Kobayashi D, Tsubuku S, Yamanaka H, Asano M, Miyajima M, Yoshida M
Department of Urology, Gunma University School of Medicine, Japan.
Drug Dev Ind Pharm. 1998 Sep;24(9):819-25. doi: 10.3109/03639049809088526.
Poly(DL-lactic acid) (PLA) microspheres containing testosterone (T) were prepared by the solvent evaporation process to evaluate their physical properties such as size distribution, shape, drug content, in vivo controlled drug release, pharmacological influences on the prostate gland in castrated rats, and histopathological findings of tissues surrounding the implants. The in vivo release of T from PLA microspheres containing 30 mg of drug obtained with chloroform was continued over a 6-week period. This effect is attributed to high dispersibility of T in the device when obtained with chloroform. Both serum drug levels and prostate gland weight recovery suggested the effects of a long-acting drug delivery system. The histopathological findings showed that the devices used were completely degraded 10 weeks after injection.
通过溶剂蒸发法制备了含睾酮（T）的聚（DL-乳酸）（PLA）微球，以评估其物理性质，如粒径分布、形状、药物含量、体内控释、对去势大鼠前列腺的药理影响以及植入物周围组织的组织病理学发现。含30mg药物并用氯仿制备的PLA微球中T的体内释放持续了6周。这种效果归因于用氯仿制备时T在装置中的高分散性。血清药物水平和前列腺重量恢复均表明了长效给药系统的作用。组织病理学发现显示，注射后10周所用装置完全降解。
