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Article Dans Une Revue Drug Development and Industrial Pharmacy Année : 2006

Cyclodextrin inclusion complexes of the central analgesic drug nefopam.

Résumé

Inclusion complexes of nefopam base (NEF) with various beta-cyclodextrins (betaCDs) were investigated. All tested betaCDs increased the apparent solubility of NEF according to a Higuchi AL type plot (except betaCD: AN type plot), which indicates the formation of 1:1 stoichiometry inclusion complexes. 1H-NMR and 13C-NMR experiments showed that complexation by CDs allowed an easy separation of the R and S enantiomers. Based on spectral data obtained from the two-dimensional rotating frame nuclear Overhauser effect spectroscopy (2D-ROESY), a reasonable geometry for the complexes could be proposed implicating the insertion of the benzoxazocine ring into the wide end of the torus cavity.
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Dates et versions

hal-00399631 , version 1 (11-11-2016)

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Citer

H. Brun, M. Paul, N. Razzouq, M. Binhas, Stéphane Gibaud, et al.. Cyclodextrin inclusion complexes of the central analgesic drug nefopam.. Drug Development and Industrial Pharmacy, 2006, 32 (10), pp.1123-34. ⟨10.1080/03639040600920663⟩. ⟨hal-00399631⟩
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