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1、InternationalJournalofPharmaceutics172(1998)179±188Effectofsurfacemorphologyofcarrierlactoseondrypowderinhalationpropertyofpranlukasthydrate1YoshiakiKawashima*,TakanoriSerigano,TomoakiHino,HiromitsuYamamoto,HirofumiTakeuchiGifuPharmaceuticalUni6ersity,5
2、-6-1,Mitahora-higash,Gifu,502-8585,JapanReceived30March1998;receivedinrevisedform25May1998;accepted10June1998AbstractTheeffectsofsurfacemorphologyofcarrierlactoseondrypowderinhalation(DPI)propertyofpranlukasthydrate(PH)wereinvestigated.ThePHwasmixedwith
3、9-foldweightsofcarrierlactose,i.e.pharmatose325M,200M,DCL-11,DCL-21,spraydriedamorphous(SDGa),-crystallized(SDGc)lactosesand¯uidizedbedgranulatedlactose(FBG)withvarioussurfacemorphologies.ThesemixedpowderswereaerosolizedbyaSpinhaler®andinvitrodeposition
4、propertieswereevaluatedbyatwinimpinger.Carrierlactosewithhigherspeci®csurfacearea,i.e.surfaceroughness,likeFBGemittedeffectivelyPHparticlesfromtheinhalationdevice,whereastheyreducedtherespirablefractioncapturedinthetwinimpinger,resultinginlowerinhalatio
5、nef®ciency,duetostrongadhesionofPHtothecarrierlactose.TheSDGchavinglotsofmicroscopicalprojectiononthesurfaceincreasedtherespirableparticlepercentoftheemittedparticles,improvingtheinhalationef®ciency.TheSDGa,smoothedsphereparticle,didnotsoimprovetheinhal
6、ationef®ciencyasexpected,owingtofairlystrongadhesionbetweenPHandlactoseparticles.Those®ndingindicatedthattheseparationofdrugparticlesfromcarrierlactosewasadeterminingsteptoimproveinhalationprocessforDPIs,asfaraslactoseparticlesemittedsatisfactorilyPHpar
7、ticlesfromtheinhalationdevice.ThesurfacemorphologydesignedlikeSDGc,havingfairlylargesurfaceareawithmicroscopicallyincreasedsurfaceroughnesswasdesirabletoimproveinhalationpropertyofDPI.©1998ElsevierScienceB.V.Allrightsreserved.Keywords:Powdersforinhalati
8、on;Carrierlactose;Particlemorphology;Crystallineform1.Introduction*Correspondingauthor.Tel.:81582373931;fax:81Drypowderinhalationaerosols(DPIs)forpul-582376524.1monarydeliveryofanti-asthmaticagent(SmithPresentaddress:FacultyofP
