Watch the presentation of this webinar here: https://bit.ly/3bJypPv Tablet coating simplified. Finding the perfect coating for your formulation can be challenging. A particle engineered polyvinyl alcohol helps you to optimize your process while maintaining full flexibility in designing the right coating formulation at the right time. In film coating applications water soluble polymers like polyvinyl alcohol (PVA) take a unique position. PVA can be used in immediate release coatings and provides an exceptional moisture and oxygen barrier. A dedicated particle design allows rapid dissolving times and due to the low viscosities of PVA solutions high solid contents can be obtained leading to a high process efficacy. The webinar will cover coating formulation development as well as novel technologies for characterization of coated tablets that can easily be implemented during production. Optical coherence technology (OCT) and laser scanning microscopy (LSM) can be valuable tools to assess the coating quality. In this webinar, you will learn: • How to create your coating formulation by utilizing a broad excipient toolbox • Potential advantages of PVA as a stable moisture and oxygen barrier to protect challenging drug substances • Creating the perfect surface finishing • How to utilize novel analytical technologies to boost your formulation development

1. The life science business of Merck KGaA,
Darmstadt, Germany operates as
MilliporeSigma in the U.S. and Canada.
PARTECK® COAT
When coating runs smoothly:
Enhance your coating process with a new
particle designed PVA
Dr. Thomas Kipping
20.05.2021, Darmstadt

2. The life science business
of Merck KGaA, Darmstadt,
Germany operates as
MilliporeSigma in the U.S.
and Canada

3. Agenda
1
2
3
Tablet film coating
Background & motivation
Parteck® COAT
Key characteristics, coating process & PAT tools
Plasticizer screening
Enhanced screening tools for formulation development
4
Summary
Advantages and future application fields

4. Agenda
1
2
3
Tablet film coating
Background & motivation
Parteck® COAT
Key characteristics, coating process & PAT tools
Plasticizer screening
Enhanced screening tools for formulation development
4
Summary
Advantages and future application fields

5. Reasons to perform tablet coating
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Tablet film coating
Improve the ability to swallow tablets
Mask the taste, odor or color of the drug
Provide physical and chemical protection of the drug
Enhance the physical elegance by use of colorants or pigments
Control the release of the drug from the tablet
Protect the drug from gastric environment of the stomach
with an acid resistant enteric coating
Coating is used to
overcome many
formulation challenges
Coatings help to improve the appearance, stability and therapeutic effect
of a formulation as well as patient compliance

6. Pre-mixed Solutions: Benefits & Limitations
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Tablet film coating
 Ease of use
 Pre-mixed ingredients
 No additional formulation required
 Reduced time for sourcing
 Impression of low price
Reasons for pre-mixed coatings
 Lower formulation know how and
innovation potential
 Limited flexibility
 Prolonged response to regulatory requests
 Limited adaptations in case of incompatibilities
 Increased dependence on supplier
 Low price to be challenged regarding total
manufacturing costs
Associated limitations
Pre-mixed solutions
Main limitations: Increased dependence on supplier and lowered
innovation potential.

7. Preparing your own coating formulation
Tablet film coating
Finishing
 Enhance elegance and optical
perception by adding colorants
or pigments
1
3
2
Polymers
 Film forming ability
 Viscosity in solution
 Enhanced functionality
Plasticizers
 Required to support film
forming ability by reducing the
glass transition temperature
 Concentration is important to
adjust film flexibility and avoid
cracking
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
4
Anti-tacking agents
 Prevent tacking of tablets
during manufacturing process
 Allow a robust process

8. Poll Question 1

9. Agenda
1
2
3
Tablet film coating
Background & motivation
Parteck® COAT
Key characteristics, coating process & PAT tools
Plasticizer screening
Enhanced screening tools for formulation development
4
Summary
Advantages and future application fields

10. What is Parteck® COAT?
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parteck® COAT
 Functional excipient designed for immediate
release coating / protective coating for individual
mixtures
 100 % polyvinyl alcohol 5-88, milled, with specified
medium particle size
 Multi-compendial: pharmaceutical-grade PVA that
surpasses the requirements of all major pharmacopeias
(USP, Ph Eur, ChP, JPE)
 Emprove® qualified product and high purity with
low sulfated ash

11. Dedicated particle technology assures high performance;
high batch-to-batch consistency for high reliability
Product characteristics at a glance
Parteck® COAT
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parameters Ranges
Angle of repose [°] 30 - 35
Bulk density [g/mL] 0.6 - 0.7
Tapped density [g/mL] 0.8 - 0.9
Particle size dV(0.10) [µm] 30 - 120
Particle size dV(0.50) [µm] 180 - 260
Particle size dV(0.90) [µm] 300 - 700
pH value of 4% solution 5.0 - 6.5
Hydrolysis degree [%]: 85 - 89
Mass Average Molar Mass Mw [g/mol] 40,000

12. 2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parteck® COAT
Standard PVA
grade 5-88
HPMC based
polymer 1
HPMC based
polymer 2
Time to dissolve
[Min]
20°C 60 > 240 > 240 > 240
40°C 35 > 240 > 240 > 240
60°C 20 30 > 240 > 240
Preparation of coating liquid with Parteck® COAT
Parteck® COAT
Optimized particle size leads to fast dissolution even at room temperatures.

13. Preparation of coating liquid with Parteck® COAT
Parteck® COAT
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
High
polymer
contents
Low viscosity even at high concentrations of 20% leading to faster
processes & higher efficacy
Effect of polymer concentration on solution viscosity

14. Polymer functionality – thermal behavior
Parteck® COAT
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Optimal range for processing – fine-tuning possible via addition of
plasticizers
Characterization of the thermal behavior of Parteck® COAT (DSC)
Info
 The glass transition
temperature is an important
indicator for the processability
and later film formation

15. Integrating a model compound
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parteck® COAT
Strategy:
 Integrate a model compound into the tablet core formulation to
evaluate a potential influence of the coatings on the release kinetics.
Tablet core formulation: Coating formulation:
Ingredient Amount [%]
Ascorbic Acid 10
Parteck® M 200 87
Silicium dioxide 1
Sodium stearyl fumarate 2
Info
 Ascorbic acid integrated in
tablet cores as model
compound
 Aim:
Evaluate the impact of
different polymer coatings
on the dissolution
behavior
Ingredient Amount [%]
Polymer 70
Triethyl citrate 20
Talcum 10
Amounts related to the solid
content of the spraying liquid;
target weight gain: 3%

16. Immediate release – Protect but don’t delay!
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parteck® COAT
PVA based coating has less influence on release kinetics compared to cellulose
based polymers
Parteck® COAT
Uncoated tablet core
HPMC based coating
T0 2 Min 4 Min 6 Min 8 Min 10 Min 12 Min
T0 2 Min 4 Min 6 Min 8 Min 10 Min 12 Min
T0 2 Min 4 Min 6 Min 8 Min 10 Min 12 Min
Flow cell, 37 °C
5 ml/Min; medium: 0.1N HCl

17. Immediate release – Protect but don’t delay!
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parteck® COAT
PVA based coating has less influence on release kinetics compared to cellulose
based polymers
Release profiles of tablets coated using Parteck® COAT, a cellulose-based polymer or without a coating
Flow cell method, 37 °C
5 ml/Min; medium: 0.1N HCl
Paddle method 50 rpm, 37 °C
900 ml; medium: KH2PO4 buffer pH 2.7

18. Stabilizing sensitive drug substances
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Reliable protection for your sensitive drug substances
Parteck® COAT
Assessment of polymer films prepared via film casting.
Evaluated film thickness: ~ 200 µm
Excellent barrier function
Oxygen transmission rate using an Oxtran 2/21 Oxygen
Permeability Instrument; samples masked to 20 cm2

19.  Optical Coherence Tomography (OCT) supports
scale-up activities by tracking coating parameters
from lab scale up to commercial manufacturing.
 OCT measured subtle differences between the
formulations with respect to
 Coating thickness
 Surface roughness
 Coating structure
Process analytical technology tools for coatings
Parteck® COAT
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
“Combining OCT and our formulation
and excipient expertise, coatings well
suited for future continuous coating
operations can be developed”
Better understanding of coating quality
brings significant benefit in
formulation and process development

20. Poll question 2

21. Agenda
1
2
3
Tablet film coating
Background & motivation
Parteck® COAT
Key characteristics, coating process & PAT tools
Plasticizer screening
Enhanced screening tools for formulation development
4
Summary
Advantages and future application fields

22. 2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
The role of plasticizers
Plasticizer screening
PVA
Plasticizer
Info
The distance between
polymer chains is
controlled by the
nature of the
plasticizer as well as
its concentration

23. Types of plasticizers
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Parteck® COAT
PEG 300
PEG 1000
PEG 3000
PEG 6000
Triethyl citrate
Glycerin
Triacetin
Parteck® SI 150
Polyols
Parteck® M200
Polyethylene glycol

24. Screening method
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Sample preparation
1. Prepare stock solutions of PVA and Plasticizer
2. Fill in 50µl of the coating solution in the DSC Pan
3. Drying over night
4. Measure the weight of the dried material
5. Close the pan
6. Start the DSC measurements
Screening procedure
1. Heating step: 25°C to 110°C at 10 °C/Min
Isothermal at 110°C for 4 Min
2. Cooling step: 110°C to -25°C at 10 °C/Min
Isothermal at -25°C for 2 Min
3. Heating step: -25°C to 250°C at 10 °C/Min
100µl aluminium pan; N2 purge at 50ml/Min

25. Impact of plasticizers
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Polymer Plasticizer
Tg
[°C]
Enthalpy Tg
[J/g]
Melting point
[°C]
Melting enthalpy
[J/g]
Parteck®
COAT No plasticizer 47,63 0,672 169,06 33,66
Parteck®
COAT Triethyl citrate 16,47 0,607 157,79 33,04
Parteck®
COAT Triacetin 13,83 0,628 156,24 56,28
Parteck®
COAT PEG 300 40,04 0,120 165,84 26,97
Parteck®
COAT PEG 1000 21,49 1,159 n.a. n.a.
Parteck®
COAT PEG 3000 n.a.a
n.a.a
172,96 20,77
Parteck®
COAT PEG 6000 n.a.b
n.a.b
175,24 17,15
Parteck®
COAT Glycerin 24,96 0,216 n.a. n.a.
Parteck®
COAT Parteck®
SI 150 45,34 0,232 152,81 14,47
Parteck®
COAT Parteck®
M 200 27,41 0,829 159,23 9,33
Tg overlaps with melting point:
aPEG 3000: 50,96 °C; 28,53 J/g
b PEG 6000: 50,74 °C; 27,77 J/g
Influence of plasticizer on thermal properties (20% w/w)
Triethyl citrate, Triacetin, PEG 1000 and polyols show strong plasticizing effects

26. Effect of different types and concentrations on tablet surface
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Simplified formula: Parteck® COAT + Anti-tacking agent + Plasticizer; amounts linked to the solid content;
concentration of solids in the spraying liquid can vary from 5 up to 20%
Amount [%]
Formulation 1 2 3 4 5 6 7 8 9 10
Parteck® COAT 70 50 70 50 70 50 70 50 70 50
Talc 20 20 20 20 20 20 20 20 20 20
Triethylcitrate 10 30
Glycerol 10 30
Triacetin 10 30
Parteck® SI 150 10 30
Parteck® M 200 10 30
Total 100 100 100 100 100 100 100 100 100 100

27. Effect of different types and concentrations on tablet surface
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
M C
Very good effects on the surface structure provided by Parteck® SI 150,
Parteck® M 200, triethyl citrate, triacetin

28. Effect of different types and concentrations on tablet surface
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Excellent surface finishing using Parteck® SI 150 and Parteck® M 200
as plasticizers.
Topographic maps created via LSM; comparison of
center point images
Conc. Triethyl citrate Glycerol Triacetin Parteck®
SI 150 Parteck®
M 200
10%
30%

29. Effect of different PEG grades on tablet surface
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Composition
Formula 1 Formula 2 Formula 3 Formula 4 Formula 5 Formula 6 Formula 7 Formula 8
Amount [%]
Parteck®
COAT 45 45 45 45 45 45 45 45
Talc 20 20 20 20 20 20 20 20
PEG 200 35
PEG 400 35
PEG 600 35
PEG 1000 35
PEG 1500 35
PEG 3000 35
PEG 4000 35
PEG 6000 35
Total 100 100 100 100 100 100 100 100

30. Effect of different PEG grades on tablet surface
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Topographic maps created via LSM; comparison of
center point images
n=6 n=12
Sweet Spot identified: PEG 1000 provides very homogenous surfaces.
Margin region surface
Central region surface

31. Effect of different PEG grades on tablet surface
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Plasticizer screening
Excellent surface finishing using PEG 1000
PEG 200 PEG 400 PEG 1000
PEG 3000 PEG 4000 PEG 6000

32. Poll question 3

33. Agenda
1
2
3
Tablet film coating
Background & motivation
Parteck® COAT
Key characteristics, coating process & PAT tools
Plasticizer screening
Enhanced screening tools for formulation development
4
Summary
Advantages and future application fields

34. Main benefits of Parteck® COAT at a glance
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Summary
Rapid preparation time
Water-soluble and rapid dissolving
PVA particle, dissolving without
heating, easy to use
Formulation flexibility
Excipients toolbox for coating
formulation development
Excellent surface finishing
Increase the value of your
formulation
Multi-compendial material
compliant with Ph Eur, ChP, JPE, USP
High concentration of
spraying liquid
Reduction of process time,
increase of coating efficacy
Reliable batch-to-batch consistency
supporting reliable reproducibility of
quality and performance of your
final drug product
Stable moisture and oxygen
barrier
Protect your sensitive APIs

35. Coating with Candurin® pigments – let it shine!
Low
opacity
Medium
opacity
High
opacity
Composition solid content [%]
Parteck® COAT 68 66 64
Talcum 10 10 10
Triethyl citrate 20 20 20
Candurin® pigments 2 4 6
Our toolbox for coating formulations
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA

36. Simple replacement of titanium dioxide possible by calcium carbonate
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Titanium dioxide replacement
Our toolbox for coating formulations
Calcium Carbonate
precipitated, EMPROVE®
ESSENTIAL
Article number:
102069
Ingredient Amount [%]
Parteck® COAT 60
Triethyl citrate 20
Talcum 10
Titanium dioxide 10
Ingredient Amount [%]
Parteck® COAT 60
Triethyl citrate 20
Talcum 10
Calcium carbonate 10
Amounts related to the solid
content of the spraying liquid;
target weight gain: 3%

37. Potential Plasticizers Article No
Polyethylene glycol 200 EMPROVE® ESSENTIAL DAB 8 817001
Polyethylene glycol 600 EMPROVE® ESSENTIAL Ph Eur 817004
Polyethylene glycol 1000 EMPROVE® ESSENTIAL Ph Eur
817009
Polyethylene glycol 1500 EMPROVE® ESSENTIAL Ph Eur 817005
Polyethylene glycol 3000 EMPROVE® ESSENTIAL Ph Eur
817019
Polyethylene glycol 4000 EMPROVE® ESSENTIAL Ph Eur
817006
Polyethylene glycol 6000 EMPROVE® ESSENTIAL Ph Eur
817007
Triethyl citrate Ph Eur,JPE,NF. 817059
Triacetin EMPROVE® ESSENTIAL Ph Eur,BP,USP
103000
Parteck® M 100 (Mannitol) EMPROVE® ESSENTIAL Ph
Eur,BP,JP,USP,E 421 100494
Parteck® SI 150 (Sorbitol) EMPROVE® ESSENTIAL Ph
Eur,BP,JP,NF,JSFA,E 420
103583
Glycerol 85% suitable for use as excipient EMPROVE® exp Ph
Eur,BP 104091
Potential Anti-tacking agents Article No
Parteck® LUB MST (MAGNESIUM STEARATE VEGETABLE
GRADE) EMPROVE® ESSENTIAL Ph Eur,BP,JP,NF,FCC
100663
Parteck® LUB CST (Calcium stearate vegetable grade)
EMPROVE® ESSENTIAL Ph Eur,BP,JP,NF,FCC 100664
Parteck® LUB STA 50 (Stearic acid 50 vegetable grade)
EMPROVE® ESSENTIAL Ph Eur,BP,JP,NF 100661
Silicon dioxide colloidal, highly dispersed EMPROVE®
ESSENTIAL Ph Eur,NF,JP,E 551 113126
Pigments (Candurin®) Article No
Candurin® Silver
120600 -
120603
Candurin® Interference
120604 -
120607
Candurin® Gold
120608 -
120610
Candurin® Ironoxide
120613 -
120619
Supporting materials for coatings
Our toolbox for coating formulations
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA

38. Basic coating parameters – enable formulation development
2021-05-20 | When coating runs smoothly: Enhance your coating process with a new particle designed PVA
Parteck® COAT
Exemplary process conditions for lab-scale pan coaters
)Parameter Optimal ranges
Pan load [kg] 1 - 2
Pan size [L] 2.5
Inlet air flow [m3/h] 75
Gun to bed distance [mm] 10 - 15
Inlet air temperature [°C] 70 – 80
Outlet air temperature [°C] 35 – 45
Spraying rate [g/min] 5 – 10
Pan Speed [rpm] 15 – 20
Pattern air pressure [bar] 0.3 – 0.7
Atomizing air pressure [bar] 0.1 – 0.3
Drying temperature [°C] 40 – 50
Tablet coater model used:
Hi-Coater LDCS; Freund-
Vector Corp., Marion, USA)

39. mengyao.zheng@emdgroup.com
thomas.kipping@emdgroup.com
Dr. Mengyao Zheng
Dr. Thomas Kipping
The vibrant M and SAFC are trademarks of Merck KGaA, Darmstadt, Germany or its affiliates. All other trademarks are
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