目的 研究復(fù)方愈麻美芬緩釋片單劑量和多劑量給藥在健康志愿者體內(nèi)的藥動(dòng)學(xué)規(guī)律。方法 采用自身對(duì)照的雙周期交叉試驗(yàn)設(shè)計(jì)，12名健康受試者單次和多次口服受試制劑復(fù)方愈麻美芬緩釋片或相應(yīng)的參比制劑，不同時(shí)間點(diǎn)收集血樣，采用LC/MS/MS法測(cè)定血漿中愈創(chuàng)甘油醚、偽麻黃堿、右美沙芬和O-去甲右美沙芬的濃度。藥動(dòng)學(xué)參數(shù)采用DAS軟件處理獲得。結(jié)果 單劑量口服受試制劑后，愈創(chuàng)甘油醚、偽麻黃堿、右美沙芬、O-去甲右美沙芬的主要參數(shù)為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。多劑量口服愈創(chuàng)甘油醚、偽麻黃堿、右美沙芬、O-去甲右美沙芬的主要參數(shù)為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。結(jié)論 復(fù)方愈麻美芬緩釋片各成分藥動(dòng)學(xué)具有明顯的緩釋特征。

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.