Abstract

SOLUBILITY ENHANCEMENT OF VARDENAFIL HYDROCHLORIDE BY PREPARATION OF SOLID DISPERSION

Shruti B. Patel, Vandana B. Patel*

ABSTRACT

Vardenafil hydrochloride is a phosphodiesterase 5 inhibitor used to treat erectile dysfunction which has comparatively earliest onset of action, tmax, better duration of effect and lower side effects. But, it suffers from the disadvantage of poor water solubility and low bioavailability (15 %). As solubility is an important factor to enhance bioavailability, solubility of vardenafil hydrochloride is required to be enhanced. In present investigation, an attempt is made to enhance solubility of vardenafil hydrochloride. For this purpose solid dispersion of vardenafil hydrochloride was prepared by solvent evaporation and fusion method. Different polymers like polyvinyl pyrrolidone, mannitol in different drug to polymer ratios were used to prepare solid dispersion. The prepared solid dispersions were evaluated for % drug content, solubility and % cumulative drug release. Results clearly indicated that there was significant increase in solubility (from 0.109 to 0.202 mg/ml in solvent evaporation and from 0.109 to 0.199 mg/ml in fusion method) and dissolution profile (from 62.24 to 95.17% in solvent evaporation and from 62.24 to 91.17 % in fusion method) of vardenafil hydrochloride. Thus it may be concluded that solubility and dissolution of vardenafil hydrochloride can be promisingly enhanced by preparation of solid dispersion by both the methods. Moreover, better results were found in the drug to polymer ratio of 1:3 in both the methods.

Keywords: vardenafil hydrochloride, erectile dysfunction, solubility, solubility enhancement technique, solid dispersion, t-test.