Transdermal Levonorgestrel for Emergency Contraception

描述(从申请者的描述中扫描)：该计划寻求 开发一种能释放1500微克左旋诺孕酮的透皮系统 在24小时内通过两块30平方厘米的贴片。这样的制度应该是 对于紧急避孕，与目前批准的口服方法一样有效， 同时提供更大的便利和更少的副作用。尽管 对于像左旋诺孕酮这样的不溶性药物，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 用人体皮肤的体外研究证实和优化HIGH 左炔诺孕酮的释放量，继续刺激性和生物利用度的研究 在兔身上，并以用于治疗的材料的评估结束 舒适的贴片能够在大范围内保持良好的皮肤接触。 这些任务圆满完成。这里提出的第二阶段工作将 完成补丁设计工作，准备和表征GMP补丁，提交 IND，并以10个受试者的人体临床剂量范围研究结束。 琼斯医院的安全性、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。 建议的商业应用：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