医药学英文文献.doc

Abstract Meloxicam- -cyclodextrin (ME- -CD) inclusion complex was prepared by a fluid-bed coating technique upon solvent removal and simultaneous depositing onto the surface of nonpareil pellets and using PVP K30 as a binding agent to facilitate good coating. The resultant pellets were spherical and intact in shape with good flowability and friability. SEM analysis showed that the pellets were smooth and had a tightly coated inclusion complex layer. In vitro dissolution of the inclusion complex pellets in pH 7.4 phosphate buffer was dramatically enhanced at an ME/CD ratio of 1/1. DSC and powder X-ray diffractometry proved the absence of crystallinity in the ME/CD inclusion complexes. Moreover, Fourier transform-infrared spectrometry together with Raman spectrometry indicated that the thiazole ring of ME was possibly included in the cavity of -CD. ? 2008 Chinese Society of Particuology and Institute of Process Engineering, Chinese Academy of Sciences. Published by Elsevier B.V. All rights reserved. Keywords: Meloxicam; Inclusion complex; -Cyclodextrin; Fluid-bed; Pellets; Dissolution; Characterization 1. Introduction Cyclodextrins (CDs) comprise a family of cyclic oligosaccha- rides, of which several members are used in many applications associated with the pharmaceutical, agrochemical, fragrance, and food industries (DavisBrewster, 2004). Basic CDs of pharmaceutical interest contain six (a-CD), seven ((3-CD) and eight (y-CD) (a一1,4)-linked a-n-glucopyranose units (Brewster Loftsson, 2007). Due to the chair configuration of the glucopyranose units, the CDs take the shape of a truncated cone or torus with the hydroxyl groups oriented to the cone exterior, which makes the entire CD molecule water-soluble (LoftssonBrewster, 1996; StellaRajewski, 1997). The central cavity of the CD molecule is lined with skeletal car- bon and ethereal oxygen moieties of the glucose residue, which make it relatively apolar and creates a hydropho- bic microenvironment (LoftssonBrewster,