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目的测定卡维地洛 (carvedilol)志愿受试者体内的药代动力学 ,并与国外标准品地拉特润 (dilatrend)对照 ,评价其相对生物利用度。方法 10名健康男性志愿受试者 ,年龄 (39± 9)岁 ,随机交叉服用卡维地洛或地拉特润 40mg ,HPLC法测定给药后不同时间的血药浓度 ,并进行药代动力学参数计算和模型拟合。结果 10名受试者 6名符合一房室模型 ,另 4名符合二房室模型。卡维地洛的药代动力学主要参数 :一房室者达峰时间Tmax(1 7± 0 4)h、最大血药浓度Cmax(75± 32 )mg/L、曲线下面积AUC (314± 12 2 )mg/L·h、半衰期t1/2 (1 7± 0 8)h、清除速率CL (141± 43)L/h ;二房室者各值相应为 (1 0± 0 4)h、(113± 89)mg/L、(337± 85 )mg/L·h、(7 9± 5 6 )h、(111± 2 3)L/h。与地拉特润相比 ,两种制剂的药代动力学参数无显著差异(P >0 0 5 )。卡维地洛的相对生物利用度为 (98 9± 11 6 ) %。结论卡维地洛的药代动力学及生物利用度与国外标准品地拉特润近似 ,两种制剂生物等效。
Objective To determine the pharmacokinetics of carvedilol volunteers in vivo and to compare its relative bioavailability with dilatrend, a foreign standard. Methods Ten healthy male volunteers, aged 39 ± 9 years, were randomized to receive either carvedilol or digrastol 40 mg. HPLC was used to determine plasma concentrations at various times after administration and pharmacokinetics Learning parameter calculation and model fitting. Results Six of the 10 subjects met the one-compartment model and the other four met the two-compartment model. The main parameters of carvedilol pharmacokinetics: peak room time in a room Tmax (17 ± 0 4) h, the maximum plasma concentration Cmax (75 ± 32) mg / L, the area under the curve AUC (314 ± (2) mg / L · h, half-life t1 / 2 (1 7 ± 0 8) h and clearance rate CL (141 ± 43) L / (113 ± 89) mg / L, (337 ± 85) mg / L · h, (7 9 ± 5 6) h and (111 ± 2 3) L / h, respectively. There was no significant difference in pharmacokinetic parameters between the two formulations (P> 0.05) compared with digratropin. The relative bioavailability of carvedilol was (98 9 ± 11 6)%. Conclusions The pharmacokinetics and bioavailability of carvedilol are close to those of foreign standards. The two preparations are bioequivalent.