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Tablet Excipients
Tablet Excipients
A tablet contains active ingredients as well as other substances known as excipients, which
have specific functions.
1. Active Ingredient/Drug/API
a. Insoluble drug- exert local effect
b. Soluble drug- exert systemic effect
2. Excipients/Additives/Inactive Pharmaceutical ingredients/Nonactive ingredients
a. Diluents/Fillers
b. Binders/Adhesive
c. Disintegrants
d. Antifrictional agent
I. Lubricants
II. Glidants
III. Antiadherants
e. Organoleptic additives
I. Colors
II. Flavoring agent
III. Sweetener
f. Co-processed Excipients
Additives/Excipients:
DILUENTS/FILLERS
Diluents are the inert substance added to increase the bulk of the tablet.
They must be nontoxic and acceptable to the drug-regulatory agencies in all countries
where the product is to be marketed.
They must be commercially available in an acceptable grade in all countries where the
product is to be manufactured.
They must be cheap compared to the active ingredients.
They must be physiologically inert.
They must be chemically stable alone and/or in combination with the drug(s) and/or
other tablet components.
They must be free of any unacceptable microbiologic “load”.
They must be color-compatible.
They must have no negative effects on the bioavailability of the drug(s) in the product.
CLASSIFICATION OF DILUENTS:
Miscellaneous
Sugars Polysaccharides Inorganic compounds
compounds
CALCIUM SALTS
Example:
Advantages:
Tetracycline products made with calcium phosphate diluent had less than half the
bioavailability of the standard product.
Divalent cation (Ca++) form insoluble complexes and salts with number of amphoteric or
acidic functionality antibiotics, which generally reduces their absorption.
LACTOSE
Advantages:
1. Lactose has no reaction with most of the drugs, whether in hydrous or anhydrous form.
2. Lactose formulations show good release rates
3. Their granulations are readily dried, and the tablet disintegration times of lactose tablets
are not strongly sensitive to variations in tablet hardness.
4. It is a low cost diluent.
Disadvantages:
Advantages:
1. If spray dried lactose is allowed to dry out and the moisture content falls below the
usual 3% level, the material loses some of its direct compressional characteristics.
2. Spray-dried lactose is especially prone to darkening in the presence of excess moisture,
amines, and other compounds owing to Maillard reactions. Hence, a neutral or acid
lubricant should be used.
STARCH
maltose 3–5%
DEXTROSE (D–Glucose)
MANNITOL
Advantages
Because of the negative heat of solution (cooling sensation in the mouth), its slow
solubility, and its pleasant feeling in the mouth, it is widely used in chewable tablets.
It is relatively non-hygroscopic and can be used in vitamin formulations.
Low calorie content and non-carcinogenic.
Disadvantages
Costly
Mannitol has poor flow characteristics and usually requires fairly high lubricant level.
SORBITOL
It is an optical isomer of mannitol.
Sometimes combined with mannitol formulations to reduce the diluent cost.
Low caloric content & Noncariogenic.
Disadvantages: It is hygroscopic at humidities above 65%.
SUCROSE
Nu Tab– 95% sucrose + 4% invert sugar + small amount of corn starch + Mg-stearate
BINDERS
Agents used to impart cohesive qualities to the powdered material are referred to as
binders or granulators.
1. They impart cohesiveness to the tablet formulation (both direct compression and wet–
granulation method) which insures the tablet remaining intact after compression.
2. They improve the free-flowing qualities by the formation of granules of desired size and
hardness.
Characteristics of binder
Method-I
1. Binders are used in dry form in the powder and then moistened with a solvent (of
the binder) to form wet lumps.
2. By this Method, the binder is not as effective in reaching and wetting each of the
particles within the mass of the powder. Each of the particles in a powder blend has
a coating of adsorbed air on its surface, and it is this film of air which must be
penetrated before the powder can be wetted by the binder solution.
Method-II
Binders are often added in solution form. It requires lower concentration of binder.
Starch Paste 5 – 25
Acacia 1-5
Gelatin 10-20
STARCH PASTE
Method of preparation
Corn starch is dispersed in cold purified water to make a 5 to 10% w/w suspension and then
warming in water both with continuous stirring until a translucent paste is formed..
(Actually hydrolysis of starch takes place.)
LIQUID GLUCOSE
50% to 74% sugar solution is used as binder. They produce hard but brittle granules.
Their cost is low.
GELATIN SOLUTION
Should be prepared freshly and added in warm condition other wise it will become
solid.
Method of preparation
The gelatin is dispersed in cold water and allowed to stand until hydrated. The hydrated
mass is warmed in water bath to dissolve.
CELLULOSIC SOLUTIONS
Method of preparation: HPMC is dispersed in hot water, under agitation. The mixture is
cooled as quickly as possible and as low as possible
HEC (Hydroxy ethyl cellulose), HPC (Hydroxy propyl cellulose) are other successful binders.
LUBRICANTS
Objectives:
1. Prevents adhesion of the tablet material to the surface of dies and punches.
2. Reduce inter-particular friction; improve the rate of flow of tablet granulation.
3. Facilitate ejection of the tablets from the die cavity.
Examples:
Talc, magnesium stearate, calcium stearate, stearic acid, hydrogenated vegetable oils and
polyethylene glycols (PEG).
Method of addition of lubricants:
1. The lubricant is divided finely by passing it through a 60 to 100 mesh nylon cloth on to
the granulation. In production this is called ‘bolting the lubricant’.
2. After addition the granulation is tumbled or mixed gently to distribute the lubricant
without coating all the particles too well.
* Complete coating will produce dissolution problem.
Soluble lubricants
Magnesium stearate
Lubricants are included to reduce the friction during tablet ejection between the walls of
the tablet and the wall of the die in which the tablet was formed.
Antiadherents are used for the purpose of reducing the sticking or adhesion of any of the
tablet ingredients or powder to the faces of the punches or to the die wall.
Glidants are intended to promote flow of the tablet granulation or powder materials by
reducing the friction between the particles.
An ingredient used for lubrication purpose may possess other two properties as well.
Lubricant Percentage
Boric acid 1
Sodium chloride 5
Sodium benzoate 5
Sodium acetate 5
Sodium oleate 5
dl-leucine 1–5
Lubricant Percentage
Sterotex 0.25-2
Talc 1-5
Wax 1-5
Sterowet 1-5
Antiadherent
Talc 1-5
Cab-O-Sil 0.1-0.5
Syloid 0.1-0.5
DL-leucine 3-10
Glidant
Talc 5
Cab-O-Sil 0.1-0.5
Syloid 0.1-0.5
Aerosil 1-3
DISINTEGRANTS
Prior to granulation
During the lubrication step prior to compression.
At both processing steps
Disintegrants can be classified chemically as Starches, clays, celluloses, alginates, gums and
cross-linked polymers.
Starch
For their disintegrating effect starches are added to the powder blends in dry state.
Mode of action:
Starch has a great affinity for water and swells when moistened, thus facilitating the
rupture of the tablet matrix.
Others have suggested that the spherical shape of the starch grains increases the
porosity of the tablet, thus promoting capillary action.
Normally 5% w/w is suggested. For rapid disintegration 10 – 15% w/w may be taken.
Starch Disintegrants
Super disintegrants
Mode of action
* Sodium lauryl sulfate is a surfactant. It increases the rate of wetting of the tablet,
thus decreases the disintegrating time.
COLOURING AGENT
Yellow Orange 5
Titanium – 77891
dioxide
Flavours are usually limited to chewable & effervescent tablets or other tablets intended to
dissolve in the mouth.
Flavor oils are added to tablet granulations in solvents, are dispersed on clays and other
adsorbents or are emulsified in aqueous granulating agents (i.e. binder).
Sweeteners: - Mainly used in chewable, effervescent & mouth dissolving tablets for
improvement of taste.
e.g. Sugar
(ii) carcinogenic
– it is banned
Co-processed Excipients
These are the mixture of one or more excipients used in combination to improve their
characteristics.
Reduces the number of excipients in a formulation.
Reduces the overall cost and time for processing.