Abstract
Background: Cardiovascular drugs delivery mechanism has significant impact on theraputic effect and benifit, actives such as Dipyridamole, Aspirin and Carvedilol phosphate are currently available in the market but there are no generic formulations available due to complexity involved in developing these formulations. These actives can be mixed as per requirement to get synergistic therapeutic effect. There are no commercial formulations available for Aspirin in pellet dosage form; Drug layering is critical aspect in the Pelletisation to achieve desired drug release it is must to have uniform, highly porous, high potency drug loading. Due to insoluble, crystalline nature, loading of aspirin, Carvedilol & dipyridamole on different substrates is extremely difficult. Objective: of this research was to develop drug loaded pellet formulations for Aspirin, Dipyridamole and Carvedilol phosphate. In this research work a pellet based drug delivery system by Wurster technolgy was envisaged, Hence basic objective was to establish drug loading on selected substrate to get high potency drug loaded pellets Investigation: of drug loading was carried out in GPCG 1.1 and Pam Glatt 125Lts. Drug loading has direct impact on formulation performance. A significant impact of manufacturing process, binder, solvent was investigated, a significantly improved drug layered pellet system was developed for crystaline drugs such as Dipyridamole, Carvedilol Phosphate & Aspirin. Observations and conclusion: Excellant drug layereing effeciency was obtianed by slecting suitable solvent and binder. A suitable HPLC method was developed to detect active content in the beads, SEM analysis of these pellets confirmed controlled porocity of drug layered pellets confirming uniformity,and suitability for their application from commercial manufacturing point of view. DSC study also confirmed the polymorphic form of the active in the formulaiton. In overall drug layered pellets such developed were sucessfully scaled up from GPCG1.1 to Pam Glatt 125lts, and thus confirmed comercial feasibility of the work done. These pellets thus can be in future coated with rate modulating polymers & can be mixed synergestically to acheive required theraputic benifit.
