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  • 标题:Pharmacokinetics of Propranolol and Its Metabolites in Horses after Intravenous or Oral Administration
  • 本地全文:下载
  • 作者:Sugako ARAMAKI ; Miwako MORI ; Masayuki NAKATA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2000
  • 卷号:23
  • 期号:11
  • 页码:1333-1340
  • DOI:10.1248/bpb.23.1333
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The pharmacokinetics characteristics of propranolol (PPL) in horses was studied by administering the drug intravenously or orally to the animals. The predominant primary pathway was ring oxidation, and 4-hydroxypropranolol glucuronide (4-OHPG) was the major metabolite in both plasma and urine. Side-chain glucuronidation and oxidation were not significant. A two-compartment model was employed for PPL followed by a one-compartment model for 4-OHPG. After oral administration, one-step absorption and two-step first pass metabolism were employed. The fraction absorbed of PPL was approximately 70% after oral administration, and the bioavailability varied among individual horses from 1 to 79% depending on the first pass metabolism. The biologic half-life (T1/2) of PPL obeys the allometric equation in some animal species including rats and horses, except for human. T1/2 of PPL in horses was approximately 2 h.
  • 关键词:pharmacokinetics;horse;propranolol;4-hydroxypropranolol;first pass metabolism
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