Abstract

This study was aimed at evaluating chitosan-microcrystalline cellulose blends as direct compression excipients. Crab shell chitosan, α-lactose monohydrate, and microcrystalline cellulose powders were characterized. Blends of the microcrystalline cellulose and chitosan in ratios 9 : 1, 4 : 1, 2 : 1, and 1 : 1 as direct compression excipients were made to constitute 60% of metronidazole tablets. Similar tablets containing blends of the microcrystalline cellulose and α-lactose monohydrate as well as those containing pure microcrystalline cellulose were also produced. The compact density, tensile strength, porosity, disintegration time, and dissolution rate of tablets were determined. Chitosan had higher moisture content (7.66%) and higher moisture sorption capacity (1.33%) compared to microcrystalline cellulose and lactose. It also showed better flow properties (Carr's index of 18.9% and Hausner's ratio of 1.23). Compact density of tablets increased but tensile strength decreased with increase in the proportion of chitosan in the binary mixtures. In contrast to lactose, the disintegration time increased and the dissolution rate decreased with increase in the proportion of chitosan. This study has shown that chitosan promotes flowability of powder mix and rapid disintegration of tablet. However, incorporation of equal proportions of microcrystalline cellulose and chitosan leads to production of extended-release tablet. Therefore, chitosan promotes tablet disintegration at low concentration and enables extended-release at higher concentration.

Highlights

  • Direct compression is the most preferred of all methods of tableting as it saves both time and energy [1]

  • Chitosan can be said to be superior to lactose as a codiluent in direct compression since rapid disintegration action which is related to poor solubility is one of the ideal requirements of a direct compression excipient [2]

  • Chitosan is characterized by good flowability and rapid disintegration action, properties that are desired of direct compression excipients

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Summary

Introduction

Direct compression is the most preferred of all methods of tableting as it saves both time and energy [1]. In this method, tablets are compressed directly from the powder blends of active ingredients and suitable excipients [2]. Direct compression is suitable for moisture and heat-sensitive materials. The desired properties of excipients for direct compression are powder fluidity, good compressibility, low moisture sensitivity, and rapid disintegration action [2, 4]. Combination of two or more excipients with different desirable properties enhances the manufacturing process and/or product performance. The quality of a delivery system is determined by its manufacturing process and the performance of the dosage form [5]

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