复方18甲基炔诺酮透皮控释传递系统的LNG人体药物动力学与药效学评价

Pharmacokinetic and Pharmacodynamic Evaluation of Compound Levonorgestrel Transdermal Controlled Delivery System in Human.

复方18甲基炔诺酮/雌二醇透皮控释传递系统(LNG/E_2 TCDS)能同时恒速释放低剂量的LNG和E_2,在1周内维持一个平稳而有效的LNG血药浓度。药动学与药效学研究证明,该系统释放的LNG能达到血清LNG目标水平,产生有效的排卵抑制(6/6)。LNG/E_2 TCDS可望发展成为一种安全、有效、非侵入性的新型生育调节避孕制剂。

A weekly transdermal controlled delivery system (TCDS) which can simultaneously deliver a low dose combination of levonorgestrel (LNG) /estradiol (E2) and maintain a relatively constant and effective serum LNG level was developed. Results of pharmacokinetic and pharmacodynamic analyses demonstrated that it is capable of reaching the target serum level of LNG and achieving high percentage of ovulaton inhibition by weekly application of LNG/E2 TCDS. The present study suggests that the developed LNG/E3 TCDS might be an effective, safe and noninvasive contraceptive for female fertility regulation.