Pharmacokinetic and Pharmacodynamic Properties of Lafutidine after Postprandial Oral Administration in Healthy Subjects: Comparison with Famotidine
Biological and Pharmaceutical Bulletin 30 巻 5 号
1003-1006 頁
2007-05 発行
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| ファイル情報(添付) | |
| タイトル ( eng ) |
Pharmacokinetic and Pharmacodynamic Properties of Lafutidine after Postprandial Oral Administration in Healthy Subjects: Comparison with Famotidine
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| 作成者 |
Shimatani Tomohiko
Hayato Seiichi
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| 収録物名 |
Biological and Pharmaceutical Bulletin
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| 巻 | 30 |
| 号 | 5 |
| 開始ページ | 1003 |
| 終了ページ | 1006 |
| 抄録 |
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.
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| 著者キーワード |
lafutidine
famotidine
pharmacokinetics
pharmacodynamics
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| NDC分類 |
医学 [ 490 ]
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| 言語 |
英語
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| 資源タイプ | 学術雑誌論文 |
| 出版者 |
The Pharmaceutical Society of Japan
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| 発行日 | 2007-05 |
| 権利情報 |
© 2007 Pharmaceutical Society of Japan
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| 出版タイプ | Version of Record（出版社版。早期公開を含む） |
| アクセス権 | オープンアクセス |
| 収録物識別子 |
[ISSN] 0918-6158
[ISSN] 1347-5215
[NCID] AA10885497
[DOI] 10.1248/bpb.30.1003
[DOI] https://doi.org/10.1248/bpb.30.1003
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