TABLETING PROPERTIES OF THE BARK AND LEAF POWDERS OF AZADIRACHTA /NDICA (A. JUSS)

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Date
1996-03
Authors
ISAH, ADAMU BABAH
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Abstract
Azadirachta indica (neem tree) is a well known medicinal plant found particularly useful in the treatment of malaria. It is readily available in the northern part of this country. Despite the wide usage of this plant in malarial chemotherapy, the dosage has not been standardized. It has therefore become imperative to commence work towards formulating thi3 plant or its parts into a suitable dosage form. In this study, attempts were made into formulating the barks and leaves into tablets. To investigate the tableting properties, the physico-chemical characteristics of the bark and leaf powders of the plant such as mean particle size and size distribution, particle morphology, flow properties Gangle of repose, flow rate and Carr's index as well as moisture contents, Using standard procedures. Compact characteristics such as thickness, hardness, variability, and disintegration times of the tablets compressed from these powders by wet granulation and direct compression methods were investigated. The effect of various binders and granule size fractions on the characteristics of tablets produced by wet granulation method and that of diluent on tablets produced by direct compression were determined. Microbiological analyses such as microbial contamination levels and flora determination, and evaluation of the antimicrobial property of the plant was also carried out. Tests were also done to detect the presence of some indicator organisms. In order to determine an effective dosage regimen for a rational therapeutic use of this plant in malaria treatment, pharmacological screening was carried out. Using a rodent parasite, Spasmodic Joelie Nigerians, in Swiss albino mice, the plant was screened for its curative, prophylactic and suppressive application in malaria. Investigations of the physio-chemical properties of the powders of the bark and leaf indicated that these powders were mostly fibrous in nature, with relatively poor flow characteristics. Tablets produced by direct compression from the leaf powders were generally unacceptable when subjected to quality control tests. Those lab-lets produced from the bark and binary mixtures of the bark and leaf powders were of better quality. Avicenna pH 101 at low concentrations produced better quality tablets compared with the other diluent s: lactose and Starch Rx 1500. Tablets produced by wet granulation method were generally better than those of the direct compression method. Maize starch and polyvinyl pyrimidine produced good quality tablets when used as binders. On the other hand, tablets produced from the bark powders using methyl-cellulose as binder were generally friable with short disintegration times. The granule size fraction used was also found to have considerable influence on the resulting compact characteristics. For example, particle size fraction less than 500 μm but greater than 150 μm gave the best quality tablets. Microbiological investigations of the bark and leaf powders indicate moderate contamination with bacterial and fungal organisms. The predominant bacterial contaminants were spore-forming and non-sparing Bacillus while Aspergillus and mold were the dominant fungal organisms. No indicator organism {E. coli.. Ps. aeruginosa.. Salmonella spp, Staph, aureus and C. albicans) was detected. Aqueous and ethanol extracts of Azadirachta indica exhibited significant inhibition on the gram positive test organisms {B. subtitle Staph, aureus), C. Albanians and E. coli. Only little activity was exerted against Ps. oleaginous by the ethanol extract. Pharmacological screening of the bark and leaf powders of Adirondack indict showed that the plant has useful prophylactic and suppressive antimalarial activities but has very little curative property. The leaf powder exhibited higher degree of antimalarial effect than the bark powder. Extrapolation of the pharmacological data from the albino mice indicated that an adult human being may need to ingest about 155 tablets of a 300 mg weight per day for significant therapeutic improvement in malaria infection.
Description
A Thesis submitted to the Postgraduate School, Ahmadu Bello University, Zaria, In Partial Fulfillment of the Requirements for the Award of the Degree of Master of Science (Pharmaceutics) Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, NIGERIA MARCH, 1996
Keywords
TABLETING,, PROPERTIES,, BARK,, LEAF,, POWDERS,, AZADIRACHTA,, NDICA,
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