

Pharmaceutical Film
Coating Compositions
STAGES OF SUGAR COATING
Uncoated core
Sugar coating is a multi-stage
process:
Sealing
Each stage is divided into
multiple steps, each step
Subcoating involving application of a liquid
system to a continuously
rotating bed of tablets. Each
application is followed by a
period of rolling to achieve
Colour coating distribution and then drying to
solidify the coating on the
tablet surface. The step is
then repeated until the desired
characteristics are achieved.
Polishing
SUGAR COATING
Advantages Disadvantages

— Low cost materials — Long process time

— Skilled operators needed

— Simple formulation
— Variable product quality

— Simple equipment — Printing needed for

branding/identification

— Attractive appearance
TRADITIONAL SUGAR COATING
PROCESS
Stage No. of applications Process time, minutes

Sealing 2-6 20 - 60

Subcoating 40 - 80 400 - 800

Smoothing 0 - 10 0 - 100

Colour coating 10 - 30 100 - 300

Polishing 2 20

Total process time 540 - 1,280 minutes

(9 - 21 hours)
TECHNOLOGIES - FILM
COATING

Uncoated Tablet

The application of a thin polymeric membrane

to the surface of a tablet

Film Coated Tablet

TECHNOLOGIES - FILM
COATING
The preferred method!
Advantages
— Thin coating
• ~ 3%, 80µ

— Rapid process Disadvantages

• ~ 90 minutes
— Coating formulation needs to be
— Reproducible quality without high
matched to core characteristics
operator skill
— Easy identification/branding
• via core intagliation
— Coating can be functional
• Modified release
• Improved stability
SUSPENSION PREPARATION - TRADITIONAL
METHOD

Polymer
Plasticizer

Pigment

Solvent
FILM COATING - SHEFFCOAT
CONCEPT

Polymer

Plasticizer

Pigment
SHEFFCOAT

Solvent
SHEFFCOAT RECONSTITUTION
Ideal vessel and stirrer dimensions

h = d

h d s =1/3 d

Stirrer motor - variable

speed 100 - 500 rpm
ds

d
SHEFFCOAT RECONSTITUTION
Method of addition

1. Add powder at the fastest rate at

which it is accepted by the vortex

2. Avoid free powder floating on

the surface

3. Increase stirrer speed if required

to maintain the vortex
IDEAL FILM COATING FORMULATION
 Basic requirements:
 High solids - rapid coating
- fast build-up to protect friable cores

 Low viscosity - easy to pump & atomize

- smooth coating

 High tensile strength - strong coating - good core protection

 Low elastic modulus - avoid problems due to drying stress/brittleness:

● logo bridging

● film peeling

● stress cracking

 High adhesion - avoidance of adhesion related problems:

● logo bridging
● film peeling
IDEAL FILM COATING FORMULATION
 Other desirable properties:

 High opacity - reduced weight gain

- improved tablet-to-tablet colour uniformity
- improved hiding of core defects
- stabilization of light-sensitive actives

 Moisture &/or atmospheric

gas barrier - improved product stability
- packaging cost savings
POLYMERS USED IN FILM-
COATING
Class Polymer

Cellulosics Hydroxypropylmethycellulose (HPMC)

Hydroxypropylcellulose (HPC)
Hydroxyethylcellulose (HEC)
Methylcellulose (MC)
Ethylcellulose (EC)

Vinyls Polyvinylpyrrolidone (PVP)

Polyvinyl alcohol (PVA)
Polyvinylacetatephthalate (PVAP)

Glycols Polyethylene glycol (PEG)

Acrylics Methacrylic acid copolymers (MAC)

 PROPERTIES OF CELLULOSIC
POLYMERS
Effect of HPMC molecular weight (viscosity
type) on solution viscosity
5
HPMC 15 mPa.s
4
Viscosity, log mPa.s

HPMC 5 mPa.s
3 *500 mPa.s

2 HPMC 3 mPa.s

0
0 5 10 15 20
Concentration, % W/W
*Notional upper limit for film coating
PROPERTIES OF CELLULOSIC
COATING FILMS
 POLYMER PERMEABILITY
CHARACTERISTICS
Water and Oxygen Permeability

2.00
g/100 sqr. CM / 24 Hr

1.50
Moisture
Permeability
1.00
Oxygen
Permeability
0.50

0.00
PVA HPC EC HEC HPMC NaCMC
Latex
PLASTICISERS IN FILM
COATING
 Plasticisers are used to reduce the glass transition
temperature of the polymer, making it more flexible:
 Reduce problems related to drying-stress such as logo-
bridging
 Assist in film formation of latex emulsion systems.

 Volatile plasticisers (e.g. propylene glycol) may be lost

during coating and should be avoided.

 Plasticisers may be prone to interactions with other film

and substrate ingredients, resulting in poor stability.
PLASTICISERS IN FILM
Commonly used types
COATING

CLASS EXAMPLES
1. Polyhydric alcohols Propylene glycol
Glycerol
Polyethylene glycols

2. Acetate esters Glyceryl triacetate

(Triacetin)
Triethyl citrate
Acetyl triethyl citrate
3. Phthalate esters
Diethylphthalate
4. Glycerides
Acetylated monoglycerides
5. Oils
Castor oil
Mineral oil
PLASTICISERS IN FILM
COATING

Effects on polymer properties

HPMC 5cP/PEG 400
Tensile Strength (σ), MPa)

50 2.5

Elastic Modulus (E), GPa

40 Elastic Modulus
2
Tensile Strength
30
1.5
20
1
10

0.5
0 5 10 15 20 25
Plasticiser Concentration, % W/W
 PLASTICISERS IN FILM
COATING

NO
PLASTICISER
 COLORANT PROPERTIES AND
FUNCTION

 Improve product appearance.

 Provide opacity
 Enhances product appearance
 Improves product stability

 Aid in product identification.

 Increase suspension solids with minimal

effect on viscosity
 Promote rapid drying/fast processing
COLORANTS USED IN FILM COATING
FORMULATIONS
TYPE EXAMPLES
1. Water soluble dyes FD&C Yellow No.5 (Tartrazine)

FD&C Blue No. 2 (Indigo Carmine)

2. FD&C Aluminum Lakes FD&C Yellow No.5 Lake

FD&C Blue No. 2 Lake

3. D&C Aluminum Lake D&C Yellow No. 10 Lake

D&C Red No 30 Lake

4. Inorganic Pigments Titanium Dioxide

Iron Oxides (Red, Yellow, Black)

5. Natural Colorants Riboflavin, carotenoids, carmine

FACTORS AFFECTING OPACITY OF
PIGMENTED FILM COATINGS

 Light reflected at the polymer/pigment interface

 Light absorption by the pigment

 Light scattering

 Light refraction
 OPACITY: Light reflection at
pigment/polymer interface

[ ]
2
η1 - η2 η1 = Refractive index of pigment
Quantity of light reflected =
η1 + η2 η2 = Refractive index of polymer

η2 Polymer η2

η1 η1
Pigment
particle

Tablet surface Tablet surface

η1 not similar to η2 η1 similar to η2
Standard Color Collection

*contains Iron Oxide

Core Characteristics
 TABLET HARDNESS
GUIDELINES
 In most cases, minimum hardness (or tablet breaking force) should be
8 - 10 kp (11.2 - 14 scu)

300mg tablet weight

Larger tablets require higher hardness values


TABLET FRIABILITY
In all cases, tablets to be film coated
should have a maximum friability value
GUIDELINES
of: 0.5% and preferably < 0.1%

STRESSED FRIABILITY

 Simulates attrition to tablet post-

coating operations
 Determines robustness of finished
dosage form
 Highlights the utility of subcoats
 100 revolutions in a friabilator at 25
rpm, 4 minutes
EFFECT OF TABLET SHAPE
 Mechanical strength of tablet cores
 Uniformity of enteric coatings
 Edge defects resulting in enteric failures
 Quantity of enteric coating necessary for acceptable
performance (prolonged process times)
 Tablet to tablet variation
 Failure to meet release criteria
 TABLET SHAPE:
EFFECT ON FILM UNIFORMITY

Face
Edge

End

Kirk Wilson and Eli Crossman; DDIP, 23(12), 1997

 TABLET SHAPE:
EFFECT ON FILM UNIFORMITY
1.0

0.9

0.8
Normalized Film Thickness

0.7

0.6 Face

0.5 Edge

0.4
End
0.3

0.2

0.1

0.0
Capsule Large oval Small oval Round

Kirk Wilson and Eli Crossman; DDIP, 23(12), 1997

TABLET SHAPE EFFECTS:
STUDY DESIGN
 Aspirin 325mg tablets (400mg total tablet weight)
 Compressed to same tablet breaking force using
Shallow concave
Standard concave
Deep concave
 Coated to a 10% weight gain of MAC in a side-vented
pan
 Sampled at 5, 6, 7, 8, 9, and 10% weight gain for
acid resistance testing
 TABLET SHAPE EFFECTS:
325 mg ASA ACID
RESISTANCE

100
100
% Acid Uptake (2 hours in 0.1N HCl)

Shallow Concave
% Acid Uptake (2 hours in 0.1N HCl)

Shallow Concave
80 Standard Concave
80 Standard Concave
Deep Concave
Deep Concave
60
60

40
40

20
20

0
0
5 6 7 8 9 10
5 6 7 8 9 10
% Theoretical WG Sheffcoat ENT
% Theoretical WG Sheffcoat ENT
TABLET SHAPE EFFECTS: ADDITION OF
SUB-COAT

Shallow Concave Tablets

 TABLET SHAPE EFFECTS: ACID
RESISTANCE

100
100
0.1N

80
hoursinin0.1N

80
325 mg ASA
60
Shallow Concave Tablet
Uptake(2(2hours

60
HCl)
HCl)

40
40
AcidUptake

NoSubcoat
No Subcoat
1%Subcoat
1% Subcoat
20
20
%%Acid

00
55 66 77 88 99 10
10
%%Theoretical
TheoreticalWG
WGSheffcoat
SheffcoatENT
ENT
TABLET SHAPE EFFECTS:
COMPOUND RADIUS
 TABLET SHAPE EFFECTS

Shallow Concave Tablets Shallow Compound Tablets

 TABLET SHAPE EFFECTS :
COMPOUND RADIUS
Shallow Compound Deep Compound
100 100
100 No Subcoat 100 No Subcoat
No Subcoat No Subcoat
1% Subcoat 1% Subcoat
% Acid Uptake (2 hours in 0.1N HCl)

% Acid Uptake (2 hours in 0.1N HCl)

1% Subcoat 1% Subcoat
% Acid Uptake (2 hours in 0.1N HCl)

% Acid Uptake (2 hours in 0.1N HCl)

80 80
80 80

60 60
60 60

40 40
40 40

20 20
20 20

0 0
0 0
5 6 7 8 9 10 5 6 7 8 9 10
5 6 7 8 9 10 5 6 7 8 9 10
% Theoretical WG ShEffcoat ENT % Theoretical WG Sheffcoat ENT
% Theoretical WG ShEffcoat ENT % Theoretical WG Sheffcoat ENT
 Detrimental Effect of Mg
Stearate

 Softer tablets
 Slower dissolution
 Effect on the film adhesion
Film adhesion effect of
Lubricant %
Effect of Mg. Stearate on
Hardness
Effect of Mg. Stearate on
HCTZ dissolution
Hardness and Dissolution
Film Coatings – Process Parameters
 Process Robustness

Objective

 Establish a process which, where possible, runs from start to finish

with minimal need for parameter changes or operator intervention.

 This is only possible where each setup item and process parameter is
optimized.
Side-vented Coating Pan

Drying
Air Duct

Perforated
Pan

Coating
Spray

Tablet
Bed

Exhaust
Plenum
Product Load

 Must be optimal for the machine design and size

─ Exhaust plenum must be fully covered with product
Low tablet load will reduce drying efficiency →
long process
─ Baffles must be fully covered within spray zone
Spraying onto baffles causes low coating
efficiency, picking
─ Low pan load reduces mixing efficiency
Causes tablet-to-tablet color variation →
long process
Intermittent cascade may cause overwetting
 Product Load - Drying
Efficiency
Correct
load

Partial
load
Optimizing Machine Load
Adjustable Exhaust "Shoe"
Product Load - Coverage of
Baffles
Partial Load
Product Load - Coverage of
Baffles
Correct Load
Selection of Correct Pan Speed
 Ideal pan speed depends on
─ Tablet core size and shape
─ Effectiveness of the baffles
─ Pan load
─ Tablet core friability
─ Smoothness/"slip" of tablets and coating
─ Drying speed of coating suspension
─ Drying capacity of coating machine
 Generally - choose the lowest pan speed that gives an even tablet
cascade through the spray zone
 Pan Speed and Uniformity
48” fully perforated
5 rpm 10 rpm pan

Sheffcoat, high
performance film
coating system
applied at
20% solids
concentration

7 minutes elapsed coating time

 Pan Speed and Uniformity

48” fully perforated

5 rpm 10 rpm pan

Sheffcoat applied at
20% solids
concentration

13 minutes elapsed coating time

 Coating Distribution

 Main causes of coating problems, non-uniform distribution of the coating

spray across the tablet bed, may be due to

─ Spray gun design

─ Too few spray guns
─ Spray gun setup
─ Design of the compressed air system
─ Atomization and pattern air pressures
─ Pan load/pan speed
 Spray Gun Design
Three-Port Air Spray Type
Fan width (pattern) control
Atomizing
air Air cap
Operating
air

Needle
Return
stop
spring
Needle
Operating Coating Fluid nozzle
piston suspension
inlet
 Spray Gun Design
Four-Port Air Spray Type
Fan width (pattern) air
Atomizing Air cap
air
Operating
air

Needle
stop Return
spring
Needle
Operating Fluid
piston Coating
suspension nozzle
inlet
Uniformity of Distribution of
Coating Spray
 Uniformity must include distribution of
─ Spray volume
─ Spray droplet size
 Uniformity must be maintained at selected fan width
 Older gun designs are uniform only at narrow fan width
─ More guns needed to cover width of tablet bed
 Newer gun designs offer uniformity at wide fan width
─ Fewer spray guns needed
 Clogging of nozzles interferes with spray uniformity
 Uniformity of Distribution of
Coating Spray
Conventional
Pattern
vs. Ideal
Fan Width
Spray GunsIdeal Gun
Conventional Gun

Circular

Narrow Fan

Wide Fan
 Number of Guns
Ideal vs. Conventional

Narrow Fan
Conventional x 4

Wide Fan
Ideal Gun x 2
Schlick 930
Standard vs. Abc

20 min 35 min 55 min

Coating Distribution - Spray Gun
Setup
 Objective
─ Achieve the most uniform distribution of spray across width of tablet
cascade
─ Spray uniform in both
 Spray volume
 Droplet size

 Parameters
─ Gun design
─ Number of guns
─ Gun-to-gun spacing
─ Gun-to-bed distance
─ Spray fan width
 Spray Gun Setup
Correct Angle to Tablet Cascade

90º

90º angle minimizes spray "bounce", reduces spray drying & increases coating efficiency
Checking Spray Pattern
Checking Spray Pattern
Balancing Gun Flow Rate
Balancing Gun Flow Rate
 Control of Coating Suspension
Flow Rate
 Requirements
─ Accurate reproducible flow rates are essential
─ Preferred pump types
 Peristaltic pumps
 Suitable for all types of coating suspension
 Gear pumps & piston pumps
 May be unsuitable for some polymer dispersion systems

─ Pressure vessels and gravity feed

 Do not provide required degree of control
Control of Coating Suspension Flow Rate
Problems with Multi-gun Systems

E 60 g/min D
40°C 60°C
X R
H Y A
A I I
U 60 g/min R
N
S G
T

E 40 g/min
40°C 60°C D
X R
H Y A
A I I
U 80 g/min
N R
S G
T

Edge
Picking &
Wear
Sticking
Factors Affecting Rate of Drying

Differential Drying
pressure air
quantity

Drying
air
temperature
Exhaust
air
quantity

+ Atomizing air pressure

+ Gun-to-bed distance
 Control & Monitoring of Drying
Process

Tablet bed
temperature
Drying air
temperature

Coating
suspension
flow rate
Exhaust
temperature