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目的:在已制得丹参酮ⅡA-甘草次酸复方脂质体(GT-Lip)中载入丹酚酸B(Sal B),制备丹酚酸B-丹参酮ⅡA-甘草次酸复方脂质体(GTS-lip),并对其稳定性进行考察。方法:通过pH梯度法将Sal B载入GTLip中,以包封率为指标,考察pH值对Sal B载入的影响;考察稀释倍数对Sal B的渗漏影响。并采用动态透析法研究GTS-lip中丹酚酸B的体外释药情况,同时考察其在小鼠体内释药情况。结果:酸性条件下,Sal B包封率随pH降低而增加,pH=3.32时包封率达82.97%。稀释倍数对Sal B包封率无较大影响,Sal B在复方脂质体1h内累积释放量占总药量的2.3%,符合药典标准,释药过程有明显的缓释特征,无突释效应,经拟合符合Hixon-crowell方程模型,小鼠体内实验呈现一定缓释特征,与体外释放结果呼应。结论:采用pH梯度法载入Sal B,制成丹酚酸B-丹参酮ⅡA-甘草次酸复方脂质体的工艺稳定可行。
OBJECTIVE: To prepare salvianolic acid B-tanshinone ⅡA-glycyrrhetinic acid liposomes (Sal B) in the tanshinoneⅡA-glycyrrhetinic acid complex liposomes (GT-Lip) GTS-lip), and its stability were investigated. Methods: Sal B was loaded into GTLip by pH gradient method. The entrapment efficiency was used as an index to investigate the effect of pH on Sal B loading. The effect of dilution on Sal B leakage was also investigated. The dynamic dialysis method was used to study the in vitro release of salvianolic acid B from GTS-lip, and its release in mice was also investigated. Results: Under acidic conditions, the encapsulation efficiency of Sal B increased with the decrease of pH, and the encapsulation efficiency reached 82.97% at pH = 3.32. The dilution factor had no significant effect on the encapsulation efficiency of Sal B. The cumulative release amount of Sal B in the compound liposomes within 1h accounted for 2.3% of the total dose, which was consistent with Pharmacopoeia standard. The drug release process had obvious sustained release characteristics, Effect. After fitted to the Hixon-crowell equation model, the in vivo experiments in mice showed certain sustained-release characteristics and echoed the in vitro release results. Conclusion: The process of Sal B-Tanshinone ⅡA-glycyrrhetinic acid liposomes loaded Sal B by pH gradient method is stable and feasible.