环糊精包合特性及包合常数的测定和预测-金小江

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labeledproteinnanoparticlesascarriersforbiotinylatedpep-tidenucleicacid[J].EurJPharmBiopharm,2000,49(3):303-3101[21]GrefR,CouvreurP,BarrattG,etal.Surface-engineerednanoparticlesformultipleligandcoupling[J].Biomaterials,2003,24(24):4529-45371[22]BalthasarS,MichaelisK,DinauerN,etal.Preparationandcharacterisationofantibodymodifiedgelatinnanoparticlesasdrugcarriersystemforuptakeinlymphocytes[J].Biomateri-als,2005,26(15):2723-27331[23]RoyI,MitraS,MaitraA,etal.Calciumphosphatenanoparticlesasnovelnon-viralvectorsfortargetedgenede-livery[J].IntJPharm,2003,250(1):25-331[24]OlivierJC.Synthesisofpegylatedimmunonanoparticles[J].PharmRes,2002,19(8):1137-11431[25],,,.[J].生物医学工程学杂志,2004,21(4):570-5741[26]YamamotoY,NagasakiY,KatoM,etal.Surfacechargemodulationofpoly(ethyleneglycol)-poly(D,L-lactide)blockcopolymermicelles:conjugationofchargedpeptides[J].ColloidSurfB(Biointerface),1999,16(1):135-1461[]2005-05-08*:周建平,博士,教授;:药物新剂型与新制剂;Tel:025-83271272;E-mail:Zhoujianp60@163.com环糊精包合特性及包合常数的测定和预测金小江,周建平*(中国药科大学药剂教研室,江苏南京210009)[]-,,-[];;;[]Q7;R91[]A[]1001-5094(2005)11-0491-07TheCharacteristicsofCyclodextrin/DrugInclusionComplexesandtheMethodsofDeterminatingandPredictingInclusionConstantsJINXiao-jiang,ZHOUJian-ping*(DepartmentofPharmaceutics,ChinaPharmaceuticalUniversity,Nanjing210009,China)[Abstract]Thecharacteristicsofcyclodextrinoritsderivatives/druginclusioncomplexeswereintroduced,includingthethermodynamicpropertiesandtheadvantagesoverothermethodstoimprovethesolubilityofwa-ter-insolubledrugs.ThesignificanceoftheinclusionconstantKwasespeciallyemphasizedandthemethodsofdeterminatingandpredictingitwerealsodiscussedindetail.[Keywords]B-Cycledextrin;Derivative;Inclusioncomplex;Inclusionconstant(CD)/,0,,,2005年第29卷第11期第491页ProgressinPharmaceuticalSciences##2005,Vol.29,No.11491(1)A-B-CD,-B-CD(44165)USP28/NF231(Tab11Thelaunchedcyclodextrins/drugindusioncomplexes)A-CDAlprostadil(PGE1)Prostavastin,,CefotiamhexetilHClPansporinTB-CDBenexateHClUlgut,LonmielDexamethasoneGlymesasonIodineMena-GargleNicotineNicoretteNimesulideNimedex,MesulidNitroglycerinNitropenOmeprazolOmebetaPGE2ProstarmonEPiroxicamBrexinTiaprofenicacidSurgamyl2--B-CDCisapridePropulsidHydrocortisoneDexocortIndomethacinIndocidItroconazole,Sporanox,MitomycinMitozytrex-B-CD17B-EstradiolAerodiolChloramphenicloClorocilB-CDVoriconazoleVfend,ZiprasidonemaleateGeodon,Zeldox,2--C-CDDiclofenacsodiumVoltarenB-CD,,,,,,,K()1,,,011g/L,10g/L50%-,5g/L,,,1B1,,1B1,,B-CD1B1,(1)[1]1A,,,B-CD1B,B-CD,,##4922005,Vol.29,No.112005年第29卷第11期第492页ProgressinPharmaceuticalSciences[Dt]:;[CDt]:;S0:1A:400B-CD1B1;B:B-CD1B11B2(Fig1.A:Phasesolubilityof1B1inclusioncomplexofanantihypertensivewithMW400andB-CD;B:Phasesolubilityof1B1and1B2inclusioncomplexesofacertaindrugandB-CD),LÊscher[2],glycofural,glycofural,HP-B-CD,5:[Dt][CDt],AB,A,BA3:AL,;AP,1B1;,AN(),B2:BS;BIBS,,,;,,BI,,,(2)[3]St:;Sc:25(Fig21Phasesolubilityof5typesofinclusioncomplexes)2-K211KK(CD)(D)(CD-D),K,1B1,:D+CDWD-CD,K=[CD-D]/([D][CD]),[CD-D][D][CD]2005年第29卷第11期第493页ProgressinPharmaceuticalSciences##2005,Vol.29,No.11493K0~105(mol/L)-1-KA-CDB-CDC-CDK123490525(mol/L)-1K,-,,212KK-[4],ALK,APANKALKmBn,mD+nCDWDm-CDn,K=[Dm-CDn]/([D]m[CD]n),n1:[Dt]=mKSm0[CDt]/(1+KSm0)+S0(1)(1),m,,m[mKS0m/(1+KS0m)]KK,,[5]HB:HBKaH++B-++CDCD|K0|K-HB-CDWB--CDKa=[B-][H+]/[HB],HB;K0=[HB-CD]/([HB][CD]),HB;K-=[B--CD]/([B-][CD]),B-:St-S0c=K0cS0c[CDt]/(1+K0cS0c)K0c=(K0[H+]+K-Ka)/(Ka+[H+])(2)S0c=(Ka+[H+])S0/[H+](3)K0cS0cpH(2)(3),,,pH:S0d=(Ka+[H+])S0/Ka(4)K0d=(K0Ka+K+[H+])/(Ka+[H+])(5)K0dS0dpH,K+(2)~(5),KocKod,KapHpH213KK,K21311K,,()(),,K:$GCOMP*=$Gintrasol+($GwC-$GwS-$GwL)+$gAC1(6)$GCOMP*=-RTlnKMF,KMF=QM*K1B1(7)KMF,;Q;M*;$Gintrasol-;$GwC$GwS$GwL;$gAC1,C1,$gA=gAC-gAS-gAL,ACASAL(,),g,[AC-(AS+AL)],$gA0,(5)~(7):lgK1B1=-lgQM*-Z/213RT-$AgC1/213RT(8)Z=$Gintrasol+($GwC-$GwS-$GwL),K1B1Z$A,,##4942005,Vol.29,No.112005年第29卷第11期第494页ProgressinPharmaceuticalSciences,K:¹-$A=-Cornors[6]X-,A-CD125!2(1!=011nm),(8)-$A125,0,-$A=0,-$A=125ºZCornors[6]K1B1(8)Z,Z,Z$AZ,KCornors[6]-A-CDlgK2151,2188;4--A-CDlgK2146,2136;-A-CDlgK1119,111721312K,,,,,:RM()Ò()HammettR()PC(),,K(QSAR),(TSAR),Levenberg-Marguardt()BFGS,,Loukas[7],7,[8]561,4-A-CD461,4-B-CD,RMÒHam-mettR6,,01964183,,(surfectan-tlikeeffects)(sel-faggregation)(3)[9]-(non-inclusioncy-clodextrincomplexes)-(inclusioncomplexes),3(Fig31Thepossibleexistingformsofdrugmoleculeinthecyclodextrinsolution)2005年第29卷第11期第495页ProgressinPharmaceuticalSciences##2005,Vol.29,No.11495[10,11],,Gabelica[12,13]A-CDA,X-,,1B1A,X--,2B1,1B1A-CD-,Correia[14]2B1--B-CD1B1--B-CD,Andronati[15]1B22B2-,(),-[16],[17],,,-,[18]Loftsson[19]-nB1,(AL),1B1=S0K/(S0K+1),1;n\2,n:St=S0+k(Csurf-CMC),k,Csurf,CMC1B1St=S0+S0K[CDt]/(S0K+1),,,,=S0K/(S0K+1)@(1+k),1Loftsson[19]HP-B-CD,1,11171134,Jobcsplot(spacefillingdocking)1B111B1,,1B1Loftsson[19],HP-B-CDHP-B-CD,2,-HP-B-CD,HP-B-CD,,-HP-B-CD,17B-HP-B-CD,4,,,,[][1]RajewskiA,StellaJ.Pharmaceuticalapplicationsofcyclodex-trins.2.Invivodrugdelivery[J].JPharmSci,1996,85(11):1142-11691[2]LÊscherW,HoenackD,RichterA,etal.Newinjectableaqueouscarbamazepinesolutionthroughco

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