Evaluation of a Non-aqueous Ibuprofen-Phospholipid Complex Formulation in Rats

In Vivo. 2016 Jul-Aug;30(4):479-83.

Abstract

Aim: In the present study, a non-aqueous ibuprofen-phospholipid complex was developed to reduce the gastrointestinal (GI) toxicity of ibuprofen.

Materials and methods: A non-aqueous ibuprofen-phospholipid complex (IBU-PC) was prepared by mixing phosal-35SB and ibuprofen. In vitro release behavior was studied using a dissolution apparatus. Irritation to gastrointestinal (GI) tract and pharmacokinetics of IBU-PC were studied in rats.

Results: Rapid release of drug occurred with approximately 85% of ibuprofen released from the composition within the first 30 min. The GI injury in IBU-PC-treated rats was minimal compared to those of Advil Liqui-gels-treated group. There was no significant difference between IBU-PC and Motrin-treated groups. The area under the concentration-time curve (AUC0~24) of IBU-PC and Motrin were 366±115 and 391±105 μg/h/ml, respectively. The relative bioavailability of IBU-PC was 94.2%.

Conclusion: IBU-PC can decrease GI adverse reaction induced by ibuprofen.

Keywords: Phosal-35SB; Phospholipid; drug delivery; gastrointestinal toxicity; ibuprofen; nonsteroidal anti-inflammatory agents; oral formulation; pharmacokinetics.

Publication types

  • Evaluation Study

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Biological Availability
  • Drug Compounding*
  • Gastrointestinal Absorption
  • Gastrointestinal Tract / metabolism*
  • Ibuprofen / chemistry
  • Ibuprofen / pharmacokinetics*
  • Male
  • Phospholipids / chemistry*
  • Rats
  • Rats, Sprague-Dawley
  • Therapeutic Equivalency

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Phospholipids
  • Ibuprofen