Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj-757086, Odisha, India..
Curr Drug Deliv. 2013 Oct;10(5):608-19. doi: 10.2174/1567201811310050012.
The present investigation describes development and optimization of pioglitazone-loaded jackfruit seed starch (JFSS)-alginate beads by ionotropic-gelation using 3(2) factorial design. The effect of polymer-blend ratio and CaCl2 concentration on the drug encapsulation efficiency (DEE, %), and cumulative drug release after 10 hours (R10h, %) was optimized. The DEE (%) of these beads were 64.80 ± 1.92 to 94.07 ± 3.82 % with sustained in vitro drug release of 64.± 1.83 to 92.66 ± 4.54 % over 10 hours. The in vitro drug release from these beads followed controlled-release pattern with super case-II transport. Particle size range of these beads was 0.77 ± 0.04 to 1.24 ± 0.09 mm. The beads were also characterized by SEM and FTIR. The swelling of these beads was influenced by pH of the test medium. The optimized pioglitazone-loaded JFSS-alginate beads showed significant hypoglycemic effect in alloxan-induced diabetic rats over prolonged period after oral administration.
本研究采用离子凝胶法，通过 3(2) 因子设计，开发并优化了载吡格列酮的菠萝蜜种子淀粉（JFSS）-海藻酸钠珠。考察了聚合物混合比和 CaCl2 浓度对药物包封效率（DEE，%）和 10 小时后累积药物释放（R10h，%）的影响。这些珠的 DEE（%）为 64.80±1.92 至 94.07±3.82%，体外药物释放可持续 10 小时，释放量为 64.±1.83 至 92.66±4.54%。这些珠的体外药物释放呈现出超二级转运的控制释放模式。这些珠的粒径范围为 0.77±0.04 至 1.24±0.09mm。这些珠还通过 SEM 和 FTIR 进行了表征。珠的溶胀受测试介质 pH 的影响。经口给予优化后的载吡格列酮的 JFSS-海藻酸钠珠在延长的时间内，对链脲佐菌素诱导的糖尿病大鼠表现出显著的降血糖作用。
