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- W2079016779 abstract "Abstract Various N-substituted [(3- or 4-aminomethyl)benzoyloxymethyl]allopurinol derivatives were synthesized by esterification of 1-(hydroxymethyl)allopurinol and evaluated as water-soluble prodrugs with the aim of developing preparations suitable for parenteral and/or rectal administration. The derivatives combine a good solubility and high chemical stability in weakly acidic solutions with a high susceptibility to undergo enzymatic hydrolysis in plasma. The derivatives were much more lipophilic than allopurinol as determined by partition experiments in octanol-aqueous buffer solution. The rectal and parenteral absorption characteristics of three derivatives and of allopurinol were assessed in rabbits. Following intravenous administration the derivatives were quickly converted yielding allopurinol in quantitative amounts. After rectal administration of the three prodrugs an absolute bioavailability of 19, 38 and 41%, respectively, was found whereas the rectal absorption of allopurinol itself was only 3%." @default.
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- W2079016779 date "1990-10-01" @default.
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- W2079016779 title "Allopurinol prodrugs. V. Water-soluble N-substituted (aminomethyl)benzoyloxymethyl allopurinol derivatives for parenteral or rectal delivery" @default.
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- W2079016779 doi "https://doi.org/10.1016/0378-5173(90)90181-3" @default.
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