麻黄透皮贴剂在豚鼠体内的药物动力学

Pharmacokinetics of ephedrine gels and extractum ephedrae gels in guinea pig

目的:建立麻黄碱在豚鼠体内的血药浓度的测定方法,研究其药代动力学过程。方法:敷贴麻黄碱和麻黄提取物贴剂后,用高效液相色谱法,测定豚鼠体内麻黄碱的血药浓度,用药动学软件拟合处理得药动学参数。结果:麻黄碱在0.5-2μg范围内呈良好的线性关系(r=0.998 0),最低检测浓度为0.02μg/mL,该麻黄碱透皮吸收属一级动力学过程。麻黄碱和麻黄提取物的主要药动学参数为:t1/2kawere 1.362 1 and 1.541 8 h,t1/2kewere 2.627 4 and 3.262 2 h,Tm axwere3.124 3 and 3.440 9 h,Cm ax were 0.115 6 and 0.081 0μg/mL,AUC were 0.081 0 and 0.741 5μg.h/mL。结论:麻黄碱在豚鼠体内快速吸收,血药浓度平稳持久,麻黄作为透皮贴剂的具有合理性。

AIM： To establish a method to determine the serum concentration of ephedrine, and to study its pharmacokinefics in guinea pig. METHODS： The serum concentration of ephedrine gels transdermal administration in guinea pig were determined by HPLC and pharmacokinetic parameters were calculated by computer. RESULTS ： The calibration curve was linear in the range of 0.5 - 2 μg with r = 0. 998 0. The limit of identification was 0.02 μg/mL. The pharmacokinetics behavior of ephedrine showed one order absorption. The main parameters after adminstrition of ephedrine gels and extractum ephedrae gels were as follows：t1/2ka were 1. 362 1 and 1. 541 8, t1/2ke were 2. 627 4 and 3. 262 2 h,Tmax= were 3. 124 3 and 3. 440 9 h,Cmax= were 0. 115 6 and 0.081 0 μg/mL,AUC were 0.081 0 and 0. 741 5 μg ·h/mL. CONCLUSION： Ephedrine shows a fast rate of absorption in guinea pig, serum concentration of ephedrine is stable and lasting potency, and indicates the reason of transdennal administration of Herba Ephedrae preparation.