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不同剂型阿莫西林经口给予犬后的生物利用度。

Bioavailability of different forms of amoxycillin administered orally to dogs.

作者信息

Küng K, Wanner M

机构信息

Institute of Veterinary Physiology, University of Zurich, Switzerland.

出版信息

Vet Rec. 1994 Dec 3;135(23):552-4.

PMID:7886889
Abstract

Amoxycillin was administered to six dogs intravenously (as the sodium salt at 20 mg/kg bodyweight) and orally (as the trihydrate at 20 mg/kg). The oral treatments followed a Latin square pattern, each dog receiving amoxycillin as a 60 ml suspension by stomach tube, or as 3 ml of drops or in the form of tablets. The concentration of the drug in the plasma was measured microbiologically and its pharmacokinetic parameters were calculated by the use of statistical moments. After intravenous administration the mean +/- sd apparent volume of distribution was 0.312 +/- 0.102 litre/kg, the steady state rate of clearance was 3.4 +/- 1.1 ml/min/kg and the mean residence time was 1.6 +/- 0.4 hours. After oral administration the liquid forms of the drug tended to be more readily absorbed than the tablets, as indicated by their higher bioavailabilities (suspension 76.8 +/- 16.7 per cent, drops 68.2 +/- 25.8 per cent, tablets 64.2 +/- 17.9 per cent). However, the differences between their pharmacokinetic parameters were not statistically significant. The respective values of Cmax for the tablets, drops and suspension were 18.6 +/- 5.3 micrograms/ml, 18.1 +/- 2.4 micrograms/ml and 20.7 +/- 2.2 micrograms/ml, of tmax 2.0 +/- 1.0 hours, 1.4 +/- 0.6 hours and 1.4 +/- 0.5 hours and of the AUC 69.5 +/- 22.5 micrograms/ml hours, 71.8 +/- 21.0 micrograms/ml hours and 80.6 +/- 21.8 micrograms/ml hours. The two useful drug products (drops and tablets) had similar pharmacokinetic profiles in the dogs and can therefore be regarded as equivalent in this species.

摘要

对6只犬静脉注射阿莫西林(以20mg/kg体重的钠盐形式)和口服给药(以20mg/kg的三水合物形式)。口服治疗采用拉丁方设计,每只犬通过胃管接受60ml阿莫西林混悬液,或3ml滴剂,或片剂形式给药。采用微生物学方法测定血浆中药物浓度,并运用统计矩计算其药代动力学参数。静脉给药后,平均±标准差的表观分布容积为0.312±0.102升/千克,稳态清除率为3.4±1.1毫升/分钟/千克,平均驻留时间为1.6±0.4小时。口服给药后,药物的液体制剂比片剂更易吸收,表现为更高的生物利用度(混悬液76.8±16.7%,滴剂68.2±25.8%,片剂64.2±17.9%)。然而,它们药代动力学参数之间的差异无统计学意义。片剂、滴剂和混悬液的Cmax分别为18.6±5.3微克/毫升、18.1±2.4微克/毫升和20.7±2.2微克/毫升,tmax分别为2.0±1.0小时、1.4±0.6小时和1.4±0.5小时,AUC分别为69.5±22.5微克/毫升·小时、71.8±21.0微克/毫升·小时和80.6±21.8微克/毫升·小时。两种有效的药物制剂(滴剂和片剂)在犬体内具有相似的药代动力学特征,因此在该物种中可视为等效。

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