Improved Solubility and Dissolution of Ibuprofen Tablet Formulations by the Co-Crystal Technique

Abstract

Background and Aims: Co-crystallization technique greatly impacts the solubility and dissolution of drugs such as ibuprofen. In this study, we aimed to evaluate the effect of different coformers in improving the solubility and dissolution of ibuprofen. Methods: Preparation was by the solvent evaporation method using benzoic acid, saccharin, and aerosil as coformers in a stoichiometric ratio of 1:1 (drug:coformer). The resulting products prepared with benzoic acid as conformer (IBA), those prepared with saccharin as coformer (ISA) and the ones prepared with aerosil as coformer (IAR) were evaluated for flow properties and saturated solubility. Fourier Transform InfraRed (FT-IR) and differential scanning calorimetry (DSC) studies were also carried out. The co-crystals were compacted into tablets (CT1, CT2, and CT3) and evaluated for uniformity of weight, tablet hardness, friability, disintegration time, and in vitro dissolution. Results: IBA exhibited superior solubility over all other batches, and it also gave the highest drug content (56.73 %). FT-IR showed no interaction and DSC thermograms revealed a decrease in the peak melting temperature of all co-crystals. All the co-crystal preparations had poor flow and poor compressibility. The tablet hardness was between 4.5 and 5.0 kgF, and the friability range was 0.51-1.22 % with CT3 being the most friable. CT1 disintegrated fastest, while CT2 had the longest disintegration time. All co-crystal tablets had higher dissolution rates than the pure ibuprofen tablet formulation in the order CT1>CT3>CT2. The mechanism of release was by non-fickian diffusion, and statistical evaluation showed the dissolution profiles of the co-crystal tablet formulations to be significantly different from that of the pure ibuprofen formulation.

Keywords

• Aerosil
• Benzoic Acid
• Co-Crystals
• Dissolution
• Ibuprofen
• Saccharin

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