Transdermal microemulsion drug delivery system for impairing male reproductive toxicity and enhancing efficacy of Tripterygium Wilfordii Hook f

Transdermal microemulsion drug delivery system for impairing male reproductive toxicity and enhancing efficacy of Tripterygium Wilfordii Hook f
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雷公藤减雄性生殖毒性增强药效的透皮微乳给药系统

DOI:
10.1016/j.fitote.2012.02.006
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发表时间:
2012-06-01
期刊:
影响因子:
3.4
通讯作者:
Sha, Xianyi
Sha, Xianyi
中科院分区:
医学3区
文献类型:
--
作者:
Wang, Xiao;Xue, Mei;Sha, Xianyi

文献摘要

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本研究旨在制备雷公藤微乳透皮给药系统。并试图解决雷公藤多甙的雄性生殖毒性问题。采用响应面中心组合设计法对处方进行优化,确定最佳处方为油酸12%,Labrasol S 19.7%。19.7%乙醇、19.7% Pharmasolve和29%水。雷公藤多甙经皮给药的透皮能力强于游离雷公藤多甙,雷公藤多甙微乳对抗炎性关节炎有明显的抑制作用,且长期给药具有较好的抗炎作用。各项药效学参数证明TWHF微乳可以降低大鼠雄性生殖毒性和肝脏毒性。提示TMDDS是一种较理想的雷公藤多甙缓释系统。(C)2012爱思唯尔有限公司版权所有。
The present study is trying to produce a transdermal microemulsion drug delivery system (TMDDS) for Tripterygium Wilfordii Hook f. (TWHF) and attempting to solve male reproductive toxicity problem of TWHF. The formulation was optimized by the central composite design with response surface methodology and was decided as 12% oleic acid, 19.7% Labrasol S. 19.7% ethanol and 19.7% Pharmasolve, and 29% water. TMDDS for TWHF had stronger transdermal ability than free TWHF, and TWHF microemulsion significantly inhibited the adjuvant-induced arthritis and at the same time, had preferable anti-inflammatory effect with the long-time administration. Various pharmacodynamics parameters proved that TWHF microemulsion can reduce the male reproductive toxicity and hepatotoxicity of rats. All these suggested that TMDDS could be a suitable delivery system for TWHF. (C) 2012 Elsevier B.V. All rights reserved.