Studies on the Metabolic Fate of Lamivudine (III): Absorption, Metabolism and Excretion of Lamivudine in Dogs.

• TAKUBO Takatoshi

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

• MORIYA Takahito

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

• MINAMIDE Yoshiyuki

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

• HIRAYAMA Seiji

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

• KATO Toshihiro

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

• NAKAMURA Ryoko

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

• KINAMI Junji

  ADME Section, Pre-clinical Research Department, Tsukuba Research Laboratories, Nippon Glaxo Ltd.

抄録

The absorption, metabolism and excretion of nucleoside analogue, lamivudine, were investigated after a single oral administration of ³H-lamivudine to male and female dogs at a dose of 2 mg/kg.<BR> 1. The total radioactivity in plasma reached the maximum at 0.9 hour after oral administration to male dogs and declined rapidly with a half-life of 2.9 hours. The concentrations of lamivudine in plasma reached the maximum at 0.8 hour after oral administration and declined with a half-life of 1.4 hours. Profiles of the plasma levels of total radioactivity or lamivudine in female dogs were similar to those in male dogs.<BR> 2. The ratio of plasma protein binding of radioactivity was below 17% and the ratio of distribution to erythrocytes of radioactivity was 35-38%, after oral administration to male dogs.<BR> 3. The excreted radioactivity in urine and feces was 85.3% and 9.5% of the dose in male dogs, respectively, 93.2% and 5.8% in female dogs within 168 hours after oral administration.<BR> 4. Lamivudine and two major metabolites, trans-sulphoxide of lamivudine and cytosine, were observed by the radio-HPLC analysis of urine collected from male and female dogs after oral administration.

収録刊行物

• 薬物動態

  薬物動態 12 (2), 102-107, 1997

  日本薬物動態学会

キーワード

• Lamivudine
• Dogs
• Absorption
• Metabolism
• Excretion

詳細情報

• CRID: 1390282679644611200
• NII論文ID: 10007530761
• NII書誌ID: AN10144117
• DOI: 10.2133/dmpk.12.102
• ISSN: 09161139
• Web Site: http://www.jstage.jst.go.jp/article/dmpk1986/12/2/12_2_102/_pdf
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可