荆芥内酯在大鼠体内的药物动力学及生物利用度  

A study of pharmacokinetics and absolute bioavailability of schizonepetin in rats

作　　者：孙熠[1] 耿婷[1] 姚卫峰[1] 丁安伟[1,2] 张丽[1] 

机构地区：[1]南京中医药大学药学院 [2]江苏省方剂研究重点实验室,江苏南京210046

出　　处：《中国药理学通报》2011年第4期558-561,共4页Chinese Pharmacological Bulletin

基　　金：国家科技重大专项课题创新药物研究开发-候选药物研究(No2009ZX09103-339)

摘　　要：目的研究荆芥内酯在大鼠体内的药代动力学特征及生物利用度。方法建立大鼠血浆中荆芥内酯的HPLC检测方法,考察大鼠灌胃或尾静脉给予不同剂量荆芥内酯24 h内的血药浓度变化,并用Kinetica 4.4药动学软件计算药动学参数。结果灌胃给予高、中、低剂量(47.87、23.94、11.97 mg.kg-1)荆芥内酯后,Cmax和AUC0-∞与给药剂量呈非线性关系。静脉给予11.97 mg.kg-1荆芥内酯后,Cmax和AUC0-∞分别为6.5 mg.L-1、18 mg.h.L-1。荆芥内酯在大鼠体内的口服绝对生物利用度为69.1%。结论该方法简便、快速、专属性强,可用于荆芥内酯在大鼠体内的药代动力学和生物利用度研究。Aim To investigate the pharmacokinetic characteristics of schizonepetin and its bioavailability in rats.Methods An HPLC method was established to analyze the plasma concentration of schizonepetin with different intragastric and intravenous administration doses to rats.Pharmacokinetic parameters were calculated by noncompartmental model in Kinetica 4.4.Results The Cmax and AUC0-∞ showed non-linearrelation after intragastric administration of 47.87,23.94 and 11.97 mg·kg-1.The Cmax and AUC0-∞ after intravenous administration of 11.97 mg·kg-1 were 6.5 mg·L-1 and 18 mg·h·L-1.And the absolute bioavailability was 69.1 %.Conclusion This method for the pharmacokinetic and absolute bioavailability study of schizonepetin in rats is simple,rapid and accurate.

关 键 词：荆芥内酯 大鼠 血药浓度 药代动力学 生物利用度 HPLC 吸收 

分 类 号：R-332[医药卫生] R282.71