Garza-Flores J, Hall P E, Perez-Palacios G
Department of Reproductive Biology, National Institute of Nutrition S. Zubirán, Mexico City, Mexico.
J Steroid Biochem Mol Biol. 1991;40(4-6):697-704. doi: 10.1016/0960-0760(91)90293-e.
Following the development and widespread use of oral hormonal contraceptives, it became evident that alternative long-acting delivery systems would be required to improve contraceptive practice in some cultural settings where injectable or subdermal routes of administration are preferred. Nowadays, long-acting contraceptives constitute an important option in family planning services in many parts of the world. Indeed, two long-acting injectable contraceptives containing just a synthetic progestogen (depot-medroxyprogesterone acetate (DMPA) and norethisterone enantate (NET-EN)) have been in clinical practice for more than 20 years. The World Health Organization's (WHO) Special Programme of Research in Human Reproduction, in collaboration with the U.S. National Institute of Child Health and Human Development (NICHD) and universities primarily in developing countries undertook a synthesis programme aimed at producing an improved injectable preparation by developing new derivatives of known steroids. One such compound (levonorgestrel 17-butanoate) is now at the stage of Phase II clinical testing. In addition, the Special Programme has developed and improved once-a-month injectable formulations and assessed their safety and efficacy in different countries worldwide. After large scale clinical testing, at least two progestogen-estrogen combinations have reached the point of introductory trials.
随着口服激素避孕药的研发和广泛使用,显而易见,在一些更倾向于注射或皮下给药途径的文化背景下,需要其他长效给药系统来改善避孕措施。如今,长效避孕药在世界许多地区的计划生育服务中构成了一个重要选择。事实上,两种仅含合成孕激素的长效注射用避孕药(醋酸甲羟孕酮长效注射液(DMPA)和庚炔诺酮(NET-EN))已在临床应用超过20年。世界卫生组织(WHO)人类生殖特别研究计划与美国国立儿童健康与人类发展研究所(NICHD)以及主要位于发展中国家的大学合作开展了一项综合计划,旨在通过开发已知甾体的新衍生物来生产一种改进的注射制剂。一种这样的化合物(左炔诺孕酮17-丁酸酯)目前正处于II期临床试验阶段。此外,该特别计划还研发并改进了每月注射一次的制剂,并在全球不同国家评估了它们的安全性和有效性。经过大规模临床试验,至少两种孕激素-雌激素组合已进入初步试验阶段。