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目的：测定国产卡维地洛在健康志愿者的药代动力学及相对生物利用度。方法：１０名健康志愿者随机交叉口服４０ｍｇ国产卡维地洛和进口Ｄｉｌａｔｒｅｎｄ。用反相ＨＰＬＣ加荧光分光光度检测器法测定。所得结果进行药动学模型拟合。在每次采血同时测量血压及脉率。结果：１０名受试者中６名药动学符合一室模型，４名符合二室模型。测得主要药动学参数ＡＵＣ，Ｃｍａｘ，Ｔｍａｘ，ｔ１／２，ＣＬ与进口的Ｄｉｌａｔｒｅｎｄ相比其平均相对生物利用度为（９８．９±１１．６）％，两药具生物等效性。正常人一次服卡维地洛后收缩压及舒张压最大下降大多出现在给药后１．５～２ｈ，幅度为（２４±８）／（１３±４）ｍｍＨｇ。结论：我国汉族正常人卡维地洛的药动学消除半衰期较短，其余参数基本一致。还提示为使卡维地洛得到更好的降压效果，以每天服用２次为宜
Objective: To determine the pharmacokinetics and relative bioavailability of domestic carvedilol in healthy volunteers. Methods: Ten healthy volunteers were randomized to receive 40 mg domestic carvedilol and imported Dilatrend. Reverse phase HPLC plus fluorescence spectrophotometry detector. The results obtained pharmacokinetic model fitting. Blood pressure and pulse rate were measured at the same time for each blood sampling. Results: Six of the 10 subjects met the one-compartment model and four matched the two-compartment model. The mean relative bioavailability (AUC, Cmax, Tmax, t1 / 2, CL) of the major pharmacokinetic parameters was 98.9 ± 11.6% compared with the imported Dilatrend. The bioavailability of the two drugs Sex. Symptoms of systolic blood pressure and diastolic blood pressure after carvedilol were observed in normal subjects mostly occurred within 1.5 ~ 2h after drug administration, and the amplitude was (24 ± 8) / (13 ± 4) mmHg. Conclusion: The half-life of carvedilol in Han nationality normal population is short and the rest parameters are basically the same. Also suggested that in order to make carvedilol better antihypertensive effect, taking 2 times daily is appropriate