In this present study, floating microspheres of repaglinide were successfully fabricated by the solvent evaporation technique with varying ratios of guar gum, hydroxypropyl methylcellulose, and ethylcellulose with polyvinyl alcohol. Microspheres were characterized by production yield, particle size, in vitro buoyancy, entrapment efficiency, in vitro drug release, and in vivo floating behavior in albino rats. The formulation process was optimized for stirring speed (X₁) and concentration of polymer ratio (X₂) on dependent variables such as percentage entrapment efficiency, percentage yield, in vitro buoyancy, and percentage of drug release by the 3² factorial Design-Expert^® 12, trial version, software. The optimized formulation was characterized by Fourier transform infrared spectroscopy, powder X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy and was successfully formulated with the highest percentage of cumulative drug release (94.26 ± 3.10), entrapment efficiency (74.70% ± 2.16%), and particle size (50.34 ± 3.67 μm) and remains buoyant for 24 h in simulated gastric fluid (0.1N HCL) with high in vitro buoyancy percent (84.90 ± 2.88). When the drug–polymer solution of dichloromethane and ethanol is dropped in polyvinyl alcohol solution, it leads to the formation of a shell and produces cavities, creating the buoyant nature of floating microspheres. X-ray imaging indicates the uniform distribution and buoyant nature of microspheres in the gastric fluid for a 10-h period.

中文翻译：

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使用 32 因子设计的基于瓜尔胶的瑞格列奈漂浮微球：制备、优化、表征和白化大鼠体内浮力行为

在本研究中，使用不同比例的瓜尔胶、羟丙基甲基纤维素和乙基纤维素与聚乙烯醇，通过溶剂蒸发技术成功制备了瑞格列奈的漂浮微球。微球的特征在于产量、粒径、体外浮力、包封率、体外药物释放和白化大鼠体内漂浮行为。配方过程针对搅拌速度 (X ₁ ) 和聚合物浓度比 (X ₂ ) 进行了优化，这些因变量取决于包封率百分比、产率百分比、体外浮力和 3 ²的药物释放百分比。factorial Design-Expert ^® 12，试用版，软件。优化后的制剂通过傅里叶变换红外光谱、粉末X射线衍射、差示扫描量热法和扫描电镜表征，成功配制具有最高的累积药物释放百分比（94.26±3.10）、包封率（74.70%±2.16） %) 和粒径 (50.34 ± 3.67 μm) 并在体外高浓度模拟胃液 (0.1N HCL) 中保持漂浮状态 24 小时浮力百分比 (84.90 ± 2.88)。当二氯甲烷和乙醇的药物-聚合物溶液滴入聚乙烯醇溶液时，会形成壳并产生空腔，从而产生漂浮微球的浮力特性。X 射线成像表明微球在 10 小时内胃液中的均匀分布和浮力性质。