药剂学英文重点

绪论

LWhatispha门naceutics?Howmanybranchesofpha门naccutics?

2.Whatisadrug?Givesemeexamples

Adrugisdefinedasanagentintendedforuseinthediagnosis,mitigation,treatment,cure,orpreventionof

diseaseinhumansorinotheranimals.

药物是有目的地用于诊断、缓解、治疗、治愈或预防人类或动物疾病的物质。

•Emetic(inducevomiting催吐齐(j)andantiemetic(preventvomiting止吐齐！J)drugs

•Diureticdrugs(increasetheflowofurine利尿剂)

・Expectorantdrugs(increaserespiratorytractfluid除痰剂)

•Catharticsorlaxatives(evacuatethebowel泻药)

•Otherdrugsdecreasetheflowofurine,diminishbodysecretions,orinduceconstipation(便秘)

3.Wheredonewdrugscomefrom?Giveexamples.

Newdrugsmaybederivedfrom

•Plant

•Animalsources

•Asbyproductsofmicrobialgrowth

•Throughchemicalsynthesis

•Molecularmodification

•Biotechnology

4.Explain:drugstandards,uhannacoDeia,ISO

Drugstandards

•Theunitedstatespharmacopeia(药典)andthenationalformulary(国家药品标准)

•Pharmakon,meaning“drug”;poiein,meaning"make”;

•Thecombinationindicatesanyrecipeorformulaorotherstandardsrequiredtomakeorprepareadrug.

•Organizedsetsofmonographsorbooksofthesestandardsarecalledpharmacopeiasorformularies.

InternationalOrganizationforstandardization(ISO)

isaninternationalconsortiumofrepresentativebodiesconstitutedtodevelopandpromoteuniformor

harmonizedinternationalstandards.

国际标准化组织是一个代表性的国际联合会，其设立是为了发展和增进国际标准的均一性和协调性。

ISO9000-IS09004usedinthepharmaceuticalindustry

•ISOincludedstandardspertainingtodevelopment,production,qualityassurance,qualitycontrol,detection

ofdefectiveproducts,qualitymanagement,andotherissuesasproductsafetyandliability.

•ISO包括标准适合开发、生产、质量保证、质量控制、缺陷产品的检测、质量管理和其他如产品安

全性和责任的问题。

•Internationallyrecognizedquality-managementsystem.

5.Howdoyouunderstandyourroleasaclinicalpharmacist?

•Communitypharmacies

Pharmacistplaysanactiveroleinthepatient,suseofprescriptionandnonprescriptionmedication,

diagnosticagents,

durablemedicalequipmentanddevices,

otherhealth-relatedproducts.

•Patient-careinstitutions

1）Managedrugdistributionandcontrolsystems

2）Provideavarietyofclinicalservicesas

drugutilizationreviews,

druguseevaluations,

therapeuticdrugmonitoring,（治疗药物的监测）

intravenousadmixtureprograms（静脉药物再己置方案）

pharmacokineticconsultservice,

investigationaldrugsupplies,

poisoncontrol,

druginformation.

•Managedcare

•Homehealthcare

•Militaryandgovernmentservice

•Academicsettings

•Professionalassociations

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Pharmaceuticalresearchandmanufacturingindustry

Themissionofthepharmacististoprovidepharmaceuticalcare.Pharmaceuticalcareisthedirect,responsible

provisionofmedication-relatedcareforthepurposeofachievingdefiniteoutcomesthatimproveapatient's

qualityoflife.

药师的使命是提供药学服务。药学服务是药物治疗有关服务的直接的、责任性的提供，目的是达到增进

患者生活质量的明确的结果。

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4

新药发展和审批进程

1（思知）Describethemethodsofdrugdiscovery

•Mostdrugsaretheresultofcarefullydesignedresearchprogramsofscreening,molecularmodification,and

mechanism-baseddrugdesign.（大多数药物是精心设计的研究过程的结果，包括：筛选、分子修饰和

基于机制的药物设计。）

•Todetectandevaluatebiologicalactivity,bioassaysareusedtodifferentiatetheeffectandpotencyofthe

testagentcomparedwithcontrolsofknownactionandeffect.（Invitro—cellculture/Invivo

Disease-specificanimalmodels）

•Newmethods,ashighthroughputscreening,arecapableofexamining15000chemicalcompoundsaweek

using10-20biologicalassays.

■High-throughputscreening（HTS）isamethodforscientificexperimentationespeciallyusedindrug

discoveryandrelevanttothefieldsofbiologyandchemistry.

•Tobeeffective,thisrequiresasizeableandchemicallydiversecollectionofcompoundstoexamine,which

manypharmaceuticalandchemicalcompanieshaveinuchemicallibraries.,,（为了有效地利用它，这需

要有相当大量的不同化学物质来测试，通常许多制药公司或化学品公司有“化合物库”）

•Molecularmodificationinvolvesthechemicalalterationofaknownandpreviouslycharacterizedorganic

compoundforthepurposeofenhancingitsusefulnessasadrug.（分子修饰涉及化学改变已知和特性明

了的有机化合物以改善其作为药物的有效性。）

2（思）Definethefollowingphrases:

（1）Prodm&s

isatermusedtodescribeacompoundthatrequiresmetabolicbiotransformationafteradministrationtoproduce

thedesiredpharmacologicallyactivecompound.

（前体药物使之能够在给药后经体内代谢性生物转化成具有期望的药理活性化合物的化合物。）

（2）aleadcompound

isaprototype（原形化学物质）chemicalcompoundthathasafundamentaldesiredbiologicorpharmacologic

activity.

（先导化合物是一种具有生物学和药理学活性基本要求的原型化学物质。）

（3）agoaldrug

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Intheory,a“goaldrug”

•wouldproducethespecificallydesiredeffect,

•beadministeredbythemostdesiredroute（generallyorally）atminimaldosageanddosingfrequency,

•haveoptimalonsetanddurationofactivity,

理论匕目标药物应能通过最理想的途径（通常为口服）以最小的剂量和给药频率给药，能产生特

异的期望疗效，具有最理想的起效和持续时间，

・exhibitnosideeffects,

•followingitsdesiredeffectwouldbeeliminatedfromthebodyefficiently,completely,andwithoutresidual

effect.

•itwouldbeeasilyproducedatlowcost,

•bepharmaceuticallyelegant,

•physicallyandchemicallystableundervariousconditionsofuseandstorage.

•（无副作用，并在发挥疗效后能完全有效地从体内消除，且无残留效应。它应该易于生产，费用低,

制剂产品美观，在不同的使用和贮藏条件下物理和化学上稳定。）

3（思）Whatphysicalandchemicalpropertiesofdrugsubstancesmustbecharacterizedduring

prefonmilationstudies?Explain.

Eachdrugsubstancehasintrinsicchemicalandphysicalcharacteristicsthatmustbeconsideredbeforethe

developmentofapharmaceuticalformulation.

①Drugsolubility

•Adrugsubstanceadministeredbyanyroutemustpossesssomeaqueoussolubilityforsystemicabsorption

andtherapeuticresponse.

•Poorlysolublecompounds（lessthanlOmg/ml）mayexhibiteitherincompleteorerratic（不稳定）

absorptionandthusproduceaminimalresponseatdesireddosage.

②Partitioncoefficient

Toproduceapharmacologicresponse,adrugmoleculemustfirstcrossabiologicmembraneofproteinandlipid,

whichactsasalipophilicbarriertomanydrugs.

③Dissolutionrate

•Therateatwhichadrugsubstancedissolvesinamediumiscalleditsdissolutionrate.

•Dissolutionratedata,whenconsideredalongwithdataonadrug'ssolubility,dissolutionconstant,and

partitioncoefficient,canprovideanindicationofthedrug*sabsorptionpotentialfollowingadministration.

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④Physicalform

Thecrystaloramorphousformsandparticlesizeofapowdereddrugcanaffectthedissolutionrate,andthusthe

rateandextentofabsorption,foranumberofdrugs.

⑤Stability

Thechemicalandphysicalstabilityofadrugsubstancealone,andwhencombinedwithformulationcomponents,

iscriticalinpreparingasuccessfulpharmaceuticalproduct.

4（思）Whatbiologicaldiaracterizationshouldbestudiedindmgdevelopmentprocess?

•Pharmacology

•Drugmetabolism

•Toxicology

5（知）

•Pharmacodynamicsisthestudyofthebiochemicalandphysiologicaleffectsofdrugsandtheirmechanisms

ofaction.

•Pharmacokineticsdealswiththeabsorption,distribution,metabolismorbiotransformation,andexcretionof

drugs.

•Clinicalpharmacologyappliespharmacologicprinciplestothestudyoftheeffectsandactionsofdrugsin

humans.

6（知）Thescheduleofdosa*orthedosageregimen,

isdeterminedduringtheclinicalinvestigationandisbasedlargelyonadrug'sinherentdurationofaction,its

pharmacokinetics,andthecharacteristicsofthedosageform.

AtreatmentIND

oratreatmentprotocolpermitstheuseofaninvestigationaldruginthetrentmentofpatientsnotenrolledinthe

clinicalstudybutwhohaveaseriousorimmediatelylife-threateningdiseaseforwhichthereisnonsatisfactory

alternativetherapy.

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3.DosageFormDesign:PharmaceuticandFormulationConsiderations

1药剂学定义

Thegeneralareaofstudyconcernedwiththe

formulation

manufacture

stability

effectiveness

ofpharmaceuticaldosageformsistermedpharmaceutics.

2Theneedfordosageforms

Besidesprovidingthemechanismforthesafeandconvenientdeliveryofaccuratedosage,dosageformsare

neededforadditionalreasons:

1)Toprotectthedrugsubstancefromthedestructiveinfluencesofatmosphericoxygenorhumidity(coated

tablets,sealedampuls)

2)Toprotectthedrugsubstancefromthedestructiveinfluenceofgastricacidafteroraladministration

(enteric-coatedtablets)

3)Toconcealthebitter,salty,oroffensivetasteorodorofadrugsubstance(capsules,coatedtablets,flavored

syrups)

4)ToprovideLiquidpreparationofsubstancesthatare

insoluble

orunstable

inthedesiredvehiclefSuspensions

5)Toprovideclearliquiddosageformsofsubstances,suchas-SyrupsSolutions

6)Toproviderate-controlleddrugaction(variouscontrolled-releasetablets,capsulesandsuspensions)

7)Toprovidetopicaldrugactionfromtopicaladministrationsites(ointments,creams,transdermalpatches,

ophthalmic,ear,andnasalpreparations)

8)Toprovidefortheinsertionofadrugintooneofthebody*sorifices(e.g.,rectalorvaginalsuppositories)

9)Toprovidefortheplacementofdrugsdirectlyintothebloodstreamorintobody*stissues(e.g.,injections)

10)Toprovidefortopicaldrugactionthroughinhalationtherapy(e.g.,inhalantsandinhalationaerosols)

3（知公式）

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Inthedissolutionofparticlesofdrug,thedissolvedmoleculesdiffuseawayfromtheindividualparticlebody.An

expressiontodescribethiswasderivedfromFick'sequationsandisknownastheNoyesandWhitney

expression.Itcanbewrittenasfollows:

dC/dt=(DS/h)(Cs・C)

whereCistheconcentrationofdrugdissolvedattimet,

Disthediffusioncoefficientofthesoluteinsolution,

Sisthesurfaceareaoftheexposedsolid

histhethicknessofthediffusionlayer

Csisthesaturationsolubilityofthedrug

k=DS/h

dc/dt=k(Cs-C)

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药物剂型设计——生物药剂学和药物动力学

1（掌）一些名词

Biopharmaceutics

istheareaofstudyembracingtherelationshipbetweenthephysical,chemical,andbiologicalsciencesasthey

applytodrugs,dosageforms,andtodrugaction.

（生物药剂学是围绕物理学、化学和生物科学及它们关于药物、剂型和药物作用相互关系的研究领域。）

药物动力学

Theareaofstudywhichelucidatesthetimecourseofdrugconcentrationinthebloodandtissuesistermed

pharmacokinetics.

Itisthestudyofthekineticsofabsorption,distribution,metabolismandexcretion（ADME）ofdrugsandtheir

correspondingpharmacologic,therapeutic,ortoxicresponseinanimalsandman.

Pharmacokineticsalsomaybeappliedinthestudyofinteractionsbetweendrugs.

Activetransport

denotesaprocessofthesoluteordrugbeingmovedacrossthemembraneagainstaconcentrationgradient,thatis,

fromasolutionoflowerconcentrationtooneofahigherconcentrationor,ifthesoluteisanion,againstan

electrochemicalpotentialgradient

（主动转运是指溶质或药物穿过生物膜的转运的过程是逆浓度梯度进行，即从低浓度向高浓度转运或当

溶质是离子时逆电化学电势梯度转运。）

endocytosis（内吞）

Manylargemoleculesandparticlescannotentercellsviapassiveoractivemechanisms.However,somemay

enter,asyet,byaprocessknownasendocytosis（内吞）

Inphagocytosis（吞噬）（celleating）

largeparticlessuspendedintheextracellularfluidareengulfedandeithertransportedintocellsoraredestroyed

withinthecell.Thisisaveryimportantprocessforlungphagocytesandcertainliverandspleencells.

Pinocytosis（胞饮）（celldrinking）

isasimilarprocessbutinvolvestheengulfingofliquidsorverysmallparticlesthatareinsuspensionwithinthe

extracellularfluid.

Thebioavailability

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describestherateandextenttowhichanactivedrugingredientortherapeuticmoietyisabsorbedfromadrug

productandbecomesavailableatthesiteofdrugaction.

Thebioequivalence

referstothecomparisonofbioavailabilitiesofdifferentformulations,drugproducts,orbatchesofthesamedrug

product.

Peakheight(Cmax)

concentrationisthemaximumdrugconcentrationobservedinthebloodplasmaorserumfollowingadoseof

thedrug.

Forconventionaldosageforms,astabletsandcapsules,theCmaxwillusuallyoccuratonlyasingletimepoint,

referredtoasTmax.

Timeofpeak(Tmax)

maximumlevelofdrugintheblood

Thisparameterreflectstherateofdrugabsorptionfromaformulation.Itistherateofdrugabsorptionthat

determinesthetimeneededfortheminimumeffectiveconcentrationtobereachedandthusfortheinitiationof

thedesiredpharmacologiceffect.

Areaundertheserumconcentrationtimecurve(AUC)

TheAUCofaconcentration-timeplotisconsideredrepresentativeofthetotalamountofdrugabsorbedintothe

circulationfollowingtheadministrationofasingledoseofthatdrug.

ThesmallertheAUC,thelessdrugabsorbed.

Pharmaceuticalequivalents

aredrugproductsthatcontainidenticalamountsoftheidenticalactivedrugingredient,i.e.,thesamesaltorester

ofthesametherapeuticmoiety,inidenticaldosageforms,butnotnecessarilycontainingthesameinactive

ingredients,andthatmeettheidenticalcompendialorotherapplicablestandardofidentity,strength,quality,and

purity,includingpotencyand,whereapplicable,contentuniformity,disintegrationtimes,and/ordissolutionrates.

(制剂等效指包含等量同种活性药物成分的药品，即：有相同治疗效应的相同盐或酯的形式，相同剂型。

但并不一定包含相同的非活性成分，具有相同的外观或其他相应的性质如规格、质量、纯度，包括效价、

含量均匀性、崩解时间和溶出速率。)

Pharmaceuticalalternatives

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aredrugproductsthatcontaintheidenticaltherapeuticmoiety,oritsprecursor,butnotnecessarilyinthesame

amountordosageformorasthesamesaltorester.Eachsuchproductindividuallymeetseithertheidenticalor

itsownrespectivecompendialorotherapplicablestandardofidentity,strength,quality,andpurity,including

potencyand,whereapplicable,contentuniformity,disintegrationtimes,and/ordissolutionrates.

(制剂替代品指含有相同治疗效果的组成部分或它的前体药物，不需要相同剂量、相同剂型、相同的盐

或酯的形式。每种药品符合同样的或各自的外观和其他相应的性质如规格、质量、纯度，包括效价，含

量均匀性、崩解时间和溶出速率。)

Bioequivalentdrug

productsarepharmaceuticalequivalentsorpharmaceuticalalternativeswhoserateandextentofabsorptiondo

notshowasignificantdifferencewhenadministeredatthesamemolardoseofthetherapeuticmoietyunder

similarexperimentalconditions,eithersingledoseormultipledose.

(生物等效性药品指在相同的试验条件下，单次或多次给予相同治疗剂量的药物，其吸收的速率和程度没

有显示显著性差异的制剂等效品或制剂替代品。)

Therapeuticequivalents

hasbeenusedtoindicatepharmaceuticalequivalentswhich,whenadministeredtothesameindividualsinthe

samedosageregimens,willprovideessentiallythesametherapeuticeffect.

Thehalf-life(Tl/2)

ofadrugdescribesthetimerequiredforadrug'sbloodorplasmaconcentrationtodecreasebyonehalf.

2(复)Whataregeneralprinciplesofdrugabsootion?

Bodymembranesaregenerallyclassifiedasthreemaintypes:

•thosecomposedofseverallayersofcells,astheskin,

•thosecomposedofasinglelayerofcells,astheintestinalepithelium,

•thoseoflessthanonecellinthickness,asthemembraneofasinglecell.

Drugsarethoughttopenetratethesebiologicmembranesintwogeneralways:

1)bypassivediffusion

Passivediffusionisusedtodescribethepassageof(drug)moleculesthroughamembranewhichbehavesinertly

inthatitdoesnotactivelyparticipateintheprocess.

Drugsabsorbedaccordingtothismethodaresaidtobepassivelyabsorbed.

2)throughspecializedtransportmechanisms

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Thistypeoftransportisthoughttoinvolvemembranecomponentsthatmaybeenzymesorsomeothertypeof

agentcapableofformingacomplexwiththedrugatthesurfacemembrane,afterwhichthecomplexmoves

acrossthemembranewherethedrugisreleased,withthecarrierreturningtotheoriginalsurface.

(这种类型的转运认为需要涉及一些生物膜的成分，可能是酶或其他能与药物在膜表面结合成复合物的

物质。复合物能移动到膜的另一侧并释放出药物，载体则重新回到膜的表面。)

3(复)WriteHendersoii・Hasselbalchequationandexplainit.

Thedegreeofadrug'sionizationdependsbothonthepHofthesolutioninwhichitispresentedtothebiologic

membraneandonthepKa.

Henderson-Hasselbalchequation

Foranacid：pH=pKa+logionizedconc.(salt)/unionizedconc.(acid)

Forabase:pH=pKa+logunionizedcone.(base)/ionizedconc.(salt)

4(复)WhatisNoyes八Vhitne、equation?

ThedissolutionofasubstancemaybedescribedbythemodifiedNoyes-Whitneyequation:

dc/dt=kS(cs-ct)

inwhichdc/dtistherateofdissolution

kisthedissolutionrateconstant

Sisthesurfaceareaofthedissolvingsolid,

Csisthesaturationconcentrationofdruginthediffusionlayer

Ctistheconcentrationofthedruginthedissolutionmediumattimet

5(复)Whatfactorscouldaffectdrugabsorption?

•increasingthesurfaceareaofthedrug,

•increasingthesolubilityofthedruginthediffusionlayer,

•factorsembodiedinthedissolutionrateconstant,k,includingtheintensityofagitationofthesolvent,

•thediffusioncoefficientofthedissolvingdrug.

1)Surfacearea

2)Crystaloramorphousdrugform

3)Saltforms

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4)Otherfactors

6(复)Describetheroutesofdrugadministrationandtheircharacteristics?

1)Oralroute

Theoralrouteisconsideredthemostnatural,uncomplicated,convenient,andsafemeansofadministeringdrugs.

Disadvantages

Slowdrugresponse

Chanceofirregularabsorptionofdrugs

Theamountortypeoffoodpresentwithinthegastrointestinaltract

Thedestructionofcertaindrugsbytheacidreactionofthestomachorbygastrointestinalenzymes.

Dosageformsapplicable

Drugsareadministeredbytheoralrouteinavarietyofpharmaceuticalforms.

Themostpopulararetablets,capsules,suspensionsandvariouspharmaceuticalsolutions.

2)Rectalroute

Somedrugsareadministeredrectallyfortheirlocaleffectsandothersfortheirsystemiceffects.

Drugsgivenrectallymaybeadministeredassolutions,suppositories,orointments.

应用范围：

Rectaladministrationforsystemicactionmaybepreferredforthosedrugsdestroyedorinactivatedbythe

environmentsofthestomachandintestines.

Theadministrationofdrugsbytherectalroutemayalsobeindicatedwhentheoralrouteisprecludedbecause

ofvomitingorwhenthepatientisunconsciousorincapableofswallowingdrugssafetywithoutchoking.

3)Parenteralroute

Thethreeprimaryroutesofparenteraladministrationaresubcutaneous,intramuscular,andintravenousalthough

thereareotherssuchasintracardiacandintraspinal.

使用范围：

Drugsdestroyedorinactivatedinthegastrointestinaltractortoopoorlyabsorbedtoprovidesatisfactoryresponse

maybeparenterallyadministered.

Theparenteralrouteisalsopreferredwhenrapidabsorptionisessential,asinemergencysituations.

Theparenteralrouteofadministrationisespeciallyusefulintreatingpatientswhoareuncooperative,

unconscious,orotherwiseunabletoacceptoralmedication.

Dosageformsapplicable

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Pharmaceutically,injectablepreparationsareusuallyeithersterilesuspensionorsolutionsofadrugsubstance

inwaterorinasuitablevegetableoil.

Drugsinsolutionactmorerapidlythandrugsinsuspension,withanaqueousvehicleprovidingfasteractionin

eachinstancethananoleaginousvehicle.

4）Epicutaneousroute

Drugsareadministeredtopically,orappliedtotheskin,fortheiractionatthesiteofapplicationorforsystemic

drugeffects.

Drugabsorptionviatheskinisenhanced

ifthedrugsubstanceisinsolution,

ifithasafavorablelipid/waterpartitioncoefficient,

ifitisanon-electrolyte.

5）Ocular,oral,andnasalroutes

Ophthalmicsolutionsandsuspensionsaresterileaqueouspreparationswithotherquantitiesessentialtothe

safetyandcomfortofthepatient.

Ophthalmicointmentsmustbesterile,andalsofreeofgrittiness.

7（复）Whatisbiotransformation?Whatarethebiochemicalmechanismsofbiotransformation?

Biotransformationisatermusedtoindicatethechemicalchangesthatoccurwithdrugswithinthebodyasthey

aremetabolizedandalteredbyvariousbiochemicalmechanisms.

Theprocessofbiotransformationiscommonlyreferredtoasthe“detoxification“oruinactivation“process.

Therearefourprincipalchemicalreactionsinvolvedinthemetabolismofdrugs:

oxidation

reduction

hydrolysis

conjugation

Othermetabolicprocesses,includingmethylation,andacylationconjugationreactions,occurwithcertain

drugstofosterelimination.

8（复）Explainshortlyaboutonecompartmentmodelandtwocompartmentmodel?

•Thesimplestpharmacokineticmodelisthesinglecompartmentopen-modelsystem.

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Thismodeldepictsthebodyasonecompartmentcharacterizedbyacertainvolumeofdistribution(Vd)that

remainsconstant.

•Inthetwo-compartmentsystem,adrugentersintoandisinstantaneouslydistributedthroughoutthecentral

compartment.

Itssubsequentdistributionintothesecondorperipheralcompartmentisslower.

9(复)Howtodevelopdosageregimens?

Therearetwoapproachestothedevelopmentofdosageregimens:

1)Theempiricalapproach,whichinvolvestheadministrationofadruginacertainquantity,notingthe

therapeuticresponseandthenmodifyingthedosageofdrugandthedosingintervalaccordingly.

2)Thekineticapproachisbasedontheassumptionthatthetherapeuticandtoxiceffectsofadrugarerelatedto

theamountofdruginthebodyortotheplasmaconcentrationofdrugatthereceptorsite.

Throughcarefulpharmacokineticevaluationofadrug*sabsorption,distribution,metabolismandexcretionin

thebodyfromasingledose,thelevelsofdrugattainedfrommultipledosingcanbeestimated.

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5PowdersandGranules

1(复)Whyisparticlesizeanalysisimportantinpharmaceuticalformulation?

Granulestypicallyfallwithintherangeof4(4.75mm)to12-sievesize,althoughgranulationsofpowders

preparedinthe12-to20-sieve(850m)rangearesometimesusedintabletmaking.

Thepurposeofparticlesizeanalysisinpharmacyistoobtainquantitativedataonthesize,distribution,and

shapesofdrugandothercomponentstobeusedinpharmaceuticalformulations.

Particlesizecaninfluenceavarietyofimportantfactors,includingthefollowing:

1)Dissolutionrateofparticlesintendedtodissolve;drugmicronizationcanincreasetherateofdrugdissolution

anditsbioavailability.

2)Suspendabilityofparticlesintendedtoremainundissolvedbutuniformlydispersedinaliquidvehicle(e.g.,

finedispersionshaveparticlesapproximately0.5-10Hm).

3)Uniformdistributionofadrugsubstanceinapowdermixtureorsoliddosageformtoensuredose-to-dose

contentuniformity.

4)Penetrabilityofparticlesintendedtobeinhaledfordepositiondeepintherespiratorytract(e.g.,1-5m).

5)Lackofgrittinessofsolidparticlesindermalointments,creams,andophthalmicpreparations(e.g.,fine

powdersmaybe50-100minsize).

2(复)Howarepowdersofchemicaldniqsofficiallydefined?

Powdersofvegetableandanimaldrugsareofficiallydefinedasfollows:

•Verycoarse(No.8):AllparticlespassthroughaNo.8sieve(2.36mm)andnotmorethan20%througha

No.60sieve(250m).

•Coarse(No.20):AllparticlespassthroughaNo.20sieve(850m)andnotmorethan40%throughaNo.

60sieve.

•Moderatelycoarse(No.40):

AllparticlespassthroughaNo.40sieve(425m)andnotmorethan40%throughaNo.80sieve(180m).

•Fine(No.60):

AllparticlespassthroughaNo.60sieve(250m)andnotmorethan40%throughaNo.100sieve(150

m).

•Veryfine(oraNo.80):

AllparticlespassthroughaNo.80sieve.Thereisnolimittogreaterfineness.

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Thepowderfinenessforchemicalsisdefinedasfollows

•Course(oraNo.20)powder-AllparticlespassthroughaNo.20sieveandnotmorethan60%throughaNo.

40sieve.

•ModeratelyCourse(oraNo.40)powder-AllparticlespassthroughaNo.40sieveandnotmorethan60%

throughaNo.60sieve.

•Fine(oraNo80)powder-AllparticlespassthroughaNo.80sieve.Thereisnolimitastogreaterfineness.

•Veryfine(oraNo.120)powder-AllparticlespassthroughaNo.120sieve.Thereisnolimitastogreater

fineness.

3(复)Whatarethemethodsfordete门ninationofparticlesize?

Anumberofmethodsexistforthedeterminationofparticlesize

1)Sieving

Particlesarepassedbymechanicalshakingthroughaseriesofsievesofknownandsuccessivelysmallersizeand

thedeterminationoftheproportionofpowderpassingthroughorbeingwithheldoneachsieve(rangeabout

40-9500m,dependinguponsievesizes).

2)Microscopy

inwhichtheparticlesaresizedthroughtheuseofacalibratedgridbackgroundorothermeasuringdevice,(range

0.2100m)

3)Sedimentationrate

inwhichparticlesizeisdeterminedbymeasuringtheterminalsettlingvelocityofparticlesthroughaliquid

mediuminagravitationalorcentrifugalenvironment.(range:0.8-300microns)

4)Lightenergydiffractionorlightscattering

Inwhichparticlesizeisdeterminedbythereductioninlightreachingthesensorastheparticle,dispersedina

liquidorgas,passesthroughthesensingzone(range0.2500microns).

5)Laserholography(激光全息照相术)

Inwhichapulsedlaserisfiredthroughanaerosolizedparticlesprayandphotographedinthreedimensions

withaholographiccamera,allowingtheparticlestobeindividuallyimagedandsized(range:1.4

lOOmicros)用一•束激光通过雾化粒子流，用全息照相术拍三维照片，观察到粒子的形态和大小。

6)Cascadeimpaction(阶式碰撞)

isbasedontheprinciplethataparticle,drivenbyanairstream,willimpactonasurfaceinitspath,providedthat

itsinertia(惯性)issufficienttoovercomethedragforcethattendstokeepitintheairstream.