Salsali M, Coutts R T, Baker G B
Department of Psychiatry, University of Alberta, W Mackenzie Health Sciences Center, Edmonton, Canada.
J Pharmacol Toxicol Methods. 1999 Aug;41(4):143-6. doi: 10.1016/s1056-8719(99)00033-7.
Dextromethorphan, a constituent of many over-the-counter cough syrups, is used as a probe drug for phenotyping subjects for their cytochrome P450 2D6 (CYP2D6) enzyme activity and for measuring CYP2D6 activity of preparations such as microsomes. In such studies, formation of the metabolite dextrorphan is used as indicator of the activity of this CYP enzyme. The present report describes an electron-capture gas chromatographic procedure developed for detection and quantification of dextrorphan in human liver microsomal preparations in vitro. After basification of the incubation mixture, dextrorphan was derivatized with pentafluorobenzoyl chloride under aqueous conditions prior to analysis on a gas chromatograph equipped with a capillary column, an electron capture detector, and a printer-integrator. Para-hydroxymephenytoin was carried through the procedure as internal standard. The procedure, which involves the derivatization of dextrorphan under aqueous conditions, is rapid and involves the use of the relatively economical procedure of electron-capture gas chromatography. The derivative is stable and possesses excellent chromatographic properties.
右美沙芬是许多非处方止咳糖浆的成分，用作检测受试者细胞色素P450 2D6（CYP2D6）酶活性的探针药物，并用于测量微粒体等制剂的CYP2D6活性。在此类研究中，代谢物右啡烷的形成用作该CYP酶活性的指标。本报告描述了一种电子捕获气相色谱法，用于体外检测和定量人肝微粒体制剂中的右啡烷。孵育混合物碱化后，右啡烷在水相条件下用五氟苯甲酰氯衍生化，然后在配备毛细管柱、电子捕获检测器和打印积分仪的气相色谱仪上进行分析。对羟基美芬妥因作为内标物全程参与该过程。该方法涉及在水相条件下对右啡烷进行衍生化，快速且采用了相对经济的电子捕获气相色谱法。衍生物稳定且具有出色的色谱特性。
