Wu Linfeng, Janagam Dileep R, Mandrell Timothy D, Johnson James R, Lowe Tao L
Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, Tennessee, 38163, USA.
Pharm Res. 2015 Jul;32(7):2180-91. doi: 10.1007/s11095-015-1686-2. Epub 2015 Apr 22.
Although great efforts have been made to develop long-acting injectable hormonal contraceptives for more than four decades, few long-acting injectable contraceptives have reached the pharmaceutical market or even entered clinical trials. On the other hand, in clinical practice there is an urgent need for injectable long-acting reversible contraceptives which can provide contraceptive protection for more than 3 months after one single injection. Availability of such products will offer great flexibility to women and resolve certain continuation issues currently occurring in clinics. Herein, we reviewed the strategies exploited in the past to develop injectable hormonal contraceptive dosages including drug microcrystal suspensions, drug-loaded microsphere suspensions and in situ forming depot systems for long-term contraception and discussed the potential solutions for remaining issues met in the previous development.
尽管四十多年来人们为开发长效注射用激素避孕药付出了巨大努力，但很少有长效注射用避孕药进入药品市场，甚至进入临床试验阶段。另一方面，在临床实践中，迫切需要一种注射用长效可逆避孕药，单次注射后能提供超过3个月的避孕保护。这类产品的出现将为女性提供极大的便利，并解决目前临床上出现的某些续用问题。在此，我们回顾了过去开发注射用激素避孕制剂所采用的策略，包括药物微晶混悬液、载药微球混悬液和用于长期避孕的原位形成贮库系统，并讨论了此前开发过程中遇到的遗留问题的潜在解决方案。
