抗AIDS薬2',3'-ジデオキシイノシン(DDI)プロドラツグの合成と油性基剤を用いた経口投与後の血中濃度推移
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概要
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Four ester derivatives of 2′, 3′-dideoxyinosine (DDI), acetate (C2-DDI), octanoate (C8-DDI), benzoate (Bz-DDI), and hemisuccinate (Suc-DDI), were synthesized from deoxyinosine, and evaluated as a prodrug of DDI, The esters were proved to quantitativery regenerate DDI in the presence of human plasma. Absolute bioavailability was evaluated by an oral administration to rats by using water or olive oil as a solvent. Hydrophobic prodrugs, C8-DDI and Bz-DDI, showed higher bioavailavility when administered as a water suspension than as an oil solution, though hydrophilic prodrugs, C2-DDI and Suc-DDI, showed higher bioavailability with an oil suspension than with a solution in water.
- 日本DDS学会の論文
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