Understanding the Performance of a Novel Direct Compression Excipient Comprising Roller Compacted Chitin.

Deeb Abu Fara,Linda Al-Hmoud,Adnan Badwan,Iyad Rashid,Babur Z Chowdhry

doi:10.3390/md18020115

Deeb Abu Fara, Linda Al-Hmoud + Show 3 more

Open Access

https://doi.org/10.3390/md18020115

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Abstract

Chitin has been investigated in the context of finding new excipients suitable for direct compression, when subjected to roller compaction. Ball milling was concurrently carried out to compare effects from different energy or stress-inducing techniques. Samples of chitin powders (raw, processed, dried and humidified) were compared for variations in morphology, X-ray diffraction patterns, densities, FT-IR, flowability, compressibility and compactibility. Results confirmed the suitability of roller compaction to convert the fluffy powder of raw chitin to a bulky material with improved flow. X-ray powder diffraction studies showed that, in contrast to the high decrease in crystallinity upon ball milling, roller compaction manifested a slight deformation in the crystal lattice. Moreover, the new excipient showed high resistance to compression, due to the high compactibility of the granules formed. This was correlated to the significant extent of plastic deformation compared to the raw and ball milled forms of chitin. On the other hand, drying and humidification of raw and processed materials presented no added value to the compressibility and compactibility of the directly compressed excipient. Finally, compacted chitin showed direct compression similarity with microcrystalline cellulose when formulated with metronidazole (200 mg) without affecting the immediate drug release action of the drug.

Highlights

Pharmaceutical excipients for direct compression (DC) applications are mostly favored in relation to saving time, cost and labour for solid dosage form preparations and tableting [1,2]
These results demonstrate that tablets comprising chitin are harder in terms of crushing force and faster in disintegration time than tablets made of MCC PH 200®
The research presented is mainly focused on the assessment of the use of roller compaction technique for the development of DC pharmaceutical excipients from raw alpha chitin

Summary

Introduction

Pharmaceutical excipients for direct compression (DC) applications are mostly favored in relation to saving time, cost and labour for solid dosage form preparations and tableting [1,2]. The foregoing advantages are due to their ability to provide the three main requirements associated with excipients for DC processing, i.e., compressibility, compactibility, and flowability [3,4]. Many DC excipients are manufactured from natural sources (e.g., cellulose and starch), from existing excipients of synthetic origin or from binary mixtures of non-DC excipients [5,6]. The necessity for structural modification and industrial manufacture is attributed to the detrimental physical properties of most pharmaceutical excipients before being processed. These properties include poor compactibility, compressibility, and flowability.

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