STUDIES ON THE TABLETING AND ANTIULCER PROPERTIES OF FICUS SUR FORSK LEAF EXTRACTS
STUDIES ON THE TABLETING AND ANTIULCER PROPERTIES OF FICUS SUR FORSK LEAF EXTRACTS
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Date
1997-08
Authors
KUNLE, OLOBAYO OLUFUNSHO
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Abstract
The justification for the use of Ficus sur (Forsk) leaves in the treatment of peptic ulcer
was investigated. This was done by extracting the dried leaves with various solvents
(polar and non polar) and determining their smooth muscle relaxant (polar extract) and
ulcero-protective effects. Their antimicrobial activity was also investigated. The results
indicated that the polar extracts had smooth muscle relaxant and ulcer protective effect,
with the hot water extract (HWE) having the most effect.
The HWE was used for formulation studies using the wet granulation method. The effect
of three diluents - Lactose, Aerosil and Heavy Magnesium Carbonate on the formulation
was investigated. Four binders - maize starch paste, PVF, sodium alginate and gelatin,
were used at three concentration levels each. The effect of magnesium stearate as
lubricant was also studied in order to determine the optimal amount required. These
effects were studied on granules and tablets. The Meckel equation was used to investigate
the compaction characteristics of the granulates.
All the granulates had good flow properties. Tablets produced with lactose as diluent had
the highest physical strength while those produced with heavy magnesium carbonate were
unsatisfactory in this respect. Some of the lactose - containing tablets however failed the
disintegration time test.
Both the binder type and concentration affected the granule and tablet properties
investigated. For example in most cases granule size increased, while bulk and tapped
densities increased with binder concentration, with the extent depending on the binder
type.
The granules were generally found to have Type B behaviour suggesting that strong
compacts will be produced from these granulates. There were however a few granulates,
such as that with 5%w/w starch mucilage as binder and lactose as diluent which gave
Type- C-like plots.
The optimum magnesium stearate concentration was found to be in the range 0.1
0.2%w/w, with respect to granule and tablet properties.
In order to improve the disintegration time of the tablets, surfactants (Tween 80 and SLS)
at two concentration levels were incorporated into the formulations. They reduced the
physical strength of the tablets. The disintegration and dissolution times however
improved in most cases, although with some others it increased. The extent of these
effects depended on the surfactant type and concentration, diluent and binder types.
'Fingerprints' for assessing the effect of formulation process and additives on the HWE
were developed. They were UV spectroscopy, TLC and biological. They showed that
these factors did not affect the HWE.
It was concluded that the use of the leaves of Ficus sur in the treatment of peptic ulcer
could be justified and that tablets of suitable properties could be formulated from the
HWE with either lactose or aerosil as diluent. The binder type and concentration will
need to be carefully selected.
Description
A thesis submitted to Ahmadu Bello University, Zaria, in partial
fulfillment of the requirements for the degree of
Doctor of Philosophy in Pharmaceutics
Department of Pharmaceutics and Pharmaceutical Microbiology,
Faculty of Pharmaceutical Sciences, Ahmadu Bello University
Zaria - Nigeria.
Keywords
STUDIES,, TABLETING,, ANTIULCER,, PROPERTIES,, FICUS,, SUR,, FORSK,, LEAF,, EXTRACTS