Siao Kristine T, Pypendop Bruno H, Ilkiw Jan E
Department of Surgical and Radiological Sciences, School of Veterinary Medicine, University of California-Davis, Davis, CA 95616, USA.
Am J Vet Res. 2010 Jul;71(7):817-21. doi: 10.2460/ajvr.71.7.817.
To determine the pharmacokinetics of gabapentin in cats after IV and oral administration.
6 healthy female adult domestic shorthair cats.
Gabapentin was administered IV (4 mg/kg) or orally (10 mg/kg) in a crossover randomized design. Blood samples were obtained immediately before gabapentin administration and at various times up to 960 minutes after IV administration or up to 1,440 minutes after oral administration. Blood samples were immediately transferred to tubes that contained EDTA and were centrifuged at 4 degrees C. Plasma was harvested and stored at -20 degrees C until analysis. Plasma concentrations of gabapentin were determined by use of liquid chromatography-mass spectrometry. Gabapentin concentration-time data were fit to compartment models.
A 3-compartment model with elimination from the central compartment best described the disposition of gabapentin administered IV to cats, but a 1-compartment model best described the disposition of gabapentin administered orally to cats. After IV administration, the mean +/- SEM apparent volume of the central compartment, apparent volume of distribution at steady state, and clearance and the harmonic mean +/- jackknife pseudo-SD for terminal half-life were 90.4 +/- 11.3 mL/kg, 650 +/- 14 mL/kg, 3 +/- 0.2 mL/min/kg, and 170 +/- 21 minutes, respectively. Mean +/- SD systemic availability and harmonic mean +/- jackknife pseudo-SD terminal half-life after oral administration were 88.7 +/- 11.1% and 177 +/- 25 minutes, respectively.
The disposition of gabapentin in cats was characterized by a small volume of distribution and a low clearance.
确定加巴喷丁经静脉注射和口服给药后在猫体内的药代动力学。
6只健康成年雌性家养短毛猫。
采用交叉随机设计，对猫静脉注射（4mg/kg）或口服（10mg/kg）加巴喷丁。在加巴喷丁给药前即刻以及静脉注射后长达960分钟或口服给药后长达1440分钟的不同时间点采集血样。血样立即转移至含有乙二胺四乙酸（EDTA）的试管中，并在4℃下离心。收集血浆并储存于-20℃直至分析。采用液相色谱-质谱法测定血浆中加巴喷丁的浓度。将加巴喷丁浓度-时间数据拟合到房室模型。
三室模型（从中央室消除）最能描述静脉注射加巴喷丁在猫体内的处置情况，但一室模型最能描述口服加巴喷丁在猫体内的处置情况。静脉注射后，中央室的平均±标准误表观容积、稳态分布容积、清除率以及终末半衰期的调和均值±折刀法伪标准差分别为90.4±11.3mL/kg、650±14mL/kg、3±0.2mL/（min·kg）和170±21分钟。口服给药后的平均±标准差全身生物利用度和终末半衰期的调和均值±折刀法伪标准差分别为88.7±11.1%和177±25分钟。
加巴喷丁在猫体内的处置特点是分布容积小和清除率低。
