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目的:研究白黎芦醇多相脂质体灌胃给药后在家兔体内的药动学特征。方法:家兔一次性灌胃白黎芦醇溶液及多相脂质体后,高效液相色谱(HPLC)法测定白黎芦醇血药浓度;通过3P97程序计算药动学参数。结果:白黎芦醇溶液及多相脂质体在家兔体血药时程变化均符合二室模型。白黎芦醇多相脂质体在家兔体内消除相半衰期t1/2β为(4.4±0.3)h,曲线下面积AUC0→3为(4.6±0.6)mg·h·L-1,清除率CL为(22.0±2.8)L·kg-1·h-1,最大血药质量浓度Cmax为(3.10±0.07)mg.L-1,与白黎芦醇溶液药动学参数比较,其差异均有统计学意义,白黎芦醇溶液药动学参数t1/2β为(1.07±0.20)h,AUC0→3为(0.97±0.04)mg·h·L-1,CL为(103.3±4.0)L·kg-1·h-1,Cmax为(1.030±0.021)mg·mL-1。结论:白黎芦醇多相脂质体可延长白黎芦醇在家兔体内半衰期、增加其曲线下面积和提高最大血药浓度,降低其清除率,有利于提高白黎芦醇生物利用度。
Objective: To study the pharmacokinetics of resveratrol multiphase liposomes in rabbits after intragastric administration. Methods: After a single dose of resveratrol solution and multiphase liposomes in rabbits, the plasma concentration of resveratrol was determined by high performance liquid chromatography (HPLC). Pharmacokinetic parameters were calculated by 3P97 program. Results: The resveratrol solution and multiphasic liposomes in rabbits were consistent with two-compartment model. The phase half-life of resveratrol multiphase liposomes was (4.4 ± 0.3) h, and the area under the curve AUC0 → 3 was (4.6 ± 0.6) mg · h · L -1. The clearance rate CL Was (22.0 ± 2.8) L · kg-1 · h-1, and the maximum plasma concentration of Cmax was (3.10 ± 0.07) mg.L-1.Compared with the resveratrol solution pharmacokinetic parameters, the differences were Statistically, the pharmacokinetic parameters of resveratrol solution were t1 / 2β (1.07 ± 0.20) h, AUC0 → 3 (0.97 ± 0.04) mg · h · L-1 and CL was (103.3 ± 4.0) L · kg-1 · h-1 and Cmax was (1.030 ± 0.021) mg · mL-1. Conclusion: The resveratrol multi-phase liposomes can prolong the half-life of resveratrol in rabbits, increase the area under the curve and increase the maximum plasma concentration, reduce the clearance rate, and improve the bioavailability of resveratrol .