PowderTechnology187(2008)214–221ContentslistsavailableatScienceDirectPowderTechnologyjournalhomepage:www.elsevier.com/locate/powtecFormulation,characteristicsandaerosolizationperformanceofazithromycinDPIpreparedbyspray-dryingMinZhao,YuYou,YachaoRen,YuZhang,XingTang⁎DepartmentofPharmaceutics,ShenyangPharmaceuticalUniversity,WenhuaRoad103,Shenyang110016,LiaoningProvince,PRChinaARTICLEINFOABSTRACTArticlehistory:Inthisstudy,anumberofdrypowderformualtionsofazithromycinforinhalationweredesignedtooptimizeReceived3May2007thecompositionandfurtherexploretherelationshipbetweenthecomposition,thephysicalpropertiesandtheReceivedinrevisedform18January2008aerosolizationperformance,hencedevelopingadrypowderinhalation(DPI)ofazithromycin(AZI)asanAccepted29February2008alternativetoitscounterpartnebulizer.Drypowdersofazithromycinwithavarietyofcarriertypesandcarrier:Availableonline7March2008drugratioswerepreparedbyspray-dryingandcharacterizedafterwardsfordifferentphysicalproperties,flKeywordsincludingparticlesizeanddistribution,morphology,owability,powderdensityandhygroscopicnature.In-−1®Azithromycinvitrodepositionwasalsoevaluatedaftertheaerosolizationofpowdersat60LminviatheAerolizerintoaDrypowderinhalationtwin-stageliquidimpinger(TI).ItwasfoundthatthetypeandamountofthecarrierhadsignificanteffectsonCarriertheaerosolizationperformanceofDPI.TheresultsalsoshowedthattheparticlesizeandflowabilityweretwoSpray-dryingcriticalphysicalpropertiesresponsiblefortheaerosolizationperformance.Specifically,moderateparticlesizeAerosolizationperformancearound5–6µmproducedrelativelyhighrespirablefractions(RF).Intermsoftheflowability,theangleofreposewithintherangeof43°–52°wasinagoodlinearrelationship(r=0.9523)withtheRFvalue.Inparticular,theadditionofL-leucinewiththecarrier:drugratioof1:5showedthehighestRFat37.5%,whichindicatedthatL-leucineisapromisingcarrierforthedrypowderformulationofAZIforinhalation.©2008ElsevierB.V.Allrightsreserved.1.Introductionareattractivecandidatesfo