氧化苦参碱磷脂复合物肠溶缓释胶囊在小鼠体内的药代动力学及相对生物利用度研究

目的:研究氧化苦参碱磷脂复合物肠溶缓释胶囊在小鼠体内的药代动力学及相对生物利用度。方法 :84只健康昆明种小鼠,随机分为两组,在规定时间内采血,用高效液相色谱法(HPLC)测定小鼠经灌胃氧化苦参碱及氧化苦参碱磷脂复合物肠溶缓释胶囊内容物后的血药浓度。以PKSolver 2.0药动学软件进行曲线拟合,按口服吸收单房室模型计算药动学参数。结果:小鼠灌胃给药氧化苦参碱及氧化苦参碱磷脂复合物肠溶缓释胶囊内容物后的浓度-时间曲线均符合口服吸收单房室模型,氧化苦参碱及氧化苦参碱磷脂复合物肠溶缓释胶囊的达峰时(Tmax)分别为(1.14±0.17)h和(1.91±0.22)h,峰浓度(Cmax)分别为(2.59±0.07)μg/m L和(3.48±0.87)μg/m L,血药浓度-时间曲线下面积(AUC)分别为(8.11±1.24)μg/m L·h和(17.46±2.16)μg/m L·h。结论:氧化苦参碱磷脂复合物肠溶缓释胶囊的相对生物利用度为215.29%,能显著提高氧化苦参碱的生物利用度。

Study on the Pharmacokinetics and Relative Bioavailability of Enteric Sustained-release Capsule of Oxymatrine Phospholipid Complex in Mice

Objective:To study the pharmacokinetics and relative bioavailability of enteric sustained-release capsule of oxymatrine phospholipid complex in mice.Methods:Total 84 healthy Kunming mice were randomly divided into two groups,the blood was collected within the specified time.Serum levels were determined by HPLC after gavage oxidation of matrine and enteric sustained-release capsule of oxymatrine phospholipid contents.PKSolver 2 pharmacokinetic software was fitted to the curve,and the pharmacokinetic parameters were calculated according to the single compartment model of the oral absorption.Results :After given oxidation of matrine and enteric sustained-release capsule of Oxymatrine phospholipid complex content,concentration-time curve accorded with one compartment model of oral absorption.The time for peak concentration in oxidation of matrine and enteric sustained-release capsule of Oxymatrine phospholipid complex was Tmax(1.14±0.17) h and(1.91±0.22) h and the peak concentration was Cmax(2.59±0.07) μg/mL and(3.48±0.87) μg/mL,AUC(8.11±1.24) μg/mL·h and(17.46±2.16) μg/mL·h respectively.Conclusion:The relative bioavailability of enteric sustained-release capsule of oxymatrine phospholipid complex was 215.29%,improving the bioavailability significantly.