Abstract

FORMULATION DEVELOPMENT AND EVALUATIONS OF AN AQUEOUS INJECTION OF GATIFLOXACIN BY NOVEL MIXED SOLVENCY TECHNIQUE

Gayakwad PS, Gavit AJ, Rajput PV,Bari MM, Barhate SD, Maheshwari RK

Abstract

In the present investigation, mixed-solvency approach has been applied for the enhancement of aqueous solubility of a poorly water soluble drug, gatifloxacin(selected as a model drug). Gatifloxacin is a synthetic fluroquinolone broad spectrum antimicrobial agent used in the treatment of bacterial infection. Aqueous injection of gatifloxacin was prepared by making various blends (keeping total concentrations 30% w/v, constant) of selected water-soluble solubilizer such as hydrotropes (nicotinamide, sodium benzoate, sodium citrate,) and co-solvents (propylene glycol, PEG-400, ethanol). Aqueous solubility of drug in case of selected blends (18 blends) ranged from 22.79 mg/ml–82.05mg/ml (as compared to the solubility in dist.water 1.19 mg/ml).The enhancement in the solubility of drug in a mixed solvent containing hydrtropes( 8% nicotinamide, 8% sodium benzoate, 4% sodium citrate) and co-solvents (4% PEG 400, 3% propylene glycol, 3% ethanol) was more than 68.95 fold. This proved a synergistic enhancement in solubility of a poorly water-soluble drug due to mixed co-solvent effect. Each solubilized product was characterized by ultraviolet and infrared techniques. Various physical properties of solution such as pH, viscosity, specific gravity and surface tension were studied. The developed formulation was studied for physical and chemical stability. This mixed solvency shall prove definitely a boon for pharmaceutical industries for the development of dosage form of poorly water soluble drugs.

Keywords: Fluroquinolones, hydrotropes, co-solvents, solubility and stability.