雷帕霉素栓剂的制备及质量评价

目的：制备一种含雷帕霉素的聚乙二醇栓剂，并对其质量进行评价。方法：以雷帕霉素为原料药，聚乙二醇2000和聚乙二醇4000为主要基质，热熔法工艺制备含药栓剂，并对其药物含量、重量差异、融变时限、药物溶出等进行评价。结果：雷帕霉素聚乙二醇栓剂外观呈白色半透明状，室温下保持较好的硬度，药物含量、重量差异和融变时限均符合栓剂要求，药物在释放介质中约25min释放达到75％以上。结论：本研究制备的雷帕霉素聚乙二醇栓剂符合中国药典栓剂质量检测要求，有望开发成雷帕霉素的一种新剂型。

Preparation and quality evaluation of rapamycin suppository

Objective： To prepare rapamycin suppository, and to evaluate its quality. Methods： Rapamycinwas used as active ingredient, polyethylene glycol 2000 and polyethylene glycol 4000 were used as main substrates. The suppositories were made using hot melt process method, and the drug content, weight difference, melting time, drug release with time were evaluated. Results： Polyethylene glycol suppository with rapamycin appeared white and translucent. Good hardness could be maintained at room temperature. The drug content, weight varia- tion and melting time limit matched the requirements for the suppository. More than 75% of the loaded drug in the suppositories was released at about 25 min in the medium. Conclusion： This preparation of rapamycin polyeth- ylene glycol （PEG） suppository can reach the quality requirements of Chinese pharmacopoeia, and may be developed as a new formulation of rapamycin.