Characterization and surface impact of paracetamol granules formed by binder dropping

Abstract

Drug bioavailability and solubility is a constant challenge with pharmaceuticals. About 80% of drugs are administered orally because the method is cost effective and convenient. The challenge for scientists and engineers is to increase the efficiency of orally administered drugs. Most active pharmaceutical ingredients (APIs) are administered in a drug formulation containing excipients or binders to prevent segregation; however, these additives can hinder drug dissolution and cause mild adverse effects. The purpose of this research is to investigate the influence of a single excipient on the properties of paracetamol tablets or granules especially the cohesiveness of the granules. Testing also included developing paracetamol granules of similar size, shape, and weight for consistency and uniformity. Granules were formed by dropping aqueous binder solution onto a powder bed or binder dropping. The active pharmaceutical ingredient, paracetamol (APAP), served as the powder for the beds. From this investigation, an optimum number of drops were determined which resulted in a common granule shape and size while preventing spreading. Surface impact force analysis was conducted to test granule stability using free fall analysis at 12 and 24 inches. Compression resistance was analyzed and force measurements recorded. Binder dropping proved an efficient method of creating paracetamol granules. Granule size was affected by choice of excipient. Excipient selection also determined granule performance and stability.