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目的制备冬凌草甲素长循环胶束,对比普通冬凌草甲素磷脂/胆盐混合胶束和冬凌草甲素长循环胶束在大鼠体内的药动学差异。方法用薄膜分散法制备冬凌草甲素长循环胶束和普通冬凌草甲素磷脂/胆盐混合胶束,测定粒径,HPLC法测定血浆中冬凌草甲素的浓度,并用DAS2.0软件计算药动学参数。结果胶束粒径为14.53±1.19 nm,PDI为0.28±0.06。冬凌草甲素长循环胶束的体内T1/2为125.25±40.78 h,是普通胶束的12.8倍,AUC为168.04±39.01μg.L-1.h-1,为普通胶束的5.8倍(P<0.05)。结论所制备的冬凌草甲素长循环胶束与普通磷脂/胆盐混合胶束相比,其体内半衰期明显延长,生物利用度显著提高,具有长循环的效果。
OBJECTIVE To prepare oridonin long circulation micelles and compare the pharmacokinetics differences between the conventional oridonin phospholipid / bile salt mixed micelles and oridonin long circulating micelles in rats. Methods A mixture of oridonin cyclophosphamide and conventional oridonin phospholipid / bile salt micelles was prepared by membrane dispersion method. The particle size was determined by HPLC. The concentration of oridonin in plasma was determined by HPLC. 0 Software calculates pharmacokinetic parameters. Results Micelle size was 14.53 ± 1.19 nm and PDI was 0.28 ± 0.06. The in vivo T1 / 2 of oridonin long-circulating micelles was 125.25 ± 40.78 h, which was 12.8 times of that of normal micelles, and the AUC was 168.04 ± 39.01 μg.L-1.h-1, which was 5.8 times that of common micelles (P <0.05). CONCLUSION: Compared with the common phospholipid / bile salt mixed micelles, the oridonin produced long circulating micelles significantly prolongs the in vivo half-life and significantly improves the bioavailability and has the effect of long circulation.