目的 研究复方愈麻美芬缓释片单剂量和多剂量给药在健康志愿者体内的药动学规律。方法 采用自身对照的双周期交叉试验设计，12名健康受试者单次和多次口服受试制剂复方愈麻美芬缓释片或相应的参比制剂，不同时间点收集血样，采用LC/MS/MS法测定血浆中愈创甘油醚、伪麻黄碱、右美沙芬和O-去甲右美沙芬的浓度。药动学参数采用DAS软件处理获得。结果 单剂量口服受试制剂后，愈创甘油醚、伪麻黄碱、右美沙芬、O-去甲右美沙芬的主要参数为t_max：1.09±0.42、3.68±1.62、5.05±2.29、3.82±1.25 h；t_1/2：3.32±3.54、6.20±0.97、12.2±3.1、7.60±0.97 h；C_max：499±159、96.1±12.9、1.82±1.18、142±34 ng/mL；AUC0_-t：2363±529、1359±284、31.4±23.6、1504±242 ng·h/mL；AUC0_-∞：2554±639、1395±303、38.4±28.4、1563±248 ng·h/mL。多剂量口服愈创甘油醚、伪麻黄碱、右美沙芬、O-去甲右美沙芬的主要参数为C_max：709±298、169±27、9.64±6.36、314±96 ng/mL；C_min：48.9±25.4、50.8±13.9、5.45±5.53、110±45 ng/mL；t_max：8.27±5.71、7.64±4.99、8.27±6.57、7.55±5.99 h；AUC0_-t：5277±2212、2741±508、199±198、4964±1387 ng·h/mL；AUC0_-∞：5718±2176、2750±511、220±226、5196±1506 ng·h/mL。结论 复方愈麻美芬缓释片各成分药动学具有明显的缓释特征。

Objective To evaluate the pharmacokinetics of Compound Yumameifen Sustained-release Tablets in healthy volunteer. Methods In a randomized crossover trial, 12 healthy subjects received a single oral dose or multiple oral doses of either test tablets Compound Yumameifen Sustained-release Tablets or reference tablet. The concentrations of guaifenesin, pseudoephedrin, dextromethorphan, and O-dextrorphan in plasma were determined by LC/MS/MS method. Pharmacokinetic parameters were obtained using DAS program. Results After single oral administration of test tablets, the mean pharmacokinetic parameters of guaifenesin, pseudoephedrin, dextromethorphan, and O-dextrorphan were as follows:t_max were 1.09 ±0.42, 3.68 ±1.62, 5.05 ±2.29, 3.82 ±1.25 h; t_1/2 were 3.32 ±3.54, 6.20 ±0.97, 12.2 ±3.1, 7.60 ±0.97 h; C_max were 499 ±159, 96.1 ±12.9, 1.82 ±1.18, 142 ±34 ng/mL; AUC0_-t:2363 ±529, 1359 ±284, 31.4 ±23.6, 1504 ±242 ng·h/mL; AUC0_-∞ were 2554 ±639, 1395 ±303, 38.4 ±28.4, 1563 ±248 ng·h/mL. After multiple oral administration of test tablets, the mean pharmacokinetic parameters of guaifenesin, pseudoephedrin, dextromethorphan, and O-dextrorphan were as follows:C_max were 709 ±298, 169 ±27, 9.64 ±6.36, 314 ±96 ng/mL; C_min were 48.9 ±25.4, 50.8 ±13.9, 5.45 ±5.53, 110 ±45 ng/mL; t_max were 8.27 ±5.71, 7.64 ±4.99, 8.27 ±6.57, 7.55 ±5.99 h; AUC0_-t were 5277 ±2212, 2741 ±508, 199 ±198, 4964 ±1387 ng·h/mL; AUC0_-∞ were 5718 ±2176, 2750 ±511, 220 ±226, 5196 ±1506 ng·h/mL. Conclusion The components in Compound Yumameifen Sustained-release Tablets have the characteristic of slow releasing properties.