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曲线下面积的残留分数作为药代动力学研究中的一个定性标准。

Residual fraction of the area under the curve as a qualitative criterion in pharmacokinetic studies.

机构信息

Centre of Pharmacokinetics Research FILAB, Ravimed Sp. z o.o., Polna 54, PL 05-119 Łajski, Poland.

出版信息

Pharmacol Rep. 2010 Mar-Apr;62(2):374-82. doi: 10.1016/s1734-1140(10)70277-2.

Abstract

The aim of the present study was to determine whether the residual area under the curve (AUC(res%); expressed as % of total value of AUC) could be used as a parameter for the qualitative evaluation of pharmacokinetic studies.We propose new criteria for the qualitative evaluation of pharmacokinetic analysis. Two sets of hypothetical data that illustrate the relationship between concentration and time were used for the analysis of drug pharmacokinetics. Non-compartmental analysis was applied for the calculations. The results obtained from the hypothetical data were compared with those obtained from an in vivo study in which 3-week-old broiler chickens were administered 10 mg/kg b.w. enrofloxacin intravenously (iv) or per os (po). In the first set of data (A-D), AUC(res%) values were as follows: A= 16.29% and B = 20.79% for iv administration and C = 29.61% and D = 27.90% for po administration. In the next set of data (E-G), AUC(res%) values after oral administration were 25.30% (E), 23.18% (F), and 20.79% (G). The AUC(res%) values after iv administration of enrofloxacin were similar to po administration; the range of iv and po administration values were 14.35% to 17.50% and 11.14% to 28.33% of the total AUC, respectively. The analysis of the hypothetical data indicates that AUC(res%) is not an optimal method for the evaluation of pharmacokinetic studies.

摘要

本研究旨在确定曲线下剩余面积(AUC(res%);表示为 AUC 总价值的%)是否可用作药代动力学研究定性评估的参数。我们提出了用于药代动力学分析定性评估的新标准。使用两组假设数据来分析药物药代动力学。非房室分析用于计算。将从假设数据中获得的结果与从静脉内(iv)或口服(po)给予 10 mg/kg bw 恩诺沙星的 3 周龄肉鸡的体内研究中获得的结果进行比较。在第一组数据(A-D)中,AUC(res%) 值如下:iv 给药的 A = 16.29%和 B = 20.79%,C = 29.61%和 D = 27.90% po 给药。在接下来的一组数据(E-G)中,口服后 AUC(res%) 值分别为 25.30%(E)、23.18%(F)和 20.79%(G)。恩诺沙星 iv 给药后的 AUC(res%) 值与 po 给药相似;iv 和 po 给药值的范围分别为 AUC 总量的 14.35%至 17.50%和 11.14%至 28.33%。假设数据的分析表明,AUC(res%) 不是药代动力学研究评估的最佳方法。

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