Some physico-chemical studies on Griffonin, an anti-sickling agent

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1990-09-16
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This work has defined certain aspects of preformulation that will need to be considered if griffonin an antisickling agent, is to be used as a drug. A relatively more efficient method of isolating griffonin from the dried root bark of Griffonia siuiplicifolia has been worked out. This method takes advantage of the insolubility of griffonin in ethyl acetate. This method is cheaper in terms of solvents used and offers higher yields. The amount of griffonin in the dried root bark of Griffonia simplicifolia has been quantitatively determined. An Infra—red assay method based on the concept of analysis of solids in potassium bromide [KBr] using an internal standard was used. The value obtained was found to be comparable with that given by the improved method of extraction. Partition coefficient studies have been carried out on griffonin. These have shown that griffonin is present as a common species in both water and octanol. The effect of gastric acid on breakdown rate of griffonin has been studied. In vitro kinetic studies based on the Arrhenius equation was applied. It was found that the deleterious effect of gastric acid on griffonin was not enough to prevent its use as a drug to be taken orally. A claim that the cyano group (-CN) in Griffonin can be converted to an amido group (-CONR2) by a hydrolytic process while leaving the rest of the molecule unaltered has been investigated. It involved refluxing a mixture of griffonin and potassium hydroxide (powdered) in a non aqueous medium. A crystalline product with a very high melting point (abo, 360°C) was obtained. However, enough evidence was not obtained from the work to prove the truth or otherwise
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A thesis submitted to the Board of Postgraduate Studies, Kwame Nkrumah University of Science and Technology, Kumasi, in partial fulfilment of the requirements for the award of the Degree of Master of Pharmacy, 1990
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