Sulpiride (SUL), anti-dopaminergic drug, has a specific site for absorption located in the upper portion of the gastrointestinal tract hence, its oral delivery represents a challenge regarding SUL absorption and bioavailability. So, a gastro-retentive oral platform of SUL was developed to increase its gastric residence time, release SUL at a controlled rate in the stomach and consequently, enable it to reach its specific absorption site. Floating microsponges were prepared via quasi-emulsion solvent diffusion method and characterised for their physico-chemical properties. In addition, Taguchi design of experiment was utilised to optimise some independent variables affecting microsponges performance. The optimised SUL microsponges showed a yield of 79.82 ± 2.37%, an encapsulation efficiency of 89.11 ± 2.28% and in vitro time for floatation of 8.0 h. Additionally, pharmacokinetics were investigated in rabbits and compared with the commercial SUL formulation, Dogmatil® capsules. Optimised SUL microsponges showed a significantly (p < .05) higher Cmax, AUC and 2-fold increase in oral bioavailability compared with the commercial product. Moreover, the optimised SUL microsponges remained present in the stomach up to 8.0 h post administration when viewed via X-ray radiographs in rabbits. It could be concluded that the floating microsponges could be useful as an oral platform to enhance the sulpiride absorption and bioavailability.

中文翻译：

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舒必利胃滞留漂浮微海绵；分析研究、体外优化和体内表征。

舒必利 (SUL) 是一种抗多巴胺能药物，具有位于胃肠道上部的特定吸收位点，因此其口服给药对 SUL 的吸收和生物利用度提出了挑战。因此，开发了 SUL 的胃滞留口服平台，以增加其在胃中的停留时间，在胃中以受控速率释放 SUL，从而使其能够到达其特定的吸收位点。采用准乳化溶剂扩散法制备了漂浮微海绵，并对其理化性质进行了表征。此外，利用田口实验设计来优化一些影响微海绵性能的自变量。优化后的 SUL 微海绵的产率为 79.82 ± 2.37%，封装效率为 89.11 ± 2.28%，体外漂浮时间为 8.0 h。此外，还在兔子中研究了药代动力学，并与商业 SUL 制剂 Dogmatil® 胶囊进行了比较。与商业产品相比，优化的 SUL 微海绵显示出显着 (p < .05) 更高的 Cmax、AUC 和口服生物利用度的 2 倍增加。此外，当通过兔子的 X 射线照片观察时，优化的 SUL 微海绵在给药后长达 8.0 小时仍存在于胃中。可以得出结论，漂浮的微海绵可用作口服平台，以提高舒必利的吸收和生物利用度。与商业产品相比，AUC 和口服生物利用度增加了 2 倍。此外，当通过兔子的 X 射线照片观察时，优化的 SUL 微海绵在给药后长达 8.0 小时仍存在于胃中。可以得出结论，漂浮的微海绵可用作口服平台，以提高舒必利的吸收和生物利用度。与商业产品相比，AUC 和口服生物利用度增加了 2 倍。此外，当通过兔子的 X 射线照片观察时，优化的 SUL 微海绵在给药后长达 8.0 小时仍存在于胃中。可以得出结论，漂浮的微海绵可用作口服平台，以提高舒必利的吸收和生物利用度。