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Kollicoat IR
February 2013
Supersedes issue dated February 2010
03_030724e-11/Page 1 of 14
WF-No.: 121971
Page 2 of 14
Kollicoat IR
Contents
Page
1. Introduction
1.1 General
2.3 Specification
3.1 Applications
4. Typical formulations
10
10
11
12
5. Storage conditions
14
6. Stability
14
7. Toxicology
14
8. PRD-No.
14
9. Packaging
14
Page 3 of 14
Kollicoat IR
1. Introduction
1.1 General
O
O
HO
n
n-x
OH
OH
The polymer consists of 75% polyvinyl alcohol units and 25% polyethylene glycol
units. The product also contains approx. 0.3% colloidal silica to improve its flow
properties.
As a result of its structure, the polymer dissolves very readily in acidic, neutral
and alkaline aqueous media. Such aqueous solutions have a comparatively low
viscosity.
Molecular weight
Solubility
Film formation
2.3 Specification
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Kollicoat IR
Kollicoat IR is registered around the world in medicinal products in all relevant regions,
including Europe, Japan and the USA. Comprehensive safety documentation is
available, including non-clinical studies.
Kollicoat IR has received self-affirmed GRAS status as of January 2013. This
status allows its formulation into products for the US dietary supplements market.
Ph.Eur.
USP/NF
PMDA (Japan)
Approved
JPE Listed
IIG listing
Though the viscosity of aqueous solutions of Kollicoat IR increases with the polymer
concentration, yet at a much lower level than that of equivalent solutions, for
instance, cellulose derivatives.
1.OE+04
1.OE+03
1.OE+02
1.OE+01
1.OE+00
10
15
20
25
Polymer concentration in water [%]
Kollicoat IR
HPMC 3 mPas
Kollicoat Protect
PVA
HPMC 6 mPas
30
Kollicoat IR reduces the surface tension of water. This makes aqueous solutions
easy to spray, and the spray droplets exhibit good wetting behavior on the tablet
surface.
Kollicoat IR
Kollicoat IR forms clear colourless films that are enormously flexible and dissolve
very rapidly in water. Kollicoat IR films are not tacky, have a high pigment binding
capacity and can readily be p
rinted. The reduction of the surface tension is specifically
important for the processing in drug layering.
Kollicoat IR has a much higher elongation at break value than cellulose derivatives.
70
60
50
Strain [N/mm2]
Page 5 of 14
40
30
20
10
0
50
100
150
Elongation [%]
200
Kollicoat IR
HPMC 3 mPas
Kollicoat Protect
PVA
HPMC 6 mPas
250
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Kollicoat IR
Kollicoat IR can be used for all applications for which a water-soluble flexible polymer
is required.
The special advantages of Kollicoat IR lie in its enormous flexibility, low viscosity
and rapid rate of dissolution.
Kollicoat IR solutions for spraying onto tablets can be applied with a high solids
content, which greatly reduces the coating time and minimizes costs.
3.2 Processing notes
5080 C
3050 C
1.56 bar
The product can very easily be cleaned off equipment with warm or cold water.
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Kollicoat IR
4. Typical formulations
4.1 Instant release coating Propranolol film-coated tablets
Composition of the tablets
The formulation is designed for 250 kg of tablets (tablet weight 250 mg;
diameter 9 mm)
Weight [g]
Proportion [%]
Polymer solution
Kollicoat IR
6.080
16.0
24.320
64.0
Talc
1.710
4.5
Titanium dioxide
1.140
3.0
570
1.5
4.180
11.0
38.000
100.0
Water
Pigment suspension
Polymer solution:
Stir the Kollicoat IR into the specified quantity of water until it has dissolved.
Pigment suspension:
Vigorously stir talc, Iron Oxide Red and titanium dioxide into the specified quantity
of water and homogenize in a high-shear mixer.
Spray suspension:
Stir the pigment suspension into the polymer solution. To avoid sedimentation
during the spraying process, the mixture must be continuously stirred.
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Kollicoat IR
Batch size
250 kg
70 C
48 C
Product temperature
50 C
Air flow
4400 m3/h
Atomizing pressure
6 bar
Spraying rate
700 g/min
Spraying time
55 min
Final drying
60 C/5 min
Quantity applied
3.8%
Tablet properties
Core
Film-coated tablet
Appearance
White
Red
Hardness
93 N
109 N
Friability
0%
0%
Disintegration time
5:53 [min:s]
5:47 [min:s]
Drug release
10 min: 49%
20 min: 98%
10 min: 54%
20 min: 99%
The formulation is designed for 5 kg of tablets (weight 330 mg; diameter 9 mm)
Proportion [%]
Polymer solution
Kollicoat IR
100.0
19.2
Water
264.0
50.8
Talc
37.4
7.2
Titanium dioxide
18.6
3.6
Water
10.0
19.2
430.0
100
Pigment suspension
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Kollicoat IR
Polymer solution:
Stir the Kollicoat IR into the specified quantity of water until it has dissolved.
Pigment suspension:
Vigorously stir talc and titanium dioxide into the specified quantity of water and
homogenize in a high-shear mixer.
Spray suspension:
Stir the pigment suspension into the polymer solution. To avoid sedimentation
during the spraying process, the mixture must be continuously stirred.
If a certain appearance of the tablet is needed 5 wt% polyethylene glycol 6000 and
Kollidon 17 (at a ratio of 9:1) should be dissolved in water and sprayed after the
spray suspension. The achieved weight gain should be between 0.30.6 mg/cm2.
Machine parameters
Coater
Batch size
5 kg
60 C
39 C
Product temperature
35 C
Air flow
180 m3/h
Atomizing pressure
3 bar
Spraying rate
30 g/min
Spraying time
18 min
Final drying
60 C/4 min
Quantity applied
3 mg/cm2 polymer
Tablet properties
Core
Film-coated tablet
Appearance
White
White
Hardness
116 N
119 N
Friability
0%
0%
Disintegration time
0:58 [min:s]
0:51 [min:s]
Drug release
10 min: 93%
20 min: 92%
10 min: 92%
20 min: 98%
Page 10 of 14
Kollicoat IR
Proportion [%]
27.0
15.0
153.0
85.0
180.0
100.0
Granulation solution
Kollicoat IR
Water
Stir the Kollicoat IR into the specified quantity of water until it has dissolved.
Due to surface effects of Riboflavin, the tracer formulation had to be applied with
a solid matter concentration of only 15%.
Weight [g]
Proportion [%]
Granulation solution
Riboflavin
10.0
Kollicoat IR
5.0
Water
85.0
100.0
Weight [g]
Proportion [%]
Polymer solution
Kollicoat Smartseal30D
50.5
ATBC
(Acetyltributyl citrate)
7.6
(15% based on pol.)
BHT
(Butylated hydroxytoluene)
1.3
(2.5% based on pol.)
DS
(docusate sodium)
1.0
(2.0% based on pol.)
Talc
39.0
1.0
100.0
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Kollicoat IR
Batch size
Coating Pan
FBP
25/30 kg/L
2.53.0 kg/L
Drum speed
18 rpm
7580 C
5568 C
600 m /h
140170
1.2 mm
Spray rate
1.2 mm
5070 ml/min
Atomising pressure
25 ml/min
1 bar
1.6 bar
High drug load could be achieved due to high film elasticity of Kollicoat IR.
4.5 Pore former in sustained release coating Propranolol single unit drug delivery system
Composition of the tablet
Weight [g]
Propanolol HCl
(granulated)
163.2
46.62
Ludipress
136.8
39.08
Kollidon VA 64
25.0
7.14
Kollidon CL
20.0
5.71
3.0
0.85
Aerosil 200
Magnesium stearate
Coating parameters
Result
Proportion [%]
2.0
0.57
Total
350.0
100.0
Parameters
Values
Pan
24 Accela-Cota
Batch size
5 kg
60 C
216 m3/h
Spray rate
30 gm/min
Drying time
5 mins.
Dissolution profile
Propranolol drug delivery systems dissolution graph
Dissolution [%]
Kollicoat SR 30 D (KSR)
+ Kollicoat IR (KIR)
= drug delivery system
100
CORE
KSR/KIR 5:5
KSR/KIR 6:4
KSR/KIR 7:3
KSR/KIR 8:2
80
60
40
20
0
0
12
16
20
24
time [h]
Page 12 of 14
Kollicoat IR
Weight [g]
Proportion [%]
57.5
5.0
1092.5
95.0
1150.0
100.0
Stir the Kollicoat IR into the specified quantity of water until it has dissolved.
Parameter settings
Binder content
in the final granules
3.05.0%
Binder content
in the polymer solution
8.012.0%
Process time
30 minutes
Temperature
Page 13 of 14
Kollicoat IR
Granulator
Set up
Top spray
Nozzle
1.0 mm
Sieve
Batch volume
5L
Batch mass
1150 g
60 C
Air quantity
80110 m3/h
Spray rate
Various
Spray pressure
1.5 bar
Product temperature
Approx. 32 C
Process time
30 minutes
Sieve
800 m
Properties of the granules Kollicoat IR led to much more homogeneous particle size distribution.
1.0
0.8
0.6
0.4
0.2
0.0
16
21
PVP K25
26
16
21
26
PVP K90
16
21
26
Kollicoat IR
125 355 m
> 355 m
Kollicoat IR led to the formation of strongest granules due to the reason that it
offers elasticity as well as plastic deformation.
Result
The peroxide free Kollicoat IR is an efficient binder combining low viscosity of the
polymer solution and strength of the final agglomerates which in turn led to high
tablets hardness.
Page 14 of 14
Kollicoat IR
5. Storage conditions
6.Stability
7.Toxicology
8.PRD-No.
30132288
9.Packaging
20 kg plastic drum
Note