基于苦楝酸RL - 100-壳聚糖互聚电解质配合物的结肠靶向布洛芬片处方开发及释药动力学评价。

ISRN Pharmaceutics Pub Date : 2013-08-06 eCollection Date: 2013-01-01 DOI:10.1155/2013/838403
Kenneth Chibuzor Ofokansi, Franklin Chimaobi Kenechukwu
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引用次数: 32

摘要

结肠靶向给药系统(CTDDSs)可用于局部治疗炎症性肠病(IBDs)。本研究采用非化学计量法,对乌龙茶RL100 (EL)与壳聚糖(CS)形成的多种聚电解质间络合物(ipec)和湿造粒法制备的ipec片作为布洛芬(IBF)的潜在口服ctdds进行了评价。结果表明,该片剂符合药典验收要求,且CS与EL形成的ipec具有ph依赖性的溶胀特性,其体外释放时间由大到小依次为:CS与EL的比例为3:2 > 2:3 > 1:1。与ipec配制的片剂中EL的羰基(- co -)基团与CS的氨基(- nh3(+))基团之间的静电相互作用能够阻止药物在胃和小肠中的释放,并有助于将药物输送到结肠。药物释放动力学分析表明,该系统主要以零级方式释放IBF。基于CS和EL的ipec可以成功地用于ibd治疗中IBF的结肠靶向递送。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes.

Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (-CO-) group of EL and amino (-NH3 (+)) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs.

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