孕二烯酮硅橡胶皮下埋植剂的长期体外释放研究

In vitro long-term drug release evaluation of gestodene silicone rubber implant

目的对孕二烯酮硅橡胶皮下埋植剂进行长期体外释放考察,研究其初期药物爆破效应和药物释放的影响因素。方法自制不同规格的孕二烯酮硅橡胶皮下埋植剂,采用蒸馏水为释放介质,考察防爆破处理和规格对药物释放的影响。结果孕二烯酮硅橡胶皮下埋植剂在为期2年的体外释放实验中释放速度恒定,符合零级释放方程,其表面释放面积越大,孕二烯酮释放速度越快,防爆破处理可有效降低药物的突释。结论孕二烯酮硅橡胶皮下埋植剂具有广阔的应用前景,为广大育龄妇女提供了一种更理想的避孕措施。

Objective To evaluate the release quantity in vitro and investigate the factors influencing drug burst-release effect and release pharmaeokinetics. Methods The stick implant of gestodene silicone rubber with different size were prepared and influence of size and pretreatment on drug release were investigated. Results Gestodene silicone rubber implant main- tained a steady release rate in two years; in vitro drug release was fitted well with zero-order release equation;the release rate accelerated as surface area of implants increased and the implants with pretreated showed a lower drug burst-release. Conclusion Gestodene silicone rubber implant is a safe and reliable method of birth-control and has important application prospects.