BACKGROUND In humans, gabapentin an analgesic, undergoes non-proportional pharmacokinetics which can alter efficacy. No information exists on the pharmacokinetics of dosages >20 mg/kg, escalating dosages or dose proportionality of gabapentin in horses. HYPOTHESIS AND OBJECTIVES Gabapentin exposure in plasma would not increase proportionally relative to the dose in horses receiving dosages ≥20 mg/kg. To assess the plasma pharmacokinetics of gabapentin after nasogastric administration of gabapentin at dosages of 10 to 160 mg/kg in adult horses. ANIMALS Nine clinically healthy adult Arabian and Quarter Horses. METHODS In a randomized blinded trial, gabapentin was administered by nasogastric intubation to horses at 10, 20 mg/kg (n = 3) and 60, 80, 120, 160 mg/kg (n = 6). Plasma was collected before and at regular times over 64 hours after administration of gabapentin. Gabapentin was quantified using a validated chromatographic method. Dose proportionality was estimated using a power model. Pharmacokinetic parameters were estimated using compartmental pharmacokinetic analysis. RESULTS Plasma pharmacokinetics parameters of gabapentin were estimated after nasogastric administration at dosages of 10 to 160 mg/kg. Gabapentin plasma concentration increased with dose increments. However, the area under the concentration curve from zero to infinity and maximal plasma concentration did not increase proportionally relative to the dose in horses. CONCLUSIONS AND CLINICAL IMPORTANCE Gabapentin exposure in plasma is not proportional relative to the dose in horses receiving nasogastric dosages of 10 to 160 mg/kg.

中文翻译：

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对成年马在胃内给予递增剂量的加巴喷丁后进行血浆处置。

背景技术在人类中，加巴喷丁镇痛药会经历非比例的药代动力学，这会改变药效。目前尚无关于> 20 mg / kg的药代动力学，加巴喷丁在马中递增剂量或剂量比例的信息。假设和目标相对于接受剂量≥20 mg / kg的马剂量，血浆中加巴喷丁的暴露不会成比例地增加。评估成年马鼻胃给药加巴喷丁剂量为10至160 mg / kg后加巴喷丁的血浆药代动力学。动物九个临床健康的成年阿拉伯和四分之一马。方法在一项随机盲试验中，通过鼻胃插管向马匹施用加巴喷丁的剂量为10、20 mg / kg（n = 3）和60、80、120、160 mg / kg（n = 6）。在施用加巴喷丁之前和之后的64小时内定期收集血浆。加巴喷丁使用经过验证的色谱方法进行定量。使用功效模型估算剂量比例。使用区室药代动力学分析估计药代动力学参数。结果加巴喷丁在鼻胃给药后以10至160 mg / kg的剂量估计其血浆药代动力学参数。加巴喷丁的血浆浓度随剂量增加而增加。但是，浓度曲线下从零到无穷大的区域以及最大血浆浓度相对于马匹的剂量没有成比例地增加。结论和临床意义血浆中加巴喷丁的暴露与接受鼻饲剂量为10至160 mg / kg的马的剂量不成比例。