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ID 47054
file
creator
Shimatani, Tomohiko
Hayato, Seiichi
subject
lafutidine
famotidine
pharmacokinetics
pharmacodynamics
NDC
Medical sciences
abstract
Lafutidine, a histamine H2-receptor antagonist, inhibits gastric acid secretion during the daytime, however, the relationship between the plasma concentration and the drug response remains unclear. The aim of this study was to compare the pharmacokinetic and pharmacodynamic properties of lafutidine and famotidine following postprandial oral administration. After a lafutidine tablet (10 mg), famotidine tablet (20 mg), or water only (control) was administered, blood samples were taken and intragastric pH was measured. The plasma concentrations of lafutidine and famotidine were determined by HPLC, and the median intragastric pH values per 30 min were used as the degrees of gastric acid suppression. Data were analyzed based on a one-compartment pharmacokinetic model and a sigmoid Emax pharmacodynamic model. Lafutidine plasma concentrations rapidly increased after administration; famotidine required some time to increase the plasma concentrations, requiring an absorption lag time in the pharmacokinetic model. Between the plasma concentration and ΔpH (the difference in intragastric pH by the drug vs. control), lafutidine showed an anticlockwise hysteresis loop which indicated equilibration delay between the plasma concentration and effect site, requiring an effect site compartment in the pharmacodynamic model; famotidine showed more parallel relationship. These results indicated that the pharmacokinetic and pharmacodynamic properties of lafutidine after postprandial oral administration were different from those of famotidine at least 4.5 h after dosing.
journal title
Biological and Pharmaceutical Bulletin
volume
Volume 30
issue
Issue 5
start page
1003
end page
1006
date of issued
2007-05
publisher
The Pharmaceutical Society of Japan
issn
0918-6158
1347-5215
ncid
publisher doi
language
eng
nii type
Journal Article
HU type
Journal Articles
DCMI type
text
format
application/pdf
text version
publisher
rights
© 2007 Pharmaceutical Society of Japan
relation url
department
Graduate School of Biomedical & Health Sciences
University Medical Hospital



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