Department of Pharmaceutics, Bengal College of Pharmaceutical Sciences and Research, Durgapur 713212, West Bengal, India.
Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj 757086, Odisha, India.
Int J Biol Macromol. 2014 Mar;64:181-9. doi: 10.1016/j.ijbiomac.2013.11.014. Epub 2013 Dec 1.
The present study deals with the development and evaluations of stomach-specific floating capsules containing salbutamol sulfate-loaded oil-entrapped alginate-based beads. Salbutamol sulfate-loaded oil-entrapped beads were prepared and capsulated within hard gelatin capsules (size 1). The effects of HPMC K4M and potato starch weight masses on drug encapsulation efficiency (DEE) of beads and cumulative drug release at 10h (R10 h) from capsules was analyzed by 3(2) factorial design. The optimization results indicate increasing of DEE in the oil-entrapped beads and decreasing R10 h from capsules with increment of HPMC K4M and potato starch weight masses. The optimized formulation showed DEE of 70.02 ± 3.16% and R10 h of 56.96 ± 2.92%. These capsules showed floatation over 6h and sustained drug release over 10h in gastric pH (1.2). In vivo X-ray imaging study of optimized floating capsules in rabbits showed stomach-specific gastroretention over a prolonged period.
本研究致力于开发和评估含有沙丁胺醇硫酸盐载药油包被海藻酸钠微球的胃内漂浮胶囊。制备了沙丁胺醇硫酸盐载药油包被微球，并将其包封在硬明胶胶囊（1 号）中。通过 3(2) 因子设计分析了 HPMC K4M 和马铃薯淀粉重量对微球药物包封效率（DEE）和胶囊 10 小时累积药物释放（R10 h）的影响。优化结果表明，随着 HPMC K4M 和马铃薯淀粉重量的增加，油包被微球的 DEE 增加，胶囊的 R10 h 降低。优化后的配方显示 DEE 为 70.02 ± 3.16%，R10 h 为 56.96 ± 2.92%。这些胶囊在 pH 值为 1.2 的胃液中可漂浮 6 小时以上，并持续释放药物 10 小时以上。在兔体内的 X 射线成像研究中，优化后的漂浮胶囊在胃内表现出长时间的胃滞留特性。
