EXPERIMENT 1  Advantages of Compressed Tablets

o Precision of dosage
MANUFACTURING LABORATORY
o Durability of the physical characteristics for
TABLETS extended periods of storage
o Stability of chemical and physiological
 are solid pharmaceutical dosage forms activities of the drug
containing drug substances with or without o Convenience of administration
suitable diluents and are prepared either by o Portability of carriage and transport
compression or molding.
o Aesthetically appealing
o Molded Tablets
 Properties of Compressed Tablets
o Compressed Tablets
o Ability to withstand the rigors of mechanical
MOLDED TABLETS OR TABLET treatment (production, packaging, shipment,
TRITURATES and dispensing)
o Freedom from defects
 These are usually made from moist material o Reasonable physical and chemical stability
using triturate mold that gives them the shape of during average storage conditions.
cut sections of a cylinder. o Ability to release the medicament in a
 Mixtures of medicinal substances and a diluent reproducible and predictable manner.
usually consisting of lactose (and powdered
sucrose in varying proportions). PRODUCTION OF TABLETS
 The powders are dampened with solutions;
pressed into molds, removed, and allowed to TABLETTING MACHINES
dry.  HOPPER – for storing the granulation
 DISPENSING TABLETS material for compression
o These tablets provide a convenient quantity  FEED FRAME/ FEED SHOE – for
of potent drug that can be incorporated distributing the granulation material into the
readily into powders and liquids die cavities
o These tablets are supplied primarily as a  DIE CAVITIES – for controlling the size
convenience for extemporaneous and shape of the tablets
compounding and should never be dispensed  PUNCHES (upper and lower) – for
as a dosage form. compacting the granulation material within
o Extemporaneously compounded tablets that the die cavities.
are made in small batchers  CAMS – for guiding the punches
 HYPODERMIC TABLETS  FRIABILITY TEST - Test to check a
o These are soft, readily soluble tablets and tablet's resistance to damages when shipped;
were originally used for the preparation of rolling process
solutions to be injected.
TYPES OF TABLETTING MACHINES
COMPRESSED TABLETS
1. SINGLE PUNCH PRESS
 These tablets are formed by the process of  For small scale production
pressing powdered, crystalline or granular  Clockwise of weight adjustment = reduce fill
materials, alone or in combination with weight of tablets; and vice versa
excipients to form a compact adherent mass of
predetermined shape
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  Upper adjust collar determines the position of
the lower punch at the point of ejection of the
finished tablet
 This is consist of a
o Hopper
o Feed shoe
o Weight adjustment collar
o One set of the cavity and punches (upper
and lower) 4. MULTI-LAYER ROTARY TABLET
o Discharge chute MACHINES
o Cam The rotary tablet machines have been developed
o Upper adjustment collar into models capable of producing multiple-layered
tablets. These machines are able to make one, two
or three layered tablets.

2. MULTI-STATION ROTARY TABLET

MACHINES

For increase production output, these machines

offer great advantages. A head carrying a number of TABLET ADDITIVES AND COMPONENTS
sets of dies and punches revolves continuously
Additives or Excipients furnish bulk or volume to
the tablets and are classified according to their
functions as follows:

1. DILUENTS OR BULKING
SUBSTANCES

These are substances that make up the major portion

of the tablet, usually:

1.a. LACTOSE USP

3. HIGH SPEED ROTARY TABLET  most often used because of the following
MACHINES
advantages:
 Faster, more efficient  it is stable and does not react with most
 increasing the number of stations (i.e. sets of
medicinal substances
punches and dies, in each revolution of the  its rapid solubility in water means quick
machine head)
release of the drug substance
 improvement in “feeding” devices
 installation of dual compression points

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  non-hygroscopic and possess a high melting
point, so it is not softened by frictional  Binders - Added in their dry form to the API and
forces of machine compression are activated by WATER or other solvents to
form a slurry or paste
1.b. STARCHES (wheat, corn, rice and potato)  These substances “glue” powders together, and
 they are employed as binders and cause them to form granules.
disintegrants  Examples of raw materials employed as binders
 it contains 12 to 14% water are:
 Amount should be calculated as it can serve o natural gums (acacia, tragacanth)
as a binder (glue) and disintegrates (counter o sugars (sucrose)
glue) o starch gelatin
 Main use is a binder o polyvinyl pyrolidone (PVP) in alcohol
o cellulose derivatives (ethylcellulose,
1.c. SUCROSE
methylcellulose in chloroform)
 Advantage: It is sometimes added to provide o Gelatin- 10-20% solution
additional sweetness, but its’ main use is as o Glucose- 50% solution
a binder because of it’s cohesive property. o Polyvinylpyrrolidone (PVP)- 2% conc.
 Disadvantage: Oxidizes (turns dark brown), o Starch paste-10-20% solution
when it comes in contact with acidic and o Sodium alginate
basic substances. o Sorbitol
 Diluent of choice for chewable tablets

1.d. MANNITOL 3. DISINTEGRANTS

 This another sugar is used for special  These are substances or agents added to
situations, due to its high cost. It as sweet compressed tablets to cause them to “break
and obtained as powder or granules. apart” or disintegrate, when placed in an
 It is extensively used for chewable tablets. aqueous medium.
 Disintegration tester – used to test
1.e. MICROCRYSTALLINE CELLULOSE  Used to oppose the efficiency of binders
(Avicel)  Examples of raw materials employed as
 a very expensive tablet diluents disintegrants are:
o STARCH – the best choice of
1.f. HYDROLYZED STARCH WITH formulators
DEXTROSE (Celutab) o NATURAL GUMS – due to its property
to swell in water
 It’s concentration is 95 to 96%; it contains 4 to
o CELLULOSE DERIVATIVES
5% polysaccharides. It is also used as a base for
chewable tablets due to sweet taste and pleasant (METHOCEL, AVICEL,
“mouth feel” ALGINATES SCMC)
o Starch- 5-20% of tablet weight.
o Starch derivative – PRIMOGEL and
EXPLOTAB (1-8%)
o Clays- VEEGUM HV, BENTONITE
2. BINDERS OR ADHESIVES OR 10% level in colored tablet only
GRANULATING AGENTS o Cellulose
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 o Cellulose derivatives- Ac- Di-Sol (Na o stearates of magnesium and zinc
CMC) o talcum powder (asbestos free)
o Alginate o sodium benzoate
o PVP (Polyvinylpyrrolidone), cross- o mixture of sodium benzoate and sodium
linked acetate
o colloidal silicone dioxide
SUPERDISINTEGRANTS:
o Leucine
 Swells up to ten fold within 30 seconds when o carbowax 400
contact water.  Examples of raw materials employed as
 This are used for sublingual and buccal tablet GLIDANTS are:
 Example: Crosscarmellose- cross-linked o Corn Starch – 5-10% conc.
cellulose, Crosspovidone- cross-linked povidone o Talc-5% conc.
(polymer), Sodium starch glycolate- cross- o Silica derivative
linked starch. o Colloidal silicas such as Cab-O-Sil, Syloid,
 A portion of disintegrant is added before Aerosil in 0.25-3% conc.
granulation and a portion before compression,
which serve as glidants or lubricant. Evaluation 5. COLORING AGENTS
of carbon dioxide in effervescent tablets is also  Helps the consumer to identify if the product is
one way of disintegration fake
 bubble formation – indication that there is  Coloring agents are added to tablet granulations
disintegration happening for the following purposes:
o for improvement of aesthetic appearance
o to provide control of the product during its
manufacturing
o as a means of identification
o The most common method of adding colorant
to a tablet formulation is to dissolve the dye
4. LUBRICANTS OR GLIDANTS OR
in the binding solution, prior to the
ANTI-ADHERENTS
granulation process.
o Another approach is to adsorb the dye on
 These are substances which:
o GLINDANTS - improve the rate flow of starch or calcium sulfate, from its aqueous
solution. The resultant powder is dried and
tablet granulation
appears uniformly blended with other
o prevent adhesion of the tablet, material to
ingredients.
the surface of the dies and punches
o LUBRICANTS - reduce particulate friction COLORANTS
o facilitate the ejection of the tablets from the
die cavities  FD&C – food, drug and cosmetics
o POOR LUBRICATION can be detected by  DYES – water soluble
 LAKES – water insoluble
the “scratch” marks on the edges of the
 FD&C Red No. 2 (amaranth)
tablets; another is the “screeching” sound of
o causes cancer in rats, unproven safety
the machine.
 Examples of raw materials employed as  FD&C Red No. 4
LUBRICANTS are:
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 o found in maraschino cherries and ingested SWEETENING AGENTS
drugs; only used in external drugs and
 For chewable tablets: Sugar, MANNITOL
cosmetics
(diluents choice for chewable tablets)
 FD&C Yellow No. 5 (tartrazine)
 SACCHARIN (artificial): 500 time’s sweeter
o causes allergic type reaction in many people
than sucrose
 D&C RED No. 2 (Eosine)
o Disadvantage: Bitter aftertaste and
 FD&C No. 6 (Sunset yellow)
carcinogenic
 FD&C Blue No. 2 (Brilliant Blue)
 ASPARTAME (artificial)
 FD&C Red No. 4 (allura red)
o Disadvantage: Lack of stability in presence
of moisture.
6. FLAVORING AGENTS
o methyl ester dipeptide of phenylalanine and
 These are substances added to tablet
formulations mainly to “mask” the undesirable aspartic acid
flavor of certain medicaments. o CONTRAINDICATED – phenylketonurics
 especially LOSARTAN
 Examples of raw materials employed as 7. ADSORBENTS
flavoring agents:
o sugars (natural or artificial)  These are substances capable of holding
o essential oils ( peppermint, lemon, quantities of fluids or moisture in an apparently
dry state.
orange, vanilla, strawberry, banana, and
 Examples of raw materials employed as
the likes)
adsorbents
o fruit acids (citric acid, tartaric acid,
o carbonates of magnesium and calcium
malic acid)
o oxides of magnesium and aluminum
FLAVORANTS o kaolin, bentonite
o veegum
 Taste of drug substance itself
o SALT – cinnamon, orange, raspberry, PREPARATION OF TABLET COMPONENTS
butterscotch, maple FOR COMPRESSION
o BITTER - wild cherry, chocolate mint,
licorice I. DRY GRANULATION
o SWEET - fruit, berry, vanilla METHOD
o SOUR OR ACID – citrus
 GRANULATION METHOD IN TABLES –
FLAVORING METHODOLOGY process of transforming the powder into
granules, process of particle enlargement by
 BLENDING – fruit flavors blend with sour aggromeration technique
taste, bitter with salty, sweet and sour  powder – small particles size
 OVERSHADOW – flavor with longer and  granules – when the powder starts to
stronger taste is added to the obvious taste aggromerate
 PHYSICAL – formation of insoluble  samples of moisture sensitive ingredients
compounds of the offending drug o ASA
 CHEMICAL – use of the processes of
o ASCORBIC ACID
adsorption or complexation
o THIAMINE
 PHYSIOLOGICAL - anesthetizing the taste
buds
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  Also called “Pre-compression” or “Double
Compression Method” B. GRANULATION BY COMPRESSION
 This method is applicable to tablet ingredients
that are or have sensitive to moisture This method is adopted for tablets components that
 unable to withstand elevated temperature during are sensitive to heat moisture or both. It is further
drying divided into two methods namely
 sufficient inherent binding or cohesive 1) Slugging by a Tablet Press
properties
 The steps included in the dry method are as  Also similar to dry granulation method
follows:  Granulation by slugging is the process of
o Weighing of ingredients compressing dry powder of tablet formulation
o Mixing of ingredients in a suitable mixer or with tablet press having die cavity large enough
blender in diameter to fill quickly.
o Slugging (poorly formed) by using flat face
punches 7/8 to 1 inch diameter 2) Use of Chilsonator
o Dry screening of slugs through a mesh screen
(by hand) or through a fitzpatrick  It consists of 2 rollers controlled by hydraulic
comminuting mill drums. The tablet materials are fed the hopper to
o Lubrication through a suitable blender the rollers which contain a spiral impeller to de-
o Compression into final tablets aerate the powder.
 Raw material → weighing → Screen → Mixing  After passing the roller, the compacted mass
→ Slugging → Milling → Screening → Mixing resembles a thin cake. The aggregates are
→ Compression formed from the “cake/ thin cake” are screened
to produce the tablet granulation.

II. WET GRANULATION

METHOD
A. DIRECT COMPRESSION
 The most widely used method of tablet
 A few crystalline substance like inorganic salts preparation. Its popularity is due to greater
(NaCl, NaBr and KCl) may be compressed probability that the granulation will meet all the
directly (without any excipients), but majority physical requirements for the compression of
are not easy to tablet. good tablets.
 To remedy this problem, the uses of directly  oldest but produce the best type of tablet
compressible vehicles are advised. These are  ingredients that are not bothered by drying or
inert substances, which may be compacted with moisture
no difficulty, and may do so even when mixed  Disadvantages:
with drugs. o the number of several steps involved
 Examples are DRIED LACTOSE, o it requires longer processing time a
ANHYDROUS LACTOSE, CALCIUM o labor cost is high
PHOSPHATE, MANNITOL, SORBITOL  Steps in the wet method are:
AND AVICEL. o Weighing of the ingredients.
 Raw material → Weighing → Screening →
Mixing → Compression.
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 o Mixing them in a suitable mixer or MO #1 ACETAMINOPHEN TABLET
blender.
Uses of Raw materials
o Granulation into a damp mass by the
addition of a binding solution. 1) Acetaminophen: Antipyretic, analgesic (API)
o Screening the mass by forcing through a
6- or 8- mesh screen. 2) Lactose: Diluent
o Drying in suitable ovens or fluid bed 3) Cornstarch: Binder, disintegrant
dryers.
o Dry screening through smaller mesh 4) Starch paste (10%): Binder
screen.
5) Talc: Lubricant
o Lubrication in a suitable blender.
o Compression into final tablets. 6) Magnesium stearate: Lubricant
 Raw materials → Weighing → Screening →
Method employed: Compression method: Wet
Wet massing → Sieving/Milling → Drying →
granulation
Screening → Mixing → Compression

C. SPECIAL PROCEDURE

1. Spray-drying

 This method consists of bringing together a

highly dispersed liquid and a sufficient volume
of hot air to produce evaporation and drying of
the liquid droplets. Thus forming granules,
ready for compression, after the active
ingredients are mixed in.
 The feed liquid may be a solution, slurry,
emulsion, gel or paste, provided it is
“pumpable” and capable of being atomized

2. Spheronization

 It is a form of pelletization which refers to the

formation of spherical particles from wet
granulations. Since the particles are round, they
have good flow properties, when dried

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