(431d) Infleunce of Natural and Synthetic Binders on Paracetamol Granules Properties

The role of binders in the formulation of tablets widely varies based on the intended application. Binders, or excipients, account for most drug formulations and provide enhanced properties that aid in drug delivery and bioavailability. Excipients are distinguished by their functionality, efficacy, safety, and qualify. Currently, scientists are seeking more naturally occurring sources (plant-based) to replace common synthetic binders such as polysorbates, povidone, polyvinylpyrrolidone (PVP) and polyethylene glycol (PEG). Natural excipients are considered non-toxic and more biocompatible. Overall, the tablet or granule cohesiveness, stability, manufacturability, and release characteristics will provide an indicator of the feasibility for using a given excipient in industrial-scale manufacturing applications. The purpose of this research is to investigate the influence various natural and semi-synthetic excipients on granule properties.

Paracetamol granules were prepared using the previously proven method of binder dropping. All excipients were dissolved into deionized water prior to placement on the powder bed. Analysis of the granules included weight and size analysis using Image-Pro Premier software, friability testing, compression testing, disintegration testing, and dissolution testing. Size measurements included diameter, aspect ratio, and projected area. Dissolution and disintegration tests were performed at a dip rate of 10 DPM in phosphate buffer solution at a pH of 7.0. The concentration of paracetamol in the solution was determined using UV-Vis spectrometry. Friability testing occurred for 100, 150, and 200 rotations. With the exception of PEG, the concentration of the excipient influenced the behavior of the paracetamol granules during dissolution and friability testing. However, the extent of the influence varied between the excipients. For most excipients, the increase in concentration produced larger granules that were more susceptible to breakage during friability testing. The bonding of the excipients determined whether the formed paracetamol granules immediately disintegrated or dissolved over time.