用于左炔诺孕酮肠胃外给药的长效注射用微球制剂。

Long-acting injectable microsphere formulation for the parenteral administration of levonorgestrel.

作者信息

Beck L R, Pope V Z, Tice T R, Gilley R M

出版信息

Adv Contracept. 1985 Jun;1(2):119-29. doi: 10.1007/BF01849793.

Abstract

The pharmacokinetic and pharmacodynamic effects of a long-acting formulation of levonorgestrel microencapsulated in a biodegradable polymer poly(DL-lactide-CO-glycolide) was tested in baboons. The polymer microspheres provided continuous release of levonorgestrel for up to 6 months following a single intramuscular injection. The treatment inhibits ovarian function for 3-6 months, depending on the dose. The duration and pattern of levonorgestrel release varies according to the quality and size of the microspheres. The microsphere delivery system offers a promising new approach to developing a long-acting injectable contraceptive based on levonorgestrel.

摘要

对包裹在可生物降解聚合物聚（DL-丙交酯-乙交酯）中的左炔诺孕酮长效制剂的药代动力学和药效学作用在狒狒身上进行了测试。单次肌肉注射后，聚合物微球可使左炔诺孕酮持续释放长达6个月。根据剂量不同，该治疗可抑制卵巢功能3至6个月。左炔诺孕酮的释放持续时间和模式因微球的质量和大小而异。微球给药系统为开发基于左炔诺孕酮的长效注射用避孕药提供了一种有前景的新方法。