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- 山崎 浩子
- アベンティスファーマ株式会社研究開発本部開発研究所薬物動態研究室
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- Roeder V
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Vicat P
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Bonnat C
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Rainbeaud M
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Mauriac C
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Laplace H
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Jaulin F
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Haegele KD
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Meili M
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Labbe G
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Abecassis P-Y
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Flor M
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Fougeat S
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Dupront A
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Coussediere D
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
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- Lenfant B
- Department of Drug Metabolism and Pharmacokinetics, Aventis Pharma
書誌事項
- タイトル別名
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- Pharmacokinetic studies of telithromycin in mouse, rat and dog
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抄録
The studies on absorption, distribution, metabolism and excretion of telithromycin (TEL) were carried out in mouse, rat and dog using 14C-TEL. Absorption rates after oral dosing were 47% in mouse and rat, 83% in dog, and bioavailability in these animals were 53, 36 and 54%, respectively. The first pass effect observed was low and moderate in rat and dog respectively, but none observed in mouse. Tmax of these animals were from 0.25 to 2 h, and suggested that TEL will be absorbed from small intestine to large intestine. The volume of distribution in mouse, rat and dog after intravenous dosing were 1.41, 10.62 and 4.9 L/kg, respectively, and total clearance of these animals were 0.80, 4.36 and 1.5 L/h/kg, respectively. The terminal plasma half-life of these animals were form 1.2 to 2.3 h. After single oral administration of doses ranging between 5 and 20mg/kg in rat, Cmax and AUC were increased dose dependently, but these increments were more than the dose-ratio and indicated a non linear pharmacokinetic profile. In rats after oral dosing, higher concentration of radioactivity in most of the tissues was measured than that in plasma, except for central nervous system. All of the radioactivity found in tissues were rapidly decreased from 6h after administration, and almost total elimination of radioactivity from the body's tissues were observed within 24 h of administration. Throughout the study, the fact that high concentration of radioactivity was detected in intestinal wall suggested probable secretion of radioactivity from the blood compartment to the lumina of the gastrointestinal tract. In vitro serum protein binding studies, TEL was bound to mouse serum protein about 90%, but was weakly bound to that of rat and dog (less than 70%). In the studies rat and dog, TEL accounted for 70.7-72.5% of plasma radioactivity in rat and dog. Its metabolites in plasma of rat were below the limit of quantification (0.005 mg eq./L), but in dog plasma, RU 76584 (N-oxidepyridine)
収録刊行物
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- 日本化学療法学会雑誌
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日本化学療法学会雑誌 51 (Supplement1), 182-199, 2003
公益社団法人 日本化学療法学会
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詳細情報 詳細情報について
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- CRID
- 1390282681267126272
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- NII論文ID
- 10012659419
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- NII書誌ID
- AN10472127
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- ISSN
- 18845886
- 13407007
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可