不同透皮促进剂及基质对黄体酮透皮作用的影响

The influence of different transcutaneous enhancers and bases on progesterone transcutaneous permeation

目的 :观察促进剂及基质对黄体酮凝胶体外透皮作用的影响。方法 :采用改良的Franz扩散池 ,以离体大鼠皮肤为透皮屏障 ,用高效液相色谱法测定不同种类和浓度的促进剂及不同基质的黄体酮凝胶的体外接受液的含量 ,进而计算其累积透皮量和稳态透皮速率。结果 :3种基质中以Carbopol+PVP作为基质的渗透作用为好 ,几种促进剂的促进作用大小顺序为 :丙二醇 (PG) +月桂氮芏卓 酮 (Azone) >月桂氮芏卓 酮 >丙二醇 +油酸 (OA) >丙二醇。Azone的理想浓度约为 1%。结论 :以 3%(Carbopol+PVP)为凝胶基质 ,1%Azone +10 %PG为促进剂时黄体酮的稳态透皮速率最快。

OBJECTIVE:To investigate the effects of transdermal enhancers and gel bases on transcutaneous permeation of progesterone.METHODS:Using improved Franz type diffusion cell and excised mouse skin in vitro as transdermal barrier,the concentration of permeation solution of progesterone was determined by HPLC in different kind and concentration enhancers and different gel bases,then cumulative permeation quantity(Q) and stability rate(J) of progesterone were calculated.RESULTS:The permeation effect of carbopol+PVP as gel base was better than others.The effects of mixed enhancers on mouse skin penetration were as follows:PG+Azone>Azone>PG+OA>PG,1% of Azone do great actor on permeability.CONCLUSIONS:The steady rate of progesterone from formulation which made of 3% (Carbopol+PVP) and 1% Azone+10% PG is larger than others. [