Journal of Pharmacy Research最新文献

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Transgenic plants: Types, benefits, public concerns and future 转基因植物:类型、利益、公众关注和未来
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.008
S. Jhansi Rani, R. Usha
{"title":"Transgenic plants: Types, benefits, public concerns and future","authors":"S. Jhansi Rani,&nbsp;R. Usha","doi":"10.1016/j.jopr.2013.08.008","DOIUrl":"10.1016/j.jopr.2013.08.008","url":null,"abstract":"<div><p>The alteration of crops to improve their production was performed through the basis of selection before the creation of transgenics. This selection has been going on for thousands of years. By the year 2050, world population may reach nine billions. Food production will need to increase at the same rate or more in order to satisfy the needs of such an enormous number of people in some older centuries. So, there is a need to use the genetic techniques to improve crops over the recent decades. Through the use of transgenics, one can produce plants with desired traits and even increased yields. The transgenics would allow for more crops that last longer and withstand pests and diseases. Transgenic plant production will allow us to feed the growing population and to produce more desirable products. The future of GM crops remains a vital debate, as its applications have several advantages and disadvantages.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 8","pages":"Pages 879-883"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87552935","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: 43
Design of lamivudine XR matrix tablets: Influence of HPMC and PEO on in vitro drug release and bioavailability in rabbits 拉米夫定XR基质片设计:HPMC和PEO对体外释药及兔体内生物利用度的影响
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.010
Prakash Katakam , Narayana Raju Padala , Babu Rao Chandu , Abdelbaset Elfituri , Shanta Kumari Adiki , Ravishankar Kommu
{"title":"Design of lamivudine XR matrix tablets: Influence of HPMC and PEO on in vitro drug release and bioavailability in rabbits","authors":"Prakash Katakam ,&nbsp;Narayana Raju Padala ,&nbsp;Babu Rao Chandu ,&nbsp;Abdelbaset Elfituri ,&nbsp;Shanta Kumari Adiki ,&nbsp;Ravishankar Kommu","doi":"10.1016/j.jopr.2013.08.010","DOIUrl":"10.1016/j.jopr.2013.08.010","url":null,"abstract":"<div><h3>Background/objectives</h3><p>In the present study oral extended release matrix tablets of lamivudine were formulated, characterized and evaluated for <em>in vitro</em> dissolution and <em>in vivo</em> bioavailability performance in rabbits.</p></div><div><h3>Methods</h3><p>Matrix tablets of lamivudine were prepared using hydroxypropyl methylcellulose K100M and its combination with polyethylene oxide as the release rate retardant polymers. The tablets were characterized for physical properties, moisture uptake studies, <em>in vitro</em> dissolution, accelerated stability (40 ± 2 °C and 75 ± 5% RH) testing. <em>In vivo</em> studies were performed by oral administration of optimized formulation in rabbits.</p></div><div><h3>Results</h3><p><em>In vitro</em> studies revealed that the release rate decreased with increase in polymer concentration, polymer viscosity and combination of polymers. The drug release from the matrix tablets followed diffusion mechanism. Comparable correlation of <em>in vitro</em> drug release was observed in the initial and accelerated stability samples of lamivudine matrix tablets prepared with hydroxypropyl methylcellulose alone and its combination with polyethylene oxide. Significant bioavailability was observed in the <em>in vivo</em> evaluation. The <em>C</em><sub>max</sub>, <em>t</em><sub>max</sub>, AUC and <em>K</em><sub>el</sub> for F-3 matrix tablets were 1361 ng/ml, 4 h, 25,013.5 ng min/ml and 0.0719 h<sup>−1</sup> respectively. DSC and FT-IR spectra of initial and stability samples showed the absence of drug–excipient incompatibility in the formulations. The developed extended release matrix tablets of lamivudine were stable up to three months.</p></div><div><h3>Conclusions</h3><p>The release of the matrix tablets for prolonged periods of time employing polyethylene oxide and hydroxypropyl methylcellulose as drug rate retarding polymers could be advantageous than conventional lamivudine tablets. The study could be extended for bioavailability studies in clinical subjects.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 8","pages":"Pages 845-852"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82957750","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: 4
Evaluation of effect of aqueous slurry of Curculigo orchioides Gaertn. rhizome in streptozotocin-induced diabetic rats 莪术水浆的效果评价。链脲佐菌素诱导的糖尿病大鼠的根茎
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.016
Avinash Patil , Swapneel Koli , Darshana A. Patil , Vinod Narayane , Anita V. Phatak
{"title":"Evaluation of effect of aqueous slurry of Curculigo orchioides Gaertn. rhizome in streptozotocin-induced diabetic rats","authors":"Avinash Patil ,&nbsp;Swapneel Koli ,&nbsp;Darshana A. Patil ,&nbsp;Vinod Narayane ,&nbsp;Anita V. Phatak","doi":"10.1016/j.jopr.2013.08.016","DOIUrl":"10.1016/j.jopr.2013.08.016","url":null,"abstract":"<div><h3>Aim</h3><p>The present study was undertaken to carry out phytochemical analysis and to investigate the antihyperglycaemic effect of aqueous slurry of <em>Curculigo orchioides</em> Gaertn. rhizome powder (ASCO) for 21 days.</p></div><div><h3>Method</h3><p>Diabetes was induced in Albino Wistar rats by single intraperitoneal administration of streptozotocin (50 mg/kg body weight). Normal as well as diabetic rats were divided into four groups to receive different treatments.</p></div><div><h3>Result</h3><p>Preliminary phytochemical analysis showed presence of glycosides, mucilage, tannins, steroids, flavonoids, saponins and essential oils. Phytochemical analysis using TLC showed presence of arbutin, bitter principles, cardiac glycosides, coumarins, essential oils, lignans, pungent-tasting principles, saponins, triterpenes and valepotriates. Acute toxicity study in rats did not show any signs of toxicity up to the dose of 2000 mg/kg body weight. In STZ induced diabetic rats, the daily oral treatment with ASCO (1000 mg/kg body weight) showed a significant reduction in blood glucose level. STZ administration severely deteriorated the histological structures of pancreas, kidney and liver of diabetic rats, which were found to be restored to certain extent in glibenclamide and ASCO treated animals.</p></div><div><h3>Conclusion</h3><p>The study indicated that ASCO is a potential antidiabetic agent and lends scientific support for its use in folk medicines.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 8","pages":"Pages 747-753"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.016","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84770109","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: 6
Assessment of antidiabetic potential of Cissampelos pareira leaf extract in streptozotocin–nicotinamide induced diabetic mice 顺子叶提取物对链脲佐菌素-烟酰胺诱导的糖尿病小鼠的降糖作用
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.06.027
Kuldeep Singh Yadav , Narayan Prasad Yadav , Karuna Shanker , Shiny C. Thomas , Saurabh Srivastav , Shruti Srivastava , Vineet Kumar Rai , Nidhi Mishra , Priyam Sinha
{"title":"Assessment of antidiabetic potential of Cissampelos pareira leaf extract in streptozotocin–nicotinamide induced diabetic mice","authors":"Kuldeep Singh Yadav ,&nbsp;Narayan Prasad Yadav ,&nbsp;Karuna Shanker ,&nbsp;Shiny C. Thomas ,&nbsp;Saurabh Srivastav ,&nbsp;Shruti Srivastava ,&nbsp;Vineet Kumar Rai ,&nbsp;Nidhi Mishra ,&nbsp;Priyam Sinha","doi":"10.1016/j.jopr.2013.06.027","DOIUrl":"10.1016/j.jopr.2013.06.027","url":null,"abstract":"<div><h3>Objective</h3><p>To validate the traditional use of <em>Cissampelos pareira</em> as an antidiabetic agent in streptozotocin–nicotinamide induced diabetic male mice.</p></div><div><h3>Methods</h3><p>Antidiabetic effect of aqueous extract of <em>C. pareira</em> leaves (CPAE) was evaluated at 250 mg/kg and 500 mg/kg body weight, p.o. doses in male albino mice over the period of 14 days. Random blood glucose level and body weight were observed periodically. Liver glycogen level, organ coefficient and other biochemical parameters were also determined after completion of the study.</p></div><div><h3>Result</h3><p>Significant (<em>p</em> &lt; 0.001) changes were observed in random blood glucose levels of mice after 14 days of treatment period at 500 mg/kg CPAE treatment. Aspartate transaminase, alanine transaminase, alkaline phosphatase, total bilirubin, triglycerides and creatinine levels were significantly (<em>p</em> &lt; 0.05) decreased while liver tissue glycogen and serum protein levels were significantly (<em>p</em> &lt; 0.05) increased after CPAE administration. No significant changes were observed in body weight and organ coefficient.</p></div><div><h3>Conclusions</h3><p>The present study concluded that the aqueous extract of <em>C. pareira</em> at 500 mg/kg body weight was capable in reducing diabetic attritions so it might be a valuable candidate for diabetes treatment.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 8","pages":"Pages 874-878"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.06.027","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84614471","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: 15
Utilization of phosphotungestic acid in the conductometric determination of loperamide hydrochloride and trimebutine antidiarrhea drugs 磷酸钨酸电导法测定盐酸洛哌丁胺和曲美布汀止泻药物的含量
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.07.031
Hoda M. Elqudaby , Gehad G. Mohamed , Ghada M.G. El Din
{"title":"Utilization of phosphotungestic acid in the conductometric determination of loperamide hydrochloride and trimebutine antidiarrhea drugs","authors":"Hoda M. Elqudaby ,&nbsp;Gehad G. Mohamed ,&nbsp;Ghada M.G. El Din","doi":"10.1016/j.jopr.2013.07.031","DOIUrl":"10.1016/j.jopr.2013.07.031","url":null,"abstract":"<div><h3>Aim</h3><p>Phosphotungestic acid (PTA), was used as titrant for the conductometric determination of loperamide hydrochloride (LOP.HCl) and trimebutine (TB) antidiarrhea drugs through ion-associated complex formation.</p></div><div><h3>Method</h3><p>The effect of the reagent concentration, temperature, molar combining ratio, and the solubility products of the formed ion-associates were studied and calculated.</p></div><div><h3>Results</h3><p>The suggested method was applied for the determination of loperamide hydrochloride and trimebutine in their pure form and pharmaceutical preparations with mean recovery values of 99.67 and 99.47 % for loperamide hydrochloride in pure form and in Imodium capsule, respectively, and 99.88 and 99.04 % for trimebutine in pure form and in Triton tablets, respectively. Relative standard deviation was less than 1.0%. The accuracy of the method was indicated by excellent recovery while low standard deviation supported the precision of the method. The sensitivity of the proposed method was discussed and the results were compared with the pharmacopeial methods.</p></div><div><h3>Conclusion</h3><p>The proposed procedure was simple, rapid, sensitive, and accurate and can be applied for the routine measurements of the cited drugs.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 8","pages":"Pages 686-691"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.07.031","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81603925","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: 11
Studies on development and characterization of gastroretentive drug delivery system for antibiotics: Cefdinir 头孢地尼抗生素胃保留给药系统的开发与表征研究
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.011
Prasad Garrepally , Chandra Sekhara Rao Gonugunta
{"title":"Studies on development and characterization of gastroretentive drug delivery system for antibiotics: Cefdinir","authors":"Prasad Garrepally ,&nbsp;Chandra Sekhara Rao Gonugunta","doi":"10.1016/j.jopr.2013.08.011","DOIUrl":"10.1016/j.jopr.2013.08.011","url":null,"abstract":"<div><h3>Aims/objective</h3><p>Oral SR gastroretentive dosage forms offer many advantages for drugs having absorption from upper GIT and improve the bioavailability of medications that are characterized by narrow absorption window. Cefdinir is a third generation cephalosporin with broad spectrum of activity with low bioavailability (20–30%) and short biological half life (1–2 h). It has better absorption from upper part of gastrointestinal tract. The purpose of present study was to formulate and develop a new GRDDS using bilayered tablet technology for cefdinir as a model drug.</p></div><div><h3>Methods</h3><p>Cefdinir bilayer tablets (CBT) were prepared by using double compression cup and core method. First layer, floating matrix layer contained different rate retarding polymers and effervescent mixture. Second layer is loading layer contained cefdinir and fast releasing components (soluble starch, sodium bicarbonate and citric acid). All CBT were evaluated for their pre and post compression parameters.</p></div><div><h3>Results</h3><p>Precompression and post compression parameter of all CBT were within the pharmacopeial limits. In vitro buoyancy behavior and matrix integrity study revealed that FLT of optimized formulation was 1.57 ± 0.52 min and the tablet remained floatable throughout the study. In vitro drug release of optimized CBT follows initially first order release upto 30 min (till their release of loading layer), then zero order release upto 12 h and kinetic profile followed the Peppas (<em>R</em><sup>2</sup> = 0.9838) and zero order (<em>R</em><sup>2</sup> = 0.9986). FTIR studies revealed no drug–excipients interactions. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, floatability, matrix integrity.</p></div><div><h3>Conclusion</h3><p>Kinetics of CBT showed biphasic release in the first phase, immediate dose was released in less than 60 min and second phase was released from matrix layer as a controlled zero order fashion. Cefdinir is a suitable drug for development of gastroretentive bilayer tablet.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 8","pages":"Pages 836-844"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.011","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87490703","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: 5
Scientific validation and formulation of three Indian Folklore medicinal plants 三种印度民间药用植物的科学验证和配方
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.012
Seru Ganapaty , Maddi Ramaiah , Prudhivi Ramakrishna , Daka Nagarjuna Reddy
{"title":"Scientific validation and formulation of three Indian Folklore medicinal plants","authors":"Seru Ganapaty ,&nbsp;Maddi Ramaiah ,&nbsp;Prudhivi Ramakrishna ,&nbsp;Daka Nagarjuna Reddy","doi":"10.1016/j.jopr.2013.08.012","DOIUrl":"10.1016/j.jopr.2013.08.012","url":null,"abstract":"<div><h3>Aims</h3><p>The present study was aimed to study the <em>in vitro</em> antioxidant property by DPPH, superoxide, and hydroxyl radical scavenging assays, <em>in vivo</em> hepatoprotective activity by CCl<sub>4</sub> induced hepatotoxicity in albino rats, formulation of polyherbal hepatoprotective tablets containing equal quantities of methanolic extract of roots of <em>Begonia laciniata</em> Roxb., whole plant of <em>Cuscuta epithymum</em> (L.) L and whole plant of <em>Dendrobium ovatum</em> (L.) Kraenzl., which were used traditionally in Chittoor and Khammam districts of Andhra Pradesh, India.</p></div><div><h3>Methods</h3><p>Formulation was developed by direct compression method using super tab-11SD, primojel, talc and magnesium stearate as excipients and then subjected to evaluation of precompression and post compression parameters.</p></div><div><h3>Results and conclusion</h3><p>All the selected plants showed dose dependant antioxidant property, highest at 360 μg dose and significant dose dependant hepatoprotective activity, highest at a dose of 400 mg/kg b.w compared to standard drug silymarin, the histopathological studies also confirmed protective effects of extracts against CCl4-induced liver injuries. The observations from formulation support the ideal properties of compressed tablets and its feasibility for large-scale commercial production.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"6 8","pages":"Pages 823-835"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.012","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82042527","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: 6
Investigation of in-vitro anthelmintic activity of ethanolic leaf extract of Boerhavia diffusa (Nyctaginaceae) including pharmacognostical and phytochemical screening 白花菊叶乙醇提取物体外驱虫活性研究,包括生药学和植物化学筛选
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.009
Ramasubramania Raja Rajagopal
{"title":"Investigation of in-vitro anthelmintic activity of ethanolic leaf extract of Boerhavia diffusa (Nyctaginaceae) including pharmacognostical and phytochemical screening","authors":"Ramasubramania Raja Rajagopal","doi":"10.1016/j.jopr.2013.08.009","DOIUrl":"10.1016/j.jopr.2013.08.009","url":null,"abstract":"<div><p>The present study clearly indicated that the crude ethanol extract of <em>Boerhavia diffusa</em> did produce anthelmintic activity against Indian earthworm <em>Pheretima posthuma</em>. The plant possesses significant anthelmintic activity at 100 mg/ml concentration measured by time taken for paralyze/death of the earth worms. The current investigation leads to conclusion that the leaves of <em>B. diffusa</em> have potent anthelmintic activity of conventionally used drug. The results did not, however, exclude the possibility that doses of the extract with lower anthelmintic activity in this study might be efficacious against other species of helminths. Further studies using <em>in vivo</em> models and to isolate active constituents from extract are required to carry out and established the effectiveness and pharmacological rational for the use of <em>B. diffusa</em> as an anthelmintic drug.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 8","pages":"Pages 774-780"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.009","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75989923","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: 9
3D QSAR based design of novel substituted urea molecules as heparanase inhibitors 基于3D QSAR的新型替代尿素分子肝素酶抑制剂设计
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.024
Raju Bathini, Sabiha Fatima, Sree Kanth Sivan, Vijjulatha Manga
{"title":"3D QSAR based design of novel substituted urea molecules as heparanase inhibitors","authors":"Raju Bathini,&nbsp;Sabiha Fatima,&nbsp;Sree Kanth Sivan,&nbsp;Vijjulatha Manga","doi":"10.1016/j.jopr.2013.08.024","DOIUrl":"10.1016/j.jopr.2013.08.024","url":null,"abstract":"<div><h3>Aim</h3><p>To study the key pharmacophore requirements for heparanase inhibition and design of new molecules.</p></div><div><h3>Method</h3><p>Three dimensional quantitative structure activity relationship (3D QSAR) methodologies namely Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) were applied, PLS analysis was performed and QSAR models were generated for a set of 43 bezoxazol-5-yl acetic acid derivatives and 1,3-bis[4-(1H-bezimidazol-2-yl)-phenyl urea reported as potent inhibitors of heparanase.</p></div><div><h3>Result</h3><p>QSAR model showed good internal and external statistical reliability that is evident from the <span><math><mrow><msubsup><mi>q</mi><mrow><mtext>loo</mtext></mrow><mn>2</mn></msubsup></mrow></math></span>, <span><math><mrow><msubsup><mi>r</mi><mrow><mtext>ncv</mtext></mrow><mn>2</mn></msubsup></mrow></math></span> and <span><math><mrow><msubsup><mi>r</mi><mrow><mtext>pred</mtext></mrow><mn>2</mn></msubsup></mrow></math></span>. CoMFA model provides a correlation of steric and electrostatic field with biological activities. CoMSIA model provides a correlation of steric, electrostatic, acceptor, donor and hydrophobic fields with biological activities.</p></div><div><h3>Conclusion</h3><p>The identified key features enabled us to design novel symmetrical 1,3-bis[4-(1H-bezimidazol-2-yl)-phenyl urea derivatives.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 8","pages":"Pages 754-761"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.024","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81312233","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: 3
Development and validation of a liquid chromatography mass spectrometry method for the determination of donepezil in human plasma 液相色谱-质谱法测定人血浆中多奈哌齐含量的建立与验证
Journal of Pharmacy Research Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.021
Prakash Katakam , Rama Rao Kalakuntla , Shanta Kumari Adiki , Babu Rao Chandu
{"title":"Development and validation of a liquid chromatography mass spectrometry method for the determination of donepezil in human plasma","authors":"Prakash Katakam ,&nbsp;Rama Rao Kalakuntla ,&nbsp;Shanta Kumari Adiki ,&nbsp;Babu Rao Chandu","doi":"10.1016/j.jopr.2013.08.021","DOIUrl":"10.1016/j.jopr.2013.08.021","url":null,"abstract":"<div><h3>Aim</h3><p>A selective, and sensitive LC–MS/MS method has been developed and validated for quantification of donepezil in human plasma using donepezil D7 as an internal standard (IS).</p></div><div><h3>Methods</h3><p>The analyte and IS were extracted by liquid–liquid extraction using dichloromethane and hexane mixture and separated by isocratic elution on C18 analytical column with 0.1% formic acid and methanol in the ratio of 70:30 (flow rate of 1 ml/min) as the mobile phase in the positive ion mode. Multiple Reaction Monitoring transitions for donepezil and internal standard are 380.2/91.2 and 387.2/98.2 respectively.</p></div><div><h3>Results</h3><p>The lower limit of quantification was 50 pg/ml with the linearity range of 50 pg/ml–25,000 pg/ml and the method was validated as per international regulatory guidelines for its selectivity, stability, accuracy, precision, and recovery.</p></div><div><h3>Conclusion</h3><p>The method can be readily applicable to pharmacokinetic and bioequivalence studies to support different regulatory submissions.</p></div>","PeriodicalId":16787,"journal":{"name":"Journal of Pharmacy Research","volume":"7 8","pages":"Pages 720-726"},"PeriodicalIF":0.0,"publicationDate":"2013-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.jopr.2013.08.021","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85677036","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: 12
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