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盐酸二甲双胍 jackfruit 种籽淀粉-藻酸盐黏膜黏附珠的配方优化与评价。

Formulation optimization and evaluation of jackfruit seed starch-alginate mucoadhesive beads of metformin HCl.

机构信息

Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj 757086, Odisha, India.

出版信息

Int J Biol Macromol. 2013 Aug;59:264-72. doi: 10.1016/j.ijbiomac.2013.04.062. Epub 2013 Apr 26.

Abstract

The present study deals with the formulation optimization of jackfruit (Artocarpus heterophyllus Lam., family: Moraceae) seed starch (JFSS)-alginate mucoadhesive beads containing metformin HCl through ionotropic gelation using 3(2) factorial design. The effect of sodium alginate to JFSS ratio and CaCl2 concentration on the drug encapsulation efficiency (DEE, %), and cumulative drug release at 10h (R10h, %) was optimized. The optimized beads containing metformin HCl showed DEE of 97.48±3.92%, R10h of 65.70±2.22%, and mean diameter of 1.16±0.11mm. The in vitro drug release from these beads was followed controlled-release (zero-order) pattern with super case-II transport mechanism. The beads were also characterized by SEM and FTIR. The swelling and degradation of these beads were influenced by pH of the test medium. The optimized beads also exhibited good mucoadhesivity and significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

摘要

本研究通过离子凝胶化方法,使用 3(2) 因子设计,对包含盐酸二甲双胍的 jackfruit(Artocarpus heterophyllus Lam.,Moraceae 科)种子淀粉(JFSS)-海藻酸钠粘膜粘附珠进行了制剂优化。优化了海藻酸钠与 JFSS 比例和 CaCl2 浓度对药物包封效率(DEE,%)和 10 小时累积药物释放(R10h,%)的影响。含有盐酸二甲双胍的优化珠显示 DEE 为 97.48±3.92%,R10h 为 65.70±2.22%,平均粒径为 1.16±0.11mm。这些珠的体外药物释放遵循控制释放(零级)模式,具有超二级转运机制。这些珠还通过 SEM 和 FTIR 进行了表征。珠的溶胀和降解受测试介质 pH 的影响。优化后的珠在口服给药后延长时间内还表现出良好的粘膜粘附性和显著的降血糖作用,可用于治疗糖尿病。

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