Palatini P, Tedeschi L, Frison G, Padrini R, Zordan R, Orlando R, Gallimberti L, Gessa G L, Ferrara S D
Department of Pharmacology, University of Padova, Italy.
Eur J Clin Pharmacol. 1993;45(4):353-6. doi: 10.1007/BF00265954.
Gamma-hydroxybutyric acid (GHB) is effective in treatment of the alcohol and opiate withdrawal syndromes. Its absorption and disposition kinetics have been studied in 8 healthy male volunteers following oral administration of single doses of 12.5, 25 and 50 mg kg-1. The AUC increased disproportionately with the dose and so the apparent oral clearance decreased significantly as the dose was increased, whereas the terminal half-life and mean residence time increased. The peak plasma concentrations normalised to the lowest dose fell significantly with increasing doses, whilst the corresponding peak times increased. These findings suggest that both the oral absorption and the elimination of GHB are capacity-limited processes. GHB did not bind to significant extent to plasma proteins over the therapeutic concentration range. The pharmacokinetic parameters in healthy volunteers were not significantly different from those previously observed in alcohol-dependent patients with compensated alcoholic liver disease.
γ-羟基丁酸（GHB）对酒精和阿片类药物戒断综合征有效。在8名健康男性志愿者口服单剂量12.5、25和50 mg kg-1后，研究了其吸收和处置动力学。曲线下面积（AUC）随剂量不成比例增加，因此随着剂量增加，表观口服清除率显著降低，而末端半衰期和平均驻留时间增加。以最低剂量标准化的血浆峰浓度随剂量增加显著下降，而相应的峰时间增加。这些发现表明，GHB的口服吸收和消除均为容量限制过程。在治疗浓度范围内，GHB与血浆蛋白的结合程度不显著。健康志愿者的药代动力学参数与先前在患有代偿性酒精性肝病的酒精依赖患者中观察到的参数无显著差异。
