%0 Journal Article
%T Study on Mixed Solvency Concept in Formulation Development of Aqueous Injection of Poorly Water Soluble Drug
%A Shailendra Singh Solanki
%A Love Kumar Soni
%A Rajesh Kumar Maheshwari
%J Journal of Pharmaceutics
%D 2013
%I Hindawi Publishing Corporation
%R 10.1155/2013/678132
%X In the present investigation, mixed-solvency approach has been applied for the enhancement of aqueous solubility of a poorly water- soluble drug, zaltoprofen (selected as a model drug), by making blends (keeping total concentrations 40% w/v, constant) of selected water-soluble substances from among the hydrotropes (urea, sodium benzoate, sodium citrate, nicotinamide); water-soluble solids (PEG-4000, PEG-6000); and co-solvents (propylene glycol, glycerine, PEG-200, PEG-400, PEG-600). Aqueous solubility of drug in case of selected blends (12 blends) ranged from 9.091 ¡À 0.011£¿mg/ml¨C43.055 ¡À 0.14£¿mg/ml (as compared to the solubility in distilled water 0.072 ¡À 0.012£¿mg/ml). The enhancement in the solubility of drug in a mixed solvent containing 10% sodium citrate, 5% sodium benzoate and 25 % S cosolvent (25% S cosolvent contains PEG200, PEG 400, PEG600, Glycerine and Propylene glycol) was more than 600 fold. This proved a synergistic enhancement in solubility of a poorly water-soluble drug due to mixed cosolvent effect. Each solubilized product was characterized by ultraviolet and infrared techniques. Various 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. 1. Introduction Formulation has numerous benefits in drug discovery and development. It enables efficacy, toxicity, and pharmacokinetic (PK) studies. Formulation can improve oral bioavailability, shorten onset of a therapeutic effect, enhance stability of drugs, and reduce dosing frequency. More consistent dosing can be achieved by reducing food effect through formulation. Formulation can reduce side effects (i.e., decreasing tissue irritation and improving taste) [1¨C3]. An intramuscular (IM) medication is given by needle into the muscle. It can be a solution, oil, or suspension. Drugs in aqueous solution are rapidly absorbed. However, very slow constant absorption can be obtained if the drug is administered in oil or suspended in other repository vehicles. Solubility may also be enhanced by altering the pH and using cosolvents but excess amount of these agents may have adverse effects. The vehicle should contain a minimum amount and low concentration of the co-solvent to reduce viscosity and toxicity effects [3¨C6]. To significantly enhance the solubility of semipolar drugs, high concentrations of non-aqueous cosolvents may be required [7].
%U http://www.hindawi.com/journals/jphar/2013/678132/