摘要
二种组成比不同的丙交酯—乙交酯共聚物以溶剂挥发法制成含炔诺酮的微球。通过体外释药、大鼠注射部位药物残留量的测定及大鼠动情周期抑制试验。证明药物用共聚物PLGA制成微球,能延缓炔诺酮的释放。体内实验显示微球能显著延长大鼠动情周期抑制的时间。且随着共聚物中GA比例的增加,炔诺酮的释药速率加快。
The different lactide-co-glycolide ratio of the PLGA microspheres containing NET was prepared by a solvent-evaporation process.The NET release from microspheres in vitro and the NET remaining in the site of injection after administration of microspheres were measured.Results indicated that the microencapsulation of NET in copolymer provided an effective method for retarding the rate of NET release.In vivo performance of the microspheres showed that the NET microspheres can significantly prolong the dureation of estrus suppression in rats. And increasing the ratio of glycolide in PLGA causes a corresponding increase of NET release rate in vitro and vivo.
关键词
微球
炔诺酮
PLGA
释药速率
microsphere
release rate
PLCA
norethisterone (NET)
