Studies on the Metabolic Fate of D0870, a New Triazole Antifungal Agent: Tissue Distribution of Radioactivity and Unchanged Compound in Rats after Single and Multiple Oral Administration of (14C)D0870.

• NAKAJIMA Hiroyuki

  Drug Metabolism and Pharmacokinetics Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd

• NAKANISHI Takeshi

  Drug Metabolism and Pharmacokinetics Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd

• NASA Hiroyasu

  Drug Metabolism and Pharmacokinetics Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd

• OHZAWA Nobuo

  Drug Metabolism and Pharmacokinetics Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd

Bibliographic Information

Other Title

• 新規トリアゾール系抗真菌薬Ｄ０８７０の生体内動態　［｀１４´Ｃ］Ｄ０８７０を単回および反復経口投与した時のラット組織分布

Abstract

Tissue distribution of total radioactivity and the unchanged compound was studied following a single and multiple oral administration of [¹⁴C]D0870 to rats.<BR> 1. Tissue levels of radioactivity after a single oral administration to male rats reached the maximum level within 6 hours, then decreased to undetectable level in most tissues within 168 hours after dosing. The tissue levels of radioactivity much exceeded the corresponding plasma level in the liver, adrenal, kidney, lung and other tissues.<BR> 2. The distribution of radioactivity in female rats showed a similar pattern to that in male rats. Slight sex differences were observed in liver and adrenal level.<BR> 3. Tissue levels of radioactivity in male rats at 24 hours after a daily oral administration for 7 days were much higher than those after a single administration, while those after daily administration for 14 and 21 days were close to those after a daily administration for 7 days.<BR> 4. The levels of radioactivity in male rats after a daily administration for 21 days reached the maximum level in most tissues at 6 hours, then declined slower than in the case of single administration study.<BR> 5. The most part of radioactivity in plasma and main tissues after both single and multiple administration was composed of the unchanged compound.

Journal

• Drug Metabolism and Pharmacokinetics

  Drug Metabolism and Pharmacokinetics 13 (6), 557-565, 1998

  The Japanese Society for the Study of Xenobiotics

Keywords

• D0870
• Antifungal
• Rat
• Distribution

Details

• CRID: 1390282679645154176
• NII Article ID: 130003560999
• NII Article ID: 10008199045
• NII Book ID: AN10144117
• DOI: 10.2133/dmpk.13.557
• ISSN: 09161139
• Web Site: http://www.jstage.jst.go.jp/article/dmpk1986/13/6/13_6_557/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1999110641
• Text Lang: ja
• Data Source:
  • JaLC
  • Crossref
  • CiNii Articles
• Abstract License Flag: Disallowed