含炔诺酮的乳酸-乙醇酸共聚物微球的制备及其体外溶出实验

Preparation and evaluation of norethisterone/poly (D, L-lactide-coglycolide) microsphers in vitro and in vivo

本实验用溶剂挥发法制备了生物可降解的含20%炔诺酮的乳酸—乙醇酸共聚物[PLGA(9:1)] 微球,探讨总结了影响微球大小的各种因素及最佳制备条件。微球经10kGy的γ射线辐照后, 灭菌效果良好,且对微球内炔诺酮含量及体外溶出速率无影响。体外溶出试验表明药物微球化后,溶出时间明显延长。同时,体内实验也证明了微球能显著延长大鼠动情周期抑制时间。

We prepared PLGA (9:1) microspherescontaining 20% norethisterone under possibleoptimum conditions. The prepared microspheresshowed a slow and steady release pattern up tomore than 96 hours in 27.5% (w/w) ethanol so-lution. In vivo performance of the microspheresindicated that a single intramuscular injection of80mg microspheres can significantly prolong theduration of estrus suppression up to 45 days inrats.