物理药剂学-课件

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ColloidaldispersionsystemClassificationofdispersedsystembasedonparticlesizeclassParticlesizeCharacteristicsofsysteme

xampleMoleculardispersionLessthan1nmInvisibleinelectronmicroscopePassthroughultrafilterandsemipermeablemembraneund

ergorapiddiffusionOxygenmolecules,ordinaryions,glucoseColloidaldispersionFrom1nmtoo.5μmNotresolvedbyordinarymicroscope(althoughmaybed

etectedunderultramicroscope)VisibleinelectronmicroscopePassthoughfilterpaperDonotpasssemipermeablemembraneD

iffusionveryslowlyColloidalsilversols,naturalandsyntheticpolymers,cheese,butter,jelly,milk,etc.Coarsedispersion

Greaterthano.5μmVisibleundermicroscopeDonotpassthoughnormalfilterpaperDonotdialyzethoughsemipermeablemenmbraneDonotdiff

usionGrainsofsand,mostpharmaceuticalemulsionsandsuspension,redbloodcellsTypesofColloidaldispersionLyophiliccolloi

dsSystemscontainingcolloidalparticlesthatinteracttoanappreiableextentwiththedispersionmediumarereferre

dtoaslyophilic(solvent-loving)colloids.hydrophilicsols:gelatin,acacia,insulin,albuminLipophiliccolloids:rubbe

r,polystyrene.Amaterialthatformsalyophiliccolloidalsysteminoneliquid(e.g.water)maynotdosoinanotherliquid(e.g.benzene).Ly

ophobiccolloidsLyophobiccolloidsiscomposedofmaterialsthathavelittleattraction.e.g.gold,silver,sulfur,arsenoussu

lfide,andsilveriodide.Themethodstopreparelyophobiccolloids•Dispersionmethods1,grindingmethod2,sonicationdispersionmethod3,arcdischargemethod

•Condensationmethods1,physicalmethods2,chemicalmethodsgrindingmethodsonicationdispersionmethodarcdischargemethod•Owingtotheintenseheatgeneratedb

ythearc,someofthemetaloftheelectrodesisdispersedasvapor,whichcondensestoformcolloidalparticles.Physicalcondensationmetho

ds1,replacementofsolventPhysicalcondensationmethods2,Steamquenchmethodchemicalcondensationmethods•2H3AsO3(w)+3H2S→As2S3(sol)+6H2O•

FeCl3(w)+3H2O(H)→Fe(OH)3(sol)+3HCl•2H2S(w)+SO2(g)→2H2O+3S(sol)•Na2S2O3+2HCl→2NaCl+H2O+SO2+S(sol)•2HAuCl4+3HCH

O+11KOH→2Au(sol)3HCOOK8KCl8HOSolpurification•1,dialysismethod•2,ultrafiltrationdialysismethod•Semipermeable

membranedialysismethod•Electrodialysisultrafiltration•Semipermeablemembraneultrafiltration•ElectroultrafiltrationAssociationcolloidsCMCthecritic

almicelleconcentration(CMC)isdefinedastheconcentrationofsurfactantsabovewhichmicellesformandalladditionalsurfactant

saddedtothesystemgotomicelles.Typeofmicelle•Cylindricalmicelle•Bilayer•Bilayervesicle•Invertedmicelle

•MicrotubuleClassificationandtypicalexamplesofassociationcolloidsExampleTypeCompoundAmphiphileGegeni

onsAnionicSodiumlaurylsulfateCH3(CH2)11OSO3-Na+CationicCetyltrimethyl-ammoniumbromideCH3(CH2)15N+(CH3)3Br-NonionicPolyoxyethylene

lauryetherCH3(CH2)10CH2O(CH2OCH2)23H—AmpholyticDimenthyldodecylammonio-propanesulfonateCH3(CH2)11N+(CH3)2(CH2)3OSO2-—Pro

pertiesofsurface-activeagentsshowingchangesthatoccursharplyattheCMCPredicttheCMCofthemixture•TodeterminetheminimumamountofsurfactantOpticalprope

rtiesofcolloidsscatteringoflightLightscatteringisaformofscatteringinwhichlightistheformofpropagatingenergywhichisscattered.Lightscatteringca

nbethoughtofasthedeflectionofarayfromastraightpath,forexamplebyirregularitiesinthepropagationmedium,particles,o

rintheinterfacebetweentwomedia.TheFaraday-TyndallEffect•Whenastrongbeamoflightispassedthroughacolloidalsol,avisiblecone,resultingfro

mthescatteringoflightbythecolloidalparticles,isformed.ThisistheFaraday-tyndalleffect.Ultramicroscope•Anultramicroscopeisamicroscopewithasy

stemofilluminationthatallowsviewingoftinyparticles.Whenthediameterofaparticleisbelowornearthewavelengthofvisiblelight(a

round500nanometers),theparticlecannotbeseeninalightmicroscopewiththeusualmethodofillumination.Theultramicroscopesystemis

basedonlightscattering,notlightreflection.UltramicroscopeElectronmicroscopeElectronmicroscope,capableofyieldingpicturesoftheactualparticl

es,eventhoseapproachingmoleculardimensions,isnowwidelyusedtoobservethesize,shape,andstructureofcolloidalpartic

les.Kineticpropertiesofcolloids1,Thermallyinduced:Brownianmovement,diffusion,osmosis.2,gravitationallyinduced:s

edimentation3,appliedexternally:viscosityBrownianMotion—therandommovementofcolloidalpartoclesThefirstsatisfactorytheoreticaltreatmentofBrownianm

otionwasmadebyAlbertEinsteinin1905.DiffusionDeducedbyEinsteinandStrokes•WhereNAisAvogadro'snumber,Risthegasconstant,ηisthec

oefficientofviscosityofthesurroundingmedium,ristheradiusofthesphericalparticle,Tistheabsolutetemperature•Diff

usionisanentropyincreasingprocess.D=RT6NAphrDiffusionOsmoticpressureSedimentation•Inagravitationalfield,heavyparticlessettletowardst

hefootofacolumnofsolutionbytheprocesscalledsedimentation.•Whenasolutionisallowedtostand,astateofequilibriumisfinallyreachedwhens

edimentationanddiffusionbalanceeachother,thatis,wheninagivenintervaloftimetheamountofmaterialwhichfallsinthedownwarddirectionthroughaun

itareaisthesameasthatwhichdiffusesupwardbecauseofthegreaterconcentrationatthelowerlevel.sedimentationdif

fusionultracentrifugationM=RTSD(1-vr)Sedimentationisnormallyveryslow,butitcanbeacceleratedbyultracentrifugation,atechniquethatreplacesthegra

vitationalfieldwithacentrifugalfield.WhereRisthegasconstant,Sisthesedimentationcoefficient,theunitSvedbergis1X10-13second,Tistheabsol

utetemperature,Disthediffusionconstant,visthevolumeof1gofparticle,ρisthedensityofmedium.supercentrifugeViscosityViscosityisenexpressionoftheresi

stancetoflowofasystemunderanappliedstress.Themoregreateristheappliedforcerequiredtomakeitflowataparticularrate.ElectricalPro

pertiesofColloidsElectrokineticPhenomena•Electrophoresis•Electroosmosis•Sedimentationpotential•StreamingpotentialElectrophoresisEle

ctroosmosisSedimentationpotentialStreamingpotentialStabilityofColloidSystems•Kineticstabilitystable•ThermodinamicstabilityLyophobiccolloid

sunstableLyophiliccolloidsstableAssociationcolloidsDLVOtheoryEnergy(+)(-)Repulsion,VRComposite,VTPotentialbarrierInterparticledistancePrimaryminimum

(atrraction)Atrractive,VASecondaryminimum(atrraction)SensitizationandProtectiveColloidalAction•Thepresenceandmagnitude

,orabsence,ofachargeonacolloidalparticleisanimportantfactorinthestabilityofcolloidalsystems.•Sensitization:theadditionofasmallamountof

hydrophilicorhydrophobiccolloidtoahydrophobiccolloidofoppositechargetendstosensitizeorevencoagulate.•Protec

tion:theadditionoflargeamountsofhydrophile,however,stabilizesthesystem,thehydrophilebeingadsorbedonthe

hydrophobicparticles.SensitizationprotectionSolubilizationAnimportantpropertyofassociationcolloidsinthesolutionistheabilityofthemicellestoincreasethe

solubilityofmaterialsthatarenormallyinsoluble,oronlyslightlysoluble,inthedispersionmediumused.Thesurface-activeagent,iftakeninternallymustbe:1,nont

oxic2,misciblewiththesolvent3,compatiblewiththematerialtobesolubilized4,freefromdisagreeableoderandtaster5,relative

lynonvolatileAssociationcolloidsDrugSolubilization•Factorsaffectingsolubilization1,thechemistryofthesurfactants2,thelocationofthedrugint

hemicells3,pH(nonionicsurfactants)Peppermintoil010010001000505050ⅡⅢⅣⅠPharmaceuticalapplicationofcolloidsPharmaceuticalapplicationofcolloids•Hydro

gelsHydrogelsHydrogelsHydrogelsPharmaceuticalapplicationofcolloids•Microparticles1,carriersforvaccines

andanticancerdrugs2,reducingtheuptakeofthenanoparticlesbythecellsofthereticuloendothelialsystem3,enhancetheiruptakebythetargetedcells4,themucos

alrouteofadministrationPharmaceuticalapplicationofcolloids•EmulsionsandmicroemulsionsEmulsionsandmicroemulsions

•self-emulsifyingdrugdeliverysystems(SEDDS)PharmaceuticalapplicationofcolloidsLipidsomeLipidsomeTheindustrializa

tionproductionofliposome•1,manufacturingtechnique:filmdespersionmethod;solventinjectionmethod.•2,Particlesizehigh-pressurehomogenizationmachin

e•3,desolventizzazionevacuumdistillation;spraydrying;freezedrying;dialysis.•4,removethefreedrugs•5,sterilityPh

armaceuticalapplicationofcolloidsCommonlyusedpolymericdrugcarriers.

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