SOLUBILITY ENHANCEMENT OF NEBIVOLOL BY HYDROTROPIC METHOD

Ghanshyam Rathore*, Satish Sahu, Chinmay Dahariya, Neelima Sahu and Jhakeshwar Prasad

ABSTRACT

Therapeutic effectiveness of a drug depends upon the bioavailability and ultimately upon the solubility of drug molecules. In case of the oral administration solubility is one of the important parameter for achieving desired concentration of drug in systemic circulation for pharmacological response to be shown. Most popular route in drug administration is oral route because of simple, uncomplicated and cost effective administration. There are many advantages of this oral route for hydrophilic drugs but major disadvantage is that lipophilic drugs are poorly insoluble and faces absorption and bio-avaibility issues. Currently, 40% of the drugs are poorly water soluble which produce side effects such as gastric irritation, peptic ulceration etc. whereas only 8% of new drug candidates have shown both high solubility and permeability. Nebivolol is a third-generation beta-a drenoceptor antagonist. It differs from other beta-a drenoceptor antagonists as it combines highly selective beta 1-adrenoceptor antagonist properties with nitric oxide-mediated vasodilator actions and beneficial effects on endothelial function. But this very useful drug use is limited due to challenge of poor water solubility (0.0403 mg/ml). Present study deals with enhancement of solubility of Nebivolol by hydrotropic method.

Keywords: Nebivolol, Solubility enhancement, Hydrotropy method, Dissolution characteristics.