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Effect of formulation variables on in vitro release of a water-soluble drug from chitosanesodium alginate matrix tablets

查看全文 作　　者：Liang [1]Li;Jinfeng [1]Li;Shanshan [1,2]Si;Linlin [1]Wang;Chenjun [1]Shi;Yujiao [1]Sun;Zhenglin [1]Liang;Shirui [1]Mao 高影响力作者 机构地区：[1]School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China;[2]Jiangsu Hengrui Medicine Co.,Ltd.,Lianyungang 222047,China高影响力机构 出　　处：《Asian Journal of Pharmaceutical Sciences》索引2015年第10卷第4期,共8页高影响力期刊 基　　金：supported by Liaoning Institutions excellent talents support plan(No.LR2013047). 摘　　要：The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using trimetazidine hydrochloride(TH)as a water-soluble model drug,influence of dissolution medium,the amount of CSeSA,the CS:SA ratio,the type of SA,the type and amount of diluents,on in vitro drug release from CSeSA based matrix tablets were studied.Drug release kinetics and release mechanisms were elucidated.In vitro release experiments were conducted in simulated gastric fluid(SGF)followed by simulated intestinal fluid(SIF).Drug release rate decreased with the increase of CSeSA amount.CS:SA ratio had only slight effect on drug release and no influence of SA type on drug release was found.On the other hand,a large amount of water-soluble diluents could modify drug release profiles.It was found that drug release kinetics showed the best fit to Higuchi equation with Fickian diffusion as the main release mechanism.In conclusion,this study demonstrated that it is possible to design extended-release tablets of watersoluble drugs using CSeSA as the matrix by optimizing formulation components,and provide better understanding about drug release from CSeSA matrix tablets. 关 键 词：CHITOSAN Sodium alginate Matrix tablets Hydrophilic matrices Trimetazidine hydrochloride EXTENDED-RELEASE
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