蟾酥脂质微球注射液的制备及其灭菌稳定性

Preparation and stability towards sterilization of Venenum Dufonis lipid microsphere for injection

目的研究蟾酥脂质微球注射液的处方工艺并考察制剂的灭菌稳定性。方法采用两级高压均质法制备蟾酥脂质微球注射液,分别考察油相组成、乳化剂用量、pH、灭菌方式对制剂灭菌稳定性的影响。结果采用质量分数为10.00%的油相[注射用中链脂肪酸甘油酯(MCT)与注射用大豆油(LCT)等比例混合],质量分数为1.20%的豆磷脂,质量分数为0.06%的油酸钠,均质前调节pH6.5,采用100℃旋转水浴灭菌30 min,制备所得的蟾酥脂质微球注射液在灭菌后仍保持良好的物理化学稳定性。结论粒子界面荷电性、空间位阻作用、pH、灭菌方式是影响蟾酥脂质微球注射液的物理化学稳定性的重要因素。

Objective To optimize the formulation and the preparation process of Venenum Dufonis lipid microsphere for injection and investigate the stability of various formulations towards sterilization.Methods A two-stage pressure homogenizer was used to prepare Venenum Dufonis lipid microsphere for injection.The effects of oil phase,emulsifier,pH and sterilization method on the stability of lipid microsphere were investigated separately.Results The optimal formulation was LCT-MCT（m∶m=1∶1,total w=10%）,1.2% soybean lecithin and 0.06% sodium oleate.pH was adjusted to 6.5 before homogenization.Finally,Chansu lipid microsphere for injection was sterilized for 30 min in rotating water-bath at 100 ℃ and exhibited good stability after the procedure of sterilization.Conclusions Physiochemical stability of lipid microsphere（LM） is affected by surface charge,stereospecific blockade,pH and sterilization.