利培酮有机原位凝胶的制备及其体外评价

Preparation and in vitro release analysis of in situ organogel of Risperidone

目的以利培酮为模型药物,制备利培酮有机原位凝胶。方法通过考察凝胶因子和抗凝剂对药物在体内外的释放及相关性的影响,确定最佳的制剂处方。结果注射用大豆油为凝胶基质,12.5%的硬脂酸为凝胶因子,NMP为抗凝剂制备的液态载药有机原位凝胶,在37℃下的体外释放周期约为72 h,体内结果与体外的基本一致。注射予大鼠,无明显的炎症反应。结论利培酮有机原位凝胶是可以延长药物释放周期的新剂型。

OBJECTIVE Using Risperieleve as a model drug to prepare in situ organogel. METHODS The relationship between gelators and anti - gelling solvents in the release of Risperidonc organogel in vitro and in vivo were investigated in order to confirm the optimum formulation. RESULTS The in vitro release period of the prepared Risperidone in situ organogel gel,which was prepared with injectable soybean oil as the base material and 12.5% stearic acid as gelator and NMR as anti - gelling solvent, was about 72 h at 37 ℃. The in vivo release got analogous resuhs. The rats injected displayed no obvious inflammation. CONCLUSION In situ organo- gel of risperidone is a novel dosage form that can prolong the drug release periods.