取健康家兔10只,随机分为2组,单剂量静注和灌服脂质体儿茶素(Catechin Liposome)25mg/kg。用高效液相色谱法测定血浆中儿茶素原药质量浓度。房室模型分析表明:健康家兔静注儿茶素脂质体的药时数据符合无吸收二室开放模型,主要药物动力学参数为:t1/2α0.18±0.01βh,t1/2β1.52±0.08βh,Vd4.48±0.24L,ClB2.05±0.07L/h,AUC29.20±1.00βmg/(L.h),K101.64±0.19h–1,K211.08±0.06h–1,K121.61±0.19h–1。健康家兔灌服脂质体儿茶素的药时数据符合一级吸收一室开放模型,主要药物动力学参数为:t1/2ka 0.27±0.03βh,t1/2ke 1.72±0.04βh,tmax0.87±0.05βh,Cmax6.53±0.62βmg/L,AUC 25.90±1.34βmg/(L.h),F 88.60±5.73%。脂质体儿茶素在健康家兔体内的药动学特征是:吸收迅速,达峰时间较短,消除慢,半衰期延长,表现分布容积大,口服生物利用度高。结果表明:儿茶素经脂质体包封后,药物动力学及组织分布均发生了明显改变。
Pharmacokinetics and bioavailability of Catechin Liposome were studied in 10 healthy rabbits following single intravenous (25mg/kg) and oral administration (25mg/kg)of the drug. Plasma concentrations of. Catechin Liposome were determined by high-performance liquid chromatography. The concentration-time data were fitted to a two-compartment model following a single intravenous injection in rabbits. The main pharmacokinetic parameters were as follows: distribution half-life (t1/2α) (0.18±0.01)h,elimination half-life (t1/2β) (1.52±0.08)h,apparent distribution volume (Vd) (4.48±0.24)L total body clearance (ClB) (2.05±0.07)L/h,the area under curve (AUC) (29.20±1.00)mg/(L.h). The drug concentration-time data also were fitted to a one-compartment open model with first order absorption after a single oral administration Catechin Liposome. The pharmacokinetic parameters were as follows: t1/2kα (0.27±0.03)h, t1/2ke(1.72±0.04)h, tmax (0.87±0.05) h, Cmax 6.53±0.62βmg/L, AUC 25.90±1.34βmg/(L.h), bioavailability F 88.60±5.73%. Pharmacokinetic characteristics of Catechin Liposome in healthy rabbits showed a rapid absorption, the time to reach Cmax is short, slow elimination, long half-life, large apparent distribution volume, and high bioavailability of oral administration. The results showed:after Catechin was prepared in liposome form, the tissue distribution and pharmacokinetics were changed significantly.
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