Springer Online Journal Archives 1860-2000
Chemistry and Pharmacology
Abstract Inclusion complexation of carmoful (1-hexylcarbamoyl-5-fluorouracil, HCFU) with three cyclodextrins (α-, β- and γ-CyDs) were studied by solubility method and X-ray diffractometry. On the basis of the phase solubility diagrams, solid complexes of HCFU with α-, β- and γ-CyDs were obtained in the molar ratios (host:guest) of 2∶1, 1∶1 and 1∶1, respectively. The dissolution rate of HCFU from the solid complexes was much greater than that of HCFU itself (α-CyD 〉 complex 〉 β-CyD complex 〉 γ-CyD complex 〉 HCFU alone). The hydrolysis of HCFU was suppressed by β-CyD, while no appreciable inhibition was observed by α- and γ-CyDs. The rapid dissolving form of HCFU-CyD complexes was found to increase significantly the serum levels of the drug after oral administration to rabbits.
Type of Medium: