Department of Pharmacy, University Medical Centre Utrecht, The Netherlands.
Eur J Pharm Sci. 2012 Dec 18;47(5):801-3. doi: 10.1016/j.ejps.2012.09.004. Epub 2012 Sep 24.
Intoxications with gamma-hydroxybutyrate (GHB) are occurring more frequently. Patients are primarily treated symptomatically. The use of activated charcoal (AC) has been suggested in several guidelines and in literature, although the clinical value of AC in GHB intoxication is a matter of debate. However, it has never been demonstrated that GHB binds to AC. Under certain conditions, prevention of absorption could be clinically relevant. Therefore, adsorption of GHB to AC in an in vitro model was tested.
A previously described in vitro model was used. Dosages of 2.5, 5, 7.5, or 10 g of standard AC (simulating in vivo dosages of approximately 25-100 g) were mixed with a dose of 800 mg GHB at 37 °C in 100 mL simulated gastric or intestinal fluid, respectively. Subsequently, the AC was separated from the liquid by centrifugation and the remaining GHB quantified by gas chromatography. GHB adsorption capacity was plotted in an adsorption curve.
Binding of GHB to AC was dose-dependent. At gastric pH, adsorption was higher than at intestinal pH, with a maximum adsorption of 84.3% and 23.3%, respectively, with 10 g of AC, corresponding with a high adult dose.
AC has clinically relevant GHB binding capacity, which is pH dependent. The normally rapid adsorption and the need for intubation argue against AC treatment in GHB intoxications. However, under certain circumstances e.g. in case of unintentional intake of GHB by children or in case of very high doses of GHB, rapid treatment with AC may still be appropriate. In vivo studies are needed to establish the clinical relevance of GHB adsorption to AC.
γ-羟基丁酸(GHB)中毒的情况越来越多。患者主要接受对症治疗。几项指南和文献中都建议使用活性炭(AC),尽管活性炭在 GHB 中毒中的临床价值存在争议。然而,从未有研究表明 GHB 与 AC 结合。在某些情况下,预防吸收可能具有临床意义。因此,在体外模型中测试了 GHB 与 AC 的吸附作用。
使用了先前描述的体外模型。将 2.5、5、7.5 或 10 g 标准 AC(模拟体内剂量约 25-100 g)与 800 mg GHB 剂量在 37°C 下分别混合于 100 mL 模拟胃液或肠液中。随后,通过离心将 AC 与液体分离,并通过气相色谱定量剩余的 GHB。绘制 GHB 吸附曲线以表示吸附能力。
GHB 与 AC 的结合呈剂量依赖性。在胃 pH 值下,吸附高于肠 pH 值,最大吸附率分别为 84.3%和 23.3%,使用 10 g AC 时,这对应于成人高剂量。
AC 对 GHB 具有临床相关的结合能力,且与 pH 值有关。通常,AC 的吸附速度很快,且需要进行插管,这反对在 GHB 中毒中使用 AC 进行治疗。然而,在某些情况下,例如儿童意外摄入 GHB 或摄入非常高剂量的 GHB 时,快速使用 AC 治疗可能仍然合适。需要进行体内研究以确定 GHB 吸附到 AC 的临床相关性。