Transdermal bioavailability and first-pass skin metabolism: A preliminary evaluation with nitroglycerin

Emi Nakashima, Patrick K. Noonan, Leslie Z. Benet

研究成果: Article査読

30 被引用数 (Scopus)

抄録

A model comprising six compartments, a systemic and presystemic compartment for nitroglycerin and each of its two dinitrate metabolites is presented to describe the interrelationships between plasma concentrations of the two metabolites and metabolism in skin after intravenous and transdermal ointment administration of nitroglycerin. Using a perfusion-limited pharmacokinetic model, the equation for the calculation of the fraction (F)of the dose of nitroglycerin systemically available from skin was derived independent of nitroglycerin plasma concentrations. Estimated F values (0.68-0.76) are comparable to values reported in Rhesus monkeys (0.80-0.84). Simulated plasma concentration-time profiles were reasonably fitted to the observed concentrations of nitroglycerin and its two metabolites after transdermal administration. This preliminary model suggests that transdermal bioavailability for a drug metabolized in the skin can be reasonably estimated.

本文言語English
ページ(範囲)423-437
ページ数15
ジャーナルJournal of Pharmacokinetics and Biopharmaceutics
15
4
DOI
出版ステータスPublished - 1987 8月

ASJC Scopus subject areas

  • 薬理学、毒性学および薬学(全般)
  • 薬理学(医学)

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