复方左炔诺孕酮/雌二醇透皮吸收贴片的研制

Study on Transdermal Compound Levonorgestrel and Estradiol Patch

目的考察研制的复方左炔诺孕酮/雌二醇(LNG/E2)透皮吸收贴片的渗透性。方法采用Valia-Chien双室渗透池进行体外经皮渗透实验,以HPLC测定药物浓度求算168h内的渗透量。结果8%月月月月酮、30%丙二醇、4%聚乙二醇400为混合促进剂,LNG和E2的含量分别为4mg·20cm-2,2.5mg·20cm-2时,研制的LNG/E2透皮贴片能使LNG和E2分别以65和43μg·d-1的速率透过人离体皮肤,黏着性较好。结论LNG和E2的体外人体皮肤渗透率可达避孕贴片设计要求。

OBJECTIVE To investigate the permeation of transdermal compound levonorgestrel （LNG） and estradiol （E2） patch. METHODS Transdermal permeability of LNG and E2 were carried out by using Valia-Chien double-compartment permeation cell and the permeation amounts of LNG and E2 within 168 h in vitro were examined by HPLC. RESULTS The LNG and E2 permeated through the human skin with different rates at 65 and 43 μg·d^-1 respectively while the enhancers were composed of 8% azone, 30% propylene glycol and 4% polyethylene glycol and the contents of LNG and E2 in patch were 4 and 2.5 mg.20 cm^-2 respectively. The adhesiveness of patch was good. CONCLUSION The human skin permeation rates of LNG and E2 can meet the requirement of contraception.