Background

Repaglinide (RPG), as an antidiabetic drug, belongs to the biopharmaceutics classification system (BCS) class II drugs. Utilizing hydrotropy and solid dispersing techniques, the solubility and bioavailability of RPG were improved, and its dropping pills were prepared in this work.

Methods

The optimal repaglinide and arginine (RPG-Arg) complex powder was prepared and charactered by the Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The stability of their complexes was evaluated by the stress testing, and the drug release in vitro and the pharmacokinetics in vivo of RPG-Arg complex were studied. Moreover, the dropping pills using RPG-ARG complex were prepared.

Results

RPG-Arg was successfully prepared and appeared to be amorphous state. The drug release from RPG-Arg dropping pills was better than that of RPG dropping pills. Meanwhile, the area under the curve (AUC) of oral RPG-Arg dropping pills and RPG-Arg solution at i.g./or i.v. administration was larger than that of RPG dropping pills and RPG suspensions, respectively.

Conclusion

The solubility and bioavailability of RPG is enhanced using hydrotropy and solid dispersion techniques, which is a simple and effective way.

中文翻译：

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利用水溶-固相分散技术提高瑞格列奈的生物利用度并制备滴丸

背景

瑞格列奈（RPG）作为降糖药，属于生物药剂学分类系统（BCS）II类药物。本工作利用水溶助长和固体分散技术，提高了RPG的溶解性和生物利用度，制备了其滴丸。

方法

制备了最佳瑞格列奈精氨酸 (RPG-Arg) 复合粉末，并通过傅里叶变换红外光谱 (FT-IR)、X 射线衍射 (XRD) 和差示扫描量热法 (DSC) 对其进行表征。通过压力试验评价其复合物的稳定性，研究RPG-Arg复合物的体外释药和体内药代动力学。此外，制备了使用RPG-ARG复合物的滴丸。

结果

RPG-Arg 制备成功，呈无定形状态。RPG-Arg滴丸的药物释放优于RPG滴丸。同时，口服RPG-Arg滴丸和RPG-Arg溶液在ig /或iv给药的曲线下面积（AUC）分别大于RPG滴丸和RPG混悬剂的曲线下面积。

结论

使用水溶和固体分散技术提高RPG的溶解度和生物利用度，这是一种简单有效的方法。