两性霉素B脂质体冻干粉的制备与性质

Preparation and Properties of Amphotericin B Liposome Freeze-Dried Powder

目的:以薄膜分散法制备两性霉素B脂质体冻干粉(AMB-Lip-FDP),并进行其质量评价。方法:采用薄膜分散法制备AMB-Lip-FDP,考察冻干工艺对AMB-Lip-FDP外观、溶解性、粒径和包封率的影响,并对制备的冻干粉性质进行表征。结果:采用薄膜分散法制备的AMB-Lip-FDP为黄色蓬松粉末,溶解性好,略有引湿性,复溶后的平均粒径为(110.2±3.6)nm,PDI为0.187±0.026,Zeta电位为(-42.6±1.4)mV,包封率为93.6%±2.7%,稳定性较好。体外释放结果表明,PBS中48 h释放约65%,具有明显的缓释性。5%葡萄糖注射液稀释,室温48 h稳定。结论:采用优化后工艺制备AMB-Lip-FDP稳定可行,具有明显缓释特征,为该产品的生物等效性评价提供研究基础。

Objective:The Amphotericin B liposome freeze-dried powder(AMB-Lip-FDP)were prepared by film dispersion method,and investigate its quality.Methods:AMB-Lip-FDP was prepared by film dispersion method.Taking appearance,solubility,particle size,encapsulation efficiency as evaluation indicators,the lyophilization process was investigated,and then the properties of the prepared lyophilized powder were characterized.Results:AMB-Lip-FDP which prepared by film dispersion method was a fluffy yellow powder with good solubility,slight moisture attraction.The average particle size after reconstraction was(110.2±3.6)nm,PDI was 0.187±0.026,Zeta potential was(-42.6±1.4)mV,the encapsulation efficiency was 93.6%±2.7%,and the stability is good.In vitro release experiments showed that the preparation was released slowly in PBS and its release rate was about 65% at 48 h.Diluted with 5% glucose injection,it was stable within 48 hours at room temperature.Conclusion:AMB-Lip-FDP prepared by the optimal process is stable and feasible,with obvious sustained-release characteristics,providing a research basis for the bioequivalence evaluation of amphotericin B liposome.