摘要
目的:建立雷公藤甲素在大鼠体内血药浓度的测定方法,研究雷公藤微乳凝胶经皮给药系统中雷公藤甲素的药代动力学过程。方法:以雷公藤片剂为对照,采用LC-MS-MS测定不同给药途径给药后,雷公藤甲素的血药浓度,采用药动学软件DAS处理得药动学参数。结果:雷公藤甲素在1～200 ng呈良好的线性关系(r=0.996 7),最低检测限为0.5μg.L-1,该雷公藤甲素属一级动力学过程,雷公藤微乳凝胶中雷公藤甲素的主要药动学参数为:t1/2为(2.4±3.00)h,tmax(6.7±1.63)h,Cmax(82.9±17.63)μg.L-1,与片剂比较,微乳凝胶达峰时间较长,但可维持较长时间平稳的血药浓度;微乳凝胶和片剂的AUC0-t分别为(2 595.3±551.15),(209.9±25.34)h.μg.L-1,二者有极显著差异(P<0.01)。结论:雷公藤经皮给药后,能在大鼠体内快速吸收,血药浓度平稳持久,雷公藤经皮给药具有合理性。
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. 996 7）. The minimum detectable concentration were 0. 5μg·L^-1. It was the first-order process. And the pharmacokinetic parameters of triptolide in microemulsion gel was as follow ： t1/2 （2. 4 ±3.00） h, tmax （ 6. 7 ± 1.63） h, Cmax （82. 9 ±17.63） μg·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 （2 595. 3 ±551.15） h·μg·L^-1 and （209. 9 ±25. 34） h·μg·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.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2011年第2期216-219,共4页
China Journal of Chinese Materia Medica
基金
国家"重大新药创制项目"科技重大专项(2008ZX09310-005)
江西省教育厅科学技术研究平台建设项目(赣教技字[2005]02)
2008年江西省卫生厅课题(2008A067)
