Abstract

HYDROTROPIC SOLUBILIZATION TECHNIQUE TO CHALLENGE THE SOLUBILITY OF POORLY WATER SOLUBLE DRUG VALSARTAN

Dr. Shikha Agrawal* and Madhavi Kasturi

Abstract

Aqueous solubility is one of the major concerns during formulation development of new drug molecules. Drug efficacy as well bioavailability can be restricted by poor aqueous solubility of drugs. Previously, many techniques have been developed to enhance aqueous solubility of drug which showed promising advantage of increased potency as well reduced side effects. Hydrotropic solubilization is one of the enhancement techniques which enhance solubility of drug to many folds with the use of hydrotropes like sodium acetate, sodium benzoate, sodium citrate, urea etc. The key objective of current research work was to enhance aqueous solubility of very poorly water soluble drug, Valsartan using hydrotropic solubilization technique. Valsartan is an orally active antihypertensive drug which is poorly water soluble (0.021mg/ml) and has low bioavailability of 23%. Rationale to choose hydrotropic solubilization for Valsartan was that hydrotropic solution may enhance solubility of drug which in turn results in enhanced dissolution rate as well bioavailability. Solubility studies were performed using various concentrations of hydrotropic solutions of sodium acetate, sodium ascorbate, sodium benzoate, piperazine, etc. These solubility studies revealed that the solubility of drug was increased 62 hundred times when added to 5% piperazine anhydrous solution and marked its importance in pharmaceutical field. The reason for high solubility may be due to higher pH of piperazine solution which could dissolve valsartan being weakly acidic in nature.

Keywords: Hydrotropy, solubility, valsartan, piperazine, sodium benzoate, solubility enhancement.