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以生物可降解聚合物聚乳酸/羟乙酸为载体,采用改良的复乳-液中蒸发法制备缓释丙氨瑞林微球注射剂,包封率为99.5%,平均体积径为91.36μm,收率大于95%。在37°C、pH7.0的生理等渗缓冲液中,微球首日释药14.3%,后以平均2.2%/d的速度释药5周,符合零级模式(r=0.994)。大鼠皮下注射微球后,首日释药15.1%,后以平均2.3%/d的速度释药5周,体内释药与体外释放间相关性良好(r=0.979)。雌性大鼠动情周期与子宫内膜异位模型试验表明,单剂量注射微球(释药速度为100μg·kg-1·d-1)后的疗效与每天给予同等剂量的常规溶液剂无显著差异。
The biodegradable polymer polylactic acid / glycolic acid was used as carrier, and the modified double emulsion - liquid medium evaporation method was used to prepare sustained release microspheres injection. The entrapment efficiency was 99.5% and the average volume diameter was 91.36μm. Rate of more than 95%. In physiological isotonic buffer (pH7.0) at 37 ° C, the microspheres release 14.3% on the first day and then release with an average rate of 2.2% / d for 5 weeks, which is consistent with the zero order model (r = 0.994). After subcutaneous injection of microspheres into rats, 15.1% of the drug was released on the first day and then released at an average rate of 2.3% / d for 5 weeks. The correlation between in vivo release and in vitro release was good (r = 0.979). The estrous cycle and endometriosis model test in female rats showed that there was no significant difference between the single dose injection microspheres (drug release rate of 100μg · kg-1 · d-1) and the same dose of conventional solution .