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口服加巴喷丁单独或与美洛昔康联合给药在反刍动物肉牛犊体内的药代动力学。

Pharmacokinetics of oral gabapentin alone or co-administered with meloxicam in ruminant beef calves.

机构信息

Department of Clinical Sciences, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506-5601, USA.

出版信息

Vet J. 2011 Oct;190(1):98-102. doi: 10.1016/j.tvjl.2010.08.008. Epub 2010 Sep 24.

DOI:10.1016/j.tvjl.2010.08.008
PMID:20869892
Abstract

Gabapentin is a γ-aminobutyric acid (GABA) analogue indicated for treatment of neuropathic pain. This study determined the pharmacokinetics of oral (PO) gabapentin alone or in combination with meloxicam in ruminant calves. Gabapentin capsules at 10mg/kg or gabapentin powder (from capsules at 15mg/kg) and meloxicam tablets (0.5mg/kg) were administered PO to six beef calves. Plasma drug concentrations were determined over 48h post-administration by liquid chromatography/mass spectrometry followed by non-compartmental pharmacokinetic analysis. The mean (± standard deviation, SD) C(max), T(max) and elimination half-life (t(½)λz) for gabapentin (10mg/kg) alone was 2.97 ± 0.40μg/mL, 9.33 ± 2.73h and 11.02 ± 3.68h, respectively. The mean (± SD) C(max), T(max) and t(½)λz for gabapentin (15mg/kg) co-administered with meloxicam was 3.57±1.04μg/mL, 7.33 ± 1.63h and 8.12±2.11h, respectively. The mean (±SD) C(max), T(max) and t(½)λz for meloxicam was 2.11± 0.19μg/mL, 11.67 ± 3.44h and 20.47 ± 9.22h, respectively. Plasma gabapentin concentrations >2μg/mL were maintained for up to 15h and meloxicam concentrations >0.2μg/mL for up to 48h. The pharmacokinetic profile of oral gabapentin and meloxicam supported clinical evaluation of these compounds for management of neuropathic pain in cattle.

摘要

加巴喷丁是一种γ-氨基丁酸(GABA)类似物,用于治疗神经性疼痛。本研究旨在确定口服(PO)加巴喷丁单独或与美洛昔康联合用于反刍幼牛的药代动力学。6 头肉牛 PO 给予 10mg/kg 加巴喷丁胶囊或来自胶囊的 15mg/kg 加巴喷丁粉和 0.5mg/kg 美洛昔康片。给药后 48 小时内通过液相色谱/质谱法测定血浆药物浓度,并进行非房室药代动力学分析。单独给予 10mg/kg 加巴喷丁时,其平均(±标准差,SD)Cmax、Tmax 和消除半衰期(t1/2λz)分别为 2.97 ± 0.40μg/mL、9.33 ± 2.73h 和 11.02 ± 3.68h。与美洛昔康共同给予 15mg/kg 加巴喷丁时,其平均(±SD)Cmax、Tmax 和 t1/2λz 分别为 3.57±1.04μg/mL、7.33 ± 1.63h 和 8.12±2.11h。美洛昔康的平均(±SD)Cmax、Tmax 和 t1/2λz 分别为 2.11± 0.19μg/mL、11.67 ± 3.44h 和 20.47 ± 9.22h。加巴喷丁的血浆浓度维持在 >2μg/mL 长达 15h,美洛昔康的浓度维持在 >0.2μg/mL 长达 48h。口服加巴喷丁和美洛昔康的药代动力学特征支持对这些化合物进行临床评估,以治疗牛的神经性疼痛。

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