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目的:优化去甲斑蝥素脂质体的制备工艺,并对其药剂学性质进行评价。方法:以包封率、平均粒径及跨距为综合指标,分别考察4种制备方法即薄膜分散法、注入法、逆相蒸发法和逆相蒸发薄膜法对去甲斑蝥素脂质体包封率和粒径的影响;以磷脂的量(X1)、磷脂/胆固醇质量比(X2)、探头式超声次数(X3)、磷酸盐缓冲液稀释倍数(X4)、油水相体积比(X5)和脂类与药物的质量比(X6)为考察因素,采用均匀设计优化逆相蒸发薄膜法制备载药脂质体的制备工艺,并对最佳工艺进行验证试验。结果:以逆相蒸发薄膜法制备脂质体包封率最高;最佳工艺:X1为200mg、X2为7∶1、X3为20次、X4为50倍、X5为1∶4、X6为30∶1;验证试验中样品脂质体包封率为(42.5±1.3)%,平均粒径为(210.9±2.1)nm,跨距为0.61±0.12。结论:成功制备了去甲斑蝥素脂质体。
OBJECTIVE: To optimize the preparation of norcantharidin liposomes and evaluate their pharmacological properties. Methods: The encapsulation efficiency, average particle size and spans were taken as the comprehensive indexes to investigate the effects of four preparation methods, ie film dispersion method, injection method, reverse phase evaporation method and reverse phase evaporation method, on the degradation of norcantharidin liposomes (X1), phospholipid / cholesterol mass ratio (X2), number of sonication (X3), dilution ratio of phosphate buffer (X4), volume ratio of oil to water phase And the mass ratio of lipid to drug (X6) were investigated. The preparation technology of drug-loaded liposomes by reverse phase evaporation was optimized by uniform design, and the best technology was verified. Results: The entrapment efficiency of liposomes prepared by reverse phase evaporation was the highest. The optimum conditions were as follows: X1 was 200mg, X2 was 7:1, X3 was 20 times, X4 was 50 times, X5 was 1: 4, X6 was 30 : 1. The liposome entrapment efficiency was (42.5 ± 1.3)% and the mean diameter was (210.9 ± 2.1) nm and the span was 0.61 ± 0.12 in validation test. Conclusion: Norcantharidin liposomes were successfully prepared.