溶剂系统对18-甲基炔诺酮渗透皮肤的影响

本文对乙醇、水、油酸等溶剂系统对左旋18-甲基炔诺酮(简称LNG)及消旋18-甲基炔酮(简称NG)渗透皮肤的影响进行了研究。实验采用Vaila-Chien双室扩散池及成人离体皮肤。结果表明,在80%乙醇水溶液中,LNG与NG的皮肤渗透速率比用生理盐水提高5～6倍,其中NG的皮肤渗透速率比LNG高1～2倍.含水乙醇与油酸复合使用时,对LNG通透皮肤具有明显的协同促进作用。当油酸—80%乙醇(0.75:9.25v/v)作为复合溶剂时。所获得的LNG皮肤渗透速率为0.53μg/cm²·h,分别比油酸或80%乙醇单独使用时提高29倍和3倍。提示正确地采用复合溶剂系统,能有效地提高LNG或NG透皮速率。

INFLUENCE OF VEHICLES ON HUMAN SKIN PERMEATION OF NORGESTREL AND LEVONORGESTREL IN VITRO

In the experiment Valia-Chien skin permeation cell and methods were constructed for investigating the influence of various vehicles on the transdermal absorption of norgestrel (NG) and levonorgestrel (LNG). All of the vehicles were saturated with NG or LNG at 37 degrees C, so variations in permeation were mainly attributable to the vehicle effects. The results showed that the transdermal fluxes of NG and LNG were increased about 5-6 fold using an optimal concentration range of aqueous ethanol as a vehicle relative to that when normal saline was used as a vehicle. The NG permeation rate was about 1-2 fold greater than that of LNG in the above--mentioned saline aqueous ethanol and neat ethanol. Oleic acid (OA) and aqueous ethanol both enhanced synergistically the permeation of LNG through the human cadaver skin. When OA--80% ethanol (0.75:9.25 v/v) was used as a co--vehicle, the flux of LNG was 0.53 micrograms/cm2.h, which was 3 fold and 29 fold respectively greater than that when 80% ethanol and neat OA were used as the vehicle.