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左旋18-甲基炔诺酮(LNG)与雌二醇(E_2)按5:2重量比配伍,以天然可生物降解的明胶为材料,用相分离法制备了复方左旋18-甲基炔诺酮微球,平均球径为10～40μm,包封率达65％～75％。制成注射液后,经加速与室温观察具有一定的物理化学稳定性,其热解活化能为134.4KJ/mol,体外溶出试验与不包球的注射液相比,T_(1/2)有极显著性差异(P<0.01),说明制成微球后具有明显的缓释作用。经复方与单方的微球注射液组织学对比观察,复方可减轻小鼠卵巢充血的副作用,提示临床应用复方时,LNG引起不规则出血等副作用有可能得以改善。
L-18-methyl norgestrel (LNG) and estradiol (E_2) by 5: 2 weight ratio compatible with natural biodegradable gelatin as material, prepared by the phase separation compound levonor 18- Ketone microspheres, the average diameter of 10 ~ 40μm, encapsulation efficiency of 65% to 75%. After injection, it has some physicochemical stability after accelerating and observing at room temperature, and its pyrolysis activation energy is 134.4KJ / mol. In vitro dissolution test compared with non-ball injection, T 1/2 Extremely significant difference (P <0.01), indicating that microspheres made with significant sustained release. By compound and unilateral microsphere injection histological contrast observation, the compound can reduce the side effects of mouse ovarian hyperemia, suggesting that clinical application of compound, LNG caused by irregular bleeding and other side effects may be improved.