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波罗蜜种子淀粉与结冷胶混合的盐酸二甲双胍粘膜粘附微球

Artocarpus heterophyllus L. seed starch-blended gellan gum mucoadhesive beads of metformin HCl.

作者信息

Nayak Amit Kumar, Pal Dilipkumar, Santra Kousik

机构信息

Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj 757 086, Odisha, India.

Department of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Koni, Bilaspur 495009, Chhattisgarh, India.

出版信息

Int J Biol Macromol. 2014 Apr;65:329-39. doi: 10.1016/j.ijbiomac.2014.01.022. Epub 2014 Jan 18.

Abstract

Jackfruit (Artocarpus heterophyllus Lam., family: Moraceae) seed starch (JFSS)-gellan gum (GG) mucoadhesive beads containing metformin HCl were developed through ionotropic gelation technique. The effect of GG to JFSS ratio and CaCl2 concentration on the drug encapsulation efficiency (DEE, %) and cumulative drug release at 10h (R10h, %) was optimized and analyzed using response surface methodology based on 3(2) factorial design. The optimized JFSS-GG beads containing metformin HCl showed DEE of 92.67±4.46%, R10h of 61.30±2.37%, and mean diameter of 1.67±0.27 mm. The optimized beads showed pH-dependent swelling and mucoadhesivity with the goat intestinal mucosa. The in vitro drug release from all these JFSS-GG beads containing metformin HCl was followed zero-order pattern (R(2)=0.9907-0.9975) with super case-II transport mechanism over a period of 10 h. The beads were also characterized by SEM and FTIR. The optimized JFSS-GG beads containing metformin HCl exhibited significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.

摘要

通过离子凝胶化技术制备了含盐酸二甲双胍的菠萝蜜(Artocarpus heterophyllus Lam.,桑科)种子淀粉(JFSS)-结冷胶(GG)粘膜粘附微球。基于3(2)析因设计,采用响应面法优化并分析了GG与JFSS的比例和CaCl2浓度对药物包封率(DEE,%)和10小时累积药物释放率(R10h,%)的影响。优化后的含盐酸二甲双胍的JFSS-GG微球的DEE为92.67±4.46%,R10h为61.30±2.37%,平均直径为1.67±0.27 mm。优化后的微球对山羊肠粘膜表现出pH依赖性溶胀和粘膜粘附性。所有含盐酸二甲双胍的JFSS-GG微球的体外药物释放在10小时内遵循零级模式(R(2)=0.9907-0.9975),具有超Ⅱ型转运机制。还通过扫描电子显微镜(SEM)和傅里叶变换红外光谱(FTIR)对微球进行了表征。口服给药后,优化后的含盐酸二甲双胍的JFSS-GG微球在四氧嘧啶诱导的糖尿病大鼠中长时间显示出显著的降血糖作用。

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