Abstract

In the present study, microcrystallinecellulose–colloidal silicon dioxide (MCC-SiO2) and carboxymethylcellulose–colloidal silicon dioxide (CMC-SiO2) conjugates have been investigated as superdisintegrants in fast dissolving tablets (FDTs). MCC-SiO2 and CMC-SiO2 conjugates were prepared and micromeritic studies, FTIR, SEM and XRD methods were utilized for characterizing the powdered conjugates. The conjugates were used for the preparation of domperidone FDTs by direct compression and the wetting time, water absorption ratio, disintegration time and in vitro drug release were evaluated. Effective pore radius of MCC-SiO2 and CMC-SiO2 conjugates for 1:1, 1:2.5 and 1:5 was found to be 13.35 ± 0.31 µm, 15.66 ± 0.17 µm and 18.38 ± 0.44 µm, and 16.81 ± 0.24 µm, 20.12 ± 0.39 µm and 26.37 ± 0.24 µm, respectively, compared to 12.21 ± 0.23 µm for MCC and 13.65 ± 0.21 µm for CMC. The results of effective pore radius indicate the wicking capability as well as the disintegration potential of MCC-SiO2 and CMC-SiO2 conjugates over pure MCC and CMC. The results of wetting time, water absorption ratio and disintegration time for MCC-SiO2 conjugates were found to be in the range of 19 ± 1.21 to 30 ± 1.33 s, 42 ± 0.28 to 49 ± 0.47% and 15 ± 2 to 40 ± 1 s, and for CMC-SiO2 conjugates were found to be in the range of 21 ± 1.13 to 40 ± 1.17 s, 42 ± 0.94 to 49 ± 0.57% and 12 ± 2 to 20 ± 3 s, respectively. Conjugation of MCC and CMC with SiO2 led to the formation of a complex with remarkable tablet superdisintegrant potential that could be used in preparing fast disintegrating tablets.

Highlights

  • Introduction published maps and institutional affilFast disintegrating tablets (FDTs) have emerged as prominent dosage forms in the recent past, as they disintegrate rapidly within the mouth in a matter of few seconds, showing rapid dissolution and fast onset of action

  • The flow properties of Microcrystalline cellulose (MCC) and carboxymethyl cellulose (CMC) were improved with the addition of SiO2

  • Carr’s index values were found to be in the range of 19.42 to 11.52 for MCC-SiO2 conjugates and 16.77 to 12.19 for CMC-SiO2 conjugates, depicting good to fair flow rate when compared to MCC (20.17) and CMC (19.43)

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Summary

Introduction

Introduction published maps and institutional affilFast disintegrating tablets (FDTs) have emerged as prominent dosage forms in the recent past, as they disintegrate rapidly within the mouth in a matter of few seconds, showing rapid dissolution and fast onset of action. Pre-gastric absorption of the FDTs in the mouth and esophagus decreases the amount of drug undergoing the first-pass metabolism and thereby results in improved bioavailability [1,2]. These dosage forms provide various other advantages such as accurate dosing, easy portability, chemical and physical stability and are highly convenient for geriatric, pediatric, bedridden and uncooperative patients [3]. They are generally represented as “quick melt”, “orally disintegrating”, “melt in mouth”, “quick dissolve”, “fast disintegrating”, “rapid melt”, “oro-dispersible”, “fast dissolve” and “mouth dissolving” etc.

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