ISRN Pharmaceutics最新文献_第4页

Effect of chemical enhancers in transdermal permeation of alfuzosin hydrochloride. 化学促进剂对盐酸阿夫唑嗪透皮的影响

ISRN Pharmaceutics Pub Date : 2012-01-01 Epub Date: 2012-12-20 DOI: 10.5402/2012/965280

D Prasanthi, P K Lakshmi

{"title":"Effect of chemical enhancers in transdermal permeation of alfuzosin hydrochloride.","authors":"D Prasanthi, P K Lakshmi","doi":"10.5402/2012/965280","DOIUrl":"10.5402/2012/965280","url":null,"abstract":"The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q(24)) of 702.28 ± 6.97 μg/cm(2) and 702.74 ± 7.49 μg/cm(2), respectively. A flux rate of 31.08 ± 0.21 μg/cm(2)/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm(2)/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"965280"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3539352/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9744716","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Application of Sephadex LH-20 for Microdetermination of Dopamine by Solid Phase Spectrophotometry. Sephadex LH-20固相分光光度法测定微量多巴胺的应用

ISRN Pharmaceutics Pub Date : 2012-01-01 Epub Date: 2012-11-28 DOI: 10.5402/2012/216068

Mehdi Taghdiri, Arash Mohamadipour-Taziyan

引用次数: 6

Pharmacokinetic-pharmacodynamic model of newly developed dexibuprofen sustained release formulations. 新研制的地布洛芬缓释制剂的药动学-药效学模型。

ISRN Pharmaceutics Pub Date : 2012-01-01 Epub Date: 2012-12-06 DOI: 10.5402/2012/451481

Selvadurai Muralidharan

{"title":"Pharmacokinetic-pharmacodynamic model of newly developed dexibuprofen sustained release formulations.","authors":"Selvadurai Muralidharan","doi":"10.5402/2012/451481","DOIUrl":"https://doi.org/10.5402/2012/451481","url":null,"abstract":"Pharmacokinetic-pharmacodynamic (PK-PD) modeling has emerged as a major tool in clinical pharmacology to optimize drug use by designing rational dosage forms and dosage regimes. Quantitative representation of the dose-concentration-response relationship should provide information for the prediction of the level of response to a certain level of drug dose. This paper describes the experimental details of the preformulation study, tablet manufacture, optimization, and bioanalytical methods for the estimation of dexibuprofen in human plasma. The hydrophilic matrix was prepared with xanthen gum with additives Avicel PH 102. The effect of the concentration of the polymer and different filler, on the in vitro drug release, was studied. Various pharmacokinetic parameters including AUC(0-t), AUC(0-∞), C(max), T(max), T(1/2), and elimination rate constant (K(el)) were determined from the plasma concentration of both formulations of test (dexibuprofen 300 mg) and reference (dexibuprofen 300 mg tablets). The merits of PK-PD in the development of dosage forms and how PK-PD model development necessitates the development of new drugs and bio analytical method development and validation are discussed. The objectives of the present study, namely, to develop and validate the methods to estimate the selected drugs in the biological fluids by HPLC, the development of in vitro dissolution methods, and PK-PD model development have been described.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":" ","pages":"451481"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/451481","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31158877","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Osmotic drug delivery system as a part of modified release dosage form. 渗透给药系统作为修饰释放剂型的一部分。

ISRN Pharmaceutics Pub Date : 2012-01-01 Epub Date: 2012-07-17 DOI: 10.5402/2012/528079

Rajesh A Keraliya, Chirag Patel, Pranav Patel, Vipul Keraliya, Tejal G Soni, Rajnikant C Patel, M M Patel

{"title":"Osmotic drug delivery system as a part of modified release dosage form.","authors":"Rajesh A Keraliya, Chirag Patel, Pranav Patel, Vipul Keraliya, Tejal G Soni, Rajnikant C Patel, M M Patel","doi":"10.5402/2012/528079","DOIUrl":"https://doi.org/10.5402/2012/528079","url":null,"abstract":"Conventional drug delivery systems are known to provide an immediate release of drug, in which one can not control the release of the drug and can not maintain effective concentration at the target site for longer time. Controlled drug delivery systems offer spatial control over the drug release. Osmotic pumps are most promising systems for controlled drug delivery. These systems are used for both oral administration and implantation. Osmotic pumps consist of an inner core containing drug and osmogens, coated with a semipermeable membrane. As the core absorbs water, it expands in volume, which pushes the drug solution out through the delivery ports. Osmotic pumps release drug at a rate that is independent of the pH and hydrodynamics of the dissolution medium. The historical development of osmotic systems includes development of the Rose-Nelson pump, the Higuchi-Leeper pumps, the Alzet and Osmet systems, the elementary osmotic pump, and the push-pull system. Recent advances include development of the controlled porosity osmotic pump, and systems based on asymmetric membranes. This paper highlights the principle of osmosis, materials used for fabrication of pumps, types of pumps, advantages, disadvantages, and marketed products of this system.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":" ","pages":"528079"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/528079","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30803458","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 110

Fabrication and development of pectin microsphere of metformin hydrochloride. 盐酸二甲双胍果胶微球的制备与开发。

ISRN Pharmaceutics Pub Date : 2012-01-01 Epub Date: 2012-08-01 DOI: 10.5402/2012/230621

Pritam Banerjee, Jyotirmoy Deb, Amitava Roy, Amitava Ghosh, Prithviraj Chakraborty

{"title":"Fabrication and development of pectin microsphere of metformin hydrochloride.","authors":"Pritam Banerjee, Jyotirmoy Deb, Amitava Roy, Amitava Ghosh, Prithviraj Chakraborty","doi":"10.5402/2012/230621","DOIUrl":"https://doi.org/10.5402/2012/230621","url":null,"abstract":"Purpose. The objective of the proposed work is to evaluate the efficacy of Pectins to qualify them as polymers for designing an oral microsphere for the delivery of selected oral antidiabetic drug-like metformin hydrochloride. Methods. Different Microspheres formulations were prepared by the water in oil (wo) emulsion solvent evaporation technique and subsequently evaluated for its different physical parameters as well as its in vitro and in vivo drug release study. Results. The formulations F2 (98.42) and F3 (98.03) showed a constant and high release in the dissolution profile, so among these two formulations, F2 was taken for development study, due to the better result shown over in other evaluation parameters. From the HPLC determinations after in vivo study, it had been found that the test samples and the standard sample had not shown any significant fluctuation in relation to their retention time. Conclusion. From in vitro and in vivo results, it may be concluded that drug-loaded pectin microspheres in 1 : 1 ratio are a suitable delivery system for metformin hydrochloride and may be used for effective management of NIDDM. From this experiment, it could be concluded that as a natural polymer, pectin has potentiality in novel drug delivery system.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":" ","pages":"230621"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/230621","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30840627","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 28

Development and stability studies of novel liposomal vancomycin formulations. 万古霉素新型脂质体制剂的研制及稳定性研究。

ISRN Pharmaceutics Pub Date : 2012-01-01 DOI: 10.5402/2012/636743

Krishna Muppidi, Andrew S Pumerantz, Jeffrey Wang, Guru Betageri

{"title":"Development and stability studies of novel liposomal vancomycin formulations.","authors":"Krishna Muppidi, Andrew S Pumerantz, Jeffrey Wang, Guru Betageri","doi":"10.5402/2012/636743","DOIUrl":"https://doi.org/10.5402/2012/636743","url":null,"abstract":"A promising strategy to improve the therapeutic efficiency of antimicrobial agents is targeted therapy. Although vancomycin has been considered a gold standard for the therapy of MRSA pneumonia, clinical failure rates have also been reported owing to its slow, time-dependent bactericidal activity, variable lung tissue penetration and poor intracellular penetration into macrophages. Liposomal encapsulation has been established as an alternative for antimicrobial delivery to infected tissue macrophages and offers enhanced pharmacodynamics, pharmacokinetics and decreased toxicity compared to standard preparations. The aim of the present work is to prepare vancomycin in two different liposomal formulations, conventional and PEGylated liposomes using different methods. The prepared formulations were optimized for their particle size, encapsulation efficiency and physical stability. The dehydration-rehydration was found to be the best preparation method. Both the conventional and PEGylated liposomal formulations were successfully formulated with a narrow particle size and size distribution and % encapsulation efficiency of 9 ± 2 and 12 ± 3, respectively. Both the formulations were stable at 4°C for 3 months. These formulations were successfully used to evaluate for their intracellular killing of MRSA and in vivo pharmacokinetic and bio-distribution studies.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"636743"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/636743","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374938","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 72

Degradation Pathway for Eplerenone by Validated Stability Indicating UP-LC Method. 稳定性指示UP-LC法对埃普利酮的降解途径。

ISRN Pharmaceutics Pub Date : 2012-01-01 DOI: 10.5402/2012/251247

Kondru Sudhakar Babu, Venkataramanna Madireddy, Venkata Somaraju Indukuri

{"title":"Degradation Pathway for Eplerenone by Validated Stability Indicating UP-LC Method.","authors":"Kondru Sudhakar Babu, Venkataramanna Madireddy, Venkata Somaraju Indukuri","doi":"10.5402/2012/251247","DOIUrl":"https://doi.org/10.5402/2012/251247","url":null,"abstract":"Degradation pathway for eplerenone is established as per ICH recommendations by validated and stability-indicating reverse phase liquid chromatographic method. Eplerenone is subjected to stress conditions of acid, base, oxidation, and thermal and photolysis. Significant degradation is observed in acid and base stress conditions. Four impurities are studied and the major degradant (RRT about 0.31) was identified by LC-MS and spectral analysis. The stress samples are assayed against a qualified reference standard and the mass balance is found close to 99.5%. Efficient chromatographic separation is achieved on a Waters symmetry C18 stationary phase with simple mobile phase combination delivered in gradient mode and quantification is carried at 240 nm at a flow rate of 1.0 mL min(-1). In the developed LC method the resolution between eplerenone and four potential impurities (imp-1, imp-2, imp-3, and imp-4) is found to be greater than 4.0. Regression analysis shows an r value (correlation coefficient) of greater than 0.999 for eplerenone and four potential impurities. This method is capable to detect the impurities of eplerenone at a level of 0.020% with respect to test concentration of 1.0 mg mL(-1) for a 20 μL injection volume. The developed UPLC method is validated with respect to specificity, linearity and range, accuracy, precision, and robustness for impurities and assay determination.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"251247"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/251247","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9376737","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Review of Pharmacological Properties and Chemical Constituents of Pimpinella anisum. 香芹的药理性质及化学成分研究进展。

ISRN Pharmaceutics Pub Date : 2012-01-01 DOI: 10.5402/2012/510795

Asie Shojaii, Mehri Abdollahi Fard

{"title":"Review of Pharmacological Properties and Chemical Constituents of Pimpinella anisum.","authors":"Asie Shojaii, Mehri Abdollahi Fard","doi":"10.5402/2012/510795","DOIUrl":"https://doi.org/10.5402/2012/510795","url":null,"abstract":"Pimpinella anisum (anise), belonging to Umbelliferae family, is an aromatic plant which has been used In Iranian traditional medicine (especially its fruits) as carminative, aromatic, disinfectant, and galactagogue. Because the wide traditional usage of Pimpinella anisum for treatment of diseases, in this review published scientific reports about the composition and pharmacological properties of this plant were collected with electronic literature search of GoogleScholar, PubMed, Sciencedirect, Scopus, and SID from 1970 to 2011. So far, different studies were performed on aniseeds and various properties such as antimicrobial, antifungal, antiviral, antioxidant, muscle relaxant, analgesic and anticonvulsant activity as well as different effects on gastrointestinal system have been reported of aniseeds. It can also reduce morphine dependence and has beneficial effects on dysmenorrhea and menopausal hot flashes in women. In diabetic patients, aniseeds showed hypoglycemic and hypolipidemic effect and reduce lipid peroxidation. The most important compounds of aniseeds essential oil were trans-anetole, estragole, γ-hymachalen, para-anisaldehyde and methyl cavicol. Due to broad spectrum of pharmacological effects, and very few clinical studies of Pimpinella anisum, more clinical trials are recommended to evaluate the beneficial effects of this plant in human models and synthesis of new drugs from the active ingredients of this plant in future.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"510795"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/510795","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9728916","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 203

Chemical Composition, Antifungal and Antibiofilm Activities of the Essential Oil of Mentha piperita L. 薄荷精油的化学成分、抑菌活性及抗菌活性研究。

ISRN Pharmaceutics Pub Date : 2012-01-01 DOI: 10.5402/2012/718645

Mohammad Jamal Saharkhiz, Marjan Motamedi, Kamiar Zomorodian, Keyvan Pakshir, Ramin Miri, Kimia Hemyari

{"title":"Chemical Composition, Antifungal and Antibiofilm Activities of the Essential Oil of Mentha piperita L.","authors":"Mohammad Jamal Saharkhiz, Marjan Motamedi, Kamiar Zomorodian, Keyvan Pakshir, Ramin Miri, Kimia Hemyari","doi":"10.5402/2012/718645","DOIUrl":"https://doi.org/10.5402/2012/718645","url":null,"abstract":"Variations in quantity and quality of essential oil (EO) from the aerial parts of cultivated Mentha piperita were determined. The EO of air-dried sample was obtained by a hydrodistillation method and analyzed by a gas chromatography/mass spectrometry (GC/MS). The antifungal activity of the EO was investigated by broth microdilution methods as recommended by Clinical and Laboratory Standards Institute. A biofilm formation inhibition was measured by using an XTT reduction assay. Menthol (53.28%) was the major compound of the EO followed by Menthyl acetate (15.1%) and Menthofuran (11.18%). The EO exhibited strong antifungal activities against the examined fungi at concentrations ranging from 0.12 to 8.0 μL/mL. In addition, the EO inhibited the biofilm formation of Candida albicans and C. dubliniensis at concentrations up to 2 μL/mL. Considering the wide range of the antifungal activities of the examined EO, it might be potentially used in the management of fungal infections or in the extension of the shelf life of food products.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"718645"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/718645","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9744718","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 142

In Vitro and In Vivo Evaluation of pH-Sensitive Hydrogels of Carboxymethyl Chitosan for Intestinal Delivery of Theophylline. 羧甲基壳聚糖ph敏感水凝胶肠道给药茶碱的体内外评价。

ISRN Pharmaceutics Pub Date : 2012-01-01 Epub Date: 2012-07-01 DOI: 10.5402/2012/763127

Hemant Kumar Singh Yadav, H G Shivakumar

{"title":"In Vitro and In Vivo Evaluation of pH-Sensitive Hydrogels of Carboxymethyl Chitosan for Intestinal Delivery of Theophylline.","authors":"Hemant Kumar Singh Yadav, H G Shivakumar","doi":"10.5402/2012/763127","DOIUrl":"https://doi.org/10.5402/2012/763127","url":null,"abstract":"Chitosan is a natural polymer which has limited solubility. Chitosan gets solubilized at acidic pH but is insoluble at basic pH. In the present study, carboxymethyl chitosan (CMC) was prepared which shows high swelling in basic pH and thus can delay the drug release and can act as matrix for extended release formulation. CMC was characterized by FTIR and NMR. pH-sensitive hydrogels of theophylline were formulated using CMC and carbopol 934. Hydrogels were evaluated for swelling, drug content in vitro drug release studies, and in vivo studies on rabbit. The swelling studies have shown little swelling in acidic pH 432% at the end of two hours and 1631% in basic pH at the end of 12 hours. The release profile of the formulation I containing CMC and carbopol in 1 : 1 ratio showed sustained release. In vivo studies showed that the release of theophylline from the prepared hydrogel formulation (Test) exhibit better prolonged action when compared to (standard) marketed sustained release formulation. The studies showed that the pH-sensitive hydrogel of CMC can be used for extended release of theophylline in intestine and can be highly useful in treating symptoms of nocturnal asthma.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":" ","pages":"763127"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/763127","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30774995","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 42