Interaction of tri-O-methyl-β-cyclodextrin with drugs View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1984-09

AUTHORS

Yoshinobu Nakai, Keiji Yamamoto, Katsuhide Terada, Hidetoshi Horibe

ABSTRACT

The effect of tri-O-methyl-β-cyclodextrin(methyl-β-CD) on the partition coefficients of drugs, such as p-nitrophenol, salicylic acid, benzoic acid, and aspirin, was studied at 25°C. The partition coefficients of these drugs were increased linearly with methyl-β-CD concentration. The increase of partition coefficients was interpreted by the 1∶1 complex formation between methyl-β-CD and the drug in CHCl3 phase. The interaction between p-nitrophenol and methyl-β-CD in solution was studied by UV and PMR spectroscopies. It was concluded that p-nitrophenol is included in the cavity of methyl-β-CD in both aqueous solution and CHCl3 solution. Inclusion compounds of these drugs with methyl-β-CD in the solid state were studied by X-ray diffractometry, IR spectroscopy, and DSC measurements. 1∶1 crystalline inclusion compounds were obtained from hot water. It is also suggested that amorphous inclusion compound was obtained by the grinding of drug with methyl-β-CD. The dissolution rate and the bioavailability of ketoprofen were significantly increased in the presence of methyl-β-CD. The bioavailability of ketoprofen after oral administration with methyl-β-CD to rats was 3.7 times that of ketoprofen alone. More... »

PAGES

523-531

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/bf00662218

DOI

http://dx.doi.org/10.1007/bf00662218

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1017385632


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