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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 for the determination of triptolide in rat plasma and to study the pharmacokinetics of triptolide in the system of transdermal administration of triptolide microemulsion. Methods: Tripterygium wilfordii tablet as a control, using LC-MS-MS determination of different routes of administration after administration of triptolide plasma concentrations, using pharmacokinetic software DAS pharmacokinetic parameters. Results: Triptolide showed a good linear relationship (r = 0.996 7) at 1 ~ 200 ng, the lowest detection limit was 0.5 μg.L-1. The triptolide was a first-order kinetic process. The main pharmacokinetic parameters of triptolide in the gel were: t1 / 2 (2.4 ± 3.00) h, tmax (6.7 ± 1.63) h, Cmax (82.9 ± 17.63) μg.L-1, , While the microemulsion gel peaked longer, but maintained a longer steady blood concentration. The AUC0-t of microemulsion gel and tablet were (2595.3 ± 551.15) and (209.9 ± 25.34) h, respectively. μg.L-1, the two have very significant difference (P <0.01). CONCLUSION: Tripterygium wilfordii can be rapidly absorbed in rats after transdermal administration, and the plasma concentration is steady and long-lasting. The transdermal administration of Tripterygium wilfordii is reasonable.