不同剂量天麻提取物中天麻素在大鼠体内的药动学研究

目的：研究天麻提取物中天麻素在大鼠体内药代动力学。方法：采用灌胃方式给予大鼠低、中、高剂量天麻提取物（剂量分别相当于天麻素单体50~100、200mg.kg-1）,于不同时间点采集大鼠血浆,样品经甲醇-乙腈沉淀蛋白后,HPLC法测定不同时间点大鼠血浆中天麻素的含量。各给药组天麻素平均血药浓度-时间数据用WinNonlin 5.2.1药动学软件进行动力学分析,组间药动学参数用SPSS sta-tistics 17.0软件进行统计分析。结果：低、中剂量组天麻素的T1/2、CL/F、MRT0-10h无显著性差异,AUC0-10h随给药剂量增加线性增大;高剂量组与中剂量组相比,T1/2显著变小,MRT0-10h显著变大。结论：天麻提取物中天麻素给药剂量在50~100mg.kg-1时,在大鼠体内符合一级吸收线性动力学过程,而剂量在200mg.kg-1以上则表现出非线性动力学特征。

Study on Pharmacokinetics of Gastrodin after Tianma Extract in Rats

Objective： To study on the pharmacokinetics of gastrodin after Tianma extract（equivalent to gastrodin 50,100,200mg·kg-1） in rats.Methods： HPLC was used to determine gastrodin plasma concentration at different times after the rats were orally administered three dosage levels of Tianma extract.The mean plasma concentration-time curves of different medication administration teams were processed by WinNonlin 5.2.1 pharmacokinetic software.The pharmacokinetic parameters of different medication administration teams were analyzed by SPSS statistics 17.0 software.Results： T1/2,CL/F,MRT0-10h was no significant difference,and AUC0-10h was linear increase between low and middle dosage group.Meanwhile,T1/2 was significantly decreased and MRT0-10h was significantly prolonged between high dosage group and middle dosage group.Conclusion： The results indicated that the in vivo kinetic process of gastrodin were fitted to first-order linear absorption un-compartment model at dosage range of 50-100mg·kg-1,and zero-order nonlinaer absorption un-compartment model at the dosage more than 200mg·kg-1.