槐定碱在小鼠体内药物代谢动力学的研究

Pharmacokinetics of sophoridine in mice

目的研究槐定碱在小鼠体内的药物代谢动力学。方法小鼠采用等剂量（2 mg·kg^-1）静脉、灌胃给药后采用LC-MS/MS法测定不同时间的血药浓度。结果灌胃给药后槐定碱的AUC0~18 h、Cmax、tmax分别为1 256.2 ng·h·mL^-1、756.3 ng·mL^-1、1 h,绝对生物利用度为41.8%;静脉给药后槐定碱的AUC0-18 h为3 005.3 ng·h·mL^-1。结论槐定碱在小鼠体内的药动学行为均符合二室模型,小鼠灌胃给药后绝对生物利用度低。

Objective To study the pharmacokinetics of sophoridine in mice. Methods Two groups of mice were treated with sophoridine at the same dose 2 mg ·kg^-1 through iv and ig, respectively. The concentration of sopho- ridine at different time was determined by LC-MS/MS. Results The pharmacokinetic parameters AUC0-18 h, Cmax, and tmax of the ig administration group were 1 256.2 ng·h·mL^-1,756.3 ng·mL^-1 and 1 h, with absolute bioavail- ability at 41.8%; while the AUC0-18h was 3 005.3 ng ·h·mL^-1 in the iv administration group. Conclusion The pharmacokinetic of sophoridine in mice can be described with two compartment model and its absolute bioavailability is considerably low when administrated intragastricaly.