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.
Copyright © 2016 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.