杨梅苷脂质体在动物体内药代吸收动力学初步研究

Preliminary study on the pharmacokinetics of myricitrin liposome in rats plasma

目的:以游离杨梅苷作对比,考察降解速率和半衰期,首次初步研究杨梅苷脂质体在大鼠体内的药代吸收动力学。方法:两组大鼠分别肌肉注射游离杨梅苷溶液和杨梅苷脂质体,间隔相同时间,分别眼球取血,高效液相色谱法(HPLC)测定药物残留含量。依据药物残留浓度和时间的关系,采用统计矩模型,利用3P97程序计算药代动力学参数,求出杨梅苷脂质体的降解速率和半衰期。结论:杨梅苷脂质体在肌肉注射的大鼠血浆中可较稳定的存在,具有载体和缓释的作用。大鼠体内的药代动力学数据表明,与游离杨梅苷溶液相比,脂质体使杨梅苷血药浓度能够维持更长的时间,给药8h后,血中仍保持一定的浓度分布,消除半衰期t1/2,α由64.3min增至243.6min,药时曲线下面积(AUC)为游离杨梅苷溶液溶液的3.41倍。

Objective：to inspect the degradation rate and half-life of elimination and study the pharmacokinetics of myricitrin liposome in rats plasma,compared with dissociated myricitrin solution.Methods：the two groups of rats were injected dissociated myricitrin solution and myricitrin liposome respectively.The plasma,in which medicine residue levels was detected by HPLC,was geted from their eyeballs after the same time.According to the relationship between the concentration of drug residues in plasma and time,using Statistical Moment Model,the pharmacokinetics parameters of myricitrin liposome,degradation rate and half-life of elimination,was calculated by the 3P97 program.Results：The fixt myricitrin liposome had a stable quality in rats plasma as carrier and controlled release formulation.Empirical data indicated that,compared with dissociated myricitrin solution,the liposome made the blood concentration keep a longer time,after 8 hours of the infusion,a certain concentration distribution can also be detected,the half-life of elimination（t1/2,α）increased from 64.3min to 243.6min,and the AUC was 3.41 times over it.