Binder and Disintegrant Performance of Native and Thermally Modified Dioscorea cayenensis Starches in Paracetamol Tablet Formulations

Abstract

The versatility of starch as pharmaceutical excipient is gaining attention in the development of natural polymers for application in tablet formulations. In this study, we reported the binder and disintegrant properties of native and modified starches extracted from Dioscorea cayenensis. The extracted starch was modified by pregelatinization (PGS1) and ethanol dehydrated pregelatinization (PGS2) and was employed as binder and disintegrant in paracetamol tablet formulations via wet granulation. Two-way analysis of variance indicated significant differences between tablet properties, measured in terms of hardness, friability and disintegration time, with respect to the starch type and concentration. Multiple comparison computed using Bonferroni post-hoc analysis indicated higher values of tablet hardness in PGS2 than PGS1 and unmodified starch (UMS) (p<0.01). UMS had the highest friability implying poor mechanical quality (Friability >3%). At 2-7% concentrations, PGS1, PGS2 and UMS demonstrated acceptable United State Pharmacopoeial disintegration time profiles for uncoated tablets. Overall results demonstrated an improved quality of the modified starches compared to the UMS with the potential application of PSG1 as binder and disintegrant in different ratios for immediate release tablet formulation. PSG2 was shown to make a good binder when sustained-release of API is required.

Application of data-intelligence algorithms for modeling the compaction performance of new pharmaceutical excipients

“…The low quality of the native starches is attributed to their poor functionality in terms of particle characteristics that directly affect their flow rate, compactibility, and compressibility characteristics. Through modification (chemical, physical, or biotechnological), these properties could be improved to obtain pharmaceutical-grade starches [3,5]. The process of such modification can be complex, consuming significant resources and time.…”