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尿液碱化和活性炭对犬口服卡洛芬药代动力学的影响。

Effects of urine alkalization and activated charcoal on the pharmacokinetics of orally administered carprofen in dogs.

作者信息

Raekallio Marja R, Honkavaara Juhana M, Säkkinen Mia S, Peltoniemi S Marikki

机构信息

Department of Equine and Small Animal Medicine, Faculty of Veterinary Medicine, University of Helsinki, Helsinki, FIN-00014, Finland.

出版信息

Am J Vet Res. 2007 Apr;68(4):423-7. doi: 10.2460/ajvr.68.4.423.

Abstract

OBJECTIVE

To investigate the effects of oral administration of activated charcoal (AC) and urine alkalinization via oral administration of sodium bicarbonate on the pharmacokinetics of orally administered carprofen in dogs.

ANIMALS

6 neutered male Beagles.

PROCEDURES

Each dog underwent 3 experiments (6-week interval between experiments). The dogs received a single dose of carprofen (16 mg/kg) orally at the beginning of each experiment; after 30 minutes, sodium bicarbonate (40 mg/kg, PO), AC solution (2.5 g/kg, PO), or no other treatments were administered. Plasma concentrations of unchanged carprofen were determined via high-performance liquid chromatography at intervals until 48 hours after carprofen administration. Data were analyzed by use of a Student paired t test or Wilcoxon matched-pairs rank test.

RESULTS

Compared with the control treatment, administration of AC decreased plasma carprofen concentrations (mean +/- SD maximum concentration was 85.9 +/- 11.9 mg/L and 58.1 +/- 17.6 mg/L, and area under the time-concentration curve was 960 +/- 233 mg/L x h and 373 +/- 133 mg/L x h after control and AC treatment, respectively). The elimination half-life remained constant. Administration of sodium bicarbonate had no effect on plasma drug concentrations.

CONCLUSIONS AND CLINICAL RELEVANCE

After oral administration of carprofen in dogs, administration of AC effectively decreased maximum plasma carprofen concentration, compared with the control treatment, probably by decreasing carprofen absorption. Results suggest that AC can be used to reduce systemic carprofen absorption in dogs receiving an overdose of carprofen. Oral administration of 1 dose of sodium bicarbonate had no apparent impact on carprofen kinetics in dogs.

摘要

目的

研究口服活性炭(AC)以及通过口服碳酸氢钠使尿液碱化对犬口服卡洛芬药代动力学的影响。

动物

6只去势雄性比格犬。

步骤

每只犬进行3次实验(实验间隔6周)。在每次实验开始时,犬口服单剂量卡洛芬(16mg/kg);30分钟后,分别给予碳酸氢钠(40mg/kg,口服)、AC溶液(2.5g/kg,口服),或不给予其他处理。在卡洛芬给药后直至48小时,定期通过高效液相色谱法测定未变化的卡洛芬血浆浓度。数据采用Student配对t检验或Wilcoxon配对秩和检验进行分析。

结果

与对照处理相比,给予AC降低了血浆卡洛芬浓度(平均±标准差,最大浓度在对照处理后为85.9±11.9mg/L,在AC处理后为58.1±17.6mg/L;时间 - 浓度曲线下面积在对照处理后为960±233mg/L·h,在AC处理后为373±133mg/L·h)。消除半衰期保持不变。给予碳酸氢钠对血浆药物浓度无影响。

结论及临床意义

犬口服卡洛芬后,与对照处理相比,给予AC可有效降低血浆卡洛芬最大浓度,可能是通过减少卡洛芬的吸收。结果表明,AC可用于减少过量服用卡洛芬的犬体内卡洛芬的全身吸收。口服1剂碳酸氢钠对犬的卡洛芬动力学无明显影响。

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