【摘要】 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。更多还原

【Abstract】 Objective: Salvianolic acid B was expected to be encapsulated into glycyrrhetinic acid-tanshinoneⅡA compound liposomes(GT-Lip) which was obtained in our prior study to prepare salvianolic Acid B-tanshinone ⅡA-glycyrrhetinic acid compound liposomes ulteriorly. Confirmatory experiments were designed to evaluate the stability of Sal B’s encapsulation. Methods: Sal B was encapsulated by pH gradient method, and ef ect of pH factor was evaluated using encapsulation eficiency(EE) of liposomes as index. Meanwhile, leakage of Sal B from GTS-lip was investigated when various diluents of liposomes were introduced. In addition, in vitro release property of Sal B was studied by dialysis method. In vivo release was investigated in mice. Results: Under acidic condition, EE of Sal B increased when pH decreased and reached 82.97% at pH 3.32. There was no obvious leakage of Sal B though GTS-lip was diluted by different multiple, and the release amount of Sal B from GTS-lip was 2.3% within the initial 60min which accorded with the standards of Chinese Pharmacopoeia. The release behavior of Sal B from GTSlip exhibited sustained release characteristics and fit well to Hixon-crowell equation model. Conclusion: It is stable and feasible to encapsulate Sal B into GTS-lip using pH gradient method.更多还原