Formulation and Evaluation of fast-dissolving tablets of Aceclofenac using Solid Dispersion methods

Abstract

Aceclofenac is a novel non-steroidal anti-inflammatory medication that functions by preventing prostaglandin formation by inhibiting the activity of the cyclooxygenase 2 (COX-2) enzyme. Compared to COX-1, it is more selective for COX-2. Aceclofenac reaches its peak blood level 1.25 to 3 hours after oral dosing and is essentially insoluble in water. It is essentially insoluble in water-based solutions. The rate-limiting phase in the medication absorption process is dissolution in the case of medicines that are poorly soluble in water. Several studies have successfully used the solid dispersion technique to increase the solubility and dissolution rates of medications that are poorly soluble in water, which in turn increases the drugs' bioavailability. Aceclofenac's dissolution can be enhanced by optimizing the solid dispersion in a fast-dissolving tablet formulation and by employing melt solvent technologies to formulate solid dispersions using water-soluble carriers such as mannitol. Within 30 minutes, the prepared tablets demonstrated efficient and quick drug dissolution in vitro. Using solid drug dispersion to formulate fast-dissolving tablets would increase medication solubility and, in turn, bioavailability while also enhancing patient compliance and convenience. Various weight ratios between the medicine and carrier were measured, including 1:1, 1:2, 1:3, 1:4, and 1:5. The drug's solubility was assessed in formulations with SD and physical mixtures. The optimized SD formulation of the medication and carrier, along with superdisintegrants such as sodium starch glycolate, croscarmellose sodium, and crospovidone, was used to create fast-dissolving ACE tablets. It was determined by IR and DSC experiments that the medication changed from its crystalline form to an amorphous state during the creation of SD. The quickest in vitro drug release (92.2%) and fastest disintegration (39s). We demonstrated by fast-dissolving tablets containing 20% crospovidone as super-disintegrants. We conclude that a promising method for producing effective, quickly dissolving Aceclofenac tablets is the combination of solid dispersion with superdisintegrants.