Production of theophylline and polyethylene glycol 4000 composites using Gas Anti-Solvent (GAS) process

Production of drug composites can be used to enhance the dissolution rate of poorly-water soluble drugs. In this research, Gas Anti-Solvent (GAS) technique was applied to produce composites between theophylline (THEO) and polyethylene glycol (PEG) by using dense carbon dioxide as an anti-solvent. It was found that the size of the composites decreased as the concentration of PEG 4000 decreased. However, when increasing the temperature the degree of aggregation and particles size were increased. It was also found that a decrease in ethanol amount in the solvent mixture of dichloromethane and ethanol resulted in a decrease of particle size. The theophylline-PEG composites with the highest drug loading of 16.70% were obtained when using the mass ratio of drug and polymer at 2:3 wt.% in the dichloromethane and ethanol solvent of 50:50%v/v and 25 degrees C. The dissolution rate of the prepared composites in phosphate buffered solution was found to be 20.8 times greater than that of the original material. (C) 2008 Elsevier B.V. All rights reserved.