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目的:制备孕二烯酮与炔雌醇复方的双层避孕贴剂,并考察其体外的特性和体内的避孕效果.方法:采用迭层浇注技术实现药物7日内的恒速释放,利用偏振光显微镜观察药物的分布,并进行含量均匀度、黏性、刺激性、释放以及经皮渗透实验评价制剂的体外特性,通过抗着床以及抗生育实验考察其避孕效果.结果:药物的体外释放符合Higuchi方程;孕二烯酮的每日渗透量约为7.5 μg/cm2,炔雌醇约为3.0 μg/cm2,且两者的体外经皮渗透呈现零级过程,渗透速率分别达到0.377 μg/(cm2·h)和0.092 μg/(cm2·h);经皮给药组的胚胎数为零,其子宫系数与空白对照组相比明显减小(P<0.01).结论:当释放层与贮库层的药物比例为1:4时,双层的经皮给药系统可以维持药物的7 d平稳释放,体内评价证明其避孕效果良好.所制备的贴剂有望成为新型的非口服避孕制剂.“,”Aim: To prepare a novel contraceptive patch containing gestodene(GEST) and ethinylestradiol(EE), and to study the in vitro characterization and in vivo contraceptive effect. Methods: Double-layer technique was applied to sustain steady 7-day permeation flux of drugs. Polariscope examination was carried out to observe the drug distribution behavior in the patch. Uniformity, adhesion, skin irritation, release and permeation tests were conducted to evaluate in vitro characterization. Anti-implantation and anti-fertility experiments were carried out to investigate its contraceptive effect. Results: The in vitro release profiles of both drugs were in accordance with Higuchi equation. The daily permeated amount of GEST per 10 cm2 patch was about 75 μg while the amount of EE was 30 μg.The in vitro transdermal permeation of both drugs from the patches displayed a zero-order process. Permeation rate constants were 0. 377 μg/(cm2·h) for GEST, and 0. 092 μg/(cm2· h) for EE, respec-tively. After transdermal administration, the embryonic number of the test groups was zero, and the uterus coefficients of those groups were significantly reduced compared with those of the control group (P < 0. 01). Conclusion: Double-layer transdermal drug delivery system(TDDS) could allow the steady 7-day permeation flux of drugs when the drug ratio between the immediate-release layer and the reservoir layer was 1:4. In vivo charac-terization demonstrated its contraceptive effects. The prepared novel patch might be a promising non-oral contra-ceptive preparation.