CAJ | 학술논문

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。
목적：：대서라막사( SRL)적환재대서체내적생물이용도진행연구。방법：이PEG6000위기질,채용용제-용융법제비SRL적환；이SRL시수편위삼비제제,이대서위실험동물,대SRL적환적생물이용도진행고찰,득도약물동역학삼수,병진행생물등효성고찰。결과：대서체내SRL적환여시수편적체봉시간일치,tmax균위1 h,량자적봉농도Cmax차이무통계학의의( P>0.05),이SRL적환적AUC0-24현저증가(P<0.05),상대생물이용도위121.98%。결론： SRL적환가제고SRL적생물이용도,치득진일보연발。
Objective:To study the relative bioavailability of sirolimus ( SRL) dropping pills in rats. Methods:PEG6000 as the base, SRL dropping pills were prepared using solvent-melting method. The SRL marketed tablets as the reference preparation and rats as the animals, the relative bioavailability of SRL dropping pills was studied to obtain the pharmaceutical parameters and bioequiavail-ability. Results:Compared with that of the reference preparation, tmax of SRL dropping pills was the same (1 h). There was no signifi-cant difference in Cmax between the dropping pills and the tablets (P>0. 05). AUC0-24 of the dropping pills was notably higher than that of the marketed tablets (P<0. 05) with the bioequiavailability of 121. 98%. Conclusion:SRL dropping pills with promising bioavail-ability are valuable to be studied further.