A quantitative relationship has been derived for the physicochemical properties and pharmacological activity of alkyl ester prodrugs of ibuprofen. A comprehensive study consisting of aqueous solubility, octanol-water partition coefficient, hydrolysis kinetics in aqueous buffer (pH 7.4) & human plasma, ulcerogenic studies, anti-inflammatory and analgesic activity was carried on alkyl ester prodrugs of ibuprofen. n-Propyl and n-butyl esters offered significant improvement in oral delivery of ibuprofen in terms of reduced gastroulcerogenicity and maintenance of pharmacological activity.
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Bansal et al. (1994) studied this question.
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