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Interspecies comparison of the oral absorption of itraconazole in laboratory animals

  • Sun Dong Yoo
  • Eunhee Kang
  • Beom Soo Shin
  • Hun Jun
  • Sang-Heon Lee
  • Kang Choon Lee
  • Kyu-Hyun Lee
Research Articles Articles

Abstract

The oral absorption and disposition of itraconazole were studied in rats, rabbits and dogs. Serum levels of itraconazole and its active metabolite, hydroxyitraconazole, were determined by a validated HPLC method. The absorption of itraconazole was relatively rapid in rats and dogs but was slower in rabbits. The terminal elimination half-life (T1/2λz), time to the peak con-centration (Tmax), dose and weight normalized area under the curve (AUC) and the peak concentration (Cmax) of itraconazole found in the dog were comparable to those reported in humans. As in humans, the metabolite to parent drug AUC ratios in rats and dogs were greater than unity but was less in rabbits. The dog appears to be an appropriate animal model while the rat, not the rabbit, may be used as an alternative animal model in predicting the oral absorption of itraconazole in humans.

Key words

Itraconazole Pharmacokinetics Absorption Hydroxyitraconazole 

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Copyright information

© The Pharmaceutical Society of Korea 2002

Authors and Affiliations

  • Sun Dong Yoo
    • 1
  • Eunhee Kang
    • 1
  • Beom Soo Shin
    • 1
  • Hun Jun
    • 1
  • Sang-Heon Lee
    • 2
  • Kang Choon Lee
    • 1
  • Kyu-Hyun Lee
    • 2
  1. 1.College of PharmacySungkyunkwan UniversitySuwonKorea
  2. 2.Formulation Research LaboratoryChoongwae Pharma Co.Taean-up, HwasungkunKorea

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