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Improvement of some pharmaceutical properties of carmoful by cycrodextrin complexation

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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.

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Authors and Affiliations

  1. Faculty of Pharmaceutical Sciences, Kumamoto University, 5-1, Oe-honmachi, 862, Kumatoto, Japan

    Masahiko Kikuchi, Yuji Uemura, Fumitoshi Hirayama, Masaki Otagiri & Kaneto Uekama

Authors
  1. Masahiko Kikuchi
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  2. Yuji Uemura
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  3. Fumitoshi Hirayama
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  4. Masaki Otagiri
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  5. Kaneto Uekama
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Kikuchi, M., Uemura, Y., Hirayama, F. et al. Improvement of some pharmaceutical properties of carmoful by cycrodextrin complexation. Journal of Inclusion Phenomena 2, 623–630 (1984). https://doi.org/10.1007/BF00662228

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  • DOI: https://doi.org/10.1007/BF00662228

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