Biopharmaceutics

&
Pharmacokinetics
2st presentation
Lecturer: Dr. Muslim Suardi, M.Si,
Apt

Kelompok 2
1. Nova Lestari (1411011043)
2. Rama saputri (1411011046)
3. Anna fadhila (1411011049)
4. Nur Azlin (1411011061)
5. Suci Dita Ramadhani (1401101164)
Dissolution:
is the process by which a solid solute enters in to a
solution.Itistheprocessofdissolvingsolidpart(solute)
inthesolvent(liquid).
Thetimeittakesforthedrugtodissolveinthefluidsat
theabsorptionsitecalleddissolutionrate.
(AnselsPharmaceuticalDosageFormsandDrugDeliverySystems,2011)
Thingsthataffectdissolutionare:

1. Temperature:
Inmostcasesofdissolutionofsolid(solute)inaliquid
involvestheabsorptionofheat.Ifthetemperatureis
increasedthenthedissolutionwillbemore&ifthe
temperatureisdecreasedthanthedissolutionwillbeless.
 Whydowestudydissolution?

Disintegration Dissolution Absorption Drug in

the blood
and the
body

4
Thingsthataffectdissolutionare:

1. Temperature:
Inmostcasesofdissolutionofsolid(solute)inaliquid
involvestheabsorptionofheat.Ifthetemperatureis
increasedthenthedissolutionwillbemore&ifthe
temperatureisdecreasedthanthedissolutionwillbeless.

2. Agitation (concentrationofthesolvent)
Dissolutionalsodependsontheconcentrationofthe
solvent.Ifthesolventismoreconcentrateddissolutionwill
beless.Ifthesolventislessconcentrateddissolutionwillbe
more.
3. Particle Size
Thedissolutionrateofdependsonitsparticlesize.
Smallparticlesize,dissolutionwillbemoreandlarge
particlesize,dissolutionwillbeless.
Thedissolutionrateofdrugsmaybeincreasedby
decreasingthedrugsparticlesize.

4. Solvent selection
Dissolutionalsodependsontheconcentrationofthesolvent.In
waterdissolutionratewillbemorethanoilysolvent.
Whenthedissolutionrateistherate-limitingstep,anything
thataffectsitwillalsoaffectabsorption.
Consequently,dissolutionratecanaffecttheonset,
intensity,anddurationofresponseandcontroltheoverall
bioavailabilityofthedrugfromthedosageform.
(AnselsPharmaceuticalDosageFormsandDrugDeliverySystems,2011)
 Thedissolutionratesofchemicalcompoundsaredetermined
bytwomethods:theconstantsurfacemethodandparticulate
dissolution.

Theconstant-surfacemethod
Thedissolutionrateobtainedbythismethod,theintrinsic
dissolution rate,ischaracteristicofeachsolidcompoundanda
givensolventinthefixedexperimentalconditions.Thevalueis
expressedasmilligramsdissolvedperminutepercentimeters
squared.
=usefulinpredictingprobableabsorptionproblemsdueto
dissolutionrate
Particulatedissolution
Aweighedamountofpowderedsampleisaddedtothe
dissolutionmediuminaconstantagitationsystem.This
methodisfrequentlyusedtostudytheinfluenceofparticle
size,surfacearea,andexcipientsupontheactiveagent.
(AnselsPharmaceuticalDosageFormsandDrugDeliverySystems,2011)
Drugsinsoliddosageformsundergovarious
stagesofreleasefromthedosageformbefore
itisabsorbed.Thesestagesinclude
disintegration,deagregasianddissolution.

Therateofdrugreachingthecirculation
systemintheprocessofdisintegration,
dissolutionandabsorption,isdeterminedby
thesloweststageofthecircuitabovetheso-
calledratelimitingstep(ShargelandYu,
1999).
Sothatthesolidparticlesdissolvedsolute
moleculesmustfirstbesplitofffroma
solidsurface,thenmoveawayfromthe
surfaceintothesolvent.Dependingon
boththeprocessandhowtheprocess
takesplace,thetransportdissolution
behaviorcanbedescribedbyphysics.In
termsofspeedofdissolutionareinvolved
inpuresubstances,therearethreebasic
modelsofgeneralphysics(Abdou,1989).
Indiscussiontounderstandthe
mechanismofdissolution,issometimes
usedoneofthemodelsoracombination
ofthesemodels.......
 a. Model diffusion layer (diffusion layer model)

ThismodelwasfirstproposedbyNerstand
Brunner.Onsolidsurfacesthereisathinlayerof
liquidwithathickness,anegativevelocity
componentintheoppositedirectionwithasolid
surface(Banakar,1992)