kollicoat ir white

Pharma Ingredients & Services

Technical Information

January 2008Supersedes issue dated April 2007

EMP 040901e-08/ of 12

Kollicoat® IR White

® = Registered trademark of BASF SE Ready-to-use coating for instant-release dosage forms

ContentsPage

1. Intro duc tion 3

1.1 General 3

1.2 Structural formula 3

1.3 Physical form 3

2. Specification and prop er ties 4

2.1 Chemical nature 4

2.2 Physicochemical properties 4

2.3 Properties of aqueous solutions 4

2.4 Film properties 6

3. Application and processing 6

3.1 Applications 6

3.2 Incompatibilities 7

3.3 Processing notes 7

4. Typical formulations 8

4.1 Aspirin instant-release film-coated tablets 8

4.2 Propranolol instant-release film-coated tablets 9

4.3 Vitamin C instant-release film-coated tablets 10

5. Storage conditions 11

6. Stability 11

7. Toxicology 11

8. PBG, PRD Nos. 11

9. Packaging 11

10. Note 11

EMP 040901e-08 January 2008 of 12 Kollicoat IR White

1. Introduction

1.1 General Kollicoat IR White is a ready-to-use coating system based on Kollicoat IR (polyvinyl alcohol-polyethylene glycol graft copolymer) that is very readily redispersible in water. The extremely rapid redispersibility is due to the innovative manufacture of this combination of pigments and polymers. It is used primarily to manufacture film coatings that dissolve in the gastric juices (instant-release coatings).

1.2 Structural formula The recipe is based mainly on the highly flexible film former Kollicoat IR, which has the following structure:

Composition Kollicoat IR 45%-74%Kollidon® VA 64 5%-10%Titanium dioxide 10%-20%Kaolin 10%-20%Sodium lauryl sulfate 1%- 5%

1.3 Physical form Kollicoat IR is a white to off-white, free-flowing powder.


2. Specifications and properties

2.1 Chemical nature Owing to the special manufacturing process for Kollicoat IR White, the fine pigments are embedded in a polymer matrix and therefore unable to separate or agglomerate. The spray-dried powder form and the particle size of approx. 200µm ensure good flowability and redispersibility in water.

2.2 Physicochemical properties Kollicoat IR White can easily be dispersed in water. The viscosity of aqueous dispersions is relatively low (see 2.3 Properties of aequeous suspensions)

Film formation An aqueous dispersion of Kollicoat IR White is cast on a smooth surface. When the water has evaporated, a clear colourless flexible film remains (see 2.4, Film properties).

Specification Test parameter Requirement

Identity (IR) Must comply

Loss on drying (Ph.Eur 2.2.32 105 °C vacuo) max. 5.0%

pH-value ( Ph.Eur 2.2.3; 20% w/w solution in water) 5.0 – 8.5

Viscosity (Brookfield, 20% w/w solution, sp 2 100 rpm, 23°C

50 – 250 mPas

Dispersibility in water (20% w/w residue on 100 µm filter)

max. 2%

Sulphated ash (Ph.Eur 2.4.1; 15 g) 24 – 38%

Acetate (GC) max. 15 000

Vinyl acetate (GC) max. 100 ppm

Residual solvents (Ph.Eur, USP)

Methanol max. 3000 ppm

Ethylene glycol

1,4 dioxane max. 100 ppm

Methyl acetate max. 1000 ppm

Ester value (Ph.Eur 2.5.2) 20 – 70 mg KOH/g

Microbial status (Ph.Eur 5.1.4, cat 3A) Must comply

Analytical procedures (non compendial methods) are supplied upon request.

Pharmacopoeias No monograph on Kollicoat IR has yet been registered in any of the main pharmacopoeias (USP, EP, JP). However, a number of products are currently being tested by the regulatory authorities in Europe, USA und Japan. The remaining components of the system conform to the corresponding monographs in EP, USP and JP.

2.3 Properties of aqueous suspensions

Viscosity The viscosity of aqueous dispersions of Kollicoat IR White increases with the polymer concentration, but remains very low.


Viscosity of aqueous Kollicoat IR White suspensions as a function of polymer concentration (at 23°C)

Viscosity of Kollicoat IR White suspensions as a function of solids concentration

Viscosity of various spray suspensions (20% w/w, 23°C)

Surface tension The surface tension of a 20 % Kollicoat IR White suspension is very low (39.5 mN/m). Good wetting and spreadability are therefore achieved even on lipophilic surfaces.


2.4 Film properties Kollicoat IR White forms smooth, white, highly flexible films that disperse very rapidly in water. Kollicoat IR White films are not tacky and can be readily printed.

Elongation at break of various ready-to-use instant-release films (23°C, 58% r. h.)

Adhesiveness Kollicoat IR White films adhere extremely well to tablet surfaces of varying lipophilic character.

Coating engravings The very low viscosity and excellent wetting and spreading properties ensure that even fine engravings are uniformly coated and no bridging occurs.

3. Application and processing

3.1 Applications Kollicoat IR White can be used in all applications where a readily redispersible, flexible coating is required. • Instant-release coating - Protects against unpleasant taste and odor,

improves appearance, makes tablet easier to swallow, gives distinctive coloring, protects active ingredients (prevents interaction).

The special advantages of Kollicoat IR White are high flexibility, low viscosity and rapid manufacture of coating suspensions. Kollicoat IR White suspensions for spraying on to tablets can be applied with a high solids content, which greatly reduces the coating time and minimizes costs. The high flexibility of the films ensures that they do not crack on the tablets. Kollicoat IR White can be combined with water-soluble dyes, lakes or iron oxides to obtain a particular shade. Water-soluble dyes and dispersible color concentrates are especially easy to use. Kollicoat IR White can also be used together with ready-mix colors (e.g. SepispersTM Dry) to make colored tablets.


3.2 Incompatibilities Ibuprofen can lead to discoloration of Kollicoat IR White coatings when film-coated tablets are stored under light. This yellowing effect is caused by an incompatibility of ibuprofen with kaolin contained in Kollicoat IR White. For ibuprofen tablets we recommend to use Kollicoat IR and titanium dioxide as pigment.

3.3 Processing notes Because of the high flexibility of Kollicoat IR White films, it is not necessary to add a plasticizer. A spray suspension is conveniently prepared as follows: Stir Kollicoat IR White into water and redisperse. The mixer speed should be adjusted so that little or no foam is produced. After stirring for 15 min, Kollicoat IR White is ready for further processing.

The figures clearly illustrate the simple redispersion of Kollicoat IR White.

On account of its much lower viscosity, Kollicoat IR White can be processed in spray suspensions of much higher concentration than other ready-to-use instant-release formulations. This greatly shortens the spraying and processing time in the manufacture of film-coated tablets. Suspensions with a solids concentration of 15 – 30% can be processed without problem.

The high elasticity of Kollicoat IR White ensures that it does not crack on the tablets when they are exposed to varying humidity during storage. The coating system can be applied on all the usual coaters, e.g. horizontal drum coaters, fluidized bed coaters, immersion sword coaters, and coating pans, under the usual conditions for aqueous solutions. The following conditions have produced good results in numerous trials: Inlet air temperature: 50-80°COutlet air temperature: 30-50°CAtomizing pressure: 2-4 barTemperature of spray suspension: 20-70°C

Cleaning The product can very easily be cleaned off equipment with warm or cold water.


4. Typical formulations

4.1 Aspirin instant-release film-coated tablets

Formulation No. P053/01

Composition of tablets 100 mg acetylsalicylic acid, 148.5 mg Ludipress® LCE, 50 mg Avicel® PH 102, 1.5 mg magnesium stearate

Composition of spray suspension The formulation is designed for 6 kg of tablets (tablet weight 300 mg, diameter 9 mm)

Weight [g] Proportion [%]

Spray suspensionKollicoat IR White 209 20Water 836 80

1 045 100

Preparation of spray suspension Spray suspension: Stir the Kollicoat IR White into the specified quantity of water. After 15 min the spray suspension is ready for further processing.

Machine parameters Coating machine Accela-Cota drum coater (24 inch)

Batch size 6 kgInlet air temperature 60°COutlet air temperature 36°CProduct temperature 35°COutlet air flow 410 m3/hAtomizing pressureForming air pressure

2 bar1 bar

Number of spray nozzles 1Spraying rate 30 g/minSpraying time 35 minFinal drying 60°C / 4 minQuantity applied 5 mg/cm2 solids

Tablet properties Core Film-coated tabletAppearance white whiteHardness 67 N 75 NFriability 0% 0%Disintegration time 3:17 [min:s] 3:29 [min:s]


4.2 Propranolol instant-release film tablets


Composition of tablets40 mg propranolol-HCl, 97.5 mg Ludipress, 12.5 mg Kollidon VA 64, 2.5 mg magnesium stearate, 97.5 mg Avicel PH 102

Composition of spray suspension The formulation is designed for 250 kg of tablets (tablet weight 250 mg, diameter 9 mm)

Weight [g] Proportion [%]Polymer suspensionKollicoat IR WhiteWater

Pigment suspension

7 75525 000

18.8060.61

Indigotin lake, E 132 495 1.20Water 8 000 19.39

41 250 100.00

Preparation of spray suspension Polymer suspension:Stir the Kollicoat IR White into the specified quantity of water.

Pigment suspension:Add the indigotin lake to the specified quantity of water and homogenize with a high-shear mixer, e.g. Ultra-Turrax.

Spray suspension:Stir the pigment suspension into the polymer suspension.

Machine parameters Coating machine Driacoater drum coater,Type 900

Batch size 250 kgInlet air temperature 70°COutlet air temperature 45°CProduct temperature 47°CAir flow 4 600 m3/hAtomizing pressure 4 barNumber of spray nozzles 6Spraying rate 700 g/minSpraying time 60 min.Final drying 60°C / 5 minQuantity applied 3.0%

Tablet properties Core Film-coated tabletAppearance white blueHardness 94 N 112 NFriability 0% 0%Disintegration time 5:51 [min:s] 6:02 [min:s]Drug release 10 min: 51% 10 min: 53%

20 min: 99% 20 min: 99%


4.3 Vitamin C instant-release film tablets

Composition of tablets


103.1 mg Vitamin C 97, 180.0 mg Ludipress, 14.4 mg Kollidon VA 64, 5.0 mg Kollidon CL, 2.5 mg magnesium stearate

Composition of spray suspension The formulation is designed for 1 kg of tablets (tablet weight 300 mg, diameter 8.5 mm)

Weight [g] Proportion [%]Polymer suspensionKollicoat IR White 25.872 18.48Water 105.000 75.00

Pigment suspension

Kollicoat IR White

Sicovit Red 30

Water

1.764

1.764

5.600

1.26

1.26

4.00140.000 100.00

Preparation of spray suspension Polymer suspension:

Stir the Kollicoat IR White into the specified quantity of water.

Pigment suspension:

Stir the Kollicoat IR White into the specified quantity of water. Then stir in the color pigment and homogenize with a high-shear mixer, e.g. Ultra-Turrax.

Spray suspension:

Stir the pigment suspension into the polymer suspension.

Machine parameters Coating machine Hi-Coater (Freund Industrial Co.)

Batch size 1 kgInlet air temperature 54 – 57°COutlet air temperature 34 – 35°CAtomizing pressure 1.5 barNumber of spray nozzles 1Spraying rate 5.2 – 5.4 g/minSpraying time 28 minFinal drying 8 min

(outlet air temp. 34 – 40°C)

Quantity applied 3.15%

Tablet properties Core Film-coated tabletAppearance white redHardness 150 N 180 NFriability 0% 0%Disintegration time 5:18 [min:s] 5:06 [min:s]


5. Storage conditions Store at room temperature.

6. Shelf life At least 3 years in the original sealed containers at room temperature.

7. Toxicology A complete toxicological characterization of Kollicoat IR White for application as a pharmaceutical adjuvant has been carried out. A summary of the available data is available on request under Secrecy Agreement.

8. PBG, PRD Nos. PBG: 10 581 609, PRD: 30235578

9. Packaging 120 l plastic drum with PE liner, 30 kg capacity.

10. Note This document, or any answers or information provided herein by BASF, does not constitute a legally binding obligation of BASF. While the descriptions, designs, data and information contained herein are presented in good faith and believed to be accurate, it is provided for your guidance only. Because many factors may affect processing or application/use, we recommend that you make tests to determine the suitability of a product for your particular purpose prior to use. It does not relieve our customers from the obligation to perform a full inspection of the products upon delivery or any other obligation. NO WARRANTIES OF ANY KIND, EITHER EXPRESS OR IMPLIED, INCLUDING WARRANTIES OF MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, ARE MADE REGARDING PRODUCTS DESCRIBED OR DESIGNS, DATA OR INFORMATION SET FORTH, OR THAT THE PRODUCTS, DESIGNS, DATA OR INFORMATION MAY BE USED WITHOUT INFRINGING THE INTELLECTUAL PROPERTY RIGHTS OF OTHERS. IN NO CASE SHALL THE DESCRIPTIONS, INFORMATION, DATA OR DESIGNS PROVIDED BE CONSIDERED A PART OF OUR TERMS AND CONDITIONS OF SALE. January 2008


BASF SE - Care Chemicals Division - Pharma Ingredients & Services - 67117 Limburgerhof - www.pharma-ingredients.basf.com


kollicoat ir white

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