Tablet Coating

Tablet Coating

Why coat tablets?

Types of coatings
 sugar coating
 film coating
 press coating (compression coating)

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Tablet Coating

It is the application of a coating material to the exterior of a tablet

with the intention of achieving benefits and properties to the
dosage form over the uncoated ones.
It involves additional steps in the manufacturing process, therefore
increasing the cost of the product.
Reasons for tablet coating

1. Extend shelf life by protection of the ingredients from the

environment (light, moisture and oxidation).

2. Coating provides an efficient sealing of the tablet cores

as a method of taste masking for drugs that have bitter or
unpleasant taste.

3. Tablets that are coated are somewhat easier to swallow

than uncoated tablets (significant for large tablets).

4. Coloured coatings mask any batch differences in the

appearance of raw materials (patient concern).
Reasons for tablet coating

5. Coloured coatings aid in the rapid identification of product

by the manufacturer, dispensing pharmacist and patient.

6. Coating tablets facilitates their handling on high speed

automatic filling and packaging equipment.

7. Cross contamination is also reduced in the manufacturing

plant, as 'dusting' from tablets is eliminated by coating.
Reasons for tablet coating

8. Functional film coatings are used to impart enteric

or controlled-release properties to the coated
tablet.

9. Coatings may be optimized with respect to

colouration and gloss to aid in their sales appeal or
to reinforce a marketing brand identification.

10. Avoid chemical incompatibilities by incorporating

another drug or adjuvant in the coat or applying
separate granular coating.
Sugar Coating

The traditional method of coating tablets.

It involves the successive application of sucrose-based

solutions to tablet cores in suitable coating equipment.

Conventional panning equipment with manual application of

syrup has been extensively used although more
specialized equipment and automated methods are now
making an impact on the sugar coating process.
Sugar Coating
stages involved:

 sealing of tablet core

 subcoating

 smoothing

 colouring

 polishing

 printing

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Film Coating
Involves spraying a solution of polymer + pigments +
plasticizers onto a rotated, mixed tablet bed to form a
thin, uniform film on tablet surface.

materials
 polymers
 solvents
 plasticizers
 colorants

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Coating Process
coating pans

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The Coating Process

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Film Formation

latex particles dispersed

in aqueous phase

formation of thin film with

water evaporation through film

continuous film

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Coating Process
coating pans
Air Flow

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Coating Process
fluid beds

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Fluidized bed coaters

A B C
Important Processing Parameters
inlet and bed temperatures

relative humidity

atomization air pressure

liquid spray rate

droplet size

drying time

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Stages of Sugar Coating Process

1. Sealing of tablet cores

2. Subcoating
3. Smoothing
4. Colouring
5. Polishing
6. Printing
Sealing

Sugar coating is an aqueous process during which the tablet

cores are thoroughly wetted by syrup applications.

A tablet sealant is therefore applied to protect the tablet cores

during this initial susceptible period from the action of
water.

Tablet sealants are generally water-insoluble polymers or film

formers applied from an organic solvent solution.
Sealing

Examples of tablet sealants include:

 Shellac - very commonly used and is best in combination
with Polyvinyl pyrrolidone (PVP) which prevents hardening
of the polymer on ageing.
 Cellulose acetate phthalate.
 Polyvinyl acetate phthalate.
 Acrylate polymers.
 Zein

over-application of tablet sealants can lead to

disintegration problems
 Subcoating
Sugar coated tablets have a completely smooth profile with
no visible edges remaining from the original tablet core.

Subcoating is applied to build up the tablet size and round the

edges.

To attain this shape the sealed tablet core must be built up to

gain the desired profile. Tablet cores for sugar coating
should have a small edge so as not to make the 'rounding'
process more difficult than it need be.

Biconvex tablets are preferred over flat surfaced tablets.

The process of subcoating is usually performed by

adding bulking agents such as calcium carbonate or
talc to the applied sucrose solutions. A gum such as
acacia is also added to the applied suspension.
Subcoating

Subcoating can be accomplished by two methods:

1. The application of a gum/sucrose solution followed by

dusting with powder and then drying. This routine is
repeated many times until the desired shape is achieved.

2. The application of a suspension of dry powder in the

gum/sucrose solution followed by drying. As above the
procedure is repeatedly performed until the correct shape is
achieved.
Subcoating

The solution used in subcoating is sucrose based and

contains a gum such as gelatin, acacia or starch
derivatives.

The gum will aid in the adhesion of the powder fillers such as
calcium carbonate or talc.

If a coating suspension is used then the solids content is

made as high as possible in order to reduce the drying
time between each application.
Smoothing

After the correct profile has been attained the subcoated

tablets will have a rather rough surface.

The purpose of the smoothing step is to cover and fill in the

imperfections in the tablet surface caused by subcoating.

They are made perfectly smooth by successive applications

of dilute syrup.

The tablets are subjected to drying air after each application.

Colour coating
Nearly all sugar coated tablets are coloured.
There are two groups of colouring substances generally used
in coloured tablet coatings:
 Water soluble dyes
 Water insoluble pigments

Pigments are much more commonly used

Polishing

After color coating the tablets will require a separate

polishing step for them to achieve an attractive
appearance.

The tablets receive one or two applications of a wax

dissolved in an organic solvent.

Usually beeswax or carnauba wax is used.

Printing

The use of indented monograms on sugar coated tablet

cores is not feasible because the considerable
thickness of coating conceals any core markings.

Instead, if identification is required then this can be

accomplished by printing with special edible printing
inks.
Process

Typically tablets are sugar coated by a panning technique.

The most simple form would be a traditional sugar coating

pan with:
 A circular metal pan mounted angularly on a stand.
The pan is 8 to 60 inches in diameter and is rotated on
its horizontal axis by a motor.
 a supply of drying air (preferably of variable
temperature and thermostatically controlled).
 a fan-assisted extract to remove dust and moisture
laden air.
Process
Standard coating pan
Process
Process
Process
 Baffles maybe used to improve the mixing efficiency
of the tablets during coating and thus uniform coating
is ensured (applied in Accela-Cota).

 Perforated pan coaters are efficient drying systems

with high coating capacity, and can be completely
automated for both sugar coating and film coating
processes.
Ideal characteristics of sugar-coated tablets

Sugar-coated tablets should ideally be of a perfectly smooth

rounded contour with even colour coverage.

They are usually polished to a high gloss

Any printing should be distinct, with no smudging or broken print.

Coating faults: splitting of the coat on storage, caused by

inadequate drying during the coating application.
Film Coating

Film coating can be defined as a process in which thin

(in the range of 20 - 200μm) polymer – based
coatings are applied on to appropriate drug-
containing cores that can be either tablets, beads,
granules, capsules or drug powders and crystals.

It is possible to utilize conventional panning equipment

but more specialized equipment are usually used with
advantages of fast coating times and high degree of
automation involved.
Film Coating

The coating liquid (solution or suspension) contains

a polymer in a suitable liquid medium in addition to
pigments and plasticizers. This solution is sprayed
on to a rotating, mixed tablet bed or fluid bed. The
drying conditions permit the removal of the solvents
so as to leave a thin deposition of coating material
around each tablet core.
Film Formation

The film formation process is the most important step in

the production of coated dosage forms since the
performance of these dosage forms depends mainly
on the quality of the films deposited on the surfaces
of the pharmaceutical substrates.

Polymeric films can be produced from organic solutions

of polymers or from aqueous pseudolatex colloidal
dispersions of polymer particles.
Film Formation
The formation of film coatings from an organic solvent-
based polymer solution involves:

 Spraying of the coating solution onto a suitable substrate.

 The wetting and deformation of the sprayed droplets.
 The entanglement of the polymer chains.
 As the solvent evaporates, the polymer gels.
 With further loss of solvent a continuous film is produced.
Film Formation

The formation of films from a pseudolatex system

involves:
 A film-forming polymer latex being deposited from an
aqueous colloidal dispersion of discrete polymer spheres.
 Individual submicron-size spheres (0.1-0.2 μm), each
containing hundreds of polymer chains, coalesce into a
continuous film as the aqueous phase evaporates.
 The polymer spheres in the latex dispersion are suspended
and separated by electrostatic repulsion.
Film Formation
Film Formers
A variety of polymers have been used in film coating for
different purposes.
Some of these polymers may be applied to improve the
product appearance, enhance stability, improve
handling properties or for taste masking.
Such coatings are usually described as non – functional
film coatings because they do not interfere with the
drug release properties of the drug containing cores.
Film Formers

Different classes of polymers can be used for non-

functional coating of solid dosage forms including:
 Cellulose derivatives (Hydroxypropyl Methylcellulose HPMC,
Hydroxypropylcellulose HPC, Hydroxyethylcellulose HEC,
Methylcellulose MC, Ethylcellulose EC, Sodium
carboxymethylcellulose NaCMC)
 Vinyls (Polyvinyl pyrrolidone, PVP)
 Glycols (Polyethylene glycols, PEG’s)
 Acrylic polymers (Dimethylaminoethyl methacrylate –
methylacrylic acid ester copolymer, Ethylacrylate –
methylmethacrylate copolymer).
 Most of these polymers are water – soluble, however water
insoluble polymers (EC and some acrylate derivatives) can
be used at low polymer loading levels as non-functional
coatings.
Film Formers

Other polymers can be used to modify the release of

the active ingredient from the drug – containing
cores. In such a case the coating is described as a
functional coating.
Modified release dosage forms are classified by the
USP into two types:
1. Extended release: One that permits at least a twofold
reduction in the dosing frequency as compared to the
situation in which the drug is presented as a conventional
dosage form.
2. Delayed release: One that releases the active ingredient
at some time other than promptly after administration
(enteric coated products for example).
Film Formers

Different types of polymers can be used to produce either

type of modified release coated dosage forms.
Enteric polymers can be either
 Natural polymers (Shellac)
 Cellulosic (Cellulose Acetate Phthalate CAP, Cellulose Acetate
Trimellitate CAT, Hydroxypropyl Methylcellulose Phthalate HPMP,
Hydroxypropyl Methylcellulose Acetate Succinate HPMAS)
 Acrylic (Poly (Methacrylate – Ethylacrylate) 1:1, Poly (Methacrylic acid –
methyl methacrylate) 1:1)
Polymers used in extended release film coating include
 Natural polymers (Zein),
 Cellulosic polymers (Ethylcellulose)
 Silicone elastomers
 Acrylic esters.
Plasticizers

Plasticizers are usually high – boiling point organic

solvents that are used to impart flexibility to the
otherwise hard or brittle polymeric materials.

Plasticizers generally cause a reduction in the cohesive

intermolecular forces along the polymer chains
resulting in various changes in polymer properties,
such as reduction in tensile strength, increase in
flexibility and reduction of polymer Tg therefore
enhancing the coalescence process and improving
the integrity of the coat.
Plasticizers
With aqueous colloidal polymer dispersions, the
addition of plasticizers is required for polymer
dispersions having a minimum film formation
temperature (MFT) above the coating temperature.

During plasticization, the plasticizer will diffuse into and

soften the polymeric particles thus promoting particle
deformation and coalescence into a homogeneous
film.
 Plasticizers

Water soluble: Glycerin, propylene glycol, low molecular

weight polyethylene glycols (PEG 200 and 400).
Triethyl citrate (Citroflex®) and surfactants such as
Tweens.

Water insoluble: Acetyl triethyl citrate (ATEC), Acetyl

tributyl citrate (ATBC), Dibutyl phthalate (DBP),
Dibutyl sebacate (DBS), Diethyl phthalate (DEP),
Tributyl citrate (TBC).
Plasticizers
Water insoluble: Oils such as oleic acid, caster oil and
coconut oil. Surfactants such as Spans and Myvacet
(acetylated mono glycerides).

With aqueous polymer dispersions, water-soluble

plasticizers dissolve whereas water-insoluble
plasticizers have to be emulsified in the aqueous
phase of the dispersion.
Pore Formers

Film coats made of impermeable or semi-permeable

polymers may be combined with water-soluble pore
formers such as micronized sucrose, sorbitol,
lactose, NaCl and Calcium phosphate.
Upon contact with dissolution fluids, the pore former
leaches out rapidly to form a multiporous rate-
controlling membrane through which the drug
diffuses in a zero order fashion.
pH dependent pore forming agents are used in enteric
coated substrates.
Colourants

Usually water-insoluble colours (pigments).

Pigments have certain advantages over water-soluble colours: they
tend to be more chemically stable towards light, provide better
opacity and covering power, and optimize the impermeability of
a given film to water vapour.
Examples of colourants:
 Iron oxide pigments.
 Titanium dioxide.
 Aluminium Lakes.
Film Coating

Average
Reconstitution
Description weight Application examples
level
gain
HPMC based Amoxycilli n, Azi thro myci n, Atenolol,
Aqueous 11% to 15% 2.5 % Amlodipine, Amitriptyline, Ampicilin
system Ciprofloxacin, Cephadroxil ,
Cimitidine, C alcium Tablets, Citrizine
HPMC based , Chloroquine Phosphate,
Organic Clarithromyci n, Erythromyci n,
5% 2.5%
solvent Ferrous Fumarate, Famotidine,
system Ferrous Sulphate, Ibu profen,
Ind apamine, Losartan Potassium,
HPMC based Levamisole, Methyl-Dopa,
Aqueous/ Aqueous 11%
Metronidazole+Tinidazole,
Organic Organic Solvent Metronidazole, Methyl Coblamine,
Solvent/ 5% 2.5% Mefenamic Acid, Metoprolol Tartrate,
Hydro Norfloxacin, Nifidipine,
Hydro Alcoholic
Alcoholic Norfloxacin+Tinidazole, Ofloxac in,
9%
system Paracetamol, Quinine Sulphate,
Roxythromyci n, Secnidazole,
PVA based Sildenafil Citrate, Trimetazidine,
Aqueous 20% to 25% 2.5% Tinidazole, Tinidazole-Doxycycli ne,
system Tinidazole + Tetracycli ne, Verapamil

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Enteric-coated
Coating resists dissolution or disruption in stomach but not in
intestines. Used for drugs that are unstable, irritating to stomach

Average
Reconstitution
Description weight Application ** examples
level
gain
Organic Enteric
Coating sys tem, Aspirin, Bisacodyl
5% 8%
Cellulose Acetate
Phtha late based
Diclofenac Sodium
Aqueous c oating
system & Organic
enteric coating Doxyl amine Succinate
Organic: 5%
system. Hydroxy 8%
Aqueous: 10%
Propyl M ethyl
Cellulose Phthalate Garlic Tablets, Omeprazol,
based system. Pentaprazole,

Aqueous 20%
Methacrylic acid Pentoxyfyli ne, Rabeprazol ,
Hydro Alcoholic
copolymer type "C"
10% 9%
USP/NF based
system Organic Sys tem Serrosipeptadise
10%
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Press Coating
Use of compression to form coat around a pre-formed core.
Used mainly to separate chemically incompatible materials
 also dual release patterns possible

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Press Coating

Press coating involves the compaction of granular material around

an already preformed core using compressing equipment similar
to that used for the core itself.

The process was developed originally to serve as alternative for

sugar and film coating in case of a very water-sensitive drugs.

The granular coating material usually contains a high proportion of

sugar to mimic the more conventional sugar coated tablets.
Press Coating

Press coating is also used in the separation of chemically

incompatible materials in tablets (combination tablets).

It is even possible to apply two press coatings where an inert

middle layer separates the active core from the coating.

The press coating also offers potential for having a dual release
pattern.

The use of the process is limited by the relative complexity of the

mechanism used in the compression equipment.
Press Coating

The success of the process depends on the use of:

 Core material that develops reasonable strength at low
compressional loads.
 Coating material in the form of fine free-flowing granules
with good binding qualities.

The coating material is supposed to have a good

particle size distribution with no agglomerates to
produce a stable powder bed that prevents the core
from tilting through the coating material below it.
Coating Problems

picking/chipping

roughness

sticking

film cracking/peeling

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Sticking and Picking

Large droplets on tablet surface are difficult to dry which may lead
to localized overwetting and sticking.

Overwetting or excessive film tackiness causes tablets to stick to

each other or to the coating pan.

On drying, at the point of contact, a piece of the film may remain

adhered to the pan or to another tablet giving a "picked"
appearance to the tablet surface and resulting in a small
exposed area of the core.

A reduction in the liquid application rate or increase in the drying

air temperature and air volume usually solve this problem.

Excessive tackiness may be an indication of a poor formulation.

Sticking and Picking
Roughness
A rough or gritty surface is a defect often observed when the
coating is applied by a spray.

Some of the droplets may dry too rapidly before reaching the tablet
bed resulting in deposits on the tablet surface of "spray dried"
particles instead of finely divided droplets of coating solution or
suspension.

Moving the nozzle closer to the tablet bed or reducing the degree of
atomization (reduce the atomization air pressure to achieve
larger droplets) can decrease the roughness due to "spray
drying."

Surface roughness also increases with pigment concentration and

polymer concentration in the coating solution.
Roughness
Orange-Peel Effect

Inadequate spreading of the coating solution before drying causes

a bumpy or “orange-peel” effect on the coating.
This indicates that spreading is impeded by too rapid drying or by
high solution viscosity.
Large droplet size of highly viscous solutions (ex. HPMC in water)
leads to poor spreading on tablet surface and hence orange
peeling.
In this case higher atomizing air pressure is required to obtain
smaller droplets. Also thinning the solution with additional
solvent may correct the problem.
Orange peeling and roughness affect the visual perception of a
coloured tablet (a rough film will appear lighter and less
saturated in colour compared to a smooth glossy film).
Bridging and Filling

During drying, the film may shrink and pull away from
the sharp corners of a bisect, resulting in a "bridging"
of the surface depression.

This defect can be so severe that the monogram or

bisect is completely obscured. This mainly
represents a problem the formulation.

Increasing the plasticizer content or changing the

plasticizer can decrease the incidence of bridging.
Cracking
Cracking occurs if internal stresses in the film exceed
the tensile strength of the film.

The tensile strength of the film can be increased by

using higher-molecular-weight polymers or polymer
blends.

Internal stresses in the film can be minimized by

adjusting the plasticizer type and concentration, and
the pigment type and concentration.
Colour Variations

Caused by processing conditions or the formulation.

Improper mixing, uneven spray pattern, and insufficient coating
may result in colour variations.
The migration of soluble dyes, plasticizers, and other additives
during drying may give the coating a mottled or spotted
appearance.
The use of lake dyes eliminates dye migration.
A re-formulation with different plasticizers and additives is the best
way to solve film instabilities caused by the ingredients.
THANK YOU

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