论文部分内容阅读
目的:对西罗莫司(SRL)滴丸在大鼠体内的生物利用度进行研究。方法:以PEG6000为基质,采用溶剂-熔融法制备SRL滴丸;以SRL市售片为参比制剂,以大鼠为实验动物,对SRL滴丸的生物利用度进行考察,得到药物动力学参数,并进行生物等效性考察。结果:大鼠体内SRL滴丸与市售片的达峰时间一致,tmax均为1 h,两者的峰浓度Cmax差异无统计学意义(P>0.05),而SRL滴丸的AUC0-24显著增加(P<0.05),相对生物利用度为121.98%。结论:SRL滴丸可提高SRL的生物利用度,值得进一步研发。
Objective: To study the bioavailability of sirolimus drops in rats. Methods: The SRL dropping pills were prepared by solvent-melt method using PEG6000 as substrate, the commercially available tablets of SRL as the reference preparation and the rats as experimental animals. The bioavailability of SRL dropping pills was investigated to get the pharmacokinetic parameters , And conduct a bioequivalence study. Results: The SRL peak in rats was consistent with the peak time of commercially available tablets, with a peak tmax of 1 h. There was no significant difference in Cmax between the two groups (P> 0.05), while AUC0-24 of SRL dropping pills was significantly (P <0.05), the relative bioavailability was 121.98%. Conclusion: SRL dropping pills can improve the bioavailability of SRL, it is worth further research and development.