylori isolates to the clarithromycin, metronidazole, and amoxicillin. Results: H. pylori resistance to clarithromycin, metronidazole, and amoxicillin were 15.3, 55.1, and 6.4%, respectively. In this studyΈ we had one multidrug resistance (MDR isolates from patient with gastritis and peptic ulcer disease. Conclusion: Information on antibiotic susceptibility profile plays an important role in empiric antibiotic treatment and management of refractive cases. According to the results obtained in this study, H. pylori resistance to clarithromycin and metronidazole was relatively high. MDR strains are emerging and will have an effect on the combination therapy.

  9. RESISTANCE TO AMOXICILLIN, CLARITHROMYCIN AND CIPROFLOXACIN OF Helicobacter pylori ISOLATED FROM SOUTHERN BRAZIL PATIENTS

    Directory of Open Access Journals (Sweden)

    Simone Ulrich Picoli

    2014-06-01

    Full Text Available Introduction: Helicobacter pylori is a bacteria which infects half the world population and is an important cause of gastric cancer. The eradication therapy is not always effective because resistance to antimicrobials may occur. The aim of this study was to determine the susceptibility profile of H. pylori to amoxicillin, clarithromycin and ciprofloxacin in the population of Southern Brazil. Material and methods: Fifty four samples of H. pylori were evaluated. The antibiotics susceptibility was determined according to the guidelines of the British Society for Antimicrobial Chemotherapy and the Comité de l'Antibiogramme de la Société Française de Microbiologie. Results: Six (11.1% H. pylori isolates were resistant to clarithromycin, one (1.9% to amoxicillin and three (5.5% to ciprofloxacin. These indices of resistance are considered satisfactory and show that all of these antibiotics can be used in the empirical therapy. Conclusion: The antibiotics amoxicillin and clarithromycin are still a good option for first line anti-H. pylori treatment in the population of Southern Brazil.

  10. Resistance pattern of Helicobacter pylori strains to clarithromycin, metronidazole, and amoxicillin in Isfahan, Iran

    Science.gov (United States)

    Khademi, Farzad; Faghri, Jamshid; Poursina, Farkhondeh; Esfahani, Bahram Nasr; Moghim, Sharareh; Fazeli, Hossein; Adibi, Peyman; Mirzaei, Nasrin; Akbari, Mojtaba; Safaei, Hajieh Ghasemian

    2013-01-01

    Background: Helicobacter pylori (H. pylori) resistance to antibiotics has become a global problem and is an important factor in determining the outcome of treatment of infected patients. The purpose of this study was to determine the H. pylori resistance to clarithromycin, metronidazole, and amoxicillin in gastrointestinal disorders patients. Materials and Methods: In this study, a total of 260 gastric antrum biopsy specimens were collected from patients with gastrointestinal disorders who referred to Endoscopy Section of the Isfahan Hospitals. The E-test and Modified Disk Diffusion Method (MDDM) were used to verify the prevalence of antibiotic resistance in 78 H. pylori isolates to the clarithromycin, metronidazole, and amoxicillin. Results: H. pylori resistance to clarithromycin, metronidazole, and amoxicillin were 15.3, 55.1, and 6.4%, respectively. In this study, we had one multidrug resistance (MDR) isolates from patient with gastritis and peptic ulcer disease. Conclusion: Information on antibiotic susceptibility profile plays an important role in empiric antibiotic treatment and management of refractive cases. According to the results obtained in this study, H. pylori resistance to clarithromycin and metronidazole was relatively high. MDR strains are emerging and will have an effect on the combination therapy. PMID:24523796

  11. A New Case of DRESS Syndrome Induced by Sulfasalazine and Triggered by Amoxicillin

    Directory of Open Access Journals (Sweden)

    Francesco Girelli

    2013-01-01

    Full Text Available Drug Rash Eosinophilia Systemic Symptoms (DRESS syndrome is a systemic hypersensitivity reaction characterized by exfoliative dermatitis and maculopapular rash, lymphadenopathy, fever, eosinophilia, leukocytosis, and involvement of internal organs as liver, lung, heart, and kidney; the disorder starts within 2–6 weeks after taking a drug with an incidence that ranges from 1/1000 to 1/10000 exposures. Fatal cases are reported. The exact pathogenesis of DRESS syndrome is not completely understood, while it is reported that amoxicillin could trigger it in patients who are taking allopurinol, sulfasalazine, NSAIDs, carbamazepine, strontium ranelate, lisinopril, lansoprazole, and minocycline. Amoxicillin could act directly, inducing the reactivation of a viral infection (HHV 6 and EBV with symptoms similar to DRESS syndrome or by reducing the patients’ ability to detoxify the body from substances chronically taken. We describe a case of a patient admitted to our hospital for a DRESS syndrome flared after amoxicilline intake during treatment with sulfasalazine; this combination can activate severe reactions often with an insidious onset that can mimic an infectious disease.

  12. [Effects of sulfur- and polymer-coated controlled release urea fertilizers on wheat yield and quality and fertilizer nitrogen use efficiency].

    Science.gov (United States)

    Ma, Fu-Liang; Song, Fu-Peng; Gao, Yang; Zou, Peng

    2012-01-01

    A field experiment was conducted to study the effects of sulfur- and polymer-coated controlled release urea fertilizers on wheat yield and its quality, plow layer soil inorganic nitrogen (N) contents, and fertilizer N use efficiency. Compared with traditional urea fertilizer, both sulfur- and polymer-coated controlled release urea fertilizers increased the grain yield by 10.4%-16.5%, and the grain protein and starch contents by 5.8%-18.9% and 0.3%-1.4%, respectively. The controlled release urea fertilizers could maintain the topsoil inorganic N contents to meet the N requirement for the wheat, especially during its late growth stage. In the meantime, the fertilizer N use efficiency was improved by 58.2%-101.2%. Polymer-coated urea produced better wheat yield and higher fertilizer N use efficiency, compared with sulfur-coated controlled release urea.

  13. The design of controlled-release formulations resistant to alcohol-induced dose dumping--a review.

    Science.gov (United States)

    Jedinger, N; Khinast, J; Roblegg, E

    2014-07-01

    The concomitant intake of alcoholic beverages together with oral controlled-release opioid formulations poses a serious safety concern since alcohol has the potential to alter the release rate controlling mechanism of the dosage form which may result in an uncontrolled and immediate drug release. This effect, known as alcohol-induced dose dumping, has drawn attention of the regulatory authorities. Thus, the Food and Drug Administration (FDA) recommends that in vitro drug release studies of controlled-release dosage forms containing drugs with narrow therapeutic range should be conducted in ethanolic media up to 40%. So far, only a limited number of robust dosage forms that withstand the impact of alcohol are available and the development of such dosage forms is still a challenge. This review deals with the physico-chemical key factors which have to be considered for the preparation of alcohol-resistant controlling dosage forms. Furthermore, appropriate matrix systems and promising technological strategies, which are suitable to prevent alcohol-induced dose dumping, are discussed. Copyright © 2014 Elsevier B.V. All rights reserved.

  14. Novel inorganic solid controlled-release inhibitor for Q235-b anticorrosion treatment in 1 M HCl

    Science.gov (United States)

    Cui, Jun; Shi, Ruirui; Pei, Yuansheng

    2017-09-01

    Borate was regarded as an interesting material for a broad range of applications. Here, we had prepared a novel borate-based controlled-release inhibitor to improve the anticorrosion performance of Q235-b in 1 M HCl. The effective components released by the inhibitor were boron and sodium, and its anticorrosion performance was investigated by various electrochemical methods The potentiodynamic polarization curve results indicated that the borate-based inhibitor showed a clear anodic-type inhibitor characteristic, and a great improvement of the resistance was obtained from the electrochemical impedance spectroscopy, resulting from the formation of a passive film with Fesbnd Osbnd B structure on the Q235-b surface. The formation process followed the Langmuir isotherm well, and the passive film showed a self-healing capability, which confirmed by the electrochemical noise. Further, the anticorrosion capability of the inhibitor gradually increased with the increasing release time. After 21 days of release, the boron concentration reached 125 mg L-1, the anticorrosion efficiency was over 97%, and a smooth surface was observed on the Q235-b surface from electron microscopy. According to these results, we believed that the borate-based controlled-release inhibitor displayed a satisfactory capability to suppress corrosion on the Q235-b surface in 1 M HCl. The present work provided a novel concept for the development of corrosion inhibitor.

  15. Cross-linked chitosan-dextran sulphate vehicle system for controlled release of ciprofloxaxin drug: An ophthalmic application

    Directory of Open Access Journals (Sweden)

    Chetan Chavan

    2017-01-01

    Full Text Available The major challenge associated with conventional eye-drop is the rapid drug loss due to precorneal defence barrier. In this context, controlled-release system of ciprofloxacin-conjugated chitosan (CS-Dextran sulphate (DS nanoparticles (NPs have been synthesized, to increase the bioavailability. The formulated drug delivery vehicle was evaluated for its therapeutic value in the simulated tear fluidat pH 7.4. Ophthalmic microbes were tested with this formulation, to confirm the drug efficacy; which showed conducive therapeutic values of both MIC and MBC. Ocular irritancy test was performed using HET-CAM test, which showed that the CS-DS system did not yield any vascular response, offering it to be a non-irritant to the ocular surface. The release studies showed monotonous controlled-release for duration of 21 h. A fine cross-linking between CS and DS has been demonstrated to form CS-DS NPs and their interaction with drug has been evaluated using conventional characterization tools.

  16. Preparation, Characterization and In Vitro / In Vivo Evaluation of Oral Time-Controlled Release Etodolac Pellets.

    Science.gov (United States)

    Zhang, Xiaoyu; Li, Qi; Ye, Mingzhu; Zhao, Zhinan; Sun, Jiayi; Yang, Xinggang; Pan, Weisan

    2018-02-01

    The objective of this study was to prepare time-controlled release etodolac pellets to facilitate drug administration according to the body's biological rhythm, optimize the drug's desired effects, and minimize adverse effects. The preparation consisted of three laminal layers from center to outside: the core, the swelling layer, and the insoluble polymer membrane. Factors influenced the core and the coating films were investigated in this study. The core pellets formulated with etodolac, lactose, and sodium carboxymethyl starch (CMS-Na) were prepared by extrusion-spheronization and then coated by a fluidized bed coater. Croscarmellose sodium (CC-Na) was selected as the swelling agent, and ethyl cellulose (EC) as the controlled release layer. The prepared pellets were characterized by scanning electron microscopy and evaluated by a dissolution test and a pharmacokinetic study. Compared with commercial available capsules, pharmacokinetics studies in beagle dogs indicated that the prepared pellets release the drug within a short period of time, immediately after a predetermined lag time. A good correlation between in vitro dissolution and in vivo absorption of the pellets was exhibited in the analysis.

  17. Design and characterization of controlled-release edible packaging films prepared with synergistic whey-protein polysaccharide complexes.

    Science.gov (United States)

    Liu, Fei; Jiang, Yanfeng; Du, Bingjian; Chai, Zhi; Jiao, Tong; Zhang, Chunyue; Ren, Fazheng; Leng, Xiaojing

    2013-06-19

    This paper describes an investigation into the properties of a doubly emulsified film incorporated with protein-polysaccharide microcapsules, which serves as a multifunctional food packaging film prepared using common edible materials in place of petroleum--based plastics. The relationships between the microstructural properties and controlled release features of a series of water-in-oil-in-water (W/O/W) microcapsulated edible films prepared in thermodynamically incompatible conditions were analyzed. The hydrophilic riboflavin (V(B2)) nano-droplets (13-50 nm) dispersed in α-tocopherol (V(E)) oil phase were embedded in whey protein-polysaccharide (WPs) microcapsules with a shell thickness of 20-56 nm. These microcapsules were then integrated in 103 μm thick WPs films. Different polysaccharides, including gum arabic (GA), low-methoxyl pectin (LMP), and κ-carrageenan (KCG), exhibited different in vitro synergistic effects on the ability of both films to effect enteric controlled release of both vitamins. GA, which showed a strong emulsifying ability, also showed better control of V(E) than other polysaccharides, and the highly charged KCG showed better control of V(B2) than GA did.

  18. Preparation and characterization of 1-naphthylacetic acid-silica conjugated nanospheres for enhancement of controlled-release performance

    Science.gov (United States)

    Ao, Mingming; Zhu, Yuncong; He, Shun; Li, Deguang; Li, Pingliang; Li, Jianqiang; Cao, Yongsong

    2013-01-01

    Chemical pesticides have been widely used to increase the yield and quality of agricultural products as they are efficient, effective, and easy to apply. However, the rapid degradation and low utilization ratio of conventional pesticides has led to environmental pollution and resource waste. Nano-sized controlled-release formulations (CRFs) can provide better penetration through the plant cuticle and deliver the active ingredients efficiently to the targeted tissue. In this paper we reported novel conjugated nanospheres derived from 1-naphthylacetic acid (NNA), 3-aminopropyltriethoxysilane (APTES) and tetraethyl orthosilicate and their application as a controlled-release plant growth regulator. The NNA and APTES conjugate was prepared through a covalent cross-linking reaction and subsequent hydrolyzation and polycondensation to synthesize NNA-silica nanospheres. The release data indicated that the release of NNA was by non-Fickian transport and increased as particle size decreased. It was also found that the acidity-alkalinity was enhanced and as the temperature increased, the release of the active ingredient was faster. The nanoconjugate displayed a better efficacy in promoting root formation than NNA technical. The present study provides a novel synthesis route for CRFs comprising a pesticide, with long-duration sustained-release performance and good environmental compatibility. This method may be extended to other pesticides that possess a carboxyl group.

  19. Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.

    Science.gov (United States)

    Qi, Xiaole; Chen, Haiyan; Rui, Yao; Yang, Fengjiao; Ma, Ning; Wu, Zhenghong

    2015-07-15

    To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30s and remain lastingly buoyant over a period of 12 h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo(®). These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach. Copyright © 2015 Elsevier B.V. All rights reserved.

  20. [Effects of controlled release nitrogen fertilizer application on dry matter accumulation and nitrogen balance of summer maize].

    Science.gov (United States)

    Si, Dong-Xia; Cui, Zhen-Ling; Chen, Xin-Ping; Lü, Fu-Tang

    2014-06-01

    Effects of four controlled release nitrogen (N) fertilizers, including two kinds of polyester coated urea (Ncau, CRU) and phosphate (NhnP) and humic acid (NhnF) coated urea on assimilates accumulation and nitrogen balance of summer maize were investigated in a mode of one-time fertilization at the regional N recommended rate. The results showed that the N release curves of the two controlled release fertilizers CRU and Ncau matched well with the summer maize N uptake. Compared with the regional N recommendation rate, CRU could increase maize yield by 4.2% and Ncau could maintain the same yield level. CRU significantly increased the dry matter accumulation rate after anthesis of summer maize, but Ncau markedly increased the dry matter accumulated ratio before anthesis. Meanwhile, CRU could reduce the apparent N losses by 19 kg N x hm(-2) in the case of large precipitation. However, NhnF and NhnP caused the yield losses by 0.1%-8.9%, and enhanced the apparent N losses. Therefore, both CRU and Ncau with one-time fertilization could be a simplified alternative to the "total control, staging regulation" fertilization technique at the regional N recommended rate for summer maize production.

  1. Continuous subcutaneous insulin infusion therapy in type 1 diabetes ...

    African Journals Online (AJOL)

    2013-01-14

    Jan 14, 2013 ... Guidelines: Continuous subcutaneous insulin infusion pump therapy in type 1 diabetes. 15. 2013 Volume 18 No 1. JEMDSA. Introduction. The first external insulin pump device to deliver continuous subcutaneous insulin infusion (CSII or “insulin pump”) therapy was used more than 30 years ago.

  2. The comparison of the intestinal adaptation effects of subcutaneous ...

    African Journals Online (AJOL)

    Aim: Insulin has been reported to have positive effects on intestinal adaptation after short bowel syndrome when applicated oral or subcutaneously. The purpose of this study is to compare the intestinal adaptation effects of subcutaneous and oral routes of insulin in rats with short bowel syndrome. Materials and Methods: ...

  3. Cost-minimization of mabthera intravenous versus subcutaneous administration

    NARCIS (Netherlands)

    Bax, P.; Postma, M.J.

    2013-01-01

    Objectives: To identify and compare all costs related to preparing and administrating MabThera for the intravenous and subcutaneous formulations in Dutch hematological patients. The a priori notion is that the costs of subcutaneous MabThera injections are lower compared to intravenous infusion due

  4. Hypercalcemia in Association With Subcutaneous Fat Necrosis of ...

    African Journals Online (AJOL)

    The case of a four weeks-old girl with subcutaneous fat necrosis and associated hypercalcemia is presented. Subcutaneous Fat Necrosis of the New born (SCFN) is an uncommon disorder which is rarely complicated with life threatening hypercalcemia. Though it is reported from many parts of the world this is the first case ...

  5. Controlled Release Urea as a Nitrogen Source for Spring Wheat in Western Canada: Yield, Grain N Content, and N Use Efficiency

    OpenAIRE

    Lenz Haderlein; T.L. Jensen; R.E. Dowbenko; A.D. Blaylock

    2001-01-01

    Controlled release nitrogen (N) fertilizers have been commonly used in horticultural applications such as turf grasses and container-grown woody perennials. Agrium, a major N manufacturer in North and South America, is developing a low-cost controlled release urea (CRU) product for use in field crops such as grain corn, canola, wheat, and other small grain cereals. From 1998 to 2000, 11 field trials were conducted across western Canada to determine if seed-placed CRU could maintain crop yield...

  6. Comparative safety and efficacy of clarithromycin and amoxicillin/clavulanate in the treatment of acute otitis media in children.

    Science.gov (United States)

    McCarty, J M; Phillips, A; Wiisanen, R

    1993-12-01

    Clarithromycin is a new macrolide antibiotic with a wide spectrum of activity that includes the pathogens commonly causing pediatric otitis media. This randomized, investigator-blinded, multicenter trial compared the safety and efficacy of clarithromycin and amoxicillin/clavulanate in the treatment of acute otitis media in patients ages 6 months to 12 years. A total of 338 patients with acute otitis media diagnosed by otoscopy were randomized to receive clarithromycin 7.5 mg/kg twice daily, maximum 500 mg twice daily (n = 161), or amoxicillin/clavulanate 13.3 mg/kg three times daily, maximum 500 mg three times daily (n = 177), for 10 days. Treatment groups were comparable with respect to demographics, severity of infection and number of previous episodes. Efficacy was assessed by clinical examination performed within 48 hours of finishing study medication. A successful clinical response was seen in 90% (121 of 135) of evaluable clarithromycin patients vs. 92% (133 of 145) of evaluable amoxicillin/clavulanate patients (P = 0.681). Clinical failure or relapse (Posttreatment Days 0 to 4) occurred in 10% (14 of 135) of clarithromycin-treated patients vs. 8% (12 of 145) of amoxicillin/clavulanate-treated patients. Gastrointestinal adverse events were the most commonly reported in both groups. Of these events diarrhea was the most frequent, occurring in 12% (19 of 161) of clarithromycin and 32% (57 of 177) of amoxicillin/clavulanate-treated patients (P clarithromycin oral suspension was comparable with amoxicillin/clavulanate oral suspension in the treatment of acute otitis media in children. Clarithromycin was better tolerated than amoxicillin/clavulanate with a lower incidence of gastrointestinal side effects.

  7. Safety of subcutaneous microinjections (mesotherapy) in musicians.

    Science.gov (United States)

    Navarte, Danik Arana; Rosset-Llobet, Jaume

    2011-06-01

    Determine the safety and tolerance of mesotherapy as a technique for the treatment of musculoskeletal complaints in musicians. 67 patients (55.2% women) were subjected to a total of 267 mesotherapy sessions. A mesotherapy needle or normal needle was used randomly. The drugs employed were thiocolchicoside and diazepam as muscular relaxants, pentoxifylline or buflomedil as vasodilators, and piroxicam as an anti-inflammatory, as directed. A visual analogue scale was used to quantify the pain produced by the microinjections as well as the degree of immediate and midterm side effects as reported on a standard questionnaire. A mean of 155.5 microinjections were performed per session, of which 45.6% were perceived as painful by the patient with a mean severity of 4.3 out of 10. The pain reduced to 0.5 out of 10 after 24 hours. The most sensitive areas were the levator scapulae and splenius muscles. Systemic symptoms were reported by 5.99% of the musicians after the mesotherapy sessions (muscular weakness 1.5%, rash 1.5%, drowsiness 1.1% and itching 1.1%, being the most frequent). The mean severity of these symptoms was 2.77 out of 10. In all cases the symptoms had completely disappeared after 24 hours. No patient referred to signs of local or systemic infection. The application of drugs by means of subcutaneous injections (mesotherapy) in musicians is a technique that is safe, well tolerated, and without any severe complications.

  8. Continuous subcutaneous insulin infusion: practical issues

    Directory of Open Access Journals (Sweden)

    Banshi D Saboo

    2012-01-01

    Full Text Available The growing number of individuals with diabetes mellitus has prompted new way of treating these patients, continuous subcutaneous insulin infusion (CSII or insulin pump therapy is an increasingly form of intensive insulin therapy. An increasing number of individuals with diabetes mellitus individuals of all ages have started using insulin pump therapy. Not everyone is a good candidate for insulin pump therapy, and the clinician needs to be able to determine which patients are able to master the techniques required and to watch for the adverse reactions that may develop. Insulin pump increases quality of life of patient with diabetes mellitus with increasing satisfaction with treatment and decrease impact of diabetes mellitus. Manual errors by insulin pump users may lead to hypo or hyperglycemia, resulting into diabetic ketoacidosis (DKA sometimes. Some of practical aspect is associated with insulin pump therapy such as selection of candidates, handling of pump and selection of site, and pump setting, henceforth this review is prepared to explore and solve the practical problems or issues associated with pump therapy.

  9. Amoxicillin and amoxicillin/clavulanate reduce ethanol intake and increase GLT-1 expression as well as AKT phosphorylation in mesocorticolimbic regions.

    Science.gov (United States)

    Goodwani, Sunil; Rao, P S S; Bell, Richard L; Sari, Youssef

    2015-10-05

    Studies have shown that administration of the β-lactam antibiotic ceftriaxone (CEF) attenuates ethanol consumption and cocaine seeking behavior as well as prevents ethanol-induced downregulation of glutamate transporter 1 (GLT-1) expression in central reward brain regions. However, it is not known if these effects are compound-specific. Therefore, the present study examined the effects of two other β-lactam antibiotics, amoxicillin (AMOX) and amoxicillin/clavulanate (Augmentin, AUG), on ethanol drinking, as well as GLT-1 and phosphorylated-AKT (pAKT) levels in the nucleus accumbens (Acb) and medial prefrontal cortex (mPFC) of alcohol-preferring (P) rats. P rats were exposed to free-choice of ethanol (15% and 30%) for five weeks and were given five consecutive daily i.p. injections of saline vehicle, 100 mg/kg AMOX or 100mg/kg AUG. Both compounds significantly decreased ethanol intake and significantly increased GLT-1 expression in the Acb. AUG also increased GLT-1 expression in the mPFC. Results for changes in pAKT levels matched those for GLT-1, indicating that β-lactam antibiotic-induced reductions in ethanol intake are negatively associated with increases in GLT-1 and pAKT levels within two critical brains regions mediating drug reward and reinforcement. These findings add to a growing literature that pharmacological increases in GLT-1 expression are associated with decreases in ethanol intake and suggest that one mechanism mediating this effect may be increased phosphorylation of AKT. Thus, GLT-1 and pAKT may serve as molecular targets for the treatment of alcohol and drug abuse/dependence. Copyright © 2015 Elsevier B.V. All rights reserved.

  10. Tunable adhesion of superoleophilic/superhydrophobic poly (lactic acid) membrane for controlled-release of oil soluble drugs.

    Science.gov (United States)

    Gao, Ailin; Liu, Fu; Xiong, Zhu; Yang, Qing

    2017-11-01

    Superhydrophobic membranes with tunable adhesion have attracted intense interests for various engineering applications. In this work, superhydrophobic sustainable poly (lactic acid) (PLA) porous membrane with tunable adhesive force from 101μN to 29μN was successfully fabricated via one-step phase separation method. The incorporation of Perfluoro-1-decene (PFD) into the PLLA/PDLA membrane via the in situ polymerization can facilely tune the PLLA/PDLA stereocomplex crystallization during phase inversion, which consequently caused the unique morphology blooming evolution from bud to full-blown state. The resulted membrane showed tunable pore size, porosity, surface area, surface roughness and superhydrophobicity, which enabled the membrane with controlled-release of oil soluble drugs. Copyright © 2017 Elsevier Inc. All rights reserved.

  11. Mussel-inspired polydopamine coated mesoporous silica nanoparticles as pH-sensitive nanocarriers for controlled release.

    Science.gov (United States)

    Zheng, Qishan; Lin, Tianran; Wu, Hanyin; Guo, Liangqia; Ye, Peirong; Hao, Yanli; Guo, Qingquan; Jiang, Jinzhi; Fu, Fengfu; Chen, Guonan

    2014-03-10

    A novel pH-sensitive controlled release system is proposed by using mussel-inspired polydopamine (PDA) coated mesoporous silica nanoparticles (MSNs) as nanocarriers. MSNs with a large pore diameter are synthesized by using 1,3,5-trimethylbenzene as a pore-expanding agent and are modified with a PDA coating by virtue of oxidative self-polymerization of dopamine in neutral pH. PDA coated MSNs are characterized by FTIR, TEM, N₂ adsorption and XPS techniques. The PDA coating can work as pH-sensitive gatekeepers to control the release of drug molecules from MSNs in response to the pH-stimulus. Doxorubicin (DOX, an anticancer drug) can be released in the acid media and blocked in the neutral media. Copyright © 2014 Elsevier B.V. All rights reserved.

  12. [Nutrient use efficiency and yield-increasing effect of single basal application of rice specific controlled release fertilizer].

    Science.gov (United States)

    Chen, Jiansheng; Xu, Peizhi; Tang, Shuanhu; Zhang, Fabao; Xie, Chunsheng

    2005-10-01

    A series of pot and field experiments and field demonstrations showed that in comparing with the commonly used specific-fertilizers containing same amounts of nutrients, single basal application of rice-specific controlled release fertilizer could increase the use efficiency of N and P by 12.2% - 22.7% and 7.0% - 35.0%, respectively in pot experiment, and the use efficiency of N by 17.1% in field experiment. In 167 field demonstrations successively conducted for 3 years in various rice production areas of Guangdong Province, single basal application of the fertilizer saved the application rate of N and P by 22.1% and 21.8%, respectively, and increased the yield by 8.2%, compared with normal split fertilization.

  13. Controlled Release of Indomethacin from Smart Starch-Based Hydrogels Prepared Acrylic Acid and b-Cyclodextrin as a Nanocarrier

    Directory of Open Access Journals (Sweden)

    Hossein Ghasemzadeh Mohammadi

    2017-01-01

    Full Text Available Controlled release of drugs can reduce the undesired effects of drug level fluctuations, and diminish the side effects as well as improve the therapeutic outcome of the drugs. In recent year, the scope of the drug delivery systems has been greatly expanded by the development of various hydrogels. The present work has focused on the design of a pH sensitive drug delivery system (DDS based on starch, acrylic acid (AA and β-cyclodextrins for controlled delivery of indomethacin. The hydrogels were prepared via graft polymerization of acrylic acid (AA onto starch and β-cyclodextrins backbones by a free radical polymerization technique. Cyclodextrins are able to form water-soluble complexes with many lipophilic water-insoluble drugs. In aqueous solutions, the drug molecules located in the central cavity of the cyclodextrin are in a dynamic equilibrium with free drug molecules. The interaction of drug with the polymer was evidenced by FTIR spectroscopy and thermal gravimetric analysis (TGA. The morphology of the samples was examined by scanning electron microscopy (SEM. The results showed that the hydrogels have good porosity and provided high surface area for the loading and release of drugs. Drug release behavior was carried out at physiological conditions of phosphate buffer, pH 8. In basic pH (like the intestine medium the hydrogels released the indomethacin, but in acidic pH (like the stomach medium there was no tendency to drug release. By increasing the amount of cyclodextrin, the rate of drug loading and release increased due to the dynamic equilibrium and interaction between the loaded drug and the cyclodextrin. This study has demonstrated that the hydrogel matrices are potentially suitable for controlled-release systems.

  14. Effect of size on the cellular endocytosis and controlled release of mesoporous silica nanoparticles for intracellular delivery.

    Science.gov (United States)

    Gan, Qi; Dai, Danwei; Yuan, Yuan; Qian, Jiangchao; Sha, Sha; Shi, Jianlin; Liu, Changsheng

    2012-04-01

    Due to the unique physicochemical properties and membrane-permeable capacity, mesoporous silica nanoparticles (MSNs) are considered as an ideal carrier for intracellular delivery. Herein, we endeavored to address the size effect of MSNs on the cellular uptake, endosomal escape and controlled release, the key steps for the intracellular delivery. The well-ordered MSNs in the range from 55-nm to 440-nm with similar pore texture were prepared by modified base-catalyzed sol-gel method. With MC3T3-E1 model cell line, the in vitro results indicated that after 12 h cultivation, MSNs within 55 ~ 440 nm could all be internalized into the cells, and further escaped out of the endosomal compartment. The efficiency of the cellular uptake and endosomal escape strongly depended on the particle size, with the best efficiencies from 100-nm MSNs. Furthermore, the MTT results indicated that these MSNs materials were all biocompatible. The controlled release experiments with hydrophobic dexamethasone and hydrophilic vitamin C as models showed that for these small-molecular drugs, the loading amount all mainly determined by the surface area of the MSNs, and the subsequent release of the drug dramatically decreased with the increasing of the particle size. By contrast, the release rate of vitamin C was much quicker than that of the dexamethasone. These findings presented here could provide new means to tailor the size of MSNs and thus to guide the design of MSNs-based intracellular delivery system. Due to the good cell biocompatibility, high cellular uptake and endosomal escape, we conjectured that the 100-nm MSNs are more favorable for the intracellular delivery of drugs in live cells.

  15. Using Dynamic Covalent Chemistry To Drive Morphological Transitions: Controlled Release of Encapsulated Nanoparticles from Block Copolymer Vesicles.

    Science.gov (United States)

    Deng, Renhua; Derry, Matthew J; Mable, Charlotte J; Ning, Yin; Armes, Steven P

    2017-06-07

    Dynamic covalent chemistry is exploited to drive morphological order-order transitions to achieve the controlled release of a model payload (e.g., silica nanoparticles) encapsulated within block copolymer vesicles. More specifically, poly(glycerol monomethacrylate)-poly(2-hydroxypropyl methacrylate) (PGMA-PHPMA) diblock copolymer vesicles were prepared via aqueous polymerization-induced self-assembly in either the presence or absence of silica nanoparticles. Addition of 3-aminophenylboronic acid (APBA) to such vesicles results in specific binding of this reagent to some of the pendent cis-diol groups on the hydrophilic PGMA chains to form phenylboronate ester bonds in mildly alkaline aqueous solution (pH ∼ 10). This leads to a subtle increase in the effective volume fraction of this stabilizer block, which in turn causes a reduction in the packing parameter and hence induces a vesicle-to-worm (or vesicle-to-sphere) morphological transition. The evolution in copolymer morphology (and the associated sol-gel transitions) was monitored using dynamic light scattering, transmission electron microscopy, oscillatory rheology, and small-angle X-ray scattering. In contrast to the literature, in situ release of encapsulated silica nanoparticles is achieved via vesicle dissociation at room temperature; moreover, the rate of release can be fine-tuned by varying the solution pH and/or the APBA concentration. Furthermore, this strategy also works (i) for relatively thick-walled vesicles that do not normally exhibit stimulus-responsive behavior and (ii) in the presence of added salt. This novel molecular recognition strategy to trigger morphological transitions via dynamic covalent chemistry offers considerable scope for the design of new stimulus-responsive copolymer vesicles (and hydrogels) for targeted delivery and controlled release of cargoes. In particular, the conditions used in this new approach are relevant to liquid laundry formulations, whereby enzymes require

  16. Development and characterization of solid dispersion-microsphere controlled release system for poorly water-soluble drug.

    Science.gov (United States)

    Malipeddi, Venkata Ramana; Dua, Kamal; Awasthi, Rajendra

    2016-10-01

    The present study aimed to improve solubility and prolong the release duration of a poorly soluble drug using a combination of two different types of formulations (solid dispersion and microspheres). The solid dispersions were prepared by fusion method using urea and mannitol as hydrophilic carriers. Microspheres were prepared by solvent evaporation method using Eudragit L-100 (EL100) and Eudragit RS PO (ERS) as rate-controlling polymers. Flurbiprofen (FBP)-urea (1:2) solid dispersion and microspheres of FBP-EL-100-ERS (1:0.25:0.75) were used for the development of controlled release formulation by mixing them in different proportions. The FBP-containing formulations were evaluated for percentage yield, drug content, morphology, in vitro release, and in vivo anti-inflammatory activity. The best selected formulation was further evaluated for the controlled and improved effects. SEM photomicrograph confirmed the spherical shape of microspheres and with particle size in the range of 73.5-85.4 μm. In vitro release of FBP from controlled release formulations indicated that the formulation containing solid dispersion:microspheres (1:0.5) yielded prolonged effect up to 10 h. The release kinetics followed zero-order, and the mechanism of drug release was found to be diffusion rate controlled. This formulation had shown better inhibition of edema of rat paw up to 16 h and identified as a suitable product for controlled delivery of FBP. In conclusion, the concept of using a binary mixture of solid dispersion and microspheres can be used for other drugs that exhibit a poor solubility in stomach pH and a faster release in intestinal pH.

  17. Impact of formulation and process variables on solid-state stability of theophylline in controlled release formulations.

    Science.gov (United States)

    Korang-Yeboah, Maxwell; Rahman, Ziyaur; Shah, Dhaval; Mohammad, Adil; Wu, Suyang; Siddiqui, Akhtar; Khan, Mansoor A

    2016-02-29

    Understanding the impact of pharmaceutical processing, formulation excipients and their interactions on the solid-state transitions of pharmaceutical solids during use and in storage is critical in ensuring consistent product performance. This study reports the effect of polymer viscosity, diluent type, granulation and granulating fluid (water and isopropanol) on the pseudopolymorphic transition of theophylline anhydrous (THA) in controlled release formulations as well as the implications of this transition on critical quality attributes of the tablets. Accordingly, 12 formulations were prepared using a full factorial screening design and monitored over a 3 month period at 40 °C and 75%. Physicochemical characterization revealed a drastic drop in tablet hardness accompanied by a very significant increase in moisture content and swelling of all formulations. Spectroscopic analysis (ssNMR, Raman, NIR and PXRD) indicated conversion of THA to theophylline monohydrate (TMO) in all formulations prepared by aqueous wet granulation in as early as two weeks. Although all freshly prepared formulations contained THA, the hydration-dehydration process induced during aqueous wet granulation hastened the pseudopolymorphic conversion of theophylline during storage through a cascade of events. On the other hand, no solid state transformation was observed in directly compressed formulations and formulations in which isopropanol was employed as a granulating fluid even after the twelve weeks study period. The transition of THA to TMO resulted in a decrease in dissolution while an increase in dissolution was observed in directly compressed and IPA granulated formulation. Consequently, the impact of pseudopolymorphic transition of theophylline on dissolution in controlled release formulations may be the net result of two opposing factors: swelling and softening of the tablets which tend to favor an increase in drug dissolution and hydration of theophylline which decreases the drug

  18. Once-daily amoxicillin versus twice-daily penicillin V in group A beta-haemolytic streptococcal pharyngitis.

    Science.gov (United States)

    Lennon, D R; Farrell, E; Martin, D R; Stewart, J M

    2008-06-01

    Rheumatic fever is a preventable chronic disease preceded by group A beta-haemolytic streptococcal (GABHS) pharyngitis. To test the non-inferiority of once-daily (QD) oral amoxicillin to the recommended twice-daily (BID) oral penicillin V in GABHS pharyngitis. This was a randomised non-inferiority trial carried out in a school-based clinic in New Zealand. Children presenting with GABHS pharyngitis were randomised to oral amoxicillin 1500 mg QD (or 750 mg if bodyweight was medication and weekend diary cards were used to monitor adherence. Eradication of GABHS, determined with follow-up throat cultures on days 3-6, 12-16 and 26-36. GABHS isolates were serotyped to distinguish bacteriological treatment failures (and relapses) from new acquisitions. Non-inferiority was defined as an upper 95% confidence limit (CL) for the difference in success of eradication in the amoxicillin and penicillin V treatment groups of rheumatic fever occurred after 7 days of amoxicillin. In this adequately powered study, once-daily oral amoxicillin is not inferior to twice-daily penicillin V for the treatment and eradication of GABHS in children with pharyngitis.

  19. Amoxicillin-associated interference in an HPLC-EC assay for urinary fractionated metanephrines: potential pitfall in pheochromocytoma biochemical diagnosis.

    Science.gov (United States)

    Barco, Sebastiano; Alpigiani, Maria Giannina; Ghiggeri, Gian Marco; Talio, Marina; Maffia, Angelo; Tripodi, Gino; Cangemi, Giuliana

    2014-10-01

    Measurement of urinary fractionated metanephrines represents a first-line test for the biochemical diagnosis of pheochromocytoma. The high performance liquid chromatography coupled to electrochemical detection (HPLC-EC) assays used in the routine clinical laboratory can be subjected to analytical interferences by the presence of drugs or their metabolites. In this paper we describe the interference on urinary normetanephrine (uNMN) caused by amoxicillin. Two pediatric patients suspected of pheochromocytoma had very high uNMN levels (2543 and 4227μg/g Cr respectively; upper reference value: 339μg/g Cr). Amoxicillin interference was assessed by comparison for co-elution with uNMN and by LC-MS/MS analysis. After amoxicillin interference was suspected and the therapy was stopped uNMN levels returned to normal (149 and 214μg/g Cr respectively). Chromatograms obtained by HPLC-EC clearly showed that amoxicillin co-elutes with uNMN. Patients' uNMN levels measured by LC-MS/MS were in the normal range. Amoxicillin is responsible for analytical interference on HPLC-EC assay for uNMN. This finding can be of help in distinguishing true-positive from false-positive results in the course of a biochemical diagnosis for pheochromocytoma. Copyright © 2014 The Canadian Society of Clinical Chemists. Published by Elsevier Inc. All rights reserved.

  20. Pharmaceutical suspension containing both immediate/sustained-release amoxicillin-loaded gelatin nanoparticles: preparation and in vitro characterization

    Science.gov (United States)

    Harsha, Sree

    2013-01-01

    Pharmaceutical suspension containing oral dosage forms delivering both immediate-release and sustained-release amoxicillin was developed as a new dosage form to eradicate Helicobacter pylori. Amoxicillin-loaded gelatin nanoparticles are able to bind with the mucosal membrane after delivery to the stomach and could escalate the effectiveness of a drug, providing dual release. The objective of this study was to develop amoxicillin nanoparticles using innovative new technology – the Büchi Nano Spray Dryer B-90 – and investigate such features as drug content, particle morphology, yield, in vitro release, flow properties, and stability. The nanoparticles had an average particle size of 571 nm. The drug content and percentage yield was 89.2% ± 0.5% and 93.3% ± 0.6%, respectively. Angle of repose of nanoparticle suspension was 26.3° and bulk density was 0.59 g/cm3. In vitro drug release of formulations was best fitted by first-order and Peppas models with R2 of 0.9841 and 0.9837 respectively; release profile was 15.9%, while; for the original drug, amoxicillin, under the same conditions, 90% was released in the first 30 minutes. The nanoparticles used in this study enabled sustained release of amoxicillin over an extended period of time, up to 12 hours, and were stable for 12 months under accelerated storage conditions of 25°C ± 2°C and 60% ± 5% relative humidity. PMID:24101859

  1. Amoxicillin/Clavulanic Acid for the Treatment of Odontogenic Infections: A Randomised Study Comparing Efficacy and Tolerability versus Clindamycin

    Directory of Open Access Journals (Sweden)

    Archiel Launch Tancawan

    2015-01-01

    Full Text Available Background. Treatment of odontogenic infections includes surgical drainage and adjunctive antibiotics. This study was designed to generate efficacy and safety data to support twice daily dosing of amoxicillin/clavulanic acid compared to clindamycin in odontogenic infections. Methods. This was a phase IV, randomised, observer blind study; 472 subjects were randomised to receive amoxicillin/clavulanic acid (875 mg/125 mg BID, n=235 or clindamycin (150 mg QID, n=237 for 5 or 7 days based on clinical response. The primary endpoint was percentage of subjects achieving clinical success (composite measure of pain, swelling, fever, and additional antimicrobial therapy required at the end of treatment. Results. The upper limit of two-sided 95% confidence interval for the treatment difference between the study arms (7.7% was within protocol specified noninferiority margin of 10%, thus demonstrating noninferiority of amoxicillin/clavulanic acid to clindamycin. Secondary efficacy results showed a higher clinical success rate at Day 5 in the amoxicillin/clavulanic acid arm. Most adverse events (raised liver enzymes, diarrhoea, and headache were similar across both arms and were of mild to moderate intensity. Conclusion. Amoxicillin/clavulanic acid was comparable to clindamycin in achieving clinical success (88.2% versus 89.7% in acute odontogenic infections and the safety profile was consistent with the known side effects of both drugs. Trial Registration. This trial is registered with Clinicaltrials.gov identifier: NCT02141217.

  2. Antibacterial efficacy of AH Plus and AH26 sealers mixed with amoxicillin, triple antibiotic paste and nanosilver

    Directory of Open Access Journals (Sweden)

    Ali Kangarlou

    2016-12-01

    Full Text Available Background. Elimination of bacteria from the root canal system is one of the aims of endodontic treatment; hence the incorporation of antibiotics into sealers can increase their antimicrobial efficacy. The aim of the present study was to determine the in vitro antimicrobial effects of AH26 and AH Plus sealers mixed with amoxicillin, triple antibiotic paste and nanosilver on Enterococcus faecalis. Methods. In this experiment, amoxicillin, triple antibiotic paste and nanosilver powder were added at 10% of the total sealer weight to AH26 and AH Plus sealers and then cultured freshly or after 1, 3, and 7 days with suspension of E. faecalis for 24 hours. The zones of growth inhibition for E. faecalis were evaluated in each group. Results. Incorporation of nanosilver did not increase antibacterial effects of the sealers. Sealers combined with amoxicillin exhibited the highest antibacterial efficacy in fresh condition. In the set specimens, the results demonstrated that the mixture of sealers and triple antibiotic pastes exhibited the greatest antibacterial efficacy. Conclusion. Amoxicillin and triple antibiotic paste significantly improved the antibacterial properties of AH Plus and AH26 sealers. Such properties decreased with time, but the use of sealer-amoxicillin/triple paste combination was still superior to using sealers alone or in combination with nanosilver.

  3. A Nodular Type of Subcutaneous Sarcoidosis: A Case Report

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Kyu Ho; Choi, Yun Sun; Kim, Byoung Suck; Joo, Jong Eun; Jung, Yoon Young; Cho, Young Kwon; An, Jin Kyung; Kim, Hyun Sook; Woo, Jung Joo [Eulji University Hospital, Daejeon (Korea, Republic of)

    2009-01-15

    Sarcoidosis is a granulomatous multisystemic disorder that rarely involves subcutaneous tissue. We describe the MR imaging findings of a subcutaneous sarcoidosis in a patient that presented with a nontender, palpable soft tissue mass on the left buttock, which was confirmed after surgical excision. The MR images showed the presence of a subcutaneous mass that breached the adjacent fascia with an irregular outline and homogeneous, slightly higher signal intensity than the surrounding muscle as seen on a T2-weighted image and with homogeneous enhancement after contrast injection. The lesion could not be differentiated from a sarcoma or a malignancy.

  4. Iatrogenic subcutaneous cervicofacial emphysema with pneumomediastinum after class V restoration.

    Science.gov (United States)

    Lee, Sang-Woon; Huh, Yoon-Hyuk; Cha, Min-Sang

    2017-02-01

    Subcutaneous facial emphysema after dental treatment is an uncommon complication caused by the invasion of high-pressure air; in severe cases, it can spread to the neck, mediastinum, and thorax, resulting in cervical emphysema, pneumomediastinum, and pneumothorax. The present case showed subcutaneous cervicofacial emphysema with pneumomediastinum after class V restoration. The patient was fully recovered after eight days of conservative treatment. The cause of this case was the penetration of high-pressure air through the gingival sulcus, which had a weakened gingival attachment. This case indicated that dentists should be careful to prevent subcutaneous emphysema during common dental treatments using a high-speed hand piece and gingival retraction cord.

  5. Metastatic breast cancer 42 years after bilateral subcutaneous mastectomies.

    Science.gov (United States)

    Jameson, M B; Roberts, E; Nixon, J; Probert, J C; Braatvedt, G D

    1997-01-01

    Subcutaneous mastectomy has a possible role as prophylaxis in patients at high risk of developing breast cancer. A case history is presented of a woman who developed metastatic breast carcinoma 42 years after bilateral subcutaneous mastectomies for non-malignant disease. This case is presented to draw attention to the persistent risk of developing breast cancer even decades after subcutaneous mastectomy and to point out that the role of such surgery in preventing breast cancer has still not been clarified. The appropriateness of prophylactic mastectomy for an individual is better assessed on the absolute risk of breast cancer developing over a defined period rather than the relative risk.

  6. Subcutaneous implantable cardioverter-defibrillator: Initial experience.

    Science.gov (United States)

    Galvão, Pedro; Cavaco, Diogo; Adragão, Pedro; Costa, Francisco; Carmo, Pedro; Morgado, Francisco; Bernardo, Ricardo; Nunes, Manuela; Abecasis, Miguel; Neves, José; Mendes, Miguel

    2014-09-01

    Implantable cardioverter-defibrillators (ICDs) are important tools in the prevention of sudden death, but implantation requires transvenous access, which is associated with complications. Subcutaneous implantable cardioverter-defibrillators (S-ICDs) may prevent some of these complications. To evaluate the therapeutics and complications associated with S-ICD systems. S-ICD implantation was planned in 23 patients, for whom the indications were vascular access problems, increased risk of infection or young patients with long predicted follow-up. The population consisted of four patients with ischemic heart disease, three of them on hemodialysis (two with subclavian vein thrombosis), five with left ventricular noncompaction, four with Brugada syndrome, three with arrhythmogenic right ventricular cardiomyopathy, one with transposition of the great vessels, two with dilated cardiomyopathy and four with hypertrophic cardiomyopathy. S-ICDs were implanted in 21 patients, two having failed to fulfil the initial screening criteria. Mean implantation time was 77 minutes, with no complications. Defibrillation tests were performed, and in one patient the generator had to be repositioned to obtain an acceptable threshold. In a mean follow-up of 14 months, 10 patients had S-ICD shocks, which were appropriate in half of them; one developed infection, one needed early replacement due to loss of telemetry and one patient died of noncardiac cause. S-ICD implantation can be performed by cardiologists with a high success rate. Initial experience appears favorable, but further studies are needed with longer follow-up times to assess the safety and efficacy of this strategy compared to conventional devices. Copyright © 2013 Sociedade Portuguesa de Cardiologia. Published by Elsevier España. All rights reserved.

  7. Disposition Kinetics of Amoxicillin in Healthy, Hepatopathic and Nephropathic Conditions in Chicken after Single Oral Administration

    Directory of Open Access Journals (Sweden)

    Moloy Kumar Bhar

    2010-12-01

    Full Text Available Fifteen broiler chickens (COBB 400 of 42 days of age weighing 1.8 to 2.0 kg were equally divided into 3 groups, each consisting of 5 birds. Hepatopathy was induced by oral administration of paracetamol while nephropathy was induced by intravenous administration of uranyl nitrate. Kinetic study was investigated in healthy, hepatopathic and nephropathic birds following single oral administration of amoxicillin at 40 mg kg-1. Blood samples were collected at different time schedule. Plasma concentrations of amoxicillin in healthy, hepatopathic and nephropathic birds were 41.90 ± 5.59, 9.93 ± 0.76 and 38.75 ± 6.08 µg ml-1, respectively at 1 hr; 15.34 ± 1.99, 18.57 ± 1.66 and 67.40 ± 2.62 µg ml-1, respectively at 4 hr and 2.03 ± 0.28, 15.54 ± 0.82 and 30.63 ± 1.58 µg ml-1, respectively at 24 hr. Maximum plasma concentration was detected at 1 hr in healthy birds (41.90 ± 5.59 µg ml-1 , at 8 hr in hepatopathic birds (23.51 ± 1.64 µg ml-1 and at 4 hr in nephropathic birds (67.40 ± 2.62 µg ml-1. The drug could not be detected in plasma beyond 24 hr in healthy, 72 hr in both hepatopathic and nephropathic birds. The concentration of amoxicillin was significantly (P < 0.01 higher in most of the samples of hepatopathic and nephropathic birds compared to healthy birds. Significant higher values (P < 0.01 of t1/2 K, AUC, and MRT and lower values of K and ClB in the hepatopathic and nephropathic birds in comparison to healthy birds were observed.

  8. Bismuth, lansoprazole, amoxicillin and metronidazole or clarithromycin as first-line Helicobacter pylori therapy.

    Science.gov (United States)

    Zhang, Wei; Chen, Qi; Liang, Xiao; Liu, Wenzhong; Xiao, Shudong; Graham, David Y; Lu, Hong

    2015-11-01

    To evaluate the efficacy and tolerability of replacing tetracycline with amoxicillin in bismuth quadruple therapy. Subjects who were infected with Helicobacter pylori and naïve to treatment were randomly (1:1) assigned to receive a 14-day modified bismuth quadruple therapy: lansoprazole 30 mg, amoxicillin 1 g, bismuth potassium citrate 220 mg (elemental bismuth), twice a day with metronidazole 400 mg four times a day (metronidazole group) or clarithromycin 500 mg twice a day (clarithromycin group). Six weeks after treatment, H. pylori eradication was assessed by 13C-urea breath test. Antimicrobial susceptibility was assessed by the twofold agar dilution method. This was a non-inferiority trial. Two hundred and fifteen subjects were randomised. Metronidazole and clarithromycin containing regimens achieved high cure rates: 94 of 97 (96.9%, 95% CI 93.5% to 100%) and 93 of 98 (94.9%, 95% CI 90.5% to 99.3%) by per-protocol and 88.9% (95% CI 83.0% to 94.8%) and 88.8% (95% CI 82.8% to 94.8%) by intention-to-treat, respectively. Amoxicillin, metronidazole and clarithromycin resistance rates were 1.5%, 45.5% and 26.5%, respectively. Only clarithromycin resistance reduced treatment success (e.g., susceptible 98.6%, resistant 76.9%, p=0.001). Adverse events were more common in the metronidazole group. These results suggest that amoxicillin can substitute for tetracycline in modified 14 day bismuth quadruple therapy as first-line treatment and still overcome metronidazole resistance in areas with high prevalence of metronidazole and clarithromycin resistance. Using clarithromycin instead of metronidazole was only effective in the presence of susceptible strains. NCT02175901. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://group.bmj.com/group/rights-licensing/permissions.

  9. Subcutaneous blood flow during insulin-induced hypoglycaemia

    DEFF Research Database (Denmark)

    Hilsted, J; Madsbad, S; Sestoft, L

    1982-01-01

    Subcutaneous blood flow was measured preceding insulin-induced hypoglycaemia, at the onset of hypoglycaemic symptoms and 2 h later in juvenile diabetics with and without autonomic neuropathy and in normal males. In all groups subcutaneous blood flow decreased at the onset of hypoglycaemic symptoms...... compared with pre-hypoglycaemic flow. Two hours after onset of hypoglycaemic symptoms, subcutaneous blood flow was still significantly decreased compared with pre-hypoglycaemic flow. In normal subjects local nerve blockade had no effect on blood flow changes during hypoglycaemia, whereas local alpha......-receptor blockade abolished the vasoconstrictor response. We suggest that circulating catecholamines stimulating vascular alpha-receptors are probably responsible for flow reduction in the subcutaneous tissue during hypoglycaemia....

  10. Severe subcutaneous generalized edema in a patient with dermatomyositis.

    Science.gov (United States)

    Ito, Yoshinaga; Kawabata, Daisuke; Yukawa, Naoichiro; Yoshifuji, Hajime; Usui, Takashi; Tanaka, Masao; Fujii, Takao; Mimori, Tsuneyo

    2007-01-01

    Subcutaneous generalized edema associated with dermatomyositis (DM)/polymyositis (PM) is extremely rare. Herein we report a case of severe subcutaneous generalized edema complicating DM. A 78-year-old woman was hospitalized in our department because of massive edema in the four limbs. Elevated muscle enzymes, heliotrope rash, results of electromyography, and muscle biopsy confirmed the diagnosis of DM. The absence of other diseases that could cause the symptoms indicated that massive edema was correlated with the pathophysiology of DM. Although myopathy and edema responded well to oral prednisolone, dysphagia persisted. We conclude that subcutaneous generalized edema can occur during the course of DM/PM, and subcutaneous vasculopathy may be involved in the pathogenesis of DM/PM.

  11. Pharmaceutical amyloidosis associated with subcutaneous insulin and enfuvirtide administration

    OpenAIRE

    D’Souza, Anita; Theis, Jason D.; Vrana, Julie A; Dogan, Ahmet

    2014-01-01

    Protein and peptide drugs administered subcutaneously, such as insulin can be amyloidogenic and result in localized amyloid deposits at the sites of medication injections. These iatrogenic amyloidoses typically present as a localized subcutaneous nodule or skin reaction at the site of administration, and often pose diagnostic challenges. We have analyzed the amyloid proteome in 52 cases of insulin and enfuvirtide associated amyloidosis using laser microdissection/tandem mass spectrometry. We ...

  12. Rescue Therapy for Helicobacter pylori Eradication: A Randomized Non-Inferiority Trial of Amoxicillin or Tetracycline in Bismuth Quadruple Therapy.

    Science.gov (United States)

    Chen, Qi; Zhang, Wei; Fu, Qingyan; Liang, Xiao; Liu, Wenzhong; Xiao, Shudong; Lu, Hong

    2016-12-01

    To compare the efficacy and safety of bismuth-containing quadruple therapy with tetracycline or amoxicillin for rescue treatment of Helicobacter pylori. The study was a non-inferiority trial of H. pylori eradication with at least two previous treatment failures. Subjects were randomized to receive 14-day therapy with b.i.d. lansoprazole 30 mg and bismuth 220 mg, plus metronidazole 400 mg q.i.d and amoxicillin 1 g t.i.d (amoxicillin group) or tetracycline 500 mg q.i.d (tetracycline group). Antimicrobial susceptibility was assessed by the agar-dilution method. Primary outcome was H. pylori eradication at 6 weeks after treatment. In all, 312 subjects were randomized, 13 were lost to follow-up; 29 violated the protocol. The intention-to-treat, per-protocol, and modified intention-to-treat eradication rates were (amoxicillin) 88.5% (138/156, 95% confidence interval (CI) 83.4-93.5%), 93.7% (133/142, 95% CI 89.7-97.7%), and 92.6% (138/149, 95% CI 88.4-96.8%). With tetracycline, they were 87.2% (136/156, 95% CI 81.9-92.4%), 95.3% (122/128, 95% CI 91.7-99.0%), and 90.7% (136/150, 95% CI 86.0-95.3%). Amoxicillin-, tetracycline-, and metronidazole-resistant rates were 8.3, 1.0, and 87.8%, respectively. Non-inferiority was confirmed (Pbismuth-containing quadruple therapy with metronidazole and amoxicillin is an alternative to classical bismuth quadruple therapy for H. pylori rescue treatment as it provides similar eradication with superior safety and compliance.

  13. Oral amoxicillin versus benzyl penicillin for severe pneumonia among kenyan children: a pragmatic randomized controlled noninferiority trial.

    Science.gov (United States)

    Agweyu, Ambrose; Gathara, David; Oliwa, Jacquie; Muinga, Naomi; Edwards, Tansy; Allen, Elizabeth; Maleche-Obimbo, Elizabeth; English, Mike

    2015-04-15

    There are concerns that the evidence from studies showing noninferiority of oral amoxicillin to benzyl penicillin for severe pneumonia may not be generalizable to high-mortality settings. An open-label, multicenter, randomized controlled noninferiority trial was conducted at 6 Kenyan hospitals. Eligible children aged 2-59 months were randomized to receive amoxicillin or benzyl penicillin and followed up for the primary outcome of treatment failure at 48 hours. A noninferiority margin of risk difference between amoxicillin and benzyl penicillin groups was prespecified at 7%. We recruited 527 children, including 302 (57.3%) with comorbidity. Treatment failure was observed in 20 of 260 (7.7%) and 21 of 261 (8.0%) of patients in the amoxicillin and benzyl penicillin arms, respectively (risk difference, -0.3% [95% confidence interval, -5.0% to 4.3%]) in per-protocol analyses. These findings were supported by the results of intention-to-treat analyses. Treatment failure by day 5 postenrollment was 11.4% and 11.0% and rising to 13.5% and 16.8% by day 14 in the amoxicillin vs benzyl penicillin groups, respectively. The most frequent cause of cumulative treatment failure at day 14 was clinical deterioration within 48 hours of enrollment (33/59 [55.9%]). Four patients died (overall mortality 0.8%) during the study, 3 of whom were allocated to the benzyl penicillin group. The presence of wheeze was independently associated with less frequent treatment failure. Our findings confirm noninferiority of amoxicillin to benzyl penicillin, provide estimates of risk of treatment failure in Kenya, and offer important additional evidence for policy making in sub-Saharan Africa. NCT01399723. © The Author 2014. Published by Oxford University Press on behalf of the Infectious Diseases Society of America.

  14. Proof of pore formation and biophysical perturbations through a 2D amoxicillin-lipid membrane interaction approach.

    Science.gov (United States)

    Lopes, Daniela; Nunes, Cláudia; Fontaine, Philippe; Sarmento, Bruno; Reis, Salette

    2017-05-01

    Amoxicillin is a worldwide used antibiotic, and it is classified as a first-line drug against Helicobacter pylori gastric infections. However, the current treatment of these infections has several limitations, such as the side effects and the low therapeutic compliance. Amoxicillin has been associated with gastrointestinal and renal side effects, with higher toxicity when the pH is lower. By considering this association and the well-known pH gradient of the gastric mucosa, this work aims to evaluate the influence of pH on the toxicity of amoxicillin. For that purpose, 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) monolayers were used since phosphatidylcholines are the most common phospholipid headgroup of biological membranes. To have insight of the effects of amoxicillin, different techniques were employed, namely, isotherm measurements, infrared reflection-absorption spectroscopy, grazing incident X-ray diffraction and Brewster angle microscopy. The monolayers of DPPC spread onto different buffer solutions (pH1.2, pH5 and pH7.4) showed different structural and packing properties. The interaction with amoxicillin also depended on the pH. At pH7.4, the highest effect was visualized at lower pressures, with partial restoration of the biophysical properties of the monolayer at 30 mN.m-1. A higher perturbation is shown at acidic pH, in which pores were visualized by Brewster angle microscopy. These perturbations may ultimately be related with amoxicillin toxicity. Copyright © 2017 Elsevier B.V. All rights reserved.

  15. Impact of amoxicillin therapy on resistance selection in patients with community-acquired lower respiratory tract infections : A randomized, placebo-controlled study

    NARCIS (Netherlands)

    Malhotra-Kumar, Surbhi; Van Heirstraeten, Liesbet; Coenen, Samuel; Lammens, Christine; Adriaenssens, Niels; Kowalczyk, Anna; Godycki-Cwirko, Maciek; Bielicka, Zuzana; Hupkova, Helena; Lannering, Christina; Mölstad, Sigvard; Fernandez-Vandellos, Patricia; Torres, Antoni; Parizel, Maxim; Ieven, Margareta; Butler, Chris C.; Verheij, Theo; Little, Paul; Goossens, Hermanon; Frimodt-Møller, Niels; Bruno, Pascale; Hering, Iris; Lemiengre, Marieke; Loens, Katherine; Malmvall, Bo Eric; Muras, Magdalena; Romano, Nuria Sanchez; Prat, Matteu Serra; Svab, Igor; Swain, Jackie; Tarsia, Paolo; Leus, Frank; Veen, Robert; Worby, Tricia

    2016-01-01

    Objectives: To determine the effect of amoxicillin treatment on resistance selection in patients with community-acquired lower respiratory tract infections in a randomized, placebo-controlled trial. Methods: Patients were prescribed amoxicillin 1 g, three times daily (n = 52) or placebo (n = 50) for

  16. Diurnal variations in subcutaneous allergen immunotherapy reactions.

    Science.gov (United States)

    Bavishi, Aakash A; Grammer, Leslie C; Pongracic, Jacqueline; Rychlik, Karen; Kumar, Rajesh; Zee, Phyllis; Greenberger, Paul A; Fishbein, Anna B

    2017-01-01

    Circadian rhythms underlie many immune responses and allergic diseases. Subcutaneous immunotherapy (SCIT) can result in adverse reactions; however, it is unclear whether such reactions have a diurnal pattern. To assess whether the timing of SCIT affects the rate of adverse reactions. This study was a retrospective medical record review of adult patients (n = 289) who received SCIT at the Northwestern Medical Faculty Foundation, Chicago, Illinois, during a 10-year period (2004-2014). Injections were given in the outpatient setting. There were a total of 17,457 injections with 574 reactions. Covariates included age, sex, median income, asthma status, vial contents, number of injections, and previous immunotherapy reactions. Logistical regression was used to calculate the odds of having a reaction with time of SCIT administration as the primary determinate. Immunotherapy reactions occurred more frequently after afternoon or evening (pm) injections (328/8721 = 3.8%) vs morning (am) injections (246/8736 = 2.8%), (χ2 = 12.26, P < .01). Systemic reactions, defined as World Allergy Organization grade 1 or higher, did not have diurnal variation (59/8721 = 0.67% for pm vs am 56/8736 = 0.64% for morning; χ2 = 0.08; P = .77). pm injections resulted in higher odds of reaction compared with am injection in a fully adjusted logistic regression model (odds ratio = 1.43; 95% confidence interval, 1.20-1.70; P < .01). When considering time as 4 categories, the highest odds of reaction were noted for the period from 15:01 to 17:30 (odds ratio, 1.55; 95% confidence interval, 1.21-2.00; P < .01). pm injections of SCIT are associated with increased cutaneous reaction rates when compared with am injections. In patients experiencing bothersome local reactions, it may be beneficial to administer SCIT in the morning. Copyright © 2016 American College of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  17. Intravenous and subcutaneous immunoglobulin G replacement therapy.

    Science.gov (United States)

    Bonilla, Francisco A

    2016-11-01

    Human polyclonal immunoglobulin G (IgG) for therapeutic use has been available for decades. This drug was developed for treatment of antibody deficiency (replacement therapy), although its use has expanded into many anti-inflammatory and immunomodulatory applications in recent years. This review focuses on IgG prescribing for replacement therapy. IgG for replacement is most often administered via the intravenous IgG (IVIG) or subcutaneous IgG (SCIG) routes. IVIG is usually administered every 34 weeks, and SCIG is usually administered weekly, although variations may be considered in all cases. Recently, a new product became available that uses hyaluronidase to facilitate absorption of large doses of SCIG less frequently (every 34 weeks, as with IVIG). There are important differences between the pharmacokinetics of these three routes of administration. IVIG therapy leads to high peaks and low troughs between infusions. IgG concentration fluctuates much less over time with SCIG. Hyaluronidase-facilitated SCIG is intermediate. SCIG may have lower bioavailability in comparison with IVIG and may require higher doses over time; this is not true for hyaluronidase SCIG. However, there are large variations in IgG half-life among individuals and with different products. Therefore, individualization of therapy is essential. Mild systemic flu-like adverse effects may affect up to 2025% of patients who receive IVIG, smaller fractions may experience more-severe symptoms, whereas anaphylaxis is exceedingly rare. General flu-like systemic adverse effects are minimal with SCIG (intermediate with hyaluronidase SCIG), but transient (24 hours), mild, local inflammatory symptoms at infusion sites are relatively common with both forms. Additional rare but important complications of IgG therapy include thrombotic events and hemolysis that can be seen at high doses with any route of administration. Renal adverse effects may occur with IVIG as well. The variety of IgG products and routes of

  18. Subcutaneous autologous serum therapy in chronic spontaneous urticaria

    Directory of Open Access Journals (Sweden)

    Kiran Vasant Godse

    2017-01-01

    Full Text Available Background: There is a felt need for trying newer therapeutic modalities in patients with chronic spontaneous urticaria, especially in the subset of patients classified as non-responders to antihistamines. Autologous serum therapy is an upcoming modality of treatment, and we decided to study its efficacy by subcutaneous route. Aims: To evaluate the effectiveness of subcutaneous autologous serum therapy (AST in CSU. Methods: This was a single blind, placebo-controlled parallel group, randomized, controlled study. Twenty-four patients with CSU (11M: 13 F were given subcutaneous AST and seventeen patients (7 M: 10F patients were given subcutaneous injection normal saline (placebo, along with levocetirizine in an on-demand basis in both groups. Results: Urticaria activity score (UAS came down from 35.74 to 7 at the end of 9 weeks and the patients' requirement of antihistamines also reduced remarkably from 5.8 to 1.7 per week in the serum group. Sub-cutaneous saline group did not show statistically significant fall in UAS. Saline group showed UAS 32.8 at zero week to 22.1 at the end of 9 weeks. DLQI showed significant fall in serum group, from 14.26 to 4 at the end of 9 weeks. Conclusion: Subcutaneous autoserum therapy is effective in treatment of CSU.

  19. Comparative Study of RP-HPLC and UV Spectrophotometric Techniques for the Simultaneous Determination of Amoxicillin and Cloxacillin in Capsules.

    Science.gov (United States)

    Giang, Do T; Hoang, Vu D

    2010-04-01

    Reversed-phase HPLC and UV spectrophotometric techniques using water as solvent have been developed and validated for the simultaneous determination of amoxicillin and cloxacillin in capsules. For both techniques, the linearity range of 60.073x2013;140.0 µg/mL was studied. The spectrophotometric data show that non-derivative techniques, such as absorbance ratio and compensation, and ratio spectra first-order derivative could be successfully used for the co-assay of amoxicillin and cloxacillin. Based on the statistical comparison of spectrophotometric and chromatographic data, the interchangeability between HPLC and UV spectrophotometric techniques has been suggested for the routine analysis.

  20. Controlled release of human growth hormone fused with a human hybrid Fc fragment through a nanoporous polymer membrane

    Science.gov (United States)

    Kim, Eung-Sam; Jang, Do Soo; Yang, Seung Yun; Lee, Mi Nam; Jin, Kyeong Sik; Cha, Hyung Jin; Kim, Jin Kon; Sung, Young Chul; Choi, Kwan Yong

    2013-05-01

    Nanotechnology has been applied to the development of more effective and compatible drug delivery systems for therapeutic proteins. Human growth hormone (hGH) was fused with a hybrid Fc fragment containing partial Fc domains of human IgD and IgG4 to produce a long-acting fusion protein. The fusion protein, hGH-hyFc, resulted in the increase of the hydrodynamic diameter (ca. 11 nm) compared with the diameter (ca. 5 nm) of the recombinant hGH. A diblock copolymer membrane with nanopores (average diameter of 14.3 nm) exhibited a constant release rate of hGH-hyFc. The hGH-hyFc protein released in a controlled manner for one month was found to trigger the phosphorylation of Janus kinase 2 (JAK2) in human B lymphocyte and to exhibit an almost identical circular dichroism spectrum to that of the original hGH-hyFc, suggesting that the released fusion protein should maintain the functional and structural integrity of hGH. Thus, the nanoporous release device could be a potential delivery system for the long-term controlled release of therapeutic proteins fused with the hybrid Fc fragment.Nanotechnology has been applied to the development of more effective and compatible drug delivery systems for therapeutic proteins. Human growth hormone (hGH) was fused with a hybrid Fc fragment containing partial Fc domains of human IgD and IgG4 to produce a long-acting fusion protein. The fusion protein, hGH-hyFc, resulted in the increase of the hydrodynamic diameter (ca. 11 nm) compared with the diameter (ca. 5 nm) of the recombinant hGH. A diblock copolymer membrane with nanopores (average diameter of 14.3 nm) exhibited a constant release rate of hGH-hyFc. The hGH-hyFc protein released in a controlled manner for one month was found to trigger the phosphorylation of Janus kinase 2 (JAK2) in human B lymphocyte and to exhibit an almost identical circular dichroism spectrum to that of the original hGH-hyFc, suggesting that the released fusion protein should maintain the functional and