注射用长效避孕给药系统研究进展

Research progress of injectable long-acting drug delivery systems for contraception

注射用长效避孕给药系统可维持避孕药恒定的血药浓度,精准控制药物持续释放几周甚至数月,从而大幅度减少给药次数,能较好解决目前临床上其他避孕制剂的续用率和依从性问题,为育龄女性提供一种相对安全、高效和简便的避孕方式。但目前相关上市产品有限,有待进一步开发新产品以满足各种避孕需求。按不同给药系统,长效避孕注射剂可分为油溶液、微晶混悬剂、微球和原位凝胶4类。经系统的文献调研,本文对各给药系统在避孕方面的研究进展作一综述,包括它们在研发阶段和临床应用中的特点,并总结归纳出开发长效避孕注射剂所面临的挑战。

Injectable long-acting drug delivery systems（ DDS） for contraception can achieve several advantages：（ 1） to maintain a constant drug concentration in the blood circulation;（ 2） to provide an opportunity to control a precise drug release rate for several weeks or even months;（ 3） to improve patient compliance and continuation rate than other currently used contraceptive agents by decreasing invasive administration and dosing frequencies; and（ 4） to provide a relatively safe,efficient and simple contraception method for women of childbearing age. However,currently available products are limited and need to be further developed to meet different requirements. According to the DDS,long-acting contraceptives for injection can be divided into four types,namely oil solution,microcrystalline suspension,microspheres and in situ gels. This article aimed at helping to understand the current progress by reviewing useful data and information,including the key points of technology and applications in the clinical and development phases. Finally,we listed the main challenges of developing the injectable long-acting DDS.