Nayak Amit Kumar, Pal Dilipkumar
Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj 757086, Odisha, India.
Int J Biol Macromol. 2013 Nov;62:137-45. doi: 10.1016/j.ijbiomac.2013.08.020. Epub 2013 Aug 28.
In this work, calcium pectinate-jackfruit (Artocarpus heterophyllus Lam.) seed starch (JFSS) mucoadhesive beads containing metformin HCl were developed through ionotropic-gelation. Effects of pectin and JFSS amounts on drug encapsulation efficiency (DEE), and cumulative drug release after 10 h (R10 h) were optimized using 3(2) factorial design. The optimized calcium pectinate-JFSS beads containing metformin HCl showed DEE of 94.11 ± 3.92%, R10 h of 48.88 ± 2.02%, and mean diameter of 2.06 ± 0.20 mm. 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 pH of test mediums was found critical for swelling and mucoadhesion of these beads. The optimized calcium pectinate-JFSS beads also exhibited good mucoadhesivity and significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.
在本研究中,通过离子凝胶法制备了含盐酸二甲双胍的果胶酸钙-菠萝蜜(Artocarpus heterophyllus Lam.)种子淀粉(JFSS)粘膜粘附微球。采用3(2)析因设计优化了果胶和JFSS用量对药物包封率(DEE)和10小时后累积药物释放率(R10 h)的影响。优化后的含盐酸二甲双胍的果胶酸钙-JFSS微球的DEE为94.11±3.92%,R10 h为48.88±2.02%,平均直径为2.06±0.20 mm。这些微球的体外药物释放遵循控释(零级)模式,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。发现测试介质的pH值对这些微球的溶胀和粘膜粘附至关重要。优化后的果胶酸钙-JFSS微球在口服给药后的长时间内,对四氧嘧啶诱导的糖尿病大鼠也表现出良好的粘膜粘附性和显著的降血糖作用。