NDLI: Pharmacokinetic Differences between Pantoprazole Enantiomers in Rats

Content Provider	Springer Nature Link
Author	Xie, Zhiyong Zhang, Yini Xu, Haiyan Zhong, Dafang
Copyright Year	2005
Abstract	The purpose of this study was to quantitatively clarify the contribution of the absorption, protein binding, and metabolism of cytochrome P450 enzymes to the enantioselective pharmacokinetics of pantoprazole enantiomers in rats.The enantioselective pharmacokinetics of pantoprazole enantiomers was estimated by an oral administration of racemic pantoprazole to rats. The pharmacokinetic differences between pantoprazole enantiomers were evaluated by the experiments of the in situ perfusion into rat small intestine, the protein binding, and the in vitro metabolism in rat liver microsomes of pantoprazole enantiomers.The mean area under the curve value of S-pantoprazole was 1.5 times greater than that of R-pantoprazole after administration of racemic pantoprazole to rats (20 mg/kg, p.o.). There were significant differences in k$_{e}$ (p < 0.05), t$_{1/2}$ (p < 0.01), and mean residence time (p < 0.01) values between the two enantiomers. In the in situ absorption study, the absorption rate constants were of no significant differences between the two enantiomers. The mean unbound fraction of R-pantoprazole was slightly greater than that of S-pantoprazole. The intrinsic clearance (CL$_{int}$) of the formation of the 5′-O-demethyl metabolite from S-pantoprazole was 4-fold lower than that from R-pantoprazole. However, the CL$_{int}$ value for the sulfone and 6-hydroxy metabolites from S-pantoprazole was higher than that from R-pantoprazole. The sum of the CL$_{int}$ of the formation of all three metabolites was 3.06 and 4.82 mL/min/mg protein for S- and R-pantoprazole, respectively.This study suggests that the enantioselective pharmacokinetics of pantoprazole enantiomers in rats is probably ascribable to their enantioselective metabolism, which is contributed by all the three metabolic pathways, including sulfoxide oxidation, 4′-O-demethylation, and 6-hydroxylation.
Starting Page	1678
Ending Page	1684
Page Count	7
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	22
Issue Number	10
e-ISSN	1573904X
Language	English
Publisher	Springer-Verlag
Publisher Date	2005-09-22
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	enantiomer enantioselectivity metabolism pantoprazole pharmacokinetics Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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