552 MIDTERM QUESTIONS AND ANSWERS

552 MIDTERM QUESTIONS AND
ANSWERS

WhatsissModifiedsRelease?s-sans✔✔Thestermsmodified-
releasesissusedstosdescribesdosagesformssthatsaltersthestimingsand/
orsthesratesofsreleasesofsasconventionalsdrugsproduct/dosagesform
-sFDAsdoessdefinesthis

SomesModifiedsReleasesSystemss-sans✔✔-ssomesofstheseshavesoverlaps
1.sDelayedsrelease
2.sRepeatedsReleasesorsRepeatsAction
4.sExtended,sSustained,sLong-Acting,sProlonged,sControlledsReleases
5.sTargetedsRelease

Delayed-releases-sans✔✔-
sdosagesformssreleasesthesdrugsatsaslaterstimesthansansimmediatesdosessystem

-sDelayed-releasescansincludesenteric-
coatedstablets,swherestimedsreleasesissachievedsbysasbarrierscoating
-stakessmorestimestosreleasesdrug;sdoesn'tsstartsdissolvingsuntilsascertainspointsofstime

Repeat-releases-sans✔✔-
smultiplesdosessofsimmediatesreleasesdrugsunitsswithsintermittentsdosing

-sSuchsassrepeat-actionstabletssandscapsules

Extended,sSustained,sLong-Acting,sProlonged,sControlledsReleases-sans✔✔-
sExtended,sSustained-

releasessystemssslowlysreleasesthesdrugsoversansextendedsperiodsofstime
-sRatesandsdurationsaresnotsalwayssdesignedstosasparticularsprofile
-
sIfsthessystemscansmaintainspredictableslevelssofsdrugsinsthestargetstissuesorscells,sitsisscon

sideredscontrolled-srelease.s(Examples:sXL,SR,CR)s
-sControlledsreleasessystemssaresalsoscalledsextendedsorssustaineds(prolonged)srelease
-sdissolvessandscontinuessdissolvingsforsaslongerstime

TargetedsReleases-sans✔✔-sSite-
specificsorstargetingsrefersstosconcentratedsdrugsreleasesatsascertainssitessuchsassastissue,
sorgan,sreceptor,sorscells

-sAsformsofscontrolledsrelease

,-sverysdifficultstosachieves
-stryingstoscontrolsdistributionsofsdrugstostargetsarea

WhatsissControlledsRelease?s-sans✔✔-
sControlledsDrugsDeliverysattemptsstosdeliversthesprecisesamountsofsastherapeuticsagents(

drug),stosasspecificssites(sitesofsaction),sforsasspecificstimes(duraterm-5tionsofstreatment)s
-sORsAchievesbothsspatials(targeted)sand/orstemporals"control"sofsthesdrug
-saslotsofspredictionsinvolved,sverysprecise,sandstargeteds
-
sThesDrugsDeliverysSystemsattemptsstoscontrolsthesdrugsconcentrationsatsthestargetstissue



DisadvantagessofsConventionalsDeliverys-sans✔✔-
sInconvenientsbecausesptscansforgetstostakesdose

-sDifficultstosmonitors
-sOverdosingspossible
-
sLargesamountssofsdrugscansbes"lost"swhensitsdoessnotsgetstosthestargetsorgansbecausesha

sstosdistributestostheswholesbody
-sDrugsgoesstosnon-targetscellssandscanscausesdamage
-sExpensives(usingsmoresdrugsthansnecessary)

ThesGoalsofsModifiedsDrugsDeliverys-sans✔✔TosAltersandsControl
-sAbsorptions
-sDistributions-sincludessCellularsUptakes
-sMetabolisms(reducesitssosmoresdrugsavailable)s
-sEliminations(reduceshowsfastseliminatedstosprolongseffectsofsdrug)s
-sToxicitys(reducesit)

WhatsissSustainedsDrugsAction?s-sans✔✔-sidealsdosagesform
-sptsonlyshasstostakesonestimesrathersthansmultiplestimes
-
sminimizessideseffectssbysdeliveringsAPIstossitesofsactions(targetsreceptors,scells,stissues,so

rsareasinsthesbody)s
-sre-patentingswithoutsnewsdrugsdevelopment.

ImprovingsPatientsCompliances-sans✔✔MinimizesPlasmasfluctuation
-sPlasmasConcentrationsvssTime
-
sSustainedsRelease:stakesslongerstosbesabsorbedsandsinstherapeuticsrangesforslongersbuts

eventuallyseliminated
-sControlled:sabsorbedsquicklysandsinstherapeuticsrangesforsasslongsassnecessarys

-sthesmorestimessyoushavestakesasmedicationsday,stheslowersptscompliance

TriesstosAchieve:sSitesSpecificsDrugsDeliverys-sans✔✔Reductionsofssideseffects
-sAnticancersdrugs

,-->sCytosinesarabinoside-sDpocyt®
-sAnti-fertilitysAgentss
-sAnti-inflammatorysdrugs

SitesSpecificsDrugsActionsorsDrugsTargetings-sans✔✔-sTargetingsorsSpatialsDelivery
-sexclusivesdrugsdeliverystosspecificsorgan,stissues,sorscellstypes
-sStillsinsdevelopmentsandsdifficult
-sDesignedstosbesdirectedstosasspecificsorgan,stissues,scellsorscellscompartment
-sTargetssincludessurfacesorscompartmentscellsmarkers,sproteinssorsevensnucleicsacids
-scanslocallysputsthesdrugsthroughspatches

RoutessofsAdministrations-sans✔✔a.sParenterals
-sRefersstosinjectionssandsIVs
-sFastsAbsorption
-sNosFirstspass
-sPainful
-sInconvenient

b.sTransdermals
-sEasysaccess
-sLargessurfacesarea
-sAvoidsfirstspasssmetabolism
-sAvoidsGIsincompatibilitysofsdrugs
-sGoodspatientscompliance
-sSlowsabsorption
-sTransportsacrosssskinscansbesaschallenge
-sNeedslipophilic
-sLowsMWsdrugs

c.sOculars
-sLocalizedsdeliverysforseyesdisorders
-sGoodsabsorptionsforsmanysdrugs
-sBypassesscertainsclearancesroutes
-sProblemsswithslosssofsdrugsinstears

d.sNasals
-sEasysadministration
-sLocalsdeliverysofsdrugs
-sRapidsabsorption
-sCansbypassesscertainsclearancesroutes

e.sPulmonarys
-sRapidsabsorption
-sLargessurfacesareasforsabsorption
-sLocalsdeliverysofsdrugs
-sCansbypassesscertainsclearancesroutesswhensdeliveredssystemically

, -sParticlessizesdeterminessanatomicsplacementsinsrespiratorystract
-sSomesdrugsmaysbesswallowed

f.sBuccalsorsSublinguals-
sNosfirstspass,sThinsmucoussmembraneswithsasrichsbloodssupply,sGoodsabsorption,sMildsp

Hs~6.0,sDrugsmustsbespotent,sCansbesswallowed.

g.sRectals-
sLesssworriessaboutspHschangessorsenzymaticsdegradationsassinsoral,sGoodsforspatientssw

hoscannotsswallow,sGoodsforsLocalsdeliverysofsdrug,sLimitedssystemicsabsorption,sDiscom
fort.

h.sOrals-
Mostscommonsroute,sEasystosformulatesandsmanufacture,sPatientscompliancesissgenerall
ysgood,sInexpensivesdosagesform,sTrickysduestosenvironmentsofsGIstractsbecausesof:sFirst
spass,spHsdegradation,sEnzymaticsdegradation,sIntestinalsmotilitys-

saffectssresidencestime,sSinglespatientsandspatient-to-

patientsvariations,sAbsorptionslimitationssinsstomach.

Stents,sImplants,sInsertss-sans✔✔a.sStents
-sXIENCEsPRIMETMscoronarysarterysdisease

b.sImplants
-sdentals

c.sInserts
-sNuvaRings®sIUDsContraceptive

VariablesstosConsiders-sans✔✔includessexamplessofscontrolled/
sustainedsoralsdrugsdeliveryssystemssbecauseshistorically,sthesoralsroutesofsadministration
shassbeensusedsthesmostsforsbothsconventionalsandsnovelsdrugsdeliveryssystems

-
sThestypessofsreleasessystemssemployedsforsoralsadministrationsincludesvirtuallyseveryscur

rentlysknownstheoreticalsmechanism

VariablesstosConsiderswhensdesigningsansOralsModified/
SustainedsDrugsDeliverysSystems-sans✔✔a.sPhysiochemicals&sDrugsProperties
pKa,sSolubility,sLogsP,sPermeability,sStability,sDosessize

b.sBiological
-sHalf-Lifes(timesfors50%sofsdrugstosbeseliminated)s
-sGIsEnvironment:sAbsorption,sMetabolism,sTargetssite

c.sOthers
-sRoutesofsdelivery
-sDiseasesstate-acutesvs.schronic