摘要
目的研究呋喃唑酮对兰索拉唑及其代谢产物在大鼠体内药动学参数的影响。方法采用HPLC-MS/MS测定与呋喃唑酮联用前后兰索拉唑、5-羟基兰索拉唑及其兰索拉唑砜的血药浓度,以DAS2.0程序拟合药动学参数。结果单次联用呋喃唑酮后,兰索拉唑的AUC值显著增加,从(487.33±122.40)增至(779.82±126.67)μg.L-1.h(P<0.05),兰索拉唑砜与兰索拉唑AUC0-4 h的比值显著降低,从(0.70±0.34)降至(0.33±0.09)(P<0.05)。结论呋喃唑酮与兰索拉唑合用后,可显著增加兰索拉唑的生物利用度。
OBJECTIVE To evaluate the effect of furazolidone on the pharmacokinetics of lansoprazole in rats. METHODS Plas- ma concentrations of lansoprazole and its metabolites, 5-hydroxylansoprazole and lansoprazole sulfone, were determined by HPLC-MS/ MS, and the pharmacokinetic parameters were calculated. RESULTS The pharmacokinetic parameters showed that furazolidone （40 mg. kg -1 ） remarkably increased the AUC0.4 L, of lansoprazole from （487.33 ＋ 122. 40） to （779. 82 ＋ 126. 67 ） remarkably （ P 〈 0. 05）, and significantly decreased the AUC0.4h ratios of lansoprazole sulfone/lansoprazole from （0. 70 ＋0. 34） to （0. 33 ＋0. 09） （P 〈 0. 05）. CONCLUSION Furazolidone inhibits the metabolism of lansoprazole via CYP3A4, and consequently improves the bioavailability of lansoprazole.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2012年第6期458-461,共4页
Chinese Pharmaceutical Journal
