O-Carboxymethyl-O-ethyl-β-cyclodextrinによる1-Hexylcarbamoyl-5-fluorouracil (HCFU) の安定性及びバイオアベイラビリティの向上

概要

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The possible utility of O-carboxymethyl-O-ethyl-β-cyclodextrin (CME-β-CyD) as a novel drug carrier was studied in vitro and in vivo, by using 1-hexylcarbamoyl-5-fluorouracil (HCFU) as a model drug. The chemical instability of HCFU in solution and solid state was improved by CME-β-CyD complexation. The in vitro release of HCFU from the CME-β-CyD complex was decelerated in acidic solution, while accelerated at neutral pH regions, showing a typical delayed-release pattern. This pattern was clearly reflected in the blood levels after the oral administration of the complex to dogs, increasing the bioavailability. The present results suggested that CME-β-CyD is useful as a delayed-release-type carrier for the oral administration of chemically labile HCFU.
社団法人日本薬学会の論文
1991-10-25