Dissolution characterization of compounded ibuprofen-containing tablet formulations for potentially faster pain relief: the effects of disintegrants

Ibuprofen is one of the most commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) to alleviate pain and inflammation. Faster disintegration and consequently dissolution of an ibuprofen-containing oral tablet is expected to speed up relief from pain and/or inflammation. The purpose of this study was to 1) compound series of ibuprofen-containing tablet formulations for oral administration with varied types and amounts of disintegrants and 2) thoroughly evaluate ibuprofen’s dissolution rates and extents from those formulations compared to a commercially available tablet. United States Pharmacopeia (USP) type II dissolution apparatus was implemented in the dissolution studies where samples were collected at predetermined time points and analyzed for ibuprofen content using a validated High Performance Liquid Chromatography (HPLC) method. Statistical analyses of dissolution results were performed based on single-factor ANOVA. Three of the six compounded formulations; ones with starch 5%, starch 20% and microcrystalline cellulose (MCC) 10% as the disintegrants, demonstrated higher rates of dissolution compared to the commercial product (p< 0.0003, 0.0032 and 0.0043, respectively). For dissolution extents, two formulations; ones with MCC 20% and hypromellose 2910 USP (E4M) 5% as the disintegrants, showed enhancement over commercial tablet (p< 0.001 and 0.0103, respectively). These results demonstrate the feasibility of compounding ibuprofen-containing tablets for oral administration with enhanced dissolution characteristics over a commercially available tablet, thereby potentially reducing time to pharmacologic effect. More importantly, our results demonstrate that sound formulation optimization of a compounded tablet formula can be directly guided by in vitro dissolution evaluations.