Titre du document / Document title

Preparation and study the 1:2 inclusion complex of carvedilol with β-cyclodextrin

Auteur(s) / Author(s)

XIANHONG WEN ⁽¹⁾ ; FEI TAN ⁽¹⁾ ; ZHIJUN JING ⁽²⁾ ; ZIUYANG LIU ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Chemistry of Zhejiang University, Zhe da yu Quan Xiao qu, Hangzhou 310027, CHINE
⁽²⁾ Zhejiang Hisun Pharmaceutical Co. Ltd., Jiaojiang 317700, CHINE

Résumé / Abstract

An inclusion complex of β-cyclodextrin with carvedilol was prepared by using a convenient new method of microwave irradiation. Phase-solubility studies demonstrated the ability of β-cyclodextrins to complex with carvedilol and increase drug solubility. The structure of inclusion complex was determined by fluorescence spectroscopy and ¹H NMR, ¹³C NMR measurements in solution. The solid inclusion was characterised by infrared spectroscopy, differential scanning calorimetry (DSC) and element analysis. These experimental results confirmed the existence of 1:2 inclusion complex of carvediolo with β-cyclodextrin, the formation constant of complex was determined by the fluorescence method. Molecular modeling predicted the energy-minimized structure of the complex.

Revue / Journal Title

Journal of pharmaceutical and biomedical analysis   ISSN 0731-7085   CODEN JPBADA 

Source / Source

2004, vol. 34, n^o3, pp. 517-523 [7 page(s) (article)] (44 ref.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Amsterdam, PAYS-BAS  (1983) (Revue)

Mots-clés anglais / English Keywords

β2-Adrenergic receptor ; β1-Adrenergic receptor ; α1-Adrenergic receptor ; Beta blocking agent ; Alpha blocking agent ; Antagonist ; β-Cyclodextrin ; Vasodilator agent ; Antihypertensive agent ; Modeling ; Microwave irradiation ; Carvedilol ;

Mots-clés français / French Keywords

Récepteur β2-adrénergique ; Récepteur β1-adrénergique ; Récepteur α1-adrénergique ; Bloquant β-adrénergique ; Bloquant α-adrénergique ; Antagoniste ; β-Cyclodextrine ; Vasodilatateur ; Antihypertenseur ; Modélisation ; Irradiation hyperfréquence ; Carvédilol ;

Mots-clés espagnols / Spanish Keywords

Receptor β2-adrenérgico ; Receptor β1-adrenérgico ; Receptor α1-adrenérgico ; Bloqueador β-adrenérgico ; Bloqueador α-adrenérgico ; Antagonista ; β-ciclodextrina ; Vasodilatador ; Antihipertensivo ; Modelización ; Irradiación hiperfrecuencia ; Carvedilol ;

Mots-clés d'auteur / Author Keywords

Carvedilol ; β-Cycloextrin ; Inclusion complex ; NMR ; Microwave irradiation ; Molecular modeling ;

Localisation / Location

INIST-CNRS, Cote INIST : 19962, 35400011648996.0080