betadex and carmofur

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.

Topics: Administration, Oral; Animals; Antineoplastic Agents; beta-Cyclodextrins; Cyclodextrins; Delayed-Action Preparations; Dogs; Drug Carriers; Drug Stability; Fluorouracil; Hydrogen-Ion Concentration; In Vitro Techniques; Intestinal Absorption; Male; Solubility

Topics: Administration, Oral; Administration, Rectal; Animals; Antineoplastic Agents; beta-Cyclodextrins; Cyclodextrins; Dextrins; Fluorouracil; Male; Rabbits; Starch

Topics: beta-Cyclodextrins; Chemical Phenomena; Chemistry; Cyclodextrins; Drug Stability; Fluorouracil