川陈皮素自组装前体脂质体的制备及其大鼠体内药代动力学研究

本文研制川陈皮素自组装前体脂质体, 并以混悬剂为对照考察其经大鼠灌胃给药后的药代动力学行为。采用一种新型前体脂质体法制备川陈皮素自组装前体脂质体, 考察其水合后粒径、包封率和稳定性等理化性质; 大鼠分别灌胃给予川陈皮素混悬剂和水合后的脂质体, 以尼莫地平为内标, 采用HPLC法测定血浆中药物浓度, 用Kinatica 4.4程序计算药代动力学参数。制得的川陈皮素前体脂质体经水合后包封率可达80%以上,平均粒径为212.1 nm, 稳定性好; 药代动力学研究显示,与混悬剂相比川陈皮素脂质体在体内吸收较快, 相对生物利用度为264.3%, MRT增加。结果表明, 川陈皮素自组装前体脂质体制备工艺简单可行; 川陈皮素制成自组装前体脂质体后, 大鼠口服吸收显著增加。

Preparation of self-assemble nobiletin proliposomes and its pharmacokinetics in rats

To prepare self-assemble nobiletin proliposomes and study its pharmacokinetic behavior in rats after ig administration, and nobiletin suspension was used as control, self-assemble nobiletin proliposomes  were prepared by a new proliposome preparation method, their physicochemical properties including encapsulation efficiency, particle size and stability of formed liposome were determined.  Plasma concentration of nobiletin was determined by HPLC taking nimodipine as internal standard.  The pharmacokinetic parameters were    calculated by Kinetica 4.4 software.  The encapsulation efficiency of nobiletin liposomes was more than 80%, with an average particle size of 212.1 nm and very good stability.  Compared to nobiletin suspension, nobiletin liposomes possessed higher absorptive rate and longer MRT, and the relative bioavailability was 264.3% in rats.  It could be concluded that self-assemble nobiletin proliposome was a simple and feasible preparation, and showed greater absorption compared with nobiletin suspension.