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MICROENCAPSULACINMICROENCAPSULACIN2013_2
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Proceso de inclusin deslidos, lquidos, o inclusogases, en partculasmicroscpicas, donde se
cubren las sustancias concapas delgadas de unmaterial polimrico.
Qu es microencapsularQu es microencapsular
2
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Partculas de dimetro entre 3-800m:
microcpsulas o microesferas
Pueden servir para liberacin controlada
de principios activos
Pueden utiliarse para proteccin de
sustancias
!as Microesferasson consideradas polvos
de "lu#o libre
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COMPOSICIN DE LASCOMPOSICIN DE LAS
MICROPARTCULASMICROPARTCULAS
a$ %aterial de n&cleo
b$ 'apa o pared o cubierta dematerial
!as micropartculas constan de dos componentes:
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CLASSIICATION O MICROPARTICLECLASSIICATION O MICROPARTICLE
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CLASSIICATION O MICROPARTICLECLASSIICATION O MICROPARTICLE
1.Microspheres:()e active agent is dispersed ordissolved in an inert pol*mer.
2!Microcapsules: ()e active agent "orms a core +omore$ surrounded b* an inert di""usion barrier.
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Microspheres:
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Microcapsules:
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"Para #$e se microe%ca&s$'a("Para #$e se microe%ca&s$'a(
Proteccin del n&cleo de su entorno.
etardar la evaporacin de un n&cleo
voltil.
%e#ora de las propiedades de mane#ode un material pega#oso.
islamiento de un n&cleo reactivocontra el ataue umico.
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/nmascarar el sabor o el olor del n&cleo.
!iberacin controlada de "rmacos.
%anipulacin segura de los materialesticos.
!iberacin selectiva del p.a.
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"Para #$e se microe%ca&s$'a("Para #$e se microe%ca&s$'a(
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UNDAMENTAL CONSIDERATIONUNDAMENTAL CONSIDERATION))
Core ma*eria' Coa*i%+ ma*eria' ,e-ic'e
So'i. Li#$i.
Microe%ca&s$'a*io%
Po'/mers)
1aes
A#$eo$s
No%a#$eo$sesins
Proteins
Pol*sacc)arides
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1! orma*io% of three immiscible phasessolvent.a core material p)ase.a coating material p)ase.
2!Deposition of the coating ma*eria' o% *-ecore ma*eria'!
3. Rigidizing the coating *-erma' cross'i%i%+ or .eso'a*io% *ec-%i#$es4!
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Pasos .e' &rocesoPasos .e' &roceso ::
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5U6 SE DE7E TENER EN5U6 SE DE7E TENER EN
CUENTA)CUENTA)
nature o" t)e core and coating materials.
t)e stabilit* and release c)aracteristics o"t)e coated materials.
t)e microencapsulationmet)ods.
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CU7IERTA CU7IERTA coating materialscoating materials44
'an be liuidor solid
()e composition: dispersed and2or dissolved
material.
()e pol*mer s)ould be capable o" "orming a "ilmt)at is co)esiveit) t)e core material.
4t s)ould be c)emicall* compatible, non-reactiveit) t)e core material.
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5enerall* )*drop)ilic 2 )*drop)obic pol*mers2acombination o" bot) are used
number o" coating materials )ave been used
success"ull*:
-gelatin-polyinyl alcohol-ethyl cellulose-cellulose acetate phthalate! etc.
15
CU7IERTA CU7IERTA coating materialscoating materials 44
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POL8MERSPOL8MERS
6(7!96(/(4'
BIODEGRADABLE
Ex:PolyanhydridesLactides, glycolides
NON-BIODEGRADABLE
Ex: epoxy polyers acrolein
PRO!EIN" Ex: al#$ins gelatin collagen
%ARBO&'DRA!E" Ex: starch carrageenan
%&E(I%ALL' (ODI)IED%ARBO&'DRA!E"
Ex: poly acryl dextran poly acryl starch
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MECANISMOS DE LI7ERACINMECANISMOS DE LI7ERACINDEL PRINCIPIO ACTI,ODEL PRINCIPIO ACTI,O
+!a pared se debe romper al momento del uso$:
17
Por presin o tensin de corte.
Por "usin de la pared.
%ediante disolucin en condicionesparticulares, e#emp recubrimiento de unp.a entrico.
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Meca%ismos .e 'i9eraci:% .e'Meca%ismos .e 'i9eraci:% .e'&ri%ci&io ac*io&ri%ci&io ac*io
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por la accin de un disolvente
por ataue enimatico
por una reaccin umica
por )idrlisis o lenta desintegracin.
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PRINCIPALES T6CNICAS DEPRINCIPALES T6CNICAS DEMICROENCAPSULACINMICROENCAPSULACIN
ir suspension tec)niues+ 1urster$
'oacervation process
pra*dr*ing ; congealing
Pan coating
olvent evaporation
Pol*meriation
/trusion
ingle ; double emulsion tec)niues
upercritical "luid anti solvent met)od +$
6ole vibration tec)nolog*
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AIR SUSPENSIONAIR SUSPENSION
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AIR SUSPENSIONAIR SUSPENSION
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COACER
,ACI
N
SIMP
LE
COACER
,ACI
N
SIMP
LE
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!uido o slidoinmiscible
/mulsin o dispersin al 30@
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COACER
,ACIN
COMPLE>A
COACER
,ACIN
COMPLE>A
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+iii$ addition o" nonsolvent, e.g. addition o" isoprop*let)er to met)*l et)*l Ketone solution o" celluloseacetate but*rate
+iv$ addition o" incompatible pol*mer to t)e pol*mersolution, e.g. addition o" pol*butadiene to t)esolution o" et)*lcellulose in toluene
+v$ inducing pol*merLpol*mer interaction, e.g.interaction o" gum arabic and gelatine at t)eir iso-electric point.
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COACER,ATION P@ASECOACER,ATION P@ASESEPARATIONSEPARATION
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Seco%. s*e&Seco%. s*e&deposition o" liuid pol*mer upon t)e core material.
i%a''/i%a''/microcapsules are stabilied b* crosslinKing,desolvation or t)ermal treatment.
+rosslin/ing+rosslin/ing"ormation o" c)emical linKs beteen molecularc)ains to "orm a t)ree-dimensional netorK o"connected molecules.
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COACER,ATION P@ASECOACER,ATION P@ASESEPARATIONSEPARATION
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()e ulcanizationo" rubber I elemental sul"urcrosslinKing+eaK plastic to a )ig)l* resilient elastomer$.
+hitosanat p M.0 an e""ective cross-linKer&olyethylenimine 0&'# +p
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upercritical "luids are highly compressed gassest)at possess several advantageous properties o" bot)
liuids and gases. small c)ange in temperature or pressure causes alarge c)ange in t)e densit* o" supercritical "luids near
t)e critical point.
()e most idel* used being supercritical carbondioide+'D
=$, alKanes+'
=to '
E$, and nitrous oide
+6=
D$. 35
Po'/mer E%ca&s$'a*io% 9/ Ra&i.Po'/mer E%ca&s$'a*io% 9/ Ra&i.E&a%sio% ofE&a%sio% of S$&ercri*ica'S$&ercri*ica'
'$i.s'$i.s
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Hluido supercrtico contiene el ingredienteactivo * el material de la cubierta, a alta presin
luego es lanado a la presin atmos"rica atravs de una peue?a bouilla.
!a cada repentina de la presin )ace ue ladesolvatacin de la cubierta se deposite alrededorde la sustancia activa +n&cleo$ * "orma una capade recubrimiento.
36
Ra&i. e&a%sio% ofRa&i. e&a%sio% ofs$&ercri*ica' so'$*io%s$&ercri*ica' so'$*io%
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()e active ingredient and t)e s)ell material must be ver*soluble in supercritical "luids.
Ner* "e pol*mers it) lo co)esive energ* densities+e.g., pol*dimet)*lsiloanes, pol*met)acr*lates$ aresoluble in supercritical "luids suc) as 'D=.
()e solubilit* o" pol*mers can be en)anced b* using co-solvents.
4n some cases nonsolvents are usedO t)is increases t)esolubilit* in supercritical "luids, but t)e s)ell materials donot dissolve at atmosp)eric pressure.
37
Po'/mer E%ca&s$'a*io% 9/ Ra&i. E&a%sio% ofPo'/mer E%ca&s$'a*io% 9/ Ra&i. E&a%sio% ofS$&ercri*ica' '$i.sS$&ercri*ica' '$i.s
DisadantageDisadantage::
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Microe%ca&s$'a*io% 9/ ra&i. e&a%sio% ofMicroe%ca&s$'a*io% 9/ ra&i. e&a%sio% ofs$&ercri*ica' so'$*io%s RESS4!s$&ercri*ica' so'$*io%s RESS4!
38
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%icroencapsulation b* rapid epansion o"supercritical solutions +/$.
5as anti-solvent +5$ process
Particles "rom a gas-saturated solution+P5$
Po'/mer E%ca&s$'a*io% 9/ Ra&i.Po'/mer E%ca&s$'a*io% 9/ Ra&i.E&a%sio% of S$&ercri*ica' '$i.s!E&a%sio% of S$&ercri*ica' '$i.s!
MET@ODSMET@ODS
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4s capable "or microencapsulating liuids andsolids o" varied sie ranges, it) diverse coating
materials.
()e encapsulated product can be supplied as
- slurr* in t)e )ardening media
- dr* poder.
Production rates o" C0 to MC pounds per )our.40
M$'*iorifice ce%*rif$+a'M$'*iorifice ce%*rif$+a'
&rocess&rocess
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()e coating is applied as a solution or as anatomied spra* to t)e desired solid core material int)e coating pan.
7suall*, to remove t)e coating solvent, arm airis passed over t)e coated materials as t)e coatingsare being applied in t)e coating pans.
4n some cases, "inal solvent removal isaccomplis)ed in dr*ing oven.
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Pa% coa*i%+Pa% coa*i%+
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Pa% coa*i%+Pa% coa*i%+
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CO EXTRUSIONCO EXTRUSION
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COBETRUSIONCOBETRUSION
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SPRA8 DR8IN< ANDSPRA8 DR8IN< AND
SPRA8 CON
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'oating solidi"ication in s&ra/ .r/i%+ is e""ectedb* rapid eaporation of a solent in )ic) t)ecoating material is dissolved.
'oating solidi"ication in s&ra/ co%+ea'i%+met)od is accomplis)ed b*:-thermally congealing a molten coating
material or
-b* solidi"*ing a dissolved coating b* introducingt)e coating core material miture into anonsolent.
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SPRA8 DR8IN< AND SPRA8SPRA8 DR8IN< AND SPRA8CON
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emoval o" t)e nonsolvent or solvent "rom t)ecoated product is t)en accomplis)ed b* sorptionetraction or evaporation tec)niues.
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SPRA8 DR8IN< AND SPRA8SPRA8 DR8IN< AND SPRA8CON
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SPRA8 DR8IN< AND SPRA8SPRA8 DR8IN< AND SPRA8CON
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olvent evaporation tec)niues are carried out ina liuid manu"acturing ve)icle +D21 emulsion$)ic) is prepared b* agitation o" to immiscibleliuids.
()e process involves dissolving microcapsulecoating +pol*mer$ in a volatile solvent )ic) isimmiscible it) t)e liuid manu"acturing ve)iclep)ase.
core material +drug$ to be microencapsulated isdissolved or dispersed in t)e coating pol*mersolution.
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SOL,ENT E,APORATIONSOL,ENT E,APORATION
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1it) agitation, t)e core L coating material mitureis dispersed in t)e liuid manu"acturing ve)iclep)ase to obtain appropriate sie microcapsules.
gitation o" s*stem is continued until t)e solventpartitions into t)e aueous p)ase and is removedb* evaporation.
()is process results in )ardened microsp)eres)ic) contain t)e active moiet*.
51
SOL,ENT E,APORATIONSOL,ENT E,APORATION
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A&&'ica*io%s ofA&&'ica*io%s ofmicroe%ca&s$'a*io%microe%ca&s$'a*io%
()e tec)nolog* )as been used idel* in t)e design
o" controlled release and sustained release dosage"orms.
(o masK t)e bitter taste o" drugs liKe Paracetamol,6itro"urantoin etc.
to reduce gastric and ot)er 5.4. tract irritations.
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CONTROLES 8
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Siee a%a'/sis
53
Mor&-o'o+/,iscosi*/ of *-e &o'/mer so'$*io%s
De%si*/ .e*ermi%a*io%
7$' .e%si*/
Ca&*$re efficie%c/
A%+'e of co%*ac*
Disso'$*io%
Po'/mer so'$9i'i*/ i% *-e So'e%*s
CONTROLES 8CONTROLES 8
CARACTERIACINCARACTERIACIN
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Es*a &rese%*aci:% se 9as: e% 'os *ra9a;os .e)Es*a &rese%*aci:% se 9as: e% 'os *ra9a;os .e)
!Se%*-i' $mar / Sa%.ee& Mo''i.ai%!!Se%*-i' $mar / Sa%.ee& Mo''i.ai%!
GraciasGracias