汉防己甲素脂质体在大鼠体内的药动学研究

Study on Pharmacokinetics of Tetrandrine Liposomes in Rats

目的考察汉防己甲素脂质体在大鼠体内的药动学特性。方法采用薄膜分散法制备汉防己甲素脂质体,大鼠尾静脉分别注射汉防己甲素脂质体或溶液剂,用HPLC测定不同时间血浆中汉防己甲素的浓度,通过3P97程序计算药动学参数。结果制得的脂质体包封率为(79.7±0.68)%,汉防己甲素脂质体和溶液剂大鼠尾静脉单次给药均符合二室开放模型,与溶液剂相比,汉防己甲素脂质体的AUC显著增加。结论汉防己甲素脂质体能显著增加汉防己甲素在大鼠体内的AUC,延长其在血液循环中的驻留时间。

OBJECTIVE To study the pharmacokinetics of Tetrandrine liposomes in rats. METHOD Tetrandrine liposomes were prepared by film dispersion-sonication method. Rats were. injected with tetrandrine liposomes or tetrandrine solution through tail vein. The concentration of tetrandrine in plasma was measured at different times by HPLC and the pharmacokinetic parameters were computed by 3P97 program package. RESULTS The liposome encapsulation efficiency rate was （79.7±0.68）%.The plasma concentration-time curves of the tetrandrine liposomes obeyed a two-compartment open model. Compared with tetrandrine solution, AUC in tetrandrine liposome had increased significantly. CONCLUSION The tetrandrine liposomes could increase AUC of tetrandrine significantly and prolong the resi- dence time of tetrandrine.