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1、ReductionofBitternessofAntihistaminicDrugsbyComplexationwithβ-CyclodextrinsNAOONO,1YUJIMIYAMOTO,1TAKAKOISHIGURO,2KEIICHIMOTOYAMA,1FUMITOSHIHIRAYAMA,2DAISUKEIOHARA,2HAKARUSEO,2SATOSHITSURUTA,2HIDETOSHIARIMA,1KANETOUEKAMA21GraduateSchoolofPharmaceuticalSciences,KumamotoUniversity,Kumamoto862-0
2、973,Japan2FacultyofPharmaceuticalSciences,SojoUniversity,Kumamoto860-0082,JapanReceived18April2010;revised24October2010;accepted30October2010Publishedonline28December2010inWileyOnlineLibrary(wileyonlinelibrary.com).DOI10.1002/jps.22417ABSTRACT:Reductionofbitternessofantihistaminicdrugsbycycl
3、odextrin(CyD)complexa-tionwasexamined.Thestabilityconstant(Kc)ofthe1:1CyDinclusioncomplexeswithantihis-taminicdrugsincreasedintheorderof2-hydroxypropyl-$-CyD(HP-$-CyD)≈$-CyD>(-CyD>"-CyDfordiphenhydramineandepinastine,andHP-$-CyD≈$-CyD>"-CyD>(-CyDforhydroxyzine,cetirizine,anddl-chlorphenirami
4、ne.Theinclusioncomplexesinhibitedthead-sorptionofantihistaminicdrugstolipidmembraneusingliposomes,asthemagnitudeofKcincreased.Fromhumangustatorysensationtests,$-CyDandHP-$-CyDpotentlysuppressedthebitternessofantihistaminicdrugsinadose-dependentmanner.Further,anarti?cialtastesensoranalysisrev
5、ealedthat$-CyDandHP-$-CyDinhibitedthebitternessofantihistaminicdrugsinsolution.TheresultssuggestthatCyDssuppressthebitternessofantihistaminicdrugsinsolutionsthroughtheformationofinclusioncomplexes.Theseresultsmayprovideusefulin-formationformaskingoreliminationofbitternessofdrugsusingCyDs.?20
6、10Wiley-Liss,Inc.andtheAmericanPharmacistsAssociationJPharmSci100:1935–1943,2011Keywords:cyclodextrins;tastemasking;inclusioncompounds;antihistaminicdrug;druginteraction;liposomes;arti?cialtastesensor;preformulationINTRODUCTIONinclusioncomplexeswithvariousmoleculesinaque-oussolutionandinsoli
7、dstates,andaresuccessfullyManypharmaceuticalmedicineshaveabittertaste,utilizedforimprovementofpharmaceuticalproper-whichmakesthemdif?cultorunpleasanttotake,giv-1–3tiesofdrugs.Recently,hydrophilicCyDderivativesingrisetononcomplianceandthusdecreasing
