甲睾酮聚乳酸微球的制备及其释药性能研究

Study on preparation and in vitro drug release of Methyltestosterone Polylactic Acid Microspheres

目的制备甲睾酮聚乳酸微球,研究其体外释药过程。方法采用乳化-溶剂挥发法制备甲睾酮聚乳酸微球;以0.25%SDS-5%乙醇(pH3.4)为释放介质,采用高效液相色谱法测定甲睾酮聚乳酸微球的体外释药量。结果甲睾酮聚乳酸微球开始释药较快,存在一定突释效应,随后以缓慢的方式释药,可用双相动力学方程100-R=35.77e0.1321t+63.91e7.372E-4t描述。结论制成的甲睾酮聚乳酸微球具有明显的缓释作用。

Objective To preparation methyltestosterone polylactic acid microspheres and study the release of drug in vitro.Methods Methyltestosterone polylactic acid microspheres were prepared using dispersion-solvent diffusion method,and the in vitro drug release was determined by HPLC 0.25%SDS-0.5%CH3CH2OH（pH 3.4） as mobile phase.Results The release of methyltestosterone polylactic acid microspheres shows a burst effect,which release quickly at first,then at a lowed speed.Its release action can be described by biphase dynamic equation 100-R=35.77e0.1321t ＋63.91e7.372E-4 t.Conclusion Methyltestosterone polylactic acid microspheres showed significant extend-release effect.