黄体酮透皮给药系统体外经皮渗透特性的研究

Studies on permeation of transdermal progesterone delivery system in vitro

目的研究黄体酮透皮给药系统的体外经皮渗透特性。方法采用聚丙烯酸酯为骨架制备黄体酮透皮贴片,以离体人皮为透皮模型,采用Valia-Chien扩散池和高效液相色谱法研究促渗剂、药物含量对黄体酮透皮给药系统经皮渗透的影响。结果23%单月桂酸甘油酯与15%棕榈酸乙酯合用对黄体酮促渗效果明显,经皮渗透速率为1.50±0.64μg·cm-2·h-1,增渗倍数达到了21.4倍。贴片中黄体酮含量由0.75mg·cm-2提高到1.0mg·cm-2时,经皮渗透速率明显增大;含量提高到1.25mg·cm-2时,经皮渗透速率无明显变化。结论单月桂酸甘油酯和棕榈酸乙酯联用对黄体酮透皮给药系统体外经皮渗透具有显著的促进作用,黄体酮的最佳含量是1.0mg·cm-2。

AIM： To study the permeation of transdermal progesterone delivery, system in vitro. METHODS： The polyacrylic matrix-type transdermal patch of progesterone was prepared. The effect of penetration enhancers and drug content of the patch on the in vitro permeability of progesterone through human skin was examined using Valia-Chien diffusion cell and high performance liquid chromatography. RESULTS： The patch consisting of 23% monolaurin and 15% ethyl palmitate showed the optimal permeation, mean permeation rate being 1.50±0.64 μg·cm^-2·h^-1 with 21.4-fold enhancement, and permeation rate increased significantly with the increase of progesterone content from 0.75 to 1.0 mg·cm^-2, and did not increase further with the increase of content from 1.0 to 1.25 mg·cm^-2 . CONCLUSION： Combination of monolaurin and ethyl palmitate can significantly increase the percutaneous absorptionof transdermal progesterone delivery system, whose optimal contents of progesterone was 1.0 mg·cm^-2.