DEVELOPMENT OF A FILLER-BINDER DISINTEGRANT FOR DIRECT COMPRESSION TABLETING BY CO-PROCESSING MICROCRYSTALLINE CELLULOSE AND CROSPOVIDONE
DEVELOPMENT OF A FILLER-BINDER DISINTEGRANT FOR DIRECT COMPRESSION TABLETING BY CO-PROCESSING MICROCRYSTALLINE CELLULOSE AND CROSPOVIDONE
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Date
2021-04
Authors
HARUNA, Fatima
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Abstract
The aim of the study was to improve the disintegration functionality of microcrystalline
cellulose (MCC) as a direct compression excipient in tablet formulation by coprocessing
MCCwith crospovidone (CPV), a superdisintegrant. Design of Experiment
(DoE) approach was adopted to optimize the composition of the co-processed excipient
(CPE). The optimized CPE containing MCC (99 %) and CPV (1 %) was prepared using
wet massing technique. Solid-state properties of CPE were characterized in comparison
to MCC and CPV using optical and scanning electron microscopy (SEM), Powder XRay
Diffraction (PXRD), Differential Scanning Calorimetry (DSC) and Fourier
Transform Infra-red spectroscopy (FT-IR). Powder properties such as flowability,
compressibility, moisture sorption capacity, moisture content, dilution potential and
lubricant sensitivity ratio (LSR) were also evaluated using standard techniques.
Compaction studies were carried out using Heckel and Kawakita equations as well as
compressibility-tabletability-compactibility (CTC) profiling. Tablets were formulated
by direct compression incorporating metronidazole as the model drug and properties of
tablets evaluated.
The study revealed an increase in particle size which enhanced the flowability of MCC
as a co-processed excipient. Solid state properties of CPE revealed a material consisting
of irregular shaped fibrous particles characterized by a rough texture. PXRD and DSC
scans presented a material that is semi-crystalline in nature. Moisture content and
moisture sorption capacity of MCC was found to decrease as a result of co-processing.
The extent of plastic deformation was reduced in MCC when co-processed with CPV
and this translated to a reduction in the tabletability of MCC. Tablets formulated with
CPE disintegrated at 11.48mins as compared to MCC tablets that disintegrated at 26.88
mins and this was reflected in the in vitro drug release profile with CPE tablets
attaining maximum drug release at 20mins compared to MCC tablets that attained
maximum drug release at 60mins. Thus, the functionality of MCC as a disintegrating
filler binder for direct compression tableting was improved by co-processing with
crospovidone.
Description
A THESIS SUBMITTED TO THE SCHOOL OF POSTGRADUATE STUDIES,
AHMADU BELLO UNIVERSITY, ZARIA IN PARTIAL FULFILLMENT OF
THE REQUIREMENTS FOR THE AWARD OF MASTER OF SCIENCE
DEGREE IN PHARMACEUTICS
DEPARTMENT OF PHARMACEUTICS AND INDUSTRIAL PHARMACY,
FACULTY OF PHARMACEUTICAL SCIENCES,
AHMADU BELLO UNIVERSITY,
ZARIA, NIGERIA
Keywords
DEVELOPMENT,, FILLER-BINDER DISINTEGRANT,, DIRECT COMPRESSION TABLETING,, CO-PROCESSING MICROCRYSTALLINE CELLULOSE AND CROSPOVIDONE