一种小型复方雷帕霉素栓剂的制备及其体外质量评价

Preparation and in vitro quality evaluation of a small type of compound rapamycin suppositories

目的:制备一种适用于大型动物腹部器官移植术后的免疫抑制药物栓剂,并对其进行质量评价。方法:以雷帕霉素(rapamycin)和他克莫司(tacrolmius)为原料药,聚乙二醇2000和聚乙二醇4000为主要基质,采用热熔法结合定量注模成型工艺制备复方栓剂,并对其外观、重量差异、融变时限、药物含量进行评价。结果:复方雷帕霉素栓剂外观呈白色半透明状,室温下硬度较好,长度短,重量差异、融变时限和药物含量均符合栓剂要求。结论:本方法制备的复方雷帕霉素栓剂质量符合栓剂要求,为该药物的新药开发奠定了基础。

Objective：To develop a small type of suppository of immunosuppressive agents to suit for large animals after abdominal organ transplantation, and carry out it’s quality evaluation. Methods：Rapamycin and ta-crolimusas were chosed as active pharmaceutical ingredients, and polyethylene glycol 2000, polyethylene glycol 4000 were used as substrate. Melting followed with a quantitative injection molding process was used to prepare the small type of compound suppository. The appearance, weight difference, melting time and drug content of the suppository were evaluated. Results：The compound rapamycin suppository was translucent, white, and had good hardness at room temperature. It’s short, and the weight variation, melting time and drug content were con-formed to the requirements of the suppository. Conclusion：The compound rapamycin suppository prepared by this method conforms to the quality of suppository, which makes a good foundation for the development of the new drug.