Abstract

SOLUBILITY ENHANCEMENT OF A POORLY SOLUBLE DRUG AND DEVELOPMENT INTO DIRECTLY COMPRESSIBLE TABLETS AND OPTIMISATION AND EVALUATION

Athulia S.*, Dr. Vinaya O. G., Mufeeda P.

ABSTRACT

Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) whichfalls into BCS class II, characterized by low water solubility andconsequently poor oral bioavailability. To enhance Flurbiprofen'ssolubility and dissolution rate, this study explored crystallo-coagglomeration(CCA) and quasi-emulsion solvent diffusion (QESD)techniques. We optimized process parameters using a centralcomposite design (CCD) approach within Design Expert software. Theindependent variables were stirring rate and the amount of PVP K30,while the dependent variables included Hausner’s ratio and cumulativedrug release (% CDR). Findings indicated that the optimizedagglomerates produced via CCA and QESD exhibited enhancedsolubility and dissolution rates compared to the pure drug. Theoptimized agglomerates were then directly compressed into tablets.The results showed that tablets made from spherical agglomerates released the drug morerapidly than those containing the pure drug, with a release of 18.13% in 60 minutes.Specifically, tablets from agglomerates produced by CCA demonstrated a drug release of92.58% in 60 minutes, while those from QESD exhibited 81.71%. In conclusion,agglomerates created using the CCA method showed superior flow properties and drugrelease profiles compared to those prepared by the QESD method, likely due to the presenceof bridging liquid.

Keywords: Flurbiprofen, Agglomerates, Bioavailability, Design expert.