Improvement of Stability and Bioavailability of 1-Hexylcarbamoyl-5-fluorouracil (HCFU) by O-Carboxymethyl-O-ethyl-β-cyclodextrin
- 1 January 1991
- journal article
- abstracts
- Published by Pharmaceutical Society of Japan in YAKUGAKU ZASSHI
- Vol. 111 (10) , 592-599
- https://doi.org/10.1248/yakushi1947.111.10_592
Abstract
The possible utility of O-carboxymethyl-O-ethyl-beta-cyclodextrin (CME-beta-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-beta-CyD complexation. The in vitro release of HCFU from the CME-beta-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-beta-CyD is useful as a delayed-release-type carrier for the oral administration of chemically labile HCFU.Keywords
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