(64c) Characterization of Paracetamol Granules Formed By Binder Dropping

Drug bioavailability and solubility is a constant challenge with pharmaceuticals. Most active pharmaceutical ingredients (APIs) are administered in a formulation containing excipients or binders to prevent segregation; however, these additives can also hinder drug dissolution. The purpose of this research is to investigate how binding agents can influence the ability of a granule to dissolve and the ability of the granule to maintain cohesiveness. Binding agents investigated are classified as natural or synthetic and included solutions of materials such as polyvinylpyrrolidone (PVP) and polyethylene glycol (PEG).

Wet granulation was chosen as the method of formulation. Initial tests in this project involved developing paracetamol granules of similar size, shape, and weight for consistency and uniformity. Granules were formed by dropping solution onto a powder bed and allowing the bed to dry for one day. Images of the granules were analyzed using Image-Pro Premier software were perimeter, area, diameter, and roundness were measured. Results of this investigation proved that using 5 drops of binder produced granules of similar size and weight (~300 mg). To test for granule stability, a surface impact test at various heights was conducted, and Vicker’s hardness was measured. Granules produced from synthetic binder solutions proved more cohesive and stable. Five binder drops produced granules without excess agglomeration around the edges with an average weight around 300 mg. Dissolution rates were determined using an Agilent Bio-Dis Apparatus 3 and UV-Vis spectrometry. The pH of the buffer solution and the dip speed of the apparatus were varied. Pure paracetamol powder or granules formed with deionized water, a very weak binder, served as a baseline for analysis. Further investigation of the granules was conducted using FTIR spectroscopy.