European Journal of Biomedical and Pharmaceutical Sciences

SALT AND NON-SALT FORMING EXCIPIENTS TO IMPROVE THE DISSOLUTION OF DEXIBUPROFEN; FORMULATION OF CHEWABLE TABLETS

Dalia Naeem*, Mohamed Osman, Gamal El Maghraby, Ebtessam Essa

ABSTRACT

Dexibuprofen is a stronger non-steroidal anti-inflammatory drug than ibuprofen but with less gastric damage. However, it suffers poor aqueous solubility. This work improved Dexibuprofen dissolution via co-processing with inert excipients with the aim of formulating chewable tablets. Wet co-grinding of Dexibuprofen with increasing proportions of mannitol or meglumine was performed after liberation from their ethanolic solutions. The prepared mixtures were investigated using differential scanning calorimetry, Fourier Transform Infrared spectroscopy, powder X-ray diffraction and dissolution behavior. Optimum co-processed mixtures were prepared into chewable tablets after addition of suitable additives. Wet co-grinding improved drug dissolution parameters compared to unprocessed one, with meglumine being superior to mannitol. Solid state characterizations reflected possible salt formation between the drug and meglumine. For mannitol mixtures, dissolution enhancement was attributed to partial amorphousization of Dexibuprofen along with particle size reduction. The selected co-processed mixtures were successively formulated into chewable tablets. In vitro dissolution studies were performed using crushed as well as intact tablets. Mannitol based tablets showed prompt drug release in both cases. However, meglumine based tablets required crushing for fast drug release indicating the need for chewing. The study introduced simple co-processing as a tool to enhance dissolution rate of Dexibuprofen with subsequent formulation of chewable tablets.

Keywords: Dexibuprofen, mannitol, meglumine, salt form, co-grinding.