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目的:研究酒石酸氢可酮片的人体药代动力学。方法:本研究采用单次给药、平行设计试验方法,按照给药剂量5、10、15 mg(低、中、高)分为三组,每组10人。通过高效液相色谱串联质谱(HPLC-MS/MS)法测定血浆中氢可酮及其两种代谢产物(去甲基氢可酮和氢吗啡酮)的浓度。采用Win Nonlin 6.1分析软件计算药代动力学参数。结果:氢可酮、去甲基氢可酮的线性范围均为0.05~50.00μg·L-1,氢吗啡酮的线性范围为0.01~10.00μg·L-1;受试者口服酒石酸氢可酮片后体内氢可酮、去甲基氢可酮的Cmax、AUC0-t和AUC0-∞随剂量增加而增加与给药剂量呈良好线性关系。研究过程中无严重不良事件发生。结论:HPLC-MS/MS测定法灵敏、准确、简便,适用于血浆中氢可酮及其代谢产物浓度的测定以及人体药代动力学研究。
Objective: To study the pharmacokinetics of hydrocodone bitartrate tablets. Methods: In this study, a single dose, parallel design test method, according to the dose of 5,10,15 mg (low, medium and high) divided into three groups of 10 people. Plasma concentrations of hydrocodone and its two metabolites (nordokinase and hydromorphone) were determined by high performance liquid chromatography tandem mass spectrometry (HPLC-MS / MS). Pharmacokinetic parameters were calculated using Win Nonlin 6.1 analysis software. Results: The linear ranges of hydrocodone and desmethyl hydrocodone were 0.05-50.00 μg · L-1, and the linear range of hydromorphone was 0.01-10.00 μg · L-1. Hydrocodone and hydrocodone The Cmax, AUC0-t and AUC0-∞ of hydrocodone and desmethylhydrocodone in the tablets increased linearly with dose after administration. No serious adverse events occurred during the study. Conclusion: The method of HPLC-MS / MS is sensitive, accurate and simple and is suitable for the determination of the concentration of hydrocodone and its metabolites in plasma and the pharmacokinetics of human.