Physicochemical profile and in vitro permeation behavior of a new class of non-steroidal anti-inflammatory drug candidates

Eur J Pharm Sci. 2010 Jun 14;40(3):217-21. doi: 10.1016/j.ejps.2010.03.015. Epub 2010 Mar 25.

Abstract

Recently a new series of nitrooxy-acyl derivatives of salicylic acid (SA) was described presenting similar anti-inflammatory activities but reduced or no gastrotoxicity compared to aspirin. In this work, lipophilicity and permeability profiles of SA derivatives were performed to evaluate their ADME properties related to oral or transdermic delivery. All tested compounds showed potential good passive permeation through gastrointestinal track and also through percutaneous barrier which could be a way to avoid the first hepatic pass.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Aspirin / analogs & derivatives*
  • Chemical Phenomena
  • Drug Evaluation, Preclinical
  • Humans
  • Intestinal Absorption
  • Membranes, Artificial
  • Nitric Oxide Donors / administration & dosage
  • Nitric Oxide Donors / chemistry
  • Nitric Oxide Donors / pharmacokinetics
  • Permeability
  • Potentiometry
  • Skin Absorption

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Membranes, Artificial
  • Nitric Oxide Donors
  • Aspirin