Pharmacokinetics of Tacrolimus(FK506) Ointment after a Single Dermal Application to the Rat.

• KAWAMURA Akio

  Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd

• IWASAKI Kazuhide

  Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd

• FUJITA Eriko

  Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd

• TERAMURA Yoshinori

  Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd

• HATA Takehisa

  Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd

抄録

The pharmacokinetics of tacrolimus (FK506) were studied in the male rat after a single dermal application of FK506 ointment over an application period of 24 hours. In the typical experiment, the amount of ointment applied was 100 mg per each rat, and application area was 10 cm². The pharmacokinetic parameters estimated were maximal blood concentration (C_max), time to reach C_max (T_max), and area under the blood concentration-time curve (AUC).<BR> 1. Blood concentrations of FK506 were determined after a single dermal application of FK506 ointment under the occlusive or non-occlusive dressing condition. After respective application of 0.5 and 0.1% FK506 ointment to the intact and damaged skin, C_max and AUC values did not differ significantly between either dressing conditions. Blood concentrations of FK506 after a single dermal application of FK506 ointment to the damaged skin were much higher than those applied to the intact skin. The bioavailability of FK506 after application of 0.5% FK506 ointment to the intact skin was 5% and that to the damaged skin was 62%.<BR> 2. After a single dermal application of 0.03, 0.1 and 0.5% FK506 ointment to the intact skin, the C_max and AUC values increased in proportion to the strength of the ointment. After a single dermal application of 0.3% FK506 ointment to 2.5, 5 and 10 cm₂ of the intact skin, the C_max and AUC values increased proportionally to the area of the skin. The C_max and AUC values did not the differ significantly after single dermal application of 10, 30, 100 and 300 mg of 0.3% FK506 ointment to the intact skin.

収録刊行物

• 薬物動態

  薬物動態 14 (1), 11-15, 1999

  日本薬物動態学会

キーワード

• Tacrolimus
• FK506
• Ointment
• Absorption
• Blood concentrations
• Single dermal application
• Rats

詳細情報

• CRID: 1390001204668616704
• NII論文ID: 10008199099
• NII書誌ID: AN10144117
• DOI: 10.2133/dmpk.14.11
• ISSN: 09161139
• Web Site: http://www.jstage.jst.go.jp/article/dmpk1986/14/1/14_1_11/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1999181720
• 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