Beck L R, Cowsar D R, Lewis D H, Cosgrove R J, Riddle C T, Lowry S L, Epperly T
Fertil Steril. 1979 May;31(5):545-51. doi: 10.1016/s0015-0282(16)44002-1.
A long-acting injectable microcapsule system for the controlled-release systemic administration of progesterone (P4) is described. The system consists of microcapsules made of the biodegradable polymer, d,l-polylactic acid, which contain crystalline P4. Following injection, P4 is released from the microcapsules by diffusion and biodegradation of the polymer matrix. The rate of P4 release from the prototype microcapsule system in vivo is 1.3 microgram of P4/day/mg of microcapsules, and the duration of release is 30 days. Vaginal estrous cycles in rats and cyclic ovarian function in baboons were inhibited for 1 month following a single injection of P4 microcapsules. The effects of continuous progesterone therapy on reproductive function in both rats and baboons are dose-dependent. The utility of the system as a once-a-month injectable contraceptive is established in the baboon model.
本文描述了一种用于孕酮（P4）控释全身给药的长效注射用微胶囊系统。该系统由可生物降解聚合物d，l-聚乳酸制成的微胶囊组成，其中含有结晶P4。注射后，P4通过聚合物基质的扩散和生物降解从微胶囊中释放出来。原型微胶囊系统中P4在体内的释放速率为1.3微克P4/天/毫克微胶囊，释放持续时间为30天。单次注射P4微胶囊后，大鼠的阴道发情周期和狒狒的周期性卵巢功能被抑制1个月。持续孕酮治疗对大鼠和狒狒生殖功能的影响是剂量依赖性的。该系统作为每月一次的注射用避孕药在狒狒模型中得到了验证。
