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研究了8名中国健康男性受试者单剂量口服奥美拉唑(omeprazole,OPZ)胶囊20mg后(-)OPZ和(+)OPZ在体内药代动力学的立体选择性规律.用手性固定相HPLC法,测定了服药后05,1.0,1.5,2.0,3.0,4.0,6.0h不同时刻血浆中(-)和(+)对映异构体的浓度刻,绘了相应的浓度时间曲线,并求出主要药代动力学参数.结果表明,不同时刻血浆中(-)OPZ的浓度始终高于(+)OPZ.OPZ对映异构体的AUC及Cmax比值(-)/(+)分别为(1.589±0.201)和(1.458±0.228),其药代动力学具有明显的立体选择性(P<0.05).
The stereoselectivity of pharmacokinetics of (-) OPZ and (+) OPZ in vivo in vivo was studied after oral administration of 20 mg omeprazole (OPZ) capsule to 8 Chinese healthy male subjects. The chiral stationary phase HPLC method was used to determine the plasma levels of (-) and (+) at different time points of 05,1.0,1.5,2.0,3.0,4.0,6.0h after treatment, ) enantiomer concentration moment, plot the corresponding concentration time curve, and find out the main pharmacokinetic parameters. The results showed that the concentrations of (-) OPZ in plasma at different time points were always higher than (+) OPZ. The AUC and Cmax ratios of OPZ enantiomers were (1.589 ± 0.201) and (1.458 ± 0.228), respectively. The pharmacokinetics of OPZ enantiomers showed obvious stereoselectivity (P <0.05).