Abstract

INTENSIFICATION OF THE SOLUBILITY OF BCS CLASS II DRUG CARVEDILOL USING SPRAY DRYING BY FORMULATING A SOLID DISPERSION

Tina Raju*

ABSTRACT

Orally administered drugs completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs play an important role in the process of formulation development. Problem of solubility is a major challenge for formulation scientist which can be solved by different technological approaches during the pharmaceutical product development work. A major problem with BCS class II drug is their low solubility in biological fluids, which results into poor bioavailability after oral administration. Carvedilol is a non-selective beta and alpha blocker which is insoluble in water. It is used in the treatment of mild to severe congestive heart failure (CHF) and high blood pressure. As the solubility is very poor the bioavailability is only 25-35%. The problem of poor solubility can be overcome using any of the physical or chemical methods of solubility enhancement. The purpose of this research was to improve the solubility of Carvedilol by spray drying technique using hydrophilic polymers β-Cyclodextrin and Plasdone-K30. Prepared solid dispersions were evaluated for drug content, saturation solubility and in-vitro drug release study. The compatibility and surface morphology was studied by Fourier Transforms Infrared spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and Scanning Electron Microscopy (SEM) respectively.

Keywords: Bioavailability, Carvedilol, Hypertension, PVP-K30, Solid dispersion.