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1、AbstractMeloxicam--cyclodextrin(ME--CD)inclusioncomplexwaspreparedbyafluid-bedcoatingtechniqueuponsolventremovalandsimultaneousdepositingontothesurfaceofnonpareilpelletsandusingPVPK30asabindingagenttofacilitategoodcoating.Theresultantpelletsweresphericalandintactinshapewithgoodfl
2、owabilityandfriability.SEManalysisshowedthatthepelletsweresmoothandhadatightlycoatedinclusioncomplexlayer.InvitrodissolutionoftheinclusioncomplexpelletsinpH7.4phosphatebufferwasdramaticallyenhancedatanME/CDratioof1/1.DSCandpowderX-raydiffractometryprovedtheabsenceofcrystallinityi
3、ntheME/CDinclusioncomplexes.Moreover,Fouriertransform-infraredspectrometrytogetherwithRamanspectrometryindicatedthatthethiazoleringofMEwaspossiblyincludedinthecavityof-CD.©2008ChineseSocietyofParticuologyandInstituteofProcessEngineering,ChineseAcademyofSciences.PublishedbyElsevie
4、rB.V.Allrightsreserved.Keywords:Meloxicam;Inclusioncomplex;-Cyclodextrin;Fluid-bed;Pellets;Dissolution;Characterization1.IntroductionCyclodextrins(CDs)compriseafamilyofcyclicoligosaccha-rides,ofwhichseveralmembersareusedinmanyapplicationsassociatedwiththepharmaceutical,agrochemic
5、al,fragrance,andfoodindustries(Davis&Brewster,2004).BasicCDsofpharmaceuticalinterestcontainsix(a-CD),seven((3-CD)andeight(y-CD)(a一1,4)-linkeda-n-glucopyranoseunits(Brewster&Loftsson,2007).Duetothechairconfigurationoftheglucopyranoseunits,theCDstaketheshapeofatruncatedconeortorusw
6、iththehydroxylgroupsorientedtotheconeexterior,whichmakestheentireCDmoleculewater-soluble(Loftsson&Brewster,1996;Stella&Rajewski,1997).ThecentralcavityoftheCDmoleculeislinedwithskeletalcar-bonandetherealoxygenmoietiesoftheglucoseresidue,whichmakeitrelativelyapolarandcreatesahydrop
7、ho-bicmicroenvironment(Loftsson&Brewster,1996;Stella&Rajewski,1997).ThesepropertiesendowtheCDswiththeabilitytohostavarietyofhydrophobicguestmoleculestoforminclusioncomplexes.Theencapsulationofdrugmoleculesintothehydrophobiccavitiesisaimedatimprovingtheirsolubility,stabilityandoth
8、erproperties,andhasbeenthebasisofmanypha
