Excipient

• Pharmacologically inactive ingredient which is

added to a pharmaceutical compound
• In many cases, an "active" substance (such as
acetylsalicylic acid) may not be easily
administered and absorbed by the human
body; in such cases the API may be dissolved
into or mixed with an excipient
 Requirements against the
excipients
• Pharmacologically inert
• Stable for handling
• Cost effective
• No interaction with the drug and other
components
• No taste, odour and colour

Note that some people may be allergic to some excipients -

for example, many people are lactose-intolerant.
 Excipient
Functions of excipients:
i) For providing essential manufacturing technology functions (binders,
glidants, lubricants may be added),
ii) For enhancing patient acceptance (flavors,
colourants may be added),
iii) For providing aid in product identification
(colourants may be added),
iv) For optimizing or modifying drug release
(disintegrants, hydrophilic polymers, wetting
agents, biodegradable polymers may be
added),
v) For enhancing stability (antioxidant, UV
absorbers may be added 4
 Types of excipients
1. Fillers 10. Preservatives
2. Diluents 11. Sorbents
3. Antiadherents 12. Sweeteners
4. Binders
5. Coatings
6. Flavours
7. Colours
8. Lubricants
9. Glidants
 1- Filler or diluent

use: to make required bulk of the tablet .

to provide better tablet properties such as to improve cohesion,
to permit use of direct compression manufacturing
to improve flowability

Most common fillers in tablets:

1. Lactose, sucrose, mannitol;
2. Dicalcium phosphate dihydrate
3. Starch
4. cellulose / microcrystalline cellolose

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 2- Binders and adhesives
Role: Ensure that granules and tablets can be formed
with the required mechanical strength (glue that holds
powders together to form granules).
- In dry powder form
- In solution
Examples:
starch paste 5-25%
gelatine solution 10-20%,
gum acacia, tragacantha, 10-25%
glucose syrup 50%,
cellulose derivative
polyvinylpyrrolidone 2% (PVP), PEG

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 3- Disintegrants

Disintegrants are substances or mixture of

substances added to the drug formulations, which
facilitate dispersion of tablets into smaller particles
for quick dissolution when it comes in contact with
water in the GIT.

Ideal properties of disintigrants:

•good hydration capacity,
•poor solubility,
•poor gel formation capacity.

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 3- Disintegrants

The Method of Disintegrant Addition:

1. Mixed with other ingredients prior to granulation & thus

incorporated within the granules (intragranular addition).
2. Mixed with the dry granules before the complete powder
mixture is compacted (extragranular addition).
3. incorporated as both an intragranular and an extragranular
portion.

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Commonly Used Disintegrants:

1. Starch:
– concentration up to 5-20% of tablet weight
– swells in contact with water
2. Polyvinyl-pyrrolidone
3. Carboxymethyl-cellulose
4. Superdisintegrants (e.g. sodium starch glycolate,
croscarmellose, crosspovidone = cross linked povidone)
– Swells up to ten fold within 30 seconds when
contact water.

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 4- Glidants

Role: Improve flowability of the powder

They are added during direct compaction and to granulation before
tabletting (they reduce interparticulate friction).

Common Glidants:
1. Talc (concentration 1-2 %).
2. Colloidal silica (0.2 %).
3. Corn Starch 5-10%

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 5- Lubricants
Role: Lubricants
• prevent adherence of granule/powder to die wall
and
• promote ejection from the die after compaction,
• reduce inter particle friction and
• improve the rate of flow of the tablet granulation

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 5- Lubricants

Disadvantages of lubricants
1. Lubricants tend to be hydrophobic, so their levels (typically
0.3 – 2%) need to be optimized:
–Under-lubricated blends tend to flow poorly and show compression
sticking problems
–Over-lubricated blends can adversely affect tablet hardness and
dissolution rate, as well as tablet strength.

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 5- Lubricants
Commonly used Lubricants
A. Water- insoluble (Fatty acids-based) lubricant
• Magnesium Stearate
• Calcium Stearate
• Stearic Acid, stearic acid salt
• Talc
• Silica derivative- colloidal silica such as Cab-O-Sil,
Aerosil in 0.25-3% conc.
• liquid paraffin, propylene glycol (PG)

B. water-soluble lubricant
- PEG 6000; less effective
- Magnesium/sodium lauryl sulfate; good lubrication and
surface wetting effect
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 6- Adsorbents

Adsorbents are the agents that can retain large quantities of

liquids.

Therefore liquids (Vitamin E, essential oils, eutectics,

hygroscopic agents) can be incorporated into tablets by addition
of adsorbents.

Large surface-adsorbes the moisture

Water-absorbtion capacity: 44-99%

Generally the liquid to be adsorbed is first mixed with the

adsorbent prior to incorporation into the formulation.

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 6- Adsorbents

Most commonly used adsorbents:

• anhydrous calcium phosphate,
• starch,
• silica colloidalis anhydrica (Aerosil)

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 7 – Antistatic agents

Reduces electrostatic charge developing

during handling of the powder.

Most commonly used antistatic agent:

•silica colloidalis anhydrica (Aerosil)

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 8- Flavours

Use: give the tablet a more pleasant taste or

to mask an unpleasant one. (Chewable tablet)

• Flavouring agents are often thermolabile and so

cannot be added prior to an operation involving heat.
• They are often mixed with the granules as an alcohol
solution.

Ex: citric acid, glycerol, orange oil, menthol, vanillin etc.

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 9- Sweeteners

They are used in chewable tablet to exclude or limit the use of

sugar in the tablets.

Most commonly used sweetenrs:

• Mannitol, lactose, sucrose, Dextrose 72% as sweet as
sucrose.
• Saccharin, 500 times sweeter than sucrose.
Disadvantage: has a bitter aftertaste
• Aspartame, largely replace saccharin., 180 times sweeter
than sucrose
Disadvantage: lack of stability in the presence of
moisture.

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 10 - Colorants

Uses: It is added to tablets to

• aid identification,
• improve patient compliance.
• mask of off color drug
• production of more elegant product.

All coloring agents must be approved and certified by

FDA.

These dyes are applied as solution in the granulating

agent.

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 10 - Colorants
Example:
Yellow 6- FD & C sunset yellow
yellow 5- FD & C Tartrazine
green 3- FD & C Fast Green
blue 1- FD & C Brilliant Blue
blue 2 – FD & C Indigotine
red 3- FD & C Erythrosine FD & C
red 22 – FD & C Eosin Y

It is added during coating.

• It can also be added prior to compaction. (can be added as
an insoluble powder or dissolved in the granulation liquid)

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 11 - Buffers
Buffers are added to
maintain a required pH since a change in
pH may cause significant alteration in
stability.

Most commonly used buffering agent in

tablet formulation includes sodium
bicarbonate, calcium carbonate, and
sodium citrate.

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 12 - Antioxidants

Antioxidants are added in tablet formulation: to

protect drug from undergoing oxidation.

Chelators may also act as antioxidant.

Most commonly used antioxidants include

•ascorbic acid and their esters
•alpha-tocopherol
•ethylene diamine
•tetra acetic acid
•sodium metabisulfite
•sodium bisulfite
•citric acid
•tartaric acid
 13. Chelating agents

tend to form complexes with trace amount of

heavy metal ions inactivating their catalytic
activity in the oxidation of medicaments.

Most commonly used chelators:

•Ethylenediamine tetracetic acid and its salts
•Dihydroxy Ethyl Glycine
•Citric Acid
•Tartaric Acid are
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 14. Dissolution Enhancers
They are the agents that alter the molecular forces between
ingredients to enhance the dissolution of solute in the solvent.

Fructose, Povidone, Surfactants are used as dissolution enhancer.

15. Dissolution Retardants

Dissolution retardants are incorporated into tablet formulation
only when controlled release of drug is required.

Waxy materials like stearic acid and their esters can be used as dissolution
retardants.

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 16. Wetting agents (surfactants)

in tablet formulation aid water uptake and thereby enhancing

disintegration and assisting in drug dissolution.
Decrease the surface tension between two liquids or between
liquid and solid, thus increase the solubility.

Anionic:
Sodium lauryl sulphate (SLS):

Cationic:
Cetrimid (antiseptic agent as well)

Nonionic:
Tweens, Spans

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Question of splitting
 1
• API
• Mannitol
• Sodium bicarbonate
• Anhydrous citric acid
• Ascorbic acid
• Cola flavour
• Orange flavour
• Aspartame
 2
• API
• Ethylcellulose
• Silicon dioxide anhydrous
• Hypromellose 6cPS
• Mannitol
• Aspartame (15 mg)
• Croscarmellose-sodium (superdisintegrant)
• Magnesium-stearate
• Lemon flavour
 3
• API
• Red iron oxide (E 172)
• Magnesium-steareate
• Hypromellose
• Poliethylene-oxide
• Sodium chloride
• Macrogol 3350
• Cellulose-acetate
• "Opadry White YS-2-7063”
• Titanium-dioxidide (E171)
• "Black Ink S-1-17823" (Black iron-oxide)
 4
• API
• Core: magnesium-stearate, povidone K30,
purified water, microcrystalline cellulose,
sodium-alginate.
• Coating: Montan-glycol wax, macrogol 6000,
macrogol 400, titanium-dioxideE 171, talc
 5
• API
• Core: hypromellose2208, hydrogenated castor
oil, carmellose-sodium, povidone (K29-32),
maltodextrine, magnesium-stearate, lactose-
monohydrate, anhydrous silicon-dioxide,
mannitol (E421), yellow iron-oxide (E172),
glycerol-dibehenate.
• Coating: "Opadry pink OY-S-24900": hipromellose,
yellow iron-oxide (E172), titanium-dioxide (E171),
macrogol 400, red iron-oxide (E172).
Geomatrix® technology
 6
• API
• Diethyl-phtalate, Eudragit L100, Eudragit
NE30D, Eudragit L30D, talc, shellac, inert
sucrose and corn starch microgranules
• Shell:
eritrosine (E 127), titanium-dioxide (E 171),
gelatine
Multiple Unit Pellet System (MUPS)
 Thank you
for your attention!
Excipients Function
Diluent Diluents make the required bulk of the
tablet when the drug dosage itself is
inadequate to produce tablets of adequate
weight and size
Binder Binders are added to tablet formulations to
add cohesiveness to powders, thus
providing the necessary bonding to form
granules, which under compaction form a
cohesive mass or a compact which is
referred to as a tablet.

Disintegrants A disintegrant is added to most tablet

formulations to facilitate a breakup or
disintegration of the tablet when11/29/2019
placed in 39
Antifrictional Function
Agents
Lubricant Lubricants are intended to reduce the
friction during tablet formation in a die
and also during ejection from die cavity.

Antiadherants Antiadherents are added to reduce

sticking or adhesion of any of the tablet
granulation or powder to the faces of the
punches or to the die wall
Glidants Glidants are intended to promote the
flow of tablet granulation or powder
mixture from hopper to the die cavity by
reducing friction between the particles.

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MISCELLANE Function
OUS
Wetting agent Wetting agents are added to tablet formulation to aid
water uptake during disintegration and assist drug
dissolution.

Dissolution Dissolution retardants as the name suggest, retards

retardant the dissolution of active pharmaceutical
ingredient(s).

Dissolution Dissolution enhancers as the name suggest, enhance

enhancer the dissolution rate of active pharmaceutical
ingredient(s).

buffers Buffers are added to provide suitable micro

environmental pH to get improved stability and / or
bioavailability.
Adsorbents Adsorbents are capable of retaining large quantities
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Excipients Function
Antioxidants Antioxidants are added to maintain product
stability, they act by being preferentially oxidized
and gradually c.onsumed over shelf life of the
product
Chelating Chelating agents are added to protect against
agents autoxidation; they act by forming complexes
with the heavy metal ions which are often
required to initiate oxidative reactions.
Colours Colours are added to tablet formulation for
following purposes: to disguise off colour drugs,
product identification and for production of more
elegant product.
Flavours Flavours are added to tablet formulation in order
to make them palatable enough in case of
chewable tablet by improving the taste.
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