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1、Monographs:Pharmaceuticalsubstances:Tenofoviridisoproxilifumaras-TenofovirdisoproxilfumarateC19H30N5O10P,C4H4O4Relativemolecularmass.635.5Chemicalname.1,1'-bis(1-methylethyl)1,1'-[({[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl}phosphonoyldioxy)dimethyl]dicarbonate(ester)hydrogen(2E)-but-2
2、-enedioate(salt);CASReg.No.202138-50-9.Description.Whitetoalmost-white,crystallinepowder.Solubility.Slightlysolubleinwater,solubleinmethanol,veryslightlysolubleindichloromethane.Category.Antiretroviral(NucleotideReverseTranscriptaseInhibitor).Storage.Tenofovirdisoproxilfumarateshouldbekeptinatight
3、lyclosedcontainer,protectedfromlight,andstoredatatemperaturebetween2and8°C.Additionalinformation.Tenofovirdisoproxilfumaratemayexhibitpolymorphism.RequirementsDefinition.Tenofovirdisoproxilfumaratecontainsnotlessthan98.5percentandnotmorethan101.0percentoftenofovirdisoproxilfumarate(C19H30N5O10P,C4
4、H4O4),calculatedwithreferencetotheanhydroussubstance.Manufacture.Theproductionmethodisvalidatedtoensurethatthesubstance,iftested,wouldcomplywith:-alimitofnotmorethan5ppmforthemutagenicimpurity9-(prop-1-enyl)-9H-purin-6-amine(impurityK),whichmaybeasynthesisrelatedsubstance,usingasuitablemethod,and-
5、alimitofnotmorethan1.0%forthetenofovirdisoproxil(S)-enantiomer(impurityG),usingasuitablechiralchromatographicmethod.Identitytests•EithertestsA,BandCortestDmaybeapplied.A.CarryouttestA.1or,whereUVdetectionisnotavailable,testA.2.A.1Carryoutthetestasdescribedunder1.14.1Thin-layerchromatography,usings
6、ilicagelR6asthecoatingsubstanceandamixtureof67volumesofdichloromethaneR,20volumesofacetonitrileR,10volumesofmethanolRand3volumesofammonia(~260g/l)TSasthemobilephase.Applyseparatelytotheplate5μlofeachof2solutionsinmethanolcontaining(A)10mgofthetestsubstancepermland(B)10mgoftenofovirdisoproxilfumara
7、teRSperml.Afterremovingtheplatefromthechromatographicchamber,allowittodryexhaustivelyinairorinacurrentofair.Examinethechromatograminultravioletlight(254nm).TheprincipalspotobtainedwithsolutionAcorrespondsinpositi
