雷公藤微乳凝胶中雷公藤甲素的药代动力学

[Pharmacokinetics of triptolide in Triptergium wilfordii microemulsion gel].

作者信息

Guan Yongmei, Yan Zhihong, Chen Lihua, Zhu Weifeng, Yang Ming

机构信息

Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2011 Jan;36(2):216-9.

PMID:21506426

Abstract

OBJECTIVE

To establish a method of determinating the plasma concentration about the triptolide in rat in vivo. And to study the pharmacokinetics of triptolide in transdermal drug delivery system of Triptergium wilfordii microemulsion gel.

METHOD

The T. wilfordii tablet was regarded as the control, the plasma concentration of triptolide was determined by LC-MS/MS after different route of administration, and the pharmacokinetic parameters were calculated by DAS.

RESULT

The linear relation of triptolide was excellent within the range of 1-200 ng (r = 0.9967). The minimum detectable concentration were 0.5 microg x L(-1). It was the first-order process. And the pharmacokinetic parameters of triptolide in microemulsion gel was as follow: t(1/2) (2.4 +/- 3.00) h,tmax (6.7 +/- 1.63) h, Cmax (82.9 +/- 17.63) microg x L(-1). To compare the tablets, the microemulsion gel has a longer peak time, and maintain a longer stable plasma concentration. The AUC of tablets and microemulsion gel were (2595.3 +/- 551.15) h x microg x L(-1) and (209.9 +/- 25.34) h x microg x L(-1) and it was a significant differences between the tablet and microemulsion gel (P < 0. 01).

CONCLUSION

T. wilfordii has rapid absorption in rat in vivo and a stable and persistent plasma concentration after transdermal drug delivery. Therefore, it is rationality after transdermal drug delivery.

摘要

目的

建立大鼠体内雷公藤甲素血药浓度的测定方法。并研究雷公藤甲素在雷公藤微乳凝胶经皮给药系统中的药代动力学。

方法

以雷公藤片为对照，采用液相色谱-串联质谱法（LC-MS/MS）测定不同给药途径后雷公藤甲素的血药浓度，并用DAS计算药代动力学参数。

结果

雷公藤甲素在1-200 ng范围内线性关系良好（r = 0.9967）。最低检测浓度为0.5 μg·L⁻¹。呈一级过程。雷公藤甲素微乳凝胶的药代动力学参数如下：t(1/2)为(2.4±3.00) h，tmax为(6.7±1.63) h，Cmax为(82.9±17.63) μg·L⁻¹。与片剂相比，微乳凝胶的达峰时间更长，血药浓度维持稳定的时间更长。片剂和微乳凝胶的AUC分别为(2595.3±551.15) h·μg·L⁻¹和(209.9±25.34) h·μg·L⁻¹，片剂与微乳凝胶之间有显著差异（P < 0.01）。