BIODEGRADABLE, CONTROLLED RELEASE OF MODERN PROGESTINS

尽管有几种新批准的孕激素， 可以作为现代低剂量口服避孕药（OC）取得成功， 业主立案法团的问题仍然存在。 取得成功的一个考虑因素 这些现代孕激素增加了剂型的适口性。 为了解决这个问题，我们的团队和其他人已经调查了很长一段时间， 避孕药从可植入剂型的长期递送。 我们 以前发现，单剂量的左炔诺孕酮，在一个小的， 聚乳酸-羟基乙酸共聚物的圆柱形植入物能够 释放治疗活性水平的左炔诺孕酮 长达两年（使用大鼠体内测量）。两个因素 我赞成这项工作的继续：（l）FDA批准一种新的口服 基于现代一代孕激素的避孕制剂， 衍生自左炔诺孕酮，其允许比以前更低的剂量 OC的，以及（2）我们开发的专有PLGA技术， 有助于FDA批准、制剂制造和样品完整性。 基于这两个领域的进展，即，药物和 配方技术，该项目将耦合这些利益与 开发可接受的长效生育调节剂量的目标 form.

In spite of the availability of several newly approved progestins, which could achieve success as modern low-dose oral contraceptives (OC), problems in OC use remain. One consideration in achieving success of these modern progestins is increasing the palatability of the dose form. In order to address this, our team and others have investigated the long term delivery of the contraceptive from an implantable dose form. We previously found that a single dose of levonorgestrel, given in a small cylindrical implant of a poly(lactic-co-glycolic) acid polymer was able to release therapeutically active levels of levonorgestrel for periods of up to two years (as measured in vivo using rats). Two factors now favor the continuation of this work: (l) the FDA approval of a new oral contraceptive formulation based on a modern generation of progestins, derived from levonorgestrel, which allow even lower doses than previous OC's, and (2) our development of a proprietary PLGA technology which facilitates FDA approval, formulation manufacture, and sample integrity. Based on the advances in these two areas, i.e., the drug and the formulation technology, this project will couple these interests with the goal of developing an acceptable, long-acting fertility regulation dose form.