ENHANCEMENT OF BIOAVAILABILITY OF CARVEDILOL USING SOLVENT DEPOSITION TECHNIQUESAbstract
Objective: Bioavailability is the key determinant of a drug for its therapeutic effectiveness, which in turn depends upon the solubility of that drug in gastro intestinal fluid. Carvedilol is a BCS class II drug. These category of drugs have low solubility and high permeability so their bioavailability is less. Solvent deposition is a promising method to improve the solubility of poorly water soluble drugs. Methods: Carvedilol solvent deposition was developed by solvent Evaporation method to modify the release and enhance solubility of the drug. The physical state of the dispersed Carvedilol in the polymer matrix was characterized by differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, Fourier-transform infrared spectroscopy, super saturation solubility testing and dissolution studies. Optimized Carvedilol solid dispersions were formulated into tablets by direct compression method. Results: Compared with pure drug and physical mixture, the dissolution of Carvedilol – Solvent deposition was enhanced dramatically. Optimized Carvedilol solvent deposition tablet showed faster drug release in comparison tomarketed tablet. Optimized formulationfollows Higuchi’s equation and the release mechanism is super case II transport. Conclusion: The present study conclusively indicated that the use of solvent depositionmethod by using water soluble carriers improved the solubility of poorly water soluble drug.
R. R. Arun* and J. Harindran
Department of Pharmaceutical Sciences, Mahatma Gandhi University RIMSR, Rubber Board P.O, Kottayam , Kerala, India
22 January, 2017
09 May, 2017
27 May, 2017
01 August, 2017