目的 将积雪草苷制成修饰脂质体，考察该制剂在体内的药动学过程及组织分布情况。方法 SD大鼠尾iv积雪草苷溶液及经过D-甘露糖或十八胺修饰和未经修饰的脂质体制剂，不同时间点采集大鼠血浆及组织，样品处理后采用HPLC法检测血浆与组织中的药物浓度，绘制药-时曲线，计算药动学参数，比较积雪草苷剂型间在体内药动学参数和组织分布的差异。结果 积雪草苷、积雪草苷脂质体、D-甘露糖-积雪草苷脂质体、十八胺-积雪草苷脂质体4种制剂的药-时曲线均符合权重为1/C²的单室模型。积雪草苷溶液及各脂质体的消除半衰期（t_1/2）分别为（14.52±0.56）、（101.35±12.47）、（149.82±20.00）、（159.58±16.46） min，药时曲线下面积（AUC）分别为（1 929.70±159.00）、（57 004.35±8 710.89）、（93 736.52±12 710.76）、（64 737.48±6 365.28） min·μg/mL。同时制成脂质体后，积雪草苷在各器官中的质量分数显著上升，在肺部的质量分数由（4.94±0.94）μg/g升至（39.12±12.04）μg/g。结论 将积雪草苷制成修饰脂质体制剂后，缓释明显，并能增强靶向作用。

Objective To prepare asiaticoside-loaded modified liposomes and to investigate the distribution and pharmacokinetics. Methods Different asiaticoside-loaded preparations (include solution, modified, and unmodified liposomes) were injected by tail vein in SD rats. HPLC method was used to detect the concentration of asiaticoside in the tissue and plasma samples. And the concentration-time profiles and pharmacokinetic parameters were then obtained and compared to get the variances. Results The concentration-time profiles of asiaticoside-loaded preparations guided along the single compartment model which the weight is 1/C². The elimination half-life of asiaticoside solution and different asiaticoside liposomes were (14.52 ±0.56), (101.35 ±12.47), (149.82 ±20.00), and (159.58 ±16.46) min, respectively. The AUC of asiaticoside solution and different asiaticoside liposomes were (1 929.70 ±159.00), (57 004.35 ±8 710.89), (93 736.52 ±12 710.76), and (64 737.48 ±6 365.28) min∙μg/mL, respectively. The mass fraction of asiaticoside in each organ increased, especially in the pulmonary which increased from (4.94 ±0.94) μg/g to (39.12 ±12.04) μg/g. Conclusion The sustained release and targeting effects in SD rats were obvious of the asiaticoside-loaded modified liposomes.

武警后勤学院基础研究项目（WHJ201501）