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Aseel Samaro
Definition
Definition according to the BP
Tablets are dosage forms that are circular in
shape with either flat or convex faces and
prepared by compressing the medicament or
mixture of medicaments usually with added
substances
Today, only a few tablet triturate products are available commercially, with
most of these produced by tablet compression.
Since tablet triturates must be readily and completely soluble in water, only
a minimal amount of pressure is applied during their manufacture.
The few tablet triturates that remain are used sublingually, such as
nitroglycerin tablets.
They contain :
antibacterials for the treatment of nonspecific vaginitis
caused by Haemophilus vaginalis
antifungals for the treatment of vulvovaginitis
candidiasis caused by Candida albicans and related
species.
INSTANTLY DISINTEGRATING
OR DISSOLVING TABLETS
Instant-release tablets (rapidly dissolving tablets, or RDTs) are
characterized by disintegrating or dissolving in the mouth within 1
minute, some within 10 seconds
Tablets of this type are designed for children and the elderly or for
any patient who has difficulty in swallowing tablets.
They liquefy on the tongue, and the patient swallows the liquid.
For use, they were simply placed under the tongue to provide
a rapid onset of action for drugs such as nitroglycerin.
Also, they have been used for drugs that are destroyed in the
gastrointestinal tract, such as testosterone, administered
sublingually for absorption to minimize the first-pass effect.
These RDTs are more convenient to carry and
administer than an oral liquid.
Packaging
They are generally packaged in cards or bubble-type
packaging with each individual tablet in its own cavity.
Not withstanding these advantages, there are a
number of disadvantages and difficulties associated
with formulating RDTs, including:
drug loading
taste masking
friability
manufacturing costs
stability of the product
COMPRESSED TABLETS
The physical features of compressed tablets are well
known:
Round, oblong or unique in shape
thick or thin
flat or convex
colored or uncolored
Weight variation
Content uniformity
Thickness
Hardness
Disintegration
Dissolution
The volume of fill is adjusted with the first few tablets to yield the
desired weight and content.
The tablets are assayed and the content of active ingredient in each
of the 10 tablets is calculated assuming homogeneous drug
distribution.
2. Content Uniformity
The degree of pressure affects not only thickness but also hardness of
the tablet; hardness is perhaps the more important criterion since it can
affect disintegration and dissolution.
4. Tablet Hardness and Friability
It is fairly common for a tablet press to exert as little as 3,000 and
as much as 40,000lb of force
All USP tablets must pass a test for disintegration, which is conducted in
vitro using a testing apparatus.
The apparatus consists of a basket and rack assembly containing six open-
ended transparent tubes of USP-specified dimensions, held vertically upon
a 10-mesh stainless steel wire screen.
Tablets must disintegrate within the times set in the individual
monograph, usually 30 minutes, but varying from about 2
minutes for nitroglycerin tablets to up to 4 hours for buccal
tablets.
The system relates combinations of a drug’s solubility (high or low) and its intestinal
permeability (high or low) as a possible basis for predicting the likelihood of
achieving a successful in vivo–in vitro correlation (IVIVC).
Using this system, drugs are placed into one of four categories as
follows:
binders
disintegrants
Lubricants
5. Avoid dustiness , The granulation of toxic materials will reduce the hazard of generation of
toxic dust, which may arise during the handling of the powders.
6. Materials, which are slightly hygroscope, may adhere & form a cake if stored as a powder.
7. Granules, being denser than the parent powder mix, occupy less volume per unit weight.
WET GRANULATION
Wet granulation is a widely employed method for the production
of compressed tablets.
rapid action.
molasses
methylcellulose (3%)
carboxymethyl- cellulose
microcrystalline cellulose.
The degree to which the granules are reduced depends on the size of the
punches to be used.
In general, the smaller the tablet to be produced, the smaller the granules.
Screens of 12- to 20-mesh size are generally used for this purpose.
Sizing of the granules is necessary so that the die cavities for tablet
compression may be completely and rapidly filled by the free-flowing
granulation.
Voids or air spaces left by too large a granulation result in the production
of uneven tablets.
Adding Lubrication and
Blending
After dry screening, a dry lubricant is dusted over the
spread-out granulation through a fine- mesh screen.
calcium stearate
stearic acid
talc,
Technologic advances
now allow the entire
process of granulation to
be completed in a
continuous fluid bed
process, using a single
piece of equipment, the
fluid bed granulator.
The fluid bed granulator performs the following
steps:
(a) preblending the formulation powder, including
o The use of the microwave reduces the drying time considerably, often by
one fourth.
o After adding lubricants and screening, the batch is ready for tablet
formation or capsule filling.
Advantages of wet
granulation
Advantages
Reduced segregation of formulation components
during storage and/or processing
Disadvantages
1. Often several processing steps are required
of the solvent
The drug may be soluble in the granulation
fluid
Heat is required to remove the solvent
DRY GRANULATION
Glidants, such as
fumed silicon dioxide
Advantages and disadvantages of
direct compression
Advantages:
1. Low labour input
2. A dry process
3. Fewest processing steps
Disadvantages:
1. Stratification (layers) may occur due to differences in particle size and
bulk density which results poor content uniformity.
2. A large dose drug may cause problem in direct compression. It requires
diluents. The tablet becomes large in size which is difficult to swallow
and also costly.
3. During handling of dry materials static charge may form which may
present uniform distribution of drug.
4. Direct compression diluent may interact with the drug. For example,
amine drug with Lactose produce discoloration of tablet
WET GRANULATION DRY GRANULATION DIRECT
COMPRESSION
1. Milling and mixing of drugs 1. Milling and mixing of 1. Milling and
and excipients drugs and excipients mixing of drugs and
excipients
2 .Preparation of binder 2. Compression into slugs or 2. Compression of
solution roll compaction tablet
3. Wet massing by addition of 3. Milling and screening of
binder solution or granulating slugs and compacted
solvent powder
4. Screening of wet mass 4. Mixing with
disintegrant/lubricant
5. Drying of the wet granules 5. Compression of tablet
6. Screening of dry granules
7. Blending with disintegrant /
lubricant and
8. Compression of tablet
Compression process
Compression: The upper punch descends and enters the die and the powder
is compressed until a tablet is formed. During the compression phase, the
lower punch can be stationary or can move upwards in the die. After
maximum applied force is reached, the upper punch leaves the powder
Ejection: During this phase, the lower punch rises until its tip reaches the
level of the top of the die. The tablet is subsequently removed from the
die and die table by a pushing device.
Tablet compression machine
1. Hopper for holding and feeding granulation to be compressed
6. Tablet ejector
Tablets Defects
Lamination
Cappin
Sticking &
g
Picking
Chippin
g
Reason:
1. Air - entrapment during compression
2. Too much of hydrophobic lubricant e.g.: Magnesium-stearate
3. Rapid decompression
3. Sticking & Picking
Sticking is one of the most common problems of tablet making. It occurs when granules
attach and stick to the faces of the punches instead of locking together to create a uniform
tablet.
Picking is a specific type of sticking in which particles stick within the letters and logos that
are embossed or debossed on the faces of the compression tooling
Solvent
Environmental
Safety
Financial
Solvent residues
Film-coating solutions may be nonaqueous or aqueous.
8. A volatile solvent to allow the spread of the other components over the tablets
while allowing rapid evaporation to permit an effective yet speedy operation.
Example: alcohol mixed with acetone.
One commercial water-based colloidal coating dispersion called
Aquacoat (FMC Corporation) contains a 30% ethyl cellulose
pseudolatex.
4. Diethyl phthalate
LOZENGES
LOLLIPOPS
Chewable tablets
Chewable tablets are pleasant-tasting tablets
formulated to disintegrate smoothly in the mouth
with or without chewing.
Mannitol 812.0mg