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THE NON-LINEAR PHARMACOKINETICS OF APRINDINE IN PATIENTS AND RATS
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- SHIMIZU Mikiko
- Department of Biopharmaceutics, Meiji Pharmaceutical University
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- OGATA Hiroyasu
- Department of Biopharmaceutics, Meiji Pharmaceutical University
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- FUKUDA Tifumi
- Department of Cardiology. Sagamidai Hospital
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- KOYAMA Kazuko
- Department of Pharmacy, Sagamidai Hospital
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- HANADA Miki
- Department of Pharmacy, Sagamidai Hospital
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- KURODA Keiko
- Department of Pharmacy, Sagamidai Hospital
Bibliographic Information
- Other Title
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- 抗不整脈薬アプリンジンの非線形体内動態
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Description
Although aprindine (AP), an anti-arrhythmic drug, had been shown to follow a non-linear pharmacokinetics in human subjects with a very large inter-subject variability, the metabolic pathways contributing the non-linear pharmacokinetic disposition of AP have not been clarified yet. Pharmacokinetics of AP and its metabolites, p-OHAP, i-OHAP and DEAP, was studied in seven arrhythmic patients administering 20mg to 60mg of AP every 12 hour for 2 weeks, and was evaluated the non-linearity using a mixed effect model analysis. The partial formation clearances of i-OHAP and p-OHAP from AP showed AP dose dependency. Metabolic parameters for formation of metabolites, p-OHAP, i-OHAP and DEAP from AP were obtained using human and rat liver microsomes, and compared. Lower capacities and higher affinities of i-OHAP and p-OHAP formations shown in human microsomes reasonably described of the non-linearity of AP disposition in humans.
Journal
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- Drug Metabolism and Pharmacokinetics
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Drug Metabolism and Pharmacokinetics 13 (supplement), 92-93, 1998
The Japanese Society for the Study of Xenobiotics
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Details 詳細情報について
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- CRID
- 1390282679646613248
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- NII Article ID
- 10007629646
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- NII Book ID
- AN10144117
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- ISSN
- 09161139
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- Text Lang
- en
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- Data Source
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- JaLC
- Crossref
- CiNii Articles
- OpenAIRE
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- Abstract License Flag
- Disallowed