Díaz-Sánchez V, Garza-Flores J, Jimenéz-Thomas S, Rudel H W
Contraception. 1987 Jan;35(1):57-68. doi: 10.1016/0010-7824(87)90051-5.
A drug delivery system which provides a sustained release of norethindrone (NET) and mestranol (ME) for one month after a single intramuscular injection was assessed as a long-acting injectable contraceptive. The system is based upon well defined particle size crystals of the synthetic steroids maintained in suspension with saline solution. Eight healthy ovulating women volunteered for the study; they received a combination of 10 mg of NET plus 1 mg of ME in 1 ml of vehicle by intramuscular injection on day five of their menstrual cycle. Blood samples were drawn at 0, 1, 5, 10, 13, 17 and 21 days after drug administration. The immunoreactive serum levels of estradiol, progesterone, NET and ethinylestradiol were measured by specific radioimmunoassay procedures to assess ovarian function and the kinetic parameters of the synthetic steroids. This newly developed contraceptive system proved to be both effective, and long-lasting as well as devoid of side effects.
一种药物递送系统，在单次肌内注射后可提供炔诺酮（NET）和美雌醇（ME）长达一个月的缓释，该系统被评估为一种长效注射用避孕药。该系统基于合成类固醇的明确粒径晶体，与盐溶液保持悬浮状态。八名健康的排卵女性自愿参与该研究；她们在月经周期的第5天通过肌内注射接受了10毫克NET加1毫克ME与1毫升赋形剂的组合。给药后第0、1、5、10、13、17和21天采集血样。通过特定的放射免疫分析程序测量雌二醇、孕酮、NET和炔雌醇的免疫反应性血清水平，以评估卵巢功能和合成类固醇的动力学参数。这种新开发的避孕系统被证明是有效、持久且无副作用的。
