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目的:制备包封率高、稳定性好的阿昔洛韦(ACV)多囊脂质体。方法:采用复乳法制备ACV多囊脂质体,以包封率为指标,以润滑剂三油酸甘油酯量(A)、药脂比(B)、缓冲液的pH值(C)及辅助乳化剂吐温-80的用量(D)为因素,设计正交试验优选工艺;采用紫外分光光度法测定其中主药含量并计算包封率;考察优选工艺所制制剂不同条件下7d内包封率的变化并计算渗漏率。结果:最佳工艺为A0.50g、B5∶150、C6.5、D0.40g,所制多囊脂质体包封率为85.82%,常温条件下贮存7d渗漏率为5.84%。结论:采用优选工艺制备的ACV多囊脂质体方法简单,包封率较高,常温下较稳定。
Objective: To prepare acyclovir (ACV) multivesicular liposomes with high encapsulation efficiency and good stability. Methods: The ACV multivesicular liposomes were prepared by the double emulsion method. The encapsulation efficiency was used as the index to determine the amount of glycerol trioleate (A), the ratio of lipid to lipid (B), the pH of the buffer solution (C) The amount of auxiliary emulsifier Tween -80 (D) as a factor, the orthogonal design of the preferred process; Determination of the main drug content by UV spectrophotometry and calculation of entrapment efficiency; Preparation of the preparation process under different conditions 7d within the envelope Rate changes and calculate the leakage rate. Results: The best technology was A0.50g, B5:150, C6.5, D0.40g. The encapsulation efficiency of the multivesicular liposomes was 85.82%. The leakage rate was 5.84% after storage for 7 days at room temperature. CONCLUSION: The ACV multivesicular liposomes prepared by the preferred method are simple, high entrapment efficiency and stable at room temperature.