Cyclodextrin Inclusion Complexes of the Central Analgesic Drug Nefopam

Autor: Muriel Paul, H. Brun, Stéphane Gibaud, Alain Astier, N. Razzouq, M. Binhas
Přispěvatelé: Department of Pharmacy, Henri Mondor University Hospitals, Henri Mondor University Hospitals, Cibles thérapeutiques, formulation et expertise pré-clinique du médicament (CITHEFOR), Université de Lorraine (UL)
Rok vydání: 2006
Předmět:
Models
Molecular
MESH: Analgesics
Non-Narcotic
Pharmaceutical Science
Beta-Cyclodextrins
02 engineering and technology
Nuclear Overhauser effect
030226 pharmacology & pharmacy
chemistry.chemical_compound
0302 clinical medicine
Nefopam
Models
Spectroscopy
Fourier Transform Infrared
MESH: Nuclear Magnetic Resonance
Biomolecular
Drug Discovery
MESH: Animals
Solubility
Spectroscopy
MESH: Biological Availability
chemistry.chemical_classification
Analgesics
Cyclodextrin
beta-Cyclodextrins
Stereoisomerism
Analgesics
Non-Narcotic
[SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences
021001 nanoscience & nanotechnology
MESH: Nefopam
MESH: Administration
Sublingual
Administration
0210 nano-technology
MESH: Models
Molecular
medicine.drug
Sublingual
MESH: beta-Cyclodextrins
Macromolecular Substances
Stereochemistry
Nuclear Magnetic Resonance
Administration
Sublingual
Biological Availability
In Vitro Techniques
MESH: Spectroscopy
Fourier Transform Infrared
Inclusion compound
03 medical and health sciences
Non-Narcotic
MESH: Water
medicine
Animals
Humans
Nuclear Magnetic Resonance
Biomolecular
Pharmacology
MESH: Humans
Organic Chemistry
Water
Molecular
MESH: Macromolecular Substances
MESH: Stereoisomerism
MESH: Solubility
Crystallography
chemistry
Fourier Transform Infrared
Enantiomer
Biomolecular
Zdroj: Drug Development and Industrial Pharmacy
Drug Development and Industrial Pharmacy, Taylor & Francis, 2006, 32 (10), pp.1123-34. ⟨10.1080/03639040600920663⟩
ISSN: 1520-5762
0363-9045
DOI: 10.1080/03639040600920663
Popis: International audience; 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.
Databáze: OpenAIRE
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