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Sample records for aripiprazole active ingredient

  1. Aripiprazole

    Science.gov (United States)

    ... bipolar disorder (manic-depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods). Aripiprazole is also used with an antidepressant to treat depression when symptoms cannot ... difficulty communicating and interacting with others). Aripiprazole may ...

  2. Effects of aripiprazole on caffeine-induced hyperlocomotion and neural activation in the striatum.

    Science.gov (United States)

    Batista, Luara A; Viana, Thércia G; Silveira, Vívian T; Aguiar, Daniele C; Moreira, Fabrício A

    2016-01-01

    Aripiprazole is an antipsychotic that acts as a partial agonist at dopamine D2 receptors. In addition to its antipsychotic activity, this compound blocks the effects of some psychostimulant drugs. It has not been verified, however, if aripiprazole interferes with the effects of caffeine. Hence, this study tested the hypothesis that aripiprazole prevents caffeine-induced hyperlocomotion and investigated the effects of these drugs on neural activity in the striatum. Male Swiss mice received injections of vehicle or antipsychotic drugs followed by vehicle or caffeine. Locomotion was analyzed in a circular arena and c-Fos protein expression was quantified in the dorsolateral, dorsomedial, and ventrolateral striatum, and in the core and shell regions of nucleus accumbens. Aripiprazole (0.1, 1, and 10 mg/kg) prevented caffeine (10 mg/kg)-induced hyperlocomotion at doses that do not change basal locomotion. Haloperidol (0.01, 0.03, and 0.1 mg/kg) also decreased caffeine-induced hyperlocomotion at all doses, although at the two higher doses, this compound reduced basal locomotion. Immunohistochemistry analysis showed that aripiprazole increases c-Fos protein expression in all regions studied, whereas caffeine did not alter c-Fos protein expression. Combined treatment of aripiprazole and caffeine resulted in a decrease in the number of c-Fos positive cells as compared to the group receiving aripiprazole alone. In conclusion, aripiprazole prevents caffeine-induced hyperlocomotion and increases neural activation in the striatum. This latter effect is reduced by subsequent administration of caffeine. These results advance our understanding on the pharmacological profile of aripiprazole.

  3. No difference in frontal cortical activity during an executive functioning task after acute doses of aripiprazole and haloperidol

    Directory of Open Access Journals (Sweden)

    Ingeborg eBolstad

    2015-05-01

    Full Text Available Background: Aripiprazole is an atypical antipsychotic drug that is characterized by partial dopamine D2 receptor agonism. Its pharmacodynamic profile is proposed to be beneficial in the treatment of cognitive impairment, which is prevalent in psychotic disorders. This study compared brain activation characteristics produced by aripiprazole with that of haloperidol, a typical D2 receptor antagonist, during a task targeting executive functioning.Methods: Healthy participants received an acute oral dose of haloperidol, aripiprazole or placebo before performing an executive functioning task while blood-oxygen-level-dependent (BOLD functional magnetic resonance imaging (fMRI was carried out. Results: There was a tendency towards reduced performance in the aripiprazole group compared to the two other groups. The image analysis yielded a strong task-related BOLD-fMRI response within each group. An uncorrected between-group analysis showed that aripiprazole challenge resulted in stronger activation in the frontal and temporal gyri and the putamen compared with haloperidol challenge, but after correcting for multiple testing there was no significant group difference. Conclusion: No significant group differences between aripiprazole and haloperidol in frontal cortical activation were obtained when corrected for multiple comparisons.This study is registered in ClinicalTrials.gov (identifier: 2009-016222-14; https://clinicaltrials.gov/.

  4. Different effects of bifeprunox, aripiprazole, and haloperidol on body weight gain, food and water intake, and locomotor activity in rats.

    Science.gov (United States)

    De Santis, Michael; Pan, Bo; Lian, Jiamei; Huang, Xu-Feng; Deng, Chao

    2014-09-01

    Following on the success of Aripiprazole with its high clinical efficacy and minimal side effects, further antipsychotic drugs (such as Bifeprunox) have been developed based on the same dopamine D2 partial agonist pharmacological profile as Aripiprazole. However clinical trials of Bifeprunox have found differing results to that of its predecessor, without the same significant clinical efficacy. This study has therefore investigated the different effects of 10 week treatment with Aripiprazole (0.75 mg/kg, 3 times per day), Bifeprunox (0.8 mg/kg, 3 times per day) and Haloperidol (0.1mg/kg, 3 times per day) on body weight gain, food and water intake, white fat mass, and 8 week treatment on locomotor activity. Treatment with Bifeprunox was found to significantly reduce all of the measured parameters except white fat mass compared to the control group. However, Aripiprazole and Haloperidol treatment reduced water intake compared to the control, without any significant effects on the other measured parameters. These findings further demonstrate the potential pharmacological differences between Aripiprazole and Bifeprunox, and identify potential weight loss side effects and increased anxiety behaviour with Bifeprunox treatment. Copyright © 2014 Elsevier Inc. All rights reserved.

  5. Oil Dispersion with Abamectin as Active Ingredient

    Directory of Open Access Journals (Sweden)

    Slavica Gašić

    2011-01-01

    Full Text Available Abamectin was developed as an insecticide, nematocide and acaricide for use on a varietyof agricultural and horticultural crops. The products with this active ingredient can befound on the market mostly formulated as emulsifiable concentrate (EC. Usually producersrecommend using the EC formulation of abamectin together with some kind of adjuvants(natural oils to improve efficacy of the active ingredient. To overcome the efficacy problemwe tried to formulate the active ingredient abamectin as oil dispersion (OD. Oil dispersion,preferably based on naturally derived oils could improve pesticide efficacy. This type of pesticideformulation contains oil instead of water as in classical suspension concentrate andtypically has better retention and coverage. In the case of abamectin, in this investigationsoybean oil was used with the mixture of different nonionic emulsifiers. Content of abamecetinin formulation was 1.8 %. The developed formulation was tested for few importantparameters. The obtained physicochemical properties for the above mentioned formulationhave shown that it is stable and could be used in plant protection.

  6. 21 CFR 344.12 - Ear drying aid active ingredient.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Ear drying aid active ingredient. 344.12 Section 344.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED....12 Ear drying aid active ingredient. The active ingredient of the product consists of...

  7. 21 CFR 358.310 - Ingrown toenail relief active ingredient.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Ingrown toenail relief active ingredient. 358.310... (CONTINUED) DRUGS FOR HUMAN USE MISCELLANEOUS EXTERNAL DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Ingrown Toenail Relief Drug Products § 358.310 Ingrown toenail relief active ingredient. The active ingredient...

  8. Polyphenols as active ingredients for cosmetic products.

    Science.gov (United States)

    Zillich, O V; Schweiggert-Weisz, U; Eisner, P; Kerscher, M

    2015-10-01

    Polyphenols are secondary plant metabolites with antioxidant, anti-inflammatory and anti-microbial activity. They are ubiquitously distributed in the plant kingdom; high amounts contain, for example, green tea and grape seeds. Polyphenolic extracts are attractive ingredients for cosmetics and pharmacy due to their beneficial biological properties. This review summarizes the effects of polyphenols in the context of anti-ageing activity. We have explored in vitro studies, which investigate antioxidant activity, inhibition of dermal proteases and photoprotective activity, mostly studied using dermal fibroblasts or epidermal keratinocytes cell lines. Possible negative effects of polyphenols were also discussed. Further, some physicochemical aspects, namely the possible interactions with emulsifiers and the influence of the cosmetic formulation on the skin delivery, were reported. Finally, few clinical studies, which cover the anti-ageing action of polyphenols on the skin after topical application, were reviewed.

  9. Aripiprazole salts. II. Aripiprazole perchlorate.

    Science.gov (United States)

    Freire, Eleonora; Polla, Griselda; Baggio, Ricardo

    2012-06-01

    The molecular structure of aripiprazole perchlorate (systematic name: 4-(2,3-dichlorophenyl)-1-{4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl}piperazin-1-ium perchlorate), C(23)H(28)Cl(2)N(3)O(2)(+)·ClO(4)(-), does not differ substantially from the recently published structure of aripiprazole nitrate [Freire, Polla & Baggio (2012). Acta Cryst. C68, o170-o173]. Both compounds have almost identical bond distances, bond angles and torsion angles. The two different counter-ions occupy equivalent places in the two structures, giving rise to very similar first-order `packing motifs'. However, these elemental arrangements interact with each other in different ways in the two structures, leading to two-dimensional arrays with quite different organizations.

  10. Choleretic Activity of Turmeric and its Active Ingredients.

    Science.gov (United States)

    Wang, Yonglu; Wang, Liyao; Zhu, Xinyi; Wang, Dong; Li, Xueming

    2016-07-01

    Turmeric, a rhizome of Curcumin longa L. is widely used as both a spice and an herbal medicine. The traditional use of turmeric in gastroenterology is mainly based on its choleretic activity. The aim of this study is to determine the effects of turmeric on bile flow (BF) and total bile acids (TBAs) excretion in a bile fistula rat model after acute duodenal administration. A significant dose-dependent enhancement in both BF and TBAs was detected after treatment with the turmeric decoctions which suggested the choleretic activity was bile acid-dependent secretion. In order to direct the active group of compounds, aqueous (AE), ethyl acetate (EtOAc), and petroleum ether (PE) extracts were investigated. The EtOAc and PE extracts showing high effects were purified to locate the active ingredients. Three curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin) and 2 sesquiterpenes (bisacurone B and ar-turmerone) were isolated. It was found Bisacurone B was the most potent choleretic ingredient followed by ar-turmerone, bisdemethoxycurcumin demethoxycurcumin, and then curcumin. The amounts of the active ingredients were quantitatively analyzed by high-performance liquid chromatography. The EtOAc and PE extracts had high sesquiterpenes and curcuminoids content, while the AE extract had poor content of sesquiterpenes and curcuminoids which affected neither BF nor TBAs. Based on the results of multiple linear regression analysis, the content of BIS and TUR were dominant factors (P < 0.01) of controlling BL and TBAs in EtOAC and PE extracts.

  11. Effects of aripiprazole versus risperidone on brain activation during planning and social-emotional evaluation in schizophrenia: A single-blind randomized exploratory study.

    Science.gov (United States)

    Liemburg, Edith J; van Es, Frank; Knegtering, Henderikus; Aleman, André

    2017-10-03

    Impaired function of prefrontal brain networks may be the source of both negative symptoms and neurocognitive problems in psychotic disorders. Whereas most antipsychotics may decrease prefrontal activation, the partial dopamine D2-receptor agonist aripiprazole is hypothesized to improve prefrontal function. This study investigated whether patients with a psychotic disorder would show stronger activation of prefrontal areas and associated regions after treatment with aripiprazole compared to risperidone treatment. In this exploratory pharmacological neuroimaging study, 24 patients were randomly assigned to either aripiprazole or risperidone. At baseline and after nine weeks treatment they underwent an interview and MRI session. Here we report on brain activation (measured with arterial spin labeling) during performance of two tasks, the Tower of London and the Wall of Faces. Aripiprazole treatment decreased activation of the middle frontal, superior frontal and occipital gyrus (ToL) and medial temporal and inferior frontal gyrus, putamen and cuneus (WoF), while activation increased after risperidone. Activation increased in the ventral anterior cingulate and posterior insula (ToL), and superior frontal, superior temporal and precentral gyrus (WoF) after aripiprazole treatment and decreased after risperidone. Both treatment groups had increased ventral insula activation (ToL) and middle temporal gyrus (WoF), and decreased occipital cortex, precuneus and caudate head activation (ToL) activation. In conclusion, patients treated with aripiprazole may need less frontal resources for planning performance and may show increased frontotemporal and frontostriatal reactivity to emotional stimuli. More research is needed to corroborate and extend these preliminary findings. Copyright © 2017 Elsevier Inc. All rights reserved.

  12. A survey of Chinese herbal ingredients with liver protection activities

    Directory of Open Access Journals (Sweden)

    Lien Linda

    2007-05-01

    Full Text Available Abstract A literature survey was conducted on herbs, their preparations and ingredients with reported liver protection activities, in which a total of 274 different species and hundreds of active ingredients have been examined. These ingredients can be roughly classified into two categories according to their activities: (1 the main ingredients, such as silybin, osthole, coumarin, glycyrrhizin, saikosaponin A, schisandrin A, flavonoids; and (2 supporting substances, such as sugars, amino acids, resins, tannins and volatile oil. Among them, some active ingredients have hepatoprotective activities (e.g. anti-inflammatory, anticancer, antioxidant, immunomodulating and liver cirrhosis-regulating effects. Calculation of physicochemical parameters indicates that the main ingredients with negative and positive Elumo values possibly display their hepatoprotective effects through different mechanisms, such as antioxidative, anti-inflammatory and immunomodulating effects. As the combination of herbs may achieve some treatment effects synergistically and/or additively, it is common in Chinese medicine to use mixtures of various medicinal herbs with pharmacologically active compounds to have synergistic and/or additive effects, or to reduce harmful effects of some pharmacologically active compounds. In particular, the active compounds with Clog P around 2 are suitable for passive transport across membranes and accessible to the target sites. Thus, Elumo and Clog P values are good indicators among the calculated parameters. Seven different physicochemical parameters (MW, Clog P, CMR, μ, Ehomo, Elumo and Hf and four major biological activities (antioxidant, anti-inflammatory, antiviral/antitumor and immunomodulating are discussed in this review. It is hoped that the discussion may provide some leads in the development of new hepatoprotective drugs.

  13. Downstream Processability of Crystal Habit-Modified Active Pharmaceutical Ingredient

    DEFF Research Database (Denmark)

    Pudasaini, Nawin; Upadhyay, Pratik Pankaj; Parker, Christian Richard

    2017-01-01

    Efficient downstream processing of active pharmaceutical ingredients (APIs) can depend strongly on their particulate properties, such as size and shape distributions. Especially in drug products with high API content, needle-like crystal habit of an API may show compromised flowability and tablet......Efficient downstream processing of active pharmaceutical ingredients (APIs) can depend strongly on their particulate properties, such as size and shape distributions. Especially in drug products with high API content, needle-like crystal habit of an API may show compromised flowability...

  14. Lipases: particularly effective biocatalysts for cosmetic active ingredients

    Directory of Open Access Journals (Sweden)

    Yvergnaux Florent

    2017-07-01

    Full Text Available Enzymes are the tools of choice in the on-going quest for non-pollutant processes to discover molecules for use in skin products. Amongst these biocatalysts, lipases offer considerable potential in terms of ingredient development and are of interest in skin dermocosmetic formulations possessing sensory or biological activities. Lipases have been studied for around thirty years and, in most cases, these enzymes function under what are deemed to be mild conditions, displaying remarkable efficacy particularly in terms of selectivity. This particularly effective strategy will be illustrated through typical synthesis, demonstrating how ester or amide active ingredients are obtained.

  15. 21 CFR 341.12 - Antihistamine active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Antihistamine active ingredients. 341.12 Section 341.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE COLD, COUGH, ALLERGY, BRONCHODILATOR, AND ANTIASTHMATIC DRUG PRODUCTS FOR...

  16. ANTIOXIDANT AND ANTITUMOR ACTIVITY OF INDONESIAN HERBAL INGREDIENTS

    OpenAIRE

    2015-01-01

    The present study was to aimed to evaluated and compare in vitro antioxidant activities of 2 Indonesian herbal ingredients (A and B), determined total phenol content., cytotoxic and apoptosis induction activities on HL-60 cells. These data were providing some useful information for people healthy dietary and the new potential application of natural antioxidant containing food materials in functional foods and also as new cancer therapeutics promising candidates. The parameters were total anti...

  17. Preparation and evaluation of combination tablet containing incompatible active ingredients.

    Science.gov (United States)

    Wang, Xiaoyan; Cui, Fude; Yonezawa, Yorinobu; Sunada, Hisakazu

    2003-07-01

    Combination preparation plays an important role in clinical treatment because of its better and wider curative synergism and weaker side effects. However, the existence of incompatibility between active ingredients or between active ingredients and excipients presents a serious obstacle in the preparation of such combination solid dosage forms. In this study, aspirin and ranitidine hydrochloride, between which there existed a chemical interaction, were selected as model drugs. Aspirin powders without any additives were granulated with hydroxypropyl methyl cellulose (HPMC) water solution as a binder using a Wurster coating apparatus and the operation conditions were optimized by Artificial Neural Network (ANN) analysis. Under these conditions, the aspirin granules prepared showed good flowability and compressibility. On the other hand, ranitidine hydrochloride was coated with Aquacoat (ethyl cellulose aqueous dispersion) after preliminary granulation with the Wurster coating apparatus. The aspirin granules and coated ranitidine hydrochloride particles were compressed into tablets with suitable excipients. The combination tablets showed good dissolution, content uniformity and improved stability of active ingredients.

  18. The cardiac safety of aripiprazole treatment in patients at high risk for torsade

    DEFF Research Database (Denmark)

    Polcwiartek, Christoffer; Sneider, Benjamin; Graff, Claus;

    2015-01-01

    prolongation risk was lower compared with placebo and active controls. Epidemiological studies linked aripiprazole to weak/moderate torsadogenicity. No studies were found associating aripiprazole with BrS suggesting low affinity for the fast sodium current. CONCLUSIONS: Aripiprazole is a low-risk antipsychotic...

  19. 75 FR 6386 - Pesticide Products; Registration Applications for a New Active Ingredient Chemical; Demiditraz

    Science.gov (United States)

    2010-02-09

    ... register pesticide products containing active ingredients not included in any previously registered pesticide products. Pursuant to the provisions of section 3(c)(4) of the Federal Insecticide, Fungicide, and... AGENCY Pesticide Products; Registration Applications for a New Active Ingredient Chemical;...

  20. Nano-microdelivery systems for oral delivery of an active ingredient

    DEFF Research Database (Denmark)

    2014-01-01

    A composition for oral delivery of one or more active ingredients in the form of a lipid nano-micro-delivery system comprising a lipid nano-micro-structure comprising at least one lipid and at least one active ingredient, said at least one active ingredient being immobilized in said lipid nano...

  1. Aripiprazole (Otsuka Pharmaceutical Co).

    Science.gov (United States)

    Ozdemir, Vural; Fourie, Jeanne; Ozdener, Fatih

    2002-01-01

    Otsuka Pharmaceuticals in collaboration with Bristol-Myers Squibb is developing aripiprazole, a dual dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist, for the potential treatment of psychoses including schizophrenia [281327], [340364]. A regulatory filing for schizophrenia in the US was submitted at the end of 2001 [340364]. The compound entered phase III trials in Japan in 1995 [192966]. Although presynaptic dopamine autoreceptor agonists may be efficacious in the treatment of schizophrenia, they may also potentially increase the risk for exacerbation of psychosis through stimulation of postsynaptic dopaminergic receptors [245791], [350478], [350479]. However, earlier neuropharmacology studies have shown that aripiprazole can act as a presynaptic D2 agonist while displaying an antagonistic effect at the postsynaptic D2 receptors [281327], [337126], [350479], [424587], [424588]. In animal models, aripiprazole inhibits the apomorphine-induced stereotypy, without causing catalepsy [281327], [337126]. Moreover, in contrast to classical antipsychotics that produce disabling movement disorders, aripiprazole does not cause an upregulation of D2 receptors or an increase in expression of the c-fos mRNA in the striatum, in agreement with the low risk for extrapyramidal side effects (EPS) during aripiprazole treatment [245781], [262096], [350481], [350483]. Collectively, aripiprazole is an important atypical antipsychotic candidate with a favorable safety profile. Moreover, the mechanism of action of aripiprazole differentiates it from both typical and atypical antipsychotics and hence, may provide important leads for pharmacotherapy of schizophrenia and other psychotic disorders. In January 2000, Lehman Brothers predicted peak sales of aripiprazole could reach US $500 million [357788]. In February 2001, Credit Suisse First Boston predicted sales of US $403 million in 2005 [399484].

  2. Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release.

    Science.gov (United States)

    Cosi, Cristina; Carilla-Durand, Elisabeth; Assié, Marie Bernadette; Ormiere, Anne Marie; Maraval, Mireille; Leduc, Nathalie; Newman-Tancredi, Adrian

    2006-03-27

    Dopamine D2 receptor antagonists induce hyperprolactinemia depending on the extent of D2 receptor blockade. We compared the effects of the new antipsychotic agents SSR181507 ((3-exo)-8-benzoyl-N-[[(2 s)7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl]methyl]-8-azabicyclo[3.2.1]octane-3-methanamine monohydrochloride), bifeprunox (DU127090: 1-(2-Oxo-benzoxazolin-7-yl)-4-(3-biphenyl)methylpiperazinemesylate) and SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4-[5-(4-fluorophenyl)-pyridin-3-ylmethyl]-piperazine) with those of aripiprazole (7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-butyloxy)-3,4-dihydro-2(1 H)-quinolinone), clozapine and haloperidol, on functional measures of dopamine D2 receptor activity in vitro and in vivo: [35S]-GTPgammaS binding to membranes from Sf9 insect cells expressing human dopamine D2 Long (hD2 L) receptors, and serum prolactin levels in the rat. All compounds antagonized apomorphine-induced G protein activation at dopamine hD2 L receptors. Antagonist potencies of aripiprazole, bifeprunox and SLV313 were similar to haloperidol (pK(b) = 9.12), whereas SSR181507 (8.16) and clozapine (7.35) were less potent. Haloperidol, SLV313 and clozapine were silent antagonists but SSR181507, bifeprunox and aripiprazole stimulated [35S]-GTPgammaS binding by 17.5%, 26.3% and 25.6%, respectively, relative to 100 microM apomorphine (Emax = 100%). pEC50s were: SSR181507, 8.08; bifeprunox, 8.97; aripiprazole, 8.56. These effects were antagonized by raclopride. Following oral administration in vivo, the drugs increased prolactin release to different extents. SLV313 and haloperidol potently (ED50 0.12 and 0.22 mg/kg p.o., respectively) stimulated prolactin release up to 86 and 83 ng/ml. Aripiprazole potently (ED50 0.66 mg/kg p.o.) but partially (32 ng/ml) induced prolactin release. SSR181507 (ED50 4.9 mg/kg p.o.) also partially (23 ng/ml) enhanced prolactin release. Bifeprunox only weakly increased prolactin at high doses (13 ng/ml at 40 mg/kg) and clozapine only

  3. Active ingredients in anti-stigma programmes in mental health.

    Science.gov (United States)

    Pinfold, Vanessa; Thornicroft, Graham; Huxley, Peter; Farmer, Paul

    2005-04-01

    This paper draws upon a review of the relevant literature and the results of the recent Mental Health Awareness in Action (MHAA) programme in England to discuss the current evidence base on the active ingredients in effective anti-stigma interventions in mental health. The MHAA Programme delivered educational interventions to 109 police officers, 78 adults from different community groups whose working lives involved supporting people with mental health problems but who had received no mental health training and 472 schools students aged 14-15. Each adult target group received two intervention sessions lasting two hours. The two school lessons were 50 minutes each. Knowledge, attitudes and behavioural intent were assessed at baseline and follow-up. In addition focus groups were held with mental health service users to explore the impact of stigma on their lives and facilitators of educational workshops were interviewed to provide expert opinion on 'what works' to reduce psychiatric stigma. Personal contact was predictive of positive changes in knowledge and attitudes for the school students but not the police officers or community adult group. The key active ingredient identified by all intervention groups and workshop facilitators were the testimonies of service users. The statements of service users (consumers) about their experience of mental health problems and of their contact with a range of services had the greatest and most lasting impact on the target audiences in terms of reducing mental health stigma.

  4. Photocatalytic degradation of sunscreen active ingredients mediated by nanostructured materials

    Science.gov (United States)

    Soto-Vazquez, Loraine

    Water scarcity and pollution are environmental issues with terrible consequences. In recent years several pharmaceutical and personal care products, such as sunscreen active ingredients, have been detected in different water matrices. Its recalcitrant behavior in the environment has caused controversies and generated countless questions about its safety. During this research, we employed an advanced oxidation process (photocatalysis) to degrade sunscreen active ingredients. For this study, we used a 3x3 system, evaluating three photocatalysts and three different contaminants. From the three catalysts employed, two of them were synthesized. ZnO nanoparticles were obtained using zinc acetate dihydrated as the precursor, and TiO2 nanowires were synthesized from titanium tetrachloride precursor. The third catalyst employed (namely, P25) was obtained commercially. The synthesized photocatalysts were characterized in terms of the morphology, elemental composition, crystalline structure, elemental oxidation states, vibrational modes and surface area, using SEM-EDS, XRD, XPS, Raman spectroscopy and BET measurements, respectively. The photocatalysts were employed during the study of the degradation of p-aminobenzoic acid, phenylbenzimidazole sulfonic acid, and benzophenone-4. In all the cases, at least 50% degradation was achieved. P25 showed degradation efficiencies above 90%, and from the nine systems, 7 of them degraded at least 86%.

  5. Plant Cell Cultures as Source of Cosmetic Active Ingredients

    Directory of Open Access Journals (Sweden)

    Ani Barbulova

    2014-04-01

    Full Text Available The last decades witnessed a great demand of natural remedies. As a result, medicinal plants have been increasingly cultivated on a commercial scale, but the yield, the productive quality and the safety have not always been satisfactory. Plant cell cultures provide useful alternatives for the production of active ingredients for biomedical and cosmetic uses, since they represent standardized, contaminant-free and biosustainable systems, which allow the production of desired compounds on an industrial scale. Moreover, thanks to their totipotency, plant cells grown as liquid suspension cultures can be used as “biofactories” for the production of commercially interesting secondary metabolites, which are in many cases synthesized in low amounts in plant tissues and differentially distributed in the plant organs, such as roots, leaves, flowers or fruits. Although it is very widespread in the pharmaceutical industry, plant cell culture technology is not yet very common in the cosmetic field. The aim of the present review is to focus on the successful research accomplishments in the development of plant cell cultures for the production of active ingredients for cosmetic applications.

  6. Aripiprazole Augmentation in Childhood Obsessive-Compulsive Disorder: Three Case Reports

    Directory of Open Access Journals (Sweden)

    Murat Yuce

    2013-08-01

    Full Text Available Aripiprazole is a third generation antipsychotic that has a partial dopamine agonistic activity. There is an increasing usage of aripiprazole in children and adolescents with schizophrenia, pervasive developmental disorders, and bipolar disorders. In these presentation, we aimed to present three pediatric obsessive%u2013compulsive disorder (OCD cases who were resistant to two different selective serotonin reuptake inhibitor treatments and prescribed aripiprazole for augmentation therapy. The results of these three cases suggest that aripiprazole is an effective and safe alternative as augmentation for childhood OCD treatment. However, to investigate the efficacy and safety of aripiprazole in childhood OCD, randomized controlled treatment studies are needed.

  7. 77 FR 48519 - Registration Applications for Pesticide Products Containing New Active Ingredients

    Science.gov (United States)

    2012-08-14

    ... be affected. The North American Industrial Classification System (NAICS) codes have been provided to..., 235 South Kresson Street, Baltimore, MD 21224-2616. Active Ingredient: Bacillus thuringiensis...

  8. 21 CFR 341.14 - Antitussive active ingredients.

    Science.gov (United States)

    2010-04-01

    ...) DRUGS FOR HUMAN USE COLD, COUGH, ALLERGY, BRONCHODILATOR, AND ANTIASTHMATIC DRUG PRODUCTS FOR OVER-THE... established for each ingredient in § 341.74(d): (a) Oral antitussives. (1) Chlophedianol hydrochloride....

  9. 21 CFR 358.110 - Wart remover active ingredients.

    Science.gov (United States)

    2010-04-01

    ... ingredient. (a) Salicylic acid 12 to 40 percent in a plaster vehicle. (b) Salicylic acid 5 to 17 percent in a collodion-like vehicle. (c) Salicylic acid 15 percent in a karaya gum, glycol plaster vehicle....

  10. Active ingredients of substance use-focused self-help groups.

    Science.gov (United States)

    Moos, Rudolf H

    2008-03-01

    This paper provides an overview of some of the probable active ingredients of self-help groups in light of four related theories that identify common social processes that appear to underlie effective psychosocial treatments for and continuing remission from these disorders. Social control theory specifies active ingredients such as bonding, goal direction and structure; social learning theory specifies the importance of norms and role models, behavioral economics and behavioral choice theory emphasizes involvement in rewarding activities other than substance use, and stress and coping theory highlights building self-efficacy and effective coping skills. A review of existing studies suggests that the emphasis on these active ingredients probably underlies some aspects of the effectiveness of self-help groups. Several issues that need to be addressed to enhance understanding of the active ingredients of action of self-help groups are discussed, including consideration of indices of Alcoholics Anonymous (AA) affiliation as active ingredients, identification of personal characteristics that may moderate the influence of active ingredients on substance use outcomes, examination of whether active ingredients of self-help groups, can amplify or compensate for treatment, identification of potential detrimental effects of involvement in self-help groups and focusing on the link between active ingredients of self-help groups and other aspects of the overall recovery milieu, such as the family and social networks.

  11. Selecting an optimal instrument to identify active ingredients of the motivational interviewing-process

    NARCIS (Netherlands)

    Dobber, Jos; Meijel, Berno van; Barkhof, Emile; Scholte op Reimer, Wilma; Latour, Corine; Peters, Ron; Linszen, Don

    2014-01-01

    Motivational Interviewing (MI) can effectively stimulate motivation for health behavior change, but the active ingredients of MI are not well known. To help clinicians further stimulate motivation, they need to know the active ingredients of MI. A psychometrically sound instrument is required to ide

  12. 75 FR 53691 - Pesticide Products; Registration Applications for a New Active Ingredient Chemical Sedaxane

    Science.gov (United States)

    2010-09-01

    ... AGENCY Pesticide Products; Registration Applications for a New Active Ingredient Chemical Sedaxane AGENCY... pesticide products containing an active ingredient not included in any previously registered pesticide products. Pursuant to the provisions of section 3(c)(4) of the Federal Insecticide, Fungicide,...

  13. Using Indices of Fidelity to Intervention Core Components to Identify Program Active Ingredients

    Science.gov (United States)

    Abry, Tashia; Hulleman, Chris S.; Rimm-Kaufman, Sara E.

    2015-01-01

    Identifying the active ingredients of an intervention--intervention-specific components serving as key levers of change--is crucial for unpacking the intervention black box. Measures of intervention fidelity can be used to identify specific active ingredients, yet such applications are rare. We illustrate how fidelity measures can be used to…

  14. 21 CFR 346.16 - Analgesic, anesthetic, and antipruritic active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Analgesic, anesthetic, and antipruritic active ingredients. 346.16 Section 346.16 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE ANORECTAL DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Active Ingredients § 346.16 Analgesic,...

  15. 21 CFR 348.10 - Analgesic, anesthetic, and antipruritic active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Analgesic, anesthetic, and antipruritic active ingredients. 348.10 Section 348.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE EXTERNAL ANALGESIC DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Active Ingredients § 348.10 Analgesi...

  16. Effects of active pharmaceutical ingredients mixtures in mussel Mytilus galloprovincialis.

    Science.gov (United States)

    Gonzalez-Rey, M; Mattos, J J; Piazza, C E; Bainy, A C D; Bebianno, M J

    2014-08-01

    Active pharmaceutical ingredients (APIs) are emergent environmental contaminants widely detected in surface waters as result of incomplete waste water treatment plant (WWTP) removal processes and improper disposal. The assessment of potential effects of APIs on non-target organisms is still scarce since besides presenting multiple chemical structures, properties and modes of action, these compounds occur as complex mixtures. This study comprises a 15-day exposure of mussels Mytilus galloprovincialis to mixtures (at environmentally relevant nominal concentrations) of non-steroidal inflammatory drugs ibuprofen (IBU) and diclofenac (DCF) (250 ng L(-1) each) and selective serotonin reuptake inhibitor (SSRI) fluoxetine (FLX) (75 ng L(-1)) (MIX 1) along with the addition of classical pro-oxidant copper (Cu) (5 μg L(-1)) (MIX 2). The goals included the assessment of oxidative stress, neurotoxic and endocrine effects on this sentinel species applying both a multibiomarker and gene expression (here and later gene expression is taken as synonym to gene transcription, although it is acknowledged that it is also affected by, e.g. translation, and mRNA and protein stability) analysis approaches. The results revealed a swifter antioxidant response in digestive glands than in gills induced by MIX 1, nevertheless the presence of Cu in MIX 2 promoted a higher lipid peroxidation (LPO) induction. Neither mixture altered acetylcholinesterase (AChE) activity, while both triggered the formation of vitellogenin-like proteins in females confirming the xenoestrogenic effect of mixtures. All these results varied with respect to those obtained in previous single exposure essays. Moreover, RT-PCR analysis revealed a catalase (CAT) and CYP4Y1 gene expression down- and upregulation, respectively, with no significant changes in mRNA levels of genes encoding superoxide dismutase (SOD) and glutathione-S-transferase (GST). Finally, this study highlights variable tissue and time-specific biomarker

  17. Aripiprazole induced non-cardiogenic pulmonary edema: a case report.

    Science.gov (United States)

    Cetin, Mustafa; Celik, Mustafa; Cakıcı, Musa; Polat, Mustafa; Suner, Arif

    2014-01-01

    Aripiprazole is a second-generation antipsychotic drug with partial dopamine agonistic activity. Although the adverse cardiovascular effects of both typical and atypical antipsychotics are well known, similar data on aripiprazole, which was recently introduced, are scarce. Herein we report a 35-year-old female that presented to our emergency department with non-cardiogenic pulmonary edema. Chest X-ray and thoracic CT showed pulmonary edema and bilateral pleural effusion. Anamnesis showed that she had been taking sertraline 200 mg d-1 for obsessive-compulsive disorder for a long time and that aripiprazole10 mg d-1 was added for augmentation 2 months prior to presentation. We think that the CYP 2D6 inhibitor sertraline might have played a role in increasing the plasma concentration and toxicity of aripiprazole in the presented patient.

  18. Aripiprazole-induced Hyperprolactinemia in a Young Female with Delusional Disorder.

    Science.gov (United States)

    Joseph, Sam Padamadan

    2016-01-01

    Hyperprolactinemia is a common adverse effect of antipsychotic medication. Switching over to aripiprazole or adjunctive aripiprazole has been advocated for optimal management of antipsychotic-induced hyperprolactinemia. Adjunctive treatment with aripiprazole has been shown to normalize prolactin levels without affecting already achieved improvements in psychotic symptoms. However, here, we present the case of a 36 year old female with delusional disorder who developed symptomatic hyperprolactinemia while on aripiprazole treatment. Dopamine acts as a tonic inhibitor of prolactin secretion through the tubero-infundibular dopaminergic system. Aripiprazole being a partial agonist has a lower intrinsic activity at the D2 receptor than dopamine, allowing it to act as both, a functional agonist and antagonist, depending on the surrounding levels of dopamine. Hence, in the absence of a competing D2 antagonist and the presence of dopamine (the natural agonist), aripiprazole could act as a functional antagonist and thus elevate prolactin levels.

  19. Studies on Insecticidal Activities and Active Ingredients of Stephania kwangsiensis Lo.

    Institute of Scientific and Technical Information of China (English)

    DENG Ye-cheng; XU Han-hong

    2005-01-01

    Insecticidal activities and active ingredients of Stephania kwangsiensis Lo. were studied for the first time. The results showed that all parts of S. kwangsiensis Lo. had contact activity against brown planthoppers, Nilaparvata lugens Stal,and the contact activity of methanol extract from root tubers was the highest, with a LD50 value being 1.5794 μg/female.l-roemerine was isolated from root tubers of S. kwangsiensis Lo. and identified, and it was the main active ingredient.l-roemerine had high contact toxicity to brown planthoppers, with a LD50 value being 0.0443 μg/female. Contact toxicity of l-roemerine to brown planthoppers was 7.48 times that of malathion, the convientional chemical insecticide used for controlling brown planthoppers.l-roemerine also had stomach poison activity against brown planthoppers.

  20. Evaluation of Potential Pharmacokinetic Drug-Drug Interaction between Armodafinil and Aripiprazole in Healthy Adults.

    Science.gov (United States)

    Darwish, M; Bond, M; Yang, R; Hellriegel, E T; Robertson, P

    2015-07-01

    Armodafinil, a moderate inducer of cytochrome P450 (CYP) 3A4, has been studied as adjunctive therapy to maintenance medications for major depressive episodes associated with bipolar I disorder. We evaluated the effect of daily dosing with armodafinil on the pharmacokinetics and safety of the CYP3A4 substrate aripiprazole, an atypical antipsychotic used to treat bipolar I disorder. Healthy adults received 15 mg aripiprazole alone and after armodafinil (250 mg/day) pretreatment. Pharmacokinetic parameters were derived from plasma concentrations of aripiprazole and its active metabolite, dehydro-aripiprazole, obtained over 16 days after each aripiprazole administration. Steady-state pharmacokinetics of armodafinil and its 2 circulating metabolites was assessed. Of 36 subjects enrolled, 24 were evaluable for pharmacokinetic analysis. Armodafinil reduced systemic exposure to aripiprazole (Cmax, - 8%; AUC0-∞, -34%) and dehydro-aripiprazole, which is both formed and eliminated in part via CYP3A4 (Cmax, - 10%; AUC0-∞, - 32%). Adverse events were generally consistent with known safety profiles of each agent. Systemic exposure to aripiprazole and dehydro-aripiprazole was moderately reduced following armodafinil pretreatment. The combination was generally well tolerated under the conditions studied. © Georg Thieme Verlag KG Stuttgart · New York.

  1. Opinions expressed by Italian National Advisory Toxicological Committee on some active ingredients of pesticides

    Energy Technology Data Exchange (ETDEWEB)

    Camoni, I. [Ist. Superiore di Sanita`, Rome (Italy). Lab. di Tossicologia Applicata

    1996-03-01

    The opinions expressed by the Italian National Advisory Toxicological Committee (CCTN) on some active ingredients of pesticides are presented. Carcinogenic and mutagenic effects of these substances have been examined and, on this basis, an evaluation and relative classification were expressed.

  2. Source characterization of nervous system active pharmaceutical ingredients in healthcare wastewaters

    Science.gov (United States)

    Nervous system active pharmaceutical ingredients (APIs), including anti-depressants and opioids, are important clinically administered pharmaceuticals within healthcare facilities. Concentrations and mass loadings of ten nervous system APIs and three nervous system API metaboli...

  3. Consensus Modeling for Prediction of Estrogenic Activity of Ingredients Commonly Used in Sunscreen Products

    Directory of Open Access Journals (Sweden)

    Huixiao Hong

    2016-09-01

    Full Text Available Sunscreen products are predominantly regulated as over-the-counter (OTC drugs by the US FDA. The “active” ingredients function as ultraviolet filters. Once a sunscreen product is generally recognized as safe and effective (GRASE via an OTC drug review process, new formulations using these ingredients do not require FDA review and approval, however, the majority of ingredients have never been tested to uncover any potential endocrine activity and their ability to interact with the estrogen receptor (ER is unknown, despite the fact that this is a very extensively studied target related to endocrine activity. Consequently, we have developed an in silico model to prioritize single ingredient estrogen receptor activity for use when actual animal data are inadequate, equivocal, or absent. It relies on consensus modeling to qualitatively and quantitatively predict ER binding activity. As proof of concept, the model was applied to ingredients commonly used in sunscreen products worldwide and a few reference chemicals. Of the 32 chemicals with unknown ER binding activity that were evaluated, seven were predicted to be active estrogenic compounds. Five of the seven were confirmed by the published data. Further experimental data is needed to confirm the other two predictions.

  4. Use of aripiprazole for delirium in the elderly: a short review.

    Science.gov (United States)

    Kirino, Eiji

    2015-03-01

    The effects and tolerability of antipsychotics in delirium treatment remain controversial. Compared to other antipsychotics, aripiprazole differs in pharmacological activity because it exerts its effect as a dopamine D2 partial agonist. The guidelines of the American Psychiatric Association rank aripiprazole highly among antipsychotics with regard to safety, and this drug is likely to be useful for delirium treatment. Here, we reviewed the efficacy and safety of aripiprazole for delirium. The results of our literature review on the efficacy and safety of delirium treatments suggest that aripiprazole is an effective treatment option for delirium in the elderly. Aripiprazole is as effective as other antipsychotics in improving delirium symptoms, and it is safer because it is less likely to cause extrapyramidal symptoms, excessive sedation, and weight gain. However, these findings are based on only a few clinical studies of elderly patients with delirium. Therefore, further investigations are necessary.

  5. Aripiprazole-induced priapism

    Directory of Open Access Journals (Sweden)

    Satya K Trivedi

    2016-01-01

    Full Text Available Priapism is a urologic emergency representing a true disorder of penile erection that persists beyond or is unrelated to sexual interest or stimulation. A variety of psychotropic drugs are known to produce priapism, albeit rarely, through their antagonistic action on alpha-1 adrenergic receptors. We report such a case of priapism induced by a single oral dose of 10 mg aripiprazole, a drug with the least affinity to adrenergic receptors among all atypical antipsychotics. Polymorphism of alpha-2A adrenergic receptor gene in schizophrenia patients is known to be associated with sialorrhea while on clozapine treatment. Probably, similar polymorphism of alpha-1 adrenergic receptor gene could contribute to its altered sensitivity and resultant priapism. In future, pharmacogenomics-based approach may help in personalizing the treatment and effectively prevent the emergence of such side effects.

  6. Research Progression of Anti-HIV Chinese Medicines and Their Natural Active Ingredients

    Institute of Scientific and Technical Information of China (English)

    Chen Jing; Fu Linchun; Li Maoqing; Chen Jiantao

    2014-01-01

    Objective: To review the research progression of Chinese medicines for anti-human immunodeifciency virus (HIV) and their natural active ingredients at home and abroad so as to provide references for pharmaceutical research and clinical medication. Methods:Abundant representative literatures at home and abroad were classiifed to introduce the anti-HIV monomers, compounds and natural active ingredients of Chinese medicines. Results:The researches on anti-HIV natural medicines have obtained great achievements, in which medicines with anti-virus and immunity-improving functions have had rapid progression and new-types for anti-virus also have had dramatic development. Conclusion:The progression of anti-HIV Chinese medicines and their active ingredients has favorable prospect.

  7. Data-mining of potential antitubercular activities from molecular ingredients of traditional Chinese medicines

    Directory of Open Access Journals (Sweden)

    Salma Jamal

    2014-07-01

    Full Text Available Background. Traditional Chinese medicine encompasses a well established alternate system of medicine based on a broad range of herbal formulations and is practiced extensively in the region for the treatment of a wide variety of diseases. In recent years, several reports describe in depth studies of the molecular ingredients of traditional Chinese medicines on the biological activities including anti-bacterial activities. The availability of a well-curated dataset of molecular ingredients of traditional Chinese medicines and accurate in-silico cheminformatics models for data mining for antitubercular agents and computational filters to prioritize molecules has prompted us to search for potential hits from these datasets.Results. We used a consensus approach to predict molecules with potential antitubercular activities from a large dataset of molecular ingredients of traditional Chinese medicines available in the public domain. We further prioritized 160 molecules based on five computational filters (SMARTSfilter so as to avoid potentially undesirable molecules. We further examined the molecules for permeability across Mycobacterial cell wall and for potential activities against non-replicating and drug tolerant Mycobacteria. Additional in-depth literature surveys for the reported antitubercular activities of the molecular ingredients and their sources were considered for drawing support to prioritization.Conclusions. Our analysis suggests that datasets of molecular ingredients of traditional Chinese medicines offer a new opportunity to mine for potential biological activities. In this report, we suggest a proof-of-concept methodology to prioritize molecules for further experimental assays using a variety of computational tools. We also additionally suggest that a subset of prioritized molecules could be used for evaluation for tuberculosis due to their additional effect against non-replicating tuberculosis as well as the additional hepato

  8. 21 CFR 338.10 - Nighttime sleep-aid active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Nighttime sleep-aid active ingredients. 338.10 Section 338.10 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE NIGHTTIME SLEEP-AID DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Active...

  9. International Conference on Harmonisation; guidance on good manufacturing practice for active pharmaceutical ingredients; availability. Notice.

    Science.gov (United States)

    2001-09-25

    The Food and Drug Administration (FDA) is announcing the availability of a guidance entitled "Q7A Good Manufacturing Practice Guidance for Active Pharmaceutical Ingredients." The guidance was prepared under the auspices of the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH). The guidance describes current good manufacturing practice (CGMP) for manufacturing of active pharmaceutical ingredients (APIs). The guidance is intended to help ensure that all APIs meet the standards for quality and purity they purport or are represented to possess.

  10. Tregitope Peptides: The Active Pharmaceutical Ingredient of IVIG?

    Directory of Open Access Journals (Sweden)

    Anne S. De Groot

    2013-01-01

    Full Text Available Five years ago, we reported the identification and characterization of several regulatory T-cell epitopes (now called Tregitopes that were discovered in the heavy and light chains of IgG (De Groot et al. Blood, 2008. When added ex vivo to human PBMCs, these Tregitopes activated regulatory T cells (Tregs, increased expression of the transcription factor FoxP3, and induced IL-10 expression in CD4+ T cells. We have now shown that coadministration of the Tregitopes in vivo, in a number of different murine models of autoimmune disease, can suppress immune responses to antigen in an antigen-specific manner, and that this response is mediated by Tregs. In addition we have shown that, although these are generally promiscuous epitopes, the activity of individual Tregitope peptides is restricted by HLA. In this brief report, we provide an overview of the effects of Tregitopes in vivo, discuss potential applications, and suggest that Tregitopes may represent one of the “active pharmaceutical ingredients” of IVIg. Tregitope applications may include any of the autoimmune diseases that are currently treated almost exclusively with intravenous immunoglobulin G (IVIG, such as Chronic Inflammatory Demyelinating Polyneuropathy (CIDP and Multifocal Motor Neuropathy (MMN, as well as gene therapy and allergy where Tregitopes may provide a means of inducing antigen-specific tolerance.

  11. Active pharmaceutical ingredients detected in herbal food supplements for weight loss samples on the Dutch market

    NARCIS (Netherlands)

    Reeuwijk, N.M.; Venhuis, B.J.; Kaste, de D.; Hoogenboom, L.A.P.; Rietjens, I.; Martena, M.J.

    2014-01-01

    Herbal food supplements claiming to reduce weight may contain active pharmacological ingredients (APIs) that can be used for the treatment of overweight and obesity. The aim of this study was to determine whether herbal food supplements for weight loss on the Dutch market contain APIs with weight lo

  12. Active ingredients of traditional Chinese medicine in the treatment of diabetes and diabetic complications.

    Science.gov (United States)

    Zhang, Tian-Tian; Jiang, Jian-Guo

    2012-11-01

    Diabetes mellitus (DM) is a chronic progressive systemic disease caused by metabolic disorder. In recent years, significant amounts of studies have shown that traditional Chinese medicine (TCM) and its active ingredients have obvious hypoglycemic effect. This paper summarizes single herbs and their active ingredients from TCM with the role of treating DM, and relevant literatures published in the past decades are reviewed. The active ingredients are divided into polysaccharides, saponins, alkaloids, flavonoids, terpenoids and others, which are described in this article from the aspects of active ingredients, sources, models, efficacy, and mechanisms. Mechanisms of TCM in treating DM are concluded: i) to promote insulin secretion and increase serum insulin levels; ii) to increase the sensitivity of insulin and improve its resistance; iii) to inhibit glucose absorption; iv) to affect glucose metabolism of insulin receptor; and v) to scavenge radicals and prevent lipid peroxidation. The separation and extraction of effective monomer from TCM is an important direction of anti-diabetic drug discovery currently. Future research about hypoglycemic mechanism of TCM based on the clinical should combine with modern scientific methods and regulatory approach to strive for more meaningful discovery and innovation.

  13. 21 CFR 358.710 - Active ingredients for the control of dandruff, seborrheic dermatitis, or psoriasis.

    Science.gov (United States)

    2010-04-01

    ..., seborrheic dermatitis, or psoriasis. 358.710 Section 358.710 Food and Drugs FOOD AND DRUG ADMINISTRATION... Psoriasis § 358.710 Active ingredients for the control of dandruff, seborrheic dermatitis, or psoriasis. The... psoriasis. (1) Coal tar, 0.5 to 5 percent. When a coal tar solution, derivative, or fraction is used as...

  14. Nano-microdelivery systems for oromucosal delivery of an active ingredient

    DEFF Research Database (Denmark)

    2014-01-01

    A composition for oromucosal delivery of at least one active ingredient, more particularly a lipid nano-microdelivery system comprising a nicotine component and/or a flavour component, wherein the nicotine component may be delivered to the oral cavity via absorption through the mucosal membranes...... thereof and/or wherein the flavour component may be delivered to the oral mucosa by controlled release....

  15. 78 FR 70043 - Pesticide Product Registration; Receipt of an Application for a New Active Ingredient

    Science.gov (United States)

    2013-11-22

    ... name: DAS-81419-2 Soybean. Active ingredients: Bacillus thuringiensis Cry1Ac protein expressed in soybean and Bacillus thuringiensis Cry1F protein expressed in soybean. Proposed classification/Use: Plant... list of North American Industrial Classification System (NAICS) codes is not intended to be...

  16. NOVEL HYDROXAMIC ACIDS HAVING HISTONE DEACETYLASE INHIBITING ACTIVITY AND ANTI-CANCER COMPOSITION COMPRISING THE SAME AS AN ACTIVE INGREDIENT

    DEFF Research Database (Denmark)

    2013-01-01

    The present invention relates to a pharmaceutical composition for anticancer including novel hydroxamic acid with histone deacetylase inhibiting activity as an active ingredient. Hydroxamic acid compound of the present invention has inhibitory activity of histone deacetylase (HDAC) and shows cyto...... cytotoxicity to a variety of cancer cells, being useful in strong anti-cancer drug.......The present invention relates to a pharmaceutical composition for anticancer including novel hydroxamic acid with histone deacetylase inhibiting activity as an active ingredient. Hydroxamic acid compound of the present invention has inhibitory activity of histone deacetylase (HDAC) and shows...

  17. 21 CFR 310.528 - Drug products containing active ingredients offered over-the-counter (OTC) for use as an...

    Science.gov (United States)

    2010-04-01

    ... drug product. Anise, cantharides, don qual, estrogens, fennel, ginseng, golden seal, gotu kola, Korean... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Drug products containing active ingredients... Requirements for Specific New Drugs or Devices § 310.528 Drug products containing active ingredients offered...

  18. Active pharmaceutical ingredient (api) from an estuarine fungus, Microdochium nivale (Fr.)

    Digital Repository Service at National Institute of Oceanography (India)

    Bhosale, S.H.; Patil, K.B.; Parameswaran, P.S.; Jagtap, T.G.

    of Environmental Biology circleshadowdwnSeptember 2011circleshadowdwn Active pharmaceutical ingredient (api) from an estuarine fungus, Microdochium nivale (Fr.) Author Details S.H. Bhosale Biochemical Sciences, National Chemical Laboratory, Pune - 411 008, India K...-inflammatory, Keratoconctivitis sicca (KCS) and immunosuppressive activity (Stiller and Opelez, 1991; Rahacek and De-Xiu, 1991; Laibowitz et al., 1993). Cyclosporine A is a potent immunosuppressant that has significantly contributed to the progress in organ transplantation...

  19. ANTIMICROBIAL ACTIVITY OF WATER EXTRACTS OF TRIKATU CHURNA AND ITS INDIVIDUAL INGREDIENT

    Directory of Open Access Journals (Sweden)

    P.R. Malvankar* and M. M. Abhyankar

    2012-04-01

    Full Text Available Trikatu churna is one of the traditional poly herbal preparation, formed by mixing equal quantities of three important spicy materials such as Piper longum L. (Piperaceae, Piper nigrum L. (Piperaceae and Zingiber officinale Roscoe (Zingiberaceae. Trikatu is also known as “ Three Bitters”. The trikatu preparation was reported to contain alkaloids, phenols, tannins, flavanoids, steroids, lignin & saponins. The objective of study is to evaluate the antimicrobial activity of trikatu churna & its individual ingredients with their preliminary phytochemical study. The aqueous extracts of trikatu churna & its each ingredient were tested for antimicrobial activity against certain bacterial strains of Escherichia coli, Staphylococcus aureus by in vitro agar well diffusion method and the results are recorded as the zone of inhibition. Trikatu churna was found to possess higher extent of phytoconstituents with promising antimicrobial activity.

  20. [Screening of anti-aging active ingredients and mechanism analysis based on molecular docking technology].

    Science.gov (United States)

    Du, Ran-Feng; Zhang, Xiao-Hua; Ye, Xiao-Tong; Yu, Wen-Kang; Wang, Yun

    2016-07-01

    Dampness evil is the source of all diseases, which is easy to cause disease and promote aging, while aging could also promote the occurence and development of diseases. In this paper, the relationship between the dampness evil and aging would be discussed, to find the anti-aging active ingredients in traditional Chinese medicine (TCM), and analyze the anti-aging mechanism of dampness eliminating drug. Molecular docking technology was used, with aging-related mammalian target of rapamycin as the docking receptors, and chemical components of Fuling, Sangzhi, Mugua, Yiyiren and Houpo as the docking molecules, to preliminarily screen the anti-aging active ingredients in dampness eliminating drug. Through the comparison with active drugs already on the market (temsirolimus and everolimus), 12 kinds of potential anti-aging active ingredients were found, but their drug gability still needs further study. The docking results showed that various components in the dampness eliminating drug can play anti-aging activities by acting on mammalian target of rapamycin. This result provides a new thought and direction for the method of delaying aging by eliminating dampness. Copyright© by the Chinese Pharmaceutical Association.

  1. Studies of phase transitions in the aripiprazole solid dosage form.

    Science.gov (United States)

    Łaszcz, Marta; Witkowska, Anna

    2016-01-05

    Studies of the phase transitions in an active substance contained in a solid dosage form are very complicated but essential, especially if an active substance is classified as a BCS Class IV drug. The purpose of this work was the development of sensitive methods for the detection of the phase transitions in the aripiprazole tablets containing initially its form III. Aripiprazole exhibits polymorphism and pseudopolymorphism. Powder diffraction, Raman spectroscopy and differential scanning calorimetry methods were developed for the detection of the polymorphic transition between forms III and I as well as the phase transition of form III into aripiprazole monohydrate in tablets. The study involved the initial 10 mg and 30 mg tablets, as well as those stored in Al/Al blisters, a triplex blister pack and HDPE bottles (with and without desiccant) under accelerated and long term conditions. The polymorphic transition was not observed in the initial and stored tablets but it was visible on the DSC curve of the Abilify(®) 10 mg reference tablets. The formation of the monohydrate was observed in the diffractograms and Raman spectra in the tablets stored under accelerated conditions. The monohydrate phase was not detected in the tablets stored in the Al/Al blisters under long term conditions. The results showed that the Al/Al blisters can be recommended as the packaging of the aripiprazole tablets containing form III.

  2. Aripiprazole: a review of its use in the management of schizophrenia in adults.

    Science.gov (United States)

    Croxtall, Jamie D

    2012-02-01

    Oral aripiprazole (Abilify®) is an atypical antipsychotic agent that is approved worldwide for use in adult patients with schizophrenia. It is a quinolinone derivative that has a unique receptor binding profile as it exhibits both partial agonist activity at dopamine D(2) receptors and serotonin 5-HT(1A) receptors and antagonist activity at 5-HT(2A) receptors. In several well designed, randomized, clinical trials of 4-6 weeks duration, aripiprazole provided symptomatic control for patients with acute, relapsing schizophrenia or schizoaffective disorder. Furthermore, following 26 weeks' treatment, the time to relapse was significantly longer for patients with chronic, stabilized schizophrenia receiving aripiprazole compared with those receiving placebo. Using a variety of efficacy outcomes, aripiprazole showed a mixed response when evaluated against other antipsychotic agents in randomized clinical trials. Longer-term data showed that improvements in remission rates and response rates favoured aripiprazole over haloperidol, although, the time to failure to maintain a response was not significantly different between the treatment arms. On the other hand, improvements in positive and negative symptom scores mostly favoured olanzapine over aripiprazole, although, the time to all-cause treatment discontinuation was not significantly different between the two treatments. Several open-label, switching trials showed that aripiprazole provided continued control of symptoms in patients with schizophrenia or schizoaffective disorder. Using a variety of efficacy outcomes or quality-of-life scores, longer-term treatment generally favoured patients switched to receive aripiprazole compared with standard-of-care oral antipsychotics. Aripiprazole was generally well tolerated in patients with schizophrenia. In particular, its use seems to be associated with a lower incidence of extrapyramidal symptoms than haloperidol and fewer weight-gain issues than olanzapine. Aripiprazole also

  3. Different effects of taking aripiprazole and risperidone on spontaneous brain activity in schizophrenics%阿立哌唑和利培酮对精神分裂症患者自发脑活动的不同影响

    Institute of Scientific and Technical Information of China (English)

    常鑫; 罗程; 侯昌月; 陈琳; 陈曦; 贺辉; 段明君; 蒋宇超; 尧德中

    2015-01-01

    Objective To explore the difference in effects of taking two different kinds of drugs aripiprazole and risperidone on spontaneous brain activity among schizophrenics. Methods Nineteen patients(9 patients taking aripiprazole and 10 patients taking risperidone),who were recruited in the Fourth Peopleˊs Hospital of Chengdu were underwent a resting - state scanning at the Center for Information in Medicine of University of Electronic Science and Technology of China. Two groupsˊfractional amplitude of low - frequency (fALFF)value were calculated and compared using two sample t - test. Results Compared with the aripiprazole group,risperidone group showed significantly decreasing areas of fALFF,including bilateral putamen,olfactory,caudate,orbitofrontal and right palli-dum;left middle temporal gyrus and left supramarginal gyrus where also shown to have increasing areas. Conclusion Indeed,there are different effects of taking aripiprazole and risperidone on spontaneous brain activity in schizophrenics,which is consistent with the pharmacological mechanism of two drugs.%目的:探究临床常用抗精神病药物阿立哌唑和利培酮对精神分裂症患者自发性脑活动的不同影响。方法纳入就诊于成都市第四人民医院的长期服用阿立哌唑进行单药治疗的精神分裂症患者9例,服用利培酮单药治疗的精神分裂症患者10例,进行静息态功能磁共振(fMRI)扫描。分析两组患者 fMRI 信号的分数低频振幅(fALFF)的组间差异。结果与阿立哌唑组比较,利培酮组 fALFF 显著降低的脑区有双侧壳核、嗅皮质、尾状核、眶部额下回和右侧苍白球;fALFF 显著增高脑区有左侧颞中回和左侧缘上回(P <0.05)。结论阿立哌唑和利培酮会对大脑产生不同影响,差异脑区符合两种药物的不同药理机制。

  4. Review article: health benefits of some physiologically active ingredients and their suitability as yoghurt fortifiers

    OpenAIRE

    Fayed, A. E

    2014-01-01

    The article is concerned with health benefits of two main physiologically active ingredients namely, Isoflavones and γ-Aminobutyric acid, with emphasis on their fitness for fortification of yoghurt to be consumed as a functional food. Isoflavones (ISO) are part of the diphenol compounds, called “phytoestrogens,” which are structurally and functionally similar to estradiol, the human estrogen, but much less potent. Because of this similarity, ISO were suggested to have preventive effects for m...

  5. Release effect of the active ingredients using a radiation cross linking technology

    Energy Technology Data Exchange (ETDEWEB)

    Hwang, Seung Hyun; Ahn, Sung Jun; Park, Jong Seok; Jeong, Sung In; Gwon, Hui Jeong; Lim, Youn Mook [Research Division for Industry and Environment, Korea Atomic Energy Research Institute, Jeongeup (Korea, Republic of); Lee, Dong Yun [Dept. of Bioengineering, Division of Applied Chemical and Bio Engineering, Hanyang University, Seoul (Korea, Republic of)

    2015-12-15

    Typical radiation cross-linked hydrogels has the characteristic that high water content, but low emission efficiency of active ingredients. Therefore, the hydrogel was prepared by the addition to collagen, which is closely related to the formation of skin wrinkles in biocompatibility and highly water-soluble carboxymethyl cellulose sodium salt (CMC) in order to preparation of hydrogels has excellent emission efficiency of active ingredients. Hydrogels were prepared by dissolving CMC and collagen each of 0.5%, 10% concentration in deionized water. Then, prepared hydrogels are performed by gamma-radiation at 1, 3, 5 kGy irradiation dose. The results showed that the gel fraction of after irradiated 3 kGy hydrogel was higher than before irradiated gelation as long as the 55.3%. The swelling rate of irradiated 3 kGy hydrogel was lower than the non-irradiated sample. The compressive strength of 3 kGy irradiated hydrogel was the highest. The visco-elastic did not show any significant differences, even after irradiation. The CMC hydrogel in this study suggested a potential use as a material for the mask pack for improved emission efficiency of the active ingredient and anti-wrinkles.

  6. Arbuscular mycorrhizal symbiosis and active ingredients of medicinal plants: current research status and prospectives.

    Science.gov (United States)

    Zeng, Yan; Guo, Lan-Ping; Chen, Bao-Dong; Hao, Zhi-Peng; Wang, Ji-Yong; Huang, Lu-Qi; Yang, Guang; Cui, Xiu-Ming; Yang, Li; Wu, Zhao-Xiang; Chen, Mei-Lan; Zhang, Yan

    2013-05-01

    Medicinal plants have been used world-wide for thousands of years and are widely recognized as having high healing but minor toxic side effects. The scarcity and increasing demand for medicinal plants and their products have promoted the development of artificial cultivation of medicinal plants. Currently, one of the prominent issues in medicinal cultivation systems is the unstable quality of the products. Arbuscular mycorrhiza (AM) affects secondary metabolism and the production of active ingredients of medicinal plants and thus influence the quality of herbal medicines. In this review, we have assembled, analyzed, and summarized the effects of AM symbioses on secondary metabolites of medicinal plants. We conclude that symbiosis of AM is conducive to favorable characteristics of medicinal plants, by improving the production and accumulation of important active ingredients of medicinal plants such as terpenes, phenols, and alkaloids, optimizing the composition of different active ingredients in medicinal plants and ultimately improving the quality of herbal materials. We are convinced that the AM symbiosis will benefit the cultivation of medicinal plants and improve the total yield and quality of herbal materials. Through this review, we hope to draw attention to the status and prospects of, and arouse more interest in, the research field of medicinal plants and mycorrhiza.

  7. [Studies on pharmacokinetics features of characteristic active ingredients of daidai flavone extract in different physiological status].

    Science.gov (United States)

    Zeng, Ling-Jun; Chen, Dan; Zheng, Li; Lian, Yun-Fang; Cai, Wei-Wei; Huang, Qun; Lin, Yi-Li

    2014-01-01

    In order to explore the clinical hypolipidemic features of Daidai flavone extract, the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats were studied and compared. The study established the quantitative determination method of naringin and neohesperidin in plasma by UPLC-MS. Study compared the pharmacokinetics differences of naringin and noehesperidin in normal and hyperlipemia rats on the basis of establishment of hyperlipemia model. Results indicated that the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats showed significant differences. The C(max) of naringin and neohesperidin in hyperlipemia rats plasma after oral administration of Daidai flavone extract increased obviously, while t1/2, MRT and AUC0-24 h decreased, compared to normal rats. But t(max) showed no differences to that of normal rats. The results further proved Daidai flavone extract would have better hypolipidemic effect in the hyperlipemia pathological status. And the characteristic active ingredients naringin and noehesperidin were the material base of Daidai flavone extract to express the hypolipidemic effect.

  8. Comparison of Active Ingredient Content of Nanwuweizi and Beiwuweizi Collected in Different Seasons Detected by HPLC-DAD

    Directory of Open Access Journals (Sweden)

    Feng YAO

    2015-12-01

    Full Text Available Abstract Objective: To compare the active ingredient content of Nanwuweizi (Kadsura longepedunculata and Beiwuweizi (Fructus Schisandrae Chinensis collected in different seasons. Methods: Microwave-assisted extraction was applied to extract the active ingredients in Nanwuweizi and Beiwuweizi, with methanol as the solvent. High performance liquid chromatography-diode array detection ℃; mobile phase: water (A - acetonitrile (B; gradient elution: 0.8 mL/min; and detection wavelength: 225 nm. (HPLC-DAD method was used to analyze the content of each ingredient, with chromatographic conditions as follows: Brava BDS C18 column (250 mm×4.6 mm, 5 μm; column temperature: 30 Results: All ingredients waiting for detection reached their peaks within 75 min, with excellent degree of separation and higher number of theoretical plates. Standard curves were drawn, and the mean value of phase relationship of each ingredient was >0.999. The content of active ingredients in lignans of Nanwuweizi and Beiwuweizi showed tendency of increase first and then decreased. In addition, all ingredients in Beiwuweizi reached their peaks in September while those in Nanwuweizi in August. Conclusion: This method can be used to detect the content of multiple ingredients in Wuweizi (Schisandra chinensis simultaneously because it is simple in operation, precise in results and excellent in repeatability.

  9. Worsened hypertension control induced by aripiprazole

    Directory of Open Access Journals (Sweden)

    Yasui-Furukori N

    2013-04-01

    Full Text Available Norio Yasui-Furukori, Akira Fujii Department of Neuropsychiatry, Graduate School of Medicine, Hirosaki University, Hirosaki, Japan Abstract: Aripiprazole is widely used in the treatment of schizophrenia and bipolar disorders. Although antipsychotics generally have hypotensive effects, two cases were identified that demonstrated hypertension during the switch from other antipsychotics to aripiprazole. The hypertensive state of these patients recovered after switching back to other antipsychotics, and these cases suggest that aripiprazole may lead to hypertension. Keywords: hypertension, aripiprazole, dopamine antagonist, 5-HT1a

  10. Aripiprazole-induced oculogyric crisis (acute dystonia

    Directory of Open Access Journals (Sweden)

    Jyotik T Bhachech

    2012-01-01

    Full Text Available Aripiprazole is the third generation atypical antipsychotic and a dopamine serotonin system stabilizer (DSS effective against positive and negative symptoms of schizophrenia. It has a low propensity for extrapyramidal side effects, causes minimal weight gain or sedation, produces no elevation in serum prolactin levels, and does not cause prolongation of QTc interval. This case report is of a patient suffering from schizophrenia (paranoid. The patient developed oculogyric crisis (acute dystonia with aripiprazole dose uptitration. Dystonic reaction resolved with promethazine administration. Naranjo′s causality assessment reveals probable association of aripiprazole with oculogyric crisis. A thorough workup and vigilance is required prior to initiation of aripiprazole in the case of schizophrenia.

  11. Soil sorption and leaching of active ingredients of Lumax® under mineral or organic fertilization.

    Science.gov (United States)

    Pinna, Maria Vittoria; Roggero, Pier Paolo; Seddaiu, Giovanna; Pusino, Alba

    2014-09-01

    The study describes the soil sorption of the herbicide Lumax®, composed of S-metolachlor (MTC), terbuthylazine (TBZ), and mesotrione (MST), as influenced by mineral and organic fertilizers. The investigation was performed on a sandy soil of an agricultural area designated as a Nitrate Vulnerable Zone, where mineral and organic fertilizers were applied for many years. Two organic fertilizers, cattle manure and slurry, respectively, and a mineral fertilizer with a nitrification inhibitor, Entec®, were compared. According to the experiments, performed with a batch method, the sorption conformed to Freundlich model. The extent of sorption of Lumax® ingredients was closely related to their octanol-water partition coefficient Kow. The respective desorption was hysteretic. Leaching trials were carried out by using water or solutions of DOM or Entec® as the eluants. Only the elution with the mineral fertilizer promoted the leaching of Lumax® active ingredients.

  12. [Important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of active ingredients of Chinese materia medica].

    Science.gov (United States)

    Bi, Xiaolin; Du, Qiu; Di, Liuqing

    2010-02-01

    Oral drug bioavailability depends on gastrointestinal absorption, intestinal transporters and metabolism enzymes are the important factors in drug gastrointestinal absorption and they can also be induced or inhibited by the active ingredients of Chinese materia medica. This article presents important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of the active ingredients of Chinese materia medica, and points out the importance of research on transport and metabolism of the active ingredients of Chinese materia medica in Chinese extract and Chinese medicinal formulae.

  13. Nanocarriers for the delivery of active ingredients and fractions extracted from natural products used in traditional Chinese medicine (TCM).

    Science.gov (United States)

    Liu, Ying; Feng, Nianping

    2015-07-01

    Traditional Chinese medicine (TCM) has been practiced for thousands of years with a recent increase in popularity. Despite promising biological activities of active ingredients and fractions from TCM, their poor solubility, poor stability, short biological half-life, ease of metabolism and rapid elimination hinder their clinical application. Therefore, overcoming these problems to improve the therapeutic efficacy of TCM preparations is a major focus of pharmaceutical sciences. Recently, nanocarriers have drawn increasing attention for their excellent and efficient delivery of active TCM ingredients or fractions. This review discusses problems in the delivery of active TCM ingredients or fractions; focuses on recent advances in nanocarriers that represent potential solutions to these problems, including lipid-based nanoparticles and polymeric, inorganic, and hybrid nanocarriers; and discusses unanswered questions in the field and criteria for the development of better nanocarriers for the delivery of active TCM ingredients or fractions to be focused on in future studies.

  14. 21 CFR 310.545 - Drug products containing certain active ingredients offered over-the-counter (OTC) for certain uses.

    Science.gov (United States)

    2010-04-01

    ...), anticholinergic, antihistamine, oral antitussive, or stimulant active ingredient. (7) Dandruff/seborrheic... Mono- and di-glycerides Niacinamide Organic vegetables Pancreatin Pantothenic acid Papain Papaya... blue Natural estrogenic hormone Niacinamide Nutmeg oil (oil of nutmeg) Oil of erigeron...

  15. Active pharmaceutical ingredient (API) production involving continuous processes – A process system engineering (PSE)-assisted design framework

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Skovby, Tommy; Kiil, Søren

    2012-01-01

    A systematic framework is proposed for the design of continuous pharmaceutical manufacturing processes. Specifically, the design framework focuses on organic chemistry based, active pharmaceutical ingredient (API) synthetic processes, but could potentially be extended to biocatalytic and fermenta...

  16. Worsened hypertension control induced by aripiprazole

    OpenAIRE

    Yasui-Furukori N; Fujii A

    2013-01-01

    Norio Yasui-Furukori, Akira Fujii Department of Neuropsychiatry, Graduate School of Medicine, Hirosaki University, Hirosaki, Japan Abstract: Aripiprazole is widely used in the treatment of schizophrenia and bipolar disorders. Although antipsychotics generally have hypotensive effects, two cases were identified that demonstrated hypertension during the switch from other antipsychotics to aripiprazole. The hypertensive state of these patients recovered after switching back to other antipsychot...

  17. Studies of Active Ingredients in Cough Syrup by Capillary Zone Electrophoresis with Amperometric Detection

    Institute of Scientific and Technical Information of China (English)

    ZHOU Tian-shu; WANG Ai-fang; WU Fang; SHI Guo-yue; FANG Yu-zhi

    2003-01-01

    The present paper covers a simple, reliable and reproducible method, based on capillary zone electrophoresis(CZE) with amperometric detection(AD), for the separation and the determination of ephedrine hydrochloride, promethazine hydrochloride and codeine phosphate. Under the optimal conditions, the three analytes were base-line separated completely within 16 min. Good linear relationships between the peak heights and the concentrations of the three analytes were obtained with the correlation coefficients better than 0.9993. The method was directly applied to the determination of the active ingredients in pharmaceutical preparations and the assay results were satisfactory.

  18. Classification of parasite eggs used as an active pharmaceutical ingredient (API)

    DEFF Research Database (Denmark)

    Bruun, J. M.; Carstensen, Jens Michael; Thamsborg, S.

    2012-01-01

    the pharmaceutical potency of eggs from the parasite Trichuris suis (pig whipworm), used as an active pharmaceutical ingredient in medicine against chronic autoimmune diseases of the intestines such as Crohn's disease and Ulcerative colitis. The analysis will combine spectral and morphological characteristics...... in order to first detect and then classify the parasite eggs based on a set of biologically inspired, quantitative features. The egg classification is currently done manually using transmitted light microscopy, but to allow for validation of this process and to reduce the operator bias, an automated system...

  19. Chromatography of crotamiton and its application to the determination of active ingredients in ointments.

    Science.gov (United States)

    Izumoto, S; Machida, Y; Nishi, H; Nakamura, K; Nakai, H; Sato, T

    1997-06-01

    Crotamiton, which is a mixture of cis and trans isomers, was investigated by several separation techniques. One of the HPLC modes, in which crotamiton eluted as a single peak, was selected for the determination of five active ingredients (crotamiton, prednisolone, glycyrrhetinic acid, dibucaine and chlorhexidine hydrochloride) in an ointment. The simultaneous determination was performed using isocratic reversed-phase mode within 20 min by employing an octyl (C8) column and a mobile phase containing sodium dodecyl sulfate (SDS) and 2-propanol. The method was successfully applied to quality control and stability testing of the ointment.

  20. How active ingredient localisation in plant tissues determines the targeted pest spectrum of different chemistries

    DEFF Research Database (Denmark)

    Buchholz, Anke; Trapp, Stefan

    2016-01-01

    information sets revealed that the intracellular localisation of active ingredients determines the performance of test compounds against different target pests because of different feeding behaviours: mites feed on mesophyll, and aphids and whiteflies mostly in the vascular system. Polar compounds have a slow...... adsorption into leaf cells and thus a favourable distribution into apoplast and xylem sap. Slightly lipophilic bases get trapped in vacuoles, which is a less suited place to control hemipteran pests but appropriate to control mites. Non-favourable cellular localisation led to a strong reduction...

  1. Identification of the main active ingredients of agrochemicals used around the Lake of Tota, Colombia

    Directory of Open Access Journals (Sweden)

    Wilson Javier Pérez-Holguín

    2016-01-01

    Full Text Available This paper presents a descriptive study aimed at identifying the main active ingredients, frequency of use, and the processes employed in the application of the agrochemicals most used around the Lake of Tota, which is considered the most important freshwater ecosystem in Colombia. A key source for this study is a survey to farmers, which sampling frame was established from a Geographical Institute Agustin Codazzi (IGAC digital map, considering only the plots with some agricultural activity and runoff into the lake. This information was supplemented with geographic data obtained from Google Maps®. As control mechanism, two additional sources were used: i a manual count of packaging of agrochemicals in a certified collection center, and ii a census of stores that supply such products in the study area. The results allow knowing the set of agrochemicals most used around the lake, their active ingredients, and the most common farming practices, some of which could entail some risk to farmers, consumers and the environment.

  2. After-brush rinsing protocols, frequency of toothpaste use: fluoride and other active ingredients.

    Science.gov (United States)

    Parnell, C; O'Mullane, D

    2013-01-01

    The intra-oral retention or substantivity of active ingredients in toothpastes is important for their effectiveness, and this is influenced by product-related and user-related factors. Product-related factors include the formulation and the compatibility of active and other agents in the toothpaste and the concentration of the active ingredient. User-related factors include biological aspects such as salivary flow and salivary clearance, and behavioural aspects, such as frequency and duration of brushing, amount of toothpaste used and post-brushing rinsing behaviour. To date, product-related factors have dominated the research agenda for toothpastes, but user-related factors have the potential to significantly enhance or reduce the effectiveness of toothpaste. In this chapter, we will focus on two of the user-related factors that have been most widely studied: (1) frequency of toothbrushing and (2) post-brushing rinsing behaviour. We will then provide an overview of how evidence on these two behaviours has been used to produce guidance both for the profession and for the public, and make suggestions for the future direction of research in this area.

  3. Determination of nickel in active pharmaceutical ingredients by electrothermal atomic absorption spectrometry.

    Science.gov (United States)

    Bubnič, Zoran; Urleb, Uroš; Kreft, Katjuša; Veber, Marjan

    2010-03-01

    An electrothermal atomic absorption spectrometric procedure for the determination of nickel in active pharmaceutical ingredients was developed. Since the recoveries of nickel by the direct dissolution of samples in diluted nitric acid were low and caused errors in the determination of Ni in pharmaceutical samples, different approaches for sample pre-treatment were examined. It was found that the microwave digestion was the most suitable way for sample preparation. Various combinations of digestion agents and different microwave conditions were tested. The combination of nitric acid and hydrogen peroxide was found to be the most appropriate. The validity of the method was evaluated by recovery studies of spiked samples and by the comparison of the results obtained by inductively coupled plasma mass spectrometry (ICP-MS). The recovery ranged from 87.5 to 104.0% and a good agreement was achieved between both methods. The detection limit and the limit of quantification were 0.6 and 2.1 µg g-1 respectively. The precision of the method was confirmed by the determination of Ni in the spiked samples and was below 4%, expressed in terms of a relative standard deviation. The method was applied to the determination of nickel in production samples of active pharmaceutical ingredients and intermediates.

  4. Methodological Establishment of HPLC-DAD for Determination of 10 Active Ingredients in Wuweizi

    Directory of Open Access Journals (Sweden)

    Feng YAO

    2015-09-01

    Full Text Available Objective: To establish high performance liquid chromatography-diode array detection (HPLC-DAD method for the determination of active ingredients of multiple lignans in Nanwuweizi (Kadsura longepedunculata and Beiwuweizi (Fructus Schisandrae Chinensis so as to set up the standard for the quality control of Wuweizi (Schisandra chinensis. Methods: Brava BDS C18 column (250 mm×4.6 mm, 5 μm was applied, with detection condition as follows: column temperature: 30℃; mobile phase: water (A-acetonitrile (B; gradient elution: 0.8 mL/min and detection wavelength: 225 nm.Results: Ten ingredients in Beiwuweizi and 5 in Nanwuweizi were completely separately within 75 min. Peak area was in favorable linear relationship with concentration. In addition, the recovery rate was 96.87-103.29% and relative standard deviation (RSD was 0.68-2.09%.Conclusion: HPLC-DAD is simple and reliable with favorable repeatability, so it can be used for the determination of multiple lignans in Wuweizi.

  5. Methodological Establishment of HPLC-DAD for Determination of 10 Active Ingredients in Wuweizi

    Institute of Scientific and Technical Information of China (English)

    YAO Feng; CHEN Da-shuai

    2015-01-01

    Objective: To establish high performance liquid chromatography-diode array detection (HPLC-DAD) method for the determination of active ingredients of multiple lignans in Nanwuweizi (Kadsura longepedunculata) and Beiwuweizi (Fructus Schisandrae Chinensis) so as to set up the standard for the quality control of Wuweizi (Schisandra chinensis). Methods: Brava BDS C18 column (250 mm×4.6 mm, 5 μm) was applied, with detection condition as follows: column temperature: 30℃; mobile phase: water (A)-acetonitrile (B); gradient elution: 0.8 mL/min and detection wavelength: 225 nm. Results: Ten ingredients in Beiwuweizi and 5 in Nanwuweizi were completely separately within 75 min. Peak area was in favorable linear relationship with concentration. In addition, the recovery rate was 96.87%-103.29% and relative standard deviation (RSD) was 0.68%-2.09%. Conclusion: HPLC-DAD is simple and reliable with favorable repeatability, so it can be used for the determination of multiple lignans in Wuweizi.

  6. Life cycle analysis within pharmaceutical process optimization and intensification: case study of active pharmaceutical ingredient production.

    Science.gov (United States)

    Ott, Denise; Kralisch, Dana; Denčić, Ivana; Hessel, Volker; Laribi, Yosra; Perrichon, Philippe D; Berguerand, Charline; Kiwi-Minsker, Lioubov; Loeb, Patrick

    2014-12-01

    As the demand for new drugs is rising, the pharmaceutical industry faces the quest of shortening development time, and thus, reducing the time to market. Environmental aspects typically still play a minor role within the early phase of process development. Nevertheless, it is highly promising to rethink, redesign, and optimize process strategies as early as possible in active pharmaceutical ingredient (API) process development, rather than later at the stage of already established processes. The study presented herein deals with a holistic life-cycle-based process optimization and intensification of a pharmaceutical production process targeting a low-volume, high-value API. Striving for process intensification by transfer from batch to continuous processing, as well as an alternative catalytic system, different process options are evaluated with regard to their environmental impact to identify bottlenecks and improvement potentials for further process development activities.

  7. Peculiar surface behavior of some ionic liquids based on active pharmaceutical ingredients.

    Science.gov (United States)

    Restolho, José; Mata, José Luis; Saramago, Benilde

    2011-02-21

    The ionic liquids based on biologically active cations and anions, commonly designated by ionic liquids based on active pharmaceutical ingredients (ILs-APIs), are interesting compounds for use in pharmaceutical applications. Lidocaine docusate, ranitidine docusate, and didecyldimethylammonium ibuprofen are examples of promising ILs-APIs that were recently synthesized. They were submitted to biological testing and calorimetric measurements, but nothing is known about their surface properties. In this work, we measured the surface tension and the contact angles on both hydrophilic and hydrophobic surfaces in a temperature range as wide as possible. Based on the wettability data, the polarity fractions were estimated using the Fowkes theory. The peculiar surface behavior observed was tentatively attributed to the presence of mesophases.

  8. Neurobehavioral and genotoxic parameters of antipsychotic agent aripiprazole in mice

    Institute of Scientific and Technical Information of China (English)

    Jaqueline Nascimento PICADA; Viviane Minuzzo PONTES; Patrícia PEREIRA; Bruna de Jesus Neto DOS SANTOS; Franciele CELSO; Jéssica Dias MONTEIRO; Kelly Morais DA ROSA; Leandro Rosa CAMACHO; Luciana Rodrigues VIEIRA; Taís Madelon FREITAS; Tatiana Grasiela DASILVA

    2011-01-01

    Aim:Aripiprazole is an antipsychotic agent to treat schizophrenia,which acts through dopamine D2 partial agonism,serotonin 5-HT1A partial agonism and 5-HT2A antagonism.This study was designed to evaluate the neurobehavioral effects and genotoxic/mutagenic activities of the agent,as well as its effects on lipoperoxidation.Methods:Open field and inhibitory avoidance tasks were used.Thirty min before performing the behavioral tasks,adult male CF-1 mice were administered aripiprazole (1,3 or 10 mg/kg,ip) once for the acute treatment,or the same doses for 5 d for the subchronic treatment.Genotoxic effects were assessed using comet assay in the blood and brain tissues.Mutagenic effects were evaluated using bone marrow micronucleus test.Lipoperoxidation was assessed with thiobarbituric acid reactive substances (TBARS).Results:Acute and subchronic treatments significantly decreased the number of crossing and rearing in the open field task.Acute treatment significantly increased the step-down latency for both the short- and long-term memory in the inhibitory avoidance task.Subchronic treatments with aripiprazole (3 and 10 mg/kg) caused significant DNA strain-break damage in peripheral blood but not in the brain.Mutagenic effect was not detected in the acute and subchronic treatments.Nor TBARS levels in the liver were affected.Conclusion:Aripiprazole improved memory,but could impair motor activities in mice.The drug increased DNA damage in blood,but did not show mutagenic effects,suggesting that it might affect long-term genomic stability.

  9. Kinetics of the esterification of active pharmaceutical ingredients containing carboxylic Acid functionality in polyethylene glycol

    DEFF Research Database (Denmark)

    Schou-Pedersen, Anne Marie V; Hansen, Steen Honoré; Moesgaard, Birthe;

    2014-01-01

    Polyethylene glycols (PEGs) are attractive as excipients in the manufacture of drug products because they are water soluble and poorly immunogenic. They are used in various pharmaceutical preparations. However, because of their terminal hydroxyl groups, PEGs can participate in esterification...... reactions. In this study, kinetics of two active pharmaceutical ingredients, cetirizine and indomethacin possessing carboxylic acid functionality, has been studied in PEG 400 and PEG 1000 at 50°C, 60°C, 70°C, and 80°C. HPLC-UV was applied for the determination of concentrations in the kinetic studies......, it is important to be aware of this drug-excipient interaction, as it can reduce the shelf-life of a low-average molecular weight PEG formulation considerably. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:2424-2433, 2014....

  10. Oxidation of Mixed Active Pharmaceutical Ingredients in Biologically Treated Wastewater by ClO2

    DEFF Research Database (Denmark)

    Moradas, Gerly; Fick, Jerker; Ledin, Anna

    2011-01-01

    Biologically treated wastewater containing a mixture of 53 active pharmaceutical ingredients (APIs)was treated with 0-20 mg/l chlorine dioxide (ClO2) solution. Wastewater effluents were taken from two wastewater treatment plants in Sweden, one with (low COD) and one without (high COD) extended...... removed at 5 mg/l ClO2 dose. Removal of the same APIs from the high COD effluent was observed when the ClO2 dose was increased to 1.25 mg/l and an increase in API removal only after treatment with 8 mg/l ClO2. This illustrates that treatment of wastewater effluents with chlorine dioxide has potential...

  11. Continuous Processing of Active Pharmaceutical Ingredients Suspensions via Dynamic Cross-Flow Filtration.

    Science.gov (United States)

    Gursch, Johannes; Hohl, Roland; Toschkoff, Gregor; Dujmovic, Diana; Brozio, Jörg; Krumme, Markus; Rasenack, Norbert; Khinast, Johannes

    2015-10-01

    Over the last years, continuous manufacturing has created significant interest in the pharmaceutical industry. Continuous filtration at low flow rates and high solid loadings poses, however, a significant challenge. A commercially available, continuously operating, dynamic cross-flow filtration device (CFF) is tested and characterized. It is shown that the CFF is a highly suitable technology for continuous filtration. For all tested model active pharmaceutical ingredients, a material-specific strictly linear relationship between feed and permeate rate is identified. Moreover, for each tested substance, a constant concentration factor is reached. A one-parameter model based on a linear equation is suitable to fully describe the CFF filtration performance. This rather unexpected finding and the concentration polarization layer buildup is analyzed and a basic model to describe the observed filtration behavior is developed.

  12. The Potential of Cyclodextrins as Novel Active Pharmaceutical Ingredients: A Short Overview

    Directory of Open Access Journals (Sweden)

    Massimiliano Pio di Cagno

    2016-12-01

    Full Text Available Cyclodextrins (CDs are cyclic oligosaccharides of natural origin that were discovered more than 100 years ago. The peculiar cone-like conformation of the sugar ring, expressing a lipophilic cavity and a hydrophilic external surface, allows these substances to spontaneously complex poorly soluble compounds in an aqueous environment. For more than 50 years, these substances have found applicability in the pharmaceutical and food industries as solubilizing agents for poorly soluble chemical entities. Nowadays, several research groups all over the world are investigating their potential as active pharmaceutical ingredients (APIs for the treatment of several illnesses (e.g., hypercholesterolemia, cancer, Niemann-Pick Type C disease. The aim of this review is to briefly retrace cyclodextrins’ legacy as complexing agents and describe the current and future prospects of this class of chemical entities in pharmaceutics as new APIs.

  13. [Adherence to treatment, by active ingredient, in patients over 65 years on multiple medication].

    Science.gov (United States)

    Núñez Montenegro, Antonio J; Montiel Luque, Alonso; Martín Aurioles, Esther; Torres Verdú, Barbara; Lara Moreno, Celinda; González Correa, José Antonio

    2014-05-01

    To assess the level of adherence, by active ingredient, to treatment and associated factors in polymedicated patients over 65 years-old. Observational, descriptive and cross-sectional study over polymedicated patients over 65 years of the Costa del Sol Health District and the North Malaga Health Area. The study was performed between January 2011 and September 2012 on 375 subjects obtained by simple random sampling from lists provided by each health centre. Data was collected by means of an interview with structured questions. Informed consent was given and signed by all patients before interview. Main results variable adherence to treatment (Morisky-Green's test). Prescription by active ingredient, socio-demographic variables, health care centre variables, and treatment associated variables. A descriptive analysis of variables was performed. Statistical inference was determined using univariate analysis (t test of Student or Mann-Whitney U, and Chi-squared), and controlling for confounding factors by multivariate analysis (linear and logistic regression). The result for therapeutic compliance was 51.7%. No statistically significant differences were observed as regards sex and age. A relationship was found in those who resided in rural areas (P=.001), lived with family (P<.05), and were not at risk of suffering from anxiety (P=.046). We found similar patient adherence to treatment despite the prescribing generic drugs. Failure to therapeutic compliance was greater in those patients who lived by themselves, in a city close to the coast, or in those patients who were at risk of suffering from anxiety. Copyright © 2013 Elsevier España, S.L. All rights reserved.

  14. Review article: health benefits of some physiologically active ingredients and their suitability as yoghurt fortifiers.

    Science.gov (United States)

    Fayed, A E

    2015-05-01

    The article is concerned with health benefits of two main physiologically active ingredients namely, Isoflavones and γ-Aminobutyric acid, with emphasis on their fitness for fortification of yoghurt to be consumed as a functional food. Isoflavones (ISO) are part of the diphenol compounds, called "phytoestrogens," which are structurally and functionally similar to estradiol, the human estrogen, but much less potent. Because of this similarity, ISO were suggested to have preventive effects for many kinds of hormone-dependent diseases. In nature, ISO usually occur as glycosides and, once deconjugated by the intestinal microflora, the ISO can be absorbed into the blood. At present, it seems convincing their possible protective actions against various cancers, osteoporosis and menopausal symptoms and high levels of blood cholesterol as well as the epidemiological evidence. Γ-Aminobutyric acid (GABA), it is an amino acid that has long been reported to lower blood pressure by intravenous administration in experimental animals and in human subjects. GABA is present in many vegetables and fruits but not in dairy products. GABA was reported to lower blood pressure in people with mild hypertension. It was suggested that low-dose oral GABA has a hypotensive effect in spontaneously hypertensive. Yoghurt beyond its ability to be probiotic food via its culturing with the gut strains, it could further carry more healthy benefits when it was fortified with physiological active ingredients, especially GABA versus ISO preferring, whether, bacteriologically or biochemically, a fortification level of 50 mg ISO/kg or 200 mg GABA/kg.

  15. Genotoxic effects of the herbicide Roundup Transorb and its active ingredient glyphosate on the fish Prochilodus lineatus.

    Science.gov (United States)

    Moreno, Natália Cestari; Sofia, Silvia Helena; Martinez, Claudia B R

    2014-01-01

    Roundup Transorb (RT) is a glyphosate-based herbicide and despite its wide use around the world there are few studies comparing the effects of the active ingredient with the formulated product. In this context the purpose of this study was to compare the genotoxicity of the active ingredient glyphosate with the formulated product RT in order to clarify whether the active ingredient and the surfactant of the RT formula may exert toxic effects on the DNA molecule in juveniles of fish Prochilodus lineatus. Erythrocytes and gill cells of fish exposed to glyphosate and to RT showed DNA damage scores significantly higher than control animals. These results revealed that both glyphosate itself and RT were genotoxic to gill cells and erythrocytes of P. lineatus, suggesting that their use should be carefully monitored considering their potential impact on tropical aquatic biota. Copyright © 2013 Elsevier B.V. All rights reserved.

  16. 78 FR 3900 - Generic Drug User Fee-Active Pharmaceutical Ingredient and Finished Dosage Form Facility Fee...

    Science.gov (United States)

    2013-01-17

    ... drug active pharmaceutical ingredient (API) and finished dosage form (FDF) facilities user fees for... applications in the backlog as of October 1, 2012, on finished dosage form (FDF) and active pharmaceutical... Finished Dosage Form Facility Fee Rates for Fiscal Year 2013 AGENCY: Food and Drug Administration,...

  17. Gallic Acid, the Active Ingredient of Terminalia bellirica, Enhances Adipocyte Differentiation and Adiponectin Secretion.

    Science.gov (United States)

    Makihara, Hiroko; Koike, Yuka; Ohta, Masatomi; Horiguchi-Babamoto, Emi; Tsubata, Masahito; Kinoshita, Kaoru; Akase, Tomoko; Goshima, Yoshio; Aburada, Masaki; Shimada, Tsutomu

    2016-01-01

    Visceral obesity induces the onset of metabolic disorders such as insulin resistance and diabetes mellitus. Adipose tissue is considered as a potential pharmacological target for treating metabolic disorders. The fruit of Terminalia bellirica is extensively used in Ayurvedic medicine to treat patients with diseases such as diabetes mellitus. We previously investigated the effects of a hot water extract of T. bellirica fruit (TB) on obesity and insulin resistance in spontaneously obese type 2 diabetic mice. To determine the active ingredients of TB and their molecular mechanisms, we focused on adipocyte differentiation using mouse 3T3-L1 cells, which are widely used to study adipocyte physiology. We show here that TB enhanced the differentiation of 3T3-L1 cells to mature adipocytes and that one of the active main components was identified as gallic acid. Gallic acid (10-30 µM) enhanced the expression and secretion of adiponectin via adipocyte differentiation and also that of fatty acid binding protein-4, which is the target of peroxisome proliferator-activated receptor gamma (PPARγ), although it does not alter the expression of the upstream genes PPARγ and CCAAT enhancer binding protein alpha. In the PPARγ ligand assay, the binding of gallic acid to PPARγ was undetectable. These findings indicate that gallic acid mediates the therapeutic effects of TB on metabolic disorders by regulating adipocyte differentiation. Therefore, TB shows promise as a candidate for preventing and treating patients with metabolic syndrome.

  18. Acetylcholinesterase inhibitory activity of Thai traditional nootropic remedy and its herbal ingredients.

    Science.gov (United States)

    Tappayuthpijarn, Pimolvan; Itharat, Arunporn; Makchuchit, Sunita

    2011-12-01

    The incidence of Alzheimer disease (AD) is increasing every year in accordance with the increasing of elderly population and could pose significant health problems in the future. The use of medicinal plants as an alternative prevention or even for a possible treatment of the AD is, therefore, becoming an interesting research issue. Acetylcholinesterase (AChE) inhibitors are well-known drugs commonly used in the treatment of AD. The aim of the present study was to screen for AChE inhibitory activity of the Thai traditional nootropic recipe and its herbal ingredients. The results showed that ethanolic extracts of four out of twenty-five herbs i.e. Stephania pierrei Diels. Kaempfera parviflora Wall. ex Baker, Stephania venosa (Blume) Spreng, Piper nigrum L at 0.1 mg/mL showed % AChE inhibition of 89, 64, 59, 50; the IC50 were 6, 21, 29, 30 microg/mL respectively. The other herbs as well as combination of the whole recipe had no synergistic inhibitory effect on AChE activity. However some plants revealed antioxidant activity. More research should have be performed on this local wisdom remedy to verify the uses in scientific term.

  19. Intestinal, portal, and peripheral profiles of daikenchuto (TU-100)'s active ingredients after oral administration.

    Science.gov (United States)

    Watanabe, Junko; Kaifuchi, Noriko; Kushida, Hirotaka; Matsumoto, Takashi; Fukutake, Miwako; Nishiyama, Mitsue; Yamamoto, Masahiro; Kono, Toru

    2015-10-01

    A pharmaceutical grade Japanese traditional medicine, daikenchuto (TU-100), consisting of Japanese pepper, processed ginger, and ginseng, has been widely used for various intestinal disorders in Japan and now under development as a new therapeutic drug in the US. It is suggested that TU-100 ingredients exert pharmacological effects on intestines via two routes, from the luminal side before absorption and the peripheral blood stream after absorption. Therefore, in order to fully understand the pharmacological actions of TU-100, it is critically important to know the intraluminal amounts and forms of ingested TU-100 ingredients. In the present study, after administrating TU-100 to rats, the concentrations of TU-100 ingredients and their conjugates in the peripheral and portal blood and ileal contents were determined by LC-MS/MS. Next, TU-100 was administered to patients with ileostomy bags, but whose small intestines are diagnosed as healthy, and the ingredients/conjugates in the ileal effluent were analyzed. The results suggest that: (1) Pepper ingredients hydroxysanshools are rapidly absorbed and enter systemic circulation, (2) Ginseng ingredients ginsenosides are transported to the colon with the least absorption, (3) Ginger ingredients gingerols are absorbed and some conjugated in the small intestine and transported via the portal vein. While only a small amount of gingerols/gingerol conjugates enter systemic circulation, considerable amounts reappear in the small intestine. Thus, the effect of TU-100 on the intestines is believed to be a composite of multiple actions by multiple compounds supplied via multiple routes.

  20. Effects of rhubarb and the active ingredients of rhubarb on the cytoplasmic free calcium in INTMNC of rabbits

    Institute of Scientific and Technical Information of China (English)

    Xiu Zhen Lin; De Lu Ma; Zhi Qing Cui; Yi Kang

    2000-01-01

    @@INTRODUCTION The recent studies have shown that rhubarb has not only the effect of removing stasis by purgation, but also intestinal barrier effects[1,2]. In order to further clarify the intestinal barrier mechanism of rhubarb, we studied the effects of rhubarb decoction and the active ingredients of rhubarb on the cytoplasmic free calcium in isolated intestinal mononuclear cells (INT-MNC)

  1. Active Ingredients of Instructional Coaching: Developing a Conceptual Framework. R2Ed Working Paper 2015-3

    Science.gov (United States)

    White, Andrew S.; Howell Smith, Michelle; Kunz, Gina M.; Nugent, Gwen C.

    2015-01-01

    Although researchers have explored the impact of instructional coaching and named possible elements believed essential to effective coaching, there has yet to emerge from the literature a coherent model of those essential elements ("active ingredients"). This qualitative study sought to identify those elements through a systematic…

  2. Collaborative Care for Patients With Severe Personality Disorders: Preliminary Results and Active Ingredients From a Pilot Study (Part I)

    NARCIS (Netherlands)

    dr Barbara Stringer; Pieter Karman; Ad Kerkhof; Bauke Koekkoek; Aartjan Beekman; prof Berno van Meijel; Adriaan Hoogendoorn

    2014-01-01

    PURPOSE: To test if a collaborative care program (CCP) with nurses in a coordinating position is beneficial for patients with severe personality disorders. DESIGN AND METHODS: A pilot study with a comparative multiple case study design using mixed methods investigating active ingredients and

  3. Effects of ginsenosides, the active ingredients of Panax ginseng, on development, growth, and life span of Caenorhabditis elegans

    Science.gov (United States)

    Ginsenosides, the active ingredients of Panax ginseng, are saponins derived from sterols. The free-living nematode Caenorhabditis elegans is a well-established model for biochemical and genetic studies in animals. Although cholesterol is an essential requirement for the growth and development of C. ...

  4. Dampened neural activity and abolition of epileptic-like activity in cortical slices by active ingredients of spices.

    Science.gov (United States)

    Pezzoli, Maurizio; Elhamdani, Abdeladim; Camacho, Susana; Meystre, Julie; González, Stephanie Michlig; le Coutre, Johannes; Markram, Henry

    2014-10-31

    Active ingredients of spices (AIS) modulate neural response in the peripheral nervous system, mainly through interaction with TRP channel/receptors. The present study explores how different AIS modulate neural response in layer 5 pyramidal neurons of S1 neocortex. The AIS tested are agonists of TRPV1/3, TRPM8 or TRPA1. Our results demonstrate that capsaicin, eugenol, menthol, icilin and cinnamaldehyde, but not AITC dampen the generation of APs in a voltage- and time-dependent manner. This effect was further tested for the TRPM8 ligands in the presence of a TRPM8 blocker (BCTC) and on TRPM8 KO mice. The observable effect was still present. Finally, the influence of the selected AIS was tested on in vitro gabazine-induced seizures. Results coincide with the above observations: except for cinnamaldehyde, the same AIS were able to reduce the number, duration of the AP bursts and increase the concentration of gabazine needed to elicit them. In conclusion, our data suggests that some of these AIS can modulate glutamatergic neurons in the brain through a TRP-independent pathway, regardless of whether the neurons are stimulated intracellularly or by hyperactive microcircuitry.

  5. Understanding real-world implementation quality and "active ingredients" of PBIS.

    Science.gov (United States)

    Molloy, Lauren E; Moore, Julia E; Trail, Jessica; Van Epps, John James; Hopfer, Suellen

    2013-12-01

    Programs delivered in the "real world" often look substantially different from what was originally intended by program developers. Depending on which components of a program are being trimmed or altered, such modifications may seriously undermine the effectiveness of a program. In the present study, these issues are explored within a widely used school-based, non-curricular intervention, Positive Behavioral Intervention and Supports. The present study takes advantage of a uniquely large dataset to gain a better understanding of the "real-world" implementation quality of PBIS and to take a first step toward identifying the components of PBIS that "matter most" for student outcomes. Data from 27,689 students and 166 public primary and secondary schools across seven states included school and student demographics, indices of PBIS implementation quality, and reports of problem behaviors for any student who received an office discipline referral during the 2007-2008 school year. Results of the present study identify three key components of PBIS that many schools are failing to implement properly, three program components that were most related to lower rates of problem behavior (i.e., three "active ingredients" of PBIS), and several school characteristics that help to account for differences across schools in the quality of PBIS implementation. Overall, findings highlight the importance of assessing implementation quality in "real-world" settings, and the need to continue improving understanding of how and why programs work. Findings are discussed in terms of their implications for policy.

  6. Consequences of new approach of chemical stability tests of active pharmaceutical ingredients (APIs

    Directory of Open Access Journals (Sweden)

    Marzena eJamrógiewicz

    2016-02-01

    Full Text Available There is a great need of broaden look on stability tests of active pharmaceutical ingredients (APIs in comparison with current requirements contained in pharmacopoeia. By usage of many modern analytical methods the conception of monitoring the changes of APIs during initial stage of their exposure to harmful factors has been developed. New knowledge must be acquired in terms of identification of each degradation products, especially volatile ones. Further research as toxicology prediction during in silico studies of determined and identified degradation products is necessary. In silico methods are known as computational toxicology or computer-assisted technologies which are used for predicting toxicology of pharmaceutical substances such as impurities or degradation products. This is a specialized software and databases intended to calculate probability of genotoxicity or mutagenicity of these substances through a chemical structure-based screening process and algorithm specific to a given software program. Applying of new analytical approach is proposed as the usage of PAT tools, XRD, HS-SPME GC-MS/MS, LC-MS/MS for stability testing. Described improvements should be taken into account in case of each drug existing already in the market as well as being implemented as new one.

  7. Impact of active ingredients on the swelling properties of orally disintegrating tablets prepared by microwave treatment.

    Science.gov (United States)

    Sano, Syusuke; Iwao, Yasunori; Kimura, Susumu; Noguchi, Shuji; Itai, Shigeru

    2014-07-01

    The impact of different active pharmaceutical ingredients (APIs) loading on the properties of orally disintegrating tablets (ODTs) prepared according to our previously reported microwave (MW) treatment process was evaluated using famotidine (FAM), acetaminophen (AAP), and ibuprofen (IBU). None of the APIs interrupted the tablet swelling during the MW treatment and the tablet hardness were improved by more than 20 N. MW treatment, however, led to a significant increase in the disintegration time of the ODTs containing IBU, but it had no impact on that of the ODTs containing FAM or AAP. This increased disintegration time of the ODTs containing IBU was attributed to the relatively low melting point of IBU (Tm=76 °C), with the IBU particles melting during the MW treatment to form agglomerates, which interrupted the penetration of water into the tablets and delayed their disintegration. The effects of the MW treatment on the chemical stability and dissolution properties of ODTs were also evaluated. The results revealed that MW treatment did not promote the degradations of FAM and AAP or delay their release from the ODTs, while dissolution of the ODTs containing IBU delayed by MW treatment. Based on these results, the MW method would be applicable to the preparation of ODTs containing APIs with melting points higher than 110 °C. Copyright © 2014 Elsevier B.V. All rights reserved.

  8. Approaches to the Development of Human Health Toxicity Values for Active Pharmaceutical Ingredients in the Environment.

    Science.gov (United States)

    Sorell, Tamara L

    2016-01-01

    Management of active pharmaceutical ingredients (API) in the environment is challenging because these substances represent a large and diverse group of compounds. Advanced wastewater treatment technologies that can remove API tend to be costly. Because of the potential resources required to address API in the environment, there is a need to establish environmental benchmarks that can serve as targets for treatment and release. To date, there are several different approaches that have been taken to derive human health toxicity values for API. These methods include traditional risk assessment approaches that calculate "safe" doses using experimental data and uncertainty (safety) factors; point of departure (POD), which starts from a therapeutic human dose and applies uncertainty factors; and threshold of toxicological concern (TTC), a generic approach that establishes threshold values across broad classes of chemicals based on chemical structure. To evaluate the use of these approaches, each of these methods was applied to three API commonly encountered in the environment: acetaminophen, caffeine, and chlorpromazine. The results indicate that the various methods of estimating toxicity values produce highly varying doses. Associated doses are well below typical intakes, or toxicity thresholds cannot be derived due to a lack of information. No uniform approach can be applied to establishing thresholds for multiple substances. Rather, an individualized approach will need to be applied to each target API.

  9. Co-crystallization: An approach to improve the performance characteristics of active pharmaceutical ingredients

    Directory of Open Access Journals (Sweden)

    Jignasa Ketan Savjani

    2015-01-01

    Full Text Available Co-crystal chemistry has recently attracted supramolecular scientists. Co-crystals are comprising of hydrogen boding assembly between different molecules. Many issues related to performance characteristics of an active pharmaceutical ingredient (API can be resolved using co-crystallization approach. Proper understanding of crystal structure of an API is required for successful formation of co-crystals with the selected co-former. This review article focus on explanation about co-crystals, intellectual property rights, their advantages and limitations. Co-crystallization can be achieved using different methods like co-grinding slurry based, solvent evaporation method, etc. Methods of co-crystallization are simple and increase the purity of the final product. Co-crystallization can be applied to the drugs prescribed in combination therapy. Stoichiometric composition of different drugs used in combination therapy can be co-crystallize to form one solid state form. Physicochemical properties of APIs such as solubility and stability can be improved using co-crystallization approach. With due regards co-crystallization should be used with caution because of some issues during manufacturing of final product.

  10. Study of Active Ingredients in Black Soybean Sprouts and Their Safety in Cosmetic Use

    Directory of Open Access Journals (Sweden)

    Yinmao Dong

    2012-10-01

    Full Text Available Active ingredients in different lengths of black soybean sprouts were extracted with water. Concentrations of the main proteins and polysaccharides were determined by the Forint phenol assay and phenol-sulfuric acid assay, respectively. Anti-oxidizing capacities of the extracts were measured in vitro using the DPPH scavenging test and whitening capacity was measured in vitro using the tyrosinase inhibition test. The effects of the bean sprout extracts on human skin fibroblasts damnified by H2O2 were studied using an MTT colorimetric assay. The safety of the extracts was determined using the red blood cell (RBC test, chick chorioallantoic membrane (CAM assay and human patch test. Results show that DPPH radical scavenging rates at different shoot lengths were all greater than 95%, while the tyrosinase inhibition capacity of the extracts reached 98%. Hemolysis rate in all extracts were lower than 10%, below the 20% regulatory limit for the RBC test. No signs of allergic reactions were observed in the human patch tests. The optimum extract was obtained from bean sprouts grown to 0.5 cm. Extracts of black bean sprouts are safe and can be used as additives in anti-aging and whitening cosmetic products.

  11. Capturing the Active Ingredients of Multicomponent Participatory Organizational Stress Interventions Using an Adapted Study Design.

    Science.gov (United States)

    Biron, Caroline; Ivers, Hans; Brun, Jean-Pierre

    2016-10-01

    Adapted study designs use process evaluation to incorporate a measure of intervention exposure and create an artificial control and intervention groups. Taking into account exposure levels to interventions combines process and outcome evaluation and strengthens the design of the study when exposure levels cannot be controlled. This study includes longitudinal data (two assessments) with added process measures at time 2 gathered from three complex participatory intervention projects in Canada in a hospital and a university. Structural equation modelling was used to explore the specific working mechanisms of particular interventions on stress outcomes. Results showed that higher exposure to interventions aiming to modify tasks and working conditions reduced demands and improved social support, but not job control, which in turn, reduced psychological distress. Exposure to interventions aiming to improve relationships was not related to psychosocial risks. Most studies cannot explain how interventions produce their effects on outcomes, especially when there are multiple concurrent interventions delivered in several contexts. This study advances knowledge on process evaluation by using an adapted study design to capture the active ingredients of multicomponent interventions and suggesting some mechanisms by which the interventions produce their effects on stress outcomes. It provides an illustration of how to conduct process evaluation and relate exposure levels to observed outcomes. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

  12. Prioritization methodology for the monitoring of active pharmaceutical ingredients in hospital effluents.

    Science.gov (United States)

    Daouk, Silwan; Chèvre, Nathalie; Vernaz, Nathalie; Bonnabry, Pascal; Dayer, Pierre; Daali, Youssef; Fleury-Souverain, Sandrine

    2015-09-01

    The important number of active pharmaceutical ingredients (API) available on the market along with their potential adverse effects in the aquatic ecosystems, lead to the development of prioritization methods, which allow choosing priority molecules to monitor based on a set of selected criteria. Due to the large volumes of API used in hospitals, an increasing attention has been recently paid to their effluents as a source of environmental pollution. Based on the consumption data of a Swiss university hospital, about hundred of API has been prioritized following an OPBT approach (Occurrence, Persistence, Bioaccumulation and Toxicity). In addition, an Environmental Risk Assessment (ERA) allowed prioritizing API based on predicted concentrations and environmental toxicity data found in the literature for 71 compounds. Both prioritization approaches were compared. OPBT prioritization results highlight the high concern of some non steroidal anti-inflammatory drugs and antiviral drugs, whereas antibiotics are revealed by ERA as potentially problematic to the aquatic ecosystems. Nevertheless, according to the predicted risk quotient, only the hospital fraction of ciprofloxacin represents a risk to the aquatic organisms. Some compounds were highlighted as high-priority with both methods: ibuprofen, trimethoprim, sulfamethoxazole, ritonavir, gabapentin, amoxicillin, ciprofloxacin, raltegravir, propofol, etc. Analyzing consumption data and building prioritization lists helped choosing about 15 API to be monitored in hospital wastewaters. The API ranking approach adopted in this study can be easily transposed to any other hospitals, which have the will to look at the contamination of their effluents.

  13. Development of a solvate as an active pharmaceutical ingredient: Developability, crystallisation and isolation challenges

    Science.gov (United States)

    Douillet, Julien; Stevenson, Neil; Lee, Mei; Mallet, Franck; Ward, Richard; Aspin, Peter; Dennehy, Daniel Robert; Camus, Laure

    2012-03-01

    The preclinical development of an active pharmaceutical ingredient (API) begins with the selection of a solid state form. A solvate may be selected for development if it is sufficiently stable and if the solvent quantity administered to the patient is lower than the tolerated potential daily exposure (PDE). The selection and process development of a solvate is presented here. The initial crystallisation process gave poor control over the particle size distribution (PSD) and inclusion of additional crystallisation solvent in the crystal lattice. These two API attributes were controlled using micronised seeds and optimising the crystallisation conditions. After filtration, slurry washing with a second solvent was used to replace the high boiling point crystallisation solvent to improve the drying efficiency. The slurry washing was modelled and studied in the laboratory to control the level of unbound crystallisation solvent in the API. The API desolvation during slurry washing was studied by considering thermodynamics, by construction of the ternary phase diagram, and kinetics aspects. This work provides useful approaches and considerations to assess the risks specific to the controlled production of a solvate that are rarely presented in the literature.

  14. Microwave-assisted extraction of active pharmaceutical ingredient from solid dosage forms.

    Science.gov (United States)

    Hoang, T H; Sharma, R; Susanto, D; Di Maso, M; Kwong, E

    2007-07-13

    The microwave assisted extraction (MAE) technique has been evaluated for the extraction of active pharmaceutical ingredients (API) from various solid dosage forms. Using immediate release tablets of Compound A as a model, optimization of the extraction method with regards to extraction solvent composition, extraction time and temperature was briefly discussed. Complete recovery of Compound A was achieved when samples were extracted using acetonitrile as the extraction solvent under microwave heating at a constant cell temperature of 50 degrees C for 5 min. The optimized MAE method was applied for content uniformity (single tablet extraction) and potency (multiple tablets extraction) assays of release and stability samples of two products of Compound A (5 and 25mg dose strength) stored at various conditions. To further demonstrate the applicability of MAE, the instrumental extraction conditions (50 degrees C for 5 min) were adopted for the extraction of montelukast sodium (Singulair) from various solid dosage forms using methanol-water (75:25, v/v) as the extraction solvent. The MAE procedure demonstrated an extraction efficiency of 97.4-101.9% label claim with the greatest RSD at 1.4%. The results compare favorably with 97.6-102.3% label claim with the greatest RSD at 2.9% obtained with validated mechanical extraction procedures. The system is affordable, user-friendly and simple to operate and troubleshoot. Rapid extraction process (7 min/run) along with high throughput capacity (up to 23 samples simultaneously) would lead to reduced cycle time and thus increased productivity.

  15. Determination of Four Active Ingredients in Vc Yinqiao Tablets by Capillary Zone Electrophoresis with Amperometric Detection

    Institute of Scientific and Technical Information of China (English)

    L(U),Jin; WANG,Qing-Jiang; CHENG,Xi; LIU,Hai-Yan; HE,Pin-Gang; FANG,Yu-Zhi

    2006-01-01

    A simple, reliable and reproducible method, based on capillary zone electrophoresis with amperometric detection (CZE-AD), has been developed for simultaneous determination of four active ingredients in Vc Yinqiao tablets including paracetamol, vitamin C, caffeic acid and chlorogenic acid. A carbon-disk electrode was used as working electrode and 0.95 V (versus SCE) was selected as detection potential. The optimal conditions of CZE experiment were 30 mmol·L-1 borate solution (pH 9.5) as running buffer, 14 kV as separation voltage and 8 s (14 kV) as electro-kinetic sampling time. Under the selected optimum conditions, paracetamol, vitamin C, caffeic acid and chlorogenic acid could be perfectly separated within 22 min, and their detection limits (S/N=3) ranged from 5 × 10-7 to 1×10-6 mol·L-1. This proposed method demonstrated good reproducibility with relative standard deviations of less than 3% for both migration time and peak current (n=7). The utility of this method was demonstrated by monitoring a kind of compound medicine named Vc Yinqiao tablets and the assay results were satisfactory.

  16. Direct analysis of palladium in active pharmaceutical ingredients by anodic stripping voltammetry.

    Science.gov (United States)

    Rosolina, Samuel M; Chambers, James Q; Xue, Zi-Ling

    2016-03-31

    Anodic stripping voltammetry, a classical electroanalytical method has been optimized to analyze trace Pd(II) in active pharmaceutical ingredient matrices. The electroanalytical approach with an unmodified glassy carbon electrode was performed in both aqueous and 95% DMSO/5% water (95/5 DMSO/H2O) solutions, without pretreatment such as acid digestion or dry ashing to remove the organics. Limits of detection (LODs) in the presence of caffeine and ketoprofen were determined to be 11 and 9.6 μg g(-1), with a relative standard deviation (RSD) of 5.7% and 2.3%, respectively. This method is simple, highly reproducible, sensitive, and robust. The instrumentation has the potential to be portable and the obviation of sample pretreatment makes it an ideal approach for determining lost catalytic metals in pharmaceutical-related industries. Furthermore, the simultaneous detection of Pd(II) with Cd(II) and Pb(II) in the low μg L(-1) range indicates that this system is capable of simultaneous multi-analyte analysis in a variety of matrices.

  17. Use of prediction methods to estimate true density of active pharmaceutical ingredients.

    Science.gov (United States)

    Cao, Xiaoping; Leyva, Norma; Anderson, Stephen R; Hancock, Bruno C

    2008-05-01

    True density is a fundamental and important property of active pharmaceutical ingredients (APIs). Using prediction methods to estimate the API true density can be very beneficial in pharmaceutical research and development, especially when experimental measurements cannot be made due to lack of material or sample handling restrictions. In this paper, two empirical prediction methods developed by Girolami and Immirzi and Perini were used to estimate the true density of APIs, and the estimation results were compared with experimentally measured values by helium pycnometry. The Girolami method is simple and can be used for both liquids and solids. For the tested APIs, the Girolami method had a maximum error of -12.7% and an average percent error of -3.0% with a 95% CI of (-3.8, -2.3%). The Immirzi and Perini method is more involved and is mainly used for solid crystals. In general, it gives better predictions than the Girolami method. For the tested APIs, the Immirzi and Perini method had a maximum error of 9.6% and an average percent error of 0.9% with a 95% CI of (0.3, 1.6%).

  18. Inactive ingredient Search for Approved Drug Products

    Data.gov (United States)

    U.S. Department of Health & Human Services — According to 21 CFR 210.3(b)(8), an inactive ingredient is any component of a drug product other than the active ingredient. Only inactive ingredients in the final...

  19. Bacteriological Effects of Dentifrices with and without Active Ingredients of Natural Origin

    Science.gov (United States)

    Latimer, Joe; Humphreys, Gavin J.; Sreenivasan, Prem K.; McBain, Andrew J.

    2014-01-01

    Compounds of natural origin are increasingly used as adjuncts to oral hygiene. We have adopted four distinct approaches to assess the antibacterial activity of dentifrices containing natural active ingredients against oral bacteria in several test systems. Corsodyl Daily (CD), Kingfisher Mint (KM), and Parodontax fluoride (PF) were compared to a dentifrice containing fluoride (Colgate Cavity Protection [CCP]) and one containing triclosan (Colgate Total [CT]). The growth inhibitory and bactericidal potency of the formulations were determined for 10 isolated oral bacteria. Effects of single exposures of simulated supragingival plaques were then determined by epifluorescence and confocal microscopy, while the effects of repeated exposures were quantified by viable counting. Additionally, dense plaques, maintained in continuous culture, were repeatedly dosed, and the outcome was assessed by viable counting and eubacterial DNA profiling. The test dentifrices exhibited variable specificity and potency against oral bacteria in axenic culture. Of the herbal formulations, KM caused the largest viability reductions in simulated supragingival plaques, with CT causing the greatest reductions overall. Following single exposures, CD caused moderate reductions, while PF had no effect. After multiple dosing, all formulations significantly reduced numbers of total, facultative, and Gram-negative anaerobes, but only KM and CT caused greater reductions than the fluoride control. KM also reduced counts of streptococci (rank order of effectiveness: CT > KM > CCP > PF > CD). Marked changes in eubacterial DNA profiles were not detected for any herbal formulation in dense plaques, although KM markedly reduced viable counts of streptococci, in agreement with supragingival data. While both nonherbal comparators displayed antibacterial activity, the triclosan-containing formulation caused greater viability reductions than the herbal and nonherbal formulations. PMID:25107974

  20. Identification of aroma active compounds of cereal coffee brew and its roasted ingredients.

    Science.gov (United States)

    Majcher, Małgorzata A; Klensporf-Pawlik, Dorota; Dziadas, Mariusz; Jeleń, Henryk H

    2013-03-20

    Cereal coffee is a coffee substitute made mainly from roasted cereals such as barley and rye (60-70%), chicory (15-20%), and sugar beets (6-10%). It is perceived by consumers as a healthy, caffeine free, non-irritating beverage suitable for those who cannot drink regular coffee made from coffee beans. In presented studies, typical Polish cereal coffee brew has been subjected to the key odorants analysis with the application of gas chromatography-olfactometry (GC-O) and aroma extract dilution analysis (AEDA). In the analyzed cereal coffee extract, 30 aroma-active volatiles have been identified with FD factors ranging from 16 to 4096. This approach was also used for characterization of key odorants in ingredients used for the cereal coffee production. Comparing the main odors detected in GC-O analysis of roasted cereals brew to the odor notes of cereal coffee brew, it was evident that the aroma of cereal coffee brew is mainly influenced by roasted barley. Flavor compound identification and quantitation has been performed with application of comprehensive multidimentional gas chromatography and time-of-flight mass spectrometry (GCxGC-ToFMS). The results of the quantitative measurements followed by calculation of the odor activity values (OAV) revealed 17 aroma active compounds of the cereal coffee brew with OAV ranging from 12.5 and 2000. The most potent odorant was 2-furfurylthiol followed by the 3-mercapto-3-methylbutyl formate, 3-isobutyl-2-methoxypyrazine and 2-ethyl-3,5-dimethylpyrazine, 2-thenylthiol, 2,3-butanedione, 2-methoxy phenol and 2-methoxy-4-vinyl phenol, 3(sec-butyl)-2-methoxypyrazine, 2-acetyl-1-pyrroline, 3-(methylthio)-propanal, 2,3-pentanedione, 4-hydroxy-2,5-dimethyl-3-(2H)-furanone, (E,E)-2,4-decadienal, (Z)-4-heptenal, phenylacetaldehyde, and 1-octen-3-one.

  1. Aripiprazole Can Improve Apraxia of Eyelid Opening in Parkinson's Disease.

    Science.gov (United States)

    Tokisato, Kaori; Fukunaga, Kimiko; Tokunaga, Makoto; Watanabe, Susumu; Nakanishi, Ryoji; Yamanaga, Hiroaki

    2015-01-01

    We herein report three cases of Parkinson's disease associated with difficulty in eyelid opening, referred to as apraxia of eyelid opening (AEO), which improved after aripiprazole treatment. In case 1, aripiprazole was administered as a psychiatric treatment. It proved to be effective in AEO with blepharospasm. In case 2 and case 3, the patients experienced AEO without blepharospasm, and a significant improvement was observed after aripiprazole treatment. In this study, the aripiprazole dosage ranged between 3 and 9 mg/day. This is the first report of aripiprazole as a potentially effective treatment for AEO in Parkinson's disease.

  2. Types of Pesticide Ingredients

    Science.gov (United States)

    Pesticide active ingredients are described by the types of pests they control or how they work. For example, algicides kill algae, biopesticides are derived from natural materials, and insecticides kill insects.

  3. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient

    OpenAIRE

    Hao Sun; Guangwen Luo; Dahui Chen; Zheng Xiang

    2016-01-01

    AbstractRhein is a major medicinal ingredient isolated from several traditional Chinese medicines, including Rheum palmatum L., Aloe barbadensis Miller, Cassia angustifolia Vahl., and Polygonum multiflorum Thunb. Rhein has various pharmacological activities, such as anti-inflammatory, antitumor, antioxidant, antifibrosis, hepatoprotective, and nephroprotective activities. Although more than 100 articles in PubMed are involved in the pharmacological mechanism of action of rhein, only a few foc...

  4. Tardive Dyskinesia and Covert Dyskinesia with Aripiprazole: A Case Series.

    Science.gov (United States)

    Patra, Suravi

    2016-01-01

    Aripiprazole, a dopamine stabilizing atypical antipsychotic is used in treatment of tardive dyskinesia caused by other neuroleptics. Tardive dyskinesia is rarely caused by Aripiprazole and has only been documented in high risk patients i.e., female gender, advanced age, affective illness, coexisting neurological disorders. Here the author describes two atypical cases of tardive dyskinesia associated with Aripiprazole. First case of tardive dyskinesia was observed in a neuroleptic naïve young adult male with paranoid illness after six months of treatment with Aripiprazole upon addition of Fluoxetine and the second case was a middle aged female with affective illness where dyskinetic movements appeared after stopping Aripiprazole. The role of Fluoxetine in causing tardive dyskinesia with Aripiprazole and covert dyskinesia due to Aripiprazole with appropriate management is discussed.

  5. The Active Ingredients of Jiang-Zhi-Ning: Study of the Nelumbo nucifera Alkaloids and Their Main Bioactive Metabolites

    Directory of Open Access Journals (Sweden)

    Wei Wang

    2012-08-01

    Full Text Available The object of this study was to identify the major active ingredients of the Chinese Traditional Medicine Jiang-Zhi-Ning (JZN based on the high performance liquid chromatography (HPLC profiles of plasma samples obtained from beagle dogs at different times after intragastric administration of JZN, crude JZN extracts, different extracted fractions, different subfractions of the active fraction and different isolated ingredients. 2-Hydroxy-1-methoxyaporphin (2H1M, an alkaloid from Nelumbo nucifera, one of the herbs that make up JZN, was identified as the constituent showing the major pharmacodynamic effect. The major metabolites of 2H1M were analyzed and identified as N-demethyl-2-hydroxy-1-methoxyaporphine-2-O-glycuronic acid, 2-hydroxy-1-methoxy-aporphine-2-O-glycuronic acid and 2-hydroxy-1-methoxy-aporphine-2-O-sulphate. This study provided a comprehensive insight into the active components of JZN.

  6. Active pharmaceutical ingredients detected in herbal food supplements for weight loss sampled on the Dutch market.

    Science.gov (United States)

    Reeuwijk, Noortje M; Venhuis, Bastiaan J; de Kaste, Dries; Hoogenboom, Ron L A P; Rietjens, Ivonne M C M; Martena, Martijn J

    2014-01-01

    Herbal food supplements claiming to reduce weight may contain active pharmacological ingredients (APIs) that can be used for the treatment of overweight and obesity. The aim of this study was to determine whether herbal food supplements for weight loss on the Dutch market contain APIs with weight loss properties. Herbal food supplements intended for weight loss (n = 50) were sampled from August 2004 to May 2013. An HPLC-DAD-MS/MS method was used to screen for the presence of the APIs in herbal supplements. In 24 samples the APIs sibutramine, desmethylsibutramine (DMS), didesmethylsibutramine (DDMS), rimonabant, sildenafil and/or the laxative phenolphthalein were identified 41 times. The presence of these APIs was, however, not stated on the label. The potential pharmacological effects of the detected APIs were estimated using data from reported effective doses of approved drugs. Use of 20 of the 24 herbal food supplements may result in potential pharmacological effects. Furthermore, risk assessment of phenolphthalein, a suspected carcinogen and found to be present in 10 supplements, based on the margin of exposure (MOE) approach, resulted in MOE values of 96-30,000. MOE values lower than 10,000 (96-220) were calculated for the daily intake levels of four out of these 10 supplements in which phenolphthalein was found. However, taking into account that weight loss preparations may be used for only a few weeks or months rather than during a lifetime, MOE values may be two to three orders of magnitude higher. The current study shows that the use of food supplements with sibutramine, DMS, DDMS and/or phenolphthalein could result in pharmacological effects.

  7. Dissolution study of active pharmaceutical ingredients using molecular dynamics simulations with classical force fields

    Science.gov (United States)

    Greiner, Maximilian; Elts, Ekaterina; Schneider, Julian; Reuter, Karsten; Briesen, Heiko

    2014-11-01

    The CHARMM, general Amber and OPLS force fields are evaluated for their suitability in simulating the molecular dynamics of the dissolution of the hydrophobic, small-molecule active pharmaceutical ingredients aspirin, ibuprofen, and paracetamol in aqueous media. The force fields are evaluated by comparison with quantum chemical simulations or experimental references on the basis of the following capabilities: accurately representing intra- and intermolecular interactions, appropriately reproducing crystal lattice parameters, adequately describing thermodynamic properties, and the qualitative description of the dissolution behavior. To make this approach easily accessible for evaluating the dissolution properties of novel drug candidates in the early stage of drug development, the force field parameter files are generated using online resources such as the SWISS PARAM servers, and the software packages ACPYPE and Maestro. All force fields are found to reproduce the intermolecular interactions with a reasonable degree of accuracy, with the general Amber and CHARMM force fields showing the best agreement with quantum mechanical calculations. A stable crystal bulk structure is obtained for all model substances, except for ibuprofen, where the reproductions of the lattice parameters and observed crystal stability are considerably poor for all force fields. The heat of solution used to evaluate the solid-to-solution phase transitions is found to be in qualitative agreement with the experimental data for all combinations tested, with the results being quantitatively optimum for the general Amber and CHARMM force fields. For aspirin and paracetamol, stable crystal-water interfaces were obtained. The (100), (110), (011) and (001) interfaces of aspirin or paracetamol and water were simulated for each force field for 30 ns. Although generally expected as a rare event, in some of the simulations, dissolution is observed at 310 K and ambient pressure conditions.

  8. Core-shell column Tanaka characterization and additional tests using active pharmaceutical ingredients.

    Science.gov (United States)

    Ludvigsson, Jufang Wu; Karlsson, Anders; Kjellberg, Viktor

    2016-12-01

    In the last decade, core-shell particles have gained more and more attention in fast liquid chromatography separations due to their comparable performance with fully porous sub-2 μm particles and their significantly lower back pressure. Core-shell particles are made of a solid core surrounded by a shell of classic fully porous material. To embrace the developed core-shell column market and use these columns in pharmaceutical analytical applications, 17 core-shell C18 columns purchased from various vendors with various dimensions (50 mm × 2.1 mm to 100 mm × 3 mm) and particle sizes (1.6-2.7 μm) were characterized using Tanaka test protocols. Furthermore, four selected active pharmaceutical ingredients were chosen as test probes to investigate the batch to batch reproducibility for core-shell columns of particle size 2.6-2.7 μm, with dimension of 100 × 3 mm and columns of particle size 1.6 μm, with dimension 100 × 2.1 mm under isocratic elution. Columns of particle size 2.6-2.7 μm were also tested under gradient elution conditions. To confirm the claimed comparable efficiency of 2.6 μm core-shell particles as sub-2 μm fully porous particles, column performances of the selected core-shell columns were compared with BEH C18 , 1.7 μm, a fully porous column material as well.

  9. Active ingredient-containing chitosan/polycaprolactone nonwoven mats: Characterizations and their functional assays

    Energy Technology Data Exchange (ETDEWEB)

    Bai, Meng-Yi, E-mail: mybai@mail.ntust.edu.tw [Graduate Institute of Biomedical Engineering, National Taiwan University of Science and Technology, Taipei 10607, Taiwan, ROC (China); Adjunct appointment to the Department of Biomedical Engineering, National Defense Medical Center, Taipei 114, Taiwan, ROC (China); Chou, Tz-Chong, E-mail: tcchou@ms5.hinet.net [Department of Biomedical Engineering, National Defense Medical Center, Taipei 114, Taiwan, ROC (China); Tsai, Jie-Chang; Yang, Hui-Ching [Graduate Institute of Biomedical Engineering, National Taiwan University of Science and Technology, Taipei 10607, Taiwan, ROC (China)

    2013-01-01

    This study demonstrates a facile method developed to generate a chitosan/polycaprolactone (CS/PCL) nonwoven mat. All nonwoven mats are composed of microfibers with an average diameter of 2.51 {+-} 0.69 {mu}m. The X-ray photoelectron spectroscopy data indicate that positively charged nitrogen was generated on the surface of the mats after undergoing CS coating. By using a non-contacting electrostatic voltmeter, we determined that the nonwoven mats exhibited a positive potential and the charge density of the CS/PCL nonwoven mat was in proportion to the thickness of the CS overlayer. Moreover, platelet aggregation and anti-bacterial ability were enhanced by the CS/PCL nonwoven mat as compared to that of PCL nonwoven mat alone. The enhancements of the CS/PCL nonwoven mat on platelet aggregation are further promoted by incorporating a 1 mM calcium ion in its CS overlayer. We also find that the addition of tea tree oil in the CS overlayer significantly inhibited LPS-induced nitrite formation in Raw 264.7 macrophages. In conclusion, our CS/PCL nonwoven mat possesses pharmacological effects including an increase of platelet aggregation, anti-bacterial, anti-adhesive, and anti-inflammatory activities. The performance of this CS/PCL nonwoven mat can be further promoted by incorporating active compounds to exert therapeutic effects in wound healing. Highlights: Black-Right-Pointing-Pointer We develop a facile method to generate active ingredient-containing CS/PCLNM. Black-Right-Pointing-Pointer Our CS/PCLNM possesses superior mechanical strength, compared to CS-blended PCL nanofibers. Black-Right-Pointing-Pointer We prove that our prepared CS/PCLNM possesses several pharmacological properties Black-Right-Pointing-Pointer The functional performances of CS/PCLNM are enhanced by incorporation of active compounds. Black-Right-Pointing-Pointer Incorporation of 1 mM of calcium ions or 100 {mu}L of TTO into the CS overlayer of CS/PCLNM is the optimum dose.

  10. Antifungal activities and active ingredients of Melodinus suaveolens Champ. ex Benth.

    Science.gov (United States)

    Xu, Yanan; Ling, Siquan; Zeng, Dongqiang; Tang, Wenwei

    2017-07-16

    Four Melodinus species with antifungal activity were found in survey of the floral resources, in Shiwan Mountain Natural Reserve, Guangxi Province, China. Crude methanolic extracts of the twigs and leaves of Melodinus suaveolens exhibited potent antifungal activities against the plant pathogenic fungi Colletotrichum musae, Colletotrichum graminicola, Colletotrichum gloeosporioides and Alternaria musae, and the ethyl acetate fraction inhibited these pathogens at rates of 85.37, 91.47, 72.77 and 89.87%, respectively (5 mg/mL). A new compound, (2R, 3S, 5S, 6R)-1-O-methyl- chiro-inositol was isolated from the ethyl acetate fraction, along with 15 known compounds. The antifungal activities of compounds (1-16) were evaluated for the first time. Compound (4) had potent antifungal activity against C. gloeosporioides, C. graminicola and A. musae.

  11. Chitin-Hyaluronan Nanoparticles: A Multifunctional Carrier to Deliver Anti-Aging Active Ingredients through the Skin

    Directory of Open Access Journals (Sweden)

    Pierfrancesco Morganti

    2014-07-01

    Full Text Available The paper describes the process to produce Chitin Nanofibril-Hyaluronan nanoparticles (CN-HA, showing their ability to easily load active ingredients, facilitate penetration through the skin layers, and increase their effectiveness and safety as an anti-aging agent. Size and characterization of CN-HA nanoparticles were determined by Scanning Electron Microscopy (SEM and Zetasizer, while encapsulation efficiency and loading capacity of the entrapped ingredients were controlled by chromatographic and spectrophotometric methods. Safeness was evidenced on fibroblasts and keratinocytes culture viability by the MTT (Methylthiazol assay; anti-aging activity was evaluated in vitro measuring antioxidant capacity, anti-collagenase activity, and metalloproteinase and pro-inflammatory release; efficacy was shown in vivo by a double-blind vehicle-controlled study for 60 days on 60 women affected by photo-aging. In addition, the CN-HA nanoparticles have shown interesting possibility to be used as active ingredients, for designing and making advanced medication by the electrospinning technology, as well as to produce transparent films for food packaging, by the casting method, and can be used also in their dry form as tissues or films without adding preservatives. These unusual CN-HA nanoparticles obtained from the use of raw materials of waste origin may offer an unprecedented occasion for making innovative products, ameliorating the quality of life, reducing pollution and safeguarding the environment’s integrity.

  12. Aripiprazole blocks acute self-administration of cocaine and is not self-administered in mice

    DEFF Research Database (Denmark)

    Sørensen, Gunnar; Sager, Thomas N; Petersen, Jørgen H

    2008-01-01

    doses (0.03, 0.1, and 0.3 mg/kg/infusion) even caused significant decreases in nose-poking activity, possibly due to extrapyramidal side effects. CONCLUSIONS: These data are consistent with a potential role for aripiprazole in treatment of cocaine addiction without abuse potential per se....

  13. Quantitative analysis of active pharmaceutical ingredients (APIs) using a potentiometric electronic tongue in a SIA flow system

    OpenAIRE

    2016-01-01

    An advanced potentiometric electronic tongue and Sequential Injection Analysis (SIA) measurement system was applied for the quantitative analysis of mixtures containing three active pharmaceutical ingredients (APIs): acetaminophen, ascorbic acid and acetylsalicylic acid, in the presence of various amounts of caffeine as interferent. The flow-through sensor array was composed of miniaturized classical ion-selective electrodes based on plasticized PVC membranes containing only ion exchangers. P...

  14. Mathematical Modeling of the Release of Active Ingredients from a Contraceptive Patch: Ortho Evra® as a Case Study

    OpenAIRE

    Trujillo-de Santiago, Grissel; Patricio Sáenz-Collins, Carlos; García-Arellano, Lizette; Moisés Álvarez, Mario

    2014-01-01

    Contraceptive patches have become a frequently used contraceptive method. We present a mathematical model that describes the serum concentration profiles of Norelgestromin (NGMN) and Ethinylestradiol (EE) released from the contraceptive patch Ortho Evra®. We propose a simple one-compartment model based on pharmacokinetics data reported in previous studies. The model assumes a time-dependent release rate and a first order elimination rate for each of the active ingredients contained in the pat...

  15. Antifeedant Activity and Active Ingredients Against Plutella xylostella from Momordica charantia Leaves

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    With the bioguided fractionation of the ethanol extracts from the leaves of Momordica charantia, we obtained two most active compounds against the feeding of the diamondback moth, Plutella xylostella larvae. The antifeedant activity of momordicine Ⅰ and momordicine Ⅱ against the second and the third instar larvae of Plutella xylostella were tested using leaf discs of cabbage in the laboratory. The results showed that momordicin Ⅰ and momordiein Ⅱ had significant antifeedant activity on the larvae of P. Xylostella, and momordicin Ⅱ was more active than momordicin Ⅰ. The concentrations for 50% antifeedant effects (AFC50) of momordicin Ⅱ against the second and the third instar larvae of P. Xylostella were 76.69 and 116.24 μg mL-1, whereas that of momordicin Ⅰ was 144.08 and 168.42 μg mL-1, respectively. In addition, momordicin Ⅰ and momordicin Ⅱ had significant inhibitive effect on the rate of weight gain and survival of P. Xylostella larvae.

  16. Effects of surfactants and thermodynamic activity of model active ingredient on transport over plant leaf cuticle.

    Science.gov (United States)

    Fagerström, Anton; Kocherbitov, Vitaly; Ruzgas, Tautgirdas; Westbye, Peter; Bergström, Karin; Engblom, Johan

    2013-03-01

    The main objective of this study was to investigate the mechanism of molecular transport across the cuticle of Clivia leaves. In vitro diffusion methodology was used to investigate the transport of a systemic fungicide, tebuconazole, over a model silicone membrane, enzymatically isolated cuticle membranes, and dermatomed leaves. It was shown that dermatomed leaves may replace enzymatically isolated cuticles. Furthermore, the effects of two surfactants, C(10)EO(7) and C(8)G(1.6), on the fungicide transport were investigated. Tebuconazole cuticle permeation was described using Fick's first law of diffusion, expressed by the thermodynamic activity of the solute in the membrane. A new method for calculation of diffusion coefficients in the membrane is proposed. To access the thermodynamic activity of the fungicide in the membranes, sorption isotherms of tebuconazole in the membrane materials studied were recorded. The thermodynamic activity of the fungicide in aqueous solutions was calculated from solubility data. For that purpose, the effect of surfactants on tebuconazole solubility was studied. The results show that addition of surfactants allows for higher concentrations of tebuconazole available for penetration. Nonetheless, at a fixed fungicide thermodynamic activity, all formulations produced the same flux over the silicone membrane independently on the fungicide concentration. This shows that the driving force across non-responding membranes is the gradient of thermodynamic activity, rather than the gradient of the fungicide concentration. In case of leaves, surfactants induced the same quantitative increase in both flux and diffusion coefficient of solute in the cuticle, while the cuticle-water partition coefficient was unaffected.

  17. Evaluation of fipronil and imidacloprid as bait active ingredients against fungus-growing termites (Blattodea: Termitidae: Macrotermitinae).

    Science.gov (United States)

    Iqbal, N; Evans, T A

    2017-05-03

    Fungus-growing termites (Macrotermitinae) are important pests in tropical countries. They are difficult to control with existing baiting methods, as chitin synthesis inhibitors are not effectual as active ingredients. We tested two neurotoxins, fipronil and imidacloprid, as potential bait active ingredients against Macrotermes gilvus (Hagen) in Singapore. In laboratory bioassays, M. gilvus showed no preference for doses of 0-64 ppm fipronil, or for doses of 0-250 ppm imidacloprid, indicating no repellence. We tested each insecticide in toilet paper as a bait matrix in a field experiment. After 28 days, termites had eaten 5-13% of the fipronil treated toilet paper, abandoned bait and monitoring stations, contacted no new stations, and repaired poorly their experimentally damaged mounds. Termites ate no imidacloprid treated toilet paper, abandoned bait stations although contacted new stations, and repaired fully their damaged mounds. Termites ate 60-70% of the control toilet paper, remained in bait stations, and fully repaired damaged mounds. After 56 days, all five fipronil colonies were eliminated, whereas all of the imidacloprid and control colonies were healthy. The results suggest that fipronil could be an effective active ingredient in bait systems for fungus-growing termites in tropical countries.

  18. 3D printed orodispersible films with Aripiprazole.

    Science.gov (United States)

    Jamróz, Witold; Kurek, Mateusz; Łyszczarz, Ewelina; Szafraniec, Joanna; Knapik-Kowalczuk, Justyna; Syrek, Karolina; Paluch, Marian; Jachowicz, Renata

    2017-05-24

    Three dimensional printing technology is gaining in importance because of its increasing availability and wide applications. One of the three dimensional printing techniques is Fused Deposition Modelling (FDM) which works on the basis of hot melt extrusion-well known in the pharmaceutical technology. Combination of fused deposition modelling with preparation of the orodispersible film with poorly water soluble substance such as aripiprazole seems to be extra advantageous in terms of dissolution rate. 3D printed as well as casted films were compared in terms of physicochemical and mechanical properties. Moreover, drug-free films were prepared to evaluate the impact of the extrusion process and aripiprazole presence on the film properties. X-ray diffractometry and thermal analyses confirmed transition of aripiprazole into amorphous state during film preparation using 3D printing technique. Amorphization of the aripiprazole and porous structure of printed film led to increased dissolution rate in comparison to casted films, which, however have slightly better mechanical properties due to their continuous structure. It can be concluded that fused deposition modelling is suitable technique and polyvinyl alcohol is applicable polymer for orodispersible films preparation. Copyright © 2017 Elsevier B.V. All rights reserved.

  19. Investigation of active pharmaceutical ingredient loss in pharmaceutical compounding of capsules.

    Science.gov (United States)

    D'Hondt, Matthias; Wynendaele, Evelien; Vandercruyssen, Kirsten; Bauters, Tiene; Vandenbroucke, Johan; Mullens, Steven; Vervaet, Chris; Remon, Jean Paul; De Spiegeleer, Bart

    2014-08-05

    Pharmaceutical compounding of capsules is still an important corner stone in today's health care. It allows for a more patient specific treatment plan as opposed to the "one size fits all"-approach, used by the pharmaceutical industry when producing fixed dose finished drug products. However, loss of active pharmaceutical ingredient (API) powder during pharmaceutical capsule compounding can lead to under-dosed finished drug products and annul the beneficiary therapeutic effects for the patient. The amount and location of API loss was experimentally determined during capsule compounding of five different preparations: 10 and 20mg hydrocortisone capsules, 4mg triamcinolone capsules and 0.25mg dexamethasone capsules, using a 10% m/m self-made or commercial trituration. The total API amount present in the five capsule preparations varied between 90.8% and 96.6%, demonstrating that for certain preparations, significant API mass loss occurred during the pharmaceutical compounding of capsules. Swabbing results of the different compounding equipment and working areas indicated the mortar surface as the largest API loss location. An agate mortar accounted for the least amount of API loss, whereas an extensively used porcelain mortar accounted for the highest amount of API loss. Optical microscopy and roughness (Ra) determination by profilometry of the different mortar surfaces revealed a significant influence of the mortar surface wear and tear on the observed API loss. This observation can be explained by physical deformation, or scratch formation, of the relatively soft porcelain mortar surface, in which the API particles can become adsorbed. Furthermore, a small effect of the capsulation device material on the API loss was also observed. The presence of a chemical molecule effect on the API loss was demonstrated through data mining using a set of assay results containing 17 different molecules and 1922 assay values. The 17 median assay values were modeled in function of

  20. The significance of different health institutions and their respective contributions of active pharmaceutical ingredients to wastewater.

    Science.gov (United States)

    Herrmann, Manuel; Olsson, Oliver; Fiehn, Rainer; Herrel, Markus; Kümmerer, Klaus

    2015-12-01

    Active pharmaceutical ingredients (APIs) have been frequently found in the environment. It is, however, still not quite clear who is mainly responsible for API emissions. Hospitals have been considered to be the main contributing point sources for wastewater (WW) discharge of APIs. However, recent studies have shown that the contribution of hospitals to the input of APIs into the aquatic environment is quite low. Due to demographic change and the increase of psychiatric diseases, health institutions (HIs) such as psychiatric hospitals and nursing homes are likely to be important sources as well, but no data is available in this respect. This study aims to assess the impact of HIs and to provide a methodology to measure their respective contributions. Drawing on pharmaceutical consumption data for the years 2010, 2011, and 2012, this study identified API usage patterns for a psychiatric hospital (146 beds), a nursing home (286 inhabitants), and a general hospital (741 beds), the latter of which comprises three separate locations. All the HIs are located in two sub-regions of a county district with about 400,000 citizens in southwestern Germany. A selection of neurological drugs was quantified in the sewer of these facilities to evaluate the correlation between consumption and emission. The API contribution of HIs was assessed by comparing the specific consumption in the facilities with the consumption in households, expressed as the emission potential (IEP). The study shows that the usage patterns of APIs in the psychiatric hospital and the nursing home were different from the general hospital. Neurological drugs such as anticonvulsants, psycholeptics, and psychoanaleptics were mainly consumed in the psychiatric hospital and the nursing home (74% and 65%, respectively). Predicted and average measured concentrations in the effluent of the investigated HIs differed mostly by less than one order of magnitude. Therefore, the consumption-based approach is a useful method

  1. Anti-inflammaging and antiglycation activity of a novel botanical ingredient from African biodiversity (Centevita™

    Directory of Open Access Journals (Sweden)

    Maramaldi G

    2013-12-01

    Full Text Available Giada Maramaldi,1 Stefano Togni,1 Federico Franceschi,1 Elian Lati21Indena SpA, Milan, Italy; 2Laboratoire BIO-EC, Longjumeau, FrancePurpose: The aim of this study was to investigate the topical efficacy of a new purified extract from Madagascar, Gotu Kola (Centella asiatica [L.] Urban, both on human explants and on human volunteers, in relation to skin wrinkling and skin protection against ultraviolet light exposure. The extract, with a peculiar content of biologically active molecules, was investigated as a novel anti-inflammaging and antiglycation agent. Its typical terpenes, known as collagen synthesis promoters, represent at least 45% of the extract. It also contains a polyphenolic fraction cooperating to the observed properties.Methods: C. asiatica purified extract was assayed on human skin explants maintained alive, and several parameters were evaluated. Among the most relevant, the thymine dimerization was evaluated by immunostaining. Malondialdehyde formation was evaluated as free-radical scavenging marker by enzyme-linked immunosorbent assay. The expression of interleukin-1a was observed by enzyme-linked immunosorbent assay as well. The product was further evaluated as an antiglycation agent, being glycation quantified by the advanced glycation product carboxymethyl lysine. C. asiatica purified extract was also evaluated as an antiwrinkling agent in a single-blind, placebo-controlled study. Formulated in a simple oil-in-water emulsion, the extent of wrinkling was assessed by skin replicas, skin firmness, skin elasticity, and collagen density measurements.Results: C. asiatica purified extract could protect DNA from ultraviolet light-induced damage, decreasing the thymine photodimerization by over 28% (P<0.05. A reduced (26%, P<0.01 expression of interleukin-1α was also observed, supporting its anti-inflammatory potential. C. asiatica purified extract showed in vitro a total inhibition of carboxymethyl lysine formation induced by the

  2. Special active ingredients and beauty-food%特种活性物及营养美容

    Institute of Scientific and Technical Information of China (English)

    韩建英

    2012-01-01

    介绍了特种活性物及营养美容的理念。消费者目前对营养美容理念的兴趣越来越浓厚,使得营养美容产品逐渐成为市场营销的热点。配方师也热衷于将营养品与美容相结合,开发出营养美容产品,并将营养美容对身体的益处都囊括在产品配方中。介绍了几种最具潜力的营养美容成分以及特种活性物成分,并对其前景进行了展望。%The idea of special active ingredients and beauty-food are introduced briefly. Nowadays, the consumers become more and more interested in the concept of beauty-food, and the beauty-food product category has gradually become the hot topic of marketing. Formulators are eager to combine the benefits of nutrition with beauty in the formulations, and develop the beauty-food products. Some diet beauty ingredients with the greatest potential are introduced, and the future of the special active ingredients and the beauty-food are prospected here.

  3. The effect of different formulations of equivalent active ingredients on the performance of two topical wound treatment products.

    Science.gov (United States)

    Gray, Mikel; Jones, David P

    2004-03-01

    Product selection for the management of pressure ulcers or perineal dermatitis is typically based on consideration of active ingredients, but a growing body of evidence suggests that delivery vehicles also may influence product safety and efficacy. A 10-day, randomized, controlled experimental study was conducted to compare the safety and efficacy of two prescription products used for the treatment of pressure ulcers and perineal dermatitis. Both products contain equivalent active ingredients (balsam of Peru, castor oil, and trypsin), but one product delivers these ingredients in an ointment base while the other uses an aerosol spray. Sixty healthy volunteers (> 65 years of age) underwent intentional creation of two equivalent skin wounds (approximately 6 mm in diameter) using an Erbium-YAG laser. Volunteers served as their own control. Wounds were randomized to treatment with one of the balsam of Peru products or saline. Wounds were evaluated every other day. Significant differences between treatments were observed for most outcome variables (edema, scabbing, erythema, epithelialization). Wounds managed with the ointment-based product had lower edema, scabbing, and erythema scores and higher epithelialization scores than the spray or saline managed wounds. The results of this study confirm that formulation of the vehicle base can have a significant effect on product safety and effectiveness.

  4. Formulation and evaluation of a water-in-oil cream containing herbal active ingredients and ferulic acid.

    Science.gov (United States)

    Moldovan, Mirela; Lahmar, Abir; Bogdan, Cătălina; Părăuan, Simona; Tomuţă, Ioan; Crişan, Maria

    2017-01-01

    The main aims of the present study were to formulate an anti-age cream based on vegetal ingredients and ferulic acid and to evaluate the physical characteristics and the efficacy of the cream. The active ingredients were Centella asiatica oil, Spilanthes acmella oil, Zingiber officinale extract and ferulic acid. Formulation 1 (F1) was prepared using glyceryl stearate and Ceteareth-25® as emulsifiers and Formulation 2 (F2) using glyceryl stearate and potassium cetyl phosphate, all other ingredients remaining the same. The physical characterization of the creams was performed and the following parameters were analyzed: viscosity, oil droplet size, polydispersity index; also, texture analysis was performed. The anti-aging effect of the F2 was evaluated by assessing the cutaneous density before and after cream application using DUB-cutis® scanner. The mean diameter of oil drops was 10.26±4.72 mm (F1) and 22.72±7.93 mm (F2) and the polydispersity index was 35.4% and 45.7%, respectively. The mean values for consistency were 594.7±10.3 g (F1) and 300.5±14.5 g (F2), the average values for adhesion were 15.61±0.8 mJ (F1) and 22.25±4.3 mJ (F2), for firmness were 51.2±0.8 g (F1) and 30.3±4.3 g (F2) and the spreadability had values between 72.63 mm2 (F1) and 73.3 mm2 (F2). In vivo study revealed that the mean values of the cutaneous density increased from 9.21±1.39 % to 12.50±1.44 % after 8 weeks of cream application. The herbal ingredients incorporated in the O/W cream base for the antioxidant activity and anti-wrinkle effect, induced changes of the cutaneous density, an important parameter which quantifies the regeneration process of the skin. An anti-age cream containing herbal active ingredients and ferulic acid with appropriate physical characteristics was obtained. In vivo study of clinical efficacy revealed a positive effect on skin density, which increased after 8 weeks of cream application.

  5. Continuous Hydrolysis and Liquid–Liquid Phase Separation of an Active Pharmaceutical Ingredient Intermediate Using a Miniscale Hydrophobic Membrane Separator

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Morthensen, Sofie Thage; Lewandowski, Daniel Jacob

    2012-01-01

    Continuous hydrolysis of an active pharmaceutical ingredient intermediate, and subsequent liquid–liquid (L-L) separation of the resulting organic and aqueous phases, have been achieved using a simple PTFE tube reactor connected to a miniscale hydrophobic membrane separator. An alkoxide product...... a PTFE membrane with 28 cm2 of active area. A less challenging separation of water and toluene was achieved at total flow rates as high as 80 mL/min, with potential to achieve even higher flow rates. The operability and flexibility of the membrane separator and a plate coalescer were compared...

  6. Two Cases of Hypersexuality Probably Associated with Aripiprazole

    OpenAIRE

    Cheon, EunJin; Koo, Bon-Hoon; Seo, Sang Soo; Lee, Jun-Yeob

    2013-01-01

    Sexual dysfunction is a common side effect in patients treated with antipsychotics but significant differences exist across different compounds. We report hypersexuality symptoms in two female patients with schizophrenia who were receiving treatment with aripiprazole. The patients experienced more frequent sexual desire and greater sexual preoccupation after taking aripiprazole. We discuss the potential neuro-chemical mechanisms for this and argue that aripiprazole's unique pharmacological pr...

  7. Artepillin C, a major ingredient of Brazilian propolis, induces a pungent taste by activating TRPA1 channels.

    Directory of Open Access Journals (Sweden)

    Taketoshi Hata

    Full Text Available Brazilian green propolis is a popular health supplement because of its various biological properties. The ethanol extract of Brazilian green propolis (EEBP is characteristic for its herb-like smell and unique pungent taste. However, the ingredients responsible for its pungency have not yet been identified. This study provides the first evidence that artepillin C is the main pungent ingredient in EEBP and that it potently activates human transient receptor potential ankyrin 1 (TRPA1 channels. EEBP was fractionated using column chromatography with a step gradient elution of an ethanol-water solution, and the fractions having the pungent taste were determined by sensory tests. HPLC analysis revealed that the pungent fraction was composed primarily of artepillin C, a prenylated derivative of cinnamic acid. Artepillin C was also identified as the pungent compound of EEBP by organoleptic examiners. Furthermore, the effects of artepillin C and other cinnamic acids found in EEBP on TRPA1 channels were examined by calcium imaging and plate reader-based assays in human TRPA1-expressing cells to investigate the molecular mechanisms underlying their pungent tastes. Artepillin C and baccharin activated the TRPA1 channel strongly, whereas drupanin caused a slight activation and p-coumaric acid showed no activation. Because the EC(50 values of artepillin C, baccharin, and allyl isothiocyanate were 1.8 µM, 15.5 µM, and 6.2 µM, respectively, artepillin C was more potent than the typical TRPA1 agonist allyl isothiocyanate. These findings strongly indicate that artepillin C is the main pungent ingredient in EEBP and stimulates a pungent taste by activating TRPA1 channels.

  8. Artepillin C, a Major Ingredient of Brazilian Propolis, Induces a Pungent Taste by Activating TRPA1 Channels

    Science.gov (United States)

    Hata, Taketoshi; Tazawa, Shigemi; Ohta, Shozo; Rhyu, Mee-Ra; Misaka, Takumi; Ichihara, Kenji

    2012-01-01

    Brazilian green propolis is a popular health supplement because of its various biological properties. The ethanol extract of Brazilian green propolis (EEBP) is characteristic for its herb-like smell and unique pungent taste. However, the ingredients responsible for its pungency have not yet been identified. This study provides the first evidence that artepillin C is the main pungent ingredient in EEBP and that it potently activates human transient receptor potential ankyrin 1 (TRPA1) channels. EEBP was fractionated using column chromatography with a step gradient elution of an ethanol-water solution, and the fractions having the pungent taste were determined by sensory tests. HPLC analysis revealed that the pungent fraction was composed primarily of artepillin C, a prenylated derivative of cinnamic acid. Artepillin C was also identified as the pungent compound of EEBP by organoleptic examiners. Furthermore, the effects of artepillin C and other cinnamic acids found in EEBP on TRPA1 channels were examined by calcium imaging and plate reader-based assays in human TRPA1-expressing cells to investigate the molecular mechanisms underlying their pungent tastes. Artepillin C and baccharin activated the TRPA1 channel strongly, whereas drupanin caused a slight activation and p-coumaric acid showed no activation. Because the EC50 values of artepillin C, baccharin, and allyl isothiocyanate were 1.8 µM, 15.5 µM, and 6.2 µM, respectively, artepillin C was more potent than the typical TRPA1 agonist allyl isothiocyanate. These findings strongly indicate that artepillin C is the main pungent ingredient in EEBP and stimulates a pungent taste by activating TRPA1 channels. PMID:23133611

  9. Combination of omega-3 Fatty acids, lithium, and aripiprazole reduces oxidative stress in brain of mice with mania.

    Science.gov (United States)

    Arunagiri, Pandiyan; Rajeshwaran, Krishnamoorthy; Shanthakumar, Janakiraman; Tamilselvan, Thangavel; Balamurugan, Elumalai

    2014-09-01

    Manic episode in bipolar disorder (BD) was evaluated in the present study with supplementation of omega-3 fatty acids in combination with aripiprazole and lithium on methylphenidate (MPD)-induced manic mice model. Administration of MPD 5 mg/kg bw intraperitoneally (i.p.) caused increase in oxidative stress in mice brain. To retract this effect, supplementation of omega-3 fatty acids 1.5 ml/kg (p.o.), aripiprazole 1.5 mg/kg bw (i.p.), and lithium 50 mg/kg bw (p.o) were given to mice. Omega-3 fatty acids alone and in combination with aripiprazole- and lithium-treated groups significantly reduced the levels of superoxide dismutase (SOD), catalase (CAT), and lipid peroxidation products (thiobarbituric acid reactive substances) in the brain. MPD treatment significantly decreased the reduced glutathione (GSH) level and glutathione peroxidase (GPx) activity, and they were restored by supplementation of omega-3 fatty acids with aripiprazole and lithium. There is no remarkable difference in the effect of creatine kinase (CK) activity between MPD-induced manic model and the treatment groups. Therefore, our results demonstrate that oxidative stress imbalance and mild insignificant CK alterations induced by administration of MPD can be restored back to normal physiological levels through omega-3 fatty acids combined with lithium and aripiprazole that attributes to effective prevention against mania in adult male Swiss albino mice.

  10. 2010年登记或上市农药品种%New Active Ingredients Registered or Launched in 2010

    Institute of Scientific and Technical Information of China (English)

    杨吉春; 吴峤; 李学建; 刘长令

    2011-01-01

    概述了2010年登记或上市的36个新农药品种,其中杀菌剂11个、杀虫剂4个、除草剂10个、熏蒸剂2个、杀线虫剂1个、生物农药和信息素8个.%A review of 36 new active ingredients registered or launched in 2010, in which there are 11 with fungicidal activity, 4 with insecticidal activity and acaricide, 10 with herbicidal activity, 2 with fumigation activity, 1 with nematicidal activity, 8 as biopesticides and pheromones.

  11. Aripiprazole for autism spectrum disorders (ASD).

    Science.gov (United States)

    Hirsch, Lauren E; Pringsheim, Tamara

    2016-06-26

    Autism spectrum disorders (ASD) include autistic disorder, Asperger's disorder and pervasive developmental disorder - not otherwise specified (PDD-NOS). Antipsychotics have been used as a medication intervention for irritability related to ASD. Aripiprazole, a third-generation, atypical antipsychotic, is a relatively new drug that has a unique mechanism of action different from that of other antipsychotics. This review updates a previous Cochrane review on the safety and efficacy of aripiprazole for individuals with ASD, published in 2011 (Ching 2011). To assess the safety and efficacy of aripiprazole as medication treatment for individuals with ASD. In October 2015, we searched the Cochrane Central Register of Controlled Trials (CENTRAL), Ovid MEDLINE, Embase, the Cumulative Index to Nursing and Allied Health Literature (CINAHL) and seven other databases as well as two trial registers. We searched for records published in 1990 or later, as this was the year aripiprazole became available. Randomised controlled trials (RCTs) of aripiprazole (administered orally and at any dosage) versus placebo for treatment of individuals with a diagnosis of ASD. Two review authors independently collected, evaluated and analysed data. We performed meta-analysis for primary and secondary outcomes, when possible. We used the GRADE (Grades of Recommendation, Assessment, Development and Evaluation) approach to rate the overall quality of the evidence. We included three trials in this review. Two were included in the previous published review, and the results of one, placebo-controlled discontinuation study were added to this review. Although we searched for studies across age groups, we found only studies conducted in children and youth. Included trials had low risk of bias across most domains. High risk of bias was seen in only one trial with incomplete outcome data. We judged the overall quality of the evidence for most outcomes to be moderate.Two RCTs with similar methods evaluated

  12. Preventive effects of Flos Perariae (Gehua water extract and its active ingredient puerarin in rodent alcoholism models

    Directory of Open Access Journals (Sweden)

    Wang Yuqiang

    2010-10-01

    Full Text Available Abstract Background Radix Puerariae is used in Chinese medicine to treat alcohol addiction and intoxication. The present study investigates the effects of Flos puerariae lobatae water extract (FPE and its active ingredient puerarin on alcoholism using rodent models. Methods Alcoholic animals were given FPE or puerarin by oral intubation prior or after alcohol treatment. The loss of righting reflex (LORR assay was used to evaluate sedative/hypnotic effects. Changes of gama-aminobutyric acid type A receptor (GABAAR subunits induced by alcohol treatment in hippocampus were measured with western blot. In alcoholic mice, body weight gain was monitored throughout the experiments. Alcohol dehydrogenase (ADH levels in liver were measured. Results FPE and puerarin pretreatment significantly prolonged the time of LORR induced by diazepam in acute alcoholic rat. Puerarin increased expression of gama-aminobutyric acid type A receptor alpha1 subunit and decreased expression of alpha4 subunit. In chronic alcoholic mice, puerarin pretreatment significantly increased body weight and liver ADH activity in a dose-dependent manner. Puerarin pretreatment, but not post-treatment, can reverse the changes of gama-aminobutyric acid type A receptor subunit expression and increase ADH activity in alcoholism models. Conclusion The present study demonstrates that FPE and its active ingredient puerarin have preventive effects on alcoholism related disorders.

  13. Evaluation of Essential Oil and its Three Main Active Ingredients of Chinese Chenopodium ambrosioides (Family: Chenopodiaceae) against Blattella germanica.

    Science.gov (United States)

    Zhu, Wei Xiang; Zhao, Kun; Chu, Sha Sha; Liu, Zhi Long

    2012-12-01

    The efficacy of essential oil of Chenopodium ambrosioides flowering aerial parts and its three main active ingredients was evaluated against Blattella germanica male adults. Composition of essential oil was determined by GC-MS. Topical application bioassay was used to evaluate contact toxicity of essential oil and three main components. Fumigant toxicity of essential oil and its main components was measured using a sealed space method. Twenty-two components were identified in the essential oil and the main components were (Z)-ascaridole (29.7%), isoascaridole (13.0%), ρ-cymene (12.7%) and piperitone (5.0%). The essential oil and (Z)-ascaridole, isoascaridole and ρ-cymene possessed fumigant toxicity against male German cockroaches with LC(50) values of 4.13, 0.55, 2.07 and 6.92 mg/L air, respectively. Topical application bioassay showed that all the three compounds were toxic to male German cockroaches and (Z)-ascaridole was the strongest with a LD(50) value of 22.02 μg/adult while the crude oil with a LD(50) value of 67.46 μg/adult. The essential oil from Chinese C. ambrosioides and its three main active ingredients may be explored as natural potential insecticides in the control of cockroaches.

  14. Physio-chemical Investigation and Natural Bond Orbital Analysis of the Most Actives Ingredient of Fennel Plant

    Directory of Open Access Journals (Sweden)

    Mansoureh Pishehabadi

    2016-10-01

    Full Text Available In this study, physio-chemical properties of effective compounds of fennel plant were investigated through using computational chemistry. To do this, trans-anethole, estragole, 3'- hydroxyanethole and 4- methoxycinnamyl alcohol compounds that the most active ingredient combinations make up the fennel plant have been carried out at three different levels of HF, BLYP and B3LYP theories using 6-31G*, 6-311G*, 6-311G**, 6-311+G and 6-311++G basis sets. Additionally, ab initio calculation in the gas phase have been studied and physio-chemical parameters including Gibbs free energy, thermal energy, enthalpy, entropy, and thermal capacity in constant volume (CV of these compounds have been computed as well as Gibbs free energy in polar solvents such as ethanol and methanol and water. Based on these obtained data the structural stabilities of these flavorful compounds have been discussed. However, in these herbal effective compounds presented here the natural bond orbital (NBO analysis has been performed which seemed quite informative to show some important atomic and structural features. The result lead to the issue that all those compounds in polar solvents, particularly alcoholic solvents solved and the compounds can be used sufficiently to extract the active ingredients of herb fennel.

  15. A Unique Combination of Nutritionally Active Ingredients Can Prevent Several Key Processes Associated with Atherosclerosis In Vitro.

    Directory of Open Access Journals (Sweden)

    Joe W E Moss

    Full Text Available Atherosclerosis is the underlying cause of cardiovascular disease that leads to more global mortalities each year than any other ailment. Consumption of active food ingredients such as phytosterols, omega-3 polyunsaturated fatty acids and flavanols are known to impart beneficial effects on cardiovascular disease although the combined actions of such agents in atherosclerosis is poorly understood. The aim of this study was to screen a nutritional supplement containing each of these active components for its anti-atherosclerotic effect on macrophages in vitro.The supplement attenuated the expression of intercellular adhesion molecule-1 and macrophage chemoattractant protein-1 in human and murine macrophages at physiologically relevant doses. The migratory capacity of human monocytes was also hindered, possibly mediated by eicosapentaenoic acid and catechin, while the ability of foam cells to efflux cholesterol was improved. The polarisation of murine macrophages towards a pro-inflammatory phenotype was also attenuated by the supplement.The formulation was able to hinder multiple key steps of atherosclerosis development in vitro by inhibiting monocyte recruitment, foam cell formation and macrophage polarisation towards an inflammatory phenotype. This is the first time a combination these ingredients has been shown to elicit such effects and supports its further study in preclinical in vivo models.

  16. Evaluation of the influence of sulfur fumigation on the pharmacokinetics of four active ingredients in Si Wu Tang.

    Science.gov (United States)

    Pei, Ke; Cai, Hao; Liu, Xiao; Tu, Sicong; Cao, Gang; Li, Huan; Zhao, Yingying; Song, Xiaoqing; Lou, Yajing; Qiao, Fengxian; Cai, Baochang

    2015-01-01

    Sulfur fumigation may induce the decrease or the chemical transformation of some active ingredients of traditional Chinese medicines in vitro. Whether sulfur fumigation can cause the pharmacokinetic changes of the active ingredients in vivo is related to the efficacy and the safety of Chinese medicines' application clinically. A sensitive, specific, and accurate method for the simultaneous determination of paeoniflorin, ferulic acid, senkyunolide A, and senkyunolide I in rat plasma by ultra high performance liquid chromatography coupled with triple quadrupole mass spectrometry was developed to evaluate the influence of sulfur fumigation to Si Wu Tang for the first time. Each compound was extracted from plasma samples by liquid-liquid extraction with ethyl acetate, and the chromatographic separation was accomplished on an Agilent Extend C18 column with a linear gradient elution. The mass spectrometric detection and analysis were performed by using an AB Sciex triple quadrupole 5500 mass spectrometer in multiple reaction monitoring mode. The validated method was successfully applied to a pharmacokinetic study of four compounds in rats after oral administration of sun-dried and sulfur-fumigated Si Wu Tang. The results provided a meaningful basis for evaluating the affection of sulfur fumigation to the clinical application and the efficacy of Si Wu Tang. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  17. Use of thin-layer chromatography to detect counterfeit sulfadoxine/pyrimethamine tablets with the wrong active ingredient in Malawi.

    Science.gov (United States)

    Khuluza, Felix; Kigera, Stephen; Jähnke, Richard W O; Heide, Lutz

    2016-04-14

    Substandard and falsified anti-malarial medicines pose a serious threat to public health, especially in low-income countries. Appropriate technologies for drug quality analysis in resource-limited settings are important for the surveillance of the formal and informal drug market. The feasibility of thin-layer chromatography (TLC) with different solvent systems was tested using the GPHF Minilab in a study of the quality of sulfadoxine/pyrimethamine tablets in Malawi. Twenty eight samples of sulfadoxine/pyrimethamine tablets were collected from randomly selected health facilities of four districts of southern Malawi. A mystery shopper approach was used when collecting samples from illegal street vendors, and an overt approach for the other facilities. Samples were subjected to visual inspection, disintegration testing and TLC analysis. 10 samples were further investigated according to the methods of the US Pharmacopeia using high performance liquid chromatography (HPLC). One sample was found to be falsified, containing a mixture of paracetamol tablets and co-trimoxazole tablets. These had been repackaged into paper strip packs labelled as a brand of sulfadoxine/pyrimethamine. TLC with different solvent systems readily proved that these tablets did not comply with their declaration, and provided strong evidence for the active pharmaceutical ingredients which were actually contained. Full pharmacopeial analysis by HPLC confirmed the results suggested by TLC for this sample, and showed two further samples to be of substandard quality. Due to the absence of the declared anti-malarial ingredients and due to the presence of other pharmaceutical ingredients, the identified falsified medicine represents a serious health risk for the population. Thin-layer chromatography (TLC) using different solvent systems proved to be a powerful method for the identification of this type of counterfeiting, presenting a simple and affordable technology for use in resource-limited settings.

  18. Postmortem Femoral Blood Reference Concentrations of Aripiprazole, Chlorprothixene, and Quetiapine

    DEFF Research Database (Denmark)

    Skov, Louise; Johansen, Sys Stybe; Linnet, Kristian

    2015-01-01

    Postmortem femoral blood concentrations of the antipsychotic drugs aripiprazole, chlorprothixene and its metabolite, and quetiapine were determined by LC-MS-MS in 25 cases for aripiprazole and 60 cases each for chlorprothixene and quetiapine. For cases where the cause of death was not related to ...

  19. Cichorium intybus root extract: A "vitamin D-like" active ingredient to improve skin barrier function.

    Science.gov (United States)

    Maia Campos, P M B G; G Mercurio, D; O Melo, M; Closs-Gonthier, B

    2017-02-01

    During the aging process, the human skin suffers many alterations including dryness, skin barrier function damage. The skin barrier function is important to the prevention of skin alterations and maintenance of homeostasis. So, the objective of this study was to assess the clinical efficacy on skin barrier function of Cichorium intybus root extract in cosmetic formulations with or without UV filters. Fifty women, aged between 45 and 60 years, were divided into two groups. One group received vehicle formulations containing UV filters, and the other group received formulations without UV filters. Both groups received a formulation containing the extract and the vehicle. The formulations were applied twice daily to the upper arms after washing with sodium lauryl sulphate. Transepidermal water loss (TEWL) and skin microrelief were evaluated before and after a 14- and 28-day period of treatment. The control regions and regions where the vehicles were applied showed an increase in the TEWL. For the formulations containing the extract, decreased TEWL and improved microrelief were observed when compared to the vehicle and control areas after a 28-day period. In conclusion, Cichorium intybus root extract showed protective and restructuring effects on the skin and stands out as an innovative ingredient to improve skin barrier function.

  20. The use of green tea extract in cosmetic formulations: not only an antioxidant active ingredient.

    Science.gov (United States)

    Gianeti, Mirela D; Mercurio, Daiane G; Campos, Patricia M B G Maia

    2013-01-01

    Green tea (GT) extracts contain polyphenols, known to be effective free radical scavengers, and other ingredients that could also provide benefits to the skin. This is a report on clinical studies using objective, noninvasive methods to evaluate the effects of cosmetic formulations containing GT. Experimental formulations were supplemented or not (vehicle) with 6% Camellia sinensis glycolic leaf extracts (GT). These formulations were applied to the forearm skin of 24 volunteers, and their effects were evaluated before and after 2 hours, 15 and 30 days according to the following parameters: stratum corneum water content, transepidermal water loss, skin viscoelastic-to-elastic ratio (Uv/Ue), and microrelief. The volunteers were instructed not to apply any formulation in an area of the forearm (control area). Experimental formulations (GT) increased skin moisture in the long-term study, indicating that GT has a prolonged moisturizing effect. The Uv/Ue was significantly enhanced after 30 days of topical application of the experimental formulation when compared with vehicle and control. After 15-30 days, skin microrelief was significantly improved due to a reduction in skin roughness. The results suggest that GT-containing cosmetic formulations have pronounced moisturizing effects and improve skin microrelief.

  1. Aripiprazole: the evidence of its therapeutic impact in schizophrenia

    Directory of Open Access Journals (Sweden)

    William Winlow

    2006-06-01

    Full Text Available William Winlow, Louise Profit, Paul ChrispCore Medical Publishing, Knutsford, UKIntroduction: An ideal antipsychotic would rapidly stabilize acute psychotic symptoms and maintain the patient, without relapse, for prolonged periods in the absence of extrapyramidal, endocrine, diabetic, or cardiovascular side effects, and without weight gain. The dopamine partial agonist aripiprazole is compared with this ideal and with conventional antipsychotics, such as haloperidol, and with atypical antipsychotics.Aims: To review the evidence for the clinical impact of aripiprazole in the treatment of patients with schizophrenia.Evidence review: There is clear evidence that aripiprazole is as effective as haloperidol in reducing the positive and negative symptoms of schizophrenia and schizoaffective disorder. In patients with schizophrenia, aripiprazole has been shown to stabilize acute psychotic symptoms, prevent relapse in stabilized patients, and maintain patients with schizophrenia following acute relapse. Furthermore, in common with other atypical antipsychotics, aripiprazole appears to be associated with a lower incidence of side effects than typical antipsychotics and may reduce discontinuation of drug therapy. Evidence also suggests that aripiprazole may be associated with a lower incidence of extrapyramidal symptoms than conventional antipsychotics, but further long-term studies concerning tardive dyskinesia are required. Studies on the cost effectiveness of aripiprazole, as well as the quality of life and general functioning of patients taking the drug are still required, although there is some evidence of improved quality of life. Further evidence comparing aripiprazole with other atypical antipsychotics would be welcome.Clinical value: In conclusion, aripiprazole is an atypical antipsychotic suitable for first-line use in patients with schizophrenia. Its clinical value in relation to other atypical antipsychotics remains to be elucidated.Key words

  2. Evaluation of Essential Oil and its Three Main Active Ingredients of Chinese Chenopodium Ambrosioides (Family: Chenopodiaceae Against Blattella Germanica

    Directory of Open Access Journals (Sweden)

    Wei Xiang Zhu

    2012-12-01

    Full Text Available Background: The efficacy of essential oil of Chenopodium ambrosioides flowering aerial parts and its three mainactive ingredients was evaluated against Blattella germanica male adults.Methods: Composition of essential oil was determined by GC-MS. Topical application bioassay was used to evaluatecontact toxicity of essential oil and three main components. Fumigant toxicity of essential oil and its main components was measured using a sealed space method.Results: Twenty-two components were identified in the essential oil and the main components were (Z-ascaridole(29.7%, isoascaridole (13.0%, ρ-cymene (12.7% and piperitone (5.0%. The essential oil and (Z-ascaridole,isoascaridole and -cymene possessed fumigant toxicity against male German cockroaches with LC50 values of 4.13,0.55, 2.07 and 6.92 mg/L air, respectively. Topical application bioassay showed that all the three compounds weretoxic to male German cockroaches and (Z-ascaridole was the strongest with a LD50 value of 22.02 g/adult while the crude oil with a LD50 value of 67.46 g/adult.Conclusion: The essential oil from Chinese C. ambrosioides and its three main active ingredients may be explored as natural potential insecticides in the control of cockroaches.

  3. [Study on characteristic spectrum of ingredients from different species Cordyceps and its anti-fibrotic activity on human embryonic fibroblasts].

    Science.gov (United States)

    Si, Nan; Peng, Bo; Zhao, Hai-Yu; Wang, Hong-Jie; Yang, Jian; Li, Jian-Rong; Sun, Wei; Bian, Bao-Lin

    2016-07-01

    In this study, 10 samples of parasites, cursive, and the whole from six different species of Cordyceps were determined and compared by HPLC and LC-MS methods. Uridine, adenosine, and cordycepin were selected as the main evaluation index. The anti-fibrotic activity of different species Cordyceps extracts was observed using in vitro TGF-β1-induced ECM accumulation in human embryonic fibroblasts CCC-ESF-1. The results demonstrated that the number of atoms and hyphae ingredients of different species showed little difference, however, the content distribution of each component has obvious significance. The in vitro anti-fibrotic activities of different species were as follow: Cordyceps flower > Cicada Cordyceps (Cicada flower)> Silkworm Cordyceps> Tussah Cordyceps>natural Cordyceps. Our preliminary data could serve as reference for the discovery of artificial alternatives of natural Cordyceps. Copyright© by the Chinese Pharmaceutical Association.

  4. TARDIVE DYSKINESIA AND OTHER EXTRAPYRAMIDAL SYMPTOMS ASSOCIATED WITH ARIPIPRAZOLE: A CASE SERIES

    Directory of Open Access Journals (Sweden)

    Nayana Sanjay

    2016-06-01

    Full Text Available BACKGROUND Aripiprazole is a third generation antipsychotic introduced in 2004 for treatment of Schizophrenia and bipolar disorders. It has partial agonist activity at dopamine D2 receptor and D2 antagonist activity under hyperdopaminergic condition. In addition, it is a partial agonist at serotonin 5HT1A receptor and antagonist at 5HT2A receptor. Because its pharmacological profile differs from other atypical antipsychotics, it was initially thought to produce lesser side effects and movement disorders. But over the years, there is a growing body of evidence in the form of case reports and case series of Aripiprazole induced movement disorders like Tardive dyskinesia, Parkinsonism, akathisia and dystonia. Of late it has been advocated for irritability associated with autism and as an augmenter for depressive disorder. It has lower potential for weight gain and sedation, as it has relatively low affinity for H1 [Histamine] receptor compared to clozapine, olanzapine and quetiapine. Based on this unique mechanism, it is claimed to have minimal or non-significant motor side effects like Tardive dyskinesia. We document a case series of 8 patients who developed Tardive dyskinesia, Parkinsonism and akathisia following treatment with Aripiprazole (ARP. METHODS This is both retrospective and observational study. Patients from outpatient and inpatient department of a tertiary psychiatric teaching hospital with an ICD-10 diagnosis of psychiatric disorder, who has experienced movement disorder while on treatment with Aripiprazole are included in this report. All these patients were under the care of authors as treating Psychiatrists. Rating scales like Abnormal Involuntary Movement Scale (AIMS, Naranjo’s Causality Scale, Barnes Akathisia Rating Scale (BARS and Simpson Angus extrapyramidal Scale (SAS were used. RESULTS Total of eight patients presented with various movement disorders associated with Aripiprazole, out of which three patients with tardive

  5. Do active ingredients in non alcoholic chlorhexidine mouth wash provide added effectiveness? Observations from a randomized controlled trial.

    Science.gov (United States)

    Santhosh, K; Surbhi, L; Harish, T; Jyothi, T; Arvind, T; Prabu, D; Suhas, K

    2010-06-01

    Chlorhexidine (CHX) is the most tested and leading oral antiseptic agent. Zinc as an active ingredient has shown additive and synergistic effect and when Sodium fluoride (NaF) was used it failed to show added effectiveness and the combined effect of NaF and Zinc chloride (ZnCl2) both as active ingredients has never been evaluated. The present study assessed the effectiveness of active ingredients and to compare the frequency of adverse events occurring with traditional CHX and CHX+NaF+ZnCl2. A randomized double blind crossover trial was executed with 24 subjects participating in two consecutive experimental phases of 21 days each with CHX and CHX+NaF+ZnCl2 mouth rinses. Each individual was assessed for gingivitis, plaque, supragingival calculus and extrinsic stains at baseline and after experimental phase and adverse events experienced were recorded. There was a significant difference (p = 0.014) between the two experimental mouth rinses for their effectiveness on gingivitis. In the CHX group, the gingival score on D21 was significantly greater by 0.13 than DO while with CHX+NaF+ZnCl2 there was a decrease in gingival score by 0.09 which was insignificant. No significant difference was observed between the interventions for plaque accumulation and formation of extrinsic stains. The difference in the mean calculus score at baseline and after experimental phase was 1.47 for CHX+NaF+ZnCl2 in contrast to 1.93 among CHX group. Oral itching, oral soreness, apthous ulcers and dryness were reported by many subjects while burning sensation was reported by very few volunteers. There was no significant difference for occurrence of adverse events between the two experimental mouthrinses. CHX+NaF+ZnCl2 mouth rinse was found to be significantly more effective in the reduction of gingivitis and supragingival calculus. No significant difference was found for the occurrence of dental plaque, extrinsic stains and adverse events between the interventions.

  6. [Chemical diversity of the biological active ingredients of salvia officinalis and some closely related species].

    Science.gov (United States)

    Máthé, Imre; Hohmann, Judit; Janicsák, Gábor; Nagy, Gábor; Dora, Rédei

    2007-01-01

    Comparative studies on the volatile and non-volatile fractions of 6 species. i.e. Salvia officinalis, S. tomentosa, S. fruticosa, S. candelabrum, S. ringens, S. lavandulifolia of the Section Salvia (Lamiaceae) have been carried out. Both fractions provide the chemical pattern matches to the chemotaxonomic character of Subfamily Nepetoideae in Erdtmanr two subfamiliar system. S. lavandulifolia had the highest essential oil content, followed by S. fruticosa, S. tomentosa, S. officinalis and S. candelabrum. S. ringens contains volatile oil only in traces. The neurotoxin thujone content was the highest in the S. officinalis oils and in that of S. fruticosa. No thujone was detected in S. lavandulifolia. The other species, e.g.: S. tomentosa contain this compound only in moderate concentrations (less than 10%). Among the non-volatile fractions of the plant ingredients the triterpene ursolic and oleanolic acids had the highest concentration in the leaves. Despite some rare cases, ursolic acid dominates the tritepene fraction. Rosmarinic and caffeic acids were measured in similar concentrations, in all species. As the case of S. officinalis shows, these compounds vary significantly in all organs during the vegetation period. Caffeic acid is also ubiquitous in the genus Salvia but as our data suggest it occurs in an order of magnitude lower concentration than rosmarinic acid. The isolation of phenylethanolid martynoside, though obtained in a rather small concentration, is of great chemotaxonomic significance, as this is the first phenylethanolid type glycoside isolated not only from the Salvia genus but also from the entire Subfamily Nepetoideae. As pheylethanolids are rather common and accumulate in significant concentrations in plants of the Subfamily Lamioideae, our opinion that the chemical differences between the two subfamilies are less qualititative than quantitative, is confirmed. This holds true of other chemical markers like monoterpenes, ursolic and oleanolic

  7. Optimization of HS-GC-FID-MS Method for Residual Solvent Profiling in Active Pharmaceutical Ingredients Using DoE.

    Science.gov (United States)

    Poceva Panovska, Ana; Acevska, Jelena; Stefkov, Gjoshe; Brezovska, Katerina; Petkovska, Rumenka; Dimitrovska, Aneta

    2016-02-01

    Within this research, a headspace (HS) gas chromatography-flame ionization detector-mass spectrometry method was developed for profiling of residual solvents (RSs) in active pharmaceutical ingredients (APIs). Design of experiment was used for optimization of sample preparation, as well as for robustness testing of the method. HS equilibration temperature and dilution medium were detected as parameters with greater impact on the sensitivity, compared with the time used for equilibration of the samples. Regardless of the sample solubility, the use of water for sample preparation was found to be crucial for better sensitivity. The use of a well-designed strategy for method development and robustness testing, additional level of identification confidence, as well as use of internal standard provided a strong and reliable analytical tool for API fingerprinting, thus enabling the authentication of the substance based on the RS profile.

  8. Quantification of potential impurities by a stability indicating UV-HPLC method in niacinamide active pharmaceutical ingredient.

    Science.gov (United States)

    Thomas, Saji; Bharti, Amber; Tharpa, Kalsang; Agarwal, Ashutosh

    2012-02-23

    A sensitive, stability indicating reverse phase UV-HPLC method has been developed for the quantitative determination of potential impurities of niacinamide active pharmaceutical ingredient. Efficient chromatographic separation was achieved on C18 stationary phase in isocratic mode using simple mobile phase. Forced degradation study confirmed that the newly developed method was specific and selective to the degradation products. Major degradation of the drug substance was found to occur under oxidative stress conditions to form niacinamide N-oxide. The method was validated according to ICH guidelines with respect to specificity, precision, linearity and accuracy. Regression analysis showed correlation coefficient value greater than 0.999 for niacinamide and its six impurities. Detection limit of impurities was in the range of 0.003-0.005% indicating the high sensitivity of the newly developed method. Accuracy of the method was established based on the recovery obtained between 93.3% and 113.3% for all impurities.

  9. Direct detection and identification of active pharmaceutical ingredients in intact tablets by helium plasma ionization (HePI mass spectrometry

    Directory of Open Access Journals (Sweden)

    Athula B. Attygalle

    2014-06-01

    Full Text Available A simple modification converts an electrospray ion source to an ambient-pressure helium plasma ionization source without the need of additional expensive hardware. Peaks for active ingredients were observed in the spectra recorded from intact pharmaceutical tablets placed in this source. A flow of heated nitrogen was used to thermally desorb analytes to gas phase. The desorption temperatures were sometimes as low as 50 °C. For example, negative-ion spectra recorded from an aspirin tablet showed peaks at m/z 137 (salicylate anion and 179 (acetylsalicylate anion which were absent in the background spectra. The overall ion intensity increased as the desorption gas temperature was elevated. Within the same acquisition experiment, both positive- and negative-ion signals for acetaminophen were recorded from volatiles emanating from Tylenol tablets by switching the polarity of the capillary back and forth. Moreover, different preparations of acetaminophen tablets could be distinguished by their ion-intensity thermograms.

  10. Direct detection and identification of active pharmaceutical ingredients in intact tablets by helium plasma ionization (HePI) mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    Athula B. Attygalle; Freneil B. Jariwala; Julius Pavlov; Zhihua Yang; Jason A. Mahr; Mabel Oviedo

    2014-01-01

    A simple modification converts an electrospray ion source to an ambient-pressure helium plasma ionization source without the need of additional expensive hardware. Peaks for active ingredients were observed in the spectra recorded from intact pharmaceutical tablets placed in this source. A flow of heated nitrogen was used to thermally desorb analytes to gas phase. The desorption temperatures were sometimes as low as 50 1C. For example, negative-ion spectra recorded from an aspirin tablet showed peaks at m/z 137 (salicylate anion) and 179 (acetylsalicylate anion) which were absent in the background spectra. The overall ion intensity increased as the desorption gas temperature was elevated. Within the same acquisition experiment, both positive- and negative-ion signals for acetaminophen were recorded from volatiles emanating from Tylenol tablets by switching the polarity of the capillary back and forth. Moreover, different preparations of acetaminophen tablets could be distinguished by their ion-intensity thermograms.

  11. Behandling af Tourettes syndrom med aripiprazol

    DEFF Research Database (Denmark)

    Stenstrøm, Anne Dorte; Sindø, Ingrid

    2008-01-01

    Tourette's syndrome (TS) is a motoric disorder characterised by multiple motor and vocal tics. The treatment for patients with moderate to severe TS includes antipsychotic medication. A case report is described in which a 20 year-old male had taken antipsychotic medication since the age of five......, due to TS. The initial treatment consisted of pimozide and risperidone, both of which had an unsatisfactorily efficacy on tics and side effects in the form of weight gain and sedation. The patient is now treated with aripiprazole and there is a marked reduction of tics and no side effects...

  12. [Effect of exogenous sucrose on growth and active ingredient content of licorice seedlings under salt stress conditions].

    Science.gov (United States)

    Liu, Fu-zhi; Yang, Jun

    2015-11-01

    Licorice seedlings were taken as experimental materials, an experiment was conducted to study the effects of exogenous sucrose on growth and active ingredient content of licorice seedlings under NaCl stress conditions. The results of this study showed that under salt stress conditions, after adding a certain concentration of exogenous sucrose, the licorice seedlings day of relative growth rate was increasing, and this stress can be a significant weakening effect, indicating that exogenous sucrose salt stress-relieving effect. The total flavonoids and phenylalanine ammonia lyase (PAL) activity were significantly increased, the exogenous sucrose can mitigated the seedling roots under salt stress, the licorice flavonoid content in the enhanced growth was largely due to the activity of PAL an increased, when the concentration of exogenous sucrose wae 10 mmol x L(-1), PAL activity reaching a maximum, when the concentration of exogenous sucrose was 15 mmol x L(-1), PAL activity turned into a downward trend, the results indicating that this mitigation has concentration effect. After applying different concentrations of exogenous sugar, the contents of liquiritin changes with the change of flavonoids content was similar. After applying different concentrations of exogenous sucrose, the content of licorice acid under salt stress was higher than the levels were not reached during salt stress, the impact of exogenous sucrose concentration gradient of licorice acid accumulation was not obvious.

  13. Two cases of hypersexuality probably associated with aripiprazole.

    Science.gov (United States)

    Cheon, Eunjin; Koo, Bon-Hoon; Seo, Sang Soo; Lee, Jun-Yeob

    2013-06-01

    Sexual dysfunction is a common side effect in patients treated with antipsychotics but significant differences exist across different compounds. We report hypersexuality symptoms in two female patients with schizophrenia who were receiving treatment with aripiprazole. The patients experienced more frequent sexual desire and greater sexual preoccupation after taking aripiprazole. We discuss the potential neuro-chemical mechanisms for this and argue that aripiprazole's unique pharmacological profile, partial agonism with high affinity at dopamine D2-receptor, may have contributed to the development of these symptoms.

  14. The prescribing pattern of a new antipsychotic: A descriptive study of aripiprazole for psychiatric in-patients

    DEFF Research Database (Denmark)

    Johansson, M.; Manniche, C.; Andersen, Stig Ejdrup

    2008-01-01

    -naive. In 25% aripiprazole, monotherapy was commenced whereas aripiprazole-antipsychotic combinations were initially prescribed in 75%. Overall, 85% of the patients received periods of antipsychotic polypharmacy and aripiprazole was combined with 17 different antipsychotics. Each patient received median three...... (range 0-8) psychoactive drugs parallel with aripiprazole. This study demonstrates reality in psychopharmacology and quote aripiprazole as example. In day-to-day practice, aripiprazole is used as part of highly individualized regimens comprising polypharmacy and excessive dosing. Although theoretically...

  15. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient

    Directory of Open Access Journals (Sweden)

    Hao Sun

    2016-08-01

    Full Text Available AbstractRhein is a major medicinal ingredient isolated from several traditional Chinese medicines, including Rheum palmatum L., Aloe barbadensis Miller, Cassia angustifolia Vahl., and Polygonum multiflorum Thunb. Rhein has various pharmacological activities, such as anti-inflammatory, antitumor, antioxidant, antifibrosis, hepatoprotective, and nephroprotective activities. Although more than 100 articles in PubMed are involved in the pharmacological mechanism of action of rhein, only a few focus on the relationship of crosstalk among multiple pharmacological mechanisms. The mechanism of rhein involves multiple pathways which contain close interactions. From the overall perspective, the pathways which are related to the targets of rhein, are initiated by the membrane receptor. Then, MAPK and PI3K-AKT parallel signaling pathways are activated, and several downstream pathways are affected, thereby eventually regulating cell cycle and apoptosis. The therapeutic effect of rhein, as a multitarget molecule, is the synergistic and comprehensive result of the involvement of multiple pathways rather than the blocking or activation of a single signaling pathway. We review the pharmacological mechanisms of action of rhein by consulting literature published in the last 100 years in PubMed. We then summarize these pharmacological mechanisms from a comprehensive, interactive, and crosstalk perspective. In general, the molecular mechanism of action of drug must be understood from a systematic and holistic perspective, which can provide a theoretical basis for precise treatment and rational drug use.

  16. Bactericidal active ingredient in cryopreserved plasma-treated water with the reduced-pH method for plasma disinfection

    Science.gov (United States)

    Kitano, Katsuhisa; Ikawa, Satoshi; Nakashima, Yoichi; Tani, Atsushi; Yokoyama, Takashi; Ohshima, Tomoko

    2016-09-01

    For the plasma disinfection of human body, plasma sterilization in liquid is crucial. We found that the plasma-treated water (PTW) has strong bactericidal activity under low pH condition. Physicochemical properties of PTW is discussed based on chemical kinetics. Lower temperature brings longer half-life and the bactericidal activity of PTW can be kept by cryopreservation. High performance PTW, corresponding to the disinfection power of 22 log reduction (B. subtilis spore), can be obtained by special plasma system equipped with cooling device. This is equivalent to 65% H2O2, 14% sodium hypochlorite and 0.33% peracetic acid, which are deadly poison for human. But, it is deactivated soon at higher temperature (4 sec. at body temperature), and toxicity to human body seems low. For dental application, PTW was effective on infected models of human extracted tooth. Although PTW has many chemical components, respective chemical components in PTW were isolated by ion chromatography. In addition to peaks of H2O2, NO2- and NO3-, a specific peak was detected. and only this fraction had bactericidal activity. Purified active ingredient of PTW is the precursor of HOO, and further details will be discussed in the presentation. MEXT (15H03583, 23340176, 25108505). NCCE (23-A-15).

  17. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient.

    Science.gov (United States)

    Sun, Hao; Luo, Guangwen; Chen, Dahui; Xiang, Zheng

    2016-01-01

    Rhein is a major medicinal ingredient isolated from several traditional Chinese medicines, including Rheum palmatum L., Aloe barbadensis Miller, Cassia angustifolia Vahl., and Polygonum multiflorum Thunb. Rhein has various pharmacological activities, such as anti-inflammatory, antitumor, antioxidant, antifibrosis, hepatoprotective, and nephroprotective activities. Although more than 100 articles in PubMed are involved in the pharmacological mechanism of action of rhein, only a few focus on the relationship of crosstalk among multiple pharmacological mechanisms. The mechanism of rhein involves multiple pathways which contain close interactions. From the overall perspective, the pathways which are related to the targets of rhein, are initiated by the membrane receptor. Then, MAPK and PI3K-AKT parallel signaling pathways are activated, and several downstream pathways are affected, thereby eventually regulating cell cycle and apoptosis. The therapeutic effect of rhein, as a multitarget molecule, is the synergistic and comprehensive result of the involvement of multiple pathways rather than the blocking or activation of a single signaling pathway. We review the pharmacological mechanisms of action of rhein by consulting literature published in the last 100 years in PubMed. We then summarize these pharmacological mechanisms from a comprehensive, interactive, and crosstalk perspective. In general, the molecular mechanism of action of drug must be understood from a systematic and holistic perspective, which can provide a theoretical basis for precise treatment and rational drug use.

  18. Lack of sustained efficacy for alcohol-based surgical hand rubs containing 'residual active ingredients' according to EN 12791.

    Science.gov (United States)

    Kampf, G; Kramer, A; Suchomel, M

    2017-02-01

    The World Health Organization recommends the use of hand rubs with 'sustained activity' for surgical hand preparation. This review aims to verify whether any of the alcohol-based hand rubs containing non-volatile 'active ingredients' such as chlorhexidine digluconate (CHG), mecetronium ethylsulphate (MES), or ortho-phenylphenol (OPP) provides such sustained efficacy for surgical hand disinfection. Literature was searched to find studies according to EN 12791. Published data sets were analysed to verify whether any of the formulations has a superior efficacy (Phand rub with 0.1% OPP in 78.2% ethanol was also not superior to the reference treatment when applied as recommended for 1.5min. It appears reasonable and responsible to limit the dermal exposure and environmental input to biocidal agents with a clear benefit such as the alcohols. In analogy to avoiding dyes and fragrances in hand rubs, formulations containing 'active' substances without a clear benefit but with potential risks should be avoided when alternative formulations with the same level of antimicrobial activity, dermal tolerance, and user acceptability are available.

  19. Studies on free-radical scavenging activity and identification of active ingredients of different plant crude extracts of Mentha piperita collected from Sur, Sultanate of Oman

    Institute of Scientific and Technical Information of China (English)

    Mohammad Amzad Hossain; Aqeela Said Hamed AL Orimi; Afaf Mohammed Weli; Qasim Al-Riyami; Jamal Nasser Al-Sabahi

    2014-01-01

    Objective: To determine free radical scavenging activity and active chemical ingredients of different plant crude extracts of Mentha piperita (M. piperita). Methods: The dried powder leaves of M. piperita were extracted with polar organic solvent by Soxhlet extractor. The crude extract and its fractions of hexane, chloroform, ethyl acetate and butanol crude extracts were prepared. The antioxidant activity of different crude extracts from M. piperita was carried out by DPPH method with minor modification, and the active chemical ingredients of different plant crude extracts of M. piperita were analyzed by gas chromatography-mass spectrometry (GC-MS). Results: Qualitative analysis of different polarities crude extracts by GC-MS found different types of active organic compounds. The antioxidant activity of different crude extracts were found to be in the order of chloroform extract> butanol extract> ethyl acetate extract> hexane extract>methanol extract. Majority identified compounds in the plant crude extracts by GC-MS were biologically active. Conclusions: Therefore, the isolation, purification, identification and characterization of bioactive compounds from various crude extracts of M. piperita might have ecological significance.

  20. Treatment of refractory catatonic schizophrenia with low dose aripiprazole

    Directory of Open Access Journals (Sweden)

    Sasaki Tsuyoshi

    2012-05-01

    Full Text Available Abstract This case is of 54-year-old female with catatonic schizophrenia, characterized by treatment resistance to the pharmacotherapy with olanzapine, risperidone, flunitrazepam, and ECT. Olanzapine and risperidone and flunitrazepam did not improve her catatonic and psychotic symptoms, and induced the extrapyramidal symptoms. The effects of ECT did not continue even for a month. However, the treatment with low-dose aripiprazole dramatically improved the patient’s psychotic symptoms and extrapyramidal symptoms. The mechanisms underlying the effects of low-dose aripiprazole in this case remain unclear, but unlike other antipsychotics, aripiprazole is a dopamine D2 partial agonist. In this regard, our results suggest that aripiprazole has numerous advantages, especially in cases of stuporous catatonia and a defective general status.

  1. Active ingredients fatty acids as antibacterial agent from the brown algae Padina pavonica and Hormophysa triquetra

    Institute of Scientific and Technical Information of China (English)

    Gihan Ahmed El Shoubaky; Essam Abd El Rahman Salem

    2014-01-01

    Objective: To estimate the fatty acids content in the brown algae Padina pavonica (P. pavonica) and Hormophysa triquetra (H. triquetra) and evaluate their potential antimicrobial activity as bioactive compounds.Methods:The fatty acid compositions of the examined species were analyzed using gas chromatography-mass spectrometry. The antimicrobial activity of crude and fatty acids was assessed using the agar plug technique.Results:The fatty acids profile ranged from C8:0 to C20:4. Concentration of saturated fatty acids in P. pavonica was in the order palmitic>myristic>stearic whereas concentration of the unsaturated fatty acids was oleic acid>palmitoleic>9-cis-hexadecenoic>linoleic acid>α-linolenic>arachidonic> elaidic acid. H. triquetra contained high concentration of saturated fatty acids than those of P. pavonica which was in the order as follows: palmitic>margaric>myristic>nonadecyclic>stearic>caprylic>tridecylic>pentadecylic>lauric while the unsaturated fatty acids consisted of oleic>nonadecenoic>non adecadienoate>margaroleic. The crude and fatty acid extracts of H. triquetra and P. pavonica were biologically active on the tested pathogens. H.triquetra exhibited a larger inhibitory zone than P. pavonica. Conclusions: The brown algae P. pavonica and H. triquetra have high efficient amount of fatty acids and showed strong antibacterial activity, especially H. triquetra.

  2. DESIGN OF FILL AND FINISH FACILITY FOR ACTIVE PHARMACEUTICAL INGREDIENTS (API

    Directory of Open Access Journals (Sweden)

    NUUR LAILA KHAIRUDDIN

    2016-08-01

    Full Text Available Fill and finish operations continue to be one of the most heavily outsourced activities in the biopharmaceutical manufacturing market today. There are a few aspects that need to be consider in outsource activities like logistic, storage condition, facility certification and audit as regulations and standards which the manufacturer should adhere. Risk would be greater and extra care should be taken when outsource from foreign fill and finish facility. Thus, the internal aseptic fill and finish facility with audit checklist will help to minimize the risk during logistic and storage and also minimize the cost for outsource fill and finish facility. The data collections are through survey and conceptual design with simulation as the execution part.

  3. Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review.

    OpenAIRE

    Bharate, Sonali S.; Bharate, Sandip B.; Bajaj, Amrita N

    2016-01-01

    Studies of active drug/excipient compatibility represent an important phase in the preformulation stage of the development of all dosage forms. The potential physical and chemical interactions between drugs and excipients can affect the chemical nature, the stability and bioavailability of drugs and, consequently, their therapeutic efficacy and safety. The present review covers the literature reports of interaction and incompatibilities of commonly used pharmaceutical excipients with differen...

  4. The possibilities of using essential oils as an active ingredients or preservatives in cosmetic products

    OpenAIRE

    2011-01-01

    An important trend in the development of the cosmetics industry is searching for new biologically active, natural compounds and preservative systems, which will find application in the natural cosmetics production. Natural cosmetics are of considerable interest nowadays and essential oils could be employed in theirs production. The huge potential of essential oils indicates the possibility of applying them in practice because of theirs antibacterial, antiseptic, antifungal, and antioxidant...

  5. Treatment of antipsychotic-induced hyperprolactinemia: an update on the role of the dopaminergic receptors D2 partial agonist aripiprazole.

    Science.gov (United States)

    De Berardis, Domenico; Fornaro, Michele; Serroni, Nicola; Marini, Stefano; Piersanti, Monica; Cavuto, Marilde; Valchera, Alessandro; Mazza, Monica; Girinelli, Gabriella; Iasevoli, Felice; Perna, Giampaolo; Martinotti, Giovanni; Di Giannantonio, Massimo

    2014-01-01

    Hyperprolactinemia is an unwanted adverse effect present in several typical and atypical antipsychotics. Aripiprazole is a drug with partial agonist activity at the level of dopamine receptors D2, which may be effective for antipsychotic- induced hyperprolactinemia. Therefore, we analyzed the literature concerning the treatment of antipsychoticinduced hyperprolactinemia with aripiprazole by updating a previous paper written on the same topic. More recent studies were reviewed. They showed that there are two options for the treatment of antipsychotic-induced hyperprolactinemia with aripiprazole. The safest strategy may require the addition of aripiprazole to ongoing treatments, in the case patients had previously responded to antipsychotic drugs and then developed hyperprolactinemia. However, it is advisable to monitor the patients in case relapses and/or side effect, although rare, might occur. Switching drugs should be considered when a patient does not appear to be responding to the previous antipsychotic, thus developing hyperprolactinemia. A cross-taper switch should always be considered, but the risk of a relapse in the disorder may occur more frequently and the patients should be closely monitored. However, limitations must be considered and further studies are needed to definitely elucidate this important issue. Some relevant patents are also described in this review.

  6. Identification of a novel component leading to anti-tumor activity besides the major ingredient cordycepin in Cordyceps militaris extract.

    Science.gov (United States)

    Wada, Takeharu; Sumardika, I Wayan; Saito, Shingo; Ruma, I Made Winarsa; Kondo, Eisaku; Shibukawa, Masami; Sakaguchi, Masakiyo

    2017-09-01

    In accordance with our previous study that was carried out to identify novel anti-tumor ingredients, chromatographic separation in combination with an anti-tumor activity assay was used for analysis of Cordyceps militaris extract in this study. Various modes of chromatography including reversed-phase, cation-exchange and anion-exchange were used to separate components of Cordyceps militaris, which showed various chemical properties. Anti-tumor activity of each fraction was assessed by a Hoechst staining-based apoptosis assay using malignant melanoma MeWo cells. By these repeated approaches through chromatographic segregation and cell biological assay, we finally succeeded in identifying the target substance from a certain fraction that included neutral hydrophilic components using a pre-column and post-column chlorine adduct ionization LC-APCI-MS method. The target substance was a mono-carbohydrate, xylitol, that induced apoptotic cell death in MeWo cells but not in normal human OUMS-24 fibroblasts. This is the first study showing that Cordyceps militaris extract contains a large amount of xylitol. Thus, our results will contribute greatly to uncovering the mysterious multifunctional herbal drug Cordyceps militaris as an anti-tumor agent. Copyright © 2017 Elsevier B.V. All rights reserved.

  7. The hallucinogenic herb Salvia divinorum and its active ingredient salvinorin A reduce inflammation-induced hypermotility in mice.

    Science.gov (United States)

    Capasso, R; Borrelli, F; Zjawiony, J; Kutrzeba, L; Aviello, G; Sarnelli, G; Capasso, F; Izzo, A A

    2008-02-01

    The hallucinogenic plant Salvia divinorum has been used for medical treatments of gastrointestinal disorders. Here, we evaluated the effect of a standardized extract from the leaves of Salvia divinorum (SDE) and of its active ingredient salvinorin A on motility in vivo, both in physiological states and during croton oil-induced intestinal inflammation. SDE (1-100 mg kg(-1)) significantly inhibited motility only in inflamed, but not in control, mice. In control mice, salvinorin A (0.01-10 mg kg(-1)) significantly inhibited motility only at the highest doses tested (3 and 10 mg kg(-1)) and this effect was not counteracted by naloxone or by the kappa-opioid receptor (KOR) antagonist nor-binaltorphimine. Inflammation significantly increased the potency of salvinorin A (but not of the KOR agonist U-50488) in reducing motility. The inhibitory effects of both salvinorin A and U-50488 in inflamed mice were counteracted by naloxone or by nor-binaltorphimine. We conclude that salvinorin A may reduce motility through activation of different targets. In physiological states, salvinorin A, at high doses, inhibited motility through a non-KOR mediated mechanism. Gut inflammation increased the potency of salvinorin A; this effect was mediated by KOR, but it was not shared by U-50488, thus suggesting that salvinorin A may have target(s) other than KOR in the inflamed gut.

  8. Intrinsic Motivation and Engagement as "Active Ingredients" in Garden-Based Education: Examining Models and Measures Derived from Self-Determination Theory

    Science.gov (United States)

    Skinner, Ellen A.; Chi, Una

    2012-01-01

    Building on self-determination theory, this study presents a model of intrinsic motivation and engagement as "active ingredients" in garden-based education. The model was used to create reliable and valid measures of key constructs, and to guide the empirical exploration of motivational processes in garden-based learning. Teacher- and…

  9. Understanding the Active Ingredients in an Effective Preschool Vocabulary Intervention: An Exploratory Study of Teacher and Child Talk during Book Reading

    Science.gov (United States)

    Wasik, Barbara A.; Hindman, Annemarie H.

    2014-01-01

    Research Findings: In order to identify the active ingredients in an effective professional development intervention focused on enhancing preschool vocabulary instruction, this study examines the frequency with which teachers and children discussed theme-related vocabulary words during shared book reading. Head Start teachers received 1 year of…

  10. 21 CFR 310.534 - Drug products containing active ingredients offered over-the-counter (OTC) for human use as oral...

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Drug products containing active ingredients offered over-the-counter (OTC) for human use as oral wound healing agents. 310.534 Section 310.534 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR...

  11. Evaluating the migration of ingredients from active packaging and development of dedicated methods: A study of two iron-based oxygen absorbers

    NARCIS (Netherlands)

    López-Cervantes, L.; Sánchez-Machado, D.I.; Pastorelli, S.; Rijk, R.; Paseiro-Losada, P.

    2003-01-01

    The behaviour of two commercial oxygen-scavenging products with respect to migration of active ingredients into foodstuffs was investigated. Migrants were identified, and by using appropriate analytical methods, migration was determined in a variety of liquid, solid or gelled food simulants and food

  12. Identification of Major Active Ingredients Responsible for Burn Wound Healing of Centella asiatica Herbs

    Directory of Open Access Journals (Sweden)

    Fang Wu

    2012-01-01

    Full Text Available Centella asiatica herbs have been prescribed as a traditional medicine for wound healing in China and Southeast Asia for a long time. They contain many kinds of triterpenoid compounds, mainly including glycosides (asiaticoside and madecassoside and corresponding aglycones (asiatic acid and madecassic acid. To identify which is the major active constituent, a comprehensive and comparative study of these compounds was performed. In vitro, primary human skin fibroblasts, originating from healthy human foreskin samples, were treated with various concentrations of asiaticoside, madecassoside, asiatic acid, and madecassic acid, respectively. Cell proliferation, collagen synthesis, MMP-1/TIMP-1 balance, and TGF-β/Smad signaling pathway were investigated. In vivo, mice were orally administered with the four compounds mentioned above for two weeks after burn injury. The speed and quality of wound healing, as well as TGF-β1 levels in skin tissues, were examined. Interestingly, in contrast to prevalent postulations, asiaticoside and madecassoside themselves, rather than their corresponding metabolites asiatic acid and madecassic acid, are recognized as the main active constituents of C. asiatica herbs responsible for burn wound healing. Furthermore, madecassoside is more effective than asiaticoside (P=0.0446 for procollagen type III synthesis in vitro, P=0.0057 for wound healing speed, and P=0.0491 for wound healing pattern in vivo, correspondingly.

  13. Determination of antioxidant activity in herbal ingredients for foods using new methods of chemical analysis

    Directory of Open Access Journals (Sweden)

    Katalina Muñoz

    2012-06-01

    Full Text Available A new procedure has been used to separate and quantify the free radical-scavenging activity of individual compounds 18 samples of Thymus vulgaris and 12 samples of Rosmarinus officinalis (both used as natural food preservatives, based on the combination of HPTLC (High Performance Thin Layer Chromatography and postchromatographic DPPH● radical derivatization. The compounds thymol and rosmarinic acid in T. vulgaris and R. officinalis, respectively, were identified by comparisons of their Rf values and UV spectra to standards analyzed under identical analytical conditions, while the quantitative data were calculated from their calibration curves. We found that not only that the biomass yield but also the metabolite content in herbs, depend on the ecotype (genetics and on the agro ecological conditions. The effect of the ambient on the metabolite content is extremely significant and also on their antioxidant activity (One-way ANOVA with Newman-Keuls Multiple Comparison post test was performed using GraphPad Prism version 4.00 for Windows, GraphPad Software. This work pretends to demonstrate the great importance of using new technologies for the selection of the best materials used as natural food preservatives.

  14. Piperine, an active ingredient of black pepper attenuates acetaminophen-induced hepatotoxicity in mice

    Institute of Scientific and Technical Information of China (English)

    Evan Prince Sabina; Annie Deborah Harris Souriyan; Deborah Jackline; Mahaboob Khan Rasool

    2010-01-01

    Objective: To explore the hepatoprotective and antioxidant effects of piperine against acetaminophen-induced hepatotoxicity in mice. Methods: In mice, hepatotoxicity was induced by a single dose of acetaminophen (900 mg/kg b.w. i.p.). Piperine (25 mg/kg b.w. i.p.) and standard drug silymarin (25 mg/kg b.w. i.p.) were given to mice, 30 min after the single injection of acetaminophen. After 4 h, the mice were decapitated. Activities of liver marker enzymes [(aspartate transaminase (AST), alanine transaminase (ALT), and alkaline phosphatase (ALP)] and inflammatory mediator tumour necrosis factor-alpha (TNF-α) were estimated in serum, while lipid peroxidation and antioxidant status (superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, glutathione-s-transferase and glutathione) were determined in liver homogenate of control and experimental mice. Results: Acetaminophen induction (900 mg/kg b.w. i.p.) significantly increased the levels of liver marker enzymes, TNF-α, and lipid peroxidation, and caused the depletion of antioxidant status. Piperine and silymarin treatment to acetaminophen challenged mice resulted in decreased liver marker enzymes activity, TNF-α and lipid peroxidation levels with increase in antioxidant status. Conclusions: The results clearly demonstrate that piperine shows promising hepatoprotective effect as comparable to standard drug silymarin.

  15. Ginkgo biloba extracts: a review of the pharmacokinetics of the active ingredients.

    Science.gov (United States)

    Ude, Christian; Schubert-Zsilavecz, Manfred; Wurglics, Mario

    2013-09-01

    Ginkgo biloba is among the most favourite and best explored herbal drugs. Standardized extracts of Ginkgo biloba represent the only herbal alternative to synthetic antidementia drugs in the therapy of cognitive decline and Alzheimer's diseases. The clinical efficiency of such standardized Ginkgo biloba extracts (GBE) is still controversial, but authors of numerous international clinical studies recommended the use of GBE in the described therapies.Extracts of Ginkgo biloba are a mixture of substances with a wide variety of physical and chemical properties and activities. Numerous pharmacological investigations lead to the conclusion that the terpene trilactones (TTL) and the flavonoids of GBE are responsible for the main pharmacological effects of the extract in the therapy of cognitive decline. Therefore, the quality of GBE products must be oriented on a defined quantity of TTL and flavonoids. Furthermore, because of their toxic potential the amount of ginkgolic acid should be less than 5 ppm.However, data on pharmacokinetics and bioavailability, especially related to the central nervous system (CNS), which is the target tissue, are relatively rare. A few investigations characterize the TTL and flavonoids of Ginkgo biloba pharmacokinetically in plasma and in the brain. Recent investigations show that significant levels of TTL and Ginkgo biloba flavonoids cross the blood-brain barrier and enter the CNS of rats after oral application of GBE. Knowledge about the pharmacokinetic behaviour of these substances is necessary to discuss the pharmacological results on a more realistic basis.

  16. [Studies on active ingredients in Corydalis, broken cell wall corydalis and its processed products].

    Science.gov (United States)

    Cao, Liu; Diu, Zhi-Ying; Wang, Ping; Sun, Wei; Tian, Yong-Liang

    2008-06-01

    To compare the contents of tetrahydropalmatine and dehydrocorydaline in corydalis, broken cell wall corydalis and its different processed products. The broken cell wall technique was used to corydalis, and then both the corydalis and broken cell wall corydalis were processed. The method of chromatography which was used to determine the contents of tetrahydropalmatine and dehydrocorydaline in corydalis broken cell wall corydalis and its different processed products was performed by RP-HPLC with Kromasil ODS-C18 (4.6 mm x 250 mm, 5 microm) column was used at 35 degrees C, acetonitrile-acetate buffer solution (pH 6.0) (30:70) as mobile phase of 1 mL x min(-1) flow rate, detection wavelength was set at 280 nm. The contents of the two active components in broken cell wall corydalis were higher than that in corydalis, while that in broken cell wall and vinegar-fried corydalis was highest in the products of breaked cell wall corydalis. Breaking the cell wall of corydalis can help to dissolute alkaloids.

  17. Use of active ingredient information for low socioeconomic status parents' decision-making regarding cough and cold medications: role of health literacy.

    Science.gov (United States)

    Yin, H Shonna; Mendelsohn, Alan L; Nagin, Perry; van Schaick, Linda; Cerra, Maria E; Dreyer, Benard P

    2013-01-01

    Parent administration of multiple medications with overlapping active ingredients places children at risk for overdose. We sought to examine how parents use active ingredient information as part of the process of selecting a cough/cold medication for their child and how health literacy plays a role. Experimental study of parents of children presenting for care in an urban public hospital pediatric clinic. Parents were asked to determine which of 3 cough/cold medications could be given to relieve a child's cold symptoms, as part of a scenario in which they had already given a dose of acetaminophen; only 1 did not contain acetaminophen. Primary dependent variable: correct selection of cough/cold medication by using active ingredient as the rationale for choice. Primary independent variable: parent health literacy (Newest Vital Sign test). Of 297 parents, 79.2% had low health literacy (Newest Vital Sign score 0-3); 35.4% correctly chose the cough/cold medication that did not contain acetaminophen. The proportion of those who made the correct choice was no different than expected from chance alone (Goodness of fit test; χ(2) = 2.1, P = .3). Only 7.7% chose the correct medication and used active ingredient as the rationale. Those with adequate literacy skills were more likely to have selected the correct medication and rationale (25.8% vs 3.0% (P = .001); adjusted odds ratio 11.1 (95% confidence interval 3.6-33.7), after we adjusted for sociodemographics, including English proficiency and education. Many parents, especially those with low health literacy, do not use active ingredient information as part of decision-making related to administering multiple medications. Published by Elsevier Inc.

  18. Use of Active Ingredient Information for Low Socioeconomic Status Parents’ Decision-making Regarding Cough and Cold Medications: Role of Health Literacy

    Science.gov (United States)

    Yin, H. Shonna; Mendelsohn, Alan L.; Nagin, Perry; van Schaick, Linda; Cerra, Maria E.; Dreyer, Benard P.

    2013-01-01

    OBJECTIVE Parent administration of multiple medications with overlapping active ingredients places children at risk for overdose. We sought to examine how parents use active ingredient information as part of the process of selecting a cough/cold medication for their child, and how health literacy plays a role. METHODS Experimental study of parents of children presenting for care in an urban public hospital pediatric clinic. Parents were asked to determine which of 3 cough/cold medications could be given to relieve a child’s cold symptoms, as part of a scenario in which they had already given a dose of acetaminophen; only 1 did not contain acetaminophen. Primary dependent variable: correct selection of cough/cold medication, using active ingredient as the rationale for choice. Primary independent variable: parent health literacy (Newest Vital Sign (NVS)). RESULTS Of 297 parents, 79.2% had low health literacy (NVS score 0–3). 35.4% correctly chose the cough/cold medication which did not contain acetaminophen. The proportion of those who made the correct choice was no different than expected from chance alone (Goodness of fit test; χ2=2.1, p=0.3). Only 7.7% chose the correct medication and used active ingredient as the rationale. Those with adequate literacy skills were more likely to have selected the correct medication and rationale (25.8% vs. 3.0% (p=0.001); AOR=11.1 [95%CI: 3.6–33.7], adjusting for sociodemographics, including English proficiency and education). CONCLUSIONS Many parents, especially those with low health literacy, do not use active ingredient information as part of decision-making related to administering multiple medications. PMID:23680341

  19. Kinetics of the esterification of active pharmaceutical ingredients containing carboxylic acid functionality in polyethylene glycol: formulation implications.

    Science.gov (United States)

    Schou-Pedersen, Anne Marie V; Hansen, Steen Honoré; Moesgaard, Birthe; Østergaard, Jesper

    2014-08-01

    Polyethylene glycols (PEGs) are attractive as excipients in the manufacture of drug products because they are water soluble and poorly immunogenic. They are used in various pharmaceutical preparations. However, because of their terminal hydroxyl groups, PEGs can participate in esterification reactions. In this study, kinetics of two active pharmaceutical ingredients, cetirizine and indomethacin possessing carboxylic acid functionality, has been studied in PEG 400 and PEG 1000 at 50 °C, 60 °C, 70 °C, and 80 °C. HPLC-UV was applied for the determination of concentrations in the kinetic studies, whereas HPLC-MS was used to identify reaction products. The esterification reactions were observed to be reversible. A second-order reversible kinetic model was applied and rate constants were determined. The rate constants demonstrated that cetirizine was esterified about 240 times faster than indomethacin at 80 °C. The shelf-life for cetirizine in a PEG 400 formulation at 25 °C expressed as t(95%) was predicted to be only 30 h. Further, rate constants for esterification of cetirizine in PEG 1000 in relation to PEG 400 decreased by a factor of 10, probably related to increased viscosity. However, it is important to be aware of this drug-excipient interaction, as it can reduce the shelf-life of a low-average molecular weight PEG formulation considerably.

  20. A Tape Method for Fast Characterization and Identification of Active Pharmaceutical Ingredients in the 2-18 THz Spectral Range

    Science.gov (United States)

    Kissi, Eric Ofosu; Bawuah, Prince; Silfsten, Pertti; Peiponen, Kai-Erik

    2015-03-01

    In order to find counterfeit drugs quickly and reliably, we have developed `tape method' a transmission spectroscopic terahertz (THz) measurement technique and compared it with a standard attenuated total reflection (ATR) THz spectroscopic measurement. We used well-known training samples, which include commercial paracetamol and aspirin tablets to check the validity of these two measurement techniques. In this study, the spectral features of some active pharmaceutical ingredients (APIs), such as aspirin and paracetamol are characterized for identification purpose. This work covers a wide THz spectral range namely, 2-18 THz. This proposed simple but novel technique, the tape method, was used for characterizing API and identifying their presence in their dosage forms. By comparing the spectra of the APIs to their dosage forms (powder samples), all distinct fingerprints present in the APIs are also present in their respective dosage forms. The positions of the spectral features obtained with the ATR techniques were akin to that obtained from the tape method. The ATR and the tape method therefore, complement each other. The presence of distinct fingerprints in this spectral range has highlighted the possibility of developing fast THz sensors for the screening of pharmaceuticals. It is worth noting that, the ATR method is applicable to flat faced tablets whereas the tape method is suitable for powders in general (e.g. curved surface tablets that require milling before measurement). Finally, we have demonstrated that ATR techniques can be used to screen counterfeit antimalarial tablets.

  1. Analysis of low active-pharmaceutical-ingredient signal drugs based on thin layer chromatography and surface-enhanced Raman spectroscopy.

    Science.gov (United States)

    Li, Xiao; Chen, Hui; Zhu, Qingxia; Liu, Yan; Lu, Feng

    2016-11-30

    Active pharmaceutical ingredients (API) embedded in the excipients of the formula can usually be unravelled by normal Raman spectroscopy (NRS). However, more and more drugs with low API content and/or low Raman scattering coefficient were insensitive to NRS analysis, which was for the first time defined as Low API-Signal Drugs (LASIDs) in this paper. The NRS spectra of these LASIDs were similar to their dominant excipients' profiles, such as lactose, starch, microcrystalline cellulose (MCC), etc., and were classified into three types as such. 21 out of 100 kinds of drugs were screened as LASIDs and characterized further by Raman microscopic mapping. Accordingly, we proposed a tailored solution to the qualitation and quantitation problem of these LASIDs, using surface-enhanced Raman spectroscopic (SERS) detection on the thin layer chromatographic (TLC) plate both in situ and after-separation. Experimental conditions and parameters including TLC support matrix, SERS substrate, detection mode, similarity threshold, internal standard, etc., were optimized. All LASIDs were satisfactorily identified and the quantitation results agreed well with those of high performance liquid chromatography (HPLC). For some structural analogues of LASIDs, although they presented highly similar SERS spectra and were tough to distinguish even with Raman microscopic mapping, they could be successfully discriminated from each other by coupling SERS (with portable Raman spectrometer) with TLC. These results demonstrated that the proposed solution could be employed to detect the LASIDs with high accuracy and cost-effectiveness. Copyright © 2016 Elsevier B.V. All rights reserved.

  2. A Hybrid MPC-PID Control System Design for the Continuous Purification and Processing of Active Pharmaceutical Ingredients

    Directory of Open Access Journals (Sweden)

    Maitraye Sen

    2014-05-01

    Full Text Available In this work, a hybrid MPC (model predictive control-PID (proportional-integral-derivative control system has been designed for the continuous purification and processing framework of active pharmaceutical ingredients (APIs. The specific unit operations associated with the purification and processing of API have been developed from first-principles and connected in a continuous framework in the form of a flowsheet model. These integrated unit operations are highly interactive along with the presence of process delays. Therefore, a hybrid MPC-PID is a promising alternative to achieve the desired control loop performance as mandated by the regulatory authorities. The integrated flowsheet model has been simulated in gPROMSTM (Process System Enterprise, London, UK. This flowsheet model has been linearized in order to design the control scheme. The ability to track the set point and reject disturbances has been evaluated. A comparative study between the performance of the hybrid MPC-PID and a PID-only control scheme has been presented. The results show that an enhanced control loop performance can be obtained under the hybrid control scheme and demonstrate that such a scheme has high potential in improving the efficiency of pharmaceutical manufacturing operations.

  3. New Trends in Cosmetics: By-Products of Plant Origin and Their Potential Use as Cosmetic Active Ingredients

    Directory of Open Access Journals (Sweden)

    Ani Barbulova

    2015-04-01

    Full Text Available In recent years, the amount of waste deriving from industrial processes has increased substantially. Many industries produce different types of disposable by-products, rich in valuable compounds. Their characterization and valorization could not only convert them into high value products with application in diverse biotechnological fields, such as Pharmaceutics, Food or Cosmetics, but would also reduce the waste environmental impact and the related treatment costs. There are many examples of cosmetic active ingredients deriving from fish, meat and dairy products, but in the present review we would like to focus on the potentialities and the current use of compounds and extracts deriving from agronomical disposable wastes in the cosmetic field. These types of products are effective, inexpensive and bio-sustainable, and thus represent a valid alternative to the regular plant derived extracts, more commonly adopted in cosmetic formulations. Moreover, if the waste products come from organic farming, they are certainly an even more valuable source of safe extracts for Cosmetics, since they lack any residual pesticide or potentially toxic chemical.

  4. Health effects of Vaccinium myrtillus L.: evaluation of efficacy and technological strategies for preservation of active ingredients.

    Science.gov (United States)

    Smeriglio, Antonella; Monteleone, Domenico; Trombetta, Domenico

    2014-01-01

    Bilberries are a rich dietary source of various phytonutrients, including anthocyanins which contribute greatly to their antioxidant capacity and have demonstrated a broad spectrum of biomedical functions. These include protection against cardiovascular disorders, age-induced oxidative stress, inflammatory responses and several degenerative diseases. Berry anthocyanins also improve neuronal and cognitive brain functions, ocular health as well as protecting genomic DNA integrity. In recent years, sales of many dietary supplements/pharmaceutical products containing anthocyanins in various dosages and formulations have been made by advertising their wide range of beneficial effects. However, there is a heightened risk of distributing deteriorated formulations to consumers due to lax regulations, in particular those applicable to phytochemical characterization and extract standardization, and in terms of quality regarding the stability of anthocyanins. Anthocyanin pigments readily degrade during industrial processing and this can have a dramatic impact on color quality and may also affect nutritional/pharmaceutical properties. This review aims to summarize the main health effects of bilberry extract used in several food supplements/pharmaceutical formulations focusing on some important aspects of anthocyanin degradation during processing and storage. It will also describe the main technological strategies which can give active ingredients greater stability, solubility and dispersibility in order to enhance formulation quality which is of great interest to the consumer and industry due to its direct and indirect impact on consumer health.

  5. Effect of particle shape of active pharmaceutical ingredients prepared by fluidized-bed jet-milling on cohesiveness.

    Science.gov (United States)

    Fukunaka, Tadashi; Sawaguchi, Kohta; Golman, Boris; Shinohara, Kunio

    2005-05-01

    Milling is a common procedure to improve bioavailability of many active pharmaceutical ingredients (APIs), which typically have low solubility in water. But such micronization can yield an increase in the cohesiveness of particles. Although particle cohesiveness is desirable for tablet strength in the subsequent formulation process, increased particle cohesiveness can lead to operational difficulties in a milling equipment due to compaction of particles inside. In this article, the impact of milling via a fluidized-bed jet-mill on the cohesive strength and interparticle force was studied using Ethenzamide as a pharmaceutical model compound. As a result, the particle shape was found to affect both the tensile strength of powder bed and the interparticle cohesive force. A powder bed, having relatively high void fraction by direct tensile test, shows a positive correlation between the cohesive force and the particle sphericity, while powders with low void fraction by diametral compression test show a positive correlation between the cohesive force and the angularity of the particle.

  6. Wide-ranging molecular mobilities of water in active pharmaceutical ingredient (API) hydrates as determined by NMR relaxation times.

    Science.gov (United States)

    Yoshioka, Sumie; Aso, Yukio; Osako, Tsutomu; Kawanishi, Toru

    2008-10-01

    In order to examine the possibility of determining the molecular mobility of hydration water in active pharmaceutical ingredient (API) hydrates by NMR relaxation measurement, spin-spin relaxation and spin-lattice relaxation were measured for the 11 API hydrates listed in the Japanese Pharmacopeia using pulsed (1)H-NMR. For hydration water that has relatively high mobility and shows Lorentzian decay, molecular mobility as determined by spin-spin relaxation time (T(2)) was correlated with ease of evaporation under both nonisothermal and isothermal conditions, as determined by DSC and water vapor sorption isotherm analysis, respectively. Thus, T(2) may be considered a useful parameter which indicates the molecular mobility of hydration water. In contrast, for hydration water that has low mobility and shows Gaussian decay, T(2) was found not to correlate with ease of evaporation under nonisothermal conditions, which suggests that in this case, the molecular mobility of hydration water was too low to be determined by T(2). A wide range of water mobilities was found among API hydrates, from low mobility that could not be evaluated by NMR relaxation time, such as that of the water molecules in pipemidic acid hydrate, to high mobility that could be evaluated by this method, such as that of the water molecules in ceftazidime hydrate. (c) 2008 Wiley-Liss, Inc. and the American Pharmacists Association

  7. Mathematical Modeling of the Release of Active Ingredients from a Contraceptive Patch: Ortho Evra® as a Case Study

    Science.gov (United States)

    Trujillo-de Santiago, Grissel; Patricio Sáenz-Collins, Carlos; García-Arellano, Lizette; Moisés Álvarez, Mario

    2014-01-01

    Contraceptive patches have become a frequently used contraceptive method. We present a mathematical model that describes the serum concentration profiles of Norelgestromin (NGMN) and Ethinylestradiol (EE) released from the contraceptive patch Ortho Evra®. We propose a simple one-compartment model based on pharmacokinetics data reported in previous studies. The model assumes a time-dependent release rate and a first order elimination rate for each of the active ingredients contained in the patch. The model was applied to noncompliance scenarios, such as total and partial detachment of the patch or prolonged use without patch replacement. The proposed model adequately describes the clinically observed evolution of NGMN and EE in serum. Predictions from the model were successfully validated using reported experimental data of serum concentrations of NGMN and EE. This simple model can be a valuable tool to predict pharmacokinetic profiles in diverse scenarios such us non-compliance situations. Alternatively, the model can be conveniently adapted to anticipate the effect of variations on patch characteristics such as differences in contact area, doses, materials, among others. PMID:24734055

  8. Occurrence and behaviour of 105 active pharmaceutical ingredients in sewage waters of a municipal sewer collection system.

    Science.gov (United States)

    Lindberg, Richard H; Östman, Marcus; Olofsson, Ulrika; Grabic, Roman; Fick, Jerker

    2014-07-01

    The concentrations and behaviour of 105 different active pharmaceutical ingredients (APIs) in the aqueous phase of sewage water within a municipal sewer collection system have been investigated. Sewage water samples were gathered from seven pump stations (one of which was located within a university hospital) and from sewage water treatment influent and effluent. The targeted APIs were quantified using a multi-residue method based on online solid phase extraction liquid chromatography tandem mass spectrometry. The method was thoroughly validated and complies with EU regulations on sample handling, limits of quantification, quality control and selectivity. 51 APIs, including antibiotics, antidepressants, hypertension drugs, analgesics, NSAIDs and psycholeptics, were found frequently within the sewer collection system. API concentrations and mass flows were evaluated in terms of their frequency of detection, daily variation, median/minimum/maximum/average concentrations, demographic dissimilarities, removal efficiencies, and mass flow profiles relative to municipal sales data. Our results suggest that some APIs are removed from, or introduced to, the aqueous phase of sewage waters within the studied municipal collection system.

  9. [Hypersexuality associated with aripiprazole: a new case and review of the literature].

    Science.gov (United States)

    Vrignaud, Laura; Aouille, Jerémie; Mallaret, Michel; Durrieu, Geneviève; Jonville-Béra, Annie-Pierre

    2014-01-01

    We report the case of a patient with hypersexuality while he was treated with aripiprazole since 6 months. Clinical manifestations were an increased libido, unusual frequent masturbation and sexual instincts. All have resolved upon discontinuation of aripiprazole, and recurred after it was restarted. The partial dopaminergic agonist effect of aripiprazole could probably explain the occurrence of this compulsive behaviour.

  10. Electrochemical flow injection analysis of hydrazine in an excess of an active pharmaceutical ingredient: achieving pharmaceutical detection limits electrochemically.

    Science.gov (United States)

    Channon, Robert B; Joseph, Maxim B; Bitziou, Eleni; Bristow, Anthony W T; Ray, Andrew D; Macpherson, Julie V

    2015-10-06

    The quantification of genotoxic impurities (GIs) such as hydrazine (HZ) is of critical importance in the pharmaceutical industry in order to uphold drug safety. HZ is a particularly intractable GI and its detection represents a significant technical challenge. Here, we present, for the first time, the use of electrochemical analysis to achieve the required detection limits by the pharmaceutical industry for the detection of HZ in the presence of a large excess of a common active pharmaceutical ingredient (API), acetaminophen (ACM) which itself is redox active, typical of many APIs. A flow injection analysis approach with electrochemical detection (FIA-EC) is utilized, in conjunction with a coplanar boron doped diamond (BDD) microband electrode, insulated in an insulating diamond platform for durability and integrated into a two piece flow cell. In order to separate the electrochemical signature for HZ such that it is not obscured by that of the ACM (present in excess), the BDD electrode is functionalized with Pt nanoparticles (NPs) to significantly shift the half wave potential for HZ oxidation to less positive potentials. Microstereolithography was used to fabricate flow cells with defined hydrodynamics which minimize dispersion of the analyte and optimize detection sensitivity. Importantly, the Pt NPs were shown to be stable under flow, and a limit of detection of 64.5 nM or 0.274 ppm for HZ with respect to the ACM, present in excess, was achieved. This represents the first electrochemical approach which surpasses the required detection limits set by the pharmaceutical industry for HZ detection in the presence of an API and paves the wave for online analysis and application to other GI and API systems.

  11. Role of aripiprazole in treatment-resistant schizophrenia

    Directory of Open Access Journals (Sweden)

    Mossaheb N

    2012-05-01

    Full Text Available Nilufar Mossaheb,1 Rainer M Kaufmann21Department of Child and Adolescent Psychiatry, 2Department of Psychiatry and Psychotherapy, Medical University, Vienna, AustriaAbstract: About one third of patients with schizophrenia respond unsatisfactorily to antipsychotic treatment and are termed “treatment-resistant”. Clozapine is still the gold standard in these cases. However, 40%–70% of patients do not improve sufficiently on clozapine either. In the search for more efficacious strategies for treatment-resistant schizophrenia, drugs with different pharmacological profiles seem to raise new hopes, but are they valid? The aim of this review was to evaluate the evidence for aripiprazole as a potential strategy in monotherapy or combination therapy for patients with treatment-resistant schizophrenia. The evidence for aripiprazole monotherapy and for the combination of aripiprazole with psychotropics other than clozapine is scant, and no recommendation can be made on the basis of the currently available data. More effort has been made in describing combinations of aripiprazole and clozapine. Most of the open-label and case studies as well as case reports have shown positive effects of this combination on overall psychopathology and to some extent on negative symptoms. Several reports describe the possibility of dose reduction for clozapine in combination with aripiprazole, a strategy that might help so-called “treatment-intolerant” patients. The findings of four randomized controlled trials with respect to changes in psychopathology seem less conclusive. The most commonly found beneficial effects are better metabolic outcomes and indicators of the possibility of reducing the clozapine dose. However, other side effects, such as akathisia, are repeatedly reported. Further, none of the studies report longer-term outcomes. In the absence of alternatives, polypharmacy is a common strategy in clinical practice. Combining aripiprazole with clozapine in

  12. 蒿属植物的农药活性及其有效成分%Pesticidal Activities and Active Ingredients of Artemisia

    Institute of Scientific and Technical Information of China (English)

    周利娟; 桑晓清; 孙永艳; 杨文杰

    2012-01-01

    Recent studies on pesticidal activities and the corresponding active ingredients of Artemisia are presented. Artemisia annua, Artemisia lavandulaefolia, Artemisia absinthium, Artemisia selengensis, Artemisia vestita, Artemisia parvijlora, Artemisia sieversiana, Artemisia scoparia, Artemisia capillarie, Artemisia mongoli-ca, Artemisia borealis, Artemisia nilagirica, Artemisia monosperma and Artemisia judaica possess insecticidal activities and the main active ingredients are cineole, borneol, camphor, caryophyllene, isoaryophyllene and farnesene. Artemisia annua, Artemisia ludoviciana, Artemisia tournefortiana, Artemisia absinthium, Artemisia herba alba, Artemisia taurica, Artemisia judaica, Artemisia borealis, Artemisia molinieri, Artemisia stolonifera show fungicidal activities and the main active ingredients are camphor, cineole, borneol, flavonoids, olefins, terpene hydrocarbons, alkanes and organic acids. Artemisia caerulescens subsp. gallica, Artemisia ordosica, Artemisia roxburghiana,Artenisia annua, Artemisia tridentate, Artemisia scoparia and Artemisia taurica exhibit herbicide activities and the main active ingredients are cineole, camphor, arteether, monoterpenes and ses-quiterpenes. Artemisia absinthium shows nematicidal activity. Artemisia absinthium and Artemisia dracunculus have mollusicidal activities. In all, Artemisia annua, Artemisia absinthium, Artemisia borealis and Artemisia judaica show multiple activities and may be used as botanical pesticides.%综述了蒿属植物的杀虫、杀螨、杀菌、除草、杀线虫和杀软体动物活性及相应的有效成分.该属中具有杀虫杀螨活性的主要有黄花蒿、野艾蒿、苦艾、蒌蒿、毛莲蒿、西南牡蒿、大籽蒿、猪毛蒿、茵陈蒿、蒙古蒿、巴儿古津蒿、南亚蒿、犹地蒿和Artemisia monsperma等,其主要有效成分是桉树脑、龙脑、樟脑、石竹烯、异石竹烯和β-法呢烯等.该属中具有杀菌活性的主要有黄花蒿、银叶艾蒿

  13. Potential ecological footprints of active pharmaceutical ingredients: an examination of risk factors in low-, middle- and high-income countries.

    Science.gov (United States)

    Kookana, Rai S; Williams, Mike; Boxall, Alistair B A; Larsson, D G Joakim; Gaw, Sally; Choi, Kyungho; Yamamoto, Hiroshi; Thatikonda, Shashidhar; Zhu, Yong-Guan; Carriquiriborde, Pedro

    2014-11-19

    Active pharmaceutical ingredients (APIs) can enter the natural environment during manufacture, use and/or disposal, and consequently public concern about their potential adverse impacts in the environment is growing. Despite the bulk of the human population living in Asia and Africa (mostly in low- or middle-income countries), limited work relating to research, development and regulations on APIs in the environment have so far been conducted in these regions. Also, the API manufacturing sector is gradually shifting to countries with lower production costs. This paper focuses mainly on APIs for human consumption and highlights key differences between the low-, middle- and high-income countries, covering factors such as population and demographics, manufacture, prescriptions, treatment, disposal and reuse of waste and wastewater. The striking differences in populations (both human and animal), urbanization, sewer connectivity and other factors have revealed that the environmental compartments receiving the bulk of API residues differ markedly between low- and high-income countries. High sewer connectivity in developed countries allows capture and treatment of the waste stream (point-source). However, in many low- or middle-income countries, sewerage connectivity is generally low and in some areas waste is collected predominantly in septic systems. Consequently, the diffuse-source impact, such as on groundwater from leaking septic systems or on land due to disposal of raw sewage or septage, may be of greater concern. A screening level assessment of potential burdens of APIs in urban and rural environments of countries representing low- and middle-income as well as high-income has been made. Implications for ecological risks of APIs used by humans in lower income countries are discussed. © 2014 The Author(s) Published by the Royal Society. All rights reserved.

  14. Characterization of solid polymer dispersions of active pharmaceutical ingredients by 19F MAS NMR and factor analysis

    Science.gov (United States)

    Urbanova, Martina; Brus, Jiri; Sedenkova, Ivana; Policianova, Olivia; Kobera, Libor

    In this contribution the ability of 19F MAS NMR spectroscopy to probe structural variability of poorly water-soluble drugs formulated as solid dispersions in polymer matrices is discussed. The application potentiality of the proposed approach is demonstrated on a moderately sized active pharmaceutical ingredient (API, Atorvastatin) exhibiting extensive polymorphism. In this respect, a range of model systems with the API incorporated in the matrix of polvinylpyrrolidone (PVP) was prepared. The extent of mixing of both components was determined by T1(1H) and T1ρ(1H) relaxation experiments, and it was found that the API forms nanosized domains. Subsequently it was found out that the polymer matrix induces two kinds of changes in 19F MAS NMR spectra. At first, this is a high-frequency shift reaching 2-3 ppm which is independent on molecular structure of the API and which results from the long-range polarization of the electron cloud around 19F nucleus induced by electrostatic fields of the polymer matrix. At second, this is broadening of the signals and formation of shoulders reflecting changes in molecular arrangement of the API. To avoid misleading in the interpretation of the recorded 19F MAS NMR spectra, because both the contributions act simultaneously, we applied chemometric approach based on multivariate analysis. It is demonstrated that factor analysis of the recorded spectra can separate both these spectral contributions, and the subtle structural differences in the molecular arrangement of the API in the nanosized domains can be traced. In this way 19F MAS NMR spectra of both pure APIs and APIs in solid dispersions can be directly compared. The proposed strategy thus provides a powerful tool for the analysis of new formulations of fluorinated pharmaceutical substances in polymer matrices.

  15. Fusion production of solid dispersions containing a heat-sensitive active ingredient by hot melt extrusion and Kinetisol dispersing.

    Science.gov (United States)

    Dinunzio, James C; Brough, Chris; Hughey, Justin R; Miller, Dave A; Williams, Robert O; McGinity, James W

    2010-02-01

    Many techniques for the production of solid dispersions rely on elevated temperatures and prolonged material residence times, which can result in decomposition of temperature-sensitive components. In this study, hydrocortisone was used as a model temperature-sensitive active ingredient to study the effect of formulation and processing techniques as well as to characterize the benefits of KinetiSol Dispersing for the production of solid dispersions. Preformulation studies were conducted using differential scanning calorimetry and hot stage microscopy to identify optimum carriers for the production of amorphous solid dispersions. After identification, solid dispersions were prepared by hot melt extrusion and KinetiSol Dispersing, with material characterized by X-ray diffraction, dissolution and potency testing to evaluate physicochemical properties. Results from the preformulation studies showed that vinylacetate:vinylpyrrolidone (PVPVA) copolymer allowed for hydrocortisone dissolution within the carrier at temperatures as low as 160 degrees C, while hydroxypropyl methylcellulose required temperatures upward of 180 degrees C to facilitate solubilization. Low substituted hydroxypropyl cellulose, a high glass transition temperature control, showed that the material was unable to solubilize hydrocortisone. Manufacturing process control studies using hot melt extruded compositions of hydrocortisone and PVPVA showed that increased temperatures and residence times negatively impacted product potency due to decomposition. Using KinetiSol Dispersing to reduce residence time and to facilitate lower temperature processing, it was possible to produce solid dispersions with improved product potency. This study clearly demonstrated the importance of carrier selection to facilitate lower temperature processing, as well as the effect of residence time on product potency. Furthermore, KinetiSol Dispersing provided significant advantages over hot melt extrusion due to the reduced

  16. Assessment of active pharmaceutical ingredient particle size in tablets by Raman chemical imaging validated using polystyrene microsphere size standards.

    Science.gov (United States)

    Kuriyama, Atsushi; Ozaki, Yukihiro

    2014-04-01

    Particle size is a critical parameter for controlling pharmaceutical quality. The aim of this study was to assess the size of the micrometer-scale active pharmaceutical ingredients (API) in tablets using Raman chemical imaging and to understand the effects of formulation on particle size. Model tablets containing National Institute of Standards and Technology traceable polystyrene microsphere size standards were developed to determine the binarization threshold value of Raman chemical images for API particle sizing in specific formulations and processes. Three sets of model tablets containing 5, 10, and 15 μm polystyrene microspheres, used to mimic API, were prepared using a commercial tablet formulation (Ebastel tablets, mean API particle size was about 5 μm). Raman mapping with a 50× objective (NA, 0.75) was applied to tablet cross-sections, and particle size of polystyrene microspheres was estimated from binary images using several binarization thresholds. Mean particle size for three sets of polystyrene microspheres showed good agreement between pre- and postformulation (the slope = 1.024, R = 1.000) at the specific threshold value ((mean + 0.5σ) of the polystyrene-specific peak intensity histogram), regardless of particle agglomeration, tablet surface roughness, and laser penetration depth. The binarization threshold value showed good applicability to Ebastel tablets, where the API-specific peak intensity histogram showed a pattern similar to that of polystyrene microspheres in model tablets. The model tablets enabled determination of an appropriate binarization threshold for assessing the mean particle size of micrometer-scale API in tablets by utilizing the unique physicochemical properties of polystyrene microspheres.

  17. Measurement of low amounts of amorphous content in hydrophobic active pharmaceutical ingredients with dynamic organic vapor sorption.

    Science.gov (United States)

    Müller, Thorsten; Schiewe, Jörg; Smal, Rüdiger; Weiler, Claudius; Wolkenhauer, Markus; Steckel, Hartwig

    2015-05-01

    Today, a variety of devices for dry powder inhalers (DPIs) is available and many different formulations for optimized deposition in the lung are developed. However, during the production of powder inhalers, processing steps may induce changes to both, the carrier and active pharmaceutical ingredients (APIs). It is well known that standard pharmaceutical operations may lead to structural changes, crystal defects and amorphous regions. Especially operations such as milling, blending and even sieving generate these effects. These disorders may induce re-crystallization and particle size changes post-production which have a huge influence on drug delivery and product stability. In this study, pilot tests with a polar solvent (water) and hydrophilic drug (Salbutamol sulfate) were performed to receive a first impression on further possible implementation of hydrophobic samples with organic solvents. Thereafter, a reliable method for the accurate detection of low amounts of amorphous content is described up to a limit of quantification (LOQ) of 0.5% for a hydrophobic model API (Ciclesonide). The organic vapor sorption method which is a gravimetric method quantifies exactly these low amounts of amorphous content in the hydrophobic powder once the suitable solvent (isopropanol), the correct p/p0 value (0.1) and the exact temperature (25°C) have been found. Afterward it was possible to quantitate low amorphous amounts in jet-milled powders (0.5-17.0%). In summary, the data of the study led to a clearer understanding in what quantity amorphous parts were generated in single production steps and how variable these parts behave to fully crystalline material. Nevertheless it showed how difficult it was to re-crystallize hydrophobic material with water vapor over a short period. For the individual samples it was possible to determine the single humidity at which the material starts to re-crystallize, the behavior against different nonpolar solvents and the calculation of the

  18. 21 CFR 310.538 - Drug products containing active ingredients offered over-the-counter (OTC) for use for ingrown...

    Science.gov (United States)

    2010-04-01

    ... offered over-the-counter (OTC) for use for ingrown toenail relief. 310.538 Section 310.538 Food and Drugs... ingredients offered over-the-counter (OTC) for use for ingrown toenail relief. (a) Any product that bears labeling claims such as for “temporary relief of discomfort from ingrown toenails,” or “ingrown...

  19. Genotoxic Potential of Two Herbicides and their Active Ingredients Assessed with Comet Assay on a Fish Cell Line, Epithelioma Papillosum Cyprini (EPC)

    DEFF Research Database (Denmark)

    Syberg, Kristian; Rank, Jette; Jensen, Klara

    2013-01-01

    The aim of this study was to optimize the epithelioma papillosum cyprini (EPC) cell line handling procedure for the comet assay to investigate the genotoxic potential of widely used pesticides. The effects of various media and handling of the EPC cell line were examined. Results indicated...... that avoiding trypsin to detach cells led to lower level of DNA damage in the negative control. Further, two commonly used herbicides (Dezormon and Optica trio) and their four active ingredients (4-chloro-o-tolyloxyacetic acid, 2,4-dichlorophenoxyacetic acid, 2-(4-chloro-2-methylphenoxy)propionic acid, 2......-(2,4-dichlorophenoxy)propionic acid) individually and in a ternary mixture were examined with the comet assay. Data showed that among the active ingredients only 2,4-D andMCPA induced DNA damage, while both herbicides were genotoxic at high concentrations....

  20. Supersaturation of Calcipotriene and Betamethasone Dipropionate in a Novel Aerosol Foam Formulation for Topical Treatment of Psoriasis Provides Enhanced Bioavailability of the Active Ingredients

    OpenAIRE

    2016-01-01

    Introduction Previous studies have demonstrated the superior efficacy of a novel aerosol foam formulation of fixed combination calcipotriene 0.005% (Cal) and betamethasone dipropionate 0.064% (BD), compared with the ointment formulation. The aim of this study is to ascertain whether enhanced bioavailability of the active ingredients due to supersaturation and/or occlusive properties can explain the observed greater clinical efficacy. Methods Solubility and evaporation experiments were conduct...

  1. Altered Gene Expression in the Schistosome-Transmitting Snail Biomphalaria glabrata following Exposure to Niclosamide, the Active Ingredient in the Widely Used Molluscicide Bayluscide

    OpenAIRE

    Si-Ming Zhang; Buddenborg, Sarah K.; Adema, Coen M.; John T Sullivan; Loker, Eric S

    2015-01-01

    In view of the call by the World Health Organization (WHO) for elimination of schistosomiasis as a public health problem by 2025, use of molluscicides in snail control to supplement chemotherapy-based control efforts is likely to increase in the coming years. The mechanisms of action of niclosamide, the active ingredient in the most widely used molluscicides, remain largely unknown. A better understanding of its toxicology at the molecular level will both improve our knowledge of snail biolog...

  2. Capillary-induced Homogenization of Matrix in Paper: A Powerful Approach for the Quantification of Active Pharmaceutical Ingredients Using Mass Spectrometry Imaging

    Science.gov (United States)

    de Menezes, Maico; de Oliveira, Diogo Noin; Catharino, Rodrigo Ramos

    2016-07-01

    Herein we present a novel approach for the quantification of active pharmaceutical ingredients (APIs) using mass spectrometry imaging. This strategy uses a filter paper previously “eluted” with a MALDI matrix solution as a support for analyte application. Samples are submitted to mass spectrometry imaging (MSI) and quantification through characteristic fingerprints is ultimately performed. Results for the content of rosuvastatin from a known formulation are comparable to those obtained with a validated HPLC method.

  3. In vitro effects of buyang huanwu decoction and its ingredients on inhibiting the specific binding of 3H-platelet activating factor to its receptor in rabbits

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    BACKGROUND: Pharmacologic action of traditional Chinese medicine compound is the comprehensive effect of various ingredients, and the interactions of various ingredients are closely correlated with the final effect. In order to reveal the compatibility mechanism of buyang huanwu decoction (BHD)'s prescription in treating and preventing ischemic cerebrovascular disease, we need to explore the effect and relation of ingredients in prescription except for considering the effect of each ingredient on the whole prescription.OBJECTIVE: To study the effect of BHD and its ingredients in the prescription on the specific binding of 3H-platelet activating factor (PAF) to its receptor (PAFR)in rabbits in vitro, and to analyze the action of each ingredient in the prescription.DESIGN: A decomposed recipe study based on orthogonal test.SETTING: Guangzhou University of Traditional Chinese Medicine.MATERIALS: Five healthy adult New Zealand rabbits of either gender were provided by the Experimental Animal Center of Guangzhou University of Traditional Chinese medicine. The prescription herbal pieces were purchased from Foshan Kangpu Pharmaceuticals Company and Jianmin Pharmaceuticals Company, and were appraised by Professor Yanchen Xu from College of Traditional Chinese Medicine, Guangzhou University of Traditional Chinese Medicine. 3H-PAF was supplied by Amersham Co.,Ltd.(Specific activity:6.475 TBq/mmol;batch number:200402); PAF standard by Biomol Co., Ltd.(batch number: P1318V).METHODS: This experiment was carried out in the Laboratory of Nuclear Medicine, Guangzhou University of Traditional Chinese Medicine between September and December 2004. ① The seven influencing factors were selected: such as Shenghuangqi , Dangguiwei, Chishao, Dilong, Taoren, Honghua, Chuanxiong. Each factor was divided into two levels, selected or not selected. The tests were arranged according to L8 (27) orthogonal test table. ②The specific binding of 3H-PAF to its receptors in rabbits was measured by

  4. [Studies on effects of Achyranthes bidentata on tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in vivo pharmacokinetics].

    Science.gov (United States)

    Cheng, Jian; Di, Liu-Qing; Shan, Jin-Jun; Zhao, Xiao-Li; Kang, An; Bi, Xiao-Lin; Li, Jun-Song

    2014-04-01

    To study on the effects of Achyranthes bidentata on Tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in rats in vivo pharmacokinetic behaviors, a method for the simultaneous determination of chlorogenic acid, isoliquiritin, harpagoside and liquiritigenin in rat plasma was established by UPLC-MS/MS. The analysis was performed on a waters Acquity BEH C18 column (2.1 mm x 100 mm, 1.7 microm) with the mixture of acetonitrile and 0.1% formic acid/water as mobile phase, and the gradient elution at a flow rate of 0.3 mL x min(-1). The analytes were detected by tandem mass spectrometry with the electrospray ionization (ESI) source and in the multiple reaction monitoring (MRM) mode. It turned out that the analytes of Tongsaimai pellets groups C(max) and AUC(Q-infinity) values were higher than that with A. bidentata group, and the C(max) values of chlorogenic acid had significantly difference (P < 0.05), the AUC(0-infinity) values of chlorogenic acid and glycyrrhizin had significantly difference (P < 0.05); The T(max) and CL values of two groups had no significantly difference. Results showed that the established method was specific, rapid, accurate and sensitive for the studies of Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic, and A. bidentata have varying degrees of effects on Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic behaviors.

  5. The simultaneous determination of active ingredients in cough-cold mixtures by isocratic reversed-phase ion-pair high-performance liquid chromatography.

    Science.gov (United States)

    Lau, O W; Chan, K; Lau, Y K; Wong, W C

    1989-01-01

    A simple, rapid and accurate method for the simultaneous determination of active ingredients in cough-cold mixtures using isocratic reversed-phase ion-pair high-performance liquid chromatography has been developed. It involves the use of an octadecylsilane column as the stationary phase with methanol, water, tetrahydrofuran, phosphoric acid mixtures as mobile phase including sodium dioctylsulphosuccinate as the ion-pair agent. The pH of the mobile phase was adjusted to 4.6 by means of phosphoric acid and ammonium hydroxide solutions. The proposed method involves the simple dilution of the samples with the mobile phase and the addition of metoclopramide hydrochloride as the internal standard. The active ingredients under investigation were chlorpheniramine, codeine, diphenhydramine, ephedrine, ethylmorphine, phenylephrine, phenylpropanolamine and pholcodine, which exist as various combinations in cough-cold mixtures. The optimum composition of the mobile phase and the optimum flow rate were determined and are reported. The method was applied to the determination of active ingredients in seven commercially available cough-cold mixtures.

  6. Non-Hodgkin Lymphoma and Occupational Exposure to Agricultural Pesticide Chemical Groups and Active Ingredients: A Systematic Review and Meta-Analysis

    Directory of Open Access Journals (Sweden)

    Leah Schinasi

    2014-04-01

    Full Text Available This paper describes results from a systematic review and a series of meta-analyses of nearly three decades worth of epidemiologic research on the relationship between non-Hodgkin lymphoma (NHL and occupational exposure to agricultural pesticide active ingredients and chemical groups. Estimates of associations of NHL with 21 pesticide chemical groups and 80 active ingredients were extracted from 44 papers, all of which reported results from analyses of studies conducted in high-income countries. Random effects meta-analyses showed that phenoxy herbicides, carbamate insecticides, organophosphorus insecticides and the active ingredient lindane, an organochlorine insecticide, were positively associated with NHL. In a handful of papers, associations between pesticides and NHL subtypes were reported; B cell lymphoma was positively associated with phenoxy herbicides and the organophosphorus herbicide glyphosate. Diffuse large B-cell lymphoma was positively associated with phenoxy herbicide exposure. Despite compelling evidence that NHL is associated with certain chemicals, this review indicates the need for investigations of a larger variety of pesticides in more geographic areas, especially in low- and middle-income countries, which, despite producing a large portion of the world’s agriculture, were missing in the literature that were reviewed.

  7. Successful treatment of a prolactinoma with the antipsychotic drug aripiprazole

    Science.gov (United States)

    Bakker, Ilse C A; Schubart, Chris D

    2016-01-01

    Summary In this report, we describe a female patient with both prolactinoma and psychotic disorder who was successfully treated with aripiprazole, a partial dopamine 2 receptor agonist. During the follow-up of more than 10 years, her psychotic symptoms improved considerably, prolactin levels normalised and the size of the prolactinoma decreased. This observation may be of clinical relevance in similar patients who often are difficult to treat with the regular dopaminergic drugs. Learning points Prolactinoma coinciding with psychosis can represent a therapeutic challenge. In contrast to many other antipsychotic drugs, aripiprazole is associated with a decrease in prolactin levels. Aripiprazole can be a valuable pharmaceutical tool to treat both prolactinoma and psychosis. PMID:27284453

  8. Biological conversion of aripiprazole lauroxil − An N-acyloxymethyl aripiprazole prodrug

    Directory of Open Access Journals (Sweden)

    Morten Rohde

    2014-01-01

    Full Text Available N-acyloxyalkylation of NH-acidic compounds can be a prodrug approach for e.g. tertiary or some N-heterocyclic amines and secondary amides and have the potential to modify the properties of the parent drug for specific uses, for example its physicochemical, pharmacokinetic or biopharmaceutical properties. Aripiprazole lauroxil was prepared as a model compound for such prodrugs and its bioconversion was investigated both in vitro and in vivo. Theoretically, N-acyloxyalkyl derivates of NH-acid compounds undergo a two-step bioconversion into the parent NH-acidic drug through an N-hydroxyalkyl intermediate. However, to our knowledge no published studies have investigated the formation of an intermediate in vivo. In the present study, it was demonstrated that the assumed N-hydroxymethyl intermediate was readily observed both in vitro and in vivo. In vivo, the observed plasma concentration of the intermediate was at the same level as the drug (aripiprazole. When prodrug intermediates are formed, it is important to make a proper pharmacological, pharmacokinetic and toxicological evaluation of the intermediates to ensure patient safety; however, several challenges were identified when testing an N-acyloxyalkyl prodrug. These included the development of a suitable bioanalytical method, the accurate prediction of prodrug bioconversion and thereby the related pharmacokinetics in humans and the toxicological potential of the intermediate.

  9. Active pharmaceutical ingredient (API) production involving continuous processes--a process system engineering (PSE)-assisted design framework.

    Science.gov (United States)

    Cervera-Padrell, Albert E; Skovby, Tommy; Kiil, Søren; Gani, Rafiqul; Gernaey, Krist V

    2012-10-01

    A systematic framework is proposed for the design of continuous pharmaceutical manufacturing processes. Specifically, the design framework focuses on organic chemistry based, active pharmaceutical ingredient (API) synthetic processes, but could potentially be extended to biocatalytic and fermentation-based products. The method exploits the synergic combination of continuous flow technologies (e.g., microfluidic techniques) and process systems engineering (PSE) methods and tools for faster process design and increased process understanding throughout the whole drug product and process development cycle. The design framework structures the many different and challenging design problems (e.g., solvent selection, reactor design, and design of separation and purification operations), driving the user from the initial drug discovery steps--where process knowledge is very limited--toward the detailed design and analysis. Examples from the literature of PSE methods and tools applied to pharmaceutical process design and novel pharmaceutical production technologies are provided along the text, assisting in the accumulation and interpretation of process knowledge. Different criteria are suggested for the selection of batch and continuous processes so that the whole design results in low capital and operational costs as well as low environmental footprint. The design framework has been applied to the retrofit of an existing batch-wise process used by H. Lundbeck A/S to produce an API: zuclopenthixol. Some of its batch operations were successfully converted into continuous mode, obtaining higher yields that allowed a significant simplification of the whole process. The material and environmental footprint of the process--evaluated through the process mass intensity index, that is, kg of material used per kg of product--was reduced to half of its initial value, with potential for further reduction. The case-study includes reaction steps typically used by the pharmaceutical

  10. Efficacy of aripiprazole in sulpiride-induced tardive oromandibular dystonia.

    Science.gov (United States)

    Imai, Noboru; Ikawa, Masako

    2011-01-01

    Tardive dystonia is a side effect of dopamine receptor-blocking agents, which are mainly used as antipsychotic drugs. The treatment of tardive dystonia is difficult and often unsuccessful. An 82-year-old woman experienced mandibular deviation to the left due to spasm of the masticatory muscles with involuntary chewing movement and Parkinsonism. She had been treated with sulpiride for motility disorder for 5 years. Parkinsonism almost disappeared after the withdrawal of sulpiride, but tardive oromandibular dystonia showed no improvement. Aripiprazole treatment at 3 mg/day improved tardive oromandibular dystonia without worsening Parkinsonism. Low-dosage aripiprazole may be effective for tardive oromandibular dystonia in patients with no other psychiatric disorder.

  11. Understanding the risks associated with the use of new psychoactive substances (NPS): high variability of active ingredients concentration, mislabelled preparations, multiple psychoactive substances in single products.

    Science.gov (United States)

    Zamengo, Luca; Frison, Giampietro; Bettin, Chiara; Sciarrone, Rocco

    2014-08-17

    New psychoactive substances (NPS), are now a large group of substances of abuse not yet completely controlled by international drug conventions, which may pose a public health threat. Anxiety, paranoia, hallucinations, seizures, hyperthermia and cardiotoxicity are some of the common adverse effects associated with these compounds. In this paper, three case reports taken from the archive of processed cases of the authors' laboratory are presented and discussed to stress the risks of possible adverse consequences for NPS users: in particular, (i) the risk deriving from the difficulty of predicting the actual consumed dose, due to variability of active ingredients concentration in consumed products, (ii) the risk deriving from the difficulty of predicting the actual active ingredients present in consumed products, as opposed to those claimed by the manufacturer, and (iii) the risk deriving from the difficulty of predicting the actual pharmacological and toxicological effects related to the simultaneous consumption of different psychoactive ingredients contained in single products, whose interactions are mostly unknown. Each of them individually provide a source of concern for possible serious health related consequences. However, they should be considered in conjunction with each others, with the worldwide availability of NPS through the web and also with the incessantly growing business derived from the manipulation and synthesis of new substances. The resulting scenario is that of a cultural challenge which demands a global approach from different fields of knowledge.

  12. [6]-gingerol and [6]-shogaol, active ingredients of the traditional Japanese medicine hangeshashinto, relief oral ulcerative mucositis-induced pain via action on Na(+) channels.

    Science.gov (United States)

    Hitomi, Suzuro; Ono, Kentaro; Terawaki, Kiyoshi; Matsumoto, Chinami; Mizuno, Keita; Yamaguchi, Kiichiro; Imai, Ryota; Omiya, Yuji; Hattori, Tomohisa; Kase, Yoshio; Inenaga, Kiyotoshi

    2017-03-01

    The traditional Japanese herbal medicine hangeshashinto (HST) has beneficial effects for the treatment of oral ulcerative mucositis (OUM) in cancer patients. However, the ingredient-based mechanism that underlies its pain-relieving activity remains unknown. In the present study, to clarify the analgesic mechanism of HST on OUM-induced pain, we investigated putative HST ingredients showing antagonistic effects on Na(+) channels in vitro and in vivo. A screen of 21 major ingredients using automated patch-clamp recordings in channel-expressing cells showed that [6]-gingerol and [6]-shogaol, two components of a Processed Ginger extract, considerably inhibited voltage-activated Na(+) currents. These two ingredients inhibited the stimulant-induced release of substance P and action potential generation in cultured rat sensory neurons. A submucosal injection of a mixture of [6]-gingerol and [6]-shogaol increased the mechanical withdrawal threshold in healthy rats. In a rat OUM model, OUM-induced mechanical pain was alleviated 30min after the swab application of HST despite the absence of anti-bacterial and anti-inflammatory actions in the OUM area. A swab application of a mixture of [6]-gingerol and [6]-shogaol induced sufficient analgesia of OUM-induced mechanical or spontaneous pain when co-applied with a Ginseng extract containing abundant saponin. The Ginseng extract demonstrated an acceleration of substance permeability into the oral ulcer tissue without an analgesic effect. These findings suggest that Na(+) channel blockage by gingerol/shogaol plays an essential role in HST-associated analgesia of OUM-induced pain. This pharmacological mechanism provides scientific evidence supporting the use of this herbal medicine in patients suffering from OUM-induced pain.

  13. Investigation of overfoaming activities and gushing mechanisms of individual beer ingredients as model substances in bottled carbonated water.

    Science.gov (United States)

    Aydın, Ahmet Alper; Ilberg, Vladimir; Titze, Jean

    2014-08-01

    Researchers in several disciplines are interested in understanding the spontaneous and eruptive overfoaming (gushing) of carbonated beverages, as it is an essential problem of both the brewing and beverage industries. In order to understand the mechanism(s) taking place in gushing beer, several beer ingredients have been investigated as model substances in a much simpler matrix of carbonated water. For this purpose, sinapic acid, vanillic acid, ferulic acid, cinnamic acid and palmitic acid have been chosen as model beer ingredients. Gushing formation of the investigated beer ingredients depends on the degree of stabilized solvated molecular carbon dioxide in water. For this purpose, functional groups capable of forming hydrogen bonds with electronegative oxygen atoms of carbon dioxide are needed. However, the solubility of the substances plays an important role in the abundance of these functional groups in undissociated form to interact with molecular carbon dioxide. The reported data provide valuable insights into the gushing problem and help to understand its formation pathways. Each gushing-positive substance has an individual mechanism related to its structural conformation and solubility level. Therefore possible gushing mechanisms have been proposed with respect to the structural changes in model substances to clarify the differences in observed overfoaming and gushing stability levels. © 2013 Society of Chemical Industry.

  14. "Natural" ingredients in cosmetic dermatology.

    Science.gov (United States)

    Baumann, Leslie; Woolery-Lloyd, Heather; Friedman, Adam

    2009-06-01

    Recently, both clinical and bench research has begun to provide scientific validation for the use of certain botanical ingredients. Related findings regarding proposed biological mechanisms of action have translated into clinical practice. Botanical compounds for which dermatologic and cosmetic applications have emerged include: olive oil, chamomile, colloidal oatmeal, oat kernal extract, feverfew, acai berry, coffee berry, curcumin, green tea, pomegranate, licorice, paper mulberry, arbutin, and soy. Many of these botanical sources offer biologically active components that require further in vitro and in vivo investigation in order for us to properly educate ourselves, and our patients, regarding over-the-counter products based on these ingredients.

  15. Polysaccharide-Containing Macromolecules in a Kampo (Traditional Japanese Herbal Medicine, Hochuekkito: Dual Active Ingredients for Modulation of Immune Functions on Intestinal Peyer's Patches and Epithelial cells

    Directory of Open Access Journals (Sweden)

    Hiroaki Kiyohara

    2011-01-01

    Full Text Available A traditional Japanese herbal (Kampo medicine, Hochuekkito (Bu-Zhong-Yi-Qi-Tang in Chinese, TJ-41 is a well-known Kampo formula, and has been found to enhance antigen-specific antibody response in not only local mucosal immune system in upper respiratory tract, but also systemic immune system through upper respiratory mucosal immune system. Although this immunopharmacological effect has been proposed to express by modulation of intestinal immune system including Peyer's patches and intestinal epithelial cells, active ingredients are not known. TJ-41 directly affected the production of bone marrow cell-proliferative growth factors from murine Peyer's patch immunocompetent cells in vitro. Among low molecular, intermediate size and macromolecular weight fractions prepared from TJ-41, only fraction containing macromolecular weight ingredients showed Peyer's patch-mediated bone marrow cell-proliferation enhancing activity. Anion-exchange chromatography and gel filtration gave 17 subfractions comprising polysaccharides and lignins from the macromolecular weight fraction of TJ-41, and some of the subfractions showed significant enhancing activities having different degrees. Some of the subfractions also expressed stimulating activity on G-CSF-production from colonic epithelial cells, and statistically significant positive correlation was observed among enhancing activities of the subfractions against Peyer's patch immunocompetent cells and epithelial cells. Among the fractions from TJ-41 oral administration of macromolecular weight ingredient fraction to mice succeeded to enhance antigen-specific antibody response in systemic immune system through upper respiratory mucosal immune system, but all the separated fractions failed to enhance the in vivo antibody response in upper respiratory tract.

  16. Successful treatment of a prolactinoma with the antipsychotic drug aripiprazole

    NARCIS (Netherlands)

    Bakker, Ilse C A; Schubart, Chris D; Zelissen, Pierre M J

    2016-01-01

    In this report, we describe a female patient with both prolactinoma and psychotic disorder who was successfully treated with aripiprazole, a partial dopamine 2 receptor agonist. During the follow-up of more than 10 years, her psychotic symptoms improved considerably, prolactin levels normalised and

  17. Cognitive-enhancing effects of aripiprazole: a case report

    Directory of Open Access Journals (Sweden)

    Galderisi Silvana

    2008-10-01

    Full Text Available Abstract Patients with schizophrenia often present mild to severe cognitive deficits which contribute to their social disability. Second-generation antipsychotics have shown only mild to moderate beneficial effects on cognition. The present case report suggests cognitive enhancing effects of aripiprazole, a dopamine partial agonist, shown to increase dopamine release in prefrontal cortex in animal studies. The patient was in his first-episode of schizophrenia, and had no previous exposure to first-generation antipsychotics. Before schizophrenia onset his cognitive functioning was poor and he could not attend regular courses to reach his high school degree; he started but was not able to attend the University courses for several years. After schizophrenia onset, he was treated, in sequence, with olanzapine, amisulpride and aripiprazole. During treatment with the first two second-generation antipsychotics, positive symptoms markedly improved while cognitive functioning remained poor. During treatment with aripiprazole, clinical remission was obtained and the patient was able to attend university courses and pass several examinations. Social functioning was markedly improved. Aripiprazole demonstrated cognitive enhancing effects in this patient. These effects were long-lasting and paralleled by a positive impact on social functioning.

  18. Silver sucrose octasulfate (IASOS™ as a valid active ingredient into a novel vaginal gel against human vaginal pathogens: in vitro antimicrobial activity assessment.

    Directory of Open Access Journals (Sweden)

    Cinzia Marianelli

    Full Text Available This in vitro study assessed the antimicrobial properties of a novel octasilver salt of Sucrose Octasulfate (IASOS as well as of an innovative vaginal gel containing IASOS (SilSOS Femme, against bacterial and yeast pathogens isolated from human clinical cases of symptomatic vaginal infections. In BHI and LAPT culture media, different ionic silver concentrations and different pHs were tested. IASOS exerted a strong antimicrobial activity towards all the pathogens tested in both culture media. The results demonstrated that salts and organic compounds present in the culture media influenced IASOS efficacy only to a moderate extent. Whereas comparable MBCs (Minimal Bactericidal Concentrations were observed for G. vaginalis (10 mg/L Ag+, E. coli and E. aerogenes (25 mg/L Ag+ in both media, higher MBCs were found for S. aureus and S. agalactiae in LAPT cultures (50 mg/L Ag+ versus 25 mg/L Ag+. No minimal concentration totally inhibiting the growth of C. albicans was found. Nevertheless, in both media at the highest ionic silver concentrations (50-200 mg/L Ag+, a significant 34-52% drop in Candida growth was observed. pH differently affected the antimicrobial properties of IASOS against bacteria or yeasts; however, a stronger antimicrobial activity at pH higher than the physiological pH was generally observed. It can be therefore concluded that IASOS exerts a bactericidal action against all the tested bacteria and a clear fungistatic action against C. albicans. The antimicrobial activity of the whole vaginal gel SilSOS Femme further confirmed the antimicrobial activity of IASOS. Overall, our findings support IASOS as a valid active ingredient into a vaginal gel.

  19. Effect of aripiprazole on mismatch negativity (MMN in schizophrenia.

    Directory of Open Access Journals (Sweden)

    Zhenhe Zhou

    Full Text Available BACKGROUND: Cognitive deficits are considered core symptoms of the schizophrenia. Cognitive function has been found to be a better predictor of functional outcome than symptom levels. Changed mismatch negativity (MMN reflects abnormalities of early auditory processing in schizophrenia. Up to now, no studies for the effects of aripiprazole on MMN in schizophrenia have been reported. METHODOLOGY/PRINCIPAL FINDINGS: Subjects included 26 patients with schizophrenia, and 26 controls. Psychopathology was rated in patients with the Positive and Negative Syndrome Scale (PANSS at baseline, after 4- and 8-week treatments with aripiprazole. Auditory stimuli for ERP consisted of 100 millisecond/1000 Hz standards, intermixed with 100 millisecond/1500 Hz frequency deviants and 250 millisecond/1000 Hz duration deviants. EEG was recorded at Fz. BESA 5.1.8 was used to perform data analysis. MMN waveforms were obtained by subtracting waveforms elicited by standards from waveforms elicited by frequency- or duration-deviant stimuli. Aripiprazole decreased all PANSS. Patients showed smaller mean amplitudes of frequency and duration MMN at baseline than did controls. A repeated measure ANOVA with sessions (i.e., baseline, 4- and 8-week treatments and MMN type (frequency vs. duration as within-subject factors revealed no significant MMN type or MMN type × session main effect for MMN amplitudes. Session main effect was significant. LSD tests demonstrated significant differences between MMN amplitudes at 8 weeks and those at both baseline and 4 weeks. There was significant negative correlation between changes in amplitudes of frequency and duration MMN and changes in PANSS total scores at baseline and follow-up periods. CONCLUSIONS: Aripiprazole improved the amplitudes of MMN. MMN offers objective evidence that treatment with the aripiprazole may ameliorate preattentive deficits in schizophrenia.

  20. Active Ingredient Analysis of Tibet Cultivated Ganoderma Lucidum%西藏人工栽培灵芝活性成分分析

    Institute of Scientific and Technical Information of China (English)

    饶恩铭; 刘涛; 次仁德吉; 宋博文

    2015-01-01

    In order to understand the main active ingredient in Tibet cultivated Ganoderma Lucidum, this article collected the local cultivated Ganoderma Lucidum as the raw materials, used anthrone-sulfuric acid spectroscopy, spectrophotometry, pre-column derivatization RP-HPLC method to analyze the main active ingredient. The results showed that the contents of Ganoderma lucidum polysaccharides, triterpenoids, amino acids in Tibet cultivated Ganoderma Lucidum were:1.199g/100g, 1.63%, 8.898g/100g. Compared with national coverage, the active ingredient of cultivated Ganoderma Lucidum is richer, and the acid and triterpenoids content is higher than that in other regions.%为了解西藏人工栽培灵芝的主要活性成分,采集当地栽培的灵芝为原材料,分别采用蒽酮-硫酸分光法、紫外分光光度法、柱前衍生化RP-HPLC方法,分析其主要活性成分。结果表明,西藏人工栽培的灵芝中灵芝多糖、三萜类、氨基酸含量依次为:1.199g/100g、1.63%、8.898g/100g,经与国内报道相比较,西藏人工灵芝活性成分比较丰富,氨基酸和三萜类含量高于其他区域。

  1. Neural correlates of delusional infestation responding to aripiprazole monotherapy: a case report

    Directory of Open Access Journals (Sweden)

    Ponson L

    2015-02-01

    Full Text Available Laura Ponson,1,2 Frédéric Andersson,1 Wissam El-Hage1,2 1Université François-Rabelais de Tours, Inserm, Imagerie et Cerveau UMR U930, Tours, France, 2CHRU de Tours, Clinique Psychiatrique Universitaire, Tours, France Background: The pathophysiology and appropriate pharmacological interventions for delusional infestation remain unknown.Case presentation: Here, we report a case of primary delusional infestation successfully treated with aripiprazole. We performed functional magnetic resonance imaging (fMRI to investigate brain structures and functional modifications. Before antipsychotic treatment, pre- versus post-treatment fMRI images revealed a marked increase in brain activation in the supplementary motor area (SMA.Conclusion: Our results highlight the efficacy and safety of aripiprazole in the treatment of delusional infestation and the possible role of SMA dysfunction in delusional infestation. Indeed, our results suggest that psychiatric improvement of delusional infestation is associated with normalization of brain activity, particularly in the SMA. Keywords: supplementary motor area, antipsychotics, fMRI

  2. Development and validation of a high-performance liquid chromatography method using diode array detection for the simultaneous quantification of aripiprazole and dehydro-aripiprazole in human plasma.

    Science.gov (United States)

    Lancelin, Frédérique; Djebrani, Kayssa; Tabaouti, Khalid; Kraoul, Linda; Brovedani, Sophie; Paubel, Pascal; Piketty, Marie-Liesse

    2008-05-01

    A high-performance liquid chromatography method with diode array detection (HPLC-DAD) was developed for quantification of aripiprazole and dehydro-aripiprazole, in human plasma. After a simple liquid-liquid extraction, chromatographic separation was carried out on a C18 reversed-phase column, using an ammonium buffer-acetonitrile mobile phase (40:60, v/v). The total run time was only 7 min at a flow-rate of 1.0 ml/min. The precision values were less than 12% and the accuracy values were ranging from 98 to 113% and the lower limit of quantification was 2 ng/ml for both compounds. Calibration curves were linear over a range of 2-1000 ng/ml. The mean trough plasma concentrations in patients treated with aripiprazole were 157 and 29 ng/ml for aripiprazole and dehydro-aripiprazole, respectively.

  3. The hallucinogenic herb Salvia divinorum and its active ingredient salvinorin A inhibit enteric cholinergic transmission in the guinea-pig ileum.

    Science.gov (United States)

    Capasso, R; Borrelli, F; Capasso, F; Siebert, D J; Stewart, D J; Zjawiony, J K; Izzo, A A

    2006-01-01

    Salvia divinorum is a widespread hallucinogenic herb traditionally employed for divination, as well as a medicament for several disorders including disturbances of gastrointestinal motility. In the present study we evaluated the effect of a standardized extract from the leaves of S. divinorum (SDE) on enteric cholinergic transmission in the guinea-pig ileum. SDE reduced electrically evoked contractions without modifying the contractions elicited by exogenous acetylcholine, thus suggesting a prejunctional site of action. The inhibitory effect of SDE on twitch response was abolished by the opioid receptor antagonist naloxone and by the kappa-opioid antagonist nor-binaltorphimine, but not by naltrindole (a delta-opioid receptor antagonist), CTOP (a mu-opioid receptor antagonist), thioperamide (a H(3) receptor antagonist), yohimbine (an alpha(2)-receptor antagonist), methysergide (a 5-hydroxytryptamine receptor antagonist), N(G)-nitro-L-arginine methyl ester (an inhibitor of NO synthase) or apamin (a blocker of Ca(2+)-activated K(+) channels). Salvinorin A, the main active ingredient of S. divinorum, inhibited in a nor-binaltorphimine- and naloxone-sensitive manner electrically induced contractions. It is concluded that SDE depressed enteric cholinergic transmission likely through activation of kappa-opioid receptors and this may provide the pharmacological basis underlying its traditional antidiarrhoeal use. Salvinorin A might be the chemical ingredient responsible for this activity.

  4. Analytical method (HPLC), validation used for identification and assay of the pharmaceutical active ingredient, Tylosin tartrate for veterinary use and its finite product Tilodem 50, hydrosoluble powder

    OpenAIRE

    2010-01-01

    In SC DELOS IMPEX ’96 SRL the quality of the active pharmaceutical ingredient (API) for the finite product Tilodem 50 - hydrosoluble powder was acomkplished in the respect of last European Pharmacopoeia.The method for analysis used in this purpose was the compendial method „Tylosin tartrate for veterinary use” in EurPh. in vigour edition and represent a variant developed and validation „in house”.The parameters which was included in the methodology validation for chromatographic method are th...

  5. Use of aripiprazole in clozapine induced enuresis: report of two cases.

    Science.gov (United States)

    Lee, Myung-Ji; Kim, Chul-Eung

    2010-02-01

    This report describes the efficacy of combined use of aripiprazole in the treatment of a patient with clozapine induced enuresis. Aripiprazole acts as a potential dopamine partial agonist and the dopamine blockade in the basal ganglia might be one of the causes of urinary incontinence and enuresis. We speculate that aripiprazole functioned as a D2 agonist in hypodopaminergic state of basal ganglia caused by clozapine and maintained dopamine level that would improve enuresis ultimately.

  6. Supersaturation of Calcipotriene and Betamethasone Dipropionate in a Novel Aerosol Foam Formulation for Topical Treatment of Psoriasis Provides Enhanced Bioavailability of the Active Ingredients.

    Science.gov (United States)

    Lind, Marianne; Nielsen, Kim Troensegaard; Schefe, Line Hollesen; Nørremark, Kasper; Eriksson, André Huss; Norsgaard, Hanne; Pedersen, Brian Thoning; Petersson, Karsten

    2016-09-01

    Previous studies have demonstrated the superior efficacy of a novel aerosol foam formulation of fixed combination calcipotriene 0.005% (Cal) and betamethasone dipropionate 0.064% (BD), compared with the ointment formulation. The aim of this study is to ascertain whether enhanced bioavailability of the active ingredients due to supersaturation and/or occlusive properties can explain the observed greater clinical efficacy. Solubility and evaporation experiments were conducted to examine the abilities of Cal/BD aerosol foam ingredients to create a supersaturated environment. Optical microscopy, Raman imaging and X-ray powder diffraction were used to examine the physical state of Cal and BD in the formulations after application, and determine whether a supersaturated state remained stable for clinically relevant time periods. In vitro skin penetration and ex vivo biomarker assays were conducted to compare the skin penetration and bioavailability of Cal and BD from the aerosol foam and ointment formulations, respectively. Occlusive properties were examined via transepidermal water loss. Solubility studies showed that Cal and BD solubility increased with increasing dimethyl ether (DME) content. Both active ingredients are completely dissolved in the final aerosol foam formulation. DME rapidly evaporates after spraying, and the amount was reduced to 0.5% of the initial amount after 2 min. This led to the formation of a supersaturated environment, where Cal and BD crystals were absent for at least 26 h after application. Cal/BD aerosol foam had significantly greater in vitro skin penetration and had increased bioavailability compared with Cal/BD ointment. Both formulations effectively occluded the skin. A stable supersaturated solution of Cal/BD in the aerosol foam leads to increased bioavailability and explains the improved clinical effect when compared to the Cal/BD ointment. The studies included in the paper are all conducted by LEO Pharma A/S or CROs on behalf of LEO

  7. Authorization and Toxicity of Veterinary Drugs and Plant Protection Products: Residues of the Active Ingredients in Food and Feed and Toxicity Problems Related to Adjuvants

    Directory of Open Access Journals (Sweden)

    Szandra Klátyik

    2017-09-01

    Full Text Available Chemical substances applied in animal husbandry or veterinary medicine and in crop protection represent substantial environmental loads, and their residues occur in food and feed products. Product approval is governed differently in these two sectors in the European Union (EU, and the occurrence of veterinary drug (VD and pesticide residues indicated by contamination notification cases in the Rapid Alert System for Food and Feed of the EU also show characteristic differences. While the initial high numbers of VD residues reported in 2002 were successfully suppressed to less than 100 cases annually by 2006 and on, the number of notification cases for pesticide residues showed a gradual increase from a low (approximately 50 cases annually initial level until 2005 to more than 250 cases annually after 2009, with a halt occurring only in 2016. Main notifiers of VD residues include Germany, Belgium, the UK, and Italy (63, 59, 42, and 31 notifications announced, respectively, and main consigning countries of non-compliances are Vietnam, India, China, and Brazil (88, 50, 34, and 23 notifications, respectively. Thus, countries of South and Southeast Asia are considered a vulnerable point with regard to VD residues entering the EU market. Unintended side effects of VDs and plant protection products may be caused not only by the active ingredients but also by various additives in these preparations. Adjuvants (e.g., surfactants and other co-formulants used in therapeutic agents and feed additives, as well as in pesticide formulations have long been considered as inactive ingredients in the aspects of the required main biological effect of the pharmaceutical or pesticide, and in turn, legal regulations of the approval and marketing of these additives specified significantly less stringent risk assessment requirements, than those specified for the active ingredients. However, numerous studies have shown additive, synergistic, or antagonistic side effects

  8. Authorization and Toxicity of Veterinary Drugs and Plant Protection Products: Residues of the Active Ingredients in Food and Feed and Toxicity Problems Related to Adjuvants

    Science.gov (United States)

    Klátyik, Szandra; Bohus, Péter; Darvas, Béla; Székács, András

    2017-01-01

    Chemical substances applied in animal husbandry or veterinary medicine and in crop protection represent substantial environmental loads, and their residues occur in food and feed products. Product approval is governed differently in these two sectors in the European Union (EU), and the occurrence of veterinary drug (VD) and pesticide residues indicated by contamination notification cases in the Rapid Alert System for Food and Feed of the EU also show characteristic differences. While the initial high numbers of VD residues reported in 2002 were successfully suppressed to less than 100 cases annually by 2006 and on, the number of notification cases for pesticide residues showed a gradual increase from a low (approximately 50 cases annually) initial level until 2005 to more than 250 cases annually after 2009, with a halt occurring only in 2016. Main notifiers of VD residues include Germany, Belgium, the UK, and Italy (63, 59, 42, and 31 notifications announced, respectively), and main consigning countries of non-compliances are Vietnam, India, China, and Brazil (88, 50, 34, and 23 notifications, respectively). Thus, countries of South and Southeast Asia are considered a vulnerable point with regard to VD residues entering the EU market. Unintended side effects of VDs and plant protection products may be caused not only by the active ingredients but also by various additives in these preparations. Adjuvants (e.g., surfactants) and other co-formulants used in therapeutic agents and feed additives, as well as in pesticide formulations have long been considered as inactive ingredients in the aspects of the required main biological effect of the pharmaceutical or pesticide, and in turn, legal regulations of the approval and marketing of these additives specified significantly less stringent risk assessment requirements, than those specified for the active ingredients. However, numerous studies have shown additive, synergistic, or antagonistic side effects between the

  9. Quality control of tuirejieduling granules using high-performance liquid chromatography fingerprint method and simultaneous determination of four main active ingredients

    Directory of Open Access Journals (Sweden)

    Aixia Yang

    2013-01-01

    Full Text Available Background: The Tuirejieduling granule is a compound preparation made from four kinds of Chinese medicines. It is effective for anti-inflammation, antivirus, defervescence and anti-bacterium; however, its quality control standards have remained unknown. Objective: To establish a simple and accurate fingerprint method for quality control of the Tuirejieduling granule. Materials and Methods: The methanol extract of the Tuirejieduling granule was used for the fingerprint analysis and the four selected active ingredients (epigoitrin, phillyrin, saikosaponin A and glycyrrhetinic acid in the extract were determined. The fingerprint method was performed on an Amethyst C18-P chromatography column by gradient elution with acetonitrile and aqueous phase (containing 0.5% H 3 PO 4 (v/v, pH 3.0. Results: Under the optimal chromatographic condition, twenty peaks were chosen as fingerprint peaks of the Tuirejieduling granules extractions. The similarities of 10 batches of Tuirejieduling granule was more than 0.99. This indicates that the different batches of Tuirejieduling granules were under the consistent quality control. Good linear behaviors over the investigated concentration ranges were obtained with the values of R2 higher than 0.99 for four studied active ingredients. The recoveries for spiked samples were in the range of 96.2-105.5%. The developed method was successfully applied to determine the contents of active constituents in different batches of Tuirejieduling granule. Conclusion: The HPLC fingerprint was proved to be a reliable method for the quality control of Tuirejieduling granule.

  10. Profile of aripiprazole in the treatment of bipolar disorder in children and adolescents

    National Research Council Canada - National Science Library

    Kirino, Eiji

    2014-01-01

    .... Here, we review the effectiveness of aripiprazole for bipolar disorder in children and adolescents, with discussion of this drug's unique pharmacological profile and various clinical study outcomes...

  11. IngredientApp

    OpenAIRE

    Sandín Estevan, Alejandro

    2014-01-01

    Aquest document descriu una aplicació per a dispositius Android. L'aplicació IngredientApp és un intent d'autocontrolar el que comprem, fem servir o mengem. Es tracta d'una aplicació a la qual s'hi defineixen unes preferències sobre els ingredients dels productes i, fent servir un smartphone, sense haver de mirar la llista d'ingredients, l'aplicatiu li advertirà si el producte compleix els seus criteris. Este documento describe una aplicación para dispositivos Android. La aplicación Ingred...

  12. Analytical method (HPLC, validation used for identification and assay of the pharmaceutical active ingredient, Tylosin tartrate for veterinary use and its finite product Tilodem 50, hydrosoluble powder

    Directory of Open Access Journals (Sweden)

    Maria Neagu

    2010-12-01

    Full Text Available In SC DELOS IMPEX ’96 SRL the quality of the active pharmaceutical ingredient (API for the finite product Tilodem 50 - hydrosoluble powder was acomkplished in the respect of last European Pharmacopoeia.The method for analysis used in this purpose was the compendial method „Tylosin tartrate for veterinary use” in EurPh. in vigour edition and represent a variant developed and validation „in house”.The parameters which was included in the methodology validation for chromatographic method are the followings: Selectivity, Linearity, Linearity range, Detection and Quantification limits, Precision, Repeatability (intra day, Inter-Day Reproductibility, Accuracy, Robustness, Solutions’ stability and System suitability. According to the European Pharmacopoeia, the active pharmaceutical ingredient is consistent, in terms of quality, if it contains Tylosin A - minimum 80% and the amount of Tylosin A, B, C, D, at minimum 95%. Identification and determination of each component separately (Tylosin A, B, C, D is possible by chromatographic separation-HPLC. Validation of analytical methods is presented below.

  13. Identification of Polymorphic Forms of Active Pharmaceutical Ingredient in Low-Concentration Dry Powder Formulations by Synchrotron X-Ray Powder Diffraction.

    Science.gov (United States)

    Egusa, Kenji; Okazaki, Fumiaki; Schiewe, Joerg; Werthmann, Ulrike; Wolkenhauer, Markus

    2017-09-13

    The identification of different (pseudo) polymorphs of an active pharmaceutical ingredient in dry powder formulations is of importance during development and entire product lifecycle, e.g., quality control. Whereas determination of polymorphic differences of pure substances is rather easy, in dry powder formulations, it is generally difficult and the difficulties increase particularly, if the substance of interest is present only in low concentrations in the formulation. Such a formulation is Spiriva(®) inhalation powder (Boehringer Ingelheim), which contains only 0.4 w/w% of the active pharmaceutical ingredient tiotropium bromide monohydrate in a matrix of α-lactose monohydrate as excipient. In this study, identification of 0.4 w/w% tiotropium bromide in the dry powder formulation was examined by X-ray powder diffraction (XRPD) using a synchrotron radiation source and the results were compared with the conventional laboratory XRPD measurements. The detection limit of tiotropium bromide by the laboratory XRPD was around 2-5 w/w%, and hence, detection of 0.4 w/w% tiotropium bromide was impossible. The synchrotron XRPD was capable to detect significantly lower level of tiotropium bromide by at least an order of magnitude. Four different polymorphic forms of tiotropium bromide present at 0.4 w/w% concentration in lactose powder blends were unambiguously identified by the synchrotron XRPD method.

  14. The effect of microcrystalline cellulose crystallinity on the hydrophilic property of tablets and the hydrolysis of acetylsalicylic acid as active pharmaceutical ingredient inside tablets.

    Science.gov (United States)

    Awa, Kimie; Shinzawa, Hideyuki; Ozaki, Yukihiro

    2015-08-01

    The crystal structures of active pharmaceutical ingredients and excipients should be strictly controlled because they influence pharmaceutical properties of products which cause the change in the quality or the bioavailability of the products. In this study, we investigated the effects of microcrystalline cellulose (MCC) crystallinity on the hydrophilic properties of tablets and the hydrolysis of active pharmaceutical ingredient, acetylsalicylic acid (ASA), inside tablets by using tablets containing 20% MCC as an excipient. Different levels of grinding were applied to MCC prior to tablet formulation, to intentionally cause structural variation in the MCC. The water penetration and moisture absorbability of the tablets increased with decreasing the crystallinity of MCC through higher level of grinding. More importantly, the hydrolysis of ASA inside tablets was also accelerated. These results indicate that the crystallinity of MCC has crucial effects on the pharmaceutical properties of tablets even when the tablets contain a relatively small amount of MCC. Therefore, controlling the crystal structure of excipients is important for controlling product qualities.

  15. Hydrolysate from a mixture of legume flours with antifungal activity as an ingredient for prolonging the shelf-life of wheat bread.

    Science.gov (United States)

    Rizzello, Carlo Giuseppe; Verni, Michela; Bordignon, Stefano; Gramaglia, Valerio; Gobbetti, Marco

    2017-06-01

    Aiming at identifying antifungal compounds from plant matrices to be used as ingredients in the bakery industry, a water/salt-soluble extract (WSE) was produced from a legume enzyme hydrolysate, consisting of a mixture of pea, lentil, and faba bean flours, and assayed towards Penicillium roqueforti DPPMAF1. Agar diffusion assays allowed the selection of the optimal processing conditions for hydrolysis. As shown by hyphal radial growth rate, the inhibition was observed towards several fungi, including Aspergillus parasiticus CBS971.97, Penicillium carneum CBS 112297, Penicillium paneum CBS 101032, Penicillium polonicum 112490. A multi-step purification was carried out to identify the active compounds. The antifungal activity was attributed to native proteins (nsLTP, ubiquitin, lectin alpha-1 chain, wound-induced basic protein, defensin-1, defensin-2) and a mixture of peptides, which were released during hydrolysis. Nine peptides were purified and identified as sequences encrypted in legume vicilins, lectins and chitinases. WSE was used as ingredient for making bread under pilot plant conditions. Chemical, structural and sensory characterization of bread showed the lack of significant changes compared to control. The bread made with the legume hydrolysate had a longer shelf-life than that of the control. Copyright © 2016 Elsevier Ltd. All rights reserved.

  16. Antifungal activity of food additives in vitro and as ingredients of hydroxypropyl methylcellulose-lipid edible coatings against Botrytis cinerea and Alternaria alternata on cherry tomato fruit.

    Science.gov (United States)

    Fagundes, Cristiane; Pérez-Gago, María B; Monteiro, Alcilene R; Palou, Lluís

    2013-09-16

    The antifungal activity of food additives or 'generally recognized as safe' (GRAS) compounds was tested in vitro against Botrytis cinerea and Alternaria alternata. Radial mycelial growth of each pathogen was measured in PDA Petri dishes amended with food preservatives at 0.2, 1.0, or 2.0% (v/v) after 3, 5, and 7 days of incubation at 25 °C. Selected additives and concentrations were tested as antifungal ingredients of hydroxypropyl methylcellulose (HPMC)-lipid edible coatings. The curative activity of stable coatings was tested in in vivo experiments. Cherry tomatoes were artificially inoculated with the pathogens, coated by immersion about 24 h later, and incubated at 20 °C and 90% RH. Disease incidence and severity (lesion diameter) were determined after 6, 10, and 15 days of incubation and the 'area under the disease progress stairs' (AUDPS) was calculated. In general, HPMC-lipid antifungal coatings controlled black spot caused by A. alternata more effectively than gray mold caused by B. cinerea. Overall, the best results for reduction of gray mold on cherry tomato fruit were obtained with coatings containing 2.0% of potassium carbonate, ammonium phosphate, potassium bicarbonate, or ammonium carbonate, while 2.0% sodium methylparaben, sodium ethylparaben, and sodium propylparaben were the best ingredients for coatings against black rot.

  17. Active Ingredients of Epimedii Folium and Ligustri Lucidi Fructus Balanced GR/HSP90 to Improve the Sensitivity of Asthmatic Rats to Budesonide

    Directory of Open Access Journals (Sweden)

    Xiufeng Tang

    2017-01-01

    Full Text Available This study aimed to investigate the possible molecular mechanisms of active ingredients of Epimedii Folium (EF and Ligustri Lucidi Fructus (LLF combined with Budesonide (Bun in asthmatic rats. Rats were divided into 5 groups, including normal group, asthma model group, Bun group, group of active ingredients of EL and LLF (EL, and group of coadministration of Bun with EL (Bun&EL. The asthmatic model was prepared by ovalbumin sensitizing and challenging. Lymphocyte apoptosis, GR protein and binding, and the protein and mRNA of GRα, GRβ, and HSP90 were tested. The results showed that Bun&EL ① markedly increased lymphocyte apoptosis, GR and HSP90 protein, and GR binding in BALF and ② enhanced the expressions of GRα and HSP90 and the ratio of GRα to GRβ or to HSP90 both in protein and in mRNA levels in lung, ③ while decrease occurred in GRβ mRNA and the mRNA ratio of GRβ to HSP90 compared with asthma or Bun group. Moreover, there was a significant correlation between GRα and GRβ in protein level, or between GRα and HSP90 both in protein and in mRNA levels. EL may effectively enhance the sensitivity of asthmatic rats to Bun via balancing GR/HSP90. And these findings will be beneficial for the treatment of asthma in the future.

  18. Ingredients: where pet food starts.

    Science.gov (United States)

    Thompson, Angele

    2008-08-01

    Every clinician is asked "What should I feed my pet?" Understanding the ingredients in pet food is an important part of making the best recommendation. Pet food can be as simple as one ingredient or as complicated as containing more than 60 ingredients. Pet food and its ingredients are regulated by the Food and Drug Administration and state feed officials. Part of that regulation is the review and definition of ingredients. Existing ingredients change and new ingredients become available so the need for ingredient definitions grows. Ingredients for product formulations are chosen based on their nutrient content, digestibility, palatability, functionality, availability, and cost. As an example, a typical, nutritionally complete dry dog food with 42 ingredients is examined and the ingredients are discussed here. Safe, healthy pet food starts with safe ingredients sourced from well-monitored suppliers. The ultimate goal of both veterinarians and pet food manufacturers is the same--long healthy lives for dogs and cats.

  19. Switching to aripiprazole for the treatment of residual mutism resulted in distinct clinical courses in two catatonic schizophrenia cases

    OpenAIRE

    Katsumasa Muneoka; Nobuhisa Kanahara; Shou Kimura

    2017-01-01

    Objectives: The efficacy of a partial agonist for the dopamine D2 receptor, aripiprazole, for catatonia in schizophrenia has been reported. Methods: We report distinct clinical courses in challenging aripiprazole to treat residual mutism after severe catatonic symptoms improved. Results: In the first case, mutism was successfully treated when the patient was switched from olanzapine to aripiprazole. In contract, switching to aripiprazole from risperidone aggravated auditory hallucinations in ...

  20. Dietary Supplement Ingredient Database

    Science.gov (United States)

    ... and US Department of Agriculture Dietary Supplement Ingredient Database Toggle navigation Menu Home About DSID Mission Current ... values can be saved to build a small database or add to an existing database for national, ...

  1. What are the active ingredients in cognitive and behavioral psychotherapy for anxious and depressed children? A meta-analytic review.

    Science.gov (United States)

    Spielmans, Glen I; Pasek, Leigh F; McFall, Joseph P

    2007-06-01

    Prior meta-analytic reviews have indicated that cognitive and behavioral treatments are efficacious in treating child and adolescent depression and anxiety. Further, a meta-analysis has suggested that behavioral treatments are superior to nonbehavioral treatments for treating anxiety and depression in youth. However, the prior meta-analysis did not examine direct comparisons between cognitive and behavioral treatments (CBT) and non-CBT treatments, leaving open the possibility that their results were artifactual. The present meta-analysis aggregated results of studies in which CBT treatments were compared with either other bona fide treatments (including other CBT therapies) or non-bona fide therapies. The heterogeneity of the distribution of differences between bona fide treatments as well as a comparison of full (e.g. CBT+Parent training) versus component treatments (e.g., CBT only) were examined. The results indicated that: (a) CBT was more efficacious than non-bona fide therapies; (b) CBT was no more efficacious than bona fide non-CBT treatments (c) the differences between bona fide treatments were homogenously distributed around zero; and (d) full CBT treatments offered no significant benefit over their components. The results strongly suggest that the theoretically purported critical ingredients of CBT are not specifically ameliorative for child and adolescent depression and anxiety.

  2. Digestible energy requirement for females of Rhamdia quelen on reproductive activity fed with ration based on vegetal ingredients

    Directory of Open Access Journals (Sweden)

    Robie A Bombardelli

    2015-07-01

    Full Text Available The present experiment was carried out to evaluate the growth and reproductive parameters of Rhamdia quelen females fed with pelleted ration containing different levels of digestible energy, and to evaluate the vigor of their offspring. The breeders were placed in tanks under conditions of photoperiod and natural temperature. The fishes were fed for 255 days with isoproteic rations pelleted containing 35% of crude protein (CP and five levels of the digestible energy (DE (2700, 2950, 3200, 3450, 3700 kcal kg-1. The fishes were distributed in a randomized experimental design compounded by five treatments and three repetitions. A 16-m² tank containing six females and three males was considered as one experimental unit. The weight and weight gain was evaluated. During the reproductive season the females were induced to breeding by hormonal manipulation and were evaluated the percentage of spawning females, the total fecundity, relative fecundity (number of oocytes per gram of spawning females, the fertilization ratio, the time to hatching and the vigor of larvae. The growth and reproductive parameters were not influenced (P > 0.05 by the increasing levels of digestible energy of the rations. The feeding of R. quelen females in breeding fit can be carried out with 2700 kcal kg-1 pelletized ration based on vegetal ingredients, without damage to reproductive performance.

  3. Aripiprazole-induced writer’s cramp: a case report

    Directory of Open Access Journals (Sweden)

    Priyajyoti Chakma

    2016-07-01

    Full Text Available Dystonia is a movement disorder, which causes sustained muscle contractions, twisting movements, and abnormal postures. Writer’s cramp is the most commonly identified tasks-specific focal dystonia of writing, characterised by abnormal muscle spasm of hand and arm. Even in the tenth revision of the International Statistical Classification of Diseases and Related Health Problems (ICD-10, writer’s cramp is classified under idiopathic nonfamilial dystonias. Our case was a 20 years, Hindu, unmarried, literate of middle socioeconomic status, from urban part of Tripura. He presented with history of difficulty to write because of a stiffening of his right hand and also he noticed that prolonged period of writing caused cramping pain. He was a diagnosed case of paranoid schizophrenia (F20.0 as per ICD-10 for last three years and was on tablet aripiprazole. Diagnosis of writer’s cramp was made which developed after six months of treatment with aripiprazole 15 mg.

  4. Characterization of the size distribution and aggregation of virus-like nanoparticles used as active ingredients of the HeberNasvac therapeutic vaccine against chronic hepatitis B

    Science.gov (United States)

    Lopez, Matilde; Rodriguez, Elias Nelson; Lobaina, Yadira; Musacchio, Alexis; Falcon, Viviana; Guillen, Gerardo; Aguilar, Julio C.

    2017-06-01

    The use of virus-like particles (VLPs) as antigens constitutes a well established strategy in preventive vaccination. These non-infective particles have a composition, size, and structure favoring their interaction and processing by the immune system. Recombinant viral nucleocapsids encapsulating bacterial nucleic acids result in potent Th1-driving immunogens. Several antigens have been coadministered with VLPs or conjugated to them to further increase their immunogenicity. In the present work we characterize the size distribution of two different recombinant VLPs obtained as components of HeberNasvac, a novel therapeutic vaccine recently registered to treat chronic hepatitis B. The vaccine ingredients, hepatitis B virus surface and nucleocapsid antigens (HBsAg and HBcAg, respectively) and the vaccine formulation, were evaluated using dynamic light scattering (DLS), transmission electron microscopy (TEM) and light obscuration technology. The results demonstrate that both antigens are nanoparticles with sizes ranging between 20-30 nm, in line with reports in the literature. In addition, DLS studies evidenced the capacity of both antigens to form homologous and heterologous aggregates, both as active ingredients as well as being part of the final product. The evaluation of subvisible particles in HeberNasvac formulation fulfills the requirements in terms of quantity and size established for parenteral pharmaceutical compositions. Invited talk at 8th Int. Workshop on Advanced Materials Science and Nanotechnology (IWAMSN2016) (Ha Long City, Vietnam, 8-12 November 2016)

  5. Pharmacokinetics and tissue distribution of five active ingredients of Eucommiae cortex in normal and ovariectomized mice by UHPLC-MS/MS.

    Science.gov (United States)

    An, Jing; Hu, Fangdi; Wang, Changhong; Zhang, Zijia; Yang, Li; Wang, Zhengtao

    2016-09-01

    1. Pinoresinol di-O-β-d-glucopyranoside (PDG), geniposide (GE), geniposidic acid (GA), aucubin (AN) and chlorogenic acid (CA) are the representative active ingredients in Eucommiae cortex (EC), which may be estrogenic. 2. The ultra high-performance liquid chromatography/tandem mass spectrometry (UHPLC-MS/MS) method for simultaneous determination of the five ingredients showed good linearity, low limits of quantification and high extraction recoveries, as well as acceptable precision, accuracy and stability in mice plasma and tissue samples (liver, spleen, kidney and uterus). It was successfully applied to the comparative study on pharmacokinetics and tissue distribution of PDG, GE, GA, AN and CA between normal and ovariectomized (OVX) mice. 3. The results indicated that except CA, the plasma and tissue concentrations of PDG, GE, GA in OVX mice were all greater than those in normal mice. AN could only be detected in the plasma and liver homogenate of normal mice, which was poorly absorbed in OVX mice and low in other measured tissues. PDG, GE and GA seem to be better absorbed in OVX mice than in normal mice proved by the remarkable increased value of AUC0-∞ and Cmax. It is beneficial that PDG, GE, GA have better plasma absorption and tissue distribution in pathological state.

  6. Successful treatment of a prolactinoma with the antipsychotic drug aripiprazole

    Directory of Open Access Journals (Sweden)

    Ilse C A Bakker

    2016-06-01

    Full Text Available In this report, we describe a female patient with both prolactinoma and psychotic disorder who was successfully treated with aripiprazole, a partial dopamine 2 receptor agonist. During the follow-up of more than 10 years, her psychotic symptoms improved considerably, prolactin levels normalised and the size of the prolactinoma decreased. This observation may be of clinical relevance in similar patients who often are difficult to treat with the regular dopaminergic drugs.

  7. Aripiprazole for acute mania in an elderly person

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    Balaji Bharadwaj

    2011-01-01

    Full Text Available New-onset bipolar disorder is rare in the elderly. Symptom profile is similar to that in young adults but the elderly are more likely to have neurological co-morbidities. There are no case reports of elderly mania being treated with aripiprazole, an atypical antipsychotic. A 78-year-old gentleman presented to us with symptoms suggestive of mania of 1 month′s duration. He had similar history 3 years ago and a family history of postpartum psychosis in his mother. There were no neurological signs on examination and work-up for an organic etiology was negative except for age-related cerebral atrophy. He improved with aripiprazole and tolerated the medications well. The use of psychotropic medications in the elderly is associated with side-effects of sedation, increased cardiovascular risk, and greater risk of extra-pyramidal side-effects. The use of partial dopaminergic antagonists like aripiprazole may be useful in the balancing of effects and side-effects.

  8. Augmentation treatment in major depressive disorder: focus on aripiprazole

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    J Craig Nelson

    2008-08-01

    Full Text Available J Craig Nelson1, Andrei Pikalov2, Robert M Berman31University of California San Francisco, San Francisco, California, USA; 2Otsuka Pharmaceutical Inc., Rockville, MD, USA; 3Bristol-Myers Squibb, Wallingford, CT, USAAbstract: Major depressive disorder (MDD is a disabling psychiatric condition for which effective treatment remains an outstanding need. Antidepressants are currently the mainstay of treatment for depression; however, almost two-thirds of patients will fail to achieve remission with initial treatment. As a result, a range of augmentation and combination strategies have been used in order to improve outcomes for patients. Despite the popularity of these approaches, limited data from double-blind, randomized, placebo-controlled studies are available to allow clinicians to determine which are the most effective augmentation options or which patients are most likely to respond to which options. Recently, evidence has shown that adjunctive therapy with atypical antipsychotics has the potential for beneficial antidepressant effects in the absence of psychotic symptoms. In particular, aripiprazole has shown efficacy as an augmentation option with standard antidepressant therapy in two, large, randomized, double-blind studies. Based on these efficacy and safety data, aripiprazole was recently approved by the FDA as adjunctive therapy for MDD. The availability of this new treatment option should allow more patients with MDD to achieve remission and, ultimately, long-term, successful outcomes.Keywords: major depression, antipsychotic, mood disorder, aripiprazole

  9. Aripiprazole-associated tic in a schizophrenia patient

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    Guo X

    2015-03-01

    Full Text Available Xieli Guo,1,2,* Dali Lu,3,* Yugang Jiang1 1Department of Neurosurgery, Second Xiangya Hospital of Central South University, Changsha, Hunan, People’s Republic of China; 2Department of Neurosurgery, Jinjiang Hospital of Quanzhou Medical College, Jinjiang, Fujian, People’s Republic of China; 3Department of Psychiatry, Xiamen Xianyue Hospital, Xiamen, Fujian, People’s Republic of China *These authors contributed equally to this work Abstract: Tic disorder, characterized by the presence of both motor and vocal tics is common in adolescents and adults. Antipsychotics including typical antipsychotics and atypical antipsychotics are generally recognized by experts as the most effective pharmacological treatment for tics. However, previous studies suggest that tic-like symptoms might manifest during treatment with atypical antipsychotics such as clo­zapine, quetiapine, but not aripiprazole. We present the first case, to our knowledge, of an adult schizophrenia patient who developed tics during treatment with aripiprazole. Keywords: aripiprazole, antipsychotics, tic, schizophrenia, side effect

  10. Antipsychotic treatments for the elderly: efficacy and safety of aripiprazole

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    Izchak Kohen

    2010-03-01

    Full Text Available Izchak Kohen1, Paula E Lester2, Sum Lam31Division of Geriatric Psychiatry, Zucker-Hillside Hospital, Glen Oaks, NY, USA; 2Division of Geriatric Medicine, Winthrop University Hospital, Mineola, NY, USA; 3Division of Pharmacy and Geriatrics, St. John’s University College of Pharmacy and Allied Health Professions, Queens, NY, USAAbstract: Delusions, hallucinations and other psychotic symptoms can accompany a number of conditions in late life. As such, elderly patients are commonly prescribed antipsychotic medications for the treatment of psychosis in both acute and chronic conditions. Those conditions include schizophrenia, bipolar disorder, depression and dementia. Elderly patients are at an increased risk of adverse events from antipsychotic medications because of age-related pharmacodynamic and pharmacokinetic changes as well as polypharmacy. Drug selection should be individualized to the patient’s previous history of antipsychotic use, current medical conditions, potential drug interactions, and potential side effects of the antipsychotic. Specifically, metabolic side effects should be closely monitored in this population. This paper provides a review of aripiprazole, a newer second generation antipsychotic agent, for its use in a variety of psychiatric disorders in the elderly including schizophrenia, bipolar disorder, dementia, Parkinson’s disease and depression. We will review the pharmacokinetics and pharmacodynamics of aripiprazole as well as dosing, diagnostic indications, efficacy studies, and tolerability including its metabolic profile. We will also detail patient focused perspectives including quality of life, patient satisfaction and adherence.Keywords: aripiprazole, antipsychotics, elderly, adverse drug reaction

  11. Qualitative Analysis of Iranian Crack to Determine the Active Ingredient in Committing Crime in order to Determine Criminal Punishment

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    Ali Hassan Rahmani

    2016-12-01

    Full Text Available Crime (the basis of criminal law is the behavior that intentionallyleadsto violation of legal orders and one of the things that hinder the realization of criminal liability is the condition called insanity. People lacking the healthy will, or unaware of the essence of the consequences their acts if they commit crimes they are not addressed in the law and do not have criminal responsibility.In a cross sectional study in Khuzestan forensic toxicology lab after 61 TLCsamplesof crack street, drug recognition tests was doneby HPLC and GC / MS. Examination of data (V22 SPSS (p value <0.05:% 93/4of crack samples were containing morphine,% 83/6 with caffeine, noscapine or dextromethorphan,% 27/9 heroin and codeine,% 37/7 six mono-acetylphloroglucinol morphine,% 34/4 acetyl codeine,% 13/1 narceine and acetaminophen, % 16/4 diazepam and% 9/8 chloramphenicol and other components of methyl amphetamines, diphenhydramine, lidocaine, thebaine, amoxicillin, amitriptyline and nortriptyline % 6/6 of samples were a mixture of methyl amphetamine - diphenhydramine and acetaminophen, it was a special type of Iraniancrack, due to the existence of amphetamines play a major role in dementia and mental illness like schizophrenia.Iraniancrack is not only different from a real crack (cocaine, but differs in the types, number and amount of additives drug ,Opioid and diluent. Crack has different amount of effective substances on the central nervous system pharmacological and non-pharmacological and psychedelic properties.Different Clinical manifestations like dementia and lack of determinationthat leads to crime.As a result, the need to determine the ingredients in the crack used in the examination of crime and helpingthe criminal justice system in determining the penalty is definite.

  12. 抗心律失常天然活性成分的研究进展%Research progress of antiarrhythmic natural active ingredients

    Institute of Scientific and Technical Information of China (English)

    方永煌; 岑柏宏; 陈瑞晗; 曹静桦; 黄国杰; 梁燕玲; 董艳芬

    2015-01-01

    Arrhythmias are common in the field of cardiovascular disease. In March 2013, World Health Organization reported that, in 2008 the population who died of cardiovascular disease has been as high as 17.3 million, and by 2030 will increase to 23.3 million. Sudden cardiac death accounts for about 40%-50%, while the majority of sudden cardiac death caused by arrhythmia, so the development of new drugs antiarrhythmic is urgent. In recent years, the development of chemical antiarrhythmic drugs getting into the bottleneck, the value of natural antiarrhythmic drug has gotten the world's attention again. At present, the active ingredient of natural antiarrhythmic drugs mainly are alkaloids, flavonoids, saponins. By a comprehensive analysis of the reported literature, the article generalizes the research progress which is about the active ingredient of natural antiarrhythmic drug in nearly a decade, in order to provide certain basis for further study on the active ingredient of natural drugs.%心律失常是心血管领域的常见病、多发病。2013年3月世界卫生组织报道,2008年死于心脑血管疾病者高达1730万,而到2030年将增至2330万。其中心脏性猝死占40%~50%,而大多数心脏性猝死由心律失常所引发,故抗心律失常新药的研发刻不容缓。近几年化学抗心律药物的研发渐入瓶颈,天然药物抗心律失常的价值重新得到世界的关注。目前天然药物抗心律失常活性成分多为生物碱类、黄酮类、皂苷类。本研究通过综合分析已报道的相关文献,概括近几年抗心律失常的天然药物活性成分研究进展,为天然药物活性成分的进一步研究提供依据。

  13. Cell-based screening identifies the active ingredients from Traditional Chinese Medicine formula Shixiao San as the inhibitors of atherosclerotic endothelial dysfunction.

    Directory of Open Access Journals (Sweden)

    Xiaofan Wang

    Full Text Available In this study, we performed a phenotypic screening in human endothelial cells exposed to oxidized low density lipoprotein (an in vitro model of atherosclerotic endothelial dysfunction to identify the effective compounds in Shixiao San. After investigating the suitability and reliability of the cell-based screening method using atorvastatin as the positive control drug, this method was applied in screening Shixiao San and its extracts. The treatment of n-butanol fraction on endothelial cells exhibited stronger healing effects against oxidized low density lipoprotein-induced insult when compared with other fractions. Cell viability, the level of nitric oxide, endothelial nitric oxide synthase and endothelin-1 were measured, respectively. The assays revealed n-butanol fraction significantly elevated the survival ratio of impaired cells in culture. In parallel, n-butanol fraction exhibited the highest inhibition of inflammation. The generation of prostaglandin-2 and adhesion molecule (soluble intercellular adhesion molecule-1 was obviously declined. Furthermore, n-butanol fraction suppressed the production of reactive oxygen species and malondialdehyde, and restored the activity of superoxide dismutase. Compounds identification of the n-butanol fraction was carried out by ultra high liquid chromatography coupled to quadrupole time-of-flight tandem mass spectrometry. The active ingredients including quercetin-3-O-(2G-α-l-rhamnosyl-rutinoside, quercetin-3-O-neohesperidoside, isorhamnetin-3-O-neohesperidoside and isorhamnetin-3-O-rutinoside revealed the ability of anti-atherosclerosis after exposing on endothelial cells. The current work illustrated the pharmacology effect of Shixiao San and clearly indicated the major active components in Shixiao San. More importantly, the proposed cell-based screening method might be particularly suitable for fast evaluating the anti-atherosclerosis efficacy of Traditional Chinese Medicines and screening out the

  14. Rapid and Sensitive Determination of Major Active Ingredients and Toxic Components in GinkgoBiloba Leaves Extract (EGb 761) by a Validated UPLC-MS-MS Method.

    Science.gov (United States)

    Wang, Yao; Liu, Yuan; Wu, Qi; Yao, Xin; Cheng, Zongqi

    2017-01-08

    An accurate, precise and sensitive ultra-performance liquid chromatography tandem mass spectrometric (UPLC-MS-MS) method was developed for the determination of flavonoids, terpene lactones, together with ginkgolic acids in Ginkgo biloba leaves extract (EGb 761). This is the first report of the simultaneous analysis of major active ingredients and toxic components in EGb 761 using UPLC-MS-MS. This analysis afforded good linearity, precision, repeatability and accuracy. In addition, the content of those major bioactive components in EGb 761 prepared by different manufacturers of China was determined to establish the effectiveness of the method. The results indicated that the quantification analysis could be readily utilized as a quality control method for EGb 761 and its other related products using flavonoids, terpene lactones and ginkgolic acids as markers.

  15. Comparison of adsorption equilibrium and kinetic models for a case study of pharmaceutical active ingredient adsorption from fermentation broths: parameter determination, simulation, sensitivity analysis and optimization

    Directory of Open Access Journals (Sweden)

    B. Likozar

    2012-09-01

    Full Text Available Mathematical models for a batch process were developed to predict concentration distributions for an active ingredient (vancomycin adsorption on a representative hydrophobic-molecule adsorbent, using differently diluted crude fermentation broth with cells as the feedstock. The kinetic parameters were estimated using the maximization of the coefficient of determination by a heuristic algorithm. The parameters were estimated for each fermentation broth concentration using four concentration distributions at initial vancomycin concentrations of 4.96, 1.17, 2.78, and 5.54 g l−¹. In sequence, the models and their parameters were validated for fermentation broth concentrations of 0, 20, 50, and 100% (v/v by calculating the coefficient of determination for each concentration distribution at the corresponding initial concentration. The applicability of the validated models for process optimization was investigated by using the models as process simulators to optimize the two process efficiencies.

  16. Monitoring and Control of a Continuous Grignard Reaction for the Synthesis of an Active Pharmaceutical Ingredient Intermediate Using Inline NIR spectroscopy

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Nielsen, Jesper; Jønch Pedersen, Michael

    2012-01-01

    Inline near-infrared (NIR) spectroscopy has been used to monitor a continuous synthesis of an active pharmaceutical ingredient (API) intermediate by a Grignard alkylation reaction. The reaction between a ketone substrate and allylmagnesium chloride may form significant impurities with excess...... feeding of the Grignard reagent beyond the stoichiometric ratio. On the other hand, limiting this reagent would imply a loss in yield. Therefore, accurate dosing of the two reactants is essential. A feedforward–feedback control loop was conceived in order to maintain the reaction as closely as possible...... to the stoichiometric ratio, leading the path to full process automation. The feedback control loop relies on NIR transmission measurements performed in a flow cell where, in contrast to labor-intensive offline HPLC analytical methods, the whole reaction product can be scanned in real time without sample dilution...

  17. Switching to aripiprazole for the treatment of residual mutism resulted in distinct clinical courses in two catatonic schizophrenia cases.

    Science.gov (United States)

    Muneoka, Katsumasa; Kanahara, Nobuhisa; Kimura, Shou

    2017-01-01

    The efficacy of a partial agonist for the dopamine D2 receptor, aripiprazole, for catatonia in schizophrenia has been reported. We report distinct clinical courses in challenging aripiprazole to treat residual mutism after severe catatonic symptoms improved. In the first case, mutism was successfully treated when the patient was switched from olanzapine to aripiprazole. In contract, switching to aripiprazole from risperidone aggravated auditory hallucinations in the second case. We will discuss the benefits and risks of using aripiprazole for the treatment of catatonic schizophrenia and the possibility of dopamine supersensitivity psychosis.

  18. Switching to aripiprazole for the treatment of residual mutism resulted in distinct clinical courses in two catatonic schizophrenia cases

    Directory of Open Access Journals (Sweden)

    Katsumasa Muneoka

    2017-02-01

    Full Text Available Objectives: The efficacy of a partial agonist for the dopamine D2 receptor, aripiprazole, for catatonia in schizophrenia has been reported. Methods: We report distinct clinical courses in challenging aripiprazole to treat residual mutism after severe catatonic symptoms improved. Results: In the first case, mutism was successfully treated when the patient was switched from olanzapine to aripiprazole. In contract, switching to aripiprazole from risperidone aggravated auditory hallucinations in the second case. Conclusions: We will discuss the benefits and risks of using aripiprazole for the treatment of catatonic schizophrenia and the possibility of dopamine supersensitivity psychosis.

  19. Switching to aripiprazole for the treatment of residual mutism resulted in distinct clinical courses in two catatonic schizophrenia cases

    Science.gov (United States)

    Muneoka, Katsumasa; Kanahara, Nobuhisa; Kimura, Shou

    2017-01-01

    Objectives: The efficacy of a partial agonist for the dopamine D2 receptor, aripiprazole, for catatonia in schizophrenia has been reported. Methods: We report distinct clinical courses in challenging aripiprazole to treat residual mutism after severe catatonic symptoms improved. Results: In the first case, mutism was successfully treated when the patient was switched from olanzapine to aripiprazole. In contract, switching to aripiprazole from risperidone aggravated auditory hallucinations in the second case. Conclusions: We will discuss the benefits and risks of using aripiprazole for the treatment of catatonic schizophrenia and the possibility of dopamine supersensitivity psychosis. PMID:28255444

  20. Efficacy of attractive toxic sugar baits (ATSB) against Aedes albopictus with garlic oil encapsulated in beta-cyclodextrin as the active ingredient.

    Science.gov (United States)

    Junnila, Amy; Revay, Edita E; Müller, Gunter C; Kravchenko, Vasiliy; Qualls, Whitney A; Xue, Rui-de; Allen, Sandra A; Beier, John C; Schlein, Yosef

    2015-12-01

    We tested the efficacy of attractive toxic sugar bait (ATSB) with garlic oil microencapsulated in beta-cyclodextrin as active ingredient against Aedes albopictus in suburban Haifa, Israel. Two three-acre gardens with high numbers of Ae. albopictus were selected for perimeter spray treatment with ATSB and ASB (bait containing no active ingredient). Baits were colored with food dye to verify feeding of the mosquitoes. The mosquito population was monitored by human landing catches and sweep net catches in the surrounding vegetation. Experiments lasted for 44 days. Treatment occurred on day 13. The mosquito population collapsed about 4 days after treatment and continued to drop steadily for 27 days until the end of the study. At the experimental site the average pre-treatment landing rate was 17.2 per 5mins. Two days post-treatment, the landing rate dropped to 11.4, and continued to drop to an average of 2.6 during the following 26 days. During the same period, the control population was stable. Few sugar fed females (8-10%) approached a human bait and anthrone tests showed relatively small amounts of sugar within their crop/gut. Around 60-70 % of males caught near our human bait were sugar positive which may indicate that the males were feeding on sugar for mating related behavior. From the vegetation treated with the toxic bait, we recovered significantly fewer (about 10-14%) males and females stained by ATSB than at the ASB-treated control. This may indicate that the toxic baits alter the resting behavior of the poisoned mosquitoes within the vegetation. Almost no Ae. albopictus females (5.2±1.4) approached human bait after treatment with ATSB. It therefore appears that microencapsulated garlic oil is an effective pesticide against Ae. albopictus when used in an ATSB system.

  1. Botanical ingredients in cosmeceuticals.

    Science.gov (United States)

    Baumann, Leslie

    2007-11-01

    During the last 10 to 15 years, complementary and alternative medicine (CAM) has become increasingly popular in the US. Within this realm of health care, oral and topical herbal supplements have become some of the most frequently used alternative therapies. Most herbal supplements are based on, or include, several botanical ingredients with long histories of traditional or folk medicine usage. Among the numerous botanical ingredients available on the market today, several are believed to confer dermatologic benefits. This article will focus on a select group of botanical compounds, many of which have long traditions in Asian medicine, with potential or exhibited dermatologic applications, including curcumin, Ginkgo biloba, ginseng, silymarin, soy, and tea tree oil. Other botanical agents, such as arnica, bromelain, chamomile, pomegranate, caffeine, green tea, licorice, and resveratrol, are also briefly considered. Some of these ingredients have been incorporated into topical formulations.

  2. Review on active ingredients from Cannabis sativa leaves and its pharmacological characteristics%汉麻叶活性成分及其药理特性的研究概况

    Institute of Scientific and Technical Information of China (English)

    杜军强; 何锦风; 何聪芬; 蒲彪; 李靖宇; 蒋勇

    2011-01-01

    Cannabis saliva leaves contains a variety of active ingredients, including cannabinoid and non -cannabinoid. Active ingredients from Cannahis saliva leaves have a high application value in the pharmacy and other fields. In this paper, the pharmacological characteristics of cannabinoid, non-cannabinoid and unknown active ingredients was summarized.%汉麻叶含有多种活性成分,包括大麻酚类化合物和非大麻酚类化合物.汉麻叶的活性成分在医药等领域有极高的应用价值.本文就大麻酚类化合物,非大麻酚类化合物和未知活性成分的药理特性展开综述.

  3. Adjunctive aripiprazole versus placebo for antipsychotic-induced hyperprolactinemia: meta-analysis of randomized controlled trials.

    Directory of Open Access Journals (Sweden)

    Xianbin Li

    Full Text Available OBJECTIVE: To compare the safety and efficacy of adjunctive aripiprazole versus placebo for antipsychotic-induced hyperprolactinemia. METHODS: POPULATION: adult patients presenting with antipsychotic-induced hyperprolactinemia diagnosed by prolactin level with or without prolactin-related symptoms. INTERVENTIONS: adjunctive aripiprazole vs. adjunctive placebo. OUTCOME MEASURES: adverse events and efficacy of treatment. STUDIES: randomized controlled trials. RESULTS: Five randomized controlled trials with a total of 639 patients (326 adjunctive aripiprazole, 313 adjunctive placebo met the inclusion criteria. Adjunctive aripiprazole was associated with a 79.11% (125/158 prolactin level normalization rate. Meta-analysis of insomnia, headache, sedation, psychiatric disorder, extrapyramidal symptom, dry mouth, and fatigue showed no significant differences in the adjunctive aripiprazole treatment group compared with the placebo group (risk difference (Mantel-Haenszel, random or fixed -0.05 to 0.04 (95% confidence interval -0.13 to 0.16; I(2 =0% to 68%, P=0.20 to 0.70. However, sedation, insomnia, and headache were more frequent when the adjunctive aripiprazole dose was higher than 15 mg/day. Meta-analysis of the prolactin level normalization indicated adjunctive aripiprazole was superior to placebo (risk difference (Mantel-Haenszel, random 0.76 (95% confidence interval 0.67 to 0.85; I(2 =43%, P<0.00001. The subgroup analysis confirmed that the subjects who received adjunctive aripiprazole 5 mg/day showed a degree of prolactin normalization similar to that of all participants. No significant differences between groups in discontinuation and improvements of psychiatric symptoms. CONCLUSION: Adjunctive aripiprazole is both safe and effective as a reasonable choice treatment for patients with antipsychotic-induced hyperprolactinemia. The appropriate dose of adjunctive aripiprazole may be 5 mg/day.

  4. In vitro cytotoxic activity of Sa-Tri-Lhung-Klod remedy and its herbal ingredients on ovarian and cervical carcinoma cell lines.

    Science.gov (United States)

    Inprasit, Janjira; Ruangnoo, Srisopa; Itharat, Arunporn

    2014-08-01

    Sa-Tri-Lhung-Klod is a Thai traditional medicine remedy for postpartum in the lists of The National Drug List ofHerbal Medicine Products AD. It consists ofseventeen herbs and were obtained by maceration and used in the form of liquor for women's health care such as treatment ofamenorrhea, menopause and blood tonic. In addition, it also usedfor postpartum care for being anti-inflammation in postpartum and prevention of cancer in women. To investigate cytotoxic activity ofSa-Tri-Lhung-Klod remedy extracts and its herbal ingredients against human ovarian carcinoma cell line (SKOV-3) and cervical adenocarcinoma (HeLa) cell line. Sa-Tri-Lhung-Klod remedy and its plant ingredients were extracted by maceration in 95% ethanol and dried using evaporator. All extracts were testedfor cytotoxic activity by sulforhodamine B (SRB) assay. Ethanolic extract ofSa-Tri-Lhung-Klod remedy displayed cytotoxic activity against SKOV-3 and HeLa with IC50 values of 72.84±1.07 and 47.24±2.83 μg/ml, respectively. It was classified as "less-active" according to the NCI guideline. However, Caesalpinia sappan, Mammea siamensis and Curcuma comosa showed high cytotoxic activity against SKOV-3 with IC50 values of 9.55±1.38 13.45±0.82 and 14.21±1.30 μg/ml, respectively. The ethanolic extracts ofCaesalpiniasappan and Mammea siamensis also exhibited cytotoxic activity against HeLa with IC50 values of 6.30±0.06 and 7.72±0.11 μg/ml, respectively. These results support the use of Sa-Tri-Lhung-Klod remedy in Thai traditional medicine for preventing of ovarian cancer and cervical cancer Caesalpinia sappan, Curcuma comosa and Mammea siamensis were strikingly active against ovarian and cervical cancer cells. Their extracts have the potential for developing as new anti-cancer drugs for women health.

  5. Functional ingredients from microalgae

    NARCIS (Netherlands)

    Buono, S.; Langellotti, A.L.; Martello, A.; Rinna, F.; Fogliano, V.

    2014-01-01

    A wide variety of natural sources are under investigation to evaluate their possible use for new functional ingredient formulation. Some records attested the traditional and ancient use of wild harvested microalgae as human food but their cultivation for different purposes started about 40 years

  6. Functional ingredients from microalgae

    NARCIS (Netherlands)

    Buono, S.; Langellotti, A.L.; Martello, A.; Rinna, F.; Fogliano, V.

    2014-01-01

    A wide variety of natural sources are under investigation to evaluate their possible use for new functional ingredient formulation. Some records attested the traditional and ancient use of wild harvested microalgae as human food but their cultivation for different purposes started about 40 years ago

  7. Peripheral Antinociception Induced by Aripiprazole Is Mediated by the Opioid System

    Directory of Open Access Journals (Sweden)

    Renata Cristina Mendes Ferreira

    2017-01-01

    Full Text Available Background. Aripiprazole is an antipsychotic drug used to treat schizophrenia and related disorders. Our previous study showed that this compound also induces antinociceptive effects. The present study aimed to assess the participation of the opioid system in this effect. Methods. Male Swiss mice were submitted to paw pressure test and hyperalgesia was induced by intraplantar injection of prostaglandin E2 (PGE2, 2 μg. Aripiprazole was injected 10 min before the measurement. Naloxone, clocinnamox, naltrindole, nor-binaltorphimine, and bestatin were given 30 min before aripiprazole. Nociceptive thresholds were measured in the 3rd hour after PGE2 injection. Results. Aripiprazole (100 μg/paw injected locally into the right hind paw induced an antinociceptive effect that was blocked by naloxone (50 μg/paw, a nonselective opioid receptor antagonist. The role of μ-, δ-, and κ-opioid receptors was investigated using the selective antagonists, clocinnamox (40 μg/paw, naltrindole (15, 30, and 60 μg/paw, and nor-binaltorphimine (200 μg/paw, respectively. The data indicated that only the δ-opioid receptor antagonist inhibited the peripheral antinociception induced by aripiprazole. Bestatin (400 μg, an aminopeptidase-N inhibitor, significantly enhanced low-dose (25 μg/paw aripiprazole-induced peripheral antinociception. Conclusion. The results suggest the participation of the opioid system via δ-opioid receptor in the peripheral antinociceptive effect induced by aripiprazole.

  8. Waterborne aripiprazole blunts the stress response in zebrafish

    Science.gov (United States)

    Barcellos, Heloísa Helena De Alcantara; Kalichak, Fabiana; da Rosa, João Gabriel Santos; Oliveira, Thiago Acosta; Koakoski, Gessi; Idalencio, Renan; de Abreu, Murilo Sander; Giacomini, Ana Cristina Varrone; Fagundes, Michele; Variani, Cristiane; Rossini, Mainara; Piato, Angelo L.; Barcellos, Leonardo José Gil

    2016-11-01

    Here we provide, at least to our knowledge, the first evidence that aripiprazole (APPZ) in the water blunts the stress response of exposed fish in a concentration ten times lower than the concentration detected in the environment. Although the mechanism of APPZ in the neuroendocrine axis is not yet determined, our results highlight that the presence of APPZ residues in the environment may interfere with the stress responses in fish. Since an adequate stress response is crucial to restore fish homeostasis after stressors, fish with impaired stress response may have trouble to cope with natural and/or imposed stressors with consequences to their welfare and survival.

  9. Effective Teachers for Students with Emotional/Behavioral Disorders: Active Ingredients Leading to Positive Teacher and Student Outcomes

    Science.gov (United States)

    Conroy, Maureen A.; Sutherland, Kevin S.

    2012-01-01

    Teachers of students with emotional/behavioral disorders (E/BD) have varied skills and abilities. Within the field there are some teachers, who teach students with E/BD by actively engaging them in learning tasks and who have few behavior problems in comparison to other teachers, who struggle with classroom management. Many researchers have found…

  10. Induction of rat hepatic cytochromes P450 by toxic ingredients in plants: lack of correlation between toxicity and inductive activity.

    Science.gov (United States)

    Yamada, H; Nakamura, T; Oguri, K

    1998-12-01

    "Animal-Plant Warfare" is one of the hypotheses for the evolution of drug-metabolizing P450s. To address the validity of this hypothesis, we examined the induction of xenobiotic-metabolizing P450s by 12 plant toxins in rats, using hepatic activity for testosterone metabolism as the index. The compounds tested were aconitine, morphine, tubocurarine, physostigmine, pilocarpine, muscarine, cocaine, atropine, amygdalin, digitonin, nicotine and solanine. Drinking water containing a test compound was given to rats for 4 days, and the hepatic activity of testosterone metabolism was determined together with monitoring body weight gain and liver weight as the indices of toxicity. The results showed that while cocaine and nicotine have a minor ability to increase testosterone 16 beta-hydroxylase activity, a marker activity for the CYP2B1 and 2, all other compounds did not have any such effect. No correlation was observed between a change in 16 beta-hydroxylase and toxicity caused by toxins. Therefore, these results did not support the idea that the inducibility of the CYP2B subfamily in animals is acquired through "Animal-Plant Warfare". Several compounds examined here increased or decreased hepatic activities of testosterone 2 alpha-, 6 beta-, 7 alpha- and 16 alpha-hydroxylation and 17-oxidation, indicating a possible effect on the CYP2A, 2C and 3A subfamily. Of these effects, a moderate correlation (r toxicity. It is therefore suggested that inhibition or suppression of the expression of CYP2C11 is one of the mechanisms in the toxicity of plant toxins for rats, although it comes from an examination using limited numbers of compounds.

  11. Kinetics of Inhibition of Monoamine Oxidase Using Cymbopogon martinii (Roxb.) Wats.: A Potential Antidepressant Herbal Ingredient with Antioxidant Activity.

    Science.gov (United States)

    Gacche, R N; Shaikh, R U; Chapole, S M; Jadhav, A D; Jadhav, S G

    2011-07-01

    The study was designed to evaluate the antioxidant activity and effect of Cymbopogon martinii (Roxb.) Wats. (Poaceae) leaves on the activity of monoamine oxidase and kinetics of enzyme inhibition. Ethanol extract of C. martinii and rat brain mitochondrial monoamine oxidase preparation ware used to study the kinetics of enzyme inhibition using double reciprocal Lineweaver-Burk plot. The DPPH was used as a source of free radical to evaluate antioxidant potential. It is observed that, the ethanolic extract of C. martinii inhibits the monoamine oxidase activity with competitive mode of inhibition. The V(max) (0.01 mM/min) remained constant while, K(m) varied from 21.00 ± 1.1, 43.33 ± 1.5 and 83.33 ± 1.4 mM for 100-500 μg/ml concentration of C. martinii. The K(i) values were calculated to be 90.00 ± 0.87, 75.00 ± 0.69, 68.18 ± 0.68 μg for 100-500 μg/ml concentration of C. martini. It also shows a significant DPPH (1,1-diphenyl-2-picryl hydrazine) radical scavenging (IC(50) = 0.34 ± 0.05 mg/ml) and reducing activity (IC(50) = 0.70 ± 0.22 mg/ml). The C. martini can be considered as a possible source of MAO inhibitor used in the treatment of depression and other neurological disorders.

  12. Usefulness of the dopamine system-stabilizer aripiprazole for reducing morphine-induced emesis.

    Science.gov (United States)

    Shiokawa, Mitsuru; Narita, Minoru; Nakamura, Atsushi; Kurokawa, Kazuhiro; Inoue, Tadao; Suzuki, Tsutomu

    2007-09-10

    In the management of pain, nausea and vomiting are some of the most distressing adverse effects induced by opioids. In the present study, we investigated the effect of the dopamine system-stabilizer aripiprazole on morphine-induced emesis. Morphine induced retching and vomiting in a dose-dependent manner in ferrets. The emetic effect of morphine was significantly suppressed by pretreatment with either the dopamine receptor antagonist haloperidol or aripiprazole. These results suggest that the co-administration of aripiprazole may be useful for reducing the severity of morphine-induced emesis.

  13. A Case of Aripiprazole-Induced Tardive Dyskinesia with Dramatic Evolution

    Science.gov (United States)

    Heitzmann, Edwige; Weiner, Luisa; Michel, Bruno

    2016-01-01

    Aripiprazole is reported to be a good clinical safety profile antipsychotic. However, recent data suggest that the risk of tardive dyskinesia could be higher than initially thought. We report the case of aripiprazole-induced tardive dyskinesia with dramatic evolution in a patient with several risk factors, including older age and exposure to antipsychotic over a period longer than six months. This case and its dramatic evolution, associated with other cases recently published, suggest reconsidering the real risk of tardive dyskinesia associated with aripiprazole, particularly in the elderly. PMID:27818825

  14. A Case of Aripiprazole-Induced Tardive Dyskinesia with Dramatic Evolution

    Directory of Open Access Journals (Sweden)

    Edwige Heitzmann

    2016-01-01

    Full Text Available Aripiprazole is reported to be a good clinical safety profile antipsychotic. However, recent data suggest that the risk of tardive dyskinesia could be higher than initially thought. We report the case of aripiprazole-induced tardive dyskinesia with dramatic evolution in a patient with several risk factors, including older age and exposure to antipsychotic over a period longer than six months. This case and its dramatic evolution, associated with other cases recently published, suggest reconsidering the real risk of tardive dyskinesia associated with aripiprazole, particularly in the elderly.

  15. Extraction and Separation of Active Ingredients in Schisandra chinensis (Turcz. Baill and the Study of their Antifungal Effects.

    Directory of Open Access Journals (Sweden)

    Haijing Yi

    Full Text Available Schisandra chinensis extracts (SEs have traditionally been used as an oriental medicine for the treatment of various human diseases, however, their further application in the biocontrol of plant disease remains poorly understood. This study was conducted to develop eco-friendly botanical pesticides from extracts of S. chinensis and assess whether they could play a key role in plant disease defense. Concentrated active fractions (SE-I, SE-II, and SE-III were obtained from S. chinensis via specific extraction and separation. Then, lignan-like substances, such as Schisanhenol B, were detected via High-Performance Liquid Chromatography-ElectroSpray Ionization-Mass Spectrometry (HPLC-ESI-MS analyses of the active fractions. Moreover, the results from biological tests on colony growth inhibition and spore germination indicated that SE-I, SE-II, and SE-III could inhibit hyphal growth and spore generation of three important plant pathogenic fungi (Monilinia fructicola, Fusarium oxysporum, and Botryosphaeria dothidea. The study of the mechanisms of resistant fungi revealed that the oxidation resistance system, including reactive oxygen species (ROS, malondialdehyde (MDA, catalase (CAT, and superoxide dismutase (SOD, was activated. The expression of genes related to defense, such as pathogenesis-related protein (PR4, α-farnesene synthase (AFS, polyphenol oxidase (PPO, and phenylalanine ammonia lyase (PAL were shown to be up-regulated after treatment with SEs, which suggested an increase in apple immunity and that fruits were induced to effectively defend against the infection of pathogenic fungi (B. dothidea. This study revealed that SEs and their lignans represent promising resources for the development of safe, effective, and multi-targeted agents against pathogenic fungi.

  16. Extraction and Separation of Active Ingredients in Schisandra chinensis (Turcz.) Baill and the Study of their Antifungal Effects

    Science.gov (United States)

    Liu, Jun; Zhang, Jie; Guo, Wei; Xiao, Weilie; Yao, Yuncong

    2016-01-01

    Schisandra chinensis extracts (SEs) have traditionally been used as an oriental medicine for the treatment of various human diseases, however, their further application in the biocontrol of plant disease remains poorly understood. This study was conducted to develop eco-friendly botanical pesticides from extracts of S. chinensis and assess whether they could play a key role in plant disease defense. Concentrated active fractions (SE-I, SE-II, and SE-III) were obtained from S. chinensis via specific extraction and separation. Then, lignan-like substances, such as Schisanhenol B, were detected via High-Performance Liquid Chromatography-ElectroSpray Ionization-Mass Spectrometry (HPLC-ESI-MS) analyses of the active fractions. Moreover, the results from biological tests on colony growth inhibition and spore germination indicated that SE-I, SE-II, and SE-III could inhibit hyphal growth and spore generation of three important plant pathogenic fungi (Monilinia fructicola, Fusarium oxysporum, and Botryosphaeria dothidea). The study of the mechanisms of resistant fungi revealed that the oxidation resistance system, including reactive oxygen species (ROS), malondialdehyde (MDA), catalase (CAT), and superoxide dismutase (SOD), was activated. The expression of genes related to defense, such as pathogenesis-related protein (PR4), α-farnesene synthase (AFS), polyphenol oxidase (PPO), and phenylalanine ammonia lyase (PAL) were shown to be up-regulated after treatment with SEs, which suggested an increase in apple immunity and that fruits were induced to effectively defend against the infection of pathogenic fungi (B. dothidea). This study revealed that SEs and their lignans represent promising resources for the development of safe, effective, and multi-targeted agents against pathogenic fungi. PMID:27152614

  17. Analysis of bioactive ingredients in the brown alga Fucus vesiculosus by capillary electrophoresis and neutron activation analysis.

    Science.gov (United States)

    Truus, Kalle; Vaher, Merike; Koel, Mihkel; Mähar, Andres; Taure, Imants

    2004-07-01

    Two different types of bioactive components of the seaweed Fucus vesiculosus were analysed: (1) polyphenols (phlorotannins) by capillary electrophoresis (CE) and (2) mineral part (including bioactive microelements) by neutron activation analysis (NAA). CE experiments were carried out using a UV detector (at 210 nm) and an uncoated silica capillary. The best separation was achieved at a voltage of 20 kV using borate or acetate buffer in a methanol/acetonitrile mixture as background electrolyte. The CE analysis data were confirmed by high-performance liquid chromatography (HPLC). Determination of mineral composition of algal biomass by NAA was performed on the basis of various nuclides; the best results (from 38 elements determined) were obtained for Mn, Fe, Zn, As, Br, Sr, I, Ba, Au and Hg.

  18. The slow relaxation dynamics in active pharmaceutical ingredients studied by DSC and TSDC: Voriconazole, miconazole and itraconazole.

    Science.gov (United States)

    Ramos, Joaquim J Moura; Diogo, Hermínio P

    2016-03-30

    The slow molecular mobility of three active pharmaceutical drugs (voriconazole, miconazole and itraconazole) has been studied by differential scanning calorimetry (DSC) and thermally stimulated depolarization currents (TSDC). This study yielded the main kinetic features of the secondary relaxations and of the main (glass transition) relaxation, in particular their distribution of relaxation times. The dynamic fragility of the three glass formers was determined from DSC data (using two different procedures) and from TSDC data. According to our results voriconazole behaves as a relatively strong liquid, while miconazole is moderately fragile and itraconazole is a very fragile liquid. There are no studies in this area published in the literature relating to voriconazole. Also not available in the literature is a slow mobility study by dielectric relaxation spectroscopy in the amorphous miconazole. Apart from that, the results obtained are in reasonable agreement with published works using different experimental techniques. Copyright © 2016 Elsevier B.V. All rights reserved.

  19. In vitro and clinical evaluation of SIG1273: a cosmetic functional ingredient with a broad spectrum of anti-aging and antioxidant activities.

    Science.gov (United States)

    Fernández, José R; Rouzard, Karl; Voronkov, Michael; Huber, Kristen L; Webb, Corey; Stock, Jeffry B; Stock, Maxwell; Gordon, Joel S; Pérez, Eduardo

    2016-06-01

    Isoprenylcysteine (IPC) small molecules were identified as a new class of anti-inflammatory compounds over 20 years ago. Since then, they have been developed as novel cosmetic functional ingredients (CFI) and topical drug candidates. SIG1273 is a second generation CFI that has previously been shown to provide a broad spectrum of benefits for the skin through its anti-inflammatory and antimicrobial properties. To determine whether SIG1273 possesses anti-aging properties in vitro and evaluate the tolerability and activity of SIG1273 when applied topically to human subjects. To model photoaging in vitro, human dermal fibroblasts (HDFs) were exposed in culture to UVA to induce collagenase (MMP-1) production. An in vitro wound-healing model was based on the activation of HDF migration into cell-free tissue culture surface. Hydrogen peroxide-induced oxidative stress was performed using HDFs to measure intracellular ROS activity. Radical scavenging capacity was determined using a colorimetric antioxidant assay kit (ABTS method). Lastly, a 4-week, 29-subject study was performed in which SIG1273 was applied topically as a cream to assess its tolerance and activity in reducing the appearance of aging. In vitro studies demonstrate SIG1273 inhibits UVA-induced MMP-1 production, hydrogen peroxide-induced oxidative stress and promotes wound healing. Moreover, SIG1273 was shown to be a radical scavenging antioxidant. Clinical assessment of SIG1273 cream (0.25%) showed it was well tolerated with significant improvement in the appearance of fine lines, coarse wrinkles, radiance/luminosity, pore size, texture/smoothness, hydration and increased firmness. SIG1273 represents a novel CFI with antioxidant, anti-aging, and anti-inflammatory properties that when applied topically is well tolerated and provides benefits to individuals with aging skin. © 2016 Wiley Periodicals, Inc.

  20. Safety assessment of a novel active ingredient, acetyl aspartic acid, according to the EU Cosmetics Regulation and the Scientific Committee on Consumer Safety guidelines.

    Science.gov (United States)

    Daly, P; Moran, G

    2015-10-01

    Acetyl aspartic acid (A-A-A) was proposed as a new novel active ingredient for use in cosmetics. The safety of A-A-A was assessed by following an in-house-developed 'New Ingredient Testing Strategy', which was designed in accordance with the Scientific Committee on Consumer Safety (SCCS) notes of guidance and the requirements of Annex I of the EU Cosmetics Regulation. The aim of the project was to determine whether A-A-A was safe for use in cosmetics and to determine a maximum permitted safe level in the formulations. A literature review was conducted, consulting over 40 different information sources. This highlighted a number of gaps which required testing data. A-A-A was tested for phototoxicity according to OECD test guideline 432, skin irritation according to OECD test guideline 439 and eye irritation according to OECD test guideline 437. Dermal absorption of A-A-A was measured according to OECD test guideline 428 and was used to calculate the margin of safety (MoS). Finally, A-A-A was tested in a human repeat insult patch test (HRIPT) and a 14-day in-use tolerance study. A-A-A was non-phototoxic and was non-irritating to skin and eyes in in vitro testing. Dermal absorption was calculated to be 5%. The MoS for A-A-A was 351, at a level of 5%, for all cosmetic product types, indicating no systemic safety toxicity concern. A-A-A at 5% under occlusive patch on a panel of 50 adult volunteers induced no skin irritation or allergic reaction in the HRIPT study. Finally, repeated application of A-A-A to the periocular area, twice per day for 14 days, in 21 female volunteers, demonstrated that 1% A-A-A was well tolerated following dermatological and ophthalmological assessment in a cosmetic formulation. A-A-A was assessed as safe by the cosmetic safety assessor for use in cosmetics at a level of 5% in all cosmetic product types, in line with the requirements of the EU Cosmetics Regulation and in accordance with the SCCS notes of guidance. © 2015 Society of Cosmetic

  1. Active Ingredients Extracted and Nanofiltration Application in Astragalus Extract%黄芪的有效成分提取与纳滤提取应用分析

    Institute of Scientific and Technical Information of China (English)

    郭立忠; 吴镝

    2015-01-01

    目的:分析黄芪的有效成分提取和纳滤提取的应用,对传统的黄芪提取工艺进行改进。方法将黄芪多糖、总皂甙作为实验对象,使用正交实验设计并用极差分析法分析数值,对比不同提取温度、时间和次数对成分含量的影响,并在水煮醇沉提取工艺中加入了纤维素酶,比较纳滤、蒸发方法的效果。结果实验表明温度<80℃、提取2次且每次60 min的纳滤浓缩提取是黄芪水提的最佳工艺。结论相比较传统水煮醇沉提取法,黄芪的纳滤浓缩提取工艺在经济、技术上有很强的优越性,在指导制剂生产、临床应用中具有一定的推广价值。%Objective To analyze the active ingredients of astragalus diarrhea extraction and nanofiltration extracted application,astragalus traditional extraction process improvements. Methods APS,saponins as subjects,the use of orthogonal experimental design and analysis of numerical range analysis by comparing the effects of different extraction temperature,time and number of ingredients,and the extraction process in boiling alcohol shen added effect of cel ulase,nanofiltration comparison,the evaporation method. Results The experimental results showed that the temperature < 80 ℃, extracting 2 times,and each time 60 min nanofiltration concentrated extract was the optimum water extraction of astragalus. Conclusion Compared to traditional boiling alcohol precipitation extraction,astragalus of nanofiltration extraction process in the economic,technical y strong advantages,it has some promotional value in guiding the preparation of manufacturing,clinical applications.

  2. Preparation of Fe3O4 Magnetic Surface Imprinted Microspheres and the Ethyl Acetate Extract Flavonoids Raspberry Concentration of Active Ingredient Applied

    Directory of Open Access Journals (Sweden)

    Xie YiHui

    2016-01-01

    Full Text Available the study is used by the co-precipitation method to make some uniform particle size and have good Fe3O4 magnetic nanoparticles and their surface modified with oleic acid ; oleic acid as the carrier of Fe3O4, quercetin as template molecule, prepared by the microwave assisted molecular imprinted polymer magnetic nanospheres; In raspberry ethyl acetate extract fingerprints for the assessment index, with orthogonal design best preparation; Characterization of equilibrium adsorption constant Kd and maximum adsorption capacity Qmax by Scatchard model.The results show that: This study explores the preparation of MIPs polymerization time by ten times, prepared by the Fe3O4 nanometer level, greatly increase the MIPs of the specific surface area, thereby increase the amount of adsorption (Kd = 0.7322mg / L, Qmax = 18.92μmol / g. Successfully extract raspberry flavonoids active ingredients from ethyl acetate which can be used for rapid and large parts of ethyl acetate enrichment raspberry flavonoids.

  3. Influence of Process Parameters on Content Uniformity of a Low Dose Active Pharmaceutical Ingredient in a Tablet Formulation According to GMP

    Directory of Open Access Journals (Sweden)

    Muselík Jan

    2014-09-01

    Full Text Available The article describes the development and production of tablets using direct compression of powder mixtures. The aim was to describe the impact of filler particle size and the time of lubricant addition during mixing on content uniformity according to the Good Manufacturing Practice (GMP process validation requirements. Processes are regulated by complex directives, forcing the producers to validate, using sophisticated methods, the content uniformity of intermediates as well as final products. Cutting down of production time and material, shortening of analyses, and fast and reliable statistic evaluation of results can reduce the final price without affecting product quality. The manufacturing process of directly compressed tablets containing the low dose active pharmaceutical ingredient (API warfarin, with content uniformity passing validation criteria, is used as a model example. Statistic methods have proved that the manufacturing process is reproducible. Methods suitable for elucidation of various properties of the final blend, e.g., measurement of electrostatic charge by Faraday pail and evaluation of mutual influences of researched variables by partial least square (PLS regression, were used. Using these methods, it was proved that the filler with higher particle size increased the content uniformity of both blends and the ensuing tablets. Addition of the lubricant, magnesium stearate, during the blending process improved the content uniformity of blends containing the filler with larger particles. This seems to be caused by reduced sampling error due to the suppression of electrostatic charge.

  4. 肉桂降糖活性成分提取方法的研究%Study on cinnamon hypoglycemic active ingredient extraction method

    Institute of Scientific and Technical Information of China (English)

    卢春连; 陆志科

    2014-01-01

    用乙醇回流提取法、超声波提取法、新装置提取法提取肉桂降糖活性成分。结果表明,新装置提取法比回流提取法、超声波提取法提取效率高,且快速简便。新装置提取法提取肉桂降糖活性成分的最佳条件为:多功能提取器装置,提取溶剂为95%乙醇,提取时间2 h,产品粗提率达21.0%。%Three methods were compared of preparing cinnamon hypoglycemic active ingredients:the etha-nol refluxing extraction,ultrasonic extraction and the new device extraction. The results showed that the new device extraction was superior to ethanol refluxing extraction and ultrasonic extraction,and the meth-od was fast and simple. The best conditions of the method were:multi-extractor device,solvent of 95%ethanol,and the time of extraction was 2 h,the coarse product rate was 21. 0% .

  5. The determination of crystal structures of active pharmaceutical ingredients from X-ray powder diffraction data: a brief, practical introduction, with fexofenadine hydrochloride as example.

    Science.gov (United States)

    Brüning, Jürgen; Schmidt, Martin U

    2015-06-01

    This study describes the general method for the determination of the crystal structures of active pharmaceutical ingredients (API) from powder diffraction data and demonstrates its use to determine the hitherto unknown crystal structure of fexofenadine hydrochloride, a third-generation antihistamine drug. Fexofenadine hydrochloride was subjected to a series of crystallisation experiments using re-crystallisation from solvents, gas diffusion, layering with an antisolvent and gel crystallisation. Powder diffraction patterns of all samples were recorded and inspected for polymorphism and for crystallinity. All samples corresponded to the same polymorph. The crystal structure was determined from an X-ray powder diffraction pattern using a real-space method with subsequent Rietveld refinement. The structure exhibits a two-dimensional hydrogen bond network. Crystal structures of API can be determined from X-ray powder diffraction data with good reliability. Fexofenadine exhibits only one polymorphic form, which is stabilised in the crystal by strong hydrogen bonds of the type (+)N-H···Cl(-), O-H···Cl(-), and between COOH groups. © 2015 Royal Pharmaceutical Society.

  6. Evaluation of effects of pharmaceutical processing on structural disorders of active pharmaceutical ingredient crystals using nanoindentation and high-resolution total scattering pair distribution function analysis.

    Science.gov (United States)

    Chen, Shuang; Sheikh, Ahmad Y; Ho, Raimundo

    2014-12-01

    Pharmaceutical unit operations such as milling and compaction can often generate disordered regions in crystals of active pharmaceutical ingredients (APIs). This may lead to changes in a number of important pharmaceutical properties including dissolution, stability, hygroscopicity, and so on. It is therefore important for pharmaceutical industry to evaluate the effects of pharmaceutical processing on API structural orders, and to investigate and develop analytical tools that are capable of accurately detecting and assessing subtle process-induced structural disorders in pharmaceutical crystals. In this study, nanoindentation was first used to determine the intrinsic mechanical properties including hardness and Young's modulus of two API crystals, compounds 1 and 2. These crystals of different mechanical properties were then milled and compacted under various conditions. The resulting structural disorders in these crystals were subsequently evaluated using synchrotron-based high-resolution total scattering pair distribution function (TS-PDF) analysis. Furthermore, principal component analysis was applied to the PDF data to assess the relative extents of disorders in the API crystals, which showed a good correlation with the process conditions. The study demonstrates that high-resolution TS-PDF analysis coupled with nanoindentation measurement is a valuable and effective tool for detecting and assessing process-induced subtle structural disorders in API crystals. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.

  7. Monitoring the dissolution of Active Pharmaceutical Ingredient and TPGS in real time via IR spectroscopy during the manufacturing of liquid dosage formulation.

    Science.gov (United States)

    Šašić, Slobodan; Palm, Andrew S; Tang, Degui

    2012-11-01

    Infrared spectroscopy is used to monitor the dissolution of the Active Pharmaceutical Ingredient (API) and an excipient (vitamin E - TPGS) during manufacturing of a liquid pharmaceutical formulation. The goal of the analysis is to explore options for real-time, on screen, and quantitative monitoring of these two components by using an iC10 instrument. As is common, the first step in the approach is to create respective calibration models for the two components and then apply those models on the spectra obtained from scale-up batches. Interestingly, while the API dissolves at the room temperature, TPGS dissolves at an acceptable rate at 50 °C so both temperatures have to be considered. It is shown that univariate models of sufficient accuracy can be developed with a straightforward applicability to the scale-up batches spectra and providing reasonably accurate estimates of the API and TPGS concentrations. Some limitations of the software on the employed instrument may diminish the prospect for the quantitative analysis of the components of interest in this formulation. Copyright © 2012 Elsevier B.V. All rights reserved.

  8. 臭参活性成分乙酸乙酯部分的分离%Separating the Active Ingredient Ethyl Smelly Reference Section

    Institute of Scientific and Technical Information of China (English)

    栾云鹏; 王启明

    2016-01-01

    The purpose of the experiment:the separation of smelly and the activity of the main ingredients. Methods:prelimi-nary extraction with 95%ethanol by petroleum ether, ethyl acetate extraction, part of the ethyl acetate extract of gradient elution with chloroform, methanol (100:0~70:30). Results:ethyl acetate extraction part of the elution of the A, B, C, D, A total of four parts.%此实验的目的:分离臭参中主要的活性成分。方法:先用95%乙醇初步提取在经过石油醚、乙酸乙酯萃取,把得到的乙酸乙酯萃取的部分用氯仿——甲醇梯度洗脱(100:0~70:30)。结果:乙酸乙酯萃取的部分洗脱出A、B、C、D共4个部分。

  9. Visualization of Protonation/Deprotonation of Active Pharmaceutical Ingredient in Solid State by Vapor Phase Amine-Selective Alkyne Tagging and Raman Imaging.

    Science.gov (United States)

    Moriyama, Kei; Yasuhara, Yukiko; Ota, Hiromi

    2017-07-01

    Here, we report a simple and direct method to visualize the protonation/deprotonation of an amine active pharmaceutical ingredient (API) in the solid state using a solid-vapor reaction with propargyl bromide and Raman imaging for the assessment of the API during the manufacturing process of solid formulations. An alkyne tagging occurred on the free form of solid haloperidol by the vapor phase reaction, and a distinct Raman signal of alkyne was detected. Alkyne signal monitoring by Raman imaging enabled us to visualize the distribution of the free-form haloperidol in a solid formulation. On the other hand, haloperidol hydrochloride did not react with propargyl bromide in the solid-vapor reaction, and the alkyne signal was not observed. Using the difference in reactivity, the protonation/deprotonation of the amine API in the solid state could be visualized. As an example of application, we tried to visually assess the protonation/deprotonation state when the free-form haloperidol was ground with acids using the solid-vapor reaction and Raman imaging and found that haloperidol was partially protonated when ground with 2 equivalents of hydrogen chloride. Furthermore, we demonstrated the relationship between the degree of protonation and the amount of water added as a medium for grinding haloperidol with succinic acid. Copyright © 2017 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

  10. Ingredients of Huangqi decoction slow biliary fibrosis progression by inhibiting the activation of the transforming growth factor-beta signaling pathway

    Directory of Open Access Journals (Sweden)

    Du Jin-Xing

    2012-04-01

    Full Text Available Abstract Background Huangqi decoction was first described in Prescriptions of the Bureau of Taiping People's Welfare Pharmacy in Song Dynasty (AD 1078, and it is an effective recipe that is usually used to treat consumptive disease, anorexia, and chronic liver diseases. Transforming growth factor beta 1 (TGFβ1 plays a key role in the progression of liver fibrosis, and Huangqi decoction and its ingredients (IHQD markedly ameliorated hepatic fibrotic lesions induced by ligation of the common bile duct (BDL. However, the mechanism of IHQD on hepatic fibrotic lesions is not yet clear. The purpose of the present study is to elucidate the roles of TGFβ1 activation, Smad-signaling pathway, and extracellular signal-regulated kinase (ERK in the pathogenesis of biliary fibrosis progression and the antifibrotic mechanism of IHQD. Methods A liver fibrosis model was induced by ligation of the common bile duct (BDL in rats. Sham-operation was performed in control rats. The BDL rats were randomly divided into two groups: the BDL group and the IHQD group. IHQD was administrated intragastrically for 4 weeks. At the end of the fifth week after BDL, animals were sacrificed for sampling of blood serum and liver tissue. The effect of IHQD on the TGFβ1 signaling pathway was evaluated by western blotting and laser confocal microscopy. Results Decreased content of hepatic hydroxyproline and improved liver function and histopathology were observed in IHQD rats. Hepatocytes, cholangiocytes, and myofibroblasts in the cholestatic liver injury released TGFβ1, and activated TGFβ1 receptors can accelerate liver fibrosis. IHQD markedly inhibited the protein expression of TGFβ1, TGFβ1 receptors, Smad3, and p-ERK1/2 expression with no change of Smad7 expression. Conclusion IHQD exert significant therapeutic effects on BDL-induced fibrosis in rats through inhibition of the activation of TGFβ1-Smad3 and TGFβ1-ERK1/2 signaling pathways.

  11. Treatment and prevention of mania in bipolar I disorder: focus on aripiprazole

    Directory of Open Access Journals (Sweden)

    David J Muzina

    2009-05-01

    Full Text Available David J MuzinaCenter for Mood Disorders Treatment and Research, Cleveland Clinic Neurological Institute, Cleveland, Ohio, USAAbstract: Aripiprazole is a second-generation antipsychotic with a unique pharmacologic receptor profile that has efficacy in the treatment and prevention of mania in bipolar I disorder. This article reviews the evidence supporting treatment of adults with bipolar I disorder using aripiprazole as monotherapy or adjunctively during acute mania and its utility as an intramuscular agent for agitation in manic patients. Results from one of the longest bipolar maintenance trials which support aripiprazole as a prophylactic mood stabilizer, specifically against manic relapses, will be discussed as well as a post-hoc analysis that suggests efficacy for rapid cycling bipolar disorder. Safety and tolerability issues, patient-focused perspectives and aripiprazole’s place in therapy for bipolar mania will be covered.Keywords: bipolar disorder, mania, prevention, aripiprazole, rapid cycling

  12. Aripiprazole for treating irritability in children & adolescents with autism: A systematic review

    OpenAIRE

    Ahmad Ghanizadeh; Sylvie Tordjman; Nematollah Jaafari

    2015-01-01

    Background & objectives: No clear therapeutic benefits of antipsychotics have been reported for the treatment of behavioural symptoms in autism. This systematic review provides an assessment of evidence for treating irritability in autism by aripiprazole. Methods: The databases of MEDLINE/PubMed and Google Scholar were searched for relevant articles about the effect of aripiprazole in children with autism. The articles were searched according to the inclusion and exclusion criteria speci...

  13. A Case of Aripiprazole-Induced Tardive Dyskinesia with Dramatic Evolution

    OpenAIRE

    Edwige Heitzmann; Hervé Javelot; Luisa Weiner; Bruno Michel

    2016-01-01

    Aripiprazole is reported to be a good clinical safety profile antipsychotic. However, recent data suggest that the risk of tardive dyskinesia could be higher than initially thought. We report the case of aripiprazole-induced tardive dyskinesia with dramatic evolution in a patient with several risk factors, including older age and exposure to antipsychotic over a period longer than six months. This case and its dramatic evolution, associated with other cases recently published, suggest reconsi...

  14. Relative bioavailability and safety of aripiprazole lauroxil, a novel once-monthly, long-acting injectable atypical antipsychotic, following deltoid and gluteal administration in adult subjects with schizophrenia.

    Science.gov (United States)

    Turncliff, Ryan; Hard, Marjie; Du, Yangchun; Risinger, Robert; Ehrich, Elliot W

    2014-11-01

    Aripiprazole lauroxil is a linker lipid ester of aripiprazole for extended-release intramuscular (IM) injection. This multicenter, randomized, open-label study evaluated the pharmacokinetics (PK), relative bioavailability, and tolerability of a single IM deltoid or gluteal injection of aripiprazole lauroxil in adult subjects with chronic stable schizophrenia or schizoaffective disorder. Forty-six subjects were randomized 1:1 to aripiprazole lauroxil 441 mg IM in the deltoid or gluteal muscle. Samples were collected through 89 days post-dose to measure levels of aripiprazole lauroxil, N-hydroxymethyl aripiprazole, aripiprazole, and dehydro-aripiprazole. Forty-three (93.5%) subjects completed all study assessments; most were CYP2D6 extensive or immediate metabolizers (96%); two (4%) were poor metabolizers. The PK of aripiprazole following aripiprazole lauroxil was characterized by a steady rise in plasma concentrations (Tmax 44-50 days), a broad peak, and prolonged exposure attributable to the dissolution of aripiprazole lauroxil and formation rate-limited elimination of aripiprazole (t1/2=15.4-19.2 days). Deltoid vs. gluteal administration resulted in slightly higher Cmax aripiprazole concentrations [1.31 (1.02, 1.67); GMR 90% CI]; total exposure (AUCinf) was similar between sites of administration [0.84 (0.57, 1.24)]. N-hydroxymethyl-aripiprazole and dehydro-aripiprazole exposures were 10% and 33-36%, respectively, of aripiprazole exposure following aripiprazole lauroxil. The most common adverse events were injection site pain in 20 subjects (43.5%) and headache in 6 subjects (13.0%) of mild intensity occurring at a similar rate with deltoid and gluteal administration. Exposure ranges with deltoid and gluteal administration overlapped, suggesting that these sites may be used interchangeably. Despite a higher incidence of adverse events, deltoid muscle provides a more accessible injection site and could facilitate patient acceptance.

  15. Aripiprazole: a review of its use in the treatment of irritability associated with autistic disorder patients aged 6-17.

    Science.gov (United States)

    Douglas-Hall, Petrina; Curran, Sarah; Bird, Victoria; Taylor, David

    2011-01-01

    A systematic review and meta-analysis were performed examining the efficacy of aripiprazole for the treatment of irritability associated with autistic disorder in children and adolescents. Aripiprazole was found to be more effective in reducing irritability compared with placebo at 8 weeks, SMD -0.64 [-0.90 to -0.39, P autism. Long-term studies are required to determine the efficacy and safety of aripiprazole in autistic disorder in children.

  16. Systems pharmacology-based approach for dissecting the active ingredients and potential targets of the Chinese herbal Bufei Jianpi formula for the treatment of COPD

    Science.gov (United States)

    Zhao, Peng; Li, Jiansheng; Li, Ya; Tian, Yange; Wang, Yonghua; Zheng, Chunli

    2015-01-01

    Background The Chinese herbal Bufei Jianpi formula (BJF) provides an effective treatment option for chronic obstructive pulmonary disease (COPD). However, the systems-level mechanism underlying the clinical effects of BJF on COPD remains unknown. Methods In this study, a systems pharmacology model based on absorption filtering, network targeting, and systems analyses was applied specifically to clarify the active compounds and therapeutic mechanisms of BJF. Then, a rat model of cigarette smoke- and bacterial infection-induced COPD was used to investigate the therapeutic mechanisms of BJF on COPD and its comorbidity. Results The pharmacological system successfully identified 145 bioactive ingredients from BJF and revealed 175 potential targets. There was a significant target overlap between the herbal constituents of BJF. These results suggested that each herb of BJF connected with similar multitargets, indicating potential synergistic effects among them. The integrated target–disease network showed that BJF probably was efficient for the treatment of not only respiratory tract diseases but also other diseases, such as nervous system and cardiovascular diseases. The possible mechanisms of action of BJF were related to activation of inflammatory response, immune responses, and matrix metalloproteinases, among others. Furthermore, we demonstrated that BJF treatment could effectively prevent COPD and its comorbidities, such as ventricular hypertrophy, by inhibition of inflammatory cytokine production, matrix metalloproteinases expression, and other cytokine production in vivo. Conclusion This study using the systems pharmacology method, in combination with in vivo experiments, helped us successfully dissect the molecular mechanism of BJF for the treatment of COPD and predict the potential targets of the multicomponent BJF, which provides a new approach to illustrate the synergetic mechanism of the complex prescription and discover more effective drugs against COPD

  17. Altered Gene Expression in the Schistosome-Transmitting Snail Biomphalaria glabrata following Exposure to Niclosamide, the Active Ingredient in the Widely Used Molluscicide Bayluscide.

    Directory of Open Access Journals (Sweden)

    Si-Ming Zhang

    Full Text Available In view of the call by the World Health Organization (WHO for elimination of schistosomiasis as a public health problem by 2025, use of molluscicides in snail control to supplement chemotherapy-based control efforts is likely to increase in the coming years. The mechanisms of action of niclosamide, the active ingredient in the most widely used molluscicides, remain largely unknown. A better understanding of its toxicology at the molecular level will both improve our knowledge of snail biology and may offer valuable insights into the development of better chemical control methods for snails. We used a recently developed Biomphalaria glabrata oligonucleotide microarray (31K features to investigate the effect of sublethal exposure to niclosamide on the transcriptional responses of the snail B. glabrata relative to untreated snails. Most of the genes highly upregulated following exposure of snails to niclosamide are involved in biotransformation of xenobiotics, including genes encoding cytochrome P450s (CYP, glutathione S-transferases (GST, and drug transporters, notably multi-drug resistance protein (efflux transporter and solute linked carrier (influx transporter. Niclosamide also induced stress responses. Specifically, six heat shock protein (HSP genes from three super-families (HSP20, HSP40 and HSP70 were upregulated. Genes encoding ADP-ribosylation factor (ARF, cAMP response element-binding protein (CREB and coatomer, all of which are involved in vesicle trafficking in the Golgi of mammalian cells, were also upregulated. Lastly, a hemoglobin gene was downregulated, suggesting niclosamide may affect oxygen transport. Our results show that snails mount substantial responses to sublethal concentrations of niclosamide, at least some of which appear to be protective. The topic of how niclosamide's lethality at higher concentrations is determined requires further study. Given that niclosamide has also been used as an anthelmintic drug for decades and

  18. Aripiprazole for treating irritability in children & adolescents with autism: A systematic review

    Directory of Open Access Journals (Sweden)

    Ahmad Ghanizadeh

    2015-01-01

    Full Text Available Background & objectives: No clear therapeutic benefits of antipsychotics have been reported for the treatment of behavioural symptoms in autism. This systematic review provides an assessment of evidence for treating irritability in autism by aripiprazole. Methods: The databases of MEDLINE/PubMed and Google Scholar were searched for relevant articles about the effect of aripiprazole in children with autism. The articles were searched according to the inclusion and exclusion criteria specifed for this review. All the double-blind, controlled, randomized, clinical trials examining the efficacy of aripiprazole for treating children and adolescents with autism were included. Results: From the 93 titles identified, 26 were irrelevant and 58 were evaluated for more details. Only five articles met the inclusive criteria. The evidence from precise randomized double blind clinical trials of aripiprazole for the treatment of autism in children and adolescents was convincing enough to recommend aripiprazole. Adverse effects were not very common and were usually mild. Interpretation & conclusions: Current evidence suggests that aripiprazole is as effective and safe as risperidone for treating irritability in autism. However, further studies with larger sample size and longer duration are required.

  19. In-vitro examination of the positive inotropic effect of caffeine and taurine, the two most frequent active ingredients of energy drinks.

    Science.gov (United States)

    Chaban, R; Kornberger, A; Branski, N; Buschmann, K; Stumpf, N; Beiras-Fernandez, A; Vahl, C F

    2017-08-10

    Our study aimed to evaluate changes in the contractile behavior of human myocardium after exposure to caffeine and taurine, the main active ingredients of energy drinks (EDs), and to evaluate whether taurine exhibits any inotropic effect at all in the dosages commonly used in EDs. Myocardial tissue was removed from the right atrial appendages of patients undergoing cardiac surgery and prepared to obtain specimens measuring 4 mm in length. A total of 92 specimens were exposed to electrical impulses at a frequency of 75 bpm for at least 40 min to elicit their maximum contractile force before measuring the isometric contractile force (ICF) and duration of contraction (CD). Following this, each specimen was treated with either taurine (group 1, n = 29), or caffeine (group 2, n = 31) or both (group 3, n = 32). After exposure, ICF and CD measuring were repeated. Post-treatment values were compared with pre-treatments values and indicated as percentages. Exposure to taurine did not alter the contraction behavior of the specimens. Exposure to caffeine, in contrast, led to a significant increase in ICF (118 ± 03%, p caffeine and taurine also induced a statistically significant increase in ICF (124 ± 4%, p caffeine was similar to that achieved by a combination of both caffeine and taurine (p = 0.2). The relative ICF levels achieved by administration of caffeine and a combination of taurine and caffeine, respectively, were both significantly higher (p caffeine altered the contraction behavior of the specimen significantly in our in-vitro model, taurine did not exhibit a significant effect. Adding taurine to caffeine did not significantly enhance or reduce the effect of caffeine.

  20. Development and validation of a stability-indicating reverse phase ultra performance liquid chromatographic method for the estimation of nebivolol impurities in active pharmaceutical ingredients and pharmaceutical formulation.

    Science.gov (United States)

    Thummala, Veera Raghava Raju; Lanka, Mohana Krishna

    2015-10-01

    A sensitive, stability-indicating gradient reverse phase ultra performance liquid chromatographic method has been developed for the quantitative estimation of nebivolol impurities in active pharmaceutical ingredient (API) and pharmaceutical formulation. Efficient chromatographic separation was achieved on an Acquity BEH C18 column (100 mm x 2.1 mm, 1.7 μm) with mobile phase of a gradient mixture. The flow rate of the mobile phase was 0.18 mL/min with column temperature of 30 degrees C and detection wavelength of 281 nm. The relative response factor values of (R*)-2-( benzylamino)-1-((S*)-6-fluorochroman-2-yl) ethanol ((R x S*) NBV-), (R)-1-((R)-6-fluorochroman-2-yl)-2-((S)-2-((S)-6-fluoro-chroman-2-yl)-2-hydroxyethyl-amino) ethanol ((RRSS) NBV-3), 1-(chroman-2-yl)-2-(2-(6-fluorochroman-2-yl)-2-hydroxyethyl amino) ethanol (monodesfluoro impurity), (S)-1-((R)-6-fluorochroman-2-yl)-2-((R)-2 (S*)-6-fluoro-chroman-2-yl)-2-hydroxyethylamino) ethanol hydrochloride ((RSRS) NBV-3) and (R*)-1-((S*)-6-fluorochroman-2-yl)-2-((S*)-2-((S*)-6-fluoro-chroman-2-yl)-2-hydroxyethylamino) ethanol ((R* S* S* S*) NBV-2) were 0.65, 0.91, 0.68, 0.92 and 0.91 respectively. Nebivolol formulation sample was subjected to the stress conditions of acid, base, oxidative, hydrolytic, thermal, humidity and photolytic degradation. Nebivolol was found to degrade significantly under peroxide stress condition. The degradation products were well resolved from nebivolol and its impurities. The peak purity test results confirmed that the nebivolol peak was homogenous and pure in all stress samples and the mass balance was found to be more than 98%, thus proving the stability-indicating power of the method. The developed method was validated according to International Conference on Hormonization (ICH) guidelines with respect to specificity, linearity, limits of detection and quantification, accuracy, precision and robustness.

  1. Dynamics of active pharmaceutical ingredients loads in a Swiss university hospital wastewaters and prediction of the related environmental risk for the aquatic ecosystems.

    Science.gov (United States)

    Daouk, Silwan; Chèvre, Nathalie; Vernaz, Nathalie; Widmer, Christèle; Daali, Youssef; Fleury-Souverain, Sandrine

    2016-03-15

    The wastewater contamination of a Swiss university hospital by active pharmaceutical ingredient (API) residues was evaluated with a three months monitoring campaign at the outlet of the main building. Flow-proportional samples were collected with an automatic refrigerated sampler and analyzed for 15 API, including antibiotics, analgesics, antiepileptic and anti-inflammatory drugs, by using a validated LC-MS/MS method. The metals Gd and Pt were also analyzed using ICP-MS. Measured concentrations were compared to the predicted ones calculated after the drug average consumption data obtained from the hospital pharmacy. The hospital contribution to the total urban load was calculated according to the consumption data obtained from city pharmacies. Lastly, the environmental hazard and risk quotients (RQ) related to the hospital fraction and the total urban consumption were calculated. Median concentrations of the 15 selected compounds were ranging from 0.04 to 675 μg/L, with a mean detection frequency of 84%. The ratio between predicted and measured environmental concentrations (PEC/MEC) has shown a good accuracy for 5 out of 15 compounds, revealing over- and under-estimations of the PEC model. Mean daily loads were ranging between 0.01 and 14.2g/d, with the exception of paracetamol (109.7 g/d). The hospital contribution to the total urban loads varied from 2.1 to 100% according to the compound. While taking into account dilution and removal efficiencies in wastewater treatment plant, only the hospital fraction of the antibiotics ciprofloxacin and sulfamethoxazole showed, respectively, a high (RQ>1) and moderate (RQ>0.1) risk for the aquatic ecosystems. Nevertheless, when considering the total urban consumption, 7 compounds showed potential deleterious effects on aquatic organisms (RQ>1): gabapentin, sulfamethoxazole, ciprofloxacin, piperacillin, ibuprofen, diclofenac and mefenamic acid. In order to reduce inputs of API residues originating from hospitals various

  2. Stability indicating LC method for rapid determination of related substances of O-desmethyl venlafaxine in active pharmaceutical ingredients and pharmaceutical formulations.

    Science.gov (United States)

    Rao, Karri Visweswara; Reddy, Kesareddy Padmaja; Kumar, Yelavarthi Ravindra

    2014-01-01

    A simple, precise and accurate stability-indicating reversed phase-high performance liquid chromatography method was developed for the quantitative determination of O-desmethyl venlafaxine (ODV) and its related substances in active pharmaceutical ingredient and pharmaceutical formulation. The method was developed using YMC-pack ODS-A (150 × 4.6 mm, 3 μm) column with mobile phase containing a gradient mixture of solvents A and B. Solvent A contained a mixture of buffer and acetonitrile in the ratio of 85:15 (v/v). The buffer consisted of 10 mM potassium dihydrogen phosphate and 2 mM 1-octane sulfonic acid sodium salt (pH adjusted to 6.0 by using diluted potassium hydroxide solution). Solvent B contained a mixture of water and acetonitrile in the ratio of 20:80 (v/v). The eluted compounds were monitored at 230 nm. ODV and its six impurities were well separated within 14 min run time. It was subjected under the stress conditions of oxidative, acid, base, water, thermal and photolytic degradation. It was sensitive towards acidic, basic, oxidative and water stress conditions, stable in photolytic and thermal degradation conditions. The degradation products were well resolved from main peak and its impurities, the mass balance in each case was >99.0%, proving the stability-indicating power of the method. The developed method was validated as per International Conference on Harmonization (ICH) guidelines with respect to its specificity, linearity (correlation coefficient >0.9996), limit of detection, limit of quantification, accuracy (recovery range 97.1-103.2%), precision (% relative standard deviation ≤1.9%) and robustness.

  3. INGREDIENT BRANDING - A GROWTH OPPORTUNITY?

    OpenAIRE

    Anca BUTNARIU

    2017-01-01

    Co-branding is an increasingly used strategy, consisting of marketing products representing two brands or more. Ingredient branding fits in the scope of co-branding, consisting of the inclusion of key attributes of one brand into another brand as ingredients. Ingredient branding is one of the many brand strategies used in marketing to provide differentiation criteria for the customers. In recent years, its importance and incidence have dramatically increased Extant research provides disparate...

  4. 21 CFR 310.529 - Drug products containing active ingredients offered over-the-counter (OTC) for oral use as insect...

    Science.gov (United States)

    2010-04-01

    ... offered over-the-counter (OTC) for oral use as insect repellents. 310.529 Section 310.529 Food and Drugs... ingredients offered over-the-counter (OTC) for oral use as insect repellents. (a) Thiamine hydrochloride... insect repellent (an orally administered drug product intended to keep insects away). There is a lack...

  5. Systems pharmacology-based approach for dissecting the active ingredients and potential targets of the Chinese herbal Bufei Jianpi formula for the treatment of COPD

    Directory of Open Access Journals (Sweden)

    Zhao P

    2015-12-01

    Full Text Available Peng Zhao,1,2 Jiansheng Li,1,2 Ya Li,1,2 Yange Tian,1,2 Yonghua Wang,2,3 Chunli Zheng3 1Key Laboratory of Chinese Internal Medicine, Henan University of Traditional Chinese Medicine, 2Key Laboratory of Chinese Internal Medicine, Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment and Chinese Medicine Development of Henan Province, Zhengzhou, 3Center of Bioinformatics, College of Life Science, Northwest A&F University, Yangling, People’s Republic of China Background: The Chinese herbal Bufei Jianpi formula (BJF provides an effective treatment option for chronic obstructive pulmonary disease (COPD. However, the systems-level mechanism underlying the clinical effects of BJF on COPD remains unknown. Methods: In this study, a systems pharmacology model based on absorption filtering, network targeting, and systems analyses was applied specifically to clarify the active compounds and therapeutic mechanisms of BJF. Then, a rat model of cigarette smoke- and bacterial infection-induced COPD was used to investigate the therapeutic mechanisms of BJF on COPD and its comorbidity. Results: The pharmacological system successfully identified 145 bioactive ingredients from BJF and revealed 175 potential targets. There was a significant target overlap between the herbal constituents of BJF. These results suggested that each herb of BJF connected with similar multitargets, indicating potential synergistic effects among them. The integrated target–disease network showed that BJF probably was efficient for the treatment of not only respiratory tract diseases but also other diseases, such as nervous system and cardiovascular diseases. The possible mechanisms of action of BJF were related to activation of inflammatory response, immune responses, and matrix metalloproteinases, among others. Furthermore, we demonstrated that BJF treatment could effectively prevent COPD and its comorbidities, such as ventricular hypertrophy, by inhibition

  6. Clinical Effectiveness of Aripiprazole in Short-term Treatment of Tic Disorder in Children and Adolescents: A Naturalistic Study

    Directory of Open Access Journals (Sweden)

    Che-Sheng Ho

    2014-02-01

    Conclusion: Aripiprazole is effective for short-term treatment of TD, especially vocal tics, in children and adolescents with mild adverse effects. However, further double-blind trials against placebo or other medications are needed to verify the efficacy of aripiprazole in the pharmacotherapy of TD.

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

    Science.gov (United States)

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

    2015-06-20

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

  8. Involvement of serotonergic, noradrenergic and dopaminergic systems in the antidepressant-like effect of ginsenoside Rb1, a major active ingredient of Panax ginseng C.A. Meyer.

    Science.gov (United States)

    Wang, Guo-Li; He, Zhong-Mei; Zhu, Hong-Yan; Gao, Yu-Gang; Zhao, Yan; Yang, He; Zhang, Lian-Xue

    2017-05-23

    Ginsenoside Rb1, a 20 (S)-protopanaxadiol, is a major active ingredient of Panax ginseng C.A. Meyer, which as the King of Chinese herbs, has been wildly used for the treatment of central nervous system diseases. Previous studies have shown that 20 (S)-protopanaxadiol possesses a novel antidepressant-like effect in the treatment of depression, whereas ginsenoside Rb1 in depression has been rarely reported. The present study was to investigate the antidepressant-like effect of ginsenoside Rb1 and its relevant mechanisms. The whole experiment was divided into two parts: one part we examined the antidepressant-like effect of ginsenoside Rb1 with open-field test (OFT), tail suspension test (TST), forced swim test (FST), 5-HTP induced head-twitch and reserpine response in mice, another part we used chronic unpredicted mild stress (CUMS) model to further explore the antidepressant-like effect of ginsenoside Rb1 with caffeine, fluoxetine and p-Chlorophenylalanine (PCPA) in rats. Furthermore, the levels of monoamine neurotransmitters of NE, 5-HT, DA and their metabolites 5-HIAA, DOPAC, HVA were all measured by ELISA kits after the CUMS protocol. Our data indicated that 7 days treatment with ginsenoside Rb1 (4, 8, 10mg/kg, p.o.) significantly decreased immobility time in the FST and TST in mice, and played important roles in mice which were induced by 5-HTP (200mg/kg, i.p.) and reserpine (4mg/kg, i.p.). On the basis of CUMS model, 21 days treatment with ginsenoside Rb1 not only had effective interactions with caffeine (5mg/kg, i.p.), fluoxetine (1mg/kg, i.p.) and PCPA (100mg/kg, i.p.), but also significantly up-regulated the 5-HT, 5-HIAA, NE and DA levels in CUMS rats' brain, whereas HVA and DOPAC had no significant difference. Moreover, there was no alteration in spontaneous locomotion in any experimental group. These results suggest that ginsenoside Rb1 exhibits significant antidepressant-like effect in behavioral tests, chronic animal model and drug interactions, its

  9. Water soluble active ingredients of Danshen--review on the Salvianolic acids%丹参水溶性有效成分--丹酚酸研究进展

    Institute of Scientific and Technical Information of China (English)

    杜冠华; 张均田

    2000-01-01

    Danshen-Radix Salviae Miltiorrhizae,is one of the common traditional Chinese medicines,which has been used clinically in the treatment of cardiovascular diseases more than 20 centuries.The active ingredients of Danshen has been researched 5 decades by the modern methods.Many researchers investigated the pharmacological effects of water soluble ingredients of Danshen-salvianolic acids in vivo and in vitro.The results demonstrated that salvianolic acids have different pharmacological effects such as potent antioxidative effects,scavenging free radicals,protect neural cells against injuries caused by anoxia, etc.In present paper,the pharmacological effects of salvianolic acids and the mechanisms of their actions are reviewed based on the research results obtained in our laboratory and other authors.

  10. Application of Natural Ingredients to Preventive Medicine.

    Science.gov (United States)

    Yokota, Junko

    2017-01-01

     The super-aging society in Japan is currently experiencing growing demand for treatments that improve health and longevity. To develop new high-functional foods and search for pharmaceutical candidates among foods and natural products, it is necessary to promote organic collaboration among researchers in pharmacy, medicine, nutrition, and other fields to encourage joint utilization of their technologies. Recently, attempts have been made to use numerous foods and natural products to prevent or treat diseases based on scientific evidence. We have been endeavoring to develop preventive medicines from foods and natural ingredients by engaging in relevant activities such as screening these substances to determine the structures of their effective ingredients, verifying pharmacological activities, and conducting clinical trials. In this study, the effectiveness of Goishi tea (postfermented tea) and Flos Lonicerae (Japanese honeysuckle) for metabolic syndrome and hepatic disorders, respectively, was explored. Multicomponent foods and natural ingredients have diverse effects produced by the actions of individual components as well as the interactions among different components. Additionally, when using natural ingredients and similar materials, it is necessary to consider the different extraction efficiencies of various methods and their absorption, deposition, metabolism, and excretion after consumption. The influence of intestinal bacteria and other factors is also critical. In our study, the administration of Goishi tea and Flos Lonicerae in animal models of disease demonstrated high functionality. Based on these findings, we plan to conduct further investigations, including clinical studies in human participants, focusing on the potential usefulness of Goishi tea and Flos Lonicerae as functional foods.

  11. Pharmacodynamic Study and Active Ingredient of Endophyte in Medicinal Plants%药用植物内生菌活性成分及药效学研究进展

    Institute of Scientific and Technical Information of China (English)

    丁仁伟; 邓毅

    2012-01-01

    查阅国内外近年相关文献,对药用植物内生菌代谢产物的种类及药效进行分析总结,概述药用植物内生菌的活性成分和药效学研究现状,提出药用植物内生菌可产生多种活性成分和药理作用,此项研究对于解决药用植物资源匮乏和发现新成分、新疗效具有重要价值.%Metabolites types of endophytes in medicinal plants and efficacy were analyzed and summarized; active ingredient and pharmacodynamic study of endophytes in medicinal plants were outlined through consulting associated literature at home and abroad in recent years, endophytes in medicinal plants can produce many kinds of active ingredients and pharmacological action. The study is valuable for covering scarcity of medicinal plants and discovering new ingredient and curative effects.

  12. Comparison the effectiveness of aripiprazole and risperidone for the treatment of acute bipolar mania

    Directory of Open Access Journals (Sweden)

    Amir Akhavan Rezayat

    2014-01-01

    Full Text Available Background: Second-generation antipsychotics, approved for the treatment of mania, are associated with adverse effects such as weight gain and metabolic disorders. Aripiprazole, a recently introduced second-generation antipsychotic, are thought to account for its low propensity for weight gain, metabolic disturbances and sedation. The purpose of this study was to investigate the effect of risperidone versus aripiprazole in the treatment of acute mania. Materials and Methods: Fifty patients with acute episodes of mania were enrolled in this study, and they were randomly assigned into a risperidone group of 24 cases and an aripiprazole group of 26 cases. In group A, aripiprazole with a dose of 5-30 mg/day and in group B, risperidone with a dose of 2-8 mg/day was given to patients. The average dose of aripiprazole was 27 mg/day, and the average dose of risperidone was 6 mg/day. The effects of each drug for the treatment of acute mania were assessed on the 1 st day of admission and on days 2, 4, 6, 8 and at weeks 2, 4 and 6 after therapy using the young mania rating scale (YMRS and at the baseline and on weeks 3 and 6 after admission using the clinical global impression (CGI scale. Results: The mean age of the group of risperidone was 34 ± 8.6 years and in a group of aripiprazole it was 34 ± 9.1 years (P = 0.83. Comparison of YMRS scores over the period of 6 weeks revealed a statistically significant difference in both groups (P < 0.0001.There was also a statistically significant difference in YMRS scores between risperidone and aripiprazole at day 8 (P = 0.026 and weeks 2 (P = 0.035 and 4 (P = 0.042. There was also a statistically significant difference in CGI-Severity scale score at weeks 3 (P = 0.003 and 6 (P = 0.000 and in CGI-Improvement scale score at weeks 3 (P = 0.005 and 6 (P = 0.002. The most common side-effect observed in both groups was headache (0%15/4 in aripiprazole vs. %16/7 in risperidone Conclusion: Aripiprazole that is readily

  13. Profile of aripiprazole in the treatment of bipolar disorder in children and adolescents.

    Science.gov (United States)

    Kirino, Eiji

    2014-01-01

    Bipolar disorder is a pernicious illness. Compared with the later-onset form, early onset bipolar disorder is associated with worse psychosocial outcomes, and is characterized by rapid cycling and increased risks of substance abuse and suicide attempts. Controlling mood episodes and preventing relapse in this group of pediatric patients requires careful treatment. Here, we review the effectiveness of aripiprazole for bipolar disorder in children and adolescents, with discussion of this drug's unique pharmacological profile and various clinical study outcomes. Aripiprazole acts as a serotonin 5-HT2A receptor antagonist, as well as a partial agonist of the serotonin 5-HT1A and dopamine D2 receptors. It can be safely used in children and adolescents, as it is highly tolerated and shows lower rates of the side effects typically observed with other antipsychotic drugs, including sedation, weight gain, hyperprolactinemia, and extrapyramidal syndrome. The presently reviewed randomized controlled trials (RCTs) and non-RCTs generally reported aripiprazole to be effective and well-tolerated in children and adolescents with bipolar disorder. However, due to the limited number of RCTs, the present conclusions must be evaluated cautiously. Furthermore, aripiprazole cannot yet be considered a preferred treatment for children and adolescents with bipolar disorder, as there is not yet evidence that aripiprazole shows greater efficacy compared to other second-generation antipsychotics. Additional data are needed from future head-to-head comparison studies.

  14. A randomized trial of aripiprazole vs blonanserin for the treatment of acute schizophrenia and related disorders.

    Science.gov (United States)

    Kishi, Taro; Matsuda, Yuki; Matsunaga, Shinji; Mukai, Tomohiko; Moriwaki, Masatsugu; Tabuse, Hideaki; Fujita, Kiyoshi; Iwata, Nakao

    2016-01-01

    There has been no direct comparison of aripiprazole and blonanserin for schizophrenia treatment. We conducted a 24-week, rater-masked, randomized trial of aripiprazole (6-30 mg/d) vs blonanserin (4-24 mg/d) in schizophrenia patients who were not taking any antipsychotic medication for more than 2 weeks before enrollment (UMIN000011194). The primary outcome measure for efficacy was improvement of Positive and Negative Syndrome Scale (PANSS) total score at week 24. Secondary outcomes were PANSS subscale scores, 21-item Hamilton Rating Scale for Depression (HAMD-21) score, response rate, discontinuation rate, and individual adverse events. Forty-four patients were recruited. The discontinuation rate was 86.4% in the aripiprazole group and 68.2% in the blonanserin treatment group. There was no significant difference in mean time to discontinuation between the groups. Although both treatment groups showed significant reductions in the PANSS total score, PANSS subscale scores, and HAMD-21 scores at week 24, the magnitudes of the changes did not differ between the groups. There were no significant differences in the incidences of adverse events including somnolence, extrapyramidal symptoms, prolactin-related adverse events, and weight change between the groups. Our results suggest similar efficacy and safety profiles of aripiprazole and blonanserin in the patients with schizophrenia. Double-blind controlled studies are needed to further explore the efficacy and safety of aripiprazole and blonanserin in schizophrenia.

  15. Dilemma of prescribing aripiprazole under the Taiwan health insurance program: a descriptive study

    Science.gov (United States)

    Hsu, Yi-Chien; Chou, Yu-Ching; Chang, Hsin-An; Kao, Yu-Chen; Huang, San-Yuan; Tzeng, Nian-Sheng

    2015-01-01

    Objectives Refractory major depressive disorder (MDD) is a serious problem leading to a heavy economic burden. Antipsychotic augmentation treatment with aripiprazole and quetiapine is approved for MDD patients and can achieve a high remission rate. This study aimed to examine how psychiatrists in Taiwan choose medications and how that choice is influenced by health insurance payments and administrative policy. Design Descriptive study. Outcome measures Eight questions about the choice of treatment strategy and atypical antipsychotics, and the reason to choose aripiprazole. Intervention We designed an augmentation strategy questionnaire for psychiatrists whose patients had a poor response to antidepressants, and handed it out during the annual meeting of the Taiwanese Society of Psychiatry in October 2012. It included eight questions addressing the choice of treatment strategy and atypical antipsychotics, and the reason whether or not to choose aripiprazole as the augmentation antipsychotic. Results Choosing antipsychotic augmentation therapy or switching to other antidepressant strategies for MDD patients with an inadequate response to antidepressants was common with a similar probability (76.1% vs 76.4%). The most frequently used antipsychotics were aripiprazole and quetiapine, however a substantial number of psychiatrists chose olanzapine, risperidone, and sulpiride. The major reason for not choosing aripiprazole was cost (52.1%), followed by insurance official policy audit and deletion in the claims review system (30.1%). Conclusion The prescribing behavior of Taiwanese psychiatrists for augmentation antipsy-chotics is affected by health insurance policy. PMID:25657586

  16. Pregnancy exposure to olanzapine, quetiapine, risperidone, aripiprazole and risk of congenital malformations. A systematic review

    DEFF Research Database (Denmark)

    Ennis, Zandra Nymand; Damkier, Per

    2015-01-01

    To review available data on first-trimester exposure to olanzapine, quetiapine, risperidone and aripiprazole and risk of congenital malformations. We performed a systematic literature search in accordance with PRISMA guidelines identifying studies containing original data on first......-trimester exposure and pregnancy outcome with respect to congenital malformations. Cumulated data for olanzapine were 1090 first-trimester-exposed pregnancies with 38 malformations resulting in a malformation rate of 3.5%. The corresponding numbers for quetiapine, risperidone and aripiprazole were 443/16 (3.6%), 432...... of congenital malformation. Data for quetiapine and risperidone do not suggest a substantially increased risk, while the risk estimate for aripiprazole remains imprecise owing to a low amount of data....

  17. Add-on treatment of aripiprazole in an adult onychophagia patient

    Directory of Open Access Journals (Sweden)

    Mehmet Cemal Kaya

    2012-12-01

    Full Text Available Nail biting (onychophagia is a common disorder whichhas not been investigated yet. There are different opinionsabout to classify onychophagia, but according toDSM-IV-TR it is classified as impulse control disorder nototherwise specified. The knowledge about treatment ofonychophagia is limited. There are a few studies abouttreatment of onychophagia with psychotherapy and astudy with pharmacotherapy. Some studies suggest thatan atypical antipsychotic aripiprazole may have beneficialeffects in the treatment of impulse control disorders. Inthis study we report a case of onychophagia which hassuccessfully treated with aripiprazole add-on to escitalopramtreatment that has never reported before. J Clin ExpInvest 2012; 3(4: 545-547Key words: Onychophagia, aripiprazole, add-on treatment

  18. Low dosage of aripiprazole induced neuroleptic malignant syndrome after interaction with other neuroleptic drugs

    Directory of Open Access Journals (Sweden)

    Albino Petrone

    2013-09-01

    Full Text Available Aripiprazole is a 2nd generation antipsychotic medication, atypical neuroleptic used for treatment of schizophrenia improving symptoms such as hallucinations, delusions, and disorganized thinking. A potentially fatal symptom complex sometimes referred to as neuroleptic malignant syndrome (NMS has been reported in association with administration of antipsychotic drugs, including aripiprazole. Rare cases of NMS occurred during aripiprazole treatment in the worldwide clinical database. The disease is characterized by a distinctive clinical syndrome of mental status change, rigidity, fever, and dysautonomia. We report on a 63-year old woman with depression syndrome who developed neuroleptic malignant syndrome after twelve days of aripripazole 5 mg per day. Our case is added to the small number already described and suggests the need for caution when aripripazole is added to increase the effect of other antipsychotics.

  19. Covert dyskinesia associated with aripiprazole: a case report and review of the literature.

    Science.gov (United States)

    Moseley, Carrie N; Simpson-Khanna, Heather A; Catalano, Glenn; Catalano, Maria C

    2013-01-01

    The atypical antipsychotic agents are felt by many to have a lower risk of inducing the development of dyskinetic movements than the conventional antipsychotic agents agents such as haloperidol and fluphenazine. However, that does not mean that treatment with the atypical antipsychotic agents carries no risk of developing dyskinesias. To the contrary, all of the atypical antipsychotic agents, including aripiprazole, have been associated with the induction of dyskinetic movements. We will present the case of a patient who developed a covert dyskinesia that manifested shortly after the discontinuation of aripiprazole. We will review the use of aripiprazole and the adverse effects most commonly associated with its use. We will also discuss the risk factors associated with the development of tardive dyskinesia and review the different clinical variations (withdrawal dyskinesia, covert dyskinesia, tardive diskinesia) of medication-induced dyskinesias.

  20. Aripiprazole in the acute and maintenance phase of bipolar I disorder

    Directory of Open Access Journals (Sweden)

    Zupancic M

    2012-01-01

    Full Text Available Melanie Zupancic1, Misty L Gonzalez2,31Southern Illinois University School of Medicine, 2Division of Medicine Psychiatry, Southern Illinois University School of Medicine, 3Southern Illinois University Edwardsville School of Pharmacy, Southern Illinois University Edwardsville, Springfield, IL, USAAbstract: Bipolar affective disorder is a disabling illness with substantial morbidity and many management challenges. Traditional mood stabilizers such as lithium, valproate, and carbamazepine are often inadequate in controlling symptoms both during the acute and maintenance phase of treatment. Aripiprazole is a second-generation antipsychotic with a unique mechanism of action. Evidence suggests that it is effective in acute manic and mixed states. There are limited data to suggest its efficacy as a maintenance agent. Future studies will be needed to better define the role of aripiprazole relative to other traditional pharmacologic agents.Keywords: aripiprazole, bipolar disorder, acute treatment, maintenance treatment

  1. Augmentation of Clozapine with Aripiprazole in Severe Psychotic Bipolar and Schizoaffective Disorders: A Pilot Study

    Science.gov (United States)

    Benedetti, Alessandra; Di Paolo, Antonello; Lastella, Marianna; Casamassima, Francesco; Candiracci, Chiara; Litta, Antonella; Ciofi, Laura; Danesi, Romano; Lattanzi, Lorenzo; Del Tacca, Mario; Cassano, Giovanni Battista

    2010-01-01

    Aim: To evaluate the efficacy and safety of the augmentation of clozapine with aripiprazole in patients with treatment-resistant schizoaffective and psychotic bipolar disorders in a retrospective manner. Pharmacodynamic and pharmacokinetic interactions between the two drugs were also investigated. Patients: Three men and 4 women (median age 36 and 40 years, respectively) who had mean scores at BPRS and CGI-Severity of 59.1±12.0 and 5.4±0.5, respectively, were treated with clozapine (mean dose 292.9±220.7 mg/day). Patients received an adjunctive treatment with aripiprazole (mean dose 6.8 ± 3.7 mg/day). Clozapine, norclozapine and aripiprazole plasma levels were measured by means of a high performance liquid chromatograpy with UV detection. Results: Total scores at BPRS decreased significantly (from 59.1±12.0 to 51.1±15.6, p=0.007) after aripirazole augmentation. In particular, the factors “thought disorder” (from 10.4±4.4 to 9.0±4.5, p=.047) and “anergia” (from 10.0±2.7 to 8.0±2.4, p=.018) significantly improved. Concomitant administration of aripiprazole and clozapine did not result in an increase in side effects over the period of treatment. Dose-normalized plasma levels of both clozapine and norclozapine and the clozapine/norclozapine metabolic ratio in all patients did not vary as well. Conclusion: The augmentation of clozapine with aripirazole was safe and effective in severe psychotic schizoaffective and bipolar disorders which failed to respond to atypical antipsychotics. A possible pharmacokinetic interaction between clozapine and aripiprazole does not account for the improved clinical benefit obtained after aripiprazole augmentation. PMID:20648219

  2. A randomized trial of aripiprazole vs blonanserin for the treatment of acute schizophrenia and related disorders

    Directory of Open Access Journals (Sweden)

    Kishi T

    2016-11-01

    Full Text Available Taro Kishi,1 Yuki Matsuda,1 Shinji Matsunaga,1 Tomohiko Mukai,1,2 Masatsugu Moriwaki,1,2 Hideaki Tabuse,3 Kiyoshi Fujita,2 Nakao Iwata1 1Department of Psychiatry, Fujita Health University School of Medicine, Toyoake, Aichi, 2Department of Psychiatry, Okehazama Hospital, Toyoake, Aichi, 3Department of Psychiatry, Holy Cross Hospital, Toki, Gifu, Japan Objective: There has been no direct comparison of aripiprazole and blonanserin for schizophrenia treatment. We conducted a 24-week, rater-masked, randomized trial of aripiprazole (6-30 mg/d vs blonanserin (4-24 mg/d in schizophrenia patients who were not taking any antipsychotic medication for more than 2 weeks before enrollment (UMIN000011194.Methods: The primary outcome measure for efficacy was improvement of Positive and Negative Syndrome Scale (PANSS total score at week 24. Secondary outcomes were PANSS subscale scores, 21-item Hamilton Rating Scale for Depression (HAMD-21 score, response rate, discontinuation rate, and individual adverse events.Results: Forty-four patients were recruited. The discontinuation rate was 86.4% in the aripiprazole group and 68.2% in the blonanserin treatment group. There was no significant difference in mean time to discontinuation between the groups. Although both treatment groups showed significant reductions in the PANSS total score, PANSS subscale scores, and HAMD-21 scores at week 24, the magnitudes of the changes did not differ between the groups. There were no significant differences in the incidences of adverse events including somnolence, extrapyramidal symptoms, prolactin-related adverse events, and weight change between the groups.Conclusion: Our results suggest similar efficacy and safety profiles of aripiprazole and blonanserin in the patients with schizophrenia. Double-blind controlled studies are needed to further explore the efficacy and safety of aripiprazole and blonanserin in schizophrenia. Keywords: aripiprazole, blonanserin, schizophrenia

  3. INGREDIENT BRANDING - A GROWTH OPPORTUNITY?

    Directory of Open Access Journals (Sweden)

    Anca BUTNARIU

    2017-05-01

    Full Text Available Co-branding is an increasingly used strategy, consisting of marketing products representing two brands or more. Ingredient branding fits in the scope of co-branding, consisting of the inclusion of key attributes of one brand into another brand as ingredients. Ingredient branding is one of the many brand strategies used in marketing to provide differentiation criteria for the customers. In recent years, its importance and incidence have dramatically increased Extant research provides disparate and limited understanding of contexts in which such contracts pay off. Our paper provides an extensive review of literature and research streams in ingredient branding, adding knowledge to theory and help for companies that need to establish and maintain a competitive advantage, by differentiating their offer on the markets they act on, in a globalized economy.

  4. Effect of Different Processing Technology of Acer. Ginnala. Maxim on the Active Ingredients and Antioxidant Activity%加工工艺对苦茶槭有效成分和抗氧化活性的影响

    Institute of Scientific and Technical Information of China (English)

    孔成诚; 方成武; 张传标; 张明燕

    2016-01-01

    To study on the effects of different processing method of Acer. Ginnala. Maxim main active ingredient and antioxidant activity, used Acer Ginnala Maxim as raw material in different processing methods, HPLC method was used to measure main active ingredient content of gallic acid. DPPH method was used to determine the scavenging effect on free radicals. Result showed that Acer. Ginnala. Maxim processing method of Black tea, gallic acid content was ( 18. 49±1. 13) mg/g, higher than processing method of green tea of (12. 45±1. 92) mg/g and dried in shade of (14. 28±1. 13) mg/g. Antioxidant activity of the different processing methods of Acer. Ginnala. Maxim was in the following order:the method of green tea (0. 443 mg/mL) < the method of dried in shade (0. 726 mg/mL) < the method of black tea (1. 286 mg/mL) . From the angle of improve the content of Gallic acid and increased the antioxidant activity, the processing method of black tea was much better.%研究了不同加工工艺对苦茶槭主要活性成分和抗氧化活性的影响,以期筛选最适合苦茶槭加工方式。对所采集的苦茶槭鲜叶以不同加工方式进行加工处理,采取HPLC法对苦茶槭主要有效成分没食子酸含量进行检测。采用DPPH法评价不同加工方法苦茶槭自由基的抗氧化活动。结果显示,采用红茶加工法的苦茶槭没食子酸含量为(18.49依1.13) mg/g高于绿茶加工法(12.45依1.92) mg/g和自然阴干法(14.28依1.13) mg/g。不同加工方法的苦茶槭IC50依次为:绿茶工艺(0.443 mg/mL)<自然阴干(0.726 mg/mL)<红茶工艺(1.286 mg/mL)。从提高苦茶槭没食子酸含量,增加抗氧化活性角度建议采用红茶加工方法。

  5. Aripiprazole in the acute and maintenance phase of bipolar I disorder.

    Science.gov (United States)

    Zupancic, Melanie; Gonzalez, Misty L

    2012-01-01

    Bipolar affective disorder is a disabling illness with substantial morbidity and many management challenges. Traditional mood stabilizers such as lithium, valproate, and carbamazepine are often inadequate in controlling symptoms both during the acute and maintenance phase of treatment. Aripiprazole is a second-generation antipsychotic with a unique mechanism of action. Evidence suggests that it is effective in acute manic and mixed states. There are limited data to suggest its efficacy as a maintenance agent. Future studies will be needed to better define the role of aripiprazole relative to other traditional pharmacologic agents.

  6. Study on the in vitro Antimicrobial Activities of Some Spice Essential Oils and Their Ingredients%香辛料精油及单体的体外抑菌活性研究

    Institute of Scientific and Technical Information of China (English)

    张海江; 王向红; 毛宇豪; 孙佳

    2014-01-01

    The in vitro antimicrobial activities of spice essential oils including Cinnamomum Verum, Syringa oblata, 0riganum vulgare L.and their main ingredients were studied using filter-paper and serial two-fold methods.The common food-borne pathogens and spoilage bacteria including E.coli, staphylococcus aureus, Salmonella, Shigella, S.cerevisiae and B.subtilis were employed as the test strains.Furthermore, the effect of pH value on the antimicrobial activity was investigated.The results indicated that all the spice essential oils and their ingredients showed good in vitro antibacterial activities against all the microbials and the acidic conditions could strengthen the activities of Cinnamomum Verum, Syringa oblata essential oil and their ingredients.%采用滤纸片法和溶液二倍稀释法研究肉桂、丁香、牛至等天然香辛料精油及其单体对大肠杆菌、金黄色葡萄球菌、沙门氏菌、志贺菌、枯草芽孢杆菌等常见食源性致病菌、腐败菌的体外抑菌活性,并考察了pH值对抑菌活性的影响。结果表明各精油及其单体对各菌株均具有良好的体外抑制作用,酸性条件有利于增强肉桂、丁香精油及其单体的抑菌活性。

  7. [Antiperspirants and deodorants--ingredients and evaluation].

    Science.gov (United States)

    Lukacs, V A; Korting, H C

    1989-01-01

    Antitranspirants and deodorants gain more and more interest. Aluminium chlorohydrate and aluminium zirkonium tetrachlorohydrate glycine complex are the most frequently used active ingredients in commercial antitranspirants today. Aluminium chloride and propantheline bromide, the anticholinergic substance, are important alternatives although less common. Active ingredients of deodorants are mainly perfumes or bactericidal/bacteriostatic substances, such as triclosan. In addition, there are substances which are meant to bind offending smells (e.g. zinc ricinoleate) or to influence the skin surface pH (e.g. triethyl citrate). As in the cosmetics industry in general, both safety and efficacy of a product are major parameters in the experimental and clinical evaluation. Establishment of efficacy is based on olfactory tests in model situations as well as on the detection of associated effects (e.g. influence on cutaneous microflora).

  8. Aripiprazole versus risperidone for treating children and adolescents with tic disorder: a randomized double blind clinical trial.

    Science.gov (United States)

    Ghanizadeh, Ahmad; Haghighi, Alireza

    2014-10-01

    There are some uncontrolled studies about the efficacy and safety of both aripiprazole and risperidone for treating tic disorder. Moreover, the efficacy of these medications has never been compared. This is the first double blind randomized clinical trial comparing the safety and efficacy of aripiprazole and risperidone for treating patients with tic disorder. Sixty children and adolescents with tic disorder were randomly allocated into one of the two groups to receive either aripiprazole or risperidone for 2 months. The primary outcome measure was the score of Yale Global Tic Severity Scale. In addition, health related quality of life and adverse events were assessed. Both aripiprazole and risperidone decreased the Yale Global Tic Severity Scale score during this trial. Moreover, both medications increased the health related quality of life score. Both aripiprazole and risperidone were tolerated well. Aripiprazole [3.22 (1.9) mg/day] decreased tic score as much as risperidone [0.6 (0.2) mg/day]. Their adverse effects and their effects on health related quality of life were comparable. However, risperidone increased the patients' social functioning more than aripiprazole in short term.

  9. 复方卡力孜然凝胶剂主要活性成分体外经皮渗透%In vitro Percutaneous Penetration of Main Active Ingredient from Fufang Kali Ziran Gel

    Institute of Scientific and Technical Information of China (English)

    邢建国; 王新春; 赵媛; 马建红; 薛桂蓬; 刘桂花

    2012-01-01

    目的:研究不同透皮促进剂对复方卡力孜然凝胶剂3种有效成分体外经皮渗透的影响,筛选有效的透皮吸收促进剂.方法:采用改良Franz扩散池法、离体鼠皮进行体外透皮试验,HPLC测定透皮吸收促进剂对3种有效成分补骨脂素、异补骨脂素及蛇床子素的累积透过量及透皮速率的影响.结果:不同促透剂对复方卡力孜然凝胶剂中补骨脂素、异补骨脂素及蛇床子素体外透皮吸收产生不同的影响,确定2%氮酮为促进剂时3种有效成分的促透效果最好.结论:2%氮酮能够促进复方卡力孜然凝胶剂3种有效成分的有效渗透,透皮吸收过程符合Higuchi方程.%Objective: To study on effects of in vitro percutaneous penetration of different penetration enhancers for three active ingredients from Fufang Kali Ziran gel, and to screen out effective transdermal absorption enhancers. Method;In vitro transdermal test was used by modified Franz diffusion cell method and in vitro rat skin, effect of cumulative penetration volume and penetration rate from transdermal absorption enhancers for three active ingredients ( psoralen, isopsoralen and osthole) was determined by HPLC. Result; Different enhancers were found to have different degree in vitro penetration enhancing effect on psoralen, isopsoralen and osthole in Fufang Kali Ziran gel,determined 2% azone had optimum promoting effect as enhancers to three active ingredients. Conclusion;2% azone could promote effective penetration of three active ingredients from Fufang Kali Ziran gel. This process of penetration absorption could be in line with Higuchi equation.

  10. TSH and PRL, side-effect markers in aripiprazole treatment: adjunctive aripiprazole-induced thyrotropin oversuppression in a young man with schizophrenia.

    Science.gov (United States)

    Ohta, Hidenobu; Inoue, Satoru; Hara, Koichiro; Watanabe, Akihiko

    2017-08-22

    A 26-year-old Japanese man was admitted to our unit with exacerbated paranoid schizophrenia. Prior to his admission, daily administration of olanzapine had been sufficient to maintain a partial remission of his schizophrenia, but due to an exacerbation of his delusions, he had then also been prescribed aripiprazole, which had been followed by no improvement in symptoms and a gradual further exacerbation of auditory delusions. Physical examinations, brain MRI and neurophysiological assessment were unremarkable. Blood analysis, however, revealed extremely low thyroid-stimulating hormone (TSH) and prolactin-releasing hormone (PRL) concentration. Interestingly, after aripiprazole discontinuation, he returned to partial remission with an increase in plasma TSH and PRL concentration. © BMJ Publishing Group Ltd (unless otherwise stated in the text of the article) 2017. All rights reserved. No commercial use is permitted unless otherwise expressly granted.

  11. 酸枣仁抗氧化成分的分离及其相互作用研究%Separation and Interaction of the Ingredients of Antioxidant Activities in Zizyphi Spinosi Semen

    Institute of Scientific and Technical Information of China (English)

    丁轲; 马崟松; 韩涛; 陈湘宁

    2013-01-01

    In order to study the antioxidant activity of Zizyphi Spinosi Semen (ZSS) which is known as a traditional Chinese herb for treatment of insomnia and anxiety, extracts of ZSS was extracted by ethyl acetate, separated by polyamide resin and isolated by C18 reverse-phase medium, orderly. The antioxidant activity of products obtained from each step was measured. The extracts of ethyl acetate, fraction B and 6' '-feruloylspinosin have the best antioxidant activity. At the same time, other two effective ingredients zizyphusine and spinosin were also separated. The antioxidant activity of the three effective ingredients was measured. The antioxidant activity was also studied by mixing zizyphusine, spinosin and 6' '-feruloylspinosin with different proportions. The results prove that the three ingredients have antagonistic effect on both the removal of free radical DPPH and total antioxidant capacity. But they have synergistic effect on chelating with metal ions. The results show that the flavone is the effective part of ZSS for the antioxidant activity, 6' '-feruloylspinosin is the ingredient of flavone in ZSS with the best antioxidant activity. However antagonistic effect on antioxidant activity of ZSS exists among the ingredients of flavone in ZSS .%为了研究酸枣仁这种传统中药的抗氧化活性,采用多项抗氧化活性指标进行评价,通过活性追踪,酸枣仁提取物依次经过乙酸乙酯萃取,聚酰胺树脂分离和 C18反相快速制备色谱分离,顺次得到抗氧化活性最好的萃取物、馏分B和黄酮组分6''-阿魏酰斯皮诺素,同时还分离得到另外两个组分斯皮诺素和酸李碱。在进一步比较了三种组分酸李碱、斯皮诺素与6''-阿魏酰斯皮诺素抗氧化活性的基础上,将三种组分按照不同配比混合后进行了抗氧化活性的研究,证明这三种物质在清除DPPH自由基的反应中呈现拮抗作用,在总抗氧化能力的反应中为拮抗作用,而在与

  12. 7 CFR 58.718 - Flavor ingredients.

    Science.gov (United States)

    2010-01-01

    ... 7 Agriculture 3 2010-01-01 2010-01-01 false Flavor ingredients. 58.718 Section 58.718 Agriculture... Material § 58.718 Flavor ingredients. Flavor ingredients used in process cheese and related products shall... quality or flavor of the finished product. In the case of bulky flavoring ingredients such as pimento, the...

  13. Aripiprazole in the treatment of Huntington’s disease: a case series

    Directory of Open Access Journals (Sweden)

    Andrea Ciammola

    2008-11-01

    Full Text Available Andrea Ciammola1, Jenny Sassone1, Clarissa Colciago1, Niccolò E Mencacci1, Barbara Poletti1, Andrea Ciarmiello2, Ferdinando Squitieri3, Vincenzo Silani11Department of Neurology and Laboratory of Neuroscience, “Dino Ferrari” Centre, University of Milan Medical School – IRCCS Istituto Auxologico Italiano, Milano, Italy; 2Unit of Nuclear Medicine, S. Andrea Hospital, La Spezia, Italy; 3Neurogenetics Unit, IRCCS Neuromed, Pozzilli (IS, ItalyObjectives: The aim of the study was to describe the effects of aripiprazole, a new atypical antipsychotic drug that acts as a partial dopamine agonist on motor, behavioral and cognitive functions in patients with genetically confirmed Huntington’s disease (HD.Methods and results: Three HD patients were evaluated for Unified Huntington Disease Rating Scale part I and II and Beck Depression Inventory at baseline, after two months and one-year treatment. Aripiprazole effectively controlled involuntary movements and psychiatric symptoms, with effects on cognitive functions.Conclusions: Our case reports suggest that aripiprazole is well tolerated, remarkably improving some of the motor and behavioral symptoms in patients affected by HD. Randomized, controlled, long-term studies are warranted.Keywords: Huntington’s disease, aripiprazole, treatment, chorea

  14. Severe arrhythmia induced by orally disintegrating aripiprazole tablets (Bosiqing®: a case report

    Directory of Open Access Journals (Sweden)

    Shao Q

    2015-12-01

    Full Text Available Qing Shao,1,2,* Wei Quan,1,2,* Xiaoni Jia,1 Jianbo Chen,1 Shanbo Ma,3 Xiaohong Zhang11Xi’an Mental Health Center, Institute of Mental Health, Xi’an Medical University, Xi’an, Shaanxi, People’s Republic of China; 2Institute of Materia Medica, School of Pharmacy, Fourth Military Medical University, Xi’an, Shaanxi, People’s Republic of China; 3Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, Xi’an, Shaanxi, People’s Republic of China*These authors contributed equally to this workAbstract: Psychotropic medications have been known to cause cardiac conduction disturbances. Not much is known about the cardiovascular side effects of newer atypical antipsychotics such as aripiprazole. A case of a 13-year-old girl with schizophrenia is presented. An analysis of the presented patient’s clinical history indicates the need for a detailed analysis of the severe arrhythmia induced by aripiprazole. This presented case report contains valuable guidelines that can be of assistance in the treatment of patients with aripiprazole.Keywords: schizophrenia, aripiprazole, arrhythmia, antipsychotics

  15. Switching antipsychotics to aripiprazole or blonanserin and plasma monoamine metabolites levels in patients with schizophrenia.

    Science.gov (United States)

    Miura, Itaru; Shiga, Tetsuya; Katsumi, Akihiko; Kanno-Nozaki, Keiko; Mashiko, Hirobumi; Niwa, Shin-Ichi; Yabe, Hirooki

    2014-03-01

    Blonanserin is a novel atypical antipsychotic drug that has efficacy equal to risperidone. We investigated the effects of aripiprazole and blonanserin on clinical symptoms and plasma levels of homovanillic acid (pHVA) and 3-methoxy-4hydroxyphenylglycol in the switching strategy of schizophrenia. Twenty two Japanese patients with schizophrenia were enrolled into this open study. The antipsychotics of all patients were switched to aripiprazole or blonanserin for the improvement of clinical symptoms or side effects. Plasma monoamine metabolites levels were analyzed with high-performance liquid chromatography. There were no significant effects for time (p = 0.346) or time × group interaction (p = 0.27) on the changes of positive and negative syndrome scale (PANSS) total score, although blonanserin decreased PANSS scores. We observed negative correlation between pHVA at baseline and the change in PANSS total score (rs = -0.450, p = 0.046). We also found positive correlation between the changes in pHVA and the changes in PANSS total (rs = 0.536, p = 0.015) and positive (rs = 0.572, p = 0.008) scores. There were no differences between blonanserin and aripiprazole in the improvement of clinical symptoms. Our results suggest that pHVA may be useful indicator for the switching strategy to aripiprazole or blonanserin in schizophrenia. Copyright © 2014 John Wiley & Sons, Ltd.

  16. Effect of Adjunctive Aripiprazole on Sexual Dysfunction in Schizophrenia: A Preliminary Open-Label Study.

    Science.gov (United States)

    Fujioi, J; Iwamoto, K; Banno, M; Kikuchi, T; Aleksic, B; Ozaki, N

    2017-03-01

    Introduction: Although adjunctive aripiprazole improves hyperprolactinemia, sufficient evidence for its effects on sexual dysfunction has not been obtained. We assessed the usefulness of adjunctive aripiprazole for schizophrenia with sexual dysfunction. Methods: 22 Japanese schizophrenia patients with antipsychotic-induced hyperprolactinemia and sexual dysfunction were enrolled, and 19 of them completed the study. Aripiprazole was administrated in a flexible titration schedule to participants according to the judgment of each doctor, and patients were followed for 24 weeks. Serum prolactin, Clinical Global Impression Scales-Severity (CGI-S), and Nagoya Sexual Function Questionnaire (NSFQ) were measured at baseline and at 4, 8, 12, and 24 weeks. Results: Prolactin at week 4 and later was significantly lower than that at baseline. Compared to baseline, we observed a significant improvement in total sexual dysfunction as measured by NSFQ at week 8 and later. In males, erectile dysfunction was significantly reduced at week 24. In females, menstrual irregularity and galactorrhea were significantly reduced at week 24. CGI-S did not significantly change. Discussion: Although the small sample size is a limitation in this study, adjunctive aripiprazole may be useful treatment for sexual dysfunction including hyperprolactinemia in schizophrenia. © Georg Thieme Verlag KG Stuttgart · New York.

  17. Anti-Phytopthora capsici Activities and Potential Use as Antifungal in Agriculture of Alpinia galanga Swartz, Curcuma longa Linn, Boesenbergia pandurata Schut and Chromolaena odorata: Bioactivities Guided Isolation of Active Ingredients

    Directory of Open Access Journals (Sweden)

    Wilart Pompimon

    2009-01-01

    Full Text Available Problem statement: Plant derived fungicides are now being subjects of many research groups. These secondary metabolites have enormous potential to inspire and influence modern agrochemical research. The study aimed to investigate the antifungal activity and their potential use as fungicides in the agriculture of crude extracts and purified compounds derived from plants used in traditional medicines. Approach: Four medicinal plants including A. galanga, C. longa, B. pandurata and C. odorata were selected and percolated with hexane, ethyl acetate, acetone or methanol. The extracts were purified and elucidated their chemical structures. Disc mycelial growth inhibition was applied in order to determine their anti P. capsici activity and the field study was performed to determine their potential use in controlling fungal infection in chili plants compared with commercial fungicides such as captan and bio-control Trichoderma virens. Results: All crude extract inhibited mycelial growth of the fungus performed with similar efficacy. ED90 was equal to 300 ppm. Among plants studied B. pandurata was the most potent against P. capsici. The proposed active ingredients were pinostrobin and pinocembrin. In the field study, pinocembrin mediated the same anti P. capsici activity as captan. B. pandurata can protect chili from infection, thus increasing crop yield of chili comparable to Trichoderma virens. Conclusion: The results clearly showed that the extracts of the four plants studied could be considered as potential sources of novel fungicides. Particularly, B. pandurata has a very high potential as raw material for developing the antifungal molecule of non-petrochemical, naturally eco-friendly, easily obtainable and not toxic to human beings and environment, at least for use in chili growing.

  18. Profile of aripiprazole in the treatment of bipolar disorder in children and adolescents

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    Kirino E

    2014-11-01

    Full Text Available Eiji Kirino1–3 1Department of Psychiatry, Juntendo University School of Medicine, 2Department of Psychiatry, Juntendo University Shizuoka Hospital, 3Juntendo Institute of Mental Health, Shizuoka, Japan Abstract: Bipolar disorder is a pernicious illness. Compared with the later-onset form, early onset bipolar disorder is associated with worse psychosocial outcomes, and is characterized by rapid cycling and increased risks of substance abuse and suicide attempts. Controlling mood episodes and preventing relapse in this group of pediatric patients requires careful treatment. Here, we review the effectiveness of aripiprazole for bipolar disorder in children and adolescents, with discussion of this drug's unique pharmacological profile and various clinical study outcomes. Aripiprazole acts as a serotonin 5-HT2A receptor antagonist, as well as a partial agonist of the serotonin 5-HT1A and dopamine D2 receptors. It can be safely used in children and adolescents, as it is highly tolerated and shows lower rates of the side effects typically observed with other antipsychotic drugs, including sedation, weight gain, hyperprolactinemia, and extrapyramidal syndrome. The presently reviewed randomized controlled trials (RCTs and non-RCTs generally reported aripiprazole to be effective and well-tolerated in children and adolescents with bipolar disorder. However, due to the limited number of RCTs, the present conclusions must be evaluated cautiously. Furthermore, aripiprazole cannot yet be considered a preferred treatment for children and adolescents with bipolar disorder, as there is not yet evidence that aripiprazole shows greater efficacy compared to other second-generation antipsychotics. Additional data are needed from future head-to-head comparison studies. Keywords: child, mania, mixed state

  19. Case Reports of Aripiprazole Causing False-Positive Urine Amphetamine Drug Screens in Children.

    Science.gov (United States)

    Kaplan, Justin; Shah, Pooja; Faley, Brian; Siegel, Mark E

    2015-12-01

    Urine drug screens (UDSs) are used to identify the presence of certain medications. One limitation of UDSs is the potential for false-positive results caused by cross-reactivity with other substances. Amphetamines have an extensive list of cross-reacting medications. The literature contains reports of false-positive amphetamine UDSs with multiple antidepressants and antipsychotics. We present 2 cases of presumed false-positive UDSs for amphetamines after ingestion of aripiprazole. Case 1 was a 16-month-old girl who accidently ingested 15 to 45 mg of aripiprazole. She was lethargic and ataxic at home with 1 episode of vomiting containing no identifiable tablets. She remained sluggish with periods of irritability and was admitted for observation. UDS on 2 consecutive days came back positive for amphetamines. Case 2 was of a 20-month-old girl who was brought into the hospital after accidental ingestion of an unknown quantity of her father's medications which included aripiprazole. UDS on the first day of admission came back positive only for amphetamines. Confirmatory testing with gas chromatography-mass spectrometry (GC-MS) on the blood and urine samples were also performed for both patients on presentation to detect amphetamines and were subsequently negative. Both patients returned to baseline and were discharged from the hospital. To our knowledge, these cases represent the first reports of false-positive amphetamine urine drug tests with aripiprazole. In both cases, aripiprazole was the drug with the highest likelihood of causing the positive amphetamine screen. The implications of these false-positives include the possibility of unnecessary treatment and monitoring of patients.

  20. Marine biotechnology for production of food ingredients.

    Science.gov (United States)

    Rasmussen, Rosalee S; Morrissey, Michael T

    2007-01-01

    The marine world represents a largely untapped reservoir of bioactive ingredients that can be applied to numerous aspects of food processing, storage, and fortification. Due to the wide range of environments they survive in, marine organisms have developed unique properties and bioactive compounds that, in some cases, are unparalleled by their terrestrial counterparts. Enzymes extracted from fish and marine microorganisms can provide numerous advantages over traditional enzymes used in food processing due to their ability to function at extremes of temperature and pH. Fish proteins such as collagens and their gelatin derivatives operate at relatively low temperatures and can be used in heat-sensitive processes such as gelling and clarifying. Polysaccharides derived from algae, including algins, carrageenans, and agar, are widely used for their ability to form gels and act as thickeners and stabilizers in a variety of foods. Besides applications in food processing, a number of marine-derived compounds, such as omega-3 polyunsaturated fatty acids and photosynthetic pigments, are important to the nutraceutical industry. These bioactive ingredients provide a myriad of health benefits, including reduction of coronary heart disease, anticarcinogenic and anti-inflammatory activity. Despite the vast possibilities for the use of marine organisms in the food industry, tools of biotechnology are required for successful cultivation and isolation of these unique bioactive compounds. In this chapter, recent developments and upcoming areas of research that utilize advances in biotechnology in the production of food ingredients from marine sources are introduced and discussed.

  1. Aripiprazole Improves Depressive Symptoms and Immunological Response to Antiretroviral Therapy in an HIV-Infected Subject with Resistant Depression

    Directory of Open Access Journals (Sweden)

    Chiara Cecchelli

    2010-01-01

    Full Text Available Aripiprazole is the first medication approved by the FDA as an add-on treatment for MDD. The impact of aripiprazole on the response to HIV is unknown. The patient we report on was diagnosed HIV-positive in 1997 and has been treated with antiretroviral therapy since then. In 2008, we diagnosed resistant major depression, hypochondria, and panic disorder. On that occasion, blood tests showed a significantly reduced CD4 count and a positive viral load. We treated this patient with aripiprazole and citalopram. Mood, somatic symptoms, and occupational functioning progressively improved. The last blood examination showed an increase in the CD4 count and a negative viral load. On the basis of the present case study and the review of the literature concerning the effects of psychotropic agents on viral replication, we suggest that the use of aripiprazole in HIV-infected subjects warrants further research.

  2. Variations of Aripiprazole-Induced Dyskinesia Existing with Concurrent Use of Amantadine and an Anticholinergic Agent in an Elderly Patient

    Directory of Open Access Journals (Sweden)

    I-Wen Sun

    2012-06-01

    Full Text Available Elderly patients are vulnerable to the adverse neurological effects of antipsychotics, particularly Parkinsonian symptoms and tardive dyskinesia. This vulnerability in the elderly becomes complex and unpredictable when aripiprazole is prescribed to replace other second-generation or first-generation antipsychotics. This report describes a 69-year-old female schizophrenic patient, who received aripiprazole after using a few antipsychotics, including the first- and second-generation ones. The tardive dyskinesia developed 6 weeks after switching to aripiprazole but subsided 4 weeks later when stopping the concurrent amantadine and decreasing the dosage of trihexyphenidyl. However, Parkinsonian symptoms developed insidiously thereafter, which remitted after the dosage of trihexyphenidyl was increased again. The possible mechanisms of the alternated adverse neurological events after a switch to aripiprazole in the chronic elderly psychosis are discussed.

  3. Optimizing the Use of Aripiprazole Augmentation in the Treatment of Major Depressive Disorder: From Clinical Trials to Clinical Practice

    Science.gov (United States)

    Han, Changsu; Wang, Sheng-Min; Lee, Soo-Jung; Jun, Tae-Youn

    2015-01-01

    Major depressive disorder (MDD) is a recurrent, chronic, and devastating disorder leading to serious impairment in functional capacity as well as increasing public health care costs. In the previous decade, switching therapy and dose adjustment of ongoing antidepressants was the most frequently chosen subsequent treatment option for MDD. However, such recommendations were not based on firmly proven efficacy data from well-designed, placebo-controlled, randomized clinical trials (RCTs) but on practical grounds and clinical reasoning. Aripiprazole augmentation has been dramatically increasing in clinical practice owing to its unique action mechanisms as well as proven efficacy and safety from adequately powered and well-controlled RCTs. Despite the increased use of aripiprazole in depression, limited clinical information and knowledge interfere with proper and efficient use of aripiprazole augmentation for MDD. The objective of the present review was to enhance clinicians' current understanding of aripiprazole augmentation and how to optimize the use of this therapy in the treatment of MDD. PMID:26306301

  4. 黄秋葵茶叶的成分分析及其水提物的抗氧化活性测定%Ingredient analysis and antioxidant activity of water extract of Abelmoschus esculentus tea

    Institute of Scientific and Technical Information of China (English)

    周兆祥; 白石琦; 邹烨; 冯伟伟; 赵婷; 王鑫彤; 朱昀; 张漪静; 仰榴青

    2015-01-01

    目的:对黄秋葵茶叶营养成分和活性成分进行分析,并对其水提取物进行抗氧化活性测定。方法:采用国标法和农业行业标准方法分析黄秋葵茶叶的营养成分和活性成分,同时测定其水提物对 DPPH 自由基、羟自由基的清除作用。结果:黄秋葵茶叶(以干基计)中灰分含量为15.32%,粗蛋白含量为27.58%,粗脂肪含量为2.27%,总糖含量为12.06%;氨基酸分析结果表明,黄秋葵茶叶含有多种人体必需氨基酸;元素分析结果表明,黄秋葵茶叶中含有丰富的钾、钙、镁、铁等元素;活性成分黄酮和多糖的含量分别为1.36%和4.70%。黄秋葵茶叶水提物清除 DPPH 自由基、羟自由基的半数抑制浓度分别为156.8 mg/L 和674.5 mg/L。结论:黄秋葵茶叶具有较好的营养价值和抗氧化保健功能,为消费者提供了一种新型的绿色健康饮品。%Objective:To analyze nutritional ingredient and active ingredient of Abelmoschus esculentus tea,and study on antioxidant activity of water extract.Methods:To analyze nutritional ingredient and ac-tive ingredient of Abelmoschus esculentus tea with GB method and agriculture standard method.Scavenging effects of water extract on DPPH and OH were determined.Results:The content of ash ,crude protein, crude fat and total carbohydrate were 1 5.32%,27.58%,2.27% and 1 2.06% of dried sample,respective-ly.The amino acid analysis results showed that Abelmoschus esculentus tea contained many kinds of essential amino acid.The trace element analysis results showed that Abelmoschus esculentus tea contained K,Ca,Mg, Fe,et al.The active ingredient flavonoids and polysaccharide were 1 .36% and 4.70%,respectively.The IC50 of water extract scavenging DPPH and OH were 1 56.8 mg/L and 674.5 mg/L,respectively.Conclu-sion:Abelmoschus esculentus tea has good nutritional value and antioxidant effect which can provide a new green health drinks

  5. Low-dose aripiprazole resolved complex hallucinations in the left visual field after right occipital infarction (Charles Bonnet syndrome).

    Science.gov (United States)

    Chen, Cheng-Che; Liu, Hsing-Cheng

    2011-06-01

    We reported a patient who suffered from complex visual hallucinations with left homonymous hemianopsia. Brain imaging showed an acute haemorrhage infarct at the right occipital lobe. Charles Bonnet syndrome (CBS) was suspected and aripiprazole was prescribed at 5 mg daily. After 3 weeks, the symptoms of hallucinations and anxiety were relieved. Although some CBS patients might be self-limited without discomfort, low-dose aripiprazole can be considered as a safe medication for significantly anxious patients with CBS.

  6. Influence of energy drink ingredients on mood and cognitive performance.

    Science.gov (United States)

    Childs, Emma

    2014-10-01

    Sales of energy products have grown enormously in recent years. Manufacturers claim that the products, in the form of drinks, shots, supplements, and gels, enhance physical and cognitive performance, while users believe the products promote concentration, alertness, and fun. Most of these products contain caffeine, a mild psychostimulant, as their foremost active ingredient. However, they also contain additional ingredients, e.g., carbohydrates, amino acids, herbal extracts, vitamins, and minerals, often in unspecified amounts and labeled as an "energy blend." It is not clear whether these additional ingredients provide any physical or cognitive enhancement beyond that provided by caffeine alone. This article reviews the available empirical data on the interactive effects of these ingredients and caffeine on sleep and cognitive performance and suggests objectives for future study. © 2014 International Life Sciences Institute.

  7. A rapid, quantitative liquid chromatography-mass spectrometry screening method for 71 active and 11 natural erectile dysfunction ingredients present in potentially adulterated or counterfeit products.

    Science.gov (United States)

    Lebel, Philippe; Gagnon, Jacques; Furtos, Alexandra; Waldron, Karen C

    2014-05-23

    A rapid LC-MS/MS method has been developed to simultaneously separate 71 erectile dysfunction (ED) drugs and 11 natural ingredients that are sometimes found alongside ED drugs, present in suspected adulterated or counterfeit samples. The separation was achieved in 10min using 2.6μm fused-core C18 particles in a 100×2.1mm column coupled to an LTQ Orbitrap XL mass spectrometer operated in positive electrospray mode. Using a straightforward methanolic extraction procedure, recovery from real samples (tablets, capsules, oral liquids and herbal products) was 92-111% and the lower and upper limits of detection and quantification were in the sub ng/mL and the sub μg/mL ranges, respectively. The intra- and inter-assay precision were ≤3.2% and 10.4% respectively across three concentrations of standards (50, 250 and 1000ng/mL) measured for 4 representative drugs spiked into a tablet-based matrix. This behavior was consistently observed for all the other compounds. The mass accuracy was less than 3ppm. Moreover, an advantage of this method is that the full scan event in the acquisition method associated with the high resolution of the Orbitrap XL allows post-analysis identification, in an untargeted approach, of additional species in the complex matrices. Our LC-MS/MS method for ED drugs was successfully applied to 32 samples and the drug identifications were in 100% agreement with those obtained by the conventional methods HPLC-UV and GC-MS. Following the complete validation of the ED method, it has been introduced in the current counterfeit identification procedures at Health Canada. Copyright © 2014 Elsevier B.V. All rights reserved.

  8. Suppressing effect of saikosaponin A, an active ingredient of Bupleurum falcatum, on chocolate self-administration and reinstatement of chocolate seeking in rats.

    Science.gov (United States)

    Lorrai, Irene; Maccioni, Paola; Carai, Mauro A M; Capra, Alessandro; Castelli, M Paola; Riva, Antonella; Morazzoni, Paolo; Gessa, Gian Luigi; Colombo, Giancarlo

    2017-01-18

    Recent lines of experimental evidence have indicated that saikosaponin A (SSA) - a bioactive ingredient of the medicinal plant, Bupleurum falcatum L. - suppressed alcohol, morphine, and cocaine self-administration in rats. The present paper was designed to assess whether the protective properties of SSA on addiction-related behaviors generalize to a hyperpalatable food such as a chocolate-flavored beverage (CFB). To this end, rats were initially trained to lever-respond for CFB [5% (w/v) Nesquik(®) powder in water] under fixed ratio (FR) 10 (FR10) schedule of reinforcement. Once lever-responding reached stable levels, rats were treated acutely with two different dose ranges of SSA (0, 0.25, 0.5, and 1mg/kg; 0, 1, 2.5, and 5mg/kg; i.p.) and exposed to the FR10 and progressive ratio (PR) schedules of reinforcement in four independent experiments. The effect of acutely administered SSA (0, 0.25, 0.5, and 1mg/kg; i.p.) on cue-induced reinstatement of seeking behavior for CFB was also assessed. Under the FR and PR schedules of reinforcement, treatment with SSA diminished lever-responding for CFB, amount of self-administered CFB, and breakpoint for CFB. All variables were virtually completely suppressed after treatment with 5mg/kg SSA. Treatment with SSA also suppressed reinstatement of CFB-seeking behavior. No dose of SSA altered rat motor-performance, evaluated exposing all rats to an inverted screen test immediately after the self-administration session. These results demonstrate that acute treatment with SSA potently suppressed several addictive-like behaviors motivated by highly hedonic nourishment. These data extend to a highly rewarding natural stimulus the anti-addictive properties of SSA recently disclosed in rats self-administering alcohol, morphine, and cocaine.

  9. A comparative analysis of nutrition components and functional active ingredients in Avena nuda and Avena sativa%裸燕麦和皮燕麦的营养及功能活性成分对比分析

    Institute of Scientific and Technical Information of China (English)

    李笑蕊; 王世霞; 幺杨; 婷婷; 刘珊; 任贵兴; 綦文涛

    2015-01-01

    The differences of nutrition components and active ingredient between Avena nuda and Avena sativa were compared.The contents of basic components (moisture and ash),nutritional compositions (starch,protein and fat)and functional active ingredient (flavonoids,polyphenols and oligosaccharide) in 5 kinds of Avena nuda and 3 kinds of Avena sativa were determined.The results showed that there were no significant differences in the contents of moisture and ash between Avena nuda and Avena sativa. The contents of crud fat,crud protein,stearic acid,oleic acid,linoleic acid,linolenic acid,flavonoids and amino acid in Avena nuda were significantly higher than those in Avena sativa,while the contents of slowly digestible starch and stachyose in Avena nuda were significantly lower than those in Avena sativa. Both Avena nuda and Avena sativa had similar composition of nutritional and functional active ingredients but the contents of them higher in Avena nuda than in Avena sativa.%对比研究裸燕麦和皮燕麦营养组分及功能活性成分的差异。以5种裸燕麦和3种皮燕麦为材料,分别测定其中基本组分(水分和灰分)、营养组分(淀粉、蛋白质和脂肪)以及功能组分(黄酮、多酚和低聚糖等)的含量。结果表明,裸燕麦和皮燕麦的水分和灰分含量无显著性差异;裸燕麦在粗脂肪、粗蛋白、硬脂酸、油酸、亚油酸、亚麻酸、黄酮和氨基酸等营养及功能组分的含量方面显著高于皮燕麦,而慢消化淀粉和水苏糖2种组分含量显著低于皮燕麦。裸燕麦和皮燕麦含有相同种类的营养及功能组分,但裸燕麦的多种营养组分及功能组分含量高于皮燕麦。

  10. Application of Refractometry in Purification Technology of Active Ingredients from Citrus aurantium by Macroporous Resin%折光法在树脂精制枳实中有效成分的应用

    Institute of Scientific and Technical Information of China (English)

    曾文雪; 姚珍珍; 涂瑶生; 陈银芳; 宋小玲; 王跃生

    2013-01-01

    目的:探讨折光法在大孔树脂纯化工艺中应用的可行性.方法:选取枳实提取物为研究对象,经AB-8型大孔吸附树脂精制有效部位,用水与50%乙醇洗脱,间隔取样,在线监测洗脱液的折光率并分析其变化规律,同时以HPLC和UV检测作为参比,判断洗脱过程中始点和终点.结果:枳实有效部位精制过程中水洗终点为第4 BV(折光率0),亦即50%乙醇洗脱始点,50%乙醇洗脱终点为第9 BV(折光率16).结论:折光法准确可靠、便捷快速,具有较强的实践指导意义.%Objective: To explore application feasibility of refractometry in purification technology of macroporous resin. Method: Taking extract of Citrus aurantium as research object, active ingredients in it was refined by AB-8 macroporous resin, washed with water and 50% ethanol, interval sampled, refractive ratio of eluent was monitored on line and analyzed its regularity. At the same time, HPLC and UV spectrophotometric method was used to determine hesperidin as references, and to judge initiation point and terminal point during elution. Result: In purification process of active ingredients from C. aurantium, water elution terminal point 4 BV ( refractive index 0) of which was the initiation point by 50% ethanol, 9 BV (refractive index 16) of 50% ethanol elution was the terminal point. Conclusion: Refractometry was accurate, reliable, convenient, quickly in purification technology of active ingredients of TCM, it had a strong practical significance.

  11. 黄花棘豆抑制植物病原菌的活性成分研究%Antifungal activity and isolation of active ingredients in Oxytropis ochrocephala

    Institute of Scientific and Technical Information of China (English)

    杨震发; 袁呈山; 杨顺义; 柳利龙; 杨晋伟; 沈慧敏

    2014-01-01

    In order to find new botanical antifungal compounds,antifungal ingredients of Oxytropis ochrocephala Bunge were isolated. Using bioassay-guided fractionation methods,antifungal ingredients were isolated and mono-meric compounds were identified by modern spectroscopy techniques from O. ochrocephala. All data were pro-cessed statistically by using SPSS 17.0. Ethanol extract of O. ochrocephala showed strong activity against the se-lected pathogenic fungi with an inhibition ratio of 82.08 % at the concentration of 10 mg/mL. The methylene chloride and ethyl acetate phases displayed a significant antifungal activity against Botrytiscinerea,with an inhibi-tion ratio of 84.30% and 83.13% ,respectively. Six compounds were isolated and identified through comparing the data obtained via spectroscopic methods and the values reported in the literature. The screening of antifungal activity showed that 3-hydroxy-4,9-dimethoxypterocarpan,3-hydroxy-9-dimethoxy pterocarpan and 3-hydroxy-8, 9-dimethoxypterocarpan had higher EC50 on tested fungi. The EC50 of 3-hydroxy-4,9-dimethoxypterocarpan against B.cinerea was 10.42μg/mL and the EC50 of 3-hydroxy-8,9-dimethoxypterocarpan against Fusarium oxys-porum was 27.09μg/mL. O. ochrocephala could be used as a biological antifungal agent and pterocarpan com-pounds are its significant antifungal ingredients.%为了测定黄花棘豆(Oxytropis ochrocephala Bunge)提取物对常见病原真菌的活性,明确其中的有效成分,以黄花棘豆为材料,结合生物活性追踪法,对黄花棘豆的抑菌活性物质进行分离,并利用现代波谱学技术进行结构鉴定。结果表明,黄花棘豆乙醇提取物对供试4种病原真菌均表现出较强的活性,10 mg/mL对番茄灰霉病菌的抑菌率达到82.08%;粗提物萃取后的二氯甲烷相和乙酸乙酯相为其活性部分,10 mg/mL对番茄灰霉病菌的抑菌率分别为84.30%和83.13%;从合并后的二氯甲烷和乙酸乙酯

  12. A retrospective study of predictive factors for effective aripiprazole augmentation of antidepressant therapy in treatment-resistant depression

    Directory of Open Access Journals (Sweden)

    Sugawara H

    2016-05-01

    Full Text Available Hiroko Sugawara,1,2 Kaoru Sakamoto,1 Tsuyoto Harada,3 Satoru Shimizu,4 Jun Ishigooka1 1Department of Psychiatry, Tokyo Women’s Medical University, 2Support Center for Women Health Care Professionals and Researchers, Tokyo Women’s Medical University, Shinjuku-ku, 3Department of Psychiatry, Tokyo Women’s Medical University Medical Center East, Arakawa-ku, 4Department of Research, Medical Research Institute, Tokyo Women’s Medical University, Shinjuku-ku, Tokyo, Japan Background: Several studies have evaluated the efficacy and tolerability of aripiprazole for augmentation of antidepressant therapy for treatment-resistant depression (TRD. Here, we investigated the efficacy of aripiprazole augmentation for TRD including both major depressive disorder and bipolar disorder and the clinical predictors of treatment efficacy in a Japanese population.  Methods: Eighty-five depressed Japanese patients who underwent aripiprazole augmentation therapy after failing to respond satisfactorily to antidepressant monotherapy were included in the study. Treatment responses were evaluated based on Clinical Global Impression Improvement scores assessed 8 weeks after initiation of aripiprazole administration. We compared demographic and diagnostic variables, psychiatric medication variables, and clinical variables between remission and nonremission groups.  Results: The aripiprazole augmentation remission rate was 36.5%. Multiple logistic regression analysis indicated that aripiprazole augmentation was significantly more effective for bipolar depression than for major depressive disorder, and both absence of comorbid anxiety disorders and current episode duration >3 months were significantly associated with the efficacy of aripiprazole augmentation.  Conclusion: Polarity of depression, comorbidity of anxiety disorders, and current episode duration may predict the efficacy of aripiprazole augmentation for TRD including both major depressive disorder and

  13. Aripiprazole Improves Associated Comorbid Conditions in Addition to Tics in Adult Patients with Gilles de la Tourette Syndrome.

    Science.gov (United States)

    Gerasch, Sarah; Kanaan, Ahmad Seif; Jakubovski, Ewgeni; Müller-Vahl, Kirsten R

    2016-01-01

    Gilles de la Tourette Syndrome (GTS) is characterized by motor and vocal tics, as well as associated comorbid conditions including obsessive-compulsive disorder (OCD), attention deficit/hyperactivity disorder (ADHD), depression, and anxiety which are present in a substantial number of patients. Although randomized controlled trials including a large number of patients are still missing, aripiprazole is currently considered as a first choice drug for the treatment of tics. The aim of this study was to further investigate efficacy and safety of aripiprazole in a group of drug-free, adult patients. Specifically, we investigated the influence of aripiprazole on tic severity, comorbidities, premonitory urge (PU), and quality of life (QoL). Moreover, we were interested in the factors that influence a patient's decision in electing for-or against- pharmacological treatment. In this prospective uncontrolled open-label study, we included 44 patients and used a number of rating scales to assess tic severity, PU, comorbidities, and QoL at baseline and during treatment with aripiprazole. Eighteen out of fortyfour patients decided for undergoing treatment for their tics with aripiprazole and completed follow-up assessments after 4-6 weeks. Our major findings were (1) aripiprazole resulted in significant reduction of tics, but did not affect PU; (2) aripiprazole significantly improved OCD and showed a trend toward improvement of other comorbidities including depression, anxiety, and ADHD; (3) neither severity of tics, nor PU or QoL influenced patients' decisions for or against treatment of tics with aripiprazole; instead patients with comorbid OCD tended to decide in favor of, while patients with comorbid ADHD tended to decide against tic treatment; (4) most frequently reported adverse effects were sleeping problems; (5) patients' QoL was mostly impaired by comorbid depression. Our results suggest that aripiprazole may improve associated comorbid conditions in addition to tics

  14. Efficacy of aripiprazole augmentation in Japanese patients with major depressive disorder: a subgroup analysis and Montgomery-Åsberg Depression Rating Scale and Hamilton Rating Scale for Depression item analyses of the Aripiprazole Depression Multicenter Efficacy study.

    Science.gov (United States)

    Ozaki, Norio; Otsubo, Tempei; Kato, Masaki; Higuchi, Teruhiko; Ono, Hiroaki; Kamijima, Kunitoshi

    2015-01-01

    Results from this randomized, placebo-controlled study of aripiprazole augmentation to antidepressant therapy (ADT) in Japanese patients with major depressive disorder (MDD) (the Aripiprazole Depression Multicenter Efficacy [ADMIRE] study) revealed that aripiprazole augmentation was superior to ADT alone and was well tolerated. In subgroup analyses, we investigated the influence of demographic- and disease-related factors on the observed responses. We also examined how individual symptom improvement was related to overall improvement in MDD. Data from the ADMIRE study were analyzed. Subgroup analyses were performed on the primary outcome measures: the mean change in the Montgomery-Åsberg Depression Rating Scale (MADRS) total score from the end of selective serotonin reuptake inhibitor (SSRI)/serotonin norepinephrine reuptake inhibitor (SNRI) treatment to the end of the randomized treatment. Changes in the MADRS total scores were consistently greater with aripiprazole than placebo in each of the subgroups. Efficacy was not related to sex, age, number of adequate ADT trials in the current episode, MDD diagnosis, number of depressive episodes, duration of the current episode, age at first depressive episode, time since the first depressive episode, type of SSRI/SNRI, or severity at the end of SSRI/SNRI treatment phase. Compared to placebo, aripiprazole resulted in significant and rapid improvement on seven of the 10 MADRS items, including sadness. These post-hoc analyses indicated that aripiprazole was effective for a variety of Japanese patients with MDD who had exhibited inadequate responses to ADT. Additionally, we suggest that aripiprazole significantly and rapidly improved the core depressive symptoms. © 2014 The Authors. Psychiatry and Clinical Neurosciences © 2014 Japanese Society of Psychiatry and Neurology.

  15. ACTIVE INGREDIENTS ACTION IN THE PLASMA JET AID COAL GASIFICATION%等离子体炬辅助煤气化中活性组分的作用

    Institute of Scientific and Technical Information of China (English)

    董光华; 庞先勇

    2012-01-01

    On the basis of the analysis for the active species character and the reaction pa rameter in the process of the plasma jet aid coal gasification, the experiments for confirming ac tive species action has been designed in this paper. Through quantum chemistry calculation, it is found that the water molecule structure was changed observably by direct action between the ac tive ingredients: singlet oxygen, O2+ etc and oxygen atom in the water molecule in the coal gasifi cation , and these actions was favorable to form free radical OH ? , which react with the carbon in the coal by the broken O-H bond. Likely reaction channel induced by the active ingredients has been posed according to the regression equations on oxygen contents in the working gas to the volume fractions of the staple- H2, CO and CO2 in the experiment.%在对等离子体炬辅助煤气化过程中活性物种的特征和反应参数分析的基础上,设计了以证实活性组分的作用实验.通过量子化学计算,发现活性组分单线态氧和O2+等与水分子的氧原子直接作用更显著地改变了水分子结构,更有利于断键形成自由基OH·,OH·可以与煤中的碳发生反应.根据实验工作气体中氧含量对实验主要产物H2,CO和CO2体积分数的回归方程,提出活性组分诱发煤气化反应的可能化学反应通道.

  16. 基于均匀设计法对酸枣仁抗抑郁有效组分的配伍研究%Uniform Designed Research on the Active Ingredients Assembling of Semen Ziziphi Spinosae for Anti-depression

    Institute of Scientific and Technical Information of China (English)

    郭蕾

    2014-01-01

    Objective To screen out the optimized compatibility proportion of three active ingredients of semen ziziphi spinosae foranti-depression.Methods Groups were ar anged fol owing uniform design. The forced swimming test,tail suspension test were car ied out to determine theanti-depressantactivity in mice.Mice immobility duration in forced swimming test and tail suspension test were observed.Results The optimized dosage of total fat y oil was 10mg/kg,total flavonoids was 100mg/kg and total saponins was 10mg/kg.Conclusion It would be possible to use uniform design combined with pharmacodynamics method in defining the optimized compatibility of active ingredients of semen ziziphi spinosae.%目的优选酸枣仁中3种抗抑郁有效组分的最佳配伍比例。方法根据均匀设计法进行分组,采用小鼠强迫游泳实验和悬尾实验,用小鼠不动时间作为药效学评价指标。结果酸枣仁抗抑郁有效组分的最优配伍为总脂肪油10mg/Kg,总黄酮100mg/Kg,总皂苷10mg/Kg。验证实验证明,酸枣仁抗抑郁有效组分的最佳配伍组合抗抑郁疗效确切。结论应用均匀设计法与药效学相结合确定酸枣仁活性组分配伍的方法是可行的。

  17. Quantitative Analysis of Active Ingredients in Compound Acetylsalicylic Acid Tablets by DOSY%复方乙酰水杨酸片中有效成分的DOSY技术分析

    Institute of Scientific and Technical Information of China (English)

    王丽敏; 仇汝臣; 黄少华

    2016-01-01

    Compound acetylsalicylic acid tablet is a clinical drug having antipyretic, analgesic and anti-inflammatory effects. The present methods to analyze the active ingredients in this drug have many disadvantages. In this study, we used polydimethylsiloxane (PDMS)-assisted diffusion ordered NMR spectroscopy (DOSY), DOSY-correlated spectroscopy (COSY), and relative quantitative1H NMR techniques to analyze the three main active ingredients in this drug. The content ratios among the 3 components could be obtained. It is argued that PDMS-assisted DOSY provides a convenient and efficient method for pharmaceutical quality control of compound acetylsalicylic acid tablets.%复方乙酰水杨酸片是临床常用的解热镇痛消炎药物,目前其有效成分的分析方法存在操作繁琐而分析速度慢等不足。该文利用二甲基硅油(PDMS)辅助的扩散排序(DOSY)技术以及扩散排序-同核相关(DOSY-COSY)联用技术,成功地对复方乙酰水杨酸片中三种有效成分的分子结构进行了快速定性分析,并且利用核磁共振氢谱(1H NMR)技术进行了相对定量分析。该方法具有方便、快捷等特点,可作为借鉴和参考用于药物的质量评价。

  18. Unidentified Inert Ingredients in Pesticides: Implications for Human and Environmental Health

    Science.gov (United States)

    Cox, Caroline; Surgan, Michael

    2006-01-01

    Background By statute or regulation in the United States and elsewhere, pesticide ingredients are divided into two categories: active and inert (sometimes referred to as other ingredients, adjuvants, or coformulants). Despite their name, inert ingredients may be biologically or chemically active and are labeled inert only because of their function in the formulated product. Most of the tests required to register a pesticide are performed with the active ingredient alone, not the full pesticide formulation. Inert ingredients are generally not identified on product labels and are often claimed to be confidential business information. Objectives In this commentary, we describe the shortcomings of the current procedures for assessing the hazards of pesticide formulations and demonstrate that inert ingredients can increase the toxicity of and potential exposure to pesticide formulations. Discussion Inert ingredients can increase the ability of pesticide formulations to affect significant toxicologic end points, including developmental neurotoxicity, genotoxicity, and disruption of hormone function. They can also increase exposure by increasing dermal absorption, decreasing the efficacy of protective clothing, and increasing environmental mobility and persistence. Inert ingredients can increase the phytotoxicity of pesticide formulations as well as the toxicity to fish, amphibians, and microorganisms. Conclusions Pesticide registration should require full assessment of formulations. Evaluations of pesticides under the National Environmental Policy Act, the Endangered Species Act, and similar statutes should include impact assessment of formulations. Environmental monitoring for pesticides should include inert ingredients. To enable independent research and risk assessment, inert ingredients should be identified on product labels. PMID:17185266

  19. Aripiprazole: a review of its use in the treatment of manic episodes in adolescents with bipolar I disorder.

    Science.gov (United States)

    McKeage, Kate

    2014-02-01

    Aripiprazole (Abilify(®)) is an atypical antipsychotic that is widely used in the treatment of psychiatric conditions. Unlike other currently available atypical antipsychotics that primarily have varying degrees of dopamine D2 receptor antagonism, aripiprazole is a partial agonist at D2 and serotonin 5-HT1A receptors, which may explain differences in tolerability profiles. Recently in the EU, oral aripiprazole 10 mg once daily for 12 weeks was approved for the treatment of moderate to severe manic episodes in adolescents (aged ≥13 years) with bipolar I disorder. Approval was based on a phase 3, 30-week US trial in children and adolescents with bipolar I disorder experiencing manic or mixed episodes. Using trial data together with ancillary analyses, the European Medicines Agency concluded that aripiprazole 10 mg once daily for 12 weeks was effective in reducing symptoms of mania, but because of the high drop-out rate, efficacy over 30 weeks of treatment was not proven. Aripiprazole was generally well tolerated in the phase 3 trial. Ancillary analyses indicated that tolerability was less favourable in younger (10-12 years) than in older (≥13 years) subjects, and less favourable with the higher (30 mg/day) than the lower dosage (10 mg/day). The drug is associated with sedation, weight gain and extrapyramidal symptoms (EPS), although the incidence of EPS over 12 weeks was not significantly different between aripiprazole 10 mg/day and placebo. Data comparing the use of atypical antipsychotics in the treatment of mania in adolescents with bipolar I disorder are limited, but evidence shows that aripiprazole provides a valuable additional therapeutic option for use in this population.

  20. 21 CFR 701.30 - Ingredient names established for cosmetic ingredient labeling.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 7 2010-04-01 2010-04-01 false Ingredient names established for cosmetic... AND HUMAN SERVICES (CONTINUED) COSMETICS COSMETIC LABELING Labeling of Specific Ingredients § 701.30 Ingredient names established for cosmetic ingredient labeling. The Commissioner establishes the...

  1. Successful treatment of catatonic syndrome in bipolar I disorder adding aripiprazole to ECT: A case report

    Directory of Open Access Journals (Sweden)

    Diego Hidalgo, MD

    2012-09-01

    Full Text Available Background and Objectives: Catatonic syndrome is a condition presenting in multiple ways, sharing many of them with the neuroleptic malignant syndrome and other diseases. This diagnostic challenge is the main cause of keep treating catatonic syndromes without neuroleptics. Methods: Review of the literature and a case report. Results: We present the case of a 19 years old bipolar I patient with a severe catatonic syndrome, with a torpid clinical evolution, partial response to benzodiazepines and ECT, which successfully resolved with intramuscular aripiprazole. We found through a systematic review (PubMed 2005-2010 that there are few but significant case reports of catatonic syndromes treated with new second generation antipsychotics for different reasons with good outcomes as ours. The pharmacological profile of aripiprazole and the low incidence of NMS reported make it a suitable option in treating this syndrome. Conclusions: We think that this case report could contribute to add more evidence for aripiprazole to be considered a good third-line option in the treatment of catatonic syndrome. However, this would require randomized controlled trials to confirm its effectiveness and safety.

  2. Blood Biomarkers Predict the Cognitive Effects of Aripiprazole in Patients with Acute Schizophrenia

    Directory of Open Access Journals (Sweden)

    Hikaru Hori

    2017-03-01

    Full Text Available Aripiprazole has been reported to exert variable effects on cognitive function in patients with schizophrenia. Therefore, in the present study, we evaluated biological markers, clinical data, and psychiatric symptoms in order to identify factors that influence cognitive function in patients with schizophrenia undergoing aripiprazole treatment. We evaluated cognitive function in 51 patients with schizophrenia using Brief Assessment of Cognition in Schizophrenia (BACS, as well as background information, psychiatric symptoms, plasma catecholamine metabolites—homovanillic acid (HVA, 3-methoxy-4-hydroxyphenylglycol (MHPG—, and serum brain-derived neurotrophic factor (BDNF. Multivariate analyses were performed in order to identify factors independently associated with cognitive function. Brain-derived neurotrophic factor levels, number of hospitalizations, and MHPG levels were associated with verbal memory and learning. Total hospitalization period and MHPG levels were associated with working memory. Age at first hospitalization and education were associated with motor speed. The number of hospital admissions, Positive and Negative Syndrome Scale negative subscale scores (PANSS-N, MHPG levels, BDNF levels, and Drug-Induced Extrapyramidal Symptoms Scale (DIEPSS scores were associated with verbal fluency. Homovanillic acid and MHPG levels, duration of illness, and PANSS-N scores were associated with attention and processing speed. Brain-derived neurotrophic factor and MHPG levels were associated with executive function. These results suggest that treatment of psychiatric symptoms and cognitive dysfunction may be improved in patients treated with aripiprazole by controlling for these contributing factors.

  3. Aripiprazole once-monthly as treatment for psychosis in Turner syndrome: literature review and case report.

    Science.gov (United States)

    Carlone, Cristiano; Pompili, Enrico; Silvestrini, Cristiana; Nicolò, Giuseppe

    2016-01-01

    Turner syndrome (TS) is a neurogenetic disorder characterized by partial or complete monosomy-X, usually resulting of a sporadic chromosomal nondisjunction. It is one of the most common sex chromosome abnormalities, affecting approximately 1 in 2,000 live born females. There are sporadic few case reports of concomitant TS with schizophrenia worldwide. No defined psychiatric condition has been traditionally related to TS, and it is not mentioned in DSM-IV. Although it is not associated with any psychiatric syndrome, several case reports in the literature describe a similar constellation of symptoms in TS that may represent a biologically-based entity. Aripiprazole once-monthly is a second generation antipsychotic recently developed. Its efficacy and non-inferiority to oral aripiprazole have been demonstrated in preventing relapse in patients with schizophrenia. Experience with oral aripiprazole and the current availability of the long-acting formulation suggest a potential benefit in a variety of clinical scenarios and therefore consideration as a treatment option in the treatment of schizophrenia and psychotic symptoms in several disease like TS.

  4. Effects of amisulpride and aripiprazole on progressive-ratio schedule performance: comparison with clozapine and haloperidol.

    Science.gov (United States)

    den Boon, F S; Body, S; Hampson, C L; Bradshaw, C M; Szabadi, E; de Bruin, N

    2012-09-01

    Clozapine and some other atypical antipsychotics (e.g. quetiapine, olanzapine) have been found to exert a characteristic profile of action on operant behaviour maintained by progressive-ratio schedules, as revealed by Killeen's Mathematical Principles of Reinforcement model of schedule-controlled behaviour. These drugs increase the value of a parameter that expresses the 'incentive value' of the reinforcer (a) and a parameter that is inversely related to the organism's 'motor capacity' (δ). This experiment examined the effects of two further atypical antipsychotics, aripiprazole and amisulpride, on progressive-ratio schedule performance in rats; the effects of clozapine and a conventional antipsychotic, haloperidol, were also examined. In agreement with previous findings, clozapine (4, 8 mg kg⁻¹) increased a and δ, whereas haloperidol (0.05, 0.1 mg kg⁻¹) reduced a and increased δ. Aripiprazole (3,30 mg kg⁻¹) increased δ but did not affect a. Amisulpride (5, 50 mg kg⁻¹) had a delayed and protracted effect: δ was increased 3-6 hours after treatment; a was increased 1.5 hours, and reduced 12-24 hours after treatment. Interpretation based on Killeen's model suggests that aripiprazole does not share clozapine's ability to enhance reinforcer value. Amisulpride produced a short-lived enhancement, followed by a long-lasting reduction, of reinforcer value. Both drugs impaired motor performance.

  5. 辛夷不同组分抗过敏作用活性比较研究%Research on the Antiallergenic Activity of the Different Ingredients from Flos Magnolia

    Institute of Scientific and Technical Information of China (English)

    孙蓉; 钱晓路; 吕莉莉

    2013-01-01

    the alcohol extract and water extract or volatile oil components by compareing the antiallergenic effect of different extract of Flos Magnolia. Conclusion The antiallergenic activity of the different ingredients from Flos Magnolia were alcohol extract >water extract> volatile oil components, and under the guidance of antiallergenic activity, the effective ingredients of Flos Magnolia was the alcohol extract. But as the complex of pharmacodynamics characteristics of TCM and the interaction between the components and molecular mechanisms of l ia were not very clear, so it is necessary to take more research of the multi-components between the pharmacological and molecular mechanisms, in order to provide references and research ideas for innovative drugs.

  6. Aripiprazole improves associated comorbid Conditions in addition to Tics in adult Patients with Gilles de la Tourette Syndrome

    Directory of Open Access Journals (Sweden)

    Sarah Gerasch

    2016-09-01

    Full Text Available Gilles de la Tourette Syndrome (GTS is characterized by motor and vocal tics, as well as associated comorbid conditions including obsessive-compulsive disorder (OCD, attention deficit/hyperactivity disorder (ADHD, depression, and anxiety which are present in a substantial number of patients. Although randomized controlled trials including a large number of patients are still missing, aripiprazole is currently considered as a first choice drug for the treatment of tics. The aim of this study was to further investigate efficacy and safety of aripiprazole in a group of drug-free, adult patients. Specifically, we investigated the influence of aripiprazole on tic severity, comorbidities, premonitory urge (PU, and quality of life (QoL. Moreover we were interested in the factors that influence a patient’s decision in electing for-or against- pharmacological treatment. In this prospective uncontrolled open-label study, we included 44 patients and used a number of rating scales to assess tic severity, PU, comorbidities, and QoL at baseline and during treatment with aripiprazole. 18 out of 44 patients decided for undergoing treatment for their tics with aripiprazole and completed follow-up assessments after 4-6 weeks. Our major findings were (1 aripiprazole resulted in significant reduction of tics, but did not affect PU; (2 aripiprazole significantly improved OCD and showed a trend towards improvement of other comorbidities including depression, anxiety and ADHD; (3 neither severity of tics, nor PU or QoL influenced patients’ decisions for or against treatment of tics with aripiprazole; instead patients with comorbid OCD tended to decide in favor of, while patients with comorbid ADHD tended to decide against tic treatment; (4 most frequently reported adverse effects were sleeping problems; (5 patients’ QoL was mostly impaired by comorbid depression. Our results suggest that aripiprazole may improve associated comorbid conditions in addition to tics

  7. Ba-Wei-Di-Huang-Wan through its active ingredient loganin counteracts substance P-enhanced NF-κB/ICAM-1 signaling in rats with bladder hyperactivity.

    Science.gov (United States)

    Tsai, Wen-Hsin; Wu, Chung-Hsin; Cheng, Chen-Hung; Chien, Chiang-Ting

    2016-09-01

    Overt bladder afferent activation may exacerbate endogenous substance P (SP) release to induce intercellular adhesion molecule-1 (ICAM-1)-mediated inflammation and reactive oxygen species (ROS) production leading to hyperactive bladder. Ba-Wei-Die-Huang-Wan (BWDHW), a traditional Chinese medicine, has been used to treat lower urinary tract symptoms in patients by undefined mechanisms. We explored the possible mechanisms and the active components of BWDHW on exogenous SP-induced bladder hyperactivity. BWDHW contained six major components: loganin, paeoniflorin, 5-hydroxymethylfurfural, cinnamic acid, cinnamaldehyde, and paeonol by high-performance liquid chromatography. In urethane-anesthetized female Wistar rats, we evaluated transcystometrogram, pelvic afferent nerve activity by electrophysiologic recording techniques, ICAM-1 expression by Western blot and immunohistochemistry, ROS amount by an ultrasensitive chemiluminescence method and possible ROS sources from the different leukocytes by specific stains in SP-treated bladder. BWDHW and its major component loganin dose-dependently inhibited H2 O2 and HOCl activity in vitro. Intragastrical BWDHW (250 mg/kg) and loganin (5 mg/kg) twice daily for 2 weeks did not affect the baseline micturition parameters. Intra-arterial SP (20 µg/rat) through neurokinin-1 receptor activation increased voiding frequency (shortened intercontraction intervals), pelvic afferent nerve activity, bladder NF-κB/ICAM-1 expression, bladder ROS amount, neutrophils adhesion to venous endothelium, CD68 (monocyte/macrophage), and mast cell infiltration in the inflamed bladder. BWDHW and loganin pretreatment significantly depressed SP-enhanced pelvic afferent nerve activity, bladder NF-κB/ICAM-1 expression, leukocyte infiltration, and ROS amount, and subsequently improved bladder hyperactivity. In conclusion, our results suggest that BWDHW and its active component loganin improves bladder hyperactivity via inhibiting SP/neurokinin-1

  8. Aripiprazole Augmentation in the Treatment of Military-Related PTSD with Major Depression: a retrospective chart review

    Directory of Open Access Journals (Sweden)

    Fikretoglu Deniz

    2011-05-01

    Full Text Available Abstract Background In this chart review, we attempted to evaluate the benefits of adding aripiprazole in veterans with military-related PTSD and comorbid depression, who had been minimally or partially responsive to their existing medications. Methods A retrospective chart review of patients who received an open-label, flexible-dose, 12- week course of adjunctive aripiprazole was conducted in 27 military veterans meeting DSM-IV criteria for PTSD and comorbid major depression. Concomitant psychiatric medications continued unchanged, except for other antipsychotics which were discontinued prior to initiating aripiprazole. The primary outcome variable was a change from baseline in the PTSD checklist-military version (PCL-M and the Beck Depression Inventory (BDI-II. Results PTSD severity (Total PCL scores decreased from 56.11 at baseline to 46.85 at 12-weeks (p Conclusions The addition of aripiprazole contributed to a reduction in both PTSD and depression symptomatology in a population that has traditionally demonstrated poor pharmacological response. Further investigations, including double-blind, placebo-controlled studies, are essential to confirm and further demonstrate the benefit of aripiprazole augmentation in the treatment of military related PTSD.

  9. Effects of acute and chronic aripiprazole treatment on choice between cocaine self-administration and food under a concurrent schedule of reinforcement in rats

    DEFF Research Database (Denmark)

    Thomsen, Morgane; Fink-Jensen, Anders; Woldbye, David

    2008-01-01

    RATIONALE: Dopamine D2-like partial agonists such as aripiprazole have received some attention as potential pharmacotherapies for the treatment of psychostimulant addiction. However, the preclinical evaluations so far have focused on acute effects of aripiprazole. OBJECTIVES: We tested the hypoth......RATIONALE: Dopamine D2-like partial agonists such as aripiprazole have received some attention as potential pharmacotherapies for the treatment of psychostimulant addiction. However, the preclinical evaluations so far have focused on acute effects of aripiprazole. OBJECTIVES: We tested......, chronic treatment with aripiprazole does not show much promise as a potential pharmacotherapy for cocaine addiction. Both acute and chronic treatment data are in agreement with published clinical findings, suggesting that the concurrent choice procedure in rats has predictive validity of efficacy...

  10. Development and Validation of a Stability Indicating RP-HPLC Method for Hydrocortisone Acetate Active Ingredient, Propyl Parahydroxybenzoate and Methyl Parahydroxybenzoate Preservatives, Butylhydroxyanisole Antioxidant, and Their Degradation Products in a Rectal Gel Formulation.

    Science.gov (United States)

    Ascaso, Magda; Pérez-Lozano, Pilar; García, Mireia; García-Montoya, Encarna; Miñarro, Montse; Ticó, Josep R; Fàbregas, Anna; Carrillo, Carolina; Sarrate, Rocío; Suñé-Negre, Josep M

    2015-01-01

    A stability indicating method was established through a stress study, wherein different methods of degradation (oxidation, hydrolysis, photolysis, and temperature) were studied simultaneously to determine the active ingredient hydrocortisone acetate, preservatives propyl parahydroxybenzoate, and methyl parahydroxybenzoate, antioxidant butylhydroxyanisole (BHA), and their degradation products in a semisolid dosage gel form. The proposed method was suitably validated using a Zorbax SB-Phenyl column and gradient elution. The mobile phase consisted of a mixture of methanol, acetonitrile, and water in different proportions according to a planned program at a flow rate of 1.5 mL/min. The diode array detector was set at 240 nm for the active substance and two preservatives, and 290 nm for BHA. The validation study was conducted according to International Conference on Harmonization guidelines for specificity, linearity, repeatability, precision, and accuracy. The method was used for QC of hydrocortisone acetate gel and for the stability studies with the aim of quantifying the active substance, preservatives, antioxidant, and degradation products. It has proved to be suitable as a fast and reliable method for QC.

  11. Lactose in dairy ingredients: Effect on processing and storage stability.

    Science.gov (United States)

    Huppertz, Thom; Gazi, Inge

    2016-08-01

    Lactose is the main carbohydrate in the milk of most species. It is present in virtually all dry dairy ingredients, with levels ranging from lactose powders. The presence of lactose has a strong effect on ingredient processing and stability. Lactose can negatively influence powder properties and lead to undesirable effects, such as the stickiness of powder resulting in fouling during drying, or caking and related phenomena during storage. In addition, being a reducing carbohydrate, lactose can also participate in the Maillard reaction with free amino groups of proteins, peptides, and free AA. In this review, the influence of the presence (or absence) of lactose on physiochemical properties of dairy ingredients is reviewed, with particular emphasis on behavior during processing and storage. Particularly important features in this respect are whether lactose is in the (glassy) amorphous phase or in the crystalline phase, which is strongly affected by precrystallization conditions (e.g., in lactose, permeate, and whey powders) and by drying conditions. Furthermore, the moisture content and water activity of the ingredients are important parameters to consider, as they determine both mobility and reactivity, influencing Maillard reactions and concomitant browning, the crystallization of amorphous lactose during storage of dairy ingredients, glass transitions temperatures, and associated stickiness and caking phenomena. For the stickiness and caking, a crucial aspect to take into account is powder particle surface composition in relation to the bulk powder. Lactose is typically underrepresented at the powder surface, as a result of which deviations between observed lactose-induced caking and stickiness temperatures, and determined glass transition temperatures arise. By considering lactose as an integral part of ingredient composition along with all other compositional and environmental properties, lactose behavior in dairy ingredients can be understood, controlled, and

  12. Chemical profiling analysis of Maca using UHPLC-ESI-Orbitrap MS coupled with UHPLC-ESI-QqQ MS and the neuroprotective study on its active ingredients

    Science.gov (United States)

    Zhou, Yanyan; Li, Peng; Brantner, Adelheid; Wang, Hongjie; Shu, Xinbin; Yang, Jian; Si, Nan; Han, Lingyu; Zhao, Haiyu; Bian, Baolin

    2017-03-01

    Lepidium meyenii (Maca), originated from Peru, has been cultivated widely in China as a popular health care food. However, the chemical and effective studies of Maca were less in-depth, which restricted its application seriously. To ensure the quality of Maca, a feasible and accurate strategy was established. One hundred and sixty compounds including 30 reference standards were identified in 6 fractions of methanol extract of Maca by UHPLC-ESI-Orbitrap MS. Among them, 15 representative active compounds were simultaneously determined in 17 samples by UHPLC-ESI-QqQ MS. The results suggested that Maca from Yunnan province was the potential substitute for the one from Peru. Meanwhile, the neuroprotective effects of Maca were investigated. Three fractions and two pure compounds showed strong activities in the 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP)-induced zebrafish model. Among them, 80% methanol elution fraction (Fr5) showed significant neuroprotective activity, followed by 100% part (Fr6). The inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) was a possible mechanism of its neuroprotective effect.

  13. Improving the Concentrations of the Active Components in the Herbal Tea Ingredient, Uraria crinita: The Effect of Post-harvest Oven-drying Processing

    Science.gov (United States)

    Chao, Jung; Dai, Yuntao; Cheng, Hao-Yuan; Lam, Wing; Cheng, Yung-Chi; Li, Ke; Peng, Wen-Huang; Pao, Li-Heng; Hsieh, Ming-Tsuen; Qin, Xue-Mei; Lee, Meng-Shiou

    2017-01-01

    Uraria crinita is widely used as a popular folk drink; however, little is known about how the post-harvest operations affect the chemical composition and bioactivity of UC. We assessed three drying methods (Oven-drying, Air-drying, Sun-drying), as well as the Oven-drying temperature using metabolomics approaches and bioactivity assays. The samples processed at 40 degree show a greater effect on the levels of estrogen receptor-alpha activity and nuclear factor erythroid 2–related factor 2 activity, anti-oxidative activity, and cyclooxygenase-2 inhibition compared with the other samples. A multivariate analysis showed a clear separation between the 40 degree Oven-dried samples and the other samples, which is consistent with the results of bioactivity assay. These results are ascribed to at least two-fold increase in the concentrations of flavonoids, spatholosineside A and triterpenoids in the oven-dried samples compared with the other groups. The proposed Oven-drying method at 40 degree results in an improved quality of UC. PMID:28079108

  14. 石榴籽油冷榨技术及活性成分生理作用研究%Pomegranate Seed Oil Cold Pressing and Physiological Role of Its Active Ingredient

    Institute of Scientific and Technical Information of China (English)

    李勇

    2011-01-01

    石榴籽油冷榨技术采用低温62℃,使脂肪氧化酶灭活,既可提高出油率,又可防止挥发油、多酚、维生素等活性物质的损失.冷榨技术与莘取法相比,出油率仅低3%-5%,但没有萃取溶剂有害物质的残留.本文介绍了冷榨技术工艺流程及操作要点,分析了石榴籽油的活性成分及其生理作用.%Pomegranate seed oil cold pressing technology inactives lipoxygenase at low temperature 62℃ ,which can increase oil yield and prevent the loss of volatile oils, polyphenols, vitamins and other active substances. Compared with extraction technology,oil yield of cold pressing technology is 3%-5% lower, but no harmful substances residues in extraction solvent. Process and operating points of cold pressing technology were introduced and physiological role of active ingredients in pomegranate seed oil was analyzed.

  15. 超临界萃取技术在蓝色化妆品活性成分提取分离中的应用进展%Application Progress of Supercritical Fluid Extraction in Development of Blue Cosmetic Active ingredients

    Institute of Scientific and Technical Information of China (English)

    毕永贤; 蒋丽刚; 陆海英

    2014-01-01

    To summarize the recent development on the utilization of supercritical fluid extraction in development of blue cos-metic active ingredients,the published articles on extracting blue cosmetic active ingredients by supercritical fluid extraction technology were reviewed and analyzed. The results showed,the supercritical fluid extraction technology in blue cosmetic ac-tive ingredients extracting especially for polyunsaturated fat acid,polyphenols,natural pigments and terpenes has its unique ad-vantages. This review will provide a reference for the further research and development of blue cosmetic active ingredients.%为探讨超临界萃取技术在蓝色化妆品活性成分提取分离中的应用现状,查阅相关文献,并对其进行归纳、分析和总结。结果发现,超临界萃取技术在在多不饱和脂肪酸、多酚、天然色素、萜类等蓝色化妆品活性成分的提取分离中有其独特的优势,可为超临界萃取技术在蓝色化妆品活性成分提取分离中的进一步发展应用提供参考依据。

  16. 丹参治疗冠心病的有效成分分析及其药理学探析%An analysis on the active ingredients and the pharmacology of Danshen on treating coronary heart disease

    Institute of Scientific and Technical Information of China (English)

    廖天南

    2012-01-01

      Objective:To investigate the active ingredients and the pharmacology of Danshen on treating coronary heart disease. Method: ①The closed microwave assisted extraction Salvia the active ingredient tanshinone; ②Cultured mouse cardiomyocytes, manufacturing mice myocardial hypoxia-reperfusion injury model, to simulate myocardial ischemia-reperfusion injury that caused by vivo coronary heart disease; ③Used salvia feeding mice, to observe toxicity; ④To observe teratogenic effects of salvia against mice sperm. Results: The effective tanshinone of salvia that treated coronary heart disease can inhibit of myocardial damage, the inhibitory rate was 84.3%, toxicological studies to prove that medicinal salvia was safe and non-toxic, non-teratogenic, effected on mouse sperm. Conclusion:The pharmacod-ynamic of Danshen sure and nontoxic.%  目的:探讨丹参治疗冠心病的有效成分并对其药理学进行分析.方法:①密闭微波辅助萃取丹参有效成分丹参酮;②培养小白鼠心肌细胞,制造小白鼠心肌细胞缺氧再灌注损伤模型,来模拟体内冠心病所致的心肌缺血再灌注损伤;③用丹参喂养小白鼠,观察其毒副反应;④观察丹参对小白鼠精子的致畸作用.结果:丹参治疗冠心病的有效成分丹参酮能有效的抑制心肌的损伤,损伤抑制率84.3%;经毒理学研究证明药用丹参安全无毒;对小白鼠精子无致畸作用.结论:丹参治疗冠心病药效肯定且无毒.

  17. RP-HPLC测定水蛭中3种蝶啶类活性成分的含量%Content Determination of Three Pteridine Active Ingredients in Leech by RP-HPLC

    Institute of Scientific and Technical Information of China (English)

    郑云枫; 程建明; 彭国平

    2011-01-01

    目的 建立RP-HPLC测定水蛭药材中3种蝶啶类活性成分含量的方法.方法 采用Kromsail C18色谱柱,以甲醇:0.05%三氟乙酸水(20:80)为流动相,检测波长为354 nm,流速为1.0mL/min,柱温30℃.结果 在以上色谱条件下3种成分可以完全分离.水蛭甲素:Y=12.181 4X+0.075 3,r=0.999 6;(36.0~0.90) μg/mL,水蛭乙素:Y=12.024X-2.124 5,r=0.999 5;(40.4~1.01)μg/mL,水蛭丙素:Y=12.814 5X-3.686 l,r=0.999 8;(42.8~1.07) μg/mL.结论 该方法简单、快速,专属性好,可用于水蛭药材的质量控制方法之一.%OBJECTIVE To establish RP-HPLC determination of the content of three pteridine active ingredients in leech. METHODS Kromsail Cu chromatographic column was used with methanol to 0.05% trifluoroacetic acid (20 '? 80) as mobile phase, detecting wave length of 354 nm, flow speed of 1.0 mL/min and column temperature of 30 "C. RESULTS Three active ingredients were separated on the conditions mentioned above. Hirudin A: Y=12.181 4X+0.075 3,r=0. 9996; (36.0~0.90)fig/mL. Hirudin B:Y = 12.024 X - 2.124 5, r=0.9995; (40. 4~1. 01)ng/mL. Hirudin C: Y = 12.814 5X-3.686 1, r=0.999 8; (42.8~1.07)f±g/mL. CONCLUSION The method proves to be easy and fast with good specificity, which can be used to control quality of leeches.

  18. Comparative research between Bai-hua Qian-hu, a Chinese traditional plant, and its active ingredient on nuclear factor-κB and tumor necrosisfactor-α in isolated ischemia-reperfusion heart of rat

    Institute of Scientific and Technical Information of China (English)

    王弛; 常天辉

    2004-01-01

    @@Ischemia-reperfusion (I/R) injury is a complicated pathophysiological process, which is involved in calcium overload, free radical production, metabolic abnormalities, and inflammatory reaction. With the development of modern molecular biology, the expression and regulation of gene in myocardial I/R injury are focused on NF-κB.1Inflammatory reactions play an important role in I/R injury.2 TNF-α, an important inflammatory cytokine, is regulated by NF-κB and counteracts the activation of NF-κB. Sometimes, improper activation of NF-κB can induce excessive inflammatory responses and injury, so, modulation of NF-κB activation may dedicate a new target in alleviation of myocardial I/R injury.3Our previous studies have proved that Bai-hua Qian-hu (Peucedanum praeruptorum Dunn, BQ), a Chinese traditional plant had cardioprotective action in I/R animals.4 Its active ingredient Pd-Ia, a Ca2+-influx blocker5 and K+-channel opener,6 had similar effects. Meanwhile, it relieved inflammatory reaction and apoptosis in I/R myocardium through inhibition of interleukin-6 and Fas, bax, bcl-2 protein expression.7 However, the effects of BQ and Pd-Ia on the activation of NF-κB and the expression of TNF-α in I/R myocardium have not been clear yet. In this study, the effects of BQ and Pd-Ia on these two factors were investigated to further ascertain the molecular protective mechanism of BQ in I/R myocardium.

  19. Functional herbal food ingredients used in type 2 diabetes mellitus.

    Science.gov (United States)

    Perera, Pathirage Kamal; Li, Yunman

    2012-01-01

    From many reports it is clear that diabetes will be one of the major diseases in the coming years. As a result there is a rapidly increasing interest in searching new medicines, or even better searching prophylactic methods. Based on a large number of chemical and pharmacological research work, numerous bioactive compounds have been found in functional herbal food ingredients for diabetes. The present paper reviews functional herbal food ingredients with regards to their anti-diabetic active principles and pharmacological test results, which are commonly used in Asian culinary system and medical system and have demonstrated clinical or/and experimental anti-diabetic effectiveness. Our idea of reviewing this article is to give more attention to these functional food ingredients as targets medicinal foods in order to prevent or slow down the development of type 2 diabetes mellitus.

  20. Aripiprazole in children and adolescents with bipolar disorder comorbid with attention-deficit/hyperactivity disorder: a pilot randomized clinical trial.

    Science.gov (United States)

    Tramontina, Silzá; Zeni, Cristian P; Ketzer, Carla R; Pheula, Gabriel F; Narvaez, Joana; Rohde, Luis Augusto

    2009-04-21

    To assess response to treatment with aripiprazole in children and adolescents with bipolar disorder comorbid with attention-deficit/hyperactivity disorder (ADHD). Children and adolescents were extensively assessed according to DSM-IV criteria for bipolar disorder comorbid with ADHD (n = 710). Those with this comorbidity who were acutely manic or in mixed states were randomly assigned in a 6-week double-blind, placebo-controlled trial to aripiprazole (n = 18) or placebo (n = 25). Primary outcome measures were assessed weekly and included the Young Mania Rating Scale; the Swanson, Nolan, and Pelham Scale-Version IV; and weight. Secondary outcome measures were the Clinical Global Impressions-Severity of Illness scale, the Child Mania Rating Scale-Parental Version (CMRS-P), the Children's Depression Rating Scale-Revised, the Kutcher Adolescent Depression Scale, and adverse events. The trial was conducted at the Hospital de Clínicas de Porto Alegre, Rio Grande do Sul, Brazil, from January 2005 to November 2007. The group receiving aripiprazole showed a significantly greater reduction in YMRS scores (P = .02, effect size [ES] = 0.80), CMRS-P scores (P = .02; ES = 0.54), and CGI-S scores (P = .04; ES = 0.28) from baseline to endpoint than the placebo group. In addition, higher rates of response (P = .02) and remission (P = .01) were found for the aripiprazole group. No significant between-group differences were found in weight, ADHD symptoms, and depressive symptoms. Adverse events significantly more frequent in the aripiprazole group were somnolence and sialorrhea. Aripiprazole was effective in reducing manic symptoms and improving global functioning without promoting severe adverse events or weight gain. No significant treatment effect in ADHD symptoms was observed. Studies are needed to assess psychopharmacologic interventions for improving ADHD symptoms in juvenile bipolar disorder comorbid with ADHD. clinicaltrials.gov Identifier: NCT00116259. Copyright 2009

  1. Dielectronic recombination of Fe 3p^q ions: a key ingredient for describing X-ray absorption in active galactic nuclei

    CERN Document Server

    Badnell, N R

    2006-01-01

    We have carried-out multi-configuration Breit-Pauli AUTOSTRUCTURE calculations for the dielectronic recombination (DR) of Fe^{8+} - Fe^{12+} ions. We obtain total DR rate coefficients for the initial ground-level which are an order of magnitude larger than those corresponding to radiative recombination (RR), at temperatures where Fe 3p^q (q=2-6) ions are abundant in photoionized plasmas. The resultant total (DR+RR) rate coefficients are then an order of magnitude larger than those currently in use by photoionized plasma modeling codes such as CLOUDY, ION and XSTAR. These rate coefficients, together with our previous results for q=0 and 1, are critical for determining the ionization balance of the M-shell Fe ions which give rise to the prominent unresolved-transition-array X-ray absorption feature found in the spectrum of many active galactic nuclei. This feature is poorly described by CLOUDY and ION, necessitating an ad hoc modification to the low-temperature DR rate coefficients. Such modifications are no lo...

  2. Qualitative Confirmation of Active Ingredient of Arbutin in Pear Leaves and Quantitative Determination by HPLC%梨树叶中有效成分熊果苷的确证及HPLC检测

    Institute of Scientific and Technical Information of China (English)

    赵洁; 何强; 姚秉华; 孔祥虹

    2011-01-01

    目的 确证梨树叶中含有熊果苷,并建立高效液相色谱法测定梨树叶中熊果苷的含量.方法 将充分粉碎的梨树叶样品用甲醇提取,蒸去甲醇后用ENVITM- 18固相萃取柱净化,采用在线获取的紫外光谱及扫描质谱对熊果苷进行确证.高效液相色谱分析时用Inertsil ODS-3色谱柱分离,甲醇-水(1:9)洗脱,282 nm检测.结果 梨树叶样品中目标物的紫外吸收光谱及子离子扫描质谱图与熊果苷标准品相同.高效液相色谱法定量分析时线性关系良好,熊果苷的回收率>93%,RSD<2.1%.结论 梨树叶中含有熊果苷有效成分,高效液相色谱法检测梨树叶中熊果苷的含量简便、快速、准确.%OBJECTIVE To confirm arbutin as an ingredient in pear leaves, and develop a method for the determination of arbutin content in pear leaves by HPLC. METHODS The full powdered pear leaves were extracted with methanol, then cleanup was performed on ENVI-18 SPE columns after methanol boiled off. Qualitative confirmation using the UV spectrum and mass spectra was acquired on-line. HPLC was performed on Inertsil ODS-3 column with DAD detection wavelength of 282 nm using methanol-water( 1: 9) as mobile phase. RESULTS The UV spectrum and mass spectra of the target chromatographic peak were the same as arbutin standard. The HPLC method showed good linear relationship, the recoveries of arbutin were all more than 93% and RSD was less than 2.1%. CONCLUSION Arbutin is an active ingredient in pear leaves, and HPLC as the content analysis method is simple, rapid and accurate.

  3. Irradiation effects of ChuanBei active ingredients with cobalt 60%钴-60辐照对川贝活性成分的影响

    Institute of Scientific and Technical Information of China (English)

    宋九华; 成英; 刘素君

    2012-01-01

    考查不同Co-60辐照剂量对川贝活性成分的影响,为川贝的灭菌贮存和质量评价提供参考.采用HPLC法分析成分的变化.在不同辐射剂量照射后,川贝的化学成分的组成基本不变(各组分的保留时间tR不受辐照影响),但钴-60辐照剂量会对川贝药材某些组分的含量有不同程度的影响,在川贝的贮存和质量评价中应引起注意.%To provide guidance of ChuanBei storage and quality evaluation through examining different Co irradiation dose. The column Shim-pack VP-ODS( 150mmx4. 6mm,5. 0μm) was used. The mobile phase consisted of A(2. 5% of phosphoric acid sodium hydrogen and 10%sodium dihydrogen phosphate solution)and B( methanol) with a gradient elution,and the flow rate was l.0mL/ min. The detection wavelength were 200 nm, and the column temperature was 30°C. The composition structure of same original ChuanBei in different radiation dose was same based on retention time( tR ) ,but some components were affected by cobalt 60 irradiation doses. There are obvious effect on some active component content of ChuanBei by Cobalt 60 irradiation. This method can be used as a means of ChuanBei storage and quality assessment.

  4. Dynamic Determination of Active Ingredients in Introduced Echinacea purpurea%引种紫锥菊不同部位有效成分含量的动态测定

    Institute of Scientific and Technical Information of China (English)

    韩琳娜; 孙俊英; 郭庆梅

    2014-01-01

    目的:研究引种紫锥菊中有效成分的动态积累规律。方法:分别采用HPLC和比色法测定紫锥菊生长过程中不同部位菊苣酸和总多酚含量。结果:一年生紫锥菊中总多酚含量变化不大,不同时期不同部位的菊苣酸含量存在差异,各部位菊苣酸含量在盛花期达最大值。结论:紫锥菊采收期取决于菊苣酸含量。研究结果可为山东引种紫锥菊提供理论依据。%This study was aimed to analyze the dynamic accumulation of active ingredients of Echinacea purpurea. Contents of cichoric acid and total polyphenols in different parts through the whole growth process were determined by HPLC and colorimetry. The results showed that the content of total polyphenol changed little in annual plant. There were differences in content of cichoric acid of different parts in different periods. And the content reached the maximum at flowering stage. It was concluded that the harvest stage depended on the content of cichoric acid. The results provided theoretical basis for induced plant in Shandong province.

  5. Research Progress of TCM Medicinal Herbs and Their Active Ingredients in Anti-bacterial Biofilms of Caries%中草药及其活性成分抗龋病细菌生物膜研究进展

    Institute of Scientific and Technical Information of China (English)

    刘玉梅; 徐静舒

    2015-01-01

    龋病是一种最常见的慢性进行性口腔疾病。中草药与传统治疗龋病的药物(如氟化物)相比有诸多优势,因此,近年来中草药抗龋成为国内外众多学者关注的热点。龋病不是单因素疾病,龋病的发生与变形链球菌、血链球菌、内氏放线菌、黏性放线菌、乳酸杆菌形成的细菌生物膜密切相关。本文就中草药及其活性成分抗龋病细菌生物膜相关研究进行简要概述。%Caries is one of the most common chronic progressive oral diseases. TCM medicinal herbs have many advantages compared with traditional dental drugs for caries (such as fluoride). In recent years, cariogenic TCM medicinal herbs have attracted the attention of many domestic and foreign scholars. Caries is not caused by a single factor. The development of caries is closely related to bacterial biofilms that are formed by streptococcus mutans, streptococcus sanguis, actinomyces inside, actinomyces and lactobacillus. Therefore, this article took a brief overview of TCM medicinal herbs and their active ingredients that inhibit the bacterial biofilms.

  6. Effect on the growth and development and induction of abnormalities by a glyphosate commercial formulation and its active ingredient during two developmental stages of the South-American Creole frog, Leptodactylus latrans.

    Science.gov (United States)

    Bach, Nadia Carla; Natale, Guillermo Sebastián; Somoza, Gustavo Manuel; Ronco, Alicia Estela

    2016-12-01

    We evaluated the acute lethal and sublethal effects of technical-grade glyphosate (GLY) and the GLY-based commercial formulation Roundup ULTRA MAX® (RU) on two Gosner stages (Gss) 25 and 36 of the South-American Creole frog, Leptodactylus latrans. Bioassays were performed following standardized methods within a wide range of concentrations (0.0007-9.62 mg of acid equivalents per liter-a.e./L-of RU and 3-300 mg/L of GLY). The endpoints evaluated were mortality, swimming activity, growth, development, and the presence of morphologic abnormalities, especially in the mouthparts. No lethal effects were observed on larvae exposed to GLY during either Gs-25 or Gs-36. The concentrations inducing 50 % lethality in RU-exposed larvae at different exposure times and Gss ranged from 3.26 to 9.61 mg a.e./L. Swimming activity was affected by only RU. Effects on growth and development and the induction of morphologic abnormalities-like oral abnormalities and edema-were observed after exposure to either GLY or RU. Gs-25 was the most sensitive stage to both forms of the herbicide. The commercial formulation was much more toxic than the active ingredient on all the endpoints assessed. Effects on growth, development, and the induction of morphologic abnormalities observed in the range of environmental concentrations reported for agroecosystems of Argentina constitute an alert to the potential detrimental effects of the herbicide that could be affecting the fitness and survival of anurans in agroecosystems.

  7. Clinical Usefulness of Aripiprazole and Lamotrigine in Schizoaffective Presentation of Tuberous Sclerosis.

    Science.gov (United States)

    Lee, Seung-Yup; Min, Jung-Ah; Lee, In Goo; Kim, Jung Jin

    2016-08-31

    Tuberous sclerosis is not as rare as once thought and has high psychiatric comorbidities. However, bipolar or psychotic features associated with tuberous sclerosis have been rarely reported. This report first presents a tuberous sclerosis patient, resembling a schizoaffective disorder of bipolar type. A patient with known tuberous sclerosis displayed mood fluctuation and psychotic features. Her symptoms did not remit along with several psychiatric medications. After hospitalization, the patient responded well with lamotrigine and aripiprazole without exacerbation. As demonstrated in this case, tuberous sclerosis may also encompass bipolar affective or psychotic features. We would like to point out the necessity to consider bipolarity in evaluating and treating tuberous sclerosis.

  8. What determines ingredient awareness of consumers? A study on ten functional food ingredients

    NARCIS (Netherlands)

    Bornkessel, S.; Bröring, S.; Omta, S.W.F.; Trijp, van J.C.M.

    2014-01-01

    Given the importance of consumer awareness of functional food ingredients for healthy food choices, the aim of this study is to explore consumers’ ingredient awareness and the determinants which influence the awareness about functional food ingredients. A sample of 200 German consumers was interview

  9. Processed Meat Ingredients: Past, Present and Future

    Science.gov (United States)

    Ingredients were first utilized to preserve meat and improve its palatability which date back to when our ancestors used salt and fire to preserve meat. Since that time man has incorporated a wide variety of ingredients to develop unique meat products and find ways to extend the shelf life of these ...

  10. 7 CFR 65.185 - Ingredient.

    Science.gov (United States)

    2010-01-01

    ... AGRICULTURAL MARKETING ACT OF 1946 AND THE EGG PRODUCTS INSPECTION ACT (CONTINUED) COUNTRY OF ORIGIN LABELING..., PEANUTS, AND GINSENG General Provisions Definitions § 65.185 Ingredient. Ingredient means a component either in part or in full, of a finished retail food product. ...

  11. Consumers' choice-blindness to ingredient information.

    Science.gov (United States)

    Cheung, T T L; Junghans, A F; Dijksterhuis, G B; Kroese, F; Johansson, P; Hall, L; De Ridder, D T D

    2016-11-01

    Food manufacturers and policy makers have been tailoring food product ingredient information to consumers' self-reported preference for natural products and concerns over food additives. Yet, the influence of this ingredient information on consumers remains inconclusive. The current study aimed at examining the first step in such influence, which is consumers' attention to ingredient information on food product packaging. Employing the choice-blindness paradigm, the current study assessed whether participants would detect a covertly made change to the naturalness of ingredient list throughout a product evaluation procedure. Results revealed that only few consumers detected the change on the ingredient lists. Detection was improved when consumers were instructed to judge the naturalness of the product as compared to evaluating the product in general. These findings challenge consumers' self-reported use of ingredient lists as a source of information throughout product evaluations. While most consumers do not attend to ingredient information, this tendency can be slightly improved by prompting their consideration of naturalness. Future research should investigate the reasons for consumers' inattention to ingredient information and develop more effective strategies for conveying information to consumers.

  12. Inulin-type fructans: functional food ingredients.

    Science.gov (United States)

    Roberfroid, Marcel B

    2007-11-01

    A food (ingredient) is regarded as functional if it is satisfactorily demonstrated to affect beneficially 1 or more target functions in the body beyond adequate nutritional effects. The term inulin-type fructans covers all beta(2inulin (DP 2-60, DP(av) = 12), oligofructose (DP 2-8, DP(av) = 4), and inulin HP (DP 10-60, DP(av) = 25) as well as Synergy 1, a specific combination of oligofructose and inulin HP. Inulin-type fructans resist digestion and function as dietary fiber improving bowel habits. But, unlike most dietary fibers, their colonic fermentation is selective, thus causing significant changes in the composition of the gut microflora with increased and reduced numbers of potentially health-promoting bacteria and potentially harmful species, respectively. Both oligofructose and inulin act in this way and thus are prebiotic: they also induce changes in the colonic epithelium and in miscellaneous colonic functions. In particular, the claim "inulin-type fructans enhance calcium and magnesium absorption" is scientifically substantiated, and the most active product is oligofructose-enriched inulin (Synergy 1). A series of studies furthermore demonstrate that inulin-type fructans modulate the secretion of gastrointestinal peptides involved in appetite regulation as well as lipid metabolism. Moreover, a large number of animal studies and preliminary human data show that inulin-type fructans reduce the risk of colon carcinogenesis and improve the management of inflammatory bowel diseases. Inulin-type fructans are thus functional food ingredients that are eligible for enhanced function claims, but, as more human data become available, risk reduction claims will become scientifically substantiated.

  13. Comparison of the Nutrient and Active Ingredients in Three Kinds of Jinxiang Allium sativum L.%3种金乡大蒜中营养活性成分的含量比较

    Institute of Scientific and Technical Information of China (English)

    周宇; 王文军; 李茜; 杨丹; 孔庆胜

    2016-01-01

    [目的]检测3种金乡大蒜中营养成分和活性物质含量,从化学分子水平探讨不同品种的差异,对于优化种质资源、提升大蒜后期加工利用的品质和附加值具有指导作用。[方法]采用食品化学的常规方法并结合大型仪器检测,测定大蒜中营养成分和活性成分的含量。[结果]基本营养成分可溶性糖、粗脂肪、蛋白质含量,以金乡紫皮蒜最高,金乡白皮蒜次之,独头蒜最少;金乡紫皮蒜维生素C含量最高,独头蒜次之,金乡白皮蒜最少;金乡白皮蒜的过氧化氢酶(CAT)活性最高,紫皮蒜次之,独头蒜最差;锗和大蒜素DADS含量则是独头蒜最高。[结论]对于偏重营养成分的利用,金乡紫皮蒜有较大优势;而对于大蒜素和锗的特色保健功能利用,独头蒜有更大优势。%Objective] The research aimed to detect the difference of contents of nutrient and active ingredients in 3 kinds of Jinxiang Allium sa-tivum L.and to explore the differences of different varieties from the chemical molecular level .It performs important functions in optimizing the germplasm resourses and improving the quality additional value of late garlic processing.[Method]The nutrient and active ingredients of 3 kinds of Jinxiang Allium sativum L.were detected by traditional chemical methods and large-scale instruments methods.[Result]In the basic nutrients, such as soluble sugar, crude fat, protein and vitamin C,the Jinxiang purple skin Allium sativum L.had the highest content, the white skin Allium sativum L.took the second place and the single clove Allium sativum L.was the least.In the contents of vitamin C ,the Jinxiang purple skin Alli-um sativum L.had the highest content,the single clove Allium sativum L.took the second place and the white skin Allium sativum L.was the least.While in the activity of catalase(CAT), the Jinxiang white skin Allium sativum L.showed the maximum activity,the purple skin Allium

  14. Aripiprazole for the treatment and prevention of acute manic and mixed episodes in bipolar I disorder in children and adolescents: a NICE single technology appraisal.

    Science.gov (United States)

    Uttley, Lesley; Kearns, Ben; Ren, Shijie; Stevenson, Matt

    2013-11-01

    As part of its single technology process, the National Institute for Health and Care Excellence (NICE) invited the manufacturers of aripiprazole (Otsuka Pharmaceutical Co. and Bristol Myers Squibb) to submit evidence of the clinical and cost effectiveness of aripiprazole for the treatment and prevention of acute manic and mixed episodes in bipolar I disorder in children and adolescents. The School of Health and Related Research Technology Appraisal Group at the University of Sheffield was commissioned to act as the independent Evidence Review Group (ERG). The ERG produced a critical review of the evidence for the clinical and cost effectiveness of the technology, based upon the manufacturers' submission to NICE. The evidence, which was derived mainly from a double-blind, phase III, placebo-controlled trial of aripiprazole in patients aged 10-17 years, showed that aripiprazole performed significantly better than placebo in reducing mania according to the primary outcome measurement (the Young Mania Rating Scale at 4 weeks). Safety outcomes indicated that aripiprazole was significantly more likely to cause extrapyramidal symptoms and somnolence than placebo. The manufacturers also presented a network meta-analysis of aripiprazole versus other atypical antipsychotics commonly used to treat manic episodes (olanzapine, quetiapine and risperidone) to show that aripiprazole performed similarly to the comparator drugs in terms of efficacy and safety. Aripiprazole was demonstrated to perform better in safety outcomes of (1) less weight gain than olanzapine and quetiapine; and (2) less prolactin increase than olanzapine, quetiapine and risperidone. Results from the manufacturers' economic evaluation showed that use of aripiprazole second-line dominated all of the other treatment strategies that were considered. However, there was considerable uncertainty in this result, and clinical advisors indicated that the actual treatment strategy employed in practice is likely to be

  15. Separation of Chiral Active Pharmaceutical Ingredients

    DEFF Research Database (Denmark)

    Chaaban, Joussef Hussein

    is regarded as a first step towards a fully continuous PC process. The current knowledge of the importance of crystallization processes in the pharmaceutical industry and the complex thermodynamic and kinetic phenomena accompanied with the separation of chiral compounds are addressed. The experimental work...

  16. PharmacoIogicaI Effects of Cortex phellodendri and Its Active Ingredient Extraction%黄柏的药理作用及其活性成分提取

    Institute of Scientific and Technical Information of China (English)

    陈阳峰; 钟晓红

    2015-01-01

    Cortex phellodendri is the dry bark of rutaceae plants Phellodendron chinense Schneid or Cortex phellodendri, which has characters of bitter and cold and effects of clearing heat,drying dampness,removing firelight and excepting steam,curing poison and sore.Cortex phellodendri has extensive pharmacological activities,such as antibacterial,antivi-ral,relieving cough,depressurization and enhance immunity,etc.Alkaloids are the main active ingredients in Cortex phellodendri,in which content of berberine is highest,which reaches to 1.4% ~5.8%.In addition,jateorrhizine,phel-lodendrine,palmatine,obaculactone and obacunone also occupy certain proportion.This article summarized the research progress on pharmacological effects of Cortex phellodendri and the extraction processes of its alkaloids.%黄柏为芸香科植物黄皮树或黄檗的干燥树皮,其性味苦寒,有清热燥湿,泻火除蒸,解毒疗疮之功效。黄柏具有广泛的药理活性,如抗菌、抗病毒、镇咳、降压以及增强免疫等。黄柏的主要活性成分为生物碱,其中小檗碱是含量最高的生物碱,可达1.4%~5.8%,另外药根碱、黄柏碱、掌叶防己碱以及黄柏内酯、黄柏酮等活性成分也占有一定比重。综述了黄柏的药理作用及其生物碱提取工艺研究进展。

  17. A Placebo-Controlled, Fixed-Dose Study of Aripiprazole in Children and Adolescents with Irritability Associated with Autistic Disorder

    Science.gov (United States)

    Marcus, Ronald N.; Owen, Randall; Kamen, Lisa; Manos, George; McQuade, Robert D.; Carson, William H.; Aman, Michael G.

    2009-01-01

    Objective: To evaluate the short-term efficacy and safety of aripiprazole in the treatment of irritability in children and adolescents with autistic disorder. Method: Two hundred eighteen children and adolescents (aged 6-17 years) with a diagnosis of autistic disorder, and with behaviors such as tantrums, aggression, self-injurious behavior, or a…

  18. An Open-Label Study of Aripiprazole : Pharmacokinetics, Tolerability, and Effectiveness in Children and Adolescents with Conduct Disorder

    NARCIS (Netherlands)

    Findling, Robert L.; Kauffman, Ralph; Sallee, Floyd R.; Salazar, Daniel E.; Sahasrabudhe, Vaishali; Kollia, Georgia; Kornhauser, David M.; Vachharajani, Nimish N.; Assuncao-Talbott, Sheila; Mallikaarjun, Suresh; Iwamoto, Taro; McQuade, Robert D.; Boulton, David W.; Blumer, Jeffrey

    2009-01-01

    Objectives: This study evaluated flexible-dose pharmacokinetics, safety, and effectiveness of aripiprazole in children and adolescents with conduct disorder (CD). Methods: This open-label, 15-day, three-center study with an optional 36-month extension enrolled a total of 23 patients: 12 children (6-

  19. Add-on effects of a low-dose aripiprazole in resolving hyperprolactinemia induced by risperidone or paliperidone.

    Science.gov (United States)

    Qiao, Ying; Yang, Fuzhong; Li, Chunbo; Guo, Qian; Wen, Hui; Zhu, Suoyu; Ouyang, Qiong; Shen, Weidi; Sheng, Jianhua

    2016-03-30

    This study investigated the effects of a low-dose aripiprazole adjunctive treatment for risperidone- or paliperidone-induced hyperprolactinemia in Han Chinese women with schizophrenia. After 4 weeks of risperidone or paliperidone treatment, 60 out of 66 patients improved significantly and experienced hyperprolactinemia. They were randomly assigned to the treatment group (aripiprazole adjunctive treatment) (n=30) or control group (non-adjunctive treatment) (n=30). The dosage of risperidone and paliperidone were maintained; and aripiprazole was maintained at 5mg/day during the 8-week study period. The prolactin levels at the end of the 8th week were significantly lower in the treatment group than in the control group. The estradiol level correlated negatively with serum prolactin level both in the treatment group and the control group at the end of the 8th week and the 4th week respectively. The Positive and Negative Syndrome Scale score improved significantly during the 8-week study period in both groups. The incidence of treatment-emergent adverse event was similar in two groups. Low-dose aripiprazole adjunctive treatment is effective in relieving risperidone- and paliperidone-induced hyperprolactinemia in female schizophrenic patients without increasing adverse event.

  20. An Open-Label Study of Aripiprazole : Pharmacokinetics, Tolerability, and Effectiveness in Children and Adolescents with Conduct Disorder

    NARCIS (Netherlands)

    Findling, Robert L.; Kauffman, Ralph; Sallee, Floyd R.; Salazar, Daniel E.; Sahasrabudhe, Vaishali; Kollia, Georgia; Kornhauser, David M.; Vachharajani, Nimish N.; Assuncao-Talbott, Sheila; Mallikaarjun, Suresh; Iwamoto, Taro; McQuade, Robert D.; Boulton, David W.; Blumer, Jeffrey

    Objectives: This study evaluated flexible-dose pharmacokinetics, safety, and effectiveness of aripiprazole in children and adolescents with conduct disorder (CD). Methods: This open-label, 15-day, three-center study with an optional 36-month extension enrolled a total of 23 patients: 12 children

  1. HPLC Determination of 9 Active Ingredients in Arundina Graminifolia%高效液相色谱法测定竹叶兰中9种活性成分含量

    Institute of Scientific and Technical Information of China (English)

    李银科; 舒丽丹; 杨海英; 叶艳青; 李明

    2014-01-01

    A method of HPLC for the determination of 9 active ingredients in Arundina Graminifolia was proposed.The sample was extracted with methanol (8+2)solution by speedy and homogeneous pulping,and an aliquot of 5.0 mL of the extract was purified by passing through MCI-GEL RP-resin SPE column.An aliquot of 2.00 mL of the eluate was taken for HPLC analysis.Waters Xbridge chromatographic column was used as stationary phase and mixtures of methanol and acetic acid (0.5 +99.5)solution with different mixing ratios were used as mobile phase in the gradient elution.UV-detection at 275 nm was adopted in the determination.Linear relationships between values of peak area and mass concentration of the 9 active ingredients were kept in definite ranges.Detection limits (3S/N)found were ranged from 20 to 30 μg·L-1 .Values of recovery found by standard addition method were in the range of 96.4%-105%,with values of RSD′s (n=7)in the range of 1.5%-2.4%.%提出了高效液相色谱法测定竹叶兰中9种活性成分含量的方法。竹叶兰样品经甲醇(8+2)溶液高速匀浆提取,分取提取液5.0 mL,经 MCI-GEL 反相树脂固相萃取小柱净化,取2.00 mL净化液供色谱分析。净化液采用 Waters Xbridge 色谱柱为分离柱,用甲醇和乙酸(0.5+99.5)溶液以不同比例混合的混合液为流动相进行梯度洗脱,在检测波长275 nm 处进行测定。9种活性成分在一定的质量浓度范围内与其峰面积呈线性关系,方法的检出限(3S/N)在20~30μg·L-1之间。加标回收率在96.4%~105%之间,测定值的相对标准偏差(n=7)在1.5%~2.4%之间。

  2. GC-MS Fingerprint of an Active Ingredients Group from Jinxuan Zhike Xunxi Powders%金玄痔科熏洗散有效部位制剂的GC-MS指纹图谱研究

    Institute of Scientific and Technical Information of China (English)

    别文华; 刘蔚; 李力; 周道年

    2015-01-01

    目的::对金玄痔科熏洗散及有效部位新制剂进行GC-MS分析,建立了有效部位新制剂的GC-MS指纹图谱。方法:采用GC-MS方法对金玄痔科熏洗散及有效部位新制剂中的主要组分进行分析,并确定指纹图谱中的特征指纹信息。结果:对10个批次的有效部位新制剂进行了测定,并得到了较为理想的包含特征信息的有效部位新制剂的GC-MS指纹图谱。结论:方法重复性好,所建立的指纹图谱为金玄痔科熏洗散有效部位新制剂的质量控制提供了有效手段。%Objective:To analyze Jinxuan Zhike Xunxi powders ( JZX) and an active ingredients group ( AIG) obtained from JZX by GC-MS, and develop a characteristic fingerprint of AIG. Methods: A gas chromatography-mass spectrum ( GC-MS) method was applied to analyze the main compositions in JZX and AIG, and the characteristic fingerprint information in the fingerprint spectrum was determined. Results:Totally 10 batches of AIG were detected, and a promising GC-MS fingerprint spectrum containing characteristic information for AIG was obtained. Conclusion: The developed fingerprint with good repeatability can be successfully applied in the quality control of AIG.

  3. HPLC determination of 4 compounds in Jinxuan Zhike Xunxi powder and its active ingredients group%新老工艺的金玄痔科熏洗散4种成分含量比较

    Institute of Scientific and Technical Information of China (English)

    刘蔚; 叶晓川; 段雪云; 陈树和; 刘焱文

    2012-01-01

    目的:建立测定金玄痔科熏洗散(JZXS)及新工艺制备的金玄痔科熏洗散(AIG)中绿原酸、咖啡酸、金丝桃苷和木犀草素的HPLC分析方法.方法:采用Venusil XBP C18柱(250mm×4.6mm,5μm);柱温30℃;流速1.0mL·min-1;流动相:乙腈-0.4%磷酸水溶液,梯度洗脱;进样量10μL;检测波长为335nm.结果:绿原酸、咖啡酸、金丝桃苷、木犀草素的线形范围分别和回归方程分别为0.760~4.560μg (r=0.999 9),Y=2 254.9X+ 131.66;0.058~0.348μg (r=0.999 9),Y=3 610.8X+7.913 5;0.046~0.276 μg(r=0.999 9),y=1 446.7X+2.124 3;0.024~0.144μg(r=0.999 9),y=2 344.5 X -0.716 2;JZXS 平均加样回收率(n=5)分别为97.4%(RSD=1.8%),98.6%(RSD=2.3%)和97.8%(RSD=2.9%);AIG平均加样回收率(n=5)为97%(RSD=1.2%),97.3%(RSD=2.5%),98.12% (RSD=2.7%)和96.9% (RSD=1.9%).结论:该方法专属性好,准确度高,为进一步完善JZXS的质量标准提供了科学依据,并为该传统制剂二次开发为创新中药品种奠定了基础.%OBJECTIVE To establish an HPLC method for determination of chlorogenic acid, caffeic acid, hyperoside and luteoloside in Jinxuan Zhike Xunxi powder(JZXS) and its active ingredients group(AIG). METHODS RP-HPLC was used, the separation was performed on Venusil XBP C18 (250 m×4. 6 mm,5μm) column by gradient elution with acetonitrile -0. 4% phosphoric acid as the mobil phase. The detection wavelength was set at 335 nm and the flow rate was 1. 0 mL·min-1 , and column temperature was 30 ℃. RESULTS The linear ranges were 0. 760-4. 560μg (Y = 2 254. 9X + 131. 66, r = 0. 999 9) for chlorogenic acid, 0. 058 - 0. 348μg (Y = 3 610. 8X +7. 913 5, r=0.9999) for caffeic acid, 0. 046 - 0. 276μg (Y = 1 446.7X + 2. 124 3, r= 0. 999 9) for hyperoside and 0. 024 - 0. 144μg (Y= 2 344. 5X - 0. 716 2,r= 0. 999 9) for luteoloside. The recoveries (n = 5) were 97. 4%(RSD= 1. 8%) ,98. 6%(RSD=2. 3%) and 97. 8%(RSD= 2. 9%), respectively in Jinxuan Zhike Xunxi paoder, and

  4. An introduction to toothpaste - its purpose, history and ingredients.

    Science.gov (United States)

    Lippert, Frank

    2013-01-01

    Toothpaste is a paste or gel to be used with a toothbrush to maintain and improve oral health and aesthetics. Since their introduction several thousand years ago, toothpaste formulations have evolved considerably - from suspensions of crushed egg shells or ashes to complex formulations with often more than 20 ingredients. Among these can be compounds to combat dental caries, gum disease, malodor, calculus, erosion and dentin hypersensitivity. Furthermore, toothpastes contain abrasives to clean and whiten teeth, flavors for the purpose of breath freshening and dyes for better visual appeal. Effective toothpastes are those that are formulated for maximum bioavailability of their actives. This, however, can be challenging as compromises will have to be made when several different actives are formulated in one phase. Toothpaste development is by no means complete as many challenges and especially the poor oral substantivity of most active ingredients are yet to overcome.

  5. Determining Whether a Definitive Causal Relationship Exists Between Aripiprazole and Tardive Dyskinesia and/or Dystonia in Patients With Major Depressive Disorder, Part 3: Clinical Trial Data.

    Science.gov (United States)

    Preskorn, Sheldon H; Macaluso, Matthew

    2016-03-01

    This series of columns has 3 main goals: (1) to explain class warnings as used by the United States Food and Drug Administration, (2) to increase awareness of movement disorders that may occur in patients treated with antipsychotic medications, and (3) to understand why clinicians should refrain from immediately assuming a diagnosis of tardive dyskinesia/dystonia (TD) in patients who develop abnormal movements during treatment with antipsychotics. The first column in the series presented a patient who developed abnormal movements while being treated with aripiprazole as an augmentation strategy for major depressive disorder (MDD) and reviewed data concerning the historical background, incidence, prevalence, and risk factors for tardive and spontaneous dyskinesias, the clinical presentations of which closely resemble each other. The second column in the series reviewed the unique mechanism of action of aripiprazole and preclinical studies and an early-phase human translational study that suggest a low, if not absent, risk of TD with aripiprazole. This column reviews clinical trial data to assess whether those data support the conclusion that aripiprazole has a low to absent risk of causing TD when used as an augmentation strategy to treat MDD. To date, no randomized, placebo-controlled trials have established a definitive link between exposure to aripiprazole and TD in patients with MDD. One long-term, open-label, safety trial examined aripiprazole as an augmentation strategy in individuals with MDD and found a rare occurrence (4/987, 0.4%, the confidence interval of which overlaps with zero) of an adverse event termed TD. In all 4 cases, the observed movements resolved within weeks of aripiprazole discontinuation, suggesting that they were either amenable to treatment or represented an acute syndrome rather than TD. No cases of TD were reported in the registration trials for the MDD indication for aripiprazole. These data were presented in a pooled analysis of

  6. 基于均匀设计的中药有效组分复方配伍研究%Uniform designed research on the active ingredients assembling of Chinese herbal for antioxidative capacity

    Institute of Scientific and Technical Information of China (English)

    杨鸿; 吴彦; 马琰岩; 吕俊海; 李晶哲

    2012-01-01

    Objective To find a suitable way of quantitative composition-activity relationship of Chinese herbal for antioxidative capacity based on uniform design. Method Chinese herbal active ingredient formula was composed of Total flavonoids of Glycyrrhiza (TFG) , ginkgo biloba extract (GBE) , Total fa-vonoids of epimedium (TFE) and astragaloside (AST) . The herbal efficacy was detected by scavenging the free radical of DPPH in vitro, and the mathematical model was constructed to describe the connection between different combinations and their antioxidative capacity by the method of LARS regression. Result The best effect was in the ratio of TFG 0. 8 mg/ml,GBE 3.144 mg/ml,TFE 0.024 mg/ml,AST 0.036 mg/ml. Conclusion Uniform designed research is one of efficient ways to describe the quantitative composition-activity relationship.%目的 探索基于均匀设计的中药抗氧化有效组分复方的研究分析方法.方法 采用均匀设计和改进最小角回归分析,对甘草总黄酮、银杏叶提取物、淫羊藿总黄酮和黄芪总苷组成的中药组分复方不同配比体外清除DPPH自由基的作用进行研究.结果 通过分析获得了中药组分配伍清除DPPH的回归方程,优化组合后进行药效学验证,结果显示该中药组分配伍最佳剂量组合为甘草总黄酮0.8 mg/ml、银杏叶提取物3.144 mg/ml、淫羊藿总黄酮0.024 mg/ml和黄芪总苷0.036 mg/ml.结论 上述中药组分配伍后能有效清除DPPH自由基;本实验采用的均匀设计结合改进最小角回归分析适合"非线性、小样本"生物实验数据数据分析,为筛选评价抗氧化中药有效组分复方提供了合适的研究方法.

  7. [Rapid analysis of added ingredients in heroin].

    Science.gov (United States)

    Wang, Ji-fen; Yu, Jing; Guo, Xin; Sun, Xing-long; Wang, Ding-fang

    2011-07-01

    The method of rapid analysis of added ingredients in heroin was studied in the present paper. Adding sucrose, fructose, glucose, starch, caffeine and phenacetin to heroin with a certain percentage, the changes in the infrared spectrum with the concentration of heroin increasing and the detection limit of the additives were determined. Whether or not heroin can be detected in the sample with high concentration of added ingredients was studied using Raman spectroscopy. Similarly, in high purity of heroin, whether or not Raman spectroscopy can detect the added ingredients was tested. Through systematic experiments, the results showed that: using infrared spectroscopy and Raman spectroscopy to test the added ingredients of heroin is a rapid and effective method. Each has both advantages and disadvantages. We should select the appropriate method according to the actual cases.

  8. ENRICHMENT OF POULTRY PRODUCTS WITH FUNCTIONAL INGREDIENTS

    OpenAIRE

    Gordana Kralik; Zlata Kralik; Manuela Grčević; Zoran Škrtić

    2012-01-01

    Primary role of food is to provide nutritive stuffs in sufficient amounts to meet nutritive requirements. However, recent scientific findings confirm assumptions that particular food or its ingredients had positive physiological and psychological effects on health. Functional food is referred to food rich in ingredients, having beneficial effects on one or more functions in an organism. By consuming functional food consumers can expect some health benefits. Production of poultry products as f...

  9. A systematic review of quality of life and weight gain-related issues in patients treated for severe and persistent mental disorders: focus on aripiprazole

    Directory of Open Access Journals (Sweden)

    Salvatore Gentile

    2009-02-01

    Full Text Available Salvatore GentileDepartment of Mental Health, ASL Salerno 1, ItalyAbstract: Aripiprazole is a relatively novel second-generation antipsychotic belonging to the chemical class of benzisoxazole derivatives and is characterized by a unique pharmacological profile which suggests that the drug acts as a dopamine-serotonin system stabilizer. Whereas all previously available antipsychotics are antagonists at D2 receptors, aripiprazole is the only available partial agonist at these receptors. Thus, it has been suggested that aripiprazole could be associated with a relatively neutral impact on bodyweight, possibly reducing risks of a detrimental impact on the quality of life that often complicates management for a large number of patients diagnosed with severe and persistent mental disorders (SPMDs treated chronically with antipsychotic medications. However, data from short- and long-term reviewed studies indicate that the prevalence rate of clinically relevant weight gain during therapy with this drug is similar to that occurring during treatments with other antipsychotic agents, either typical or atypical. Moreover, information on the impact of aripiprazole therapy on the quality of life of patients diagnosed with SPMDs is scarce and characterized by conflicting results. Given these results, further, large, well-designed studies are needed before confirming potential advantages of aripiprazole over first-generation antipsychotics and other SGAs.Keywords: aripiprazole, effectiveness, quality of life, safety, weight gain

  10. No negative symptoms in healthy volunteers after single doses of amisulpride, aripiprazole, and haloperidol: a double-blind placebo-controlled trial.

    Science.gov (United States)

    Park, Chul-Hyun; Park, Tae-Won; Yang, Jong-Chul; Lee, Keon-Hak; Huang, Guang-Biao; Tong, Zhao; Park, Myung-Sook; Chung, Young-Chul

    2012-03-01

    Noncompliance and poor outcome in patients with schizophrenia are closely related to the negative symptoms secondary to antipsychotics. No controlled study has evaluated whether amisulpride and aripiprazole induce negative symptoms. The aim of this study was to assess the effects of single doses of amisulpride, aripiprazole, haloperidol, and risperidone in healthy volunteers. Seventy-eight young volunteers took part in this double-blind, randomized, placebo-controlled, parallel study of four antipsychotics: 400 mg amisulpride, 10 mg aripiprazole, 3 mg haloperidol, and 2 mg risperidone. Assessments of negative symptoms were done 4 h after administration using both subjective rating scales (Neuroleptic Induced Deficit Syndrome Scale and Subjective Deficit Syndrome Scale) and an objective rating scale (Scale for the Assessment of Negative Symptoms). Risperidone only produced significant increases on the avolition score of the Neuroleptic Induced Deficit Syndrome Scale and blunted affect and alogia scores of the Scale for the Assessment of Negative Symptoms compared with placebo. The effect on blunted affect persisted after controlling for mental sedation. Amisulpride, aripiprazole, and haloperidol did not induce negative symptoms. Aripiprazole and risperidone induced mild extrapyramidal symptoms. The most common adverse events were somnolence and cognitive slowing. These data indicate that a single risperidone dose induces negative symptoms in normal volunteers, whereas amisulpride, aripiprazole, and haloperidol do not. These characteristics of antipsychotics should be considered when choosing optimal drugs for patients with psychosis.

  11. The supernova rate: a critical ingredient and an important tool

    CERN Document Server

    Mannucci, F

    2009-01-01

    In this review I summarize the role of supernova rate as a critical ingredient of modern astrophysics, and as an important tool to understand SN explosions. Many years of active observations and theoretical modeling have produced several important results. In particular, linking SN rates with parent stellar populations has proved to be an important strategy. Despite these advances, the situation is far from clear, in particular for the SNe Ia.

  12. Burning characteristics of chemically isolated biomass ingredients

    Energy Technology Data Exchange (ETDEWEB)

    Haykiri-Acma, H.; Yaman, S.; Kucukbayrak, S. [Istanbul Technical University, Chemical and Metallurgical Engineering Faculty, Chemical Engineering Department, 34469 Maslak, Istanbul (Turkey)

    2011-01-15

    This study was performed to investigate the burning characteristics of isolated fractions of a biomass species. So, woody shells of hazelnut were chemically treated to obtain the fractions of extractives-free bulk, lignin, and holocellulose. Physical characterization of these fractions were determined by SEM technique, and the burning runs were carried out from ambient to 900 C applying thermal analysis techniques of TGA, DTG, DTA, and DSC. The non-isothermal model of Borchardt-Daniels was used to DSC data to find the kinetic parameters. Burning properties of each fraction were compared to those of the raw material to describe their effects on burning, and to interpret the synergistic interactions between the fractions in the raw material. It was found that each of the fractions has its own characteristic physical and thermal features. Some of the characteristic points on the thermograms of the fractions could be followed definitely on those of the raw material, while some of them seriously shifted to other temperatures or disappeared as a result of the co-existence of the ingredients. Also, it is concluded that the presence of hemicellulosics and celluloses makes the burning of lignin easier in the raw material compared to the isolated lignin. The activation energies can be arranged in the order of holocellulose < extractives-free biomass < raw material < lignin. (author)

  13. Biochemical basis for functional ingredient design from fruits.

    Science.gov (United States)

    Jacob, Jissy K; Tiwari, Krishnaraj; Correa-Betanzo, Julieta; Misran, Azizah; Chandrasekaran, Renu; Paliyath, Gopinadhan

    2012-01-01

    Functional food ingredients (nutraceuticals) in fruits range from small molecular components, such as the secondary plant products, to macromolecular entities, e.g., pectin and cellulose, that provide several health benefits. In fruits, the most visible functional ingredients are the color components anthocyanins and carotenoids. In addition, several other secondary plant products, including terpenes, show health beneficial activities. A common feature of several functional ingredients is their antioxidant function. For example, reactive oxygen species (ROS) can be oxidized and stabilized by flavonoid components, and the flavonoid radical can undergo electron rearrangement stabilizing the flavonoid radical. Compounds that possess an orthodihydroxy or quinone structure can interact with cellular proteins in the Keap1/Nrf2/ARE pathway to activate the gene transcription of antioxidant enzymes. Carotenoids and flavonoids can also exert their action by modulating the signal transduction and gene expression within the cell. Recent results suggest that these activities are primarily responsible for the health benefits associated with the consumption of fruits and vegetables.

  14. Phenolic content and antioxidant properties of green chilli paste and its ingredients

    Directory of Open Access Journals (Sweden)

    Griangsak Chairote

    2010-05-01

    Full Text Available Green chilli paste and its ingredients (chilli, red onion and garlic from different stages of processing were analysed for total phenolic content and antioxidant properties, i.e. total antioxidant capacity, DPPH radical scavenging activity, and β-carotene bleaching activity. The effects of processing stage on total phenolic content and antioxidant properties of green chilli paste and its ingredients were discussed, along with the correlation between the total phenolic content and the antioxidant properties.

  15. Safety and efficacy of aripiprazole for the treatment of pediatric Tourette syndrome and other chronic tic disorders

    Directory of Open Access Journals (Sweden)

    Cox JH

    2016-06-01

    Full Text Available Joanna H Cox,1 Stefano Seri,2,3 Andrea E Cavanna,2,4,5 1Heart of England NHS Foundation Trust, 2School of Life and Health Sciences, Aston Brain Centre, Aston University, 3Children’s Epilepsy Surgery Programme, The Birmingham Children’s Hospital NHS Foundation Trust, 4Department of Neuropsychiatry, Birmingham and Solihull Mental Health NHS Foundation Trust, Birmingham, 5Sobell Department of Motor Neuroscience and Movement Disorders, Institute of Neurology and UCL, London, UK Abstract: Tourette syndrome is a childhood-onset chronic tic disorder characterized by multiple motor and vocal tics and often accompanied by specific behavioral symptoms ranging from obsessionality to impulsivity. A considerable proportion of patients report significant impairment in health-related quality of life caused by the severity of their tics and behavioral symptoms and require medical intervention. The most commonly used medications are antidopaminergic agents, which have been consistently shown to be effective for tic control, but are also associated with poor tolerability because of their adverse effects. The newer antipsychotic medication aripiprazole is characterized by a unique mechanism of action (D2 partial agonism, and over the last decade has increasingly been used for the treatment of tics. We conducted a systematic literature review to assess the available evidence on the efficacy and safety of aripiprazole in pediatric patients with Tourette syndrome and other chronic tic disorders (age range: 4–18 years. Our search identified two randomized controlled trials (involving 60 and 61 participants and ten open-label studies (involving between six and 81 participants. The majority of these studies used two validated clinician-rated instruments (Yale Global Tic Severity Scale and Clinical Global Impression scale as primary outcome measures. The combined results from randomized controlled trials and open-label studies showed that aripiprazole is an

  16. Dilemma of prescribing aripiprazole under the Taiwan health insurance program: a descriptive study

    Directory of Open Access Journals (Sweden)

    Hsu YC

    2015-01-01

    Full Text Available Yi-Chien Hsu,1,2 Yu-Ching Chou,3 Hsin-An Chang,1,2,4 Yu-Chen Kao,1,2,5 San-Yuan Huang,1,2 Nian-Sheng Tzeng1,2,4 1Department of Psychiatry, Tri-Service General Hospital, Taipei, Taiwan; 2School of Medicine, 3School of Public Health, 4Student Counseling Center, National Defense Medical Center, Taipei, Taiwan; 5Department of Psychiatry, Tri-Service General Hospital, Song-Shan Branch, Taipei, Taiwan Objectives: Refractory major depressive disorder (MDD is a serious problem leading to a heavy economic burden. Antipsychotic augmentation treatment with aripiprazole and quetiapine is approved for MDD patients and can achieve a high remission rate. This study aimed to examine how psychiatrists in Taiwan choose medications and how that choice is influenced by health insurance payments and administrative policy.Design: Descriptive study.Outcome measures: Eight questions about the choice of treatment strategy and atypical antipsychotics, and the reason to choose aripiprazole.Intervention: We designed an augmentation strategy questionnaire for psychiatrists whose patients had a poor response to antidepressants, and handed it out during the annual meeting of the Taiwanese Society of Psychiatry in October 2012. It included eight questions addressing the choice of treatment strategy and atypical antipsychotics, and the reason whether or not to choose aripiprazole as the augmentation antipsychotic.Results: Choosing antipsychotic augmentation therapy or switching to other antidepressant strategies for MDD patients with an inadequate response to antidepressants was common with a similar probability (76.1% vs 76.4%. The most frequently used antipsychotics were aripiprazole and quetiapine, however a substantial number of psychiatrists chose olanzapine, risperidone, and sulpiride. The major reason for not choosing aripiprazole was cost (52.1%, followed by insurance official policy audit and deletion in the claims review system (30.1%.Conclusion: The prescribing

  17. Analysis on safety assessment and active ingredient of functional textiles%功能性纺织品的安全性评估及其功能因子的分析

    Institute of Scientific and Technical Information of China (English)

    魏孟媛; 和杉杉; 段冀渊; 陈宇凤; 薛文良

    2014-01-01

    我国对功能性纺织品的需求很大,目前功能性纺织品的功能主要通过纺织品的后整理实现。后整理会对环境和消费者造成一定的危害。通过对市场上功能性纺织品功能因子的调研,并与相关法规及资料(包括欧盟REACH法规附录17及其SVHC高关注度物质,美国服装鞋类协会受限物质清单RSL,美国加州65号法案,我国化学品环境风险防控“十二五”规划,《纺织行业有毒有害物质消除指南》)进行了整理比对,明确了市场中功能因子存在的安全隐患,为功能性纺织品的安全性检验提供一定的依据。%There is a great demand for functional textile in China .Functional textiles have been developed that rely upon the approach of finishing , whose chemical agents have chances to be harmful to our environment and consumers’ health.Integrating the survey results on functional textiles with related acts and rules , the active ingredients of toxicity in functional textiles and provides advice on further safety inspections were listed .The above mentioned actions and rules are REACH ( appendix 17 and the SVHC ) , RSL established by AAFA , safe drinking water and toxic enforcement act of 1986 , prevention and control for environmental risks of chemicals in 12 th five-year plan of China and “Toxics use elimination guideline for the textile industry 1.0 by greenpeace”.

  18. Determination of palladium, platinum and rhodium in used automobile catalysts and active pharmaceutical ingredients using high-resolution continuum source graphite furnace atomic absorption spectrometry and direct solid sample analysis

    Energy Technology Data Exchange (ETDEWEB)

    Resano, Martín, E-mail: mresano@unizar.es [Department of Analytical Chemistry, Aragón Institute of Engineering Research (I3A), University of Zaragoza, Pedro Cerbuna 12, 50009 Zaragoza (Spain); Flórez, María del Rosario [Department of Analytical Chemistry, Aragón Institute of Engineering Research (I3A), University of Zaragoza, Pedro Cerbuna 12, 50009 Zaragoza (Spain); Queralt, Ignasi [Institute of Earth Sciences Jaume Almera ICTJA-CSIC, Sole Sabarís s/n, 08028 Barcelona (Spain); Marguí, Eva [Department of Chemistry, Faculty of Sciences, Universitat de Girona, Campus Montilivi s/n, 17071 Girona (Spain)

    2015-03-01

    This work investigates the potential of high-resolution continuum source graphite furnace atomic absorption spectrometry for the direct determination of Pd, Pt and Rh in two samples of very different nature. While analysis of active pharmaceutical ingredients is straightforward and it is feasible to minimize matrix effects, to the point that calibration can be carried out against aqueous standard solutions, the analysis of used automobile catalysts is more challenging requiring the addition of a chemical modifier (NH{sub 4}F·HF) to help in releasing the analytes, a more vigorous temperature program and the use of a solid standard (CRM ERM®-EB504) for calibration. However, in both cases it was possible to obtain accurate results and precision values typically better than 10% RSD in a fast and simple way, while only two determinations are needed for the three analytes, since Pt and Rh can be simultaneously monitored in both types of samples. Overall, the methods proposed seem suited for the determination of these analytes in such types of samples, offering a greener and faster alternative that circumvents the traditional problems associated with sample digestion, requiring a small amount of sample only (0.05 mg per replicate for catalysts, and a few milligrams for the pharmaceuticals) and providing sufficient sensitivity to easily comply with regulations. The LODs achieved were 6.5 μg g{sup −1} (Pd), 8.3 μg g{sup −1} (Pt) and 9.3 μg g{sup −1} (Rh) for catalysts, which decreased to 0.08 μg g{sup −1} (Pd), 0.15 μg g{sup −1} (Pt) and 0.10 μg g{sup −1} (Rh) for pharmaceuticals. - Highlights: • Solid sampling HR CS GFAAS permits the fast and direct determination of Pd, Pt and Rh. • 2 determinations suffice for the 3 elements (2 of them can be measured simultaneously). • Samples as different as car catalysts and pharmaceuticals can be accurately analyzed. • Aqueous standards (pharmaceuticals) or a solid CRM (catalysts) is used for calibration.

  19. Extraction of active ingredients in Honey suckle and their function in cosmetics%金银花活性成分提取及其抗氧化和抑菌功效研究

    Institute of Scientific and Technical Information of China (English)

    宋小锋; 原增艳; 许平辉

    2012-01-01

    利用超声波预处理结合乙醇回流提取法从金银花中提取活性成分,通过响应面分析法设计实验,得到了较佳的提取工艺:超声波预处理30.9 min,乙醇的体积分数为73.7%,提取温度为68.5℃,每次提取2.1h,提取2次,在此条件下绿原酸提取率达到88.39%.通过与阳性物质Vc比较检验了提取物的功效,证明金银花提取物具有较好的体外抗氧化能力;通过对大肠杆菌、金黄色葡萄球菌、黑曲霉的抑制分析,证明金银花提取物具有良好的抑菌防腐能力.%Active ingredients in Honey suckle were extracted by ultrasonic -aided ethanol method. The optimal processing conditions for the extraction were identified by using the software "Design Expert 7. 1. 3 Tril". Pretreatment time is 30. 9 min under aid of ultrasonic wave. Ethanol with volume fraction of 73. 7% was used as the solvent. Temperature was 68. 5 ℃. Extraction of two times was operated with each of 2. 1 h. Under the afore - said conditions, yield of chlorogenic acid achieves 88.39%. Comparing with positive material vitamin C,the efficacy of the extract was investigated and experimental results showed that the extract has a good in - vitro antioxidation capability. Bacteriostasis tests were carried out against colibacillus, Staphylococcus aureus and Aspergillus niger and the results showed that the Honey suckle extract has strong bacteriostatic and antiseptic capabilities.

  20. 9 CFR 113.50 - Ingredients of biological products.

    Science.gov (United States)

    2010-01-01

    ... 9 Animals and Animal Products 1 2010-01-01 2010-01-01 false Ingredients of biological products... REQUIREMENTS Ingredient Requirements § 113.50 Ingredients of biological products. All ingredients used in a licensed biological product shall meet accepted standards of purity and quality; shall be...

  1. HPLC法测定复方前列舒丸中6个活性成分%Determination of six active ingredients in Compound Qianlieshu Pills by HPLC

    Institute of Scientific and Technical Information of China (English)

    李征; 董斌; 李宪刚

    2016-01-01

    Objective To establish an HPLC method for simultaneous determination of six active ingredients plantamajoside, naringin, hesperidin, neohesperidin, epimedin C, and icariin in Compound Qianlieshu Pills. Methods The determination was carried out with Agilent Zorbax C18 column (250 mm × 4.6 mm, 5μm). The mobile phase consisted of acetonitrile-0.1%phosphoric acid solution with gradient elution. The detection wavelengths were 330 nm in 0—20 min (determination of plantamajoside) , 283 nm in 20—40 min (determination of naringin, hesperidin, and neohesperidin) , and 270 nm in 40—50 min ( determination of epimedin C and icariin). The column temperature was set at 35℃, and the flow rate was 1.0 mL/min with injection volume of 5μL. Results There were good linear relationships of plantamajoside, naringin, hesperidin, neohesperidin, epimedin C, and icariin in the concentration ranges of 10.11—202.20, 49.62—992.40, 15.46—309.20, 44.62—892.40, 18.39—367.80, and 52.18—1 043.60 ng. The average recoveries were 97.4%, 98.8%, 99.5%, 98.9%, 97.2%, and 95.6% with RSD 0.83%, 1.2%, 1.4%, 1.5%, 1.5%, and 1.0%, respectively. Conclusion The method is simple and valid, and can simultaneously determine six active ingredients plantamajoside, naringin, hesperidin, neohesperidin, epimedin C, and icariin, which can be used in quantity control for Compound Qianlieshu Pills.%目的:建立HPLC法同时测定复方前列舒丸中大车前苷、柚皮苷、橙皮苷、新橙皮苷、朝藿定C、淫羊藿苷6个活性成分的方法。方法采用安捷伦Zorbax C18色谱柱(250 mm×4.6 mm,5µm);流动相为乙腈–0.1%磷酸水溶液,梯度洗脱;检测波长为330 nm(0~20 min,测定大车前苷)、283 nm(20~40 min,测定柚皮苷、橙皮苷、新橙皮苷)、270 nm(40~50 min,测定朝藿定C、淫羊藿苷);柱温为35℃;体积流量为1.0 mL/min;进样量为5µL。结果大车前苷、柚皮苷、橙皮苷、新橙皮苷

  2. The partial dopamine D2 receptor agonist aripiprazole is associated with weight gain in adolescent anorexia nervosa.

    Science.gov (United States)

    Frank, Guido K W; Shott, Megan E; Hagman, Jennifer O; Schiel, Marissa A; DeGuzman, Marisa C; Rossi, Brogan

    2017-04-01

    Finding medication to support treatment of anorexia nervosa has been difficult. Neuroscience-based approaches may help in this effort. Recent brain imaging studies in adults and adolescents with anorexia nervosa suggest that dopamine-related reward circuits are hypersensitive and could provide a treatment target. Here, we present a retrospective chart review of 106 adolescents with anorexia nervosa some of whom were treated with the dopamine D2 receptor partial agonist aripiprazole during treatment in a specialized eating disorder program. The results show that aripiprazole treatment was associated with greater increase in body mass index (BMI) during treatment. The use of dopamine receptor agonists may support treatment success in anorexia nervosa and should be further investigated. © 2017 Wiley Periodicals, Inc.

  3. Salivary and serum biomarkers for the study of side effects of aripiprazole coprescribed with mirtazapine in rats

    Science.gov (United States)

    Bogdan, Maria; Silosi, Isabela; Surlin, Petra; Tica, Andrei Adrian; Tica, Oana Sorina; Balseanu, Tudor-Adrian; Rauten, Anne-Marie; Camen, Adrian

    2015-01-01

    The aim of this study was to investigate whether the co-administration of aripiprazole and mirtazapine could determine weight gain and lipid metabolism disorders in Wistar rats, compared to the same side effects produced by mirtazapine alone, and the risk of hepatotoxicity due to the combination of the two substances. Tumor necrosis factor alpha (TNF-α), liver fatty acid binding protein (L-FABP/FABP1) and repulsive guidance molecule C/hemojuvelin (RGM-C/HJV) levels were determined in serum and in saliva. Also, serum levels for total cholesterol (TC), low and high-density lipoprotein (LDL, HDL), triglycerides (TG), aspartate aminotransferase (ASAT) and alanine amino transferase (ALAT) were assessed. We found positive and statistically significant correlations between serum and salivary levels of TNF-α, L-FABP/FABP1 and RGM-C/HJV. Mirtazapine determined significantly differences of TNF-α and L-FABP serum levels; final body weight; TC and LDL levels, leading to higher concentrations than its association with aripiprazole. Although not statistically significant, mirtazapine group experienced higher values for salivary levels of TNF-α, TG and ASAT, and lower values for HDL, compared to aripiprazole + mirtazapine group. The results suggest that aripiprazole might improve some of the disturbances caused by mirtazapine, and that the two drugs combination cause no additional alterations in liver function. Also, the findings indicate that TNF-α, L-FABP/FABP1 and RGM-C/HJV levels can be helpful as biomarkers for metabolic disturbances and impaired function of hepatocytes, and that their salivary determination can replace serum determination. PMID:26221370

  4. Salivary and serum biomarkers for the study of side effects of aripiprazole coprescribed with mirtazapine in rats.

    Science.gov (United States)

    Bogdan, Maria; Silosi, Isabela; Surlin, Petra; Tica, Andrei Adrian; Tica, Oana Sorina; Balseanu, Tudor-Adrian; Rauten, Anne-Marie; Camen, Adrian

    2015-01-01

    The aim of this study was to investigate whether the co-administration of aripiprazole and mirtazapine could determine weight gain and lipid metabolism disorders in Wistar rats, compared to the same side effects produced by mirtazapine alone, and the risk of hepatotoxicity due to the combination of the two substances. Tumor necrosis factor alpha (TNF-α), liver fatty acid binding protein (L-FABP/FABP1) and repulsive guidance molecule C/hemojuvelin (RGM-C/HJV) levels were determined in serum and in saliva. Also, serum levels for total cholesterol (TC), low and high-density lipoprotein (LDL, HDL), triglycerides (TG), aspartate aminotransferase (ASAT) and alanine amino transferase (ALAT) were assessed. We found positive and statistically significant correlations between serum and salivary levels of TNF-α, L-FABP/FABP1 and RGM-C/HJV. Mirtazapine determined significantly differences of TNF-α and L-FABP serum levels; final body weight; TC and LDL levels, leading to higher concentrations than its association with aripiprazole. Although not statistically significant, mirtazapine group experienced higher values for salivary levels of TNF-α, TG and ASAT, and lower values for HDL, compared to aripiprazole + mirtazapine group. The results suggest that aripiprazole might improve some of the disturbances caused by mirtazapine, and that the two drugs combination cause no additional alterations in liver function. Also, the findings indicate that TNF-α, L-FABP/FABP1 and RGM-C/HJV levels can be helpful as biomarkers for metabolic disturbances and impaired function of hepatocytes, and that their salivary determination can replace serum determination.

  5. Enhancement of encapsulation efficiency of nanoemulsion-containing aripiprazole for the treatment of schizophrenia using mixture experimental design

    Directory of Open Access Journals (Sweden)

    Fard Masoumi HR

    2015-10-01

    Full Text Available Hamid Reza Fard Masoumi, Mahiran Basri, Wan Sarah Samiun, Zahra Izadiyan, Chaw Jiang Lim Nanodelivery Group, Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, Serdang, Selangor, Malaysia Abstract: Aripiprazole is considered as a third-generation antipsychotic drug with excellent therapeutic efficacy in controlling schizophrenia symptoms and was the first atypical anti­psychotic agent to be approved by the US Food and Drug Administration. Formulation of nanoemulsion-containing aripiprazole was carried out using high shear and high pressure homo­genizers. Mixture experimental design was selected to optimize the composition of nanoemulsion. A very small droplet size of emulsion can provide an effective encapsulation for delivery system in the body. The effects of palm kernel oil ester (3–6 wt%, lecithin (2–3 wt%, Tween 80 (0.5–1 wt%, glycerol (1.5–3 wt%, and water (87–93 wt% on the droplet size of aripiprazole nanoemulsions were investigated. The mathematical model showed that the optimum formulation for preparation of aripiprazole nanoemulsion having the desirable criteria was 3.00% of palm kernel oil ester, 2.00% of lecithin, 1.00% of Tween 80, 2.25% of glycerol, and 91.75% of water. Under optimum formulation, the corresponding predicted response value for droplet size was 64.24 nm, which showed an excellent agreement with the actual value (62.23 nm with residual standard error <3.2%. Keywords: schizoaffective disorder, antipsychotic drug, bipolar I disorder, D-optimal mixture design, optimization formulation

  6. Switching to Aripiprazole as a Strategy for Weight Reduction: A Meta-Analysis in Patients Suffering from Schizophrenia

    Directory of Open Access Journals (Sweden)

    Yoram Barak

    2011-01-01

    Full Text Available Weight gain is one of the major drawbacks associated with the pharmacological treatment of schizophrenia. Existing strategies for the prevention and treatment of obesity amongst these patients are disappointing. Switching the current antipsychotic to another that may favorably affect weight is not yet fully established in the psychiatric literature. This meta-analysis focused on switching to aripiprazole as it has a pharmacological and clinical profile that may result in an improved weight control. Nine publications from seven countries worldwide were analyzed. These encompassed 784 schizophrenia and schizoaffective patients, 473 (60% men and 311 (40% women, mean age 39.4±7.0 years. The major significant finding was a mean weight reduction by −2.55±1.5 kgs following the switch to aripiprazole (<.001. Switching to an antipsychotic with a lower propensity to induce weight gain needs be explored as a strategy. Our analysis suggests aripiprazole as a candidate for such a treatment strategy.

  7. Long-term safety and tolerability of aripiprazole once-monthly in maintenance treatment of patients with schizophrenia.

    Science.gov (United States)

    Fleischhacker, W Wolfgang; Sanchez, Raymond; Johnson, Brian; Jin, Na; Forbes, Robert A; McQuade, Robert; Baker, Ross A; Carson, William; Kane, John M

    2013-07-01

    The aim of this study was to evaluate the safety and tolerability of aripiprazole once-monthly (ARI-OM) for the maintenance treatment of schizophrenia. This long-term, pivotal study had four phases: oral conversion (phase 1, 4-6 weeks); oral stabilization (phase 2, 4-12 weeks); ARI-OM stabilization with coadministration of oral aripiprazole in the first 2 weeks (phase 3, 12-36 weeks); and a 52-week, randomized [phase 4, ARI-OM vs. placebo (2 : 1)], double-blind, maintenance phase. Safety was assessed across study phases by the time of first onset of adverse events, as were objective measures of extrapyramidal symptoms, fasting metabolic parameters, and body weight. Patient enrollment was phase 1=633; phase 2=710, of whom 210 entered phase 2 directly; phase 3=576; and phase 4=403 (ARI-OM, n=269; placebo, n=134). Adverse events (>5%) in any phase were insomnia, headache, anxiety, akathisia, increase in weight, injection-site pain, and tremor. Headache, somnolence, and nausea had a peak first onset within 4 weeks of treatment initiation. The incidence of extrapyramidal symptoms was similar in all phases. There were no unexpected changes in weight or shifts in fasting metabolic parameters across all study phases. ARI-OM had a safety and tolerability profile comparable with oral aripiprazole in maintenance treatment of schizophrenia.

  8. Chemical Ingredients of Cordyceps militaris

    OpenAIRE

    Hur, Hyun

    2008-01-01

    Medicinal mushrooms, including Cordyceps militaris, have received attention in Korea because of their biological activities. In the fruiting body and in corpus of C. militaris, the total free amino acid content was 69.32 mg/g and 14.03 mg/g, respectively. In the fruiting body, the most abundant amino acids were lysine, glutamic acid, proline and threonine. The fruiting body was rich in unsaturated fatty acids, which comprised about 70% of the total fatty acids. The most abundant unsaturated a...

  9. Chemical Ingredients of Cordyceps militaris

    OpenAIRE

    Hur, Hyun

    2008-01-01

    Medicinal mushrooms, including Cordyceps militaris, have received attention in Korea because of their biological activities. In the fruiting body and in corpus of C. militaris, the total free amino acid content was 69.32 mg/g and 14.03 mg/g, respectively. In the fruiting body, the most abundant amino acids were lysine, glutamic acid, proline and threonine. The fruiting body was rich in unsaturated fatty acids, which comprised about 70% of the total fatty acids. The most abundant unsaturated a...

  10. Aripiprazole Injection

    Science.gov (United States)

    ... for them, such as increased sexual urges or behaviors, excessive shopping, and binge eating. Call your doctor if you have intense urges to shop, eat, have sex, or gamble, or if you are unable to control your behavior. Tell your family members about this risk so ...

  11. Época e princípios ativos para a quebra de dormência de caquizeiro cv. Fuyu Time and active ingredients for bud break of japanese persimmon cv. Fuyu

    Directory of Open Access Journals (Sweden)

    Ricardo Antonio Ayub

    2009-09-01

    Full Text Available Este trabalho foi realizado com o objetivo de aumentar o período de oferta do caqui 'Fuyu' e buscar alternativas à falta de opções para estimular a brotação, avaliando-se épocas e diferentes princípios ativos na quebra de dormência dos frutos. Os tratamentos testados foram: óleo mineral (OM, cianamida hidrogenada (CH e a mistura de macro e micronutrientes, em três épocas de aplicação, constituindo-se esquema fatorial com 5 tratamentos e 3 épocas de aplicação. Os tratamentos testados foram: T1-testemunha; T2- 0,5 % OM; T3-: 2 % CH + 0,5 % OM; T4- 1 % micronutrientes + 0,2 % macronutrientes + 0,5 % OM; T5- 2 % micronutrientes + 0,2 % macronutrientes + 0,5 % OM. Avaliaram-se o número de brotos por ramo, a porcentagem de gemas brotadas e o número de ramos com broto, o número e a produção de frutos por planta. A antecipação da época de quebra de dormência provocou a diminuição do número de frutos produzidos na região centro-sul do Paraná. A produção de frutos foi diretamente proporcional à porcentagem de gemas brotadas no primeiro surto de brotação. A aplicação de cianamida hidrogenada promoveu antecipação da brotação e aumento na produção de frutos de caquizeiro; no entanto, a mistura de micronutrientes e óleo mineral não influenciou na brotação e produção de frutos de caquizeiro.This work aimed to rise fruit market period and search options to stimulate bud break, evaluating three dates and different active ingredients in bud break of persimmon 'Fuyu'. Mineral oil, hydrogen cyanamide (CH, micro and macronutrients mixture were tested in three application dates in a factorial scheme with 5 treatments and 3 application dates. The traetments were: T1-control, T2- 0.5 % OM, T3-: 2 % CH + 0.5 % OM, T4- 1 % micronutrients + 0.2 % macronutrients + 0.5 % OM; T5- 2 % micronutrients + 0.2 % macronutrients + 0.5 % OM. It was analyzed the number of sprouts per branch, the sprouting percentage, the number of

  12. Chemical Ingredients of Cordyceps militaris

    Science.gov (United States)

    2008-01-01

    Medicinal mushrooms, including Cordyceps militaris, have received attention in Korea because of their biological activities. In the fruiting body and in corpus of C. militaris, the total free amino acid content was 69.32 mg/g and 14.03 mg/g, respectively. In the fruiting body, the most abundant amino acids were lysine, glutamic acid, proline and threonine. The fruiting body was rich in unsaturated fatty acids, which comprised about 70% of the total fatty acids. The most abundant unsaturated acid was linoleic acid. There were differences in adenosine and cordycepin contents between the fruiting body and the corpus. The adenosine concentration was 0.18% in the fruiting body and 0.06% in the corpus, and the cordycepin concentration was 0.97% in the fruiting body and 0.36% in the corpus. PMID:23997632

  13. ENRICHMENT OF POULTRY PRODUCTS WITH FUNCTIONAL INGREDIENTS

    Directory of Open Access Journals (Sweden)

    Gordana Kralik

    2012-06-01

    Full Text Available Primary role of food is to provide nutritive stuffs in sufficient amounts to meet nutritive requirements. However, recent scientific findings confirm assumptions that particular food or its ingredients had positive physiological and psychological effects on health. Functional food is referred to food rich in ingredients, having beneficial effects on one or more functions in an organism. By consuming functional food consumers can expect some health benefits. Production of poultry products as functional food is getting more important on foreign markets while portion of such products on domestic food market is insignificant. The aim of this paper is to present possibilities for enrichment of poultry products, such as broiler and turkey meat and chicken eggs, as they can be characterized as functional food. Functional ingredients in poultry products are polyunsaturated fatty acids (LNA, EPA and DHA and antioxidants. Enrichment of poultry products with the stated ingredients that are beneficial for human health is subject of many researches, and only recently have researches been directed towards assessment of market sustainability of such products.

  14. Overview of Food Ingredients, Additives and Colors

    Science.gov (United States)

    ... Improve Taste, Texture and Appearance: Spices, natural and artificial flavors, and sweeteners are added to enhance the taste of food. ... Q What is the difference between natural and artificial ingredients? Is a naturally ... low-calorie sweeteners cause adverse reactions? Q How do they add ...

  15. Effects of dopamine D2 receptor partial agonist antipsychotic aripiprazole on dopamine synthesis in human brain measured by PET with L-[β-11C]DOPA.

    Directory of Open Access Journals (Sweden)

    Hiroshi Ito

    Full Text Available Dopamine D(2 receptor partial agonist antipsychotic drugs can modulate dopaminergic neurotransmission as functional agonists or functional antagonists. The effects of antipsychotics on presynaptic dopaminergic functions, such as dopamine synthesis capacity, might also be related to their therapeutic efficacy. Positron emission tomography (PET was used to examine the effects of the partial agonist antipsychotic drug aripiprazole on presynaptic dopamine synthesis in relation to dopamine D(2 receptor occupancy and the resulting changes in dopamine synthesis capacity in healthy men. On separate days, PET studies with [(11C]raclopride and L-[β-(11C]DOPA were performed under resting condition and with single doses of aripiprazole given orally. Occupancy of dopamine D(2 receptors corresponded to the doses of aripiprazole, but the changes in dopamine synthesis capacity were not significant, nor was the relation between dopamine D(2 receptor occupancy and these changes. A significant negative correlation was observed between baseline dopamine synthesis capacity and changes in dopamine synthesis capacity by aripiprazole, indicating that this antipsychotic appears to stabilize dopamine synthesis capacity. The therapeutic effects of aripiprazole in schizophrenia might be related to such stabilizing effects on dopaminergic neurotransmission responsivity.

  16. Determining Whether a Definitive Causal Relationship Exists Between Aripiprazole and Tardive Dyskinesia and/or Dystonia in Patients With Major Depressive Disorder, Part 4: Case Report Data.

    Science.gov (United States)

    Macaluso, Matthew; Flynn, Alexandra; Preskorn, Sheldon

    2016-05-01

    This series of columns has 3 main goals: (1) to explain class warnings as used by the United States Food and Drug Administration, (2) to increase awareness of movement disorders that may occur in patients treated with antipsychotic medications, and (3) to understand why clinicians should refrain from immediately assuming a diagnosis of tardive dyskinesia/dystonia (TD) in patients who develop abnormal movements during treatment with antipsychotics. The first column in the series presented a patient who developed abnormal movements while being treated with aripiprazole as an augmentation strategy for major depressive disorder and reviewed data concerning the historical background, incidence, prevalence, and risk factors for tardive and spontaneous dyskinesias, the clinical presentations of which closely resemble each other. The second column in the series reviewed the unique mechanism of action of aripiprazole and reviewed preclinical studies and an early-phase human translational study that suggest a low, if not absent, risk of TD with aripiprazole. The third column in this series reviewed the registration trial data for aripiprazole across all of its indications and found a raw incidence of TD ranging from 0.004 (4 out of 987) in long-term studies of the drug as an augmentation strategy for major depressive disorder to 0.0016 (19 out of 11,897) based on all short-term (ie, weeks to causal relationship between aripiprazole and TD exists.

  17. SPE-UPLC-MS/MS method for sensitive and rapid determination of aripiprazole in human plasma to support a bioequivalence study.

    Science.gov (United States)

    Patel, Daxesh P; Sharma, Primal; Sanyal, Mallika; Shrivastav, Pranav S

    2013-04-15

    An improved and rugged UPLC-MS/MS method has been developed and validated for sensitive and rapid determination of aripiprazole in human plasma using aripiprazole-d8 as the internal standard (IS). The analyte and IS were extracted from 100 μL of human plasma by solid-phase extraction using Phenomenex Strata-X (30 mg, 1 cc) cartridges. Chromatography was achieved on an Acquity UPLC BEH C18 (50 mm × 2.1 mm, 1.7 μm) analytical column using methanol: 10mM ammonium formate (85:15, v/v) as the mobile phase with isocratic elution. Quantitation was done using multiple reaction monitoring in the positive ionization mode. The linearity of the method was established in the concentration range 0.05-80 ng/mL. The mean extraction recovery was greater than 96% across QC levels, while intra- and inter batch accuracy and precision (% CV) values ranged from 97.4 to 101.9% and from 1.20 to 3.72% respectively. The relative matrix effect in eight different lots of plasma samples, expressed as % CV for the calculated slopes of calibration curves was 1.08%. The stability of aripiprazole was studied under different storage conditions. The validated method was used to support a bioequivalence study of 10mg aripiprazole formulation in 36 healthy Indian subjects.

  18. Reduction of Severity of Recurrent Psychotic Episode by Sustained Treatment with Aripiprazole in a Schizophrenic Patient with Dopamine Supersensitivity: A Case Report

    Science.gov (United States)

    Tadokoro, Shigenori; Nonomura, Naho; Kanahara, Nobuhisa; Hashimoto, Kenji; Iyo, Masaomi

    2017-01-01

    Dopamine supersensitivity psychosis (DSP) is a type of acute exacerbation of recurrent psychosis caused by long-term treatment with antipsychotics in schizophrenic patients. Although DSP is exceedingly troublesome for clinicians, effective treatment has not yet been established. Based on clinical research and our animal study, we hypothesize that aripiprazole, an atypical anti-psychotic, may reduce the exacerbation of recurrent psychotic episodes. We report the case of a 46-year-old female who suffered from schizophrenia with DSP. In this case, sustained treatment with a high dose of aripiprazole gradually reduced the severity of her recurrent psychotic episodes. In conclusion, sustained treatment with aripiprazole may reduce the exacerbation of recurrent psychotic episodes in schizophrenic patients with DSP, and may be an effective treatment of DSP. PMID:28138118

  19. Thermal Decomposition of IMX-104: Ingredient Interactions Govern Thermal Insensitivity

    Energy Technology Data Exchange (ETDEWEB)

    Maharrey, Sean [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Wiese-Smith, Deneille [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Highley, Aaron M. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Steill, Jeffrey D. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Behrens, Richard [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Kay, Jeffrey J. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States)

    2015-04-01

    This report summarizes initial studies into the chemical basis of the thermal insensitivity of INMX-104. The work follows upon similar efforts investigating this behavior for another DNAN-based insensitive explosive, IMX-101. The experiments described demonstrate a clear similarity between the ingredient interactions that were shown to lead to the thermal insensitivity observed in IMX-101 and those that are active in IMX-104 at elevated temperatures. Specifically, the onset of decomposition of RDX is shifted to a lower temperature based on the interaction of the RDX with liquid DNAN. This early onset of decomposition dissipates some stored energy that is then unavailable for a delayed, more violent release.

  20. Dimeric Surfactants: Promising Ingredients of Cosmetics and Toiletries

    Directory of Open Access Journals (Sweden)

    Naveen Kumar

    2013-11-01

    Full Text Available Surfactants are an essential ingredient for cosmetic, toiletries and personal care products for enhancing their performance. Dimeric surfactants demonstrate superiority compared to conventional surfactants in all areas of application. Dimeric surfactants are extremely promising for utilization in various cosmetic formulations viz. shampoo, lotions, creams, conditioners etc. These surfactants possess extremely unique surface properties viz. lower surface tension, unique micellization, low critical micelle concentration (CMC and antimicrobial activity, higher solubilization etc. Dimerics enhance the performances of cosmetics in an extraordinary manner and provide eco-friendly preparations for human epidermis.

  1. Impact of Light Intensity on Biosynthesis of Active Ingredients in Epimedium%光照对淫羊藿活性成分生物合成的影响

    Institute of Scientific and Technical Information of China (English)

    魏国燕; 陈建军; 廖思红; 王瑛

    2012-01-01

    淫羊藿作为传统的中药材,具有补肾阳、强筋骨、祛风湿等功效.其主要功能活性成分为黄酮醇苷成分淫羊藿苷、朝藿定A、B、C等.本实验在武汉植物园内的药园和园外园两个不同生长环境下,研究两种不同光照对巫山淫羊藿(Epimedium wushanense T.S.Ying)WY品系和箭叶淫羊藿(Epimedium sagittatum( Sieb.& Zucc.)Maxim.) LT1、HN3品系4种主要活性成分生物合成的影响.结果显示,在药园环境生长的淫羊藿的光合速率要高于园外园生长的淫羊藿,药园生长的箭叶淫羊藿LT1、HN3品系的4种活性成分含量均高于园外园生长的同品系,而巫山淫羊藿WY品系则相反.光合速率对4种活性成分含量的积累有一定影响,与朝藿定A、B和淫羊藿苷含量呈显著正相关,与朝藿定C含量呈显著负相关.文中对光合速率与活性成分积累间的关系进行了讨论,还针对不同的淫羊藿品系提出了相应的栽培建议.%As a traditional Chinese medicinal herb, epimedii has effects on toning kidney, strengthening bones and muscles,and treating rheumatism. Its bioactive ingredients are mainly prenylated flavonol glycosides, including icariin, epimedin A,B,and C. Two light conditions [Yao-yuan (Medicinal Herb Garden) of Wuhan Botanical Garden,Yuan-wai-yuan of Wuhan Botanical Garden] were used to study how light affected the biosynthesis of the major bioactive ingredients in Epimedium wushanense T. S. Ying and Epimedium sagittatum (Sieb. & Zucc. ) Maxim. Results showed that the photosynthesis rate was higher in Yao-yuan than in Yuan-wai-yuan for both species. The four bioactive ingredients of E. sagittatum were higher in Yao-yuan than in Yuan-wai-yuan,but the opposite was found for E. wushanense. Photosynthesis rate had significant positive correlation with the content of epimedin A,B and icariin,but had significant negative correlation with epimedin C. The relationship between photosynthesis rate and accumulation of

  2. Ingredients and meals rather than recipes

    DEFF Research Database (Denmark)

    Woolrych, Alan; Hornbæk, Kasper; Frøkjær, Erik

    2011-01-01

    scheme for evaluation resources is developed, and the scheme is extended with project specific resources that impact the effective use of methods. With these reviews and analyses in place, implications for research, teaching, and practice are derived. Throughout, the article draws on culinary analogies....... A recipe is nothing without its ingredients, and just as the quality of what is cooked reflects the quality of its ingredients, so too does the quality of usability work reflect the quality of resources as configured and combined. A method, like a recipe, is at best a guide to action for those adopting......To better support usability practice, most usability research focuses on evaluation methods. New ideas in usability research are mostly proposed as new evaluation methods. Many publications describe experiments that compare methods. Comparisons may indicate that some methods have important...

  3. Aripiprazole in the maintenance treatment of bipolar disorder: a critical review of the evidence and its dissemination into the scientific literature.

    Directory of Open Access Journals (Sweden)

    Alexander C Tsai

    2011-05-01

    Full Text Available BACKGROUND: Aripiprazole, a second-generation antipsychotic medication, has been increasingly used in the maintenance treatment of bipolar disorder and received approval from the U.S. Food and Drug Administration for this indication in 2005. Given its widespread use, we sought to critically review the evidence supporting the use of aripiprazole in the maintenance treatment of bipolar disorder and examine how that evidence has been disseminated in the scientific literature. METHODS AND FINDINGS: We systematically searched multiple databases to identify double-blind, randomized controlled trials of aripiprazole for the maintenance treatment of bipolar disorder while excluding other types of studies, such as open-label, acute, and adjunctive studies. We then used a citation search to identify articles that cited these trials and rated the quality of their citations. Our evidence search protocol identified only two publications, both describing the results of a single trial conducted by Keck et al., which met criteria for inclusion in this review. We describe four issues that limit the interpretation of that trial as supporting the use of aripiprazole for bipolar maintenance: (1 insufficient duration to demonstrate maintenance efficacy; (2 limited generalizability due to its enriched sample; (3 possible conflation of iatrogenic adverse effects of abrupt medication discontinuation with beneficial effects of treatment; and (4 a low overall completion rate. Our citation search protocol yielded 80 publications that cited the Keck et al. trial in discussing the use of aripiprazole for bipolar maintenance. Of these, only 24 (30% mentioned adverse events reported and four (5% mentioned study limitations. CONCLUSIONS: A single trial by Keck et al. represents the entirety of the literature on the use of aripiprazole for the maintenance treatment of bipolar disorder. Although careful review identifies four critical limitations to the trial's interpretation

  4. 21 CFR 101.4 - Food; designation of ingredients.

    Science.gov (United States)

    2010-04-01

    ... that do not contain dietary ingredients, such as excipients, fillers, artificial colors, artificial sweeteners, flavors, or binders, shall be included in the ingredient list. (h) The common or usual name...

  5. Aripiprazole loaded poly(caprolactone) nanoparticles: Optimization and in vivo pharmacokinetics.

    Science.gov (United States)

    Sawant, Krutika; Pandey, Abhijeet; Patel, Sneha

    2016-09-01

    In the present investigation, a Quality by Design strategy was applied for formulation and optimization of aripiprazole (APZ) loaded PCL nanoparticles (APNPs) using nanoprecipitation method keeping entrapment efficiency (%EE) and particle size (PS) as critical quality attributes. Establishment of design space was done followed by analysis of its robustness and sensitivity. Characterization of optimized APNPs was done using DSC, FT-IR, PXRD and TEM studies and was evaluated for drug release, hemocompatibility and nasal toxicity. PS, zeta potential and %EE of optimized APNPs were found to be 199.2±5.65nm, -21.4±4.6mV and 69.2±2.34% respectively. In vitro release study showed 90±2.69% drug release after 8h. Nasal toxicity study indicated safety of developed formulation for intranasal administration. APNPs administered via intranasal route facilitated the brain distribution of APZ incorporated with the AUC0→8 in rat brain approximately 2 times higher than that of APNPs administered via intravenous route. Increase in Cmax was observed which might help in dose reduction along with reduction in dose related side effects. The results of the study indicate that intranasally administered APZ loaded PCL NPs can potentially transport APZ via nose to brain and can serve as a non-invasive alternative for the delivery of APZ to brain.

  6. Ingredients and change processes in occupational therapy for children: a grounded theory study.

    Science.gov (United States)

    Armitage, Samantha; Swallow, Veronica; Kolehmainen, Niina

    2017-05-01

    There is limited evidence about the effectiveness of occupational therapy interventions for participation outcomes in children with coordination difficulties. Developing theory about the interventions, i.e. their ingredients and change processes, is the first step to advance the evidence base. To develop theory about the key ingredients of occupational therapy interventions for children with coordination difficulties and the processes through which change in participation might happen. Grounded theory methodology, as described by Kathy Charmaz, was used to develop the theory. Children and parents participated in semi-structured interviews to share their experiences of occupational therapy and processes of change. Data collection and analysis were completed concurrently using constant comparison methods. Five key ingredients of interventions were described: performing activities and tasks; achieving; carer support; helping and supporting the child; and labelling. Ingredients related to participation by changing children's mastery experience, increasing capability beliefs and sense of control. Parents' knowledge, skills, positive emotions, sense of empowerment and capability beliefs also related to children's participation. The results identify intervention ingredients and change pathways within occupational therapy to increase participation. It is unclear how explicitly and often therapists consider and make use of these ingredients and pathway.

  7. HPLC-DAD法同时测定更年安片中6个活性成分的含量%HPLC-DAD simultaneous determination of six active ingredients in Gengnian' an tablets

    Institute of Scientific and Technical Information of China (English)

    施法; 侯峰; 陆军; 郭汉文; 张满来; 郝延军

    2012-01-01

    目的:建立同时分析测定更年安片中6个活性成分(2,3,5,4'-四羟基二苯乙烯-2 -O-β-D-葡萄糖苷、毛蕊花糖苷、仙茅苷、丹皮酚、哈巴俄苷、五味子醇甲)的方法.方法:采用HPLC-DAD法,色谱柱为奥泰Alltima ODS( 250 mm×4.6mm,5μm),以乙腈为流动相A,0.05%磷酸溶液为流动相B,梯度洗脱,流速1.0mL·min-1,检测波长为254 nm(测定五味子醇甲)、284 nm(测定仙茅苷、丹皮酚、哈巴俄苷)、330 nm(测定2,3,5,4'-四羟基二苯乙烯-2 -O-β-D-葡萄糖苷、毛蕊花糖苷).结果:2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷、毛蕊花糖苷、仙茅苷、丹皮酚、哈巴俄苷、五味子醇甲线性范围分别为0.0404~1.616 μg(r =0.9999),0.0194~0.774 μg(r =0.9998),0.0202 ~0.810μg(r =0.9997),0.0201~0.804μg(r=0.9999),0.0206~0.826μg(r=0.9998),0.0398~1.592 μg(r=0.9999).平均加样回收率(n=6)分别为97.8%,98.2%,97.9%,98.3%,101.2%,97.5%;RSD分别为1.2%,1.1%,0.95%,1.1%,0.97%,1.1%.结论:该方法操作简单,重复性好,为评价和监控更年安片的质量提供可靠的方法.%Objective;To establish a method for simultaneous determination of six active ingredients(2,3,5,4' -tetrahydroxystilbene -2 - 0 -β - D - glucoside, acteoside, curculigoside, paeonol, harpagoside, schisandrin). Methods; The determination was carried out with Alltima ODS column ( 250 mm x 4. 6 mm, 5 μm); The mobile phase consisted of acetonitrile( A) -0. 05% phosphoric acid solution( B) with gradient elution at a flow rate of 1. 0 Ml · min-1; The detection wavelengths were 254 nm for schisandrin, 284 nm for curculigoside, paeonol and harpagoside, 330 nm for 2,3,5,4' -tetrahydroxystilbene -2 - 0 -β - D - glucoside and acteoside. ResultS;The calibration curves were linear in the ranges of 0. 0404 -1.616 μg for 2,3,5 ,4' - tetrahydroxystilbene -2 - 0 -0 -D -glucoside(r =0. 9999), 0. 0194 -0. 774 μg for acteoside (r =0. 9998), 0. 0202 -0. 810 |xg for

  8. Anticarcinogenic effect of saffron (Crocus sativus L.) and its ingredients.

    Science.gov (United States)

    Samarghandian, Saeed; Borji, Abasalt

    2014-04-01

    Conventional and newly emerging treatment procedures such as chemotherapy, catalytic therapy, photodynamic therapy and radiotherapy have not succeeded in reversing the outcome of cancer diseases to any drastic extent, which has led researchers to investigate alternative treatment options. The extensive repertoire of traditional medicinal knowledge systems from various parts of the world are being re-investigated for their healing properties Crocus sativus L., commonly known as saffron, is the raw material for one of the most expensive spice in the world, and it has been used in folk medicine for centuries. Chemical analysis has shown the presence of more than 150 components in saffron stigmas. The more powerful components of saffron are crocin, crocetin and safranal. Studies in animal models and with cultured human malignant cell lines have demonstrated antitumor and cancer preventive activities of saffron and its main ingredients, possible mechanisms for these activities are discussed. More direct evidence of anticancer effectiveness of saffron as chemo-preventive agent may come from trials that use actual reduction of cancer incidence as the primary endpoint. This review discusses recent literature data and our results on the cancer chemopreventive activities of saffron and its main ingredients.

  9. Anticarcinogenic effect of saffron (Crocus sativus L. and its ingredients

    Directory of Open Access Journals (Sweden)

    Saeed Samarghandian

    2014-01-01

    Full Text Available Conventional and newly emerging treatment procedures such as chemotherapy, catalytic therapy, photodynamic therapy and radiotherapy have not succeeded in reversing the outcome of cancer diseases to any drastic extent, which has led researchers to investigate alternative treatment options. The extensive repertoire of traditional medicinal knowledge systems from various parts of the world are being re-investigated for their healing properties Crocus sativus L., commonly known as saffron, is the raw material for one of the most expensive spice in the world, and it has been used in folk medicine for centuries . Chemical analysis has shown the presence of more than 150 components in saffron stigmas. The more powerful components of saffron are crocin, crocetin and safranal. Studies in animal models and with cultured human malignant cell lines have demonstrated antitumor and cancer preventive activities of saffron and its main ingredients, possible mechanisms for these activities are discussed. More direct evidence of anticancer effectiveness of saffron as chemo-preventive agent may come from trials that use actual reduction of cancer incidence as the primary endpoint. This review discusses recent literature data and our results on the cancer chemopreventive activities of saffron and its main ingredients.

  10. Ingredient and labeling issues associated with allergenic foods.

    Science.gov (United States)

    Taylor, S L; Hefle, S L

    2001-01-01

    Foods contain a wide range of food ingredients that serve numerous technical functions. Per capita consumer exposure to most of these food ingredients is rather low with a few notable exceptions such as sugar and starch. Some food ingredients including edible oils, hydrolyzed proteins, lecithin, starch, lactose, flavors and gelatin may, at least in some products, be derived from sources commonly involved in IgE-mediated food allergies. These ingredients should be avoided by consumers with allergies to the source material if the ingredient contains detectable protein residues. Other food ingredients, including starch, malt, alcohol and vinegar, may be derived in some cases from wheat, rye or barley, the grains that are implicated in the causation of celiac disease. If these ingredients contain gluten residues, then they should be avoided by celiac sufferers. A few food ingredients are capable of eliciting allergic sensitization, although these ingredients would be classified as rarely allergenic. These ingredients include carmine, cochineal extract, annatto, tragacanth gum and papain. Food manufacturers should declare the presence of allergenic food ingredients in the ingredient listings on product labels so that allergic consumers can know to avoid these potentially hazardous products.

  11. Long-term safety and tolerability of open-label aripiprazole augmentation of antidepressant therapy in major depressive disorder

    Directory of Open Access Journals (Sweden)

    Berman R

    2011-05-01

    Full Text Available Robert M Berman1, Michael E Thase2, Madhukar H Trivedi3, James A Hazel4, Sabrina Vogel Marler5, Robert D McQuade6, William Carson7, Ross A Baker8, Ronald N Marcus91Neuroscience Global Clinical Research Bristol-Myers Squibb, Wallingford, CT, USA; 2Department of Psychiatry, University of Pennsylvania School of Medicine, Philadelphia, PA, USA; 3Division of Mood Disorders Research Program and Clinic, University of Texas Southwestern Medical School, Dallas, TX, USA; 4Neuroscience Global Clinical Research, Bristol-Myers Squibb, Wallingford, CT, USA; 5Global Biometric Sciences, Bristol-Myers Squibb, Wallingford, CT, USA; 6Global Medical Affairs at Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, NJ, USA; 7Global Clinical Development, Otsuka Pharmaceutical Development and Commercialization Inc, Princeton, NJ, USA; 8Neuroscience Medical Strategy, Bristol-Myers Squibb Company, Plainsboro, NJ, USA; 9Neuroscience Global Clinical Research, Bristol-Myers Squibb, Wallingford, CT, USABackground: Effective management of major depressive disorder often includes the long-term use of multiple medications, and the longer-term utility and safety of adjunctive aripiprazole has not been evaluated in a controlled setting.Patients and methods: Patients (n = 706 completing one of two 14-week double-blind studies of aripiprazole augmentation, as well as de novo patients (n = 296 nonresponsive to current antidepressant therapy, were enrolled in this open-label study. Patients received open-label aripiprazole for up to 52 weeks.Results: Open-label treatment was completed by 323 patients (32.2%. At endpoint (n = 987, the mean dose of aripiprazole was 10.1 mg/day. Common (>15% of patients spontaneously reported adverse events were akathisia (26.2%, fatigue (18.0%, and weight gain (17.1%. The incidence of serious adverse events was 4.0%. Four spontaneous reports of possible tardive dyskinesia were submitted (0.4%; all resolved within 45 days of drug

  12. Research and Compare the Antioxidant Active Ingredients of Pomegranate Vinegar,MuIberry Vinegar and BIueberry Vinegar%蓝莓醋、石榴醋、桑葚醋抗氧化活性成分的研究与比较

    Institute of Scientific and Technical Information of China (English)

    侯丽娟; 何思鲁; 赵翡; 王颉

    2016-01-01

    以市售蓝莓醋、石榴醋、桑葚醋为试验原料,对三种水果醋进行抗氧化活性成分分析和测定,研究其主要活性成分含量与清除 DPPH 自由基之间的相关性,并对其抗氧化性能进行对比。试验结果表明:三种水果醋都具有一定的抗氧化活性,其中石榴醋的抗氧化能力最强,总酚、总黄酮、抗坏血酸含量达到110.03,480.47,110 mg/kg;当加入400 mg/kg 三种水果醋时,其 DPPH 自由基清除率分别达到57.58%,63.66%,54.10%;其抗氧化活性成分与 DPPH 自由基的清除能力成正相关。水果醋具有良好的抗氧化活性,是目前较为优质的调味品,该试验为水果醋产品的进一步开发奠定了坚实的理论基础。%Take pomegranate vinegar,mulberry vinegar and blueberry vinegar as the test materials, analyze and determine the antioxidant active ingredients of the three kinds of fruit vinegar,research the correlation between the content of antioxidant active ingredients and clearing DPPH radical,and compare the antioxidation performance with one another.The results show that three kinds of fruit vinegar has a certain antioxidant activity,among them,the antioxidant capacity of pomegranate vinegar is the strongest.The content of total phenols,total flavonoids and ascorbic acid is about 110.03,480.47,110 mg/kg.When adding the three kinds of fruit vinegar with 400 mg/kg,the DPPH radical scavenging is 57.58%, 63.66%, 54.10%. It is positively correlated between antioxidant active ingredients and DPPH radical scavenging activity. Fruit vinegar has a good antioxidant activity and it is high-quality condiment.It will lay a solid theoretical foundation for the further development of fruit vinegar products.

  13. High-performance liquid chromatography-electrospray ionization-tandem mass spectrometry method for determination of active ingredients in technical zhongshengmycin%中生菌素原药有效成分高效液相色谱-串联质谱分析方法的建立

    Institute of Scientific and Technical Information of China (English)

    乔港; 魏少鹏; 姬志勤

    2012-01-01

    建立了采用高效液相色谱-串联质谱(HPLC-ESI-MS/MS)分析中生菌素(zhongshengmycins)原药中各有效成分(链丝菌素A~F)的方法.原药用去离子水超声辅助提取后经离心过滤,反相离子对高效液相色谱分离,二级质谱检测,标准样品定量离子外标法定量.结果表明:在15.63~500μg/mL质量浓度范围内,中生菌素原药各组分的仪器响应值与进样质量浓度之间呈良好的线性关系,相关系数R2>0.990 5;方法具有较好的精密度和准确度,6次重复进样,其相对标准偏差(RSD)在0.33% ~ 1.96%之间;在0.1、0.5和1μg/mg 3个添加水平下,各组分的回收率在98.2%~101.1%之间.样品实测结果表明:供试原药中链丝菌素D的含量最高,为297.65 μg/g;其次是链丝菌素B、C和F,含量分别为247.77、285.64和115.92 μg/g;链丝菌素A和E的含量较低,分别为15.63和19.60 μg/g.该方法能满足中生菌素原药中各有效成分定性及定量分析的要求.%A reliable method for determination of active ingredients in technical zhongshengmycin material was established using high-performance liquid chromatography coupled to tandem mass spectrometry (HPLC-ESI-MS/MS). The active ingredients in technique material were extracted by the ultrasound-assisted method, and then the aqueous extract was cleaned up by centrifugation and filtration. After separated by reverse-phase ion-pair chromatography, the characteristic MS/MS ions were detected by mass spectrometer and quantified with external standard method. A good linear relationship between response and concentration was obtained in the range of 15.63 -500 μg/mL,and its correlation coefficient was above 0.990 5. The relative standard derivations for different ingredients were in the range of 0. 33% - 1. 96%. The recovery rates for different ingredients were 98. 2% -101. 1% in the spiking levels of 0. 1,0. 5 and 1 μg/mg. The contents of streptothricins D,B,C,F,A and E in the tested technical

  14. Aripiprazole loaded poly(caprolactone) nanoparticles: Optimization and in vivo pharmacokinetics

    Energy Technology Data Exchange (ETDEWEB)

    Sawant, Krutika; Pandey, Abhijeet; Patel, Sneha

    2016-09-01

    In the present investigation, a Quality by Design strategy was applied for formulation and optimization of aripiprazole (APZ) loaded PCL nanoparticles (APNPs) using nanoprecipitation method keeping entrapment efficiency (%EE) and particle size (PS) as critical quality attributes. Establishment of design space was done followed by analysis of its robustness and sensitivity. Characterization of optimized APNPs was done using DSC, FT-IR, PXRD and TEM studies and was evaluated for drug release, hemocompatibility and nasal toxicity. PS, zeta potential and %EE of optimized APNPs were found to be 199.2 ± 5.65 nm, − 21.4 ± 4.6 mV and 69.2 ± 2.34% respectively. In vitro release study showed 90 ± 2.69% drug release after 8 h. Nasal toxicity study indicated safety of developed formulation for intranasal administration. APNPs administered via intranasal route facilitated the brain distribution of APZ incorporated with the AUC{sub 0→8} in rat brain approximately 2 times higher than that of APNPs administered via intravenous route. Increase in C{sub max} was observed which might help in dose reduction along with reduction in dose related side effects. The results of the study indicate that intranasally administered APZ loaded PCL NPs can potentially transport APZ via nose to brain and can serve as a non-invasive alternative for the delivery of APZ to brain. - Highlights: • It explores intra-nasal route for treatment of schizophrenia. • Quality by Design strategy has been used for optimization and assessesment of design space robustness. • PCL nanoparticles enhance penetration of drug into brain leading to increased C{sub max} and decrease in T{sub max}. • It can act as potential platform for treatment of schizophrenia with decreased dose related toxicities.

  15. Aripiprazole-montmorillonite: a new organic-inorganic nanohybrid material for biomedical applications.

    Science.gov (United States)

    Oh, Yeon-Ji; Choi, Goeun; Choy, Young Bin; Park, Je Won; Park, Jung Hyun; Lee, Hwa Jeong; Yoon, Yeo Joon; Chang, Hee Chul; Choy, Jin-Ho

    2013-04-08

    Poor aqueous solubility and the unpleasant taste of aripiprazole (APZ) have been recurring problems, owing to its low bioavailability and low patient tolerance, respectively. Herein, we prepared a nanohybrid system that was based on a bentonite clay material, montmorillonite (MMT), which could both mask the taste and enhance the solubility of APZ (i.e., APZ-MMT). To further improve the efficacy of this taste masking and drug solubility, APZ-MMT was also coated with a cationic polymer, polyvinylacetal diethylamino acetate (AEA). In vitro dissolution tests at neutral pH showed that the amount of drug that was released from the AEA-coated APZ-MMT was greatly suppressed (<1%) for the first 3 min, thus suggesting that AEA-coated APZ-MMT has strong potential for the taste masking of APZ. Notably, in simulated gastric juice at pH 1.2, the total percentage of APZ that was released within the first 2 h increased up to 95% for AEA-coated APZ-MMT. Furthermore, this in vitro release profile was also similar to that of Abilify®, a commercially available medication. In vivo experiments by using Sprague-Dawley rats were also performed to compare the pharmacokinetics of AEA-coated APZ-MMT and Abilify®. AEA-coated APZ-MMT exhibited about 20% higher systemic exposure of APZ and its metabolite, dehydro-APZ, compared with Abilify®. Therefore, a new MMT-based nanovehicle, which is coated with a cationic polymer, can act as a promising delivery system for both taste masking and for enhancing the bioavailability of APZ. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  16. Switching to aripiprazole in outpatients with schizophrenia experiencing insufficient efficacy and/or safety/tolerability issues with risperidone: a randomized, multicentre, open-label study.

    Science.gov (United States)

    Ryckmans, V; Kahn, J P; Modell, S; Werner, C; McQuade, R D; Kerselaers, W; Lissens, J; Sanchez, R

    2009-05-01

    This study evaluated the safety/tolerability and effectiveness of aripiprazole titrated-dose versus fixed-dose switching strategies from risperidone in patients with schizophrenia experiencing insufficient efficacy and/or safety/tolerability issues. Patients were randomized to an aripiprazole titrated-dose (starting dose 5 mg/day) or fixed-dose (dose 15 mg/day) switching strategy with risperidone down-tapering. Primary endpoint was rate of discontinuation due to adverse events (AEs) during the 12-week study. Secondary endpoints included positive and negative syndrome scale (PANSS), clinical global impressions - improvement of illness scale (CGI-I), preference of medication (POM), subjective well-being under neuroleptics (SWN-K) and GEOPTE (Grupo Español para la Optimización del Tratamiento de la Esquizofrenia) scales. Rates of discontinuations due to AEs were similar between titrated-dose and fixed-dose strategies (3.5% vs. 5.0%; p=0.448). Improvements in mean PANSS total scores were similar between aripiprazole titrated-dose and fixed-dose strategies (-14.8 vs. -17.2; LOCF), as were mean CGI-I scores (2.9 vs. 2.8; p=0.425; LOCF) and SWN-K scores (+8.6 vs.+10.3; OC,+7.8 vs.+9.8; LOCF). Switching can be effectively and safely achieved through a titrated-dose or fixed-dose switching strategy for aripiprazole, with down-titration of risperidone.

  17. Is aripiprazole the only choice of treatment of the patients who developed anti-psychotic agents-induced leucopenia and neutropenia? A case report.

    Science.gov (United States)

    Yalcin, Demet Ozen; Goka, Erol; Aydemir, M Cigdem; Kisa, Cebrail

    2008-05-01

    Leucopenia and neutropenia could be side effects of anti-psychotic drugs, especially clozapine. However, there is evidence that other anti-psychotics can cause leucopenia and neutropenia. We present the clinical follow-up and treatment process of a patient, who had initially developed quetiapine and amisulpride related neutropenia, but not with aripiprazole.

  18. Inventions on baker's yeast strains and specialty ingredients.

    Science.gov (United States)

    Gélinas, Pierre

    2009-06-01

    Baker's yeast is one of the oldest food microbial starters. Between 1927 and 2008, 165 inventions on more than 337 baker's yeast strains were patented. The first generation of patented yeast strains claimed improved biomass yield at the yeast plant, higher gassing power in dough or better survival to drying to prepare active dry baker's yeast. Especially between 1980 and 1995, a major interest was given to strains for multiple bakery applications such as dough with variable sugar content and stored at refrigeration (cold) or freezing temperatures. During the same period, genetically engineered yeast strains became very popular but did not find applications in the baking industry. Since year 2000, patented baker's yeast strains claimed aroma, anti-moulding or nutritive properties to better meet the needs of the baking industry. In addition to patents on yeast strains, 47 patents were issued on baker's yeast specialty ingredients for niche markets. This review shows that patents on baker's yeast with improved characteristics such as aromatic or nutritive properties have regularly been issued since the 1920's. Overall, it also confirms recent interest for a very wide range of tailored-made yeast-based ingredients for bakery applications.

  19. Adjunctive aripiprazole in the treatment of risperidone-induced hyperprolactinemia: A randomized, double-blind, placebo-controlled, dose-response study.

    Science.gov (United States)

    Chen, Jing-Xu; Su, Yun-Ai; Bian, Qing-Tao; Wei, Li-He; Zhang, Rong-Zhen; Liu, Yan-Hong; Correll, Christoph; Soares, Jair C; Yang, Fu-De; Wang, Shao-Li; Zhang, Xiang-Yang

    2015-08-01

    Hyperprolactinemia is an unwanted adverse effect associated with several antipsychotics. The addition of partial dopamine receptor agonist aripiprazole may attenuate antipsychotic-induced hyperprolactinemia effectively. However, the ideal dosing regimen for this purpose is unknown. We aimed to evaluate the dose effects of adjunctive treatment with aripiprazole on prolactin levels and hyperprolactinemia in schizophrenia patients. Stable subjects 18-45 years old with schizophrenia and hyperprolactinemia (i.e., >24 ng/ml for females and >20 ng/ml for males) were randomly assigned to receive 8 weeks of placebo (n=30) or oral aripiprazole 5mg/day (n=30), 10mg/day (n=29), or 20mg/day (n=30) added on to fixed dose risperidone treatment. Serum prolactin levels were measured at baseline and after 2, 4 and 8 weeks; clinical symptoms and side effects were assessed at baseline and week 8 using the Positive and Negative Syndrome Scale, Clinical Global Impressions Severity scale, Barnes Akathisia Scale, Simpson-Angus Scale and UKU Side Effects Rating Scale. Of 119 randomized patients, 107 (89.9%) completed the 8-week study. At study end, all three aripiprazole doses resulted in significantly lower prolactin levels (beginning at week 2), higher response rates (≥30% prolactin reduction) and higher prolactin normalization rates than placebo. Effects were significantly greater in the 10 and 20mg/day groups than the 5mg/day group. No significant changes were observed in any treatment groups regarding psychopathology and adverse effect ratings. Adjunctive aripiprazole treatment was effective and safe for resolving risperidone-induced hyperprolactinemia, producing significant and almost maximal improvements by week 2 without significant effects on psychopathology and side effects.

  20. A skin sensitization risk assessment approach for evaluation of new ingredients and products.

    Science.gov (United States)

    Gerberick, G F; Robinson, M K

    2000-06-01

    Skin sensitization risk assessment of new ingredients or products is critical before their introduction into the marketplace. The risk assessment process described in this article involves evaluation of skin sensitization hazard, consideration of all potential human exposures, comparative ingredient/product benchmarking, and, when appropriate, the management of the risk. In this article, a risk assessment process is reviewed along with a description of the risk assessment tools that are employed for evaluating a new ingredient or product. The basic process we use for evaluating the skin sensitization risk of a new product or ingredient is considered a no effect/safety factor approach. The tools used for conducting a risk assessment include structure activity relationship analysis, exposure assessment, preclinical testing (e.g., local lymph node assay [LNNA]) and clinical testing (e.g., human repeat insult patch testing [HRIPT]). The skin sensitization risk assessment process described in this paper has been used successfully for many years for the safe introduction of new products into the marketplace. This process is dynamic--it can be applied to a diversity of product categories (e.g., shampoo, transdermal drug). In summary, the skin sensitization risk assessment process described in this article allows one to carefully assess the skin sensitization potential of a new ingredient or product so that it can be safely introduced into the marketplace.

  1. 瑞香狼毒活性成分对东亚飞蝗的生物活性和病理学研究%Bioactivity and histopathology study of the active ingredients from Stellera chamaej asme L .against Locusta migratoria manilensis(Meyen)

    Institute of Scientific and Technical Information of China (English)

    高嫚潞; 吴朗; 陈龙; 周卫; 陶科; 侯太平

    2013-01-01

    The activity of ligarine extracts from Stellera chamaej asme L .against Locusta migratoria manilensis(Meyen) was tested and compared by bioassay methods . The biological activity and histopathological effects of the active ingredients from Stellera chamaej asme L .on Locusta migratoria manilensis(Meyen) and mid-gut cells were determined .The results showed that the active ingredients from Stellera chamaej asme L .had anti-feeding activity ,contacting activity ,stomach toxicity activity and inhibition of growth and development on Locusta migratoria manilensis(Meyen) .The AFC50of complete anti-feeding activity were 317 .63mg/L ,113 .20mg/L in 24 hour and 48 hour ;The LC50 of contacting activity were 548 .21 mg/L and the LC50 of stomach toxicity activity were 2486 .19 mg/L in 96 hour for ligarine extracts from Stellera chamaej asme L .,active ingredients also had strong effect on growth and development of Locusta migratoria manilensis(Meyen) .The EC50of growth inhibition rate was 39 .75 mg/L in 48 hour . The histopathology studies on mid-gut from Locusta migratoria manilensis(Meyen) showed that the ligarine extracts from Stellera chamaej asme L .damage the normal structure of mid-gut and lead to columnar epithelial cells fell off and death .%采用活体生物试验方法进行活性跟踪,选取瑞香狼毒对东亚飞蝗毒杀活性最高的石油醚萃取部分,测定瑞香狼毒活性成分对东亚飞蝗的生物活性及其中肠消化道的组织病理学影响.结果表明:瑞香狼毒活性成分对东亚飞蝗具有拒食、触杀、胃毒活性及生长发育抑制作用,其中拒食活性最为显著,24 h、48 h拒食中浓度(A FC50)分别为317.63、113.20 mg/L ;96 h触杀致死中浓度(LC50)、胃毒致死中浓度(LC50)分别为548.21 mg/L、2486.19 mg/L ;生长发育抑制作用也十分明显,48 h生长发育抑制中浓度(EC50)为39.75 mg/L .东亚飞蝗中肠组织病理学变化研究结果表明,

  2. Probiotics - the versatile functional food ingredients.

    Science.gov (United States)

    Syngai, Gareth Gordon; Gopi, Ragupathi; Bharali, Rupjyoti; Dey, Sudip; Lakshmanan, G M Alagu; Ahmed, Giasuddin

    2016-02-01

    Probiotics are live microbes which when administered in adequate amounts as functional food ingredients confer a health benefit on the host. Their versatility is in terms of their usage which ranges from the humans to the ruminants, pigs and poultry, and also in aquaculture practices. In this review, the microorganisms frequently used as probiotics in human and animal welfare has been described, and also highlighted are the necessary criteria required to be fulfilled for their use in humans on the one hand and on the other as microbial feed additives in animal husbandry. Further elaborated in this article are the sources from where probiotics can be derived, the possible mechanisms by which they act, and their future potential role as antioxidants is also discussed.

  3. The effect of antipsychotic medication on sexual function and serum prolactin levels in community-treated schizophrenic patients: results from the Schizophrenia Trial of Aripiprazole (STAR study (NCT00237913

    Directory of Open Access Journals (Sweden)

    Pans Miranda

    2008-12-01

    Full Text Available Abstract Background The aim of this paper is to evaluate the effect of antipsychotics for the treatment of schizophrenia in a community based study on sexual function and prolactin levels comparing the use of aripiprazole and standard of care (SOC, which was a limited choice of three widely used and available antipsychotics (olanzapine, quetiapine or risperidone (The Schizophrenia Trial of Aripiprazole [STAR] study [NCT00237913]. Method This open-label, 26-week, multi-centre, randomised study compared aripiprazole to SOC (olanzapine, quetiapine or risperidone in patients with schizophrenia (DSM-IV-TR criteria. The primary effectiveness variable was the mean total score of the Investigator Assessment Questionnaire (IAQ at Week 26. The outcome research variables included the Arizona Sexual Experience scale (ASEX. This along with the data collected on serum prolactin levels at week 4, 8, 12, 18 and 26 will be the focus of this paper. Results A total of 555 patients were randomised to receive aripiprazole (n = 284 or SOC (n = 271. Both treatment groups experienced improvements in sexual function from baseline ASEX assessments. However at 8 weeks the aripiprazole treatment group reported significantly greater improvement compared with the SOC group (p = 0.007; OC. Although baseline mean serum prolactin levels were similar in the two treatment groups (43.4 mg/dL in the aripiprazole group and 42.3 mg/dL in the SOC group, p = NS at Week 26 OC, mean decreases in serum prolactin were 34.2 mg/dL in the aripiprazole group, compared with 13.3 mg/dL in the SOC group (p Conclusion The study findings suggest that aripiprazole has the potential to reduce sexual dysfunction, which in turn might improve patient compliance.

  4. Analysis of ingredient and heating value of municipal solid waste

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Great differences between municipal solid wastes(MSW) produced at different places and different times in terms of such parameters as physical ingredient and heating value lead to difficulty in effective handling of MSW. In this paper, ingredient,heating value and their temporal varying trends of typical MSW in Beijing were continuously measured and analyzed. With consideration of the process in pyrolysis and incineration, correlation between physical ingredients and heating values was induced, favorable for evaluation of heating value needed in handling of MSW from simple analysis of physical ingredients of it.

  5. Effective sunscreen ingredients and cutaneous irritation in patients with rosacea.

    Science.gov (United States)

    Nichols, K; Desai, N; Lebwohl, M G

    1998-06-01

    Patients with rosacea are particularly susceptible to the irritation caused by sunscreen ingredients. The purpose of this bilateral comparison study was to examine the effects of different ingredients found in sunscreen on facial cutaneous irritancy in patients with rosacea. patients clinically diagnosed with rosacea were asked to test different preparations of common sunscreens on their faces. The results show that the presence or absence of appropriate protective ingredients, such as dimethicone and cyclomethicone in the vehicle, may prevent irritation from other sunscreen ingredients in patients with inflammatory conditions such as rosacea.

  6. The antipsychotics clozapine and olanzapine increase plasma glucose and corticosterone levels in rats: comparison with aripiprazole, ziprasidone, bifeprunox and F15063.

    Science.gov (United States)

    Assié, Marie-Bernadette; Carilla-Durand, Elisabeth; Bardin, Laurent; Maraval, Mireille; Aliaga, Monique; Malfètes, Nathalie; Barbara, Michèle; Newman-Tancredi, Adrian

    2008-09-11

    Several novel antipsychotics activate serotonin 5-HT1A receptors as well as antagonising dopamine D2/3 receptors. Such a pharmacological profile is associated with a lowered liability to produce extrapyramidal side effects and enhanced efficacy in treating negative and cognitive symptoms of schizophrenia. However, 5-HT1A receptor agonists increase plasma corticosterone and many antipsychotics disturb the regulation of glucose. Here, we compared the influence on plasma glucose and corticosterone of acute treatments with 'new generation' antipsychotics which target dopamine D2/3 receptors and 5-HT1A receptors, with that of atypical antipsychotics, and with haloperidol. Olanzapine and clozapine, antipsychotics that are known to produce weight gain and diabetes in humans, both at 10 mg/kg p.o., substantially increased plasma glucose (from 0.8 to 1.7 g/l) at 1 h after administration, an effect that returned to control levels after 4 h. In comparison, F15063 (40 mg/kg p.o.) was without effect at any time point. Olanzapine and clozapine dose-dependently increased plasma glucose concentrations as did SLV313 and SSR181507. Haloperidol and risperidone had modest effects whereas aripiprazole, ziprasidone and bifeprunox, antipsychotics that are not associated with metabolic dysfunction in humans, and F15063 had little or no influence on plasma glucose. The same general pattern of response was found for plasma corticosterone levels. The present data provide the first comparative study of conventional, atypical and 'new generation' antipsychotics on glucose and corticosterone levels in rats. A variety of mechanisms likely underlie the hyperglycemia and corticosterone release observed with clozapine and olanzapine, whilst the balance of dopamine D2/3/5-HT1A interaction may contribute to the less favourable impact of SLV313 and SSR181507 compared with that of bifeprunox and F15063.

  7. A Double-Blind and Placebo-Controlled Trial of Aripiprazole in Symptomatic Youths at Genetic High Risk for Bipolar Disorder.

    Science.gov (United States)

    Findling, Robert L; Youngstrom, Eric A; Rowles, Brieana M; Deyling, Elizabeth; Lingler, Jacqui; Stansbrey, Robert J; McVoy, Molly; Lytle, Sarah; Calabrese, Joseph R; McNamara, Nora K

    2017-07-31

    To determine if acute treatment with aripiprazole (APZ) would be superior to treatment with placebo in reducing dysfunctional symptoms of elevated mood and/or irritability in symptomatic children and adolescents at familial high risk for bipolar disorder (BPD) whose mood episodes occur spontaneously. These are patients we have previously referred to as suffering from "cyclotaxia." This was single-site, randomized, double-blind, placebo-controlled outpatient clinical trial in which youths aged 5-17 years who met diagnostic criteria for either cyclothymic disorder (CYC) or BPD not otherwise specified (BP-NOS) were randomly assigned to receive either APZ or placebo. Eligible participants had at least one parent with BPD, another first- or second-degree relative afflicted with a mood disorder, and also had not responded to psychotherapy. Treatment with APZ was initiated at a dose of approximately 0.1 mg/kg/day and could be increased by approximately 0.05 mg/kg/day at each study visit. Patients were seen weekly for 4 weeks and then every other week thereafter for 12 weeks. The primary outcome measure was mean change from baseline on Young Mania Rating Scale (YMRS) total score. A total of 59 patients (30 APZ, 29 placebo) aged 11.8 (SD = 2.7) years were randomized and returned for at least one postbaseline assessment. The mean total daily doses of active APZ and placebo were 7.1 mg (SD = 3.7) and 7.4 mg (SD = 4.2), respectively. At the 12-week time point, APZ was superior to placebo on the primary outcome measure (p children and adolescents with cyclotaxia.

  8. Final report of the Cosmetic Ingredient Review Expert Panel amended safety assessment of Calendula officinalis-derived cosmetic ingredients.

    Science.gov (United States)

    Andersen, F Alan; Bergfeld, Wilma F; Belsito, Donald V; Hill, Ronald A; Klaassen, Curtis D; Liebler, Daniel C; Marks, James G; Shank, Ronald C; Slaga, Thomas J; Snyder, Paul W

    2010-01-01

    Calendula officinalis extract, C officinalis flower, C officinalis flower extract, C officinalis flower oil, and C officinalis seed oil are cosmetic ingredients derived from C officinalis. These ingredients may contain minerals, carbohydrates, lipids, phenolic acids, flavonoids, tannins, coumarins, sterols and steroids, monoterpenes, sesquiterpenes, triterpenes, tocopherols, quinones, amino acids, and resins. These ingredients were not significantly toxic in single-dose oral studies using animals. The absence of reproductive/developmental toxicity was inferred from repeat-dose studies of coriander oil, with a similar composition. Overall, these ingredients were not genotoxic. They also were not irritating, sensitizing, or photosensitizing in animal or clinical tests but may be mild ocular irritants. The Cosmetic Ingredient Review (CIR) Expert Panel concluded that these ingredients are safe for use in cosmetics in the practices of use and concentration given in this amended safety assessment.

  9. Beneficial in vivo effect of aripiprazole on neuronal regeneration following neuronal loss in the dentate gyrus: evaluation using a mouse model of trimethyltin-induced neuronal loss/self-repair in the dentate gyrus.

    Science.gov (United States)

    Yoneyama, Masanori; Hasebe, Shigeru; Kawamoto, Noriko; Shiba, Tatsuo; Yamaguchi, Taro; Kikuta, Maho; Shuto, Makoto; Ogita, Kiyokazu

    2014-01-01

    Aripiprazole is used clinically as an atypical antipsychotic. We evaluated the effect of in vivo treatment with aripiprazole on the proliferation and differentiation of neural stem/progenitor cells in a mouse model, trimethyltin-induced neuronal loss/self-repair in the hippocampal dentate gyrus (referred as "impaired animals") [Ogita et al., J Neurosci Res. 82, 609 - 621 (2005)]. In the impaired animals, an increased number of 5-bromo-2'-deoxyuridine (BrdU)-positive cells was seen in the dentate gyrus at the initial time window of the self-repair stage. At the same time window, a single treatment with aripiprazole significantly increased the number of cells positive for both BrdU and nestin in the dentate gyrus of the impaired animals. Chronic treatment with aripiprazole promoted the proliferation/survival and neuronal differentiation of the cells newly-generated following the neuronal loss in the dentate gyrus of the impaired animals. The chronic treatment with aripiprazole improved depression-like behavior seen in the impaired animals. Taken together, our data suggest that aripiprazole had a beneficial effect on neuronal regeneration following neuronal loss in the dentate gyrus through indirectly promoted proliferation/survival and neuronal differentiation of neural stem/progenitor cells in the subgranular zone of the dentate gyrus.

  10. 核桃根、茎、叶提取物对蚕豆的遗传毒性分析%Genetic toxicity of active ingredients extracted from roots,stems, and leaves of walnut on Vicia faba

    Institute of Scientific and Technical Information of China (English)

    黄元河; 潘乔丹

    2012-01-01

    [目的]研究核桃根、茎、叶不同提取物的化感作用机制,为开发新型无公害植物源除草剂提供科学依据.[方法]采用蚕豆根生长试验和蚕豆微核试验,测定核桃根、茎、叶不同提取物对蚕豆生长的影响和遗传毒性.[结果]经核桃根、叶正丁醇提取物培养24和48h的蚕豆根生长减慢,当核桃根、叶正丁醇提取物浓度大于0.050 g/mL时,培养72 h的蚕豆根生长停滞.微核试验结果,核桃根、叶正丁醇提取物能抑制蚕豆根尖细胞生长,损伤其遗传物质,导致其有丝分裂指数下降、微核率增高,与对照相比呈显著性差异(P<0.05),且在试验浓度范围内(0.025~0.100 g/mL)表现出显著的浓度效应和时间效应.[结论]核桃根和叶中含有一定遗传毒性的化感物质,能够抑制植物细胞分裂,导致细胞遗传物质损伤,对周围植物产生不可逆的遗传损伤效应.%In order to provide scientific evidences for the development of pollution-free botanical herbicides, this study explored the allelopathic mechanism of different extracts from the roots, stems, and leaves of walnut (Juglans regia L.). [ Method jThe Vicia (aba root growth test and micronucleus test were used to study the effects of the different ingredients derived from the roots, stems, and leaves of walnut on Vicia faba growth and their genetic toxicity. [ResultJThe research results showed that the Vicia faba root grew slowly after being cultured by the n-butanol extracts (0.025, 0.050, 0.100 g/mL) from walnut roots and leaves for 24 and 48 hrs, respectively. When the extracts concentration was greater than 0.050 g/mL, the Vicia faba root, which was cultured for 72 hrs, stopped growing. The micronuclear test indicated that the n-butanol extracts of roots and leaves could inhibit the growth of Vicia faba root tip cells and damage the genetic material, which resulted in the mitotic index of Vicia faba root tips to decrease and micronuclear rate to

  11. Efficacy and tolerability of aripiprazole once monthly for schizophrenia: a systematic review and meta-analysis of randomized controlled trials

    Directory of Open Access Journals (Sweden)

    Oya K

    2015-09-01

    Full Text Available Kazuto Oya, Taro Kishi, Nakao Iwata Department of Psychiatry, Fujita Health University School of Medicine, Toyoake, Aichi, Japan Objective: We conducted a systematic review and meta-analysis of the efficacy of aripiprazole once monthly (AOM for schizophrenia.Methods: Randomized controlled trials (RCTs on AOM, published until June 25, 2015, were retrieved from PubMed, Cochrane, and PsycINFO databases. Relative risk (RR, standardized mean difference (SMD, 95% confidence intervals (95% CIs, and numbers needed to treat/harm (NNT/NNH were calculated.Results: We identified four relevant RCTs (total n=1,860, two placebo-controlled trials, one noninferiority trial comparing AOM to oral aripiprazole (OA, and one including therapeutic doses of AOM and OA, as well as an AOM dose below therapeutic threshold (control arm. AOM was superior to placebo for decreasing Positive and Negative Syndrome Scale (PANSS total scores (SMD =-0.65, 95% CI =-0.90 to -0.41, n=1,126. However, PANSS total scores did not differ significantly between pooled AOM and OA groups. The pooled AOM group showed significantly lower incidence of all-cause discontinuation (RR =0.54, 95% CI =0.41–0.71, n=1,139, NNH =4 and inefficacy (RR =0.28, 95% CI =0.21–0.38, n=1,139, NNH =5 than placebo, but was not superior to placebo regarding discontinuation due to adverse events (AEs or death. The AOM group exhibited a lower incidence of all-cause discontinuation than OA (RR =0.78, 95% CI =0.64–0.95, n=986, NNH =14, but there were no intergroup differences in discontinuation due to inefficacy, AEs, or death. There were no significant differences in extrapyramidal symptoms scale scores between AOM and placebo or between AOM and OA. AOM resulted in higher weight gain than placebo (SMD =0.41, 95% CI =0.18–0.64, n=734 but lower than OA (SMD =-0.16, 95% CI =-0.29 to -0.02, n=847.Conclusion: AOM has antipsychotic efficacy and low risk of discontinuation due to AEs. Keywords: schizophrenia

  12. A 64-week, multicenter, open-label study of aripiprazole effectiveness in the management of patients with schizophrenia or schizoaffective disorder in a general psychiatric outpatient setting

    Directory of Open Access Journals (Sweden)

    Chiu Nan-Ying

    2010-09-01

    Full Text Available Abstract Objective To evaluate the overall long-term effectiveness of aripiprazole in patients with schizophrenia in a general psychiatric practice setting in Taiwan. Methods This was a prospective, open-label, multicenter, post-market surveillance study in Taiwanese patients with a Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition (DSM-IV diagnosis of schizophrenia or schizoaffective disorder requiring a switch in antipsychotic medication because current medication was not well tolerated and/or clinical symptoms were not well controlled. Eligible patients were titrated to aripiprazole (5-30 mg/day over a 12-week switching phase, during which their previous medication was discontinued. Patients could then enter a 52-week, long-term treatment phase. Aripiprazole was flexibly dosed (5-30 mg/day at the discretion of the treating physicians. Efficacy was assessed using the Clinical Global Impression scale Improvement (CGI-I score, the Clinical Global Impression scale Severity (CGI-S score, The Brief Psychiatry Rating Scale (BPRS, and the Quality of Life (QOL scale, as well as Preference of Medicine (POM ratings by patients and caregivers. Safety and tolerability were also assessed. Results A total of 245 patients were enrolled and switched from their prior antipsychotic medications, and 153 patients entered the 52-week extension phase. In all, 79 patients (32.2% completed the study. At week 64, the mean CGI-I score was 3.10 and 64.6% of patients who showed response. Compared to baseline, scores of CGI-S, QOL, and BPRS after 64 weeks of treatment also showed significant improvements. At week 12, 65.4% of subjects and 58.9% of caregivers rated aripiprazole as better than the prestudy medication on the POM. The most frequently reported adverse events (AEs were headache, auditory hallucinations and insomnia. A total of 13 patients (5.3% discontinued treatment due to AEs. No statistically significant changes were noted with respect to

  13. How Much Do We Really Know About Our Favorite Cosmeceutical Ingredients?

    Science.gov (United States)

    Levin, Jacquelyn; Momin, Saira B.

    2010-01-01

    To date, we are unaware of a review that has investigated common cosmeceutical ingredients in order to answer the three specif