Kollicoat Ir White 2

  • October 2019
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Kollicoat® IR White Instant white for instant release coating.

2

The Preface

Coating tablets is now standard practice for solid dosage forms in pharmaceuticals and dietary supplements.

Trademarks are owned by BASF Aktiengesellschaft

Not only can tablet coating enhance shelf life, but research studies show that consumers prefer to swallow a coated tablet rather than an uncoated one. The coating color also enables strong product and brand identity to be achieved and helps patients to

identify the right medication. OTC coated tablets are perceived by consumers to be more effective than uncoated tablets because their appearance is similar to that of prescription drugs. There are also other reasons for applying a film coating:

■ Protection of active ingredients against light and moisture ■ The possibility of printing a logo, dosage etc. on the tablet for easier identification

■ Reduction of friability, which reduces dust formation during packaging ■ Increased mechanical stability during manufacture, packaging and transportation ■ Attractive coatings improve the appearance of tablets and increase patient compliance

The Preface

In most cases coating polymers cannot be used alone in solid oral dosage forms such as tablets, pellets or granules, but have to be used together with further additives. As it is much easier to handle just one mixture of polymers and additives, there is a clear trend toward so-called coating systems. These coating systems comprise polymers, plasticizers, coloring agents and other necessary excipients; these can be stirred into water or an organic

solvent using a low-shear mixer to produce a suspension for film coating of tablets. Kollicoat® IR White now combines the advantages of Kollicoat® IR with an innovative method of manufacture. Kollicoat® IR White is a rapid dispersible coating system which produces a coating suspension within 10 to 15 minutes. Compared with hydroxypropyl methylcellulose (HPMC), Kollicoat® IR has several advantages:

■ Higher pigment loading capacity facilitates coloring of the dosage form ■ Low viscosity allows for higher concentrations of solids and significantly reduces the processing time ■ High solubility in water results in easier cleaning of the equipment ■ High flexibility of the polymers allows engraved tablets to be coated with high quality results

Based on Kollicoat® IR expertise

3

4

The Product

Product form: The basis of Kollicoat® IR White is Kollicoat® IR, which is a graft copolymer consisting of 75 % polyvinyl alcohol units and 25 % polyethylene glycol units with a molecular weight of approximately 45,000 Daltons. Further additives in Kollicoat® IR White include copovidone, titanium dioxide, kaolin, silicon dioxide and sodium lauryl sulfate.

Pharmacopoeia: To date, no monographs for Kollicoat® IR have been published in any of the major pharmacopoeias; however, several products have been submitted for approval to the authorities e. g. in Europe, USA and Japan. The other ingredients comply with the respective monographs in the European Pharmacopoeia, United States Pharmacopoeia and the Japanese Pharmaceutical Excipients.

The Application

In its function as an instant release film coating, Kollicoat® IR White:

Faster dispersions with Kollicoat® IR White

■ Protects against unpleasant taste or odor ■ Covers ingredients’ colors ■ Improves the appearance of the dosage form ■ Makes tablets easier to swallow and increases patient compliance ■ Provides an excellent basis for printing tablets ■ Protects light-sensitive active ingredients ■ Produces a distinctive appearance (coloring)

While Kollicoat® IR can be applied as a ready-to-use clear coat, Kollicoat® IR White is a white coating system which can be sprayed from aqueous suspensions to produce white tablets. Further to this it may also be used together with a color premix (e. g. Sepisperse™ Dry) to produce colored tablets.

Trademark not owned by BASF: Sepisperse™

5

6

The Formulation

Kollicoat® IR White can be dispersed much quicker than HPMCbased coating systems. The processing of Kollicoat® IR White is an easy two-step procedure: 1. Weighing of the necessary amount of coating system and water 2. Stirring of the coating suspension for 10 to 15 minutes with a low-shear mixer

0 min

Due to the low viscosity of polymer solutions, concentrations of solids of up to 30 % can be prepared and sprayed easily. The coating can be applied in all usual coaters, e. g. horizontal drum coaters, fluidized bed coaters, immersion sword coaters and coating pans under normal conditions for aqueous solutions.

The Formulation

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

The following conditions have been used successfully in numerous trials: ■ Inlet air temperature: 50–80 °C (122–176 °F) ■ Outlet air temperature: 30–50 °C (86–122 °F) ■ Atomizing pressure: 2–4 bar

Kollicoat® IR White shows superior mechanical properties compared to competitive products.

Elongation at break 23 °C/58 % r. h.

45

41.4

elongation at break [%]

40 35 30 25 20 15 10 5

0.9

2.6

0 Kollicoat® IR White

Main competitor A

Main competitor B

10 min

7

8

The Example

Propranolol HCl film-coated tablets with a 3.4 % coating level Composition of the spray suspension: The formulation is designed for a batch size of 7 kg of tablets (tablet weight 300 mg; diameter 9 mm).

Kollicoat® IR White Sepisperse™ Dry 5520 Red Water

231 g 30 g 1,044 g

17.6 % 2.4 % 80.0 %

Machine parameters: Coating machine

Accela Cota 24-inch, perforated drum coater

Batch size Inlet air temperature Outlet air temperature Product temperature Airflow Atomizing pressure Pattern air pressure Number of spray nozzles Spraying rate Spraying time Final drying Quantity applied

7 kg 60 °C/140 °F 38–43 °C/100–110 °F 39–41 °C/102–106 °F 220 m3/h 2 bar 1 bar 1 35 g/min 37 min 60 °C/140 °F/5 min 3.4 %

Tablet properties: Core

Appearance Hardness Friability

White 89 N 0%

Film-coated tablet

Pink 106 N 0%

The Example

Preparation of the spray suspension: Kollicoat® IR White is stirred into the specified amount of water in which Sepisperse™ Dry had been dispersed. In order to prevent foam formation, a stirrer with good mixing properties at low/ medium rotation speed should be used. The spray suspension should be stirred during the spraying process to avoid sedimentation of the pigments.

9

As shown in the figure below, Kollicoat® IR White shows excellent properties in coating engraved tablets. No bridging can be observed.

500 µm

SEM of a film-coated tablet (letter A)

Examples for colorants approved worldwide.

The following colorants have been successfully tested together with Kollicoat® IR White as a basis:

Color

Name

E-Number

CAS

Color index

Blue Red

FD&C No. 1 Sicovit® Red Alura red/ FD & C red 40 Carmin Sicovit® Yellow Sunset yellow/ FD & C yellow No. 6 Sicovit® Brown (yellow and black) Fast Green/ FD & C green No. 3 Green S

132 172 129

860-22-0 1309-37-1 25956-17-6

73015 77491 16035

120 172 110

– 51274-00-1 2783-94-0

75470 77492 15985

172

77491+77499



12227-89-3+ 12227-89-3 2353-45-0

142



44090

Yellow

Brown Green Trademark not owned by BASF: Sepisperse™

42053

10

The Overview

So far, the polymer most frequently used in instant release coating systems is HPMC. However, the use of HPMC for instant release film coating has certain drawbacks. These are primarily:

■ Aqueous HPMC solutions have a high viscosity. Thus, HPMC needs to be processed in low concentrated aqueous solutions. This gives rise to long spraying processes and high energy consumption for the evaporation of water. ■ HPMC is a brittle polymer that does not form flexible films without high amounts of plasticizer. The use of plasticizers can cause a number of problems.

■ The spreading behavior of HPMC is poor, which makes it very difficult to coat engraved tablets. Based on these weaknesses, that also apply to other polymers currently used for film coating, there is a strong demand for a new excipient in this application field: Kollicoat® IR White.

Please write in block letters. Thank you.

The Summary

Please apply postage stamp.

Title/Name Department

11 Company Address

The processing of Kollicoat® IR White is an easy two-step procedure: 1. Weighing of the necessary amount of coating system and water 2. Stirring of the coating suspension for 10 to 15 minutes with a low-shear mixer

The major advantages of the product are: ■ Very quickly dispersible in water ■ Due to the special method of production used, films are very homogeneous and smooth ■ As the pigments are embedded in the polymer, no segregation can occur ■ The system is miscible with colorants such as iron oxides or lakes to give colored coatings

All the benefits of Kollicoat® IR in comparison with HPMC also apply to Kollicoat® IR White: ■ High solids concentration can be sprayed, which shortens production time ■ High flexibility of the films ■ Easily printable films ■ Easy-to-clean equipment with either cold or warm water ■ Engraved tablets can be coated with excellent results

Town

Reply card

Country

BASF Aktiengesellschaft G-MEP/ME – Li 554 Attn: Dr. Hubertus Folttmann Carl-Bosch-Straße 64 D-67117 Limburgerhof Germany

Telephone Fax e-Mail

Fax Reply Local contact: or Headquarters Germany:

+49-621-60-2 86 40

Please complete, copy and fax to us, or detach the postcard and send it to us.

Please send the following information:

■ Technical information on Kollicoat® Protect.

■ Technical information on Kollicoat® IR White.

■ Technical information on Kollicoat® IR.

■ Sample of Kollicoat® IR White 0.5 kg.

■ Technical information on Kollicoat® MAE grades.

■ Please contact me, I would like to know more about Kollicoat® IR White.

■ Newsletter “ExAct” (Excipients & Actives for Pharma).

Please write in block letters. Thank you.

The Summary

Please apply postage stamp.

Title/Name Department

11 Company Address

The processing of Kollicoat® IR White is an easy two-step procedure: 1. Weighing of the necessary amount of coating system and water 2. Stirring of the coating suspension for 10 to 15 minutes with a low-shear mixer

The major advantages of the product are: ■ Very quickly dispersible in water ■ Due to the special method of production used, films are very homogeneous and smooth ■ As the pigments are embedded in the polymer, no segregation can occur ■ The system is miscible with colorants such as iron oxides or lakes to give colored coatings

All the benefits of Kollicoat® IR in comparison with HPMC also apply to Kollicoat® IR White: ■ High solids concentration can be sprayed, which shortens production time ■ High flexibility of the films ■ Easily printable films ■ Easy-to-clean equipment with either cold or warm water ■ Engraved tablets can be coated with excellent results

Town

Reply card

Country

BASF Aktiengesellschaft G-MEP/ME – Li 554 Attn: Dr. Hubertus Folttmann Carl-Bosch-Straße 64 D-67117 Limburgerhof Germany

Telephone Fax e-Mail

Fax Reply Local contact: or Headquarters Germany:

+49-621-60-2 86 40

Please complete, copy and fax to us, or detach the postcard and send it to us.

Please send the following information:

■ Technical information on Kollicoat® Protect.

■ Technical information on Kollicoat® IR White.

■ Technical information on Kollicoat® IR.

■ Sample of Kollicoat® IR White 0.5 kg.

■ Technical information on Kollicoat® MAE grades.

■ Please contact me, I would like to know more about Kollicoat® IR White.

■ Newsletter “ExAct” (Excipients & Actives for Pharma).

Please send the following information:

■ Technical information on Kollicoat® Protect.

■ Technical information on Kollicoat® IR White.

■ Technical information on Kollicoat® IR.

■ Sample of Kollicoat® IR White 0.5 kg.

■ Technical information on Kollicoat® MAE grades.

■ Please contact me, I would like to know more about Kollicoat® IR White.

■ Newsletter “ExAct” (Excipients & Actives for Pharma).

■ Excipients Kollidon® grades Group of povidone and copovidone products suitable mainly as tablet binders, crospovidone as tablet disintegrant and dissolution enhancer. Kollidon® SR Matrix sustained release polymer. Ludipress® grades Direct tabletting aids for faster product development and speedier processing. Kollicoat ® grades Range of aqueous based film formers, cost efficient and ecological.

We look forward to answering any questions you may have. Please fill in the postcard, detach it and return it to the address overleaf.

Cremophor ® grades and Solutol® HS 15 Range of different ethoxylated emulsifiers and solubilizers suitable for topical, oral and parenteral formulations. Soluphor ® P 2-pyrrolidone. Lutrol® grades Range of PEGs (Lutrol® E range) and poloxamers (Lutrol® F range) for a wide variety of pharmaceutical dosage forms.

■ Actives Analgesics Anesthetics Anti-Malarial Agents Anti-Viral Agents Appetite Suppressant Central Nervous System Choloretic Agents Dermatica Desinfectant Gastrointestinal System Respiratory System Stimulants Sympathicomimetica Urinary System Vaso-Constrictors Intermediate Vitamins ■ Custom Synthesis ■ Value Added

Pharma Solutions by BASF

Asia BASF Asia Pacific Regional HQ Pharma Solutions Dr. Danilo Mercado BASF East Asia Regional Headquarters Ltd. 45th Floor, Jardine House, No.1 Connaught Place, Central, Hong Kong Phone: +852-27311-588 Fax.: +852-27349-638 mercadd@ basf-east-asia.com.hk

Europe BASF Aktiengesellschaft MEE/HP – J 550 Mr. Peter Hoffmann D-67056 Ludwigshafen Germany Phone: +49-621-60-7 69 28 Fax: +49-621-60-7 69 40 peter.wolfgang.hoffmann@ basf.com

www.pharma-solutions.basf.com

North America BASF Corporation Pharma Solutions Mr. Javier Beeck 100 Campus Drive Florham Park, NJ 07932 USA Phone: +1-973-245-6381 Fax: +1-973-245-6763 javier.beeck@ basf.com

South America BASF S.A. Human Fine Chemicals Ms. Vanessa Occhipinti Estrada Samuel Aizemberg, 1707 09851-550 São Bernardo do Campo – SP Brazil Phone: +55-11-4343-3341 Fax: +55-11-4343-2255 vanessa.occhipinti@ basf.com

BASF Aktiengesellschaft Fine Chemicals Division Pharma Solutions 67056 Ludwigshafen Germany

BASF wishes to create a prosperous and sustainable future with you as our customer – and partner.

■ Fax +49-621-60-2 86 40 ■ [email protected] ■ www.pharma-solutions.basf.com

BASF – the world’s leading chemical company – can look back on well over 140 years of success and has attained an outstanding position as a reliable partner. Our portfolio for the pharmaceutical industry comprises a comprehensive range of major active ingredients and excipient brands as well as exclusive synthesis services.

MEMP 040902e-00

Please contact your local BASF company or one of the following regional centers:

BASF offers more than cGMP quality and supply safety: technical expertise. Our technical service is always at your side.

Please send the following information:

■ Technical information on Kollicoat® Protect.

■ Technical information on Kollicoat® IR White.

■ Technical information on Kollicoat® IR.

■ Sample of Kollicoat® IR White 0.5 kg.

■ Technical information on Kollicoat® MAE grades.

■ Please contact me, I would like to know more about Kollicoat® IR White.

■ Newsletter “ExAct” (Excipients & Actives for Pharma).

■ Excipients Kollidon® grades Group of povidone and copovidone products suitable mainly as tablet binders, crospovidone as tablet disintegrant and dissolution enhancer. Kollidon® SR Matrix sustained release polymer. Ludipress® grades Direct tabletting aids for faster product development and speedier processing. Kollicoat ® grades Range of aqueous based film formers, cost efficient and ecological.

We look forward to answering any questions you may have. Please fill in the postcard, detach it and return it to the address overleaf.

Cremophor ® grades and Solutol® HS 15 Range of different ethoxylated emulsifiers and solubilizers suitable for topical, oral and parenteral formulations. Soluphor ® P 2-pyrrolidone. Lutrol® grades Range of PEGs (Lutrol® E range) and poloxamers (Lutrol® F range) for a wide variety of pharmaceutical dosage forms.

■ Actives Analgesics Anesthetics Anti-Malarial Agents Anti-Viral Agents Appetite Suppressant Central Nervous System Choloretic Agents Dermatica Desinfectant Gastrointestinal System Respiratory System Stimulants Sympathicomimetica Urinary System Vaso-Constrictors Intermediate Vitamins ■ Custom Synthesis ■ Value Added

Pharma Solutions by BASF

Asia BASF Asia Pacific Regional HQ Pharma Solutions Dr. Danilo Mercado BASF East Asia Regional Headquarters Ltd. 45th Floor, Jardine House, No.1 Connaught Place, Central, Hong Kong Phone: +852-27311-588 Fax.: +852-27349-638 mercadd@ basf-east-asia.com.hk

Europe BASF Aktiengesellschaft MEE/HP – J 550 Mr. Peter Hoffmann D-67056 Ludwigshafen Germany Phone: +49-621-60-7 69 28 Fax: +49-621-60-7 69 40 peter.wolfgang.hoffmann@ basf.com

www.pharma-solutions.basf.com

North America BASF Corporation Pharma Solutions Mr. Javier Beeck 100 Campus Drive Florham Park, NJ 07932 USA Phone: +1-973-245-6381 Fax: +1-973-245-6763 javier.beeck@ basf.com

South America BASF S.A. Human Fine Chemicals Ms. Vanessa Occhipinti Estrada Samuel Aizemberg, 1707 09851-550 São Bernardo do Campo – SP Brazil Phone: +55-11-4343-3341 Fax: +55-11-4343-2255 vanessa.occhipinti@ basf.com

BASF Aktiengesellschaft Fine Chemicals Division Pharma Solutions 67056 Ludwigshafen Germany

BASF wishes to create a prosperous and sustainable future with you as our customer – and partner.

■ Fax +49-621-60-2 86 40 ■ [email protected] ■ www.pharma-solutions.basf.com

BASF – the world’s leading chemical company – can look back on well over 140 years of success and has attained an outstanding position as a reliable partner. Our portfolio for the pharmaceutical industry comprises a comprehensive range of major active ingredients and excipient brands as well as exclusive synthesis services.

MEMP 040902e-00

Please contact your local BASF company or one of the following regional centers:

BASF offers more than cGMP quality and supply safety: technical expertise. Our technical service is always at your side.

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