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健康犬口服25毫克/千克克拉维菌素和速诺后克拉维酸的吸收情况各异。

Variable absorption of clavulanic acid after an oral dose of 25 mg/kg of Clavubactin and Synulox in healthy dogs.

作者信息

Vree T B, Dammers E, Van Duuren E

机构信息

Institute for Anaesthesiology, University Medical Center Sint Radboud, Nijmegen, The Netherlands.

出版信息

J Vet Pharmacol Ther. 2003 Jun;26(3):165-71. doi: 10.1046/j.1365-2885.2003.00476.x.

Abstract

The aims of this investigation were to calculate the pharmacokinetic parameters and to identify parameters, based on individual plasma concentration-time curves of amoxicillin and clavulanic acid in dogs, that may govern the observed differences in absorption of both drugs. The evaluation was based on the data from plasma concentration-time curves obtained following a single dose in an open, randomized, two-way crossover study involving 24 male Beagle dogs treated with two Amoxi-Clav formulations (A Clavubactin and B Synulox, each with 200/50 mg). Plasma amoxicillin and clavulanic acid concentrations were determined using validated bioassay methods. The half-life of elimination of amoxicillin was 1.5 h (t1/2 = 1.52 +/- 0.19 h, Cmax = 11.4 +/- 2.74 microg/mL), and that of clavulanic acid 0.76 h (t1/2 = 0.71 +/- 0.23 h, Cmax = 2.06 +/- 1.05 microg/mL). There was a fivefold variation in the AUCt of clavulanic acid for both formulations, while the AUCt of amoxicillin varied by a factor of 2. The mean ratio of the AUCt amoxicillin : clavulanic acid was 12.7 +/- 3.65 for formulation A and 11.8 +/- 5.22 for formulation B (P = 0.51).

摘要

本研究的目的是计算药代动力学参数,并根据阿莫西林和克拉维酸在犬体内的个体血浆浓度-时间曲线确定可能导致两种药物吸收差异的参数。该评估基于在一项开放、随机、双向交叉研究中单次给药后获得的血浆浓度-时间曲线数据,该研究涉及24只雄性比格犬,用两种阿莫西林-克拉维制剂(A Clavubactin和B Synulox,每种含200/50mg)进行治疗。使用经过验证的生物测定方法测定血浆阿莫西林和克拉维酸浓度。阿莫西林的消除半衰期为1.5小时(t1/2 = 1.52 +/- 0.19小时,Cmax = 11.4 +/- 2.74微克/毫升),克拉维酸的消除半衰期为0.76小时(t1/2 = 0.71 +/- 0.23小时,Cmax = 2.06 +/- 1.05微克/毫升)。两种制剂中克拉维酸的AUCt有五倍的差异,而阿莫西林的AUCt差异为两倍。制剂A中阿莫西林与克拉维酸的AUCt平均比值为12.7 +/- 3.65,制剂B为11.8 +/- 5.22(P = 0.51)。

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