ENHANCED SOLUBILITY OF ANTIHYPERTENSIVE DRUG USING HYDROPHILIC CARRIER-BASED POTENT SOLID DISPERSION SYSTEMS

Abstract

Oral bioavailability enhancement of drug having poor water solubility is considered as a very hard task in the formulation development of such drugs. The development of solid dispersions helps to enhance bioavailability of poorly water soluble drugs to overcome the limitations of various approaches such as salt formation, solubilization by cosolvents, and particle size reduction. Studies revealed that drugs in solid dispersion need not necessarily exist in the micronized state. Carvedilol’s β-adrernergic receptor blocking ability decreases the heart rate, myocardial contractility and myocardial oxygen demand. Carvedilol and its metabolites also prevent OH- radical induced decrease in sarcoplasmic reticulum Ca-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in the chronic heart failure by preventing free radical damage. Carvedilol belongs to BCS class-II drug having poor water solubility. For the improvement of solubility solid dispersions of carvedilol were prepared using fusion method. Various concentrations of polymers like mannitol and PVPK-30 were used for the preparation o solid dispersions.