Transdermal Levonorgestrel for Emergency Contraception

描述（从申请人的描述扫描）：该计划旨在 开发一种能够输送1，500 ug左炔诺孕酮的透皮系统 在24小时的过程中通过两个30 cm 2的贴片。这样的制度应该是 与目前批准的口服方法一样有效的紧急避孕， 同时提供更大的便利性和更少的副作用。虽然 像左炔诺孕酮这样不溶性的药物所需的透皮剂量很高， BIOTEK过去的经验表明，这是可以实现的。第一阶段开始 通过对人体皮肤的体外研究， 左炔诺孕酮通量，继续进行刺激性和生物利用度研究 在家兔中进行，并以评价用于 能够在大面积上保持良好皮肤接触的舒适贴片。 这些任务已圆满完成。第二阶段的工作将 完成贴剂设计工作，制备和表征GMP贴剂，提交 IND，并以10例受试者的人体临床剂量范围研究结束， 安全性、卵泡反应和左炔诺孕酮的药代动力学 东弗吉尼亚医学院研究所 拟议商业应用：不可用

DESCRIPTION (Scanned from the applicant's description): This program seeks to develop a transdermal system capable of delivering 1,500 ug of levonorgestrel over the course of 24 hours through two 30 cm2 patches. Such a system should be as effective for emergency contraception as the currently approved oral method, while offering greater convenience and fewer side effects. Although the required transdermal dose is high for a drug as insoluble as levonorgestrel, BIOTEK's past experience suggested that it could be achieved. Phase I began with an in vitro study on human skin to confirm and optimize high levonorgestrel fluxes, continued with a study of irritation and bioavailability in rabbits, and concluded with an evaluation of materials for use in comfortable patches capable of maintaining good skin contact over a large area. These tasks were successfully completed. The Phase II work proposed here will complete patch design work, prepare and characterize GMP patches, submit an IND, and conclude with a 10-subject human clinical dose ranging study of safety, follicular response, and levonorgestrel pharmacokinetics at the Jones Institute of the Eastern Virginia Medical School. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE