Abstract
BackgroundExcipients with improved functionality have continued to be developed by the particle engineering strategy of co-processing. The aim of this study was to evaluate the compaction and tableting properties of composite particles of microcrystalline cellulose (MCC) and crospovidone (CPV) engineered by co-processing.ResultsHeckel analysis of the compaction behavior revealed a decrease in plasticity of co-processed excipient (CPE) when compared to MCC due to an increase in Heckel yield pressure from 144 to 172 MPa. The compressibility-tabletability-compactibility (CTC) profile revealed a decrease in individual parameters for CPE when compared to MCC. CPE was found to be more sensitive to the lubricant effect of sodium stearyl fumarate (SSF) when compared to MCC and less sensitive to magnesium stearate (MST) when compared to MCC. A higher dilution potential was obtained for MCC (60%) compared to 44% for CPE when metronidazole was used as model drug. Tableting properties revealed that metronidazole tablets generated with CPE by direct compression disintegrated within 15 min and gave a rapid drug release when compared to MCC as a direct compression (DC) excipient.ConclusionThe compaction and tableting properties of CPE were characterized and yielded tablets with better disintegration and drug release profile when compared to MCC. This study, therefore, confirms the suitability of co-processing as a proven strategy in engineering the performance of excipients.
Highlights
Excipients with improved functionality have continued to be developed by the particle engineering strategy of co-processing
True density A mean value of 1.48 g/mL was obtained as true density for both microcrystalline cellulose (MCC) and co-processed excipient (CPE) in comparison to a lower value obtained for CPV (1.23 g/mL)
A Heckel parameter, which measures the degree of plasticity in a material was ranked in the following order, MCC
Summary
Excipients with improved functionality have continued to be developed by the particle engineering strategy of co-processing. The aim of this study was to evaluate the compaction and tableting properties of composite particles of microcrystalline cellulose (MCC) and crospovidone (CPV) engineered by co-processing. Pressure is applied to transform the powder bed into solid compacts of suitable mechanical strength. This is a necessary step in the tablet-making process. The present study aims to evaluate the compaction and tableting properties of the composite particles of MCC and CPV designed for use as a coprocessed multifunctional excipient in direct compression formulations. Dilution potential studies will be carried out to determine the drug-loading capacity of the excipient that will yield tablets of sufficient mechanical strength. To the best of our literature review, no such study has been carried out
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