氧化苦参碱缓释片在犬体内的药物动力学

Pharmacokinetics of Oxymatrine Sustained-release Tablets in Dogs

研究氧化苦参碱缓释片在家犬体内单剂量和多剂量口服给药后的药物动力学。采用HPLC法测定家犬口服氧化苦参碱缓释片和普通胶囊后的血药浓度,结果表明,氧化苦参碱药-时曲线符合双室模型特征。单剂量口服缓释片和胶囊后Ka分别为(0.60±0.11)和(1.22±0.11)h-1;Tmax分别为(2.83±0.26)和(1.58±0.20)h;Cmax分别为(1.96±0.73)和(3.06±0.42)μg/ml,氧化苦参碱缓释片相对胶囊生物利用度F为(90.22±5.7)%。多剂量口服两种制剂4天后达稳态,波动系数分别为(1.37±0.35)和(1.59±0.40)。

Pharmacokinetics of oxymatrine sustained-release tablets and its capsules were investigated in six dogs for a single oral dose and multiple oral doses, respectively. The concentration of oxymatrine in plasma was determined by HPLC. The results showed that the concentration-time curves conformed to two-compartment model. The pharmacokinetic parameters after single dose were Kα （0.60 ±0.11） and （ 1.22 ± 0.11） h^-1, Tmax （2.83 ± 0.26） and （1.58 ± 0.20） h, Cmax （1.96±0.73） and （3.06±0.42）μg/ml for test and reference drugs, respectively. The relative bioavailability of test drug was （90.22 ± 5.7） %. After treated with multiple oral doses for 4 days, the concentration of oxymatrine got to a steady-state level, with FI of （1.37 ± 0.35） and （1.59 ± 0.40） for test and reference drugs, respectively.