Professional Documents
Culture Documents
By Gamal Shazly
Tablet Coatings
Tablet coating is the application of a coating
material to the exterior of a tablet with the
intention of conferring benefits and properties to
the dosage form over the uncoated variety.
can be
Therapy
To minimise irritation of the oesophagus and stomach.
Minimise inactivation in the stomach.
Improve drug effectiveness.
Improve patient compliance e.g. easier to swallow, masks unpleasant taste.
Technology
Minimise dust formation and contamination with respect to tablets.
Masks batch differences in the appearance of raw materials.
Facilitates their handling on high speed automated filling and packaging
equipment.
Improves drug stability e.g. Protection of active ingredient from
environment such as sunlight, moisture.
Marketing
Aid sales appeal as improved appearance and acceptability with respect to
gloss and colouration.
Mask unpleasant taste.
Sugar coating
Traditionally sugar coatings formed the bulk of coated tablets but today film coatings
are the more modern technology in tablet coating.
Description of tablets: Smooth, rounded and polished to a high gloss.
Process: Multistage process involving 6 separate operations.
1.
2.
3.
4.
5.
6.
Multistage process
1.
2.
Sub coating -by adding bulking agents such as calcium carbonate or talc in
3.
Smoothing process
4.
5.
6.
Colouring
included.
Process details
Typically tablets are sugar coated by a panning technique. The simplest form would
be a traditional sugar-coating pan with a supply of drying air (preferably of variable
temperature and thermostatically controlled) and a fan-assisted extract to remove
dust- and moisture-laden air.
Methods of applying the coating syrup include manually using a ladle, and,
automatic control. In modern equipment some form of automatic control is available
for the application of coating syrups.
Coating faults
These are usually associated with process defects, such as splitting of the
coat on storage, caused by inadequate drying during the coating application.
Film coating
Approach to coating tablets, capsules, or pellets by
polymeric material.
Advantages
Produce tablets in a single step process in relatively short period of time. Process enables
functional coatings to be incorporated into the dosage form.
Disadvantages
There are environmental and safety implications of using organic solvents as well as their
financial expense.
Process:
Single stage process, which involves spraying a coating solution containing the following;
1. Polymer
2. Solvent
3. Plasticizer
4. Colourant
The solution is sprayed onto a rotating tablet bed followed by drying, which facilitates the
removal of the solvent leaving behind the deposition of thin film of coating materials around
each tablet.
Viscosity
The polymers should have a low viscosity for a given concentration. This will
permit the easy, trouble-free spraying of their solutions in industrial film
coating equipment.
Permeability
the polymers should be efficient barriers against the permeability of water
Vapour or other atmospheric gases. These properties vary widely between
the individual polymers.
Mechanical properties
polymer chosen for a film coat formulation must :
Be of adequate strength to withstand the impact and abrasion encountered
in normal handling. Insufficient coating strength will be demonstrated by
the development of cracks and other imperfections in the coating.
comply with the relevant regulatory and pharmacopoeial requirements
current in the intended marketing area.
Examples of the polymers used;
- Cellulose derivatives e.g. MC, HPC, HPMC
- Methacrylate amino ester copolymers.
Examples;
Polyols - Polyethylene glycol 400
Organic esters - diethyl phthalate
Oils/glycerides - fractional coconut oil
Process details
The vast majority of film coated tablets are produced by a process
which involves spraying of the coating material on to a bed of
tablets. Accela Cota is one example of equipment used for film
coating.
Coating faults
These arise from two distinct causes:
1. Processing: for example, inadequate drying conditions will permit coating
previously deposited on the tablet surface to stick against neighbouring
tablets. When parted, this will reveal the original core surface
underneath.
Sugar coating
Tablet appearance
Tablet appearance
Rounded with high degree of polish
Retains shape of original core
Larger weight increase 30-50% due to
Small weight increase of 2-3% due to
coating material
coating material
Logo or break lines are possible
logo or break lines possible
Process
Process
Difficult to automated e.g. traditional coating pan
Can be automated e.g. Accela Cota
Considerable training operation required
Easy training operation
Multistage process
Single stage process
Not able to be used for controlled release
Easily adaptable for controlled release
apart from enteric coating.
allows for functional coatings.
coating pans
fluid beds
PRESS COATING
involves the compaction of granular material around an already preformed
Core using compression equipment similar to that used for the core itself,.
Functional coatings
Functional coatings are coatings, which perform a
pharmaceutical function.
These include;
Controlled release coating
Enteric coating
Multiparticulates (Pellets or Beads), find favor over conventional nondisintegrating tablets for controlled release use, owing to a number of factors:
1. Their small size (typically 0.72.00 mm) allows them to pass through the
constricted pyloric sphincter and distribute themselves along the
gastrointestinal tract. This tends to overcome the disadvantage that whole
tablets have of a rather irregular passage through the gastrointestinal tract
and consequent irregular absorption
3-Should an individual bead or pellet fail and release all of its contents at once the
patient Would not be exposed to any undue risk. This is Certainly not the case if a
non-disintegrating tablet failed, when the consequences would Potentially be
serious
Types of multiparticulate
Extruded/spheroflized granulates
produced in modified granulating equipment , with the drug granulation extruded through
a mesh or other device under pressure to form small granulates which are
subsequently spheronized.
Non-pareilsThese are sucrose spheres which are coated with the drug plus an adhesive
water-soluble polymer (Fig 28.4). After their formation and any necessary intermediate
steps such as drying, they may be coated with the controlled-release coating.
1. Diffusion
On contact with the aqueous fluids of the gastrointestinal tract, water will enter
the interior of the particle by diffusion. Dissolution of the drug will occur and
drug solution will diffuse across the controlled-release coat to the exterior.
2. Erosion
Some coatings can be designed to erode gradually with time, thereby
releasing the drug contained within the pellet.
3. Osmosis
In allowing water to enter, an osmotic pressure can be built up within the
interior of the pellet. drug solution will be forced out of the pellet to the
exterior .
Enteric coating
The technique involved in enteric coating is protection of the tablet core from
disintegration in the acidic environment of the stomach by employing pH sensitive
polymer, which swell or solubilize in response to an increase in pH to release the drug.
The enteric polymers (CAP,PVAP, suitable acrylic derivative ) are capable of
forming a direct film in a film-coating process. Sufficient weight of enteric
polymer must be used to ensure an efficient enteric effect. This is normally two
or three times that required for a simple film coating.