Development of Theophylline Effervescent Powder for Pulmonary Drug Delivery

Abstract

Introduction: The objective of this current study was to develop theophylline effervescent powder for pulmonary drug delivery. The spray-drying technique combined with effervescence technique was utilized as the means to improve water solubility and hygroscopic properties of theophylline. There were formulations developed in this study, i.e. Conventional Theophylline Powder, Effervescent Base Powder, Theophylline Effervescent Powder and Theophylline Effervescent Powder +PEG. The hygroscopic properties, polymorphism change, water solubility and content analysis of those formulations were assessed. Result: The spray-drying technique combined with effervescence technique proved to be able to produce dry powder for inhalers. However the characteristics of those spray-dried powders showed to be very hygroscopic. When incorporated PEG 1500 (5 and 10%) into formulations was effective to reduce its hygroscopicity. The preliminary solubility test had shown that Theophylline Effervescent Powder dissolved fastest in water and Theophylline Effervescent Powder+PEG dissolved slowest. The polymorphism of all formulations prepared by spray-drying technique was amorphous form. Content analysis of theophylline in those formulations was in the range of 95.40 – 104.51%. Conclusion: The spray-drying technique combined with effervescence technique proved to be able to produce dry powder for inhalers, which powder had amorphous form, improve dissolved water solubility of theophylline and PEG were incorporated that can be reduce its hygroscopicity. This results can develop for pulmonary drug delivery in the future.