Departamento de Química, Universidade Federal de São Carlos, São Carlos, São Paulo, Brazil.
Chirality. 2012 Apr;24(4):289-93. doi: 10.1002/chir.21995. Epub 2012 Feb 17.
This work reports the result of the enantioselective disposition of pantoprazole, omeprazole, and lansoprazole in a same group of Brazilian health subjects. Ten nongenotyped healthy subjects were used for this study. Each subject received a single oral dose of 80 mg of pantoprazole, 40 mg of omeprazole, and 30 mg of lansoprazole, and the plasma concentrations of the enantiomers were measured for 8 h postdose. For pantoprazole and omeprazole, among the 10 volunteers investigated, only one volunteer (Subject # 4) presented higher plasma concentrations of the (+)-enantiomer than those of (-)-enantiomer. Nevertheless, the area under the concentration-time curve of the (+)-lansoprazole was higher than those the (-)-lansoprazole for all subjects. The comparison of proton pump inhibitors' enantiomers disposition from a single group volunteer demonstrated that pantoprazole and omeprazole can be used to differentiate extensive from poor CYP2C19 metabolizer while lansoprazole cannot do it.
这项工作报道了同一组巴西健康受试者中泮托拉唑、奥美拉唑和兰索拉唑对映体处置的结果。本研究使用了 10 名非基因分型的健康受试者。每位受试者接受了 80 毫克泮托拉唑、40 毫克奥美拉唑和 30 毫克兰索拉唑的单次口服剂量，并在给药后 8 小时测量了对映体的血浆浓度。对于泮托拉唑和奥美拉唑，在所研究的 10 名志愿者中，只有一名志愿者（受试者 #4）表现出 (+)-对映体的血浆浓度高于 (-)-对映体。然而，所有受试者的 (+)-兰索拉唑的浓度-时间曲线下面积均高于 (-)-兰索拉唑。从单一志愿者组比较质子泵抑制剂对映体的处置表明，泮托拉唑和奥美拉唑可用于区分广泛代谢型和弱 CYP2C19 代谢型，而兰索拉唑则不能。
