【摘要】 在 18名男性健康受试者中研究国产右美沙芬缓释混悬液的药物动力学特性及生物等效性。采用双周期交叉设计 ,反相高效液相色谱 -荧光检测法测定血浆中右美沙芬活性代谢物去甲右美沙芬的浓度。单剂量口服 6 0 m g右美沙芬缓释混悬液与进口对照品的 cmax分别为 4 36 .8± 116 .7和 4 0 9.5± 113.7ng/m l;Tmax为 3.3± 1.0和 3.4±0 .8h;T1 /2 为 7.5± 2 .7和 7.5± 3.1h;AUC0→ tn为 3435± 6 6 4 .2和 32 6 9± 6 2 6 .0 ng· ml- 1 · h。多剂量服药达稳态后两制剂的波动度分别为 (12 1.9± 37.1% )和 (133.2± 4 0 .6 ) %。主要药动学参数经统计学检验表明 :国产右美沙芬缓释混悬液与进口同类产品具生物等效性 ,相对生物利用度为 (10 5 .9± 13.8) %。更多还原

【Abstract】 The bioequivalence and pharmacokinetics of domestic dextromethorphan hydrobromide extended release suspension was investigated in 18 healthy man volunteers, according to randomized crossover design. The plasma concentration of dextrophan, the active metabolite of dextromethorphan, was determined by RP HPLC with fluorescence detection. The pharmacokinetic parameters for the single oral dose of 60 mg dextromethorphan hydrobromide extended release suspension were c max 436.8 ± 116.7 and 409.5 ± 113.7 ng/ml ; T max 3.3 ± 1.0 and 3.4 ± 0.8 h ; T 1/2 7.5 ± 2.7 and 7.5 ± 3.1 h ±; AUC 0→ t n 3435± 664.2 and 3269± 626.0 ng·ml -1 ·h , for testing and imported reference formulations, respectively. For the multiple dosing, the degree of fluctuation ( DF ) was (121.9 ± 37.1) % and (133.2±40.6)%, respectively. The results of two one side test showed that the two formulations may be considered as bio equivalent. The relative bioavailability for the test formulation was (105.9±13.8)%.更多还原