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09/02/2015

UCL SCHOOL OF PHARMACY


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Film Coating
(PHAY 2002)
Dr Min Zhao
Office 210
min.zhao@ucl.ac.uk
10th Feb 2015

UCL SCHOOL OF PHARMACY


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Learning Objectives:
By the end of the lecture, you should be able to:
describe the different types of coating
discuss the different functions of film coating
describe the general coating process

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Lecture Content:

Film coating
What is film coating?
Why film coat?
Film coating ingredients
Film coating process
Drug release from film coats
Testing film coats
Sugar coating
Compression coating
Gelatin coating

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Film coating
What is film coating?

The application of a thin layer of material to the surface of a tablet,


granule or pellet

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Why film coat?


---think about plain tablet

Modifying appearance
To improve appearance

Elegance
Coloured APIs
Mottled tablets
Batch variations

Blinding for clinical trials


If active is coloured/ mottled etc
Placebo and active can be coated to match

Product identification
Brand identity
Product identification
For benefit of pharmacist/ patient/ manufacturer

Psychological reasons
Tablet colour associated with perceived effects
E.g. red/yellow orange associated with stimulated effect; blue and green
assocated with tranquilsing effec
De Craen et al 1996 BMJ

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Taste masking

Stability

Patient acceptability
Blinding for clinical trials
Protection of a drug from the surrounding environment
Moisture barrier coating
Oxygen barrier coatings
Light protective coatings

To confer mechanical strength


To facilitate handling of tablets on production lines
Modifying drug release
Enteric coating
pH sensitive

Extended-release formulations
Site-specific formulations

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Film coating ingredients


(2- 4% of core total weight)

Polymer
A film former capable of producing smooth thin films reproducible
under the prescribed coating conditions.
HMPC (hydroxypropylmethylcellulose) shows good film strength.
HPC (hydroxypropylcellulose) shows good film flexibility.

Plasticizer
Small molecules which interpose themselves on a molecular scale
between polymer stands
Affords flexibility and elasticity to the coat; decrease film brittleness
Modify physical properties of polymers
Lower the glass transition temperature
Polyethylene glycol (PEG), Polypropylene glycol and coconut oil,
diethylphthalate

Colourant/ pigments
In microgram per tablet amounts

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Solvent vehicle
Organic vs aqueous
conc. normally approximately 10 %w/v

Pore-formers
A hydrophilic/ water soluble material dispersed throughout a waterinsoluble coat to facilitate drug release
Only for water insoluble coatings
Water soluble material which provides pores through which drug
release can occur
Starch can also be used
Water swellable

Anti-tack agents

Opacifier

Make the coating less sticky


Titanium dioxide (at 25 to 50 % of polymer weight)
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Film coating process: an overview

Film coating is the deposition of a thin uniform film of polymer


formulation surrounding a tablet/ capsule/ pellet
Polymers are dissolved in organic/ aqueous solution or suspended as
an aqueous suspension

Polymer solution/ suspensions are sprayed through a nozzle under air


pressure which atomises the liquid
Breaks it up into tiny droplets

Meanwhile tablet cores are tumbling/ fluidised in the coater and


exposed to an air inlet of high temperature

Polymer droplets hit the tablet (or pellet) core, the solvent/ water
evaporates
Dried material then remains on the surface of the tablets/ pellets

Droplets build up until a coherent coat has been formed


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Film coating process: mechanisms


Warm air flow
Direction of
rotation of coater
Perforated drum
Tablet bed

Coating suspension

Warm air flow


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Evaporation starts to occur


droplets become more
concentrated

Polymer droplets deposit on


surface and dry. Polymer
chains intermingle and start to
coalesce

Spray

Polymer droplets are sprayed

Coalescence, deformation and cohesion (autohesion) occur


Blue solvent
Red polymer
chain

Tablet core

A coherent
film coat is
formed

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Film coating process: steps in detail

Tablet bed heated up to 35 to 40C and jogged occasionally

Wet droplet sprayed onto a tablet

Droplet spreads over the tablet surface


movement of the tablet in the tablet bed

Droplet spreads between tablets


movement of one tablet over another

Warm air dries the water from the droplet

Continual movement of tablet bed


tablets are well mixed
each tablet receives multiple droplets, building up the coat

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Film coating process: variables

movement of individual tablets

Tablet size / shape


Pan loading
Pan rotation speed
Baffle arrangement

Suspension spray rate


Suspension viscosity
Spray nozzle size

Inlet air temperature tablet bed temperature

droplet size

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Film coating process: critical parameters

Pan speed
Keep tablets tumbling
Spray orientation
Each tablet needs to be exposed to the spray regions
Inlet and outlet air temperature
Too hot and the solution dries before it hits the tablet
Too cold and evaporation does not occur from tablet surface
(making tablet surface sticky)
Pump speed/ spray rate
Atomising air pressure
Controls droplet size and spray
Exhaust facilities to remove dust/ solvents

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Film coating process: monitoring the process

Tablet appearance
colour coverage and depth

Weight gain of tablets


weigh 20 tablets at the start and every 15 minutes
calculate weight gain
may get some dehydration of tablets initially

Weight of suspension used


normally assume 10 to 30 % excess suspension

Tablet bed temperature

Exhaust air temperature


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Problems with film coating

Tablets sticking together


caused by too much water at any one time/not drying fast enough)
causes clumps of tablets/uneven coating

reduce spray rate ( decrease water)


increase suspension concentration ( decrease water)
increase inlet air temperature ( increase drying rate)
increase pan rotation speed ( increase water transfer)
increase tablet curvature ( decrease contact points)
bad

good

good

Poor elegance/rough surface


Coating formulation may need optimisation
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Lack of coherent coating


may need longer time/thicker coating
coat to recommended weight gain

Tablet abrasion
tablet is too friable (eg direct compression formulations)
alter tablet formulation / manufacturing process
tablet has too many points (eg star shape)
alter tablet shape
tablet bed is too heavy (pan perforations act as a
cheesegrater)
reduce pan load
spray a thicker coat initially to give a barrier
reduce the pan rotation speed
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Bridging - In-filling of tablet markings

caused by too much liquid and too deep markings


reduce spray rate
increase inlet air temperature
increase pan rotation speed
change tablet markings (shallower and wider)
in-filling
film coat

tablet core
Good coating

Bad coating
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Core tablet shape is important for film coating


round is best and shaped tablets are bad

good

OK

OK

bad

very bad

very bad

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Film coating process: equipment

http://www.lbbohle.de

http://www.corporate.basf.com
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http://www.vectorcorporation.com/flash/hicoater.html
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http://www.vectorcorporation.com/flash/flocoater.html
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Drug release mechanisms: water soluble coats

Water-soluble polymers (immediate-release)


Dissolution of polymer on reaching stomach fluids
pH-sensitive coating
Polymer becomes ionised and water soluble upon reaching
appropriate pH and dissolves
Active ingredients can incorporated into coats

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Drug release mechanisms: water-insoluble coats

Dissolution through the aqueous pores of an incomplete film

One of the major mechanisms for drug release through a water insoluble
polymer is diffusion through the continuous plasticized polymer phase.

The ingress of water through these pores can also result in osmotically driven
release.

This method assumes that there are molecular sized openings in the film, left by
the cross-linking chains of the polymer, and drug molecules may diffuse through
these, the process being termed hindered molecular diffusion (Ozturk et al.
1990).
These openings must be wetted for this diffusion to occur, and this is aided by
the plasticizer.
Osmotically driven release can also occur by this mechanism

Diffusion through plasticizer channels may also occur

Pore formers can be included

Active ingredients can be incorporated into the coat

This effect becoming increasingly important if the plasticizer concentration is


high
Water soluble materials distributed throughout the coating
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Testing film coats


Properties of a film coat

Quality control

Non-toxic
Soluble in appropriate solvents
Good film former
At an appropriate temperature
Good mechanical strength
Smooth
Coherent coating
No holes
Stable
Does not age

Weight gain of tablets


Ensure same amount of coating is
applied to each tablet
Drug Release
USP/ BSP Specifications for film
coats
Disintegration test (30 mins)
Film coated MR products should
pass appropriate QC dissolution
methods
E.g. T80 / pH specific release
Elegance
Stability
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Sugar coating

Successive application of sucrose solutions to tablet cores


- Sealing of tablet cores
- Water impermeable polymer (e.g. Shellac, cellulose
acetate phthlate, PVAP)
- Subcoating
- Sugar + bulking agents (e.g. calcium carbonate/ talc) +
gum (e.g. acacia)
- Smoothing
-sucrose syrup
- Colouring
- Polishing

-beeswax, carnuba wax


- Printing
Much thicker coating than film coating
Shiny surface
Manipulate taste/ colour easily
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Process of sugar coating

www.glatt.com

Film coating vs Sugar coating


Film coating

Sugar coating

Appearance

Retains contour of original

Rounded, polished appearance

Weight gain

3-5%

50-100%

Process

Single stage

Multiple stages

Functional coating

1.5-2 hours

>8 hours

Can be used for MR

Generally immediate release


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Compression coating

Compressing a granular material around a tablet core


Utilises special tablet presses
Technically difficult
Alignment of coating material and core
Sensitive to irregularities in granule size

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Gelatin coating

Compressed tablet coated with gelatin

Gelatin can be spray coated


Or cold-shrinking of flexible gel caps

To ease swallowing

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Reference
Pharmaceutical Technology: Tableting Technology Volume 2
(Compression) [Hardcover]
Michael H. Rubinstein (Author), James I. Wells (Editor)
Chapter 16 Tabletting
Chapter 22 The strength of pharmaceutical tablets
Chapter 25 Granules structure
Chapter 26 Morphology and strength development in solid and
solidifying interparticle bridges in granules of pharmaceutical powders
Handbook of Powder Technology, Volume 11, 2007, Pages 735-778
Kendal Pitt, Csaba Sinka
Chapter 16 Characterization of Thin Films and Coatings
Handbook of Deposition Technologies for Films and Coatings (Third
Edition), 2010, Pages 749-864
D.R. Baer, S. Thevuthasan
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