Background

This work aimed to design and optimize the gastro-retentive drug delivery system (GRDDS) by employing dual principles, i.e., floating and osmotic for pioglitazone hydrochloride (PGH). PGH is commonly prescribed for chronic type II diabetes mellitus (DM).

Method

Floating osmotic drug delivery system (FODDS)–based tablet was prepared to employ a 3²-full factorial design to investigate the influence of HPMC-K4M and NaHCO₃ on floating lag time and in vitro drug release. Furthermore, graphical optimization was carried out to get the optimal combination based on desirability. The excipients-drug interaction was performed by using DSC and FTIR studies.

Results

The optimized bath (OF-O) showed floating lag time (s) = 35.55 ± 2.5 and in vitro drug release (%) = 93.27 ± 2.2. The OF-O showed prolonged release of PGH over 8 h in 0.1 N HCl (pH 1.2). The in vivo estimation of buoyancy in human volunteers in fasted and fed conditions revealed that tablets stayed buoyant in gastric fluid for 8 h. The study concluded that the developed formulation could enhance gastric retention and provide prolonged delivery of PGH.

Conclusion

The implementation of dual principles further widens the scope of gastro-retentive drug delivery (GRDDS) for prolonging the drug release in the gastric cavity.

中文翻译：

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盐酸吡格列酮胃滞留双原理浮动渗透给药系统设计：体外体内评价

背景

本工作旨在利用盐酸吡格列酮（PGH）的漂浮和渗透双重原理设计和优化胃滞留给药系统（GRDDS）。PGH 通常用于治疗慢性 II 型糖尿病 (DM)。

方法

^{采用3 2}全析因设计制备基于漂浮渗透给药系统（FODDS）的片剂，以研究HPMC-K4M 和NaHCO ₃对漂浮滞后时间和体外药物释放的影响。此外，还进行了图形优化，以获得基于需求的最佳组合。通过使用 DSC 和 FTIR 研究进行赋形剂-药物相互作用。

结果

优化浴 (OF-O) 显示漂浮滞后时间 (s) = 35.55 ± 2.5，体外药物释放 (%) = 93.27 ± 2.2。OF-O 在 0.1 N HCl（pH 1.2）中显示 PGH 延长释放超过 8 小时。对人类志愿者在禁食和进食条件下的浮力的体内评估表明，片剂在胃液中保持浮力达 8 小时。研究得出的结论是，所开发的制剂可以增强胃潴留并延长 PGH 的输送时间。

结论

双重原理的实施进一步拓宽了胃滞留药物递送（GRDDS）的范围，以延长药物在胃腔内的释放。