国产卡维地洛片药代动力学及相对生物利用度研究

Pharmacokinetics and Relative Bioavailability of Carvedilol Tablets in Healthy Volunteers

10石健康志愿者随机交叉单剂量口服20mg国产与进口卡维地洛片进行药代动力学和相对生物利用度研究。采用高效液相色谱-荧光法测定其血药浓度。结果表明，卡维地洛口服后体内动力学过程符合二房室模型，国产与进口片剂的Tmax分别为1．15±0．88和1.15±0．78h，Cmax分别为72．5±27．3和71．4±27．9μg·L-1，T1/2β分别为7.57±2.61和7.74±3.22h，AUC0-t分别为281.8±62.2和308.6±114．4μg·L-1·h，AUC0-∞分别为314．9±67．1和345．8±127．9μg·L-1·h。国产卡维地洛片相对生物利用度为98．5±24．6％。两种片剂的药代动力学参数经配对t检验无显著差异（P＞0.05）。AUC0-t、AUC0-∞、Cmax值对数转换后经方差分析，双单侧t检验及90％置信区间法作等效性判定，认为两种片剂为生物等效制剂。

The Pharmacokinetics and relative bioavailability of domestic and importedcarvedilol tablets were studied following a single oral dose of 20mg given to 10 normalmale volunteers in a randomized crossover design. Plasma levels were determined by HPLC-fluorescence. The time course of plasma concentration of careedilol tablets after oral dosingwas fitted to the two compartment model. The main pharmacokinetic parameters were Cmax72.5±27.3 and 71.4± 27.9 μg·L-1 at 1.15±0.88 and 1.15± 0.78 h, T1/2β7.57±2.61and 7.74±3.22 h, AUCo-t,281 .8±62.2 and 308.6±114.4 μg·L-1·h, AUC0~∞ 314.9±67.1 and 345.8±127.9 μg·-1·h for domestic and imported tablets, respectively.The relative bioavailability of domestic tablets was 98.5±24.6%. The bioequivalence ofthe two tablets were calculated by analysis of variance, two one-sidedt tests and 90%-confidence intervals. The results of statistical analysis demonstrated that the two tabletswere bioequivalent.