Abstract

FORMULATION STUDIES ON ENHANCEMENT OF SOLUBILITY, DISSOLUTION RATE OF CARVIDOLOL BY EMPLOYING COMPLEXATION AND SURFACTANT METHOD

Amrutha P. R.*, Yogananda R., Anukumar E. and Muthi Ul Haque

ABSTRACT

Carvidilol widely prescribed BCS Class II Antihypertension drug exhibits low and variable oral bioavailability due to its poor aqueous solubility. Hence it requires enhancement in solubility and dissolution rate. The objective of the present investigation is to enhance the solubility, dissolution rate of Carvidilol by the use of Cyclodextrins (βCD and HPβCD) and surfactant, Solutol HS15. The individual main effects and combined (interaction) effects of cyclodextrins (βCD and HPβCD) and surfactant Solutol HS15 on the solubility and dissolution rate of Carvidilol were evaluated in a experiments. Carvidilol -CD-surfactant complex systems were prepared employing selected combinations of CDs and surfactant in each case by kneading method. The results of the present investigation clearly indicated that the individual main effects as well as combined effects of CDs (βCD and HPβCD) and surfactant Solutol HS15 in enhancing the solubility and dissolution rate (K1) of Carvidilol. Combination of Solutol HS15 with CDs (βCD and HPβCD) resulted in a much higher enhancement in the solubility and dissolution rate (K1) of Carvidilol. Hence a combination of cyclodextrins (βCD and HPβCD) and Solutol HS15 is recommended for enhancing the solubility, dissolution rate and bioavailability of Carvidilol, a BCS Class II drug.

Keywords: Solubility, Carvedilol, ? Cyclodextrin, HP?Cyclodextrin, Solutol HS 15, Complexation and surfactant method.