兰索拉唑肠溶微丸的制备及其在犬体内药动学

Study on the preparation of lansoprazole enteric-coated pellets and the pharmacokinetics of lansoprazole in dogs' plasma

目的:探讨兰索拉唑肠溶微丸的制备及其在犬体内的药动学。方法:采用液相层积法制备兰索拉唑肠溶微丸胶囊,以市售达克普隆作为参比制剂,建立适宜的分析方法,检测家犬体内血浆中药物浓度,绘制药时曲线,用3P97软件进行药动学参数的分析。结果:通过处方的筛选和工艺的优化,由最优处方在最佳工艺条件下制得的微丸圆整度好,脆碎度、含水量均合格,理论载药量为10%。兰索拉唑制成肠溶微丸胶囊后生物利用度、达峰时间及体内滞留时间与参比制剂类似,相对生物利用度102.89%。结论:本实验成功地对兰索拉唑的剂型进行了改造,且药动学研究显示它的生物利用度不亚于市售药达克普隆,其他药动学参数也较为相似。

OBJECTIVE To prepare lansoprazole enteric-coated pellets and study the pharmacokinetics of lansoprazole in dogs＇ plasma. METHODS The lansoprazole enteric-coated pellets were prepared by means of the reversed-phase HPLC meth od,with the marketed drug Takepron as the reference preparation. A suitable analysis method was established to detect the drug concentration in dogs＂ plasma in vivo and draw the drug-time curve. Pharmacokinetic parameters were calculated using the pharmacokinetie software 5P97. RESULTS The lansoprazole pellets had good appearance, friability and the water contents, which were qualified. The theoretical drug loading was 10%. The pharmacokinetic results showed that the bioavailability, tmax and MRT were similar to Takepron. Relative bioavailability was 102. 89%. CONCLUSION The present study successfully transformed the formulations of lansoprazole, and the pharmacokinetie resuhs showed that the bioavailability of the new formu lations was no less than the marketed drugs Takepron, in addition, the other pharmacokinetic parameters were also similar.