目的研制盐酸川芎嗪脂质体并考察其在小鼠体内的组织分布。方法以硫酸铵梯度法制备盐酸川芎嗪脂质体,用 HPLC测定经尾静脉给药后小鼠体内血液及组织中的药物浓度。结果制备的盐酸川芎嗪脂质体包封率为48.82％;平均粒径 6.5 μm。与盐酸川芎嗪普通注射液对照,它们在小鼠的心、肝、脾、肺、肾组织中的分布特性有不同程度的改变,其中盐酸川芎嗪脂质体在肺组织的浓度是对照组的4.7倍。结论硫酸铵梯度法制备盐酸川芎嗪脂质体可行,产物具有明显的肺靶向性。

OBJECTIVE To study the preparation of the ligustrazine hydrochloride (LTH) liposome and its distribution in mice.METHODS The liposome was prepared by the ammonim sulfate gradient technology. Blood and tissue drug concentration was determined by HPLC, and the drug distribution in mice was investigated after an iv administration (the liposome and the drug solution) .RESULTS The entrapped efficiency of the liposome was 48.82% and its mean size was 6.5 μm. The relative distribution percentage of LTH-liposome in lung after an iv administration was about 4.7 times as that of the LTH solution control group under the same conditions.CONCLUSION The preparation of the ligustrazine hydrochloride lipsome by the ammonim sulfate gradient technology is practicable and successful and the liposome owned targeting property on the lung.