Formulation and evaluation of aceclofenac injection made by mixed hydrotropic solubilization technique.

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) that exhibits analgesic, antipyretic and anti-inflammatory activities. It is practically insoluble in water. The effect of hydrotropes such as urea and sodium citrate and blends (urea + sodium citrate) on the solubility of aceclofenac was investigated. The enhancement in the solubility of aceclofenac was more than 5 and 25 folds in 30% sodium citrate solution and 30% urea solution, respectively, as compared to its solubility in distilled water. The enhancement in the solubility of aceclofenac in a mixed hydrotropic solution containing ≥ 20% urea and 10% sodium citrate solution was more than 250 folds (compared to its solubility in distilled water). This proved a synergistic enhancement in solubility of a poorly water- soluble drug due to mixed hydrotropy. Synergistic combination of hydrotropic agents can minimize the amount of hydrotropic agents employed, minimizing the chances of their toxicities. Aqueous injection of aceclofenac, using the mixed hydrotropic solubilization technique, was developed and by using the lyophilization method, the problem of inadequate stability of aceclofenac in aqueous solution was overcome. The developed formulation was studied for physical and chemical stability.