EXCIPIENTS

Dr. Asiimwe Anthony.

 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 substance in question
may be dissolved into or mixed with an
excipient
 The excipient must
• Be safe in the amount used in the drug
• Not affect the bioavailability and performance
of the drug
• Be manufactured in accordance with good
standards
• Note that some people may be allergic to
some excipients - for example, many people
are lactose-intolerant.
 How do we choose the right excipient?

• Depending on;

 The route of administration and

 Form of medication, different excipients may

be used.
 Types of excipients
1. Antiadherents 10. Preservatives
2. Binders 11. Sorbents
3. Coatings 12. Sweeteners
4. Fillers
5. Diluents
6. Flavours
7. Colours
8. Lubricants
9. Glidants
 1. ANTIADHERENTS
• Used to reduce the adhesion between the
powder (granules) and the punch faces and thus
prevent sticking to tablet punches.
• They are also used to help protect tablets from
sticking.
• Most commonly used is magnesium stearate.
 2. Binders
• Binders ensure that tablets & granules can be formed with
required mechanical strength (Hold the ingredients in a tablet
together).
• Binders are usually:
– Saccharides & their derivatives:
– Disaccharides: sucrose, lactose;
– Polysaccharides & their derivatives: starches, cellulose
or modified cellulose such as microcrystalline cellulose
& cellulose ethers such as hydroxypropyl cellulose
(HPC);
– Sugar alcohols such as xylitol, sorbitol or mantitol;
• Protein: Gelatin
• Synthetic polymers: Polyvinylpyrrolidone (PVP),
Polyethylene glycol (PEG)...
 Binders are classified according to
their application:
• Solution :Binders are dissolved in a solvent (for
example water or alcohol can be used in wet
granulation processes)
– Examples include gelatin, cellulose, cellulose
derivatives, polyvinylpyrrolidone, starch, sucrose &
polyethylene glycol.
• Dry : Binders are added to the powder blend,
either after a wet granulation step, or as part of a
direct powder compression (DC) formula
– Examples include cellulose, methyl cellulose,
polyvinylpyrrolidone and polyethylene glycol.
 3. COATINGS
USES:
•Protect tablet ingredients from deterioration by
moisture in the air & make large or unpleasant-
tasting tablets easier to swallow.
•For most coated tablets, a cellulose ether
hydroxypropylmethylcellulose (HPMC) film coating is
used which is free of sugar & potenti allergen
• Capsules are coated with gelatin.
 4. DISINTEGRANT
• Expand & dissolve when wet causing the tablet to break apart
in the digestive tract, releasing the active ingredients for
absorption.
• Disintegrant types include:
i. Water uptake facilitators
ii. 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
 5. FILLERS
• Fillers fill out the size of a tablet or capsule, making it
practical to produce & 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 & 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.
 6. FLAVOURS
• Used to mask unpleasant tasting of the active
ingredients & improve the likelihood that the
patient will complete a course of medication
• Flavourings may be natural (e.g. fruit extract) or
artificial
• For example, to improve a bitter product we can
use :
– Mint , cherry or anise
• To improve a salty product –
– peach , apricot or liquorice may be used
• To improve a sour product
– raspberry or liquorice may be used
 7. COLORS
• Substances added to improve the appearance of a
formulation.
• Color consistency is important as it allows easy
identification of a medication.
 8. LUBRICANTS
• Lubricants are agents added in small quantities to
tablet & capsule formulations to improve certain
processing characteristics like:
– Prevent ingredients from clumping together &
from sticking to the tablet punches or capsule
filling machine.
– Ensure that tablet formation & ejection can occur
with low friction between the solid & die wall.
• Common minerals like; Talc or silica & Fats e.g.
vegetable stearin, magnesium stearate or stearic acid
are the most frequently used lubricants in tablets or
hard gelatin capsules.
 9. GLIDANTS
• Used to promote powder flow by reducing
interparticle friction & cohesion.
• These are used in combination with lubricants as
they have no ability to reduce die wall friction
• Examples include; Fumed silica, talc &
magnesium carbonate.
 10. PRESERVATIVES
• Are added to products to prevent decomposition by
microbial growth or by undesirable chemical changes.
• Typical preservatives used in pharmaceutical
formulations are;
– Antioxidants like vitamin A, vitamin E, vitamin C,
retinyl palmitate & selenium.
– The amino acids cysteine & methionine.
– Citric acid & sodium citrate.
– Synthetic preservatives like the parabens: methyl
paraben and propyl paraben.
 11. SORBENTS
• Used for tablet/capsule moisture-proofing by
limited fluid sorbing (taking up of a liquid or a gas
either by adsorption or by absorption) in a dry
state.
 12. SWEETNERS
• Are added to make the ingredients more
palatable, especially in chewable tablets such as
antacid or liquids like cough syrup.
• Therefore, tooth decay is sometimes associated
with cough syrup abuse.
• Sugar can be used to disguise unpleasant tastes
or smells.
 EXAMPLE
Each tablet contains:
• hydrogenated castor oil
• hydroxypropylcellulose
• Mannitol
• microcrystalline cellulose
• polyethylene glycol 6000
• The pink film coating contains
– ferric oxide
– hypromellose 2910
– lactose monohydrate
– titanium dioxide
– triacetin.
• The tablets are polished with Carnauba wax
 FUNCTION OF EACH
• hydrogenated castor oil
– lubricant • The others are
• hydroxypropylcellulose homework
– Disentigrant and binder
• Mannitol
– Sweetner and
disintegrant