Journal of Bioequivalence & Bioavailability

Solubility enhancement of felodipine by solid dispersions with a novel polymeric solubilizer soluplus?

3^rd World Congress Bioavailability & Bioequivalence

March 26-28, 2012 Marriott Hotel & Convention Centre, Hyderabad, India

Murali Monohar Pandey, G Krishna Kumar, Ramakrishna R., Dr. Shrikant Chardet

Posters: J Bioequiv Availab

Abstract:

F elodipine (FLD) is a calcium channel blocker, that selectively reduces smooth muscle contractile activity in resistant vessels and is widely used in the treatment of hypertension, heart failure and angina pectoris. Soluplus? (SOL) is a polyvinyl caprolactum- polyvinyl acetate- polyethylene glycol graft copolymer with an amphiphilic chemical structure. The solid dispersions were prepared by solvent casting method. For this, FLD and SOL in ratios of 1:2, 1:4, 1:6 and 1:10 respectively were dissolved in minimum required volume of ethanol. The resultant solution was poured into Petri plates and kept in oven at 40 ?C for drying. The dried mass was powdered in mortar, sieved using #60 mesh screen and stored at room temperature. The solid dispersions were characterized by differential scanning calorimetery (DSC), powder X-ray diffraction (XRD) & and fourier transform- infrared spectroscopy (FT-IR). Physical mixtures (PM) of the same ratios were also prepared. The solubility studies of PM and SD were conducted in phosphate buffer (pH 6.8). The samples were analyzed on UV-Visible spectrophotometer at 360 nm wavelength. The solubility of pure felodipine in phosphate buffer pH 6.8 is 31.6 μg/ml. We observed increase in solubility of felodipine in both the PM and SD with the increase in the amount of soluplus?. The greatest increase (30 fold) was observed in the SD containing 1:10 of felodipine and soluplus?. Solid dispersions prepared using soluplus? could be a very useful option for Felodipine solubility enhancement could be used to prepare formulations with enhanced bioavailability