右旋泮托拉唑在人体内构型转化的研究右旋泮托拉唑在人体内构型转化的研究
Studies on chiral inversion of dextropantoprazole in human
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摘要: 目的研究右旋泮托拉唑在健康人体内的构型转化。方法志愿者单剂量口服右旋泮托拉唑肠溶胶囊后,采集血浆样品,用HPLC法测定血浆中泮托拉唑两对映体总浓度,再用α1-酸糖蛋白手性柱分离泮托拉唑对映体,测定其色谱峰面积比值,计算得到右旋和左旋泮托拉唑血浆浓度。结果左旋泮托拉唑的平均AUC0-t不超过泮托拉唑AUC0-t的1.5%。结论中国健康志愿者口服右旋泮托拉唑后,在体内不发生构型转化。Abstract: AimTo study the chiral inversion of dextropantoprazole in human. MethodsThree healthy Chinese male volunteers after an oral dose of 40 mg dextropantoprazole. An HPLC method was developed and used to determine the total plasma concentrations of each enantiomer. The ratios of the enantiomers in plasma samples were measured on a Chiral-AGP column. The plasma concentration of each enantiomer was then calculated using the ratios of enantiomers and total concentrations of the two enantiomers previously measured. ResultsThe AUC0-t of levopantoprazole was only 1.5% of the total AUC0-t of enantiomers. ConclusionThe chiral inversion from dextropantoprazole to levopantoprazole does not occur in the three healthy Chinese male volunteers after an oral dose of 40 mg dextropantoprazol.
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