STUDIES ON THE TABLETING AND ANTIULCER PROPERTIES OF FICUS SUR FORSK LEAF EXTRACTS

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STUDIES ON THE TABLETING AND ANTIULCER PROPERTIES OF FICUS SUR FORSK LEAF EXTRACTS

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.

STUDIES ON THE TABLETING AND ANTIULCER PROPERTIES OF FICUS SUR FORSK LEAF EXTRACTS

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