DESIGN AND DEVELOPMENT OF A STARCH-BASED MULTIFUNCTIONAL EXCIPIENT (STARGELASIL) FOR TABLET FORMULATION
DESIGN AND DEVELOPMENT OF A STARCH-BASED MULTIFUNCTIONAL EXCIPIENT (STARGELASIL) FOR TABLET FORMULATION
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Date
2016-03
Authors
APEJI, YONNI ESHOVO
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Abstract
The concept of co-processing as a particle engineering technique has been used as a tool
to improve the functionality of many existing excipients. This study was designed to
improve the functionality of cassava starch as excipient for direct compression by coprocessing
with gelatin and colloidal silicon dioxide.
The Design of Experiment (DoE) approach was employed to optimize the percentage
ratios of the primary excipients for the co-processed excipient. Fourteen experimental
formulations containing varying proportions of the primary excipients were prepared by
the method of co-fusion and twelve tablets each weighing 400 mg each were produced
for each formulation using the Hydraulic Carver Press. The compressed tablets were
kept for 24 h in the desiccator and evaluated for tensile strength and disintegration time.
The data obtained from the tabletswere suitably analysed using the Design Expert
software and fittedto a special quartic model that correlated the effect of varying the
proportions of the excipients in the different formulations on tablet properties.The
composition of the co-processed excipient that produced tablets of desirable
characteristics after optimization was found to be cassava starch (90 %), gelatin (7.5 %)
and colloidal silicon dioxide (2.5 %).
The optimized co-processed excipient subsequently known as “StarGelaSil” (SGS) was
prepared in large quantities and stored in an airtight container for further studies. Solidstate
characterization was conducted on SGS to determine its particle size, shape,
distribution, surface morphology, degree of crystallinity, hygroscopicity, compatibility
etc using established analytical techniques. Powder properties of SGS were also
determined by measuring its flowability using the angle of repose, bulk and tapped
densities, porosity, dilution potential, lubricant sensitivity ratio etc. The compaction
behaviour of SGS was analysed using Heckel and Kawakita equations and the compressibility, tabletability, compactability (CTC) profile was determined in
comparison to the physical mixture of the primary excipients (SGS-PM). Tablets were
formulated by direct compression using Ibuprofen as the drug of choice and compared
with tablets produced using Prosolv® and StarLac® as reference standards.
The results revealed that co-processed particles of SGS were largelyamorphous and
spherical in shape with rough surfaces. There was no incompatibility between the
excipients used for co-processing and between drug and co-processed excipient. Flow
properties were enhanced as a result of co-processing. A superior CTC profile was
obtained for SGS when compared with SGS-PM. The tablets produced by SGS
conformed to the specifications of USP (2009) and compared well with those of the
reference excipients in terms of tensile strength, disintegration time and drug-release
profile.
This study concluded that co-processing was able to improve the functionality ofcassava
starch as excipient for direct compression. Hence, the excipient can be developed for
usein pharmaceutical industry as a choice material for direct compression
Description
A THESIS SUBMITTED TO THE SCHOOL OF POSTGRADUATE STUDIES,
AHMADU BELLO UNIVERSITY IN PARTIAL FULFILMENT OF THE
REQUIREMENTS FOR THE AWARD OF THE DOCTOR OF PHILOSOPHY
DEGREE IN PHARMACEUTICS
DEPARTMENT OF PHARMACEUTICS AND PHARMACEUTICAL
MICROBIOLOGY,
FACULTY OF PHARMACEUTICAL SCIENCES,
AHMADU BELLO UNIVERSITY, ZARIA
Keywords
DESIGN,, DEVELOPMENT,, STARCH-BASED,, MULTIFUNCTIONAL EXCIPIENT,, (STARGELASIL),, TABLET FORMULATION,