Excipients used in the

manufacture of tablets
 EXCIPIENTS
• Diluents/Fillers
• Binders
• Disintegrants
• Lubricants
• Glidants
• Miscellaneous.
1.Diluents/fillers
• Diluents are employed in the formulation of tablets (by all methods)
to increase the mass of the tablets that contain a low concentration of
therapeutic agent and thereby render the manufacturing process
more reliable and reproducible.
• Diluents must exhibit good compression properties and be
inexpensive.
 Examples of diluents for tablets
• (1) anhydrous lactose
• (2) lactose monohydrate
• (3) spray-dried lactose
• (4) starch
• (5) dibasic calcium phosphate
• (6) microcrystalline cellulose (MCC)
• (7) mannitol.
CONT…………….
• The choice of filler usually is based on the experience of the
manufacturer with the material, its relative cost, and its compatibility
with the other formulation ingredients.
• For example, calcium salts must not be used as fillers with tetracycline
antibiotics because of an interaction between the two agents that
results in reduced tetracycline absorption from the gastrointestinal
tract.
• Among the fillers most preferred are lactose, because of its solubility
and compatibility, and microcrystalline cellulose, because of its easy
compaction, compatibility, and consistent uniformity of supply
2.Binders

• Binders are predominantly (but not exclusively) polymeric

components that are employed in the production of tablets by the
wet granulation method of manufacture.
• In this role, binders are either added as a solution or as a solid into
the powder mix (following which the granulating fluid, typically water,
is added).
 Examples and properties of binders commonly used in the
manufacture
of tablets
Binder Concentration General comments

Hydroxypropylmethylcellulose 2–5% w/w The required concentration is dependent on

molecular weight (grade) used

Polyvinylpyrrollidone 0.5–5% w/w The required concentration is dependent on

molecular weight (grade) used

Hydroxypropylcellulose 2–6% w/w The required concentration is dependent on

molecular weight (grade) used
 Examples and properties of binders commonly used in the
manufacture
of tablets
Binder Concentration General comments

Sucrose 50–67% w/w Added as a syrup Produces hard tablets whose properties
are affected by moisture

Microcrystalline cellulose 20–90% w/w Often used as a binder and diluent

Acacia 1–5% w/w Produces hard tablets

3.Disintegrants
• Disintegrating agents include croscarmellose,corn and potato
starches, sodium starch glycolate, sodium carboxymethylcellulose,
polyvinylpyrrolidone (PVP), crospovidone, cation exchange resins,
alginic acid, and other materials that swell or expand on exposure to
moisture and effect the rupture or breakup of the tablet in the
gastrointestinal tract.
• Croscarmellose (2%) and sodium starch glycolate (5%) are often
preferred because of their high water uptake and rapid action.
• One commercial brand of sodium starch glycolate is reported to swell
up to 300% of its volume in water
Cont …….
• When starch is employed, 5% to 10% is usually suitable, but up to
about 20% may be used to promote more rapid tablet disintegration.
• The total amount of disintegrant used is not always added in
preparing the granulation.
• Often a portion (sometimes half) is reserved and added to the
finished granulation prior to tablet formation.
• This results in double disintegration of the tablet.
4.Lubricants
• During compression lubricants act at the interface between the face
of the die and the surface of the tablet and act to reduce the friction
at this interface during ejection of the tablet from the tablet press.
• Inadequate lubrication of this interface results in the production of
tablets with a pitted surface and is due to the inability of the tablet
surface to detach from the surface of the tablet die.
• The appearance of the tablet is an important pharmacopoeial (and
consumer) requirement and, therefore, inadequate lubrication will
lead to rejection of the tablet batch.
EXAMPLES OF LUBRICANTS
• Talc
• Magnesium stearate
• Calcium stearate