盐酸二甲双胍伊波加胶-结冷胶黏膜粘附珠的响应面法制备。
Ispaghula mucilage-gellan mucoadhesive beads of metformin HCl: development by response surface methodology.
机构信息
Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj 757086, Odisha, India.
Department of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Koni, Bilaspur 495 009, C.G., India.
出版信息
Carbohydr Polym. 2014 Jul 17;107:41-50. doi: 10.1016/j.carbpol.2014.02.022. Epub 2014 Feb 15.
Response surface methodology based on 3(2) factorial design was used to develop ispaghula (Plantago ovata F.) husk mucilage (IHM)-gellan gum (GG) mucoadhesive beads containing metformin HCl through Ca(2+)-ion cross-linked ionotropic-gelation technique for the use in oral drug delivery. GG to IHM ratio and cross-linker (CaCl2) concentration were investigated as independent variables. Drug encapsulation efficiency (DEE, %) and cumulative drug release after 10h (R10h, %) were analyzed as dependent variables. The optimized mucoadhesive beads (F-O) showed DEE of 94.24 ± 4.18%, R10h of 59.13 ± 2.27%. These beads were also characterized by SEM and FTIR analyses. The in vitro drug release from these beads showed controlled-release (zero-order) pattern with super case-II transport mechanism over 10h. The optimized beads showed pH-dependent swelling and good mucoadhesivity with the goat intestinal mucosa. The optimized IHM-GG mucoadhesive beads containing metformin HCl exhibited significant antidiabetic effect in alloxan-induced diabetic rats over 10h.
基于 3(2) 析因设计的响应面法被用于开发伊车前（Plantago ovata F.）种皮粘液（IHM）-结冷胶（GG）粘膜粘附珠，通过 Ca(2+)离子交联离子凝胶技术将盐酸二甲双胍包埋其中，用于口服药物传递。GG 与 IHM 的比例和交联剂（CaCl2）浓度被作为独立变量进行研究。药物包封效率（DEE，%）和 10 小时后累积药物释放（R10h，%）被分析为依赖变量。优化的粘膜粘附珠（F-O）显示出 94.24±4.18%的 DEE 和 59.13±2.27%的 R10h。这些珠子还通过 SEM 和 FTIR 分析进行了表征。这些珠子的体外药物释放显示出在 10 小时内具有控释（零级）模式和超二级传输机制。优化的珠子表现出 pH 依赖性溶胀和与山羊肠粘膜良好的粘膜粘附性。含有盐酸二甲双胍的优化的 IHM-GG 粘膜粘附珠在 10 小时内对所有糖尿病大鼠表现出显著的降血糖作用。
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