愈酚甲麻那敏分散片的人体药动学研究

目的建立测定人血浆中愈创木酚甘油醚的高效液相法，以研究健康志愿者口服愈酚甲麻那敏分散片后愈创木酚甘油醚的药动学过程。方法色谱条件：Agilent Eclipse XDB—C18为色谱柱，以乙腈-磷酸二氢铵（体积比20：80，浓磷酸调至pH值3．0）为流动相，氧去甲右美沙芬为内标，紫外检测波长为230nm。结果愈创木酚甘油醚质量浓度在25～2000ng·mL^-1范围内线性关系良好（r=0．9977），定量下限为25ng·mL^-1。20名受试者单剂量口服愈酚甲麻那敏分散片后的主要动力学参数Cmax为（474±142）ng·mL^-1，tmax为（0．275±0．123）h，t1/2为（0．83±0．55）h，AUC0→4为（451±165）ng·h·mL^-1，AUC0→∞为（505±159）ng·h·mL^-1。结论本文所建立的方法简便、准确、可靠，可满足愈创木酚甘油醚临床药动学研究的需要。

Determination of guaifenesin in compound preparation in human plasma by HPLC and its pharmacokinetic study

Objective To determine the content of guaifenesin in human plasma samples by HPLC and to study its pharmacokinetics. Methods The plasma samples were separated on Agilent Eclipse XDB-C18 column with acetonitrile-ammonium dihydrogen phosphate （ 20：80, which was adjusted with phosphoric acid to pH3.0） as mobile phase and as dextrophan as internal standard. The detection wavelength was set at 230 nm. Results The concentration of guaifenesin showed good linearity in the range of 25 - 2 000 ng ·mL^-1 （ r = 0. 997 7 ） , with lower limit of quantification at 25 ng ·mL^-1. The main pharmacokinetic parameters in 20 healthy volunteers after administration of single oral dose of chlorphenamine maleate dispersible tablets were the following： Cmax ：（474 ±142）ng·mL^-1,tmax ：（0. 275 ±0.123 ）h,t,/2 ： （0.83 e 0.55）h,AUC0→4：（451 ±165） ng ·h·mL^-1 ,AUC0→∞（505 ±159） ng ·h·mL^-1. Conclusion The method was simple, accurate and reliable to use in clinical pharmacokinetic study of guaifenesin.