Pharmacokinetic and Pharmacodynamic Properties of Lafutidine after Postprandial Oral Administration in Healthy Subjects : Comparison with Famotidine(Biopharmacy)
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概要
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Lafutidine, a histamine H_2-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 Iafutidine 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 E_<max> 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), Iafutidine 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.
- 公益社団法人日本薬学会の論文
- 2007-05-01
著者
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Ikawa Kazuro
Department Of Clinical Pharmacotherapy Graduate School Of Biomedical Sciences Hiroshima University
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MORIKAWA Norifumi
Department of Clinical Pharmacotherapy, Division of Clinical Pharmacotherapeutics, Graduate School o
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TAZUMA SUSUMU
Department of General Medicine, Division of Clinical Pharmacotherapeutics, Graduate School of Biomed
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SHIMATANI Tomohiko
Department of General Medicine, Hiroshima University Hospital
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HAYATO Seiichi
Department of Clinical Pharmacotherapy, Hiroshima University
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Shimatani Tomohiko
Department Of General Medicine Hiroshima University
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Morikawa Norifumi
Department Of Clinical Pharmacotherapy Graduate School Of Biomedical Sciences Hiroshima University
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Morikawa N
Department Of Clinical Pharmacotherapy Hiroshima University
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Tazuma Susumu
Department Of Genaral Medicine Hiroshima University Hospital
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Hayato Seiichi
Department Of Clinical Pharmacotherapy Hiroshima University
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Ikawa Kazuro
Department Of Clinical Pharmacotherapy Hiroshima University
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Ikawa Kazuro
Department Of Clinical Pharmacotherapy Division Of Clinical Pharmacotherapeutics Graduate School Of
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TAZUMA Susumu
Department of General Medicine, Hiroshima University
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