Sedative as well as protective effects during hypoxia have been described for gamma-hydroxybutyric acid (GHB). Six swine (Sus scrofa domesticus) of 6 weeks old were administered NaGHB at a dose of 500 mg/kg intravenously (IV) and 500 and 750 mg/kg orally (PO) in a triple cross-over design. Repeated blood sampling was performed to allow pharmacokinetic analysis of GHB. Whole blood concentration at time point 0 after IV administration was 1727.21 ± 280.73 μg/mL, with a volume of distribution of 339.45 ± 51.41 mL/kg and clearance of 164.94 ± 47.05 mL/(kg h). The mean peak plasma concentrations after PO administration were 326.57 ± 36.70 and 488.01 ± 154.62 μg/mL for 500 mg/kg and 750 mg/kg, respectively. These were recorded at 1.42 ± 0.72 and 1.58 ± 0.58 h after PO dose for GHB 500 mg/kg and 750 mg/kg, respectively. The elimination half-life for IV and PO 500 mg/kg and PO 750 mg/kg dose was respectively 1.33 ± 0.30, 1.16 ± 0.31 and 1.11 ± 0.33 h. The bioavailability (F) for PO administration was 45%. No clinical adverse effects were observed after PO administration. Deep sleep was seen in one animal after IV administration, other animals showed head pressing and ataxia.

中文翻译：

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γ-羟基丁酸在6周龄猪（Sus scrofa Domesticus）静脉和口服给药后的药代动力学

γ-羟基丁酸 (GHB) 在缺氧期间具有镇静和保护作用。在三重交叉设计中，对六只 6 周龄的猪（Sus scrofa Domesticus）进行静脉注射（IV）剂量为 500 mg/kg，口服剂量为 500 mg/kg 和 750 mg/kg（PO）的 NaGHB。重复进行血液采样以进行 GHB 的药代动力学分析。静脉给药后第0时间点的全血浓度为1727.21±280.73μg/mL，分布容积为339.45±51.41mL/kg，清除率为164.94±47.05mL/(kg·h)。PO给药后500mg/kg和750mg/kg的平均血浆峰浓度分别为326.57±36.70和488.01±154.62μg/mL。这些值分别是在口服 500 mg/kg 和 750 mg/kg GHB 后 1.42 ± 0.72 和 1.58 ± 0.58 小时记录的。IV和PO 500 mg/kg和PO 750 mg/kg剂量的消除半衰期分别为1.33±0.30、1.16±0.31和1.11±0.33小时。PO 给药的生物利用度 ( F ) 为 45%。PO给药后未观察到临床不良反应。静脉注射后，一只动物出现深度睡眠，其他动物表现出头部压迫和共济失调。