Pharmaceutical excipients

Making of preparations involves different techniques, shall train a students to be competant enough to know about different excipients.

1. 1
Pharmaceutical Excipients
Asst. Prof. Om M. Bagade
M. Pharm, D. I. P. L, PhD Pursuing
Department of Pharmaceutics

2. Objective:
Tomakestudentsunderstandregardingthe
Meaningofexcipients&theirrole&its
importance.
Outcome:
Makingofpreparationsinvolvesdifferent
techniques,shalltrainastudentstobe
competantenoughtoknowaboutdifferent
excipients.

3. Excipient
Pharmacologicallyinactiveingredient
whichisaddedtoapharmaceutical
compound
Inmanycases,an"active"substance(such
asacetylsalicylicacid)maynotbeeasily
administeredandabsorbedbythehuman
body;insuchcasesthesubstancein

4. The excipient must
Besafeintheamountusedinthedrug
Notaffectthebioavailabilityand
performanceofthedrug
Bemanufacturedinaccordancewithgood
standards
Notethatsomepeoplemaybeallergicto
someexcipients-forexample,many
peoplearelactose-intolerant.

5. Criteria to choose the right
excipient?
Depending on the route of administration,
and form of medication, different
excipients may be used

6. Types of excipients
1.Antiadherents
2.Binders
3.Coatings
4.Fillers
5.Diluents
6.Flavours
7.Colours
8.Lubricants
9.Glidants
10. Preservatives
11. Sorbents
12. Sweeteners

7. Antiadhertent
Usedtoreducetheadhesionbetweenthe
powder(granules)andthepunchfacesand
thuspreventstickingtotabletpunches.
Theyarealsousedtohelpprotecttablets
fromsticking
Mostcommonlyusedismagnesium
stearate

8. Binders
Hold the ingredients in a tablet together.
Binders ensure that tablets and granules can be
formed with required mechanical strength
Binders are usually:
Saccharides and their derivatives:
Disaccharides: sucrose, lactose;
Polysaccharides and their derivatives: starches, cellulose or
modified cellulose such as microcrystalline cellulose and
cellulose ethers such as hydroxypropyl cellulose (HPC);
Sugar alcohols such as xylitol, sorbitol or mantitol;
Protein: gelatin
Synthetic polymers: polyvinylpyrrolidone (PVP),
polyethylene glycol (PEG)...

9. Binders are classified according to
their application:
•Solution:bindersaredissolvedinasolvent(forexamplewater
oralcoholcanbeusedinwetgranulationprocesses)
–Examplesincludegelatin,cellulose,cellulosederivatives,
polyvinylpyrrolidone,starch,sucroseandpolyethylene
glycol.
•Dry:bindersareaddedtothepowderblend,eitherafterawet
granulationstep,oraspartofadirectpowdercompression(DC)
formula
–Examplesincludecellulose,methylcellulose,
polyvinylpyrrolidoneandpolyethyleneglycol.

10. Coatings
Protect tabletingredientsfrom
deteriorationbymoistureintheairand
makelargeorunpleasant-tastingtablets
easiertoswallow.
Formostcoatedtablets,acelluloseether
hydroxypropylmethylcellulose(HPMC)
filmcoatingisusedwhichisfreeofsugar
andpotentiallergen
Capsulesarecoatedwithgelatin.

11. Disintegrant
Expand and dissolve when wet causing the tablet to break
apart in the digestive tract, releasing the active ingredients
for absorption.
Disintegrant types include:
Water uptake facilitators
Tablet rupture promoters
They ensure that when the tablet is in contact with water, it
rapidly breaks down into smaller fragments, facilitating
dissolution.
Examples of disintegrants include:
Crosslinked polymers: crosslinked polyvinylpyrrolidone
(crospovidone), crosslinked sodium carboxymethyl
cellulose (croscarmellose sodium).
The modified starch sodium starch glycolate

12. Fillers
Fillers fill out the size of a tablet or capsule, making it practical to
produce and convenient for the consumer to use
A good filler must be inert, compatible with the other
components of the formulation, non-hygroscopic, relatively
cheap, compatible, and preferably tasteless or pleasant tasting.
Example :
Plant cellulose (pure plant filler) is a popular filler in tablets
or hard gelatin capsules.
Dibasic calcium phosphate is another popular tablet filler
Lactose , sucrose, glucose, mannitol, sorbitol, calcium
carbonate, and magnesium stearate

13. Flavours
•Usedtomaskunpleasanttastingoftheactive
ingredientsandimprovethelikelihoodthatthe
patientwillcompleteacourseofmedication
•Flavouringsmaybenatural(e.g.fruitextract)or
artificial
•Forexample,toimproveabitterproductwecan
use:
–Mint,cherryoranise
•Toimproveasaltyproduct–
–peach,apricotorliquoricemaybeused
•Toimproveasourproduct
–raspberryorliquoricemaybeused

14. Colors
Substancesaddedtoimprovethe
appearanceofaformulation.
Colorconsistencyisimportantasitallows
easyidentificationofamedication.

15. Lubricants
Lubricantsareagentsaddedinsmall
quantitiestotabletandcapsuleformulations
toimprovecertainprocessingcharacteristics
like:
Preventingredientsfromclumpingtogetherand
fromstickingtothetabletpunchesorcapsule
fillinmachine
Ensurethattabletformationandejectioncan
occurwithlowfrictionbetweenthesolidanddie
wall.
Commonmineralsliketalcorsilica,and
fats,e.g.vegetablestearin,magnesium
stearateorstearicacidarethemostfrequently

16. Glidants
Usedtopromotepowderflowbyreducing
interparticlefrictionandcohesion
Theseareusedincombinationwithlubricants
astheyhavenoabilitytoreducediewall
friction
Examplesincludefumedsilica,talc,and
magnesiumcarbonate.

17. Preservatives
•Substancethatisaddedtoproductsto
preventdecompositionbymicrobialgrowthor
byundesirablechemicalchanges
•Sometypicalpreservativesusedin
pharmaceuticalformulationsare
–AntioxidantslikevitaminA,vitaminE,vitamin
C,retinylpalmitate,andselenium
–Theaminoacidscysteineandmethionine
–Citricacidandsodiumcitrate
–Syntheticpreservativesliketheparabens:methyl
parabenandpropylparaben

18. Sorbents
areusedfortablet/capsulemoisture-
proofingbylimitedfluidsorbing(takingup
ofaliquidoragaseitherbyadsorptionor
byabsorption)inadrystate

19. Sweetners
areaddedtomaketheingredientsmore
palatable,especiallyinchewabletablets
suchasantacidorliquidslikecoughsyrup
Therefore,toothdecayissometimes
associatedwithcoughsyrupabuse.Sugar
canbeusedtodisguiseunpleasanttastesor
smells

20. Each tablet contains:
•hydrogenated castor oil
•hydroxypropylcellulose
•Mannitol
•microcrystalline cellulose
•polyethylene glycol 6000
•The pink film coating contains
–ferric oxide
–hypromellose2910
–lactose monohydrate
–titanium dioxide
–triacetin.
•The tablets are polished with Carnauba wax

21. Function of each
hydrogenated castor
oil
lubricant
hydroxypropylcellulose
Disentigrant and
binder
Mannitol
Sweetner and
disintegrant

22. What Do you Think about
following . . .
Q.1.DefineExcipients.
Q.2.ExplainindetailabouttheClassificationof
Excipients?
Q.3.Explainindetailthemeritsanddemeritsof
Excipients?
Q.4.StatetheimportanceofExcipientsin
pharmacy?