灌胃射干合剂后大鼠体内盐酸麻黄碱药动学研究

目的：给大鼠灌胃射干合剂后,了解射干合剂中盐酸麻黄碱在大鼠血清中药动学。方法：采用液质联用技术测定盐酸麻黄碱含量,大鼠灌胃射干合剂（1.0 ml/100 g）后,盐酸麻黄碱血浓变化,采用药动学软件计算,求出盐酸麻黄碱的药动学参数；采用代谢笼技术,计算射干合剂中盐酸麻黄碱在24h内大鼠尿液、粪便中回收率。结果：得到盐酸麻黄碱的药动学参数为Tmax：（1.30±0.23）h,T1/2：（21.17±1.35）h,Cmax：（278.86±46.41）ng·ml-1,AUC0-∞：（1221.98±412.64）ng·ml-1,Vc/F：（1.70±0.15）L；盐酸麻黄碱在24 h内可在尿中回收85.66%；粪便中未能测得盐酸麻黄碱。结论：盐酸麻黄碱在大鼠体内24 h基本排泄完；服用射干合剂不会造成体内麻黄碱的蓄积；大鼠体内盐酸麻黄碱主要经肾脏排泄。

Pharmacokinetics of Ephedrine Hydrochloride in Rats after Intragastric Administration of Shegan Mixtures

Objective： To determine the pharmacokinetics of ephedrine hydrochloride in rats after intragastric administration of Shegan mixtures. Methods：Shegan mixtures （1. 0 ml/100 g） were administered to each rat by gavage. Blood samples were collected after the administration. Plasma concentration of ephedrine hydrochloride was determined by LC-MS/MS. The pharmacokinetic parame-ters of ephedrine hydrochloride were obtained using the pharmacokinetic software. Urine and fecal samples were collected in 24 hours after the administration using metabolic cage to determine the recovery of ephedrine hydrochloride. Results： The pharmacokinetic pa-rameters of ephedrine hydrochloride were as follows：Tmax of （1. 30 ± 0. 23）h,T1/2 of （21. 17 ± 1. 35）h, Cmax of （278. 86 ± 46. 41）ng ·ml-1,AUC0-∞ of （1221.98 ±412.64）ng·ml-1 and Vc/F of （1.70 ±0.15）L. Totally 85.66% ephedrine hydrochloride could be recovered from urine in 24 hours after the administration;however, it was not detected in the fecal samples. Conclusion： Most of e-phedrine hydrochloride is excreted through kidney in 24h,therefore, Shegan mixtures can＆#39;t cause the accumulation of ephedrine hydro-chloride in rats.