Kollicoat IR White 2

Kollicoat® IR WhiteInstant white for instant release coating.

The Preface2

Not only can tablet coating en-hance 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

Coating tablets is now standard practice for

solid dosage forms in pharmaceuticals and dietary supplements.

Trademarks are owned by BASF Aktiengesellschaft

■ 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

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 fi lm coating:

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

The Preface 3

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, plas-ticizers, 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 fi lm coating of tablets.

Kollicoat® IR White now combi-nes the advantages of Kollicoat® IR with an innovative method of manufacture. Kollicoat® IR White is a rapid dispersible coating sys-tem which produces a coating suspension within 10 to 15 minu-tes. Compared with hydroxypro-pyl methylcellulose (HPMC), Kolli-coat® IR has several advantages:

■ Higher pigment loading capa- city facilitates coloring of the dosage form■ Low viscosity allows for higher concentrations of solids and signifi cantly reduces the processing time■ High solubility in water results in easier cleaning of the equipment■ High fl exibility of the polymers allows engraved tablets to be coated with high quality results

Based on Kollicoat® IR expertise

The Product4

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 approxima-tely 45,000 Daltons. Further addi-tives 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 pharmacopo-eias; however, several products have been submitted for approval to the authorities e. g. in Europe, USA and Japan. The other ingre-dients comply with the respective monographs in the European Pharmacopoeia, United States Pharmacopoeia and the Japa-nese Pharmaceutical Excipients.

The Application

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 suspen-sions 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.

In its function as an instant release fi lm coating, 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)

Faster dispersionswith Kollicoat® IR White

5

Trademark not owned by BASF:Sepisperse™

6 The Formulation

Kollicoat® IR White can be dispersed much

quicker than HPMC-based coating systems.

The processing of Kollicoat® IR White is an easy two-step procedure:

1. Weighing of the necessary amount of coating system and water2. Stirring of the coating suspension for 10 to 15 minutes with a low-shear mixer

Due to the low viscosity of poly-mer 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, fl uidized bed coat-ers, immersion sword coaters and coating pans under normal conditions for aqueous solutions.

0 min

7The Formulation

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

Elongation at break 23 °C/58 % r. h.

Kollicoat® IR White

Main compe-titor A

Main compe-titor B

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40

35

30

25

20

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The product can be very easi-ly cleaned off equipment with warm or cold water.

10 min

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

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41.4

8 The Example

Tablet properties: Core Film-coated tablet

Appearance White PinkHardness 89 N 106 NFriability 0 % 0 %

Propranolol HCl fi lm-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 231 g 17.6 %Sepisperse™ Dry 5520 Red 30 g 2.4 %Water 1,044 g 80.0 %

Machine parameters:

Coating machine Accela Cota 24-inch, perforated drum coater

Batch size 7 kgInlet air temperature 60 °C/140 °FOutlet air temperature 38–43 °C/100–110 °FProduct temperature 39–41 °C/102–106 °FAirfl ow 220 m3/hAtomizing pressure 2 barPattern air pressure 1 barNumber of spray nozzles 1Spraying rate 35 g/minSpraying time 37 minFinal drying 60 °C/140 °F/5 minQuantity applied 3.4 %

9The Example

Preparation of the spray suspension:

Kollicoat® IR White is stirred into the specifi ed 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.

Trademark not owned by BASF:Sepisperse™

SEM of a fi lm-coated tablet (letter A)

500 µm

Examples for colorants approved worldwide.

Color Name E-Number CAS Color index

Blue FD&C No. 1 132 860-22-0 73015Red Sicovit® Red 172 1309-37-1 77491 Alura red/ 129 25956-17-6 16035 FD & C red 40 Carmin 120 – 75470Yellow Sicovit® Yellow 172 51274-00-1 77492 Sunset yellow/ 110 2783-94-0 15985 FD & C yellow No. 6 Brown Sicovit® Brown 172 12227-89-3+ 77491+77499 (yellow and black) 12227-89-3Green Fast Green/ – 2353-45-0 42053 FD & C green No. 3 Green S 142 – 44090

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

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

10 The Overview

■ 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 fl exible fi lms without high amounts of plasti- cizer. The use of plasticizers can cause a number of problems.

■ The spreading behavior of HPMC is poor, which makes it very diffi cult to coat engraved tablets.

Based on these weaknesses, that also apply to other polymers currently used for fi lm coating, there is a strong demand for a new excipient in this application fi eld: Kollicoat® IR White.

So far, the polymer most frequently used in instant release coating

systems is HPMC. However, the use

of HPMC for instant release fi lm coating

has certain drawbacks. These are primarily:

11



The Summary

The major advantages of the product are:

■ Very quickly dispersible in water■ Due to the special method of production used, fi lms 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 benefi ts of Kollicoat® IR in comparison with HPMC also apply to Kollicoat® IR White:

■ High solids concentration can be sprayed, which shortens production time■ High fl exibility of the fi lms■ Easily printable fi lms■ Easy-to-clean equipment with either cold or warm water■ Engraved tablets can be coated with excellent results

BASF AktiengesellschaftG-MEP/ME – Li 554Attn: Dr. Hubertus FolttmannCarl-Bosch-Straße 64D-67117 LimburgerhofGermany

Please send the following information:

■ Technical information on Kollicoat® IR White.

■ Sample of Kollicoat® IR White 0.5 kg.

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

■ Technical information on Kollicoat® Protect.

■ Technical information on Kollicoat® IR.

■ Technical information on Kollicoat® MAE grades.

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

Fax Reply

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

Title/Name

Department

Company

Address

Town

Country

Telephone

Fax

e-Mail

Local contact:

or Headquarters Germany:

+49-621-60-2 86 40

11



The Summary

The major advantages of the product are:

■ Very quickly dispersible in water■ Due to the special method of production used, fi lms 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 benefi ts of Kollicoat® IR in comparison with HPMC also apply to Kollicoat® IR White:

■ High solids concentration can be sprayed, which shortens production time■ High fl exibility of the fi lms■ Easily printable fi lms■ Easy-to-clean equipment with either cold or warm water■ Engraved tablets can be coated with excellent results

BASF AktiengesellschaftG-MEP/ME – Li 554Attn: Dr. Hubertus FolttmannCarl-Bosch-Straße 64D-67117 LimburgerhofGermany









Fax Reply

Please write in block letters.

Thank you.

Reply card

Please apply

postage stamp.

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

Title/Name

Department

Company

Address

Town

Country

Telephone

Fax

e-Mail

Local contact:

or Headquarters Germany:

+49-621-60-2 86 40

AsiaBASF Asia Pacifi c Regional HQPharma Solutions Dr. Danilo MercadoBASF East Asia Regional Headquarters Ltd.45th Floor, Jardine House,No.1 Connaught Place,Central, Hong KongPhone: +852-27311-588Fax.: [email protected]

North AmericaBASF CorporationPharma Solutions Mr. Javier Beeck100 Campus DriveFlorham Park, NJ 07932USAPhone: +1-973-245-6381Fax: [email protected]

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

www.pharma-solutions.basf.com

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

EuropeBASF AktiengesellschaftMEE/HP – J 550 Mr. Peter HoffmannD-67056 LudwigshafenGermanyPhone: +49-621-60-7 69 28Fax: +49-621-60-7 69 [email protected]

South AmericaBASF S.A.Human Fine Chemicals Ms. Vanessa Occhipinti Estrada Samuel Aizemberg, 170709851-550 São Bernardo do Campo – SPBrazilPhone: +55-11-4343-3341Fax: +55-11-4343-2255 [email protected]









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.

■ ExcipientsKollidon® gradesGroup of povidone and copovidone products suitable mainly as tablet binders, crospovidone as tablet disintegrant and dissolution enhancer.Kollidon® SRMatrix sustained release polymer.Ludipress® gradesDirect tabletting aids for faster product develop-ment and speedier processing. Kollicoat® gradesRange of aqueous based fi lm formers, cost effi cient and ecological.

Cremophor® grades and Solutol® HS 15Range of different ethoxylated emulsifi ers and solubilizers suitable for topical, oral and parenteral formulations. Soluphor® P2-pyrrolidone.Lutrol® gradesRange of PEGs (Lutrol® E range) and poloxamers (Lutrol® F range) for a wide variety of pharmaceutical dosage forms.

■ ActivesAnalgesicsAnestheticsAnti-Malarial AgentsAnti-Viral AgentsAppetite SuppressantCentral Nervous SystemCholoretic AgentsDermaticaDesinfectantGastrointestinal SystemRespiratory SystemStimulantsSympathicomimeticaUrinary SystemVaso-ConstrictorsIntermediate

Vitamins

■ Custom Synthesis

■ Value Added

ME

MP

04

09

02

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0

BASF offers more than cGMP quality and supply safety: technical expertise. Our technical service is always at your side. BASF wishes to create a prosperous and sustain-able future with you as our customer – and partner.

BASF AktiengesellschaftFine Chemicals DivisionPharma Solutions67056 LudwigshafenGermany

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

Pharma Solutions by BASF

AsiaBASF Asia Pacifi c Regional HQPharma Solutions Dr. Danilo MercadoBASF East Asia Regional Headquarters Ltd.45th Floor, Jardine House,No.1 Connaught Place,Central, Hong KongPhone: +852-27311-588Fax.: [email protected]

North AmericaBASF CorporationPharma Solutions Mr. Javier Beeck100 Campus DriveFlorham Park, NJ 07932USAPhone: +1-973-245-6381Fax: [email protected]

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

www.pharma-solutions.basf.com

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

EuropeBASF AktiengesellschaftMEE/HP – J 550 Mr. Peter HoffmannD-67056 LudwigshafenGermanyPhone: +49-621-60-7 69 28Fax: +49-621-60-7 69 [email protected]

South AmericaBASF S.A.Human Fine Chemicals Ms. Vanessa Occhipinti Estrada Samuel Aizemberg, 170709851-550 São Bernardo do Campo – SPBrazilPhone: +55-11-4343-3341Fax: +55-11-4343-2255 [email protected]









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.

■ ExcipientsKollidon® gradesGroup of povidone and copovidone products suitable mainly as tablet binders, crospovidone as tablet disintegrant and dissolution enhancer.Kollidon® SRMatrix sustained release polymer.Ludipress® gradesDirect tabletting aids for faster product develop-ment and speedier processing. Kollicoat® gradesRange of aqueous based fi lm formers, cost effi cient and ecological.

Cremophor® grades and Solutol® HS 15Range of different ethoxylated emulsifi ers and solubilizers suitable for topical, oral and parenteral formulations. Soluphor® P2-pyrrolidone.Lutrol® gradesRange of PEGs (Lutrol® E range) and poloxamers (Lutrol® F range) for a wide variety of pharmaceutical dosage forms.

■ ActivesAnalgesicsAnestheticsAnti-Malarial AgentsAnti-Viral AgentsAppetite SuppressantCentral Nervous SystemCholoretic AgentsDermaticaDesinfectantGastrointestinal SystemRespiratory SystemStimulantsSympathicomimeticaUrinary SystemVaso-ConstrictorsIntermediate

Vitamins

■ Custom Synthesis

■ Value Added

ME

MP

04

09

02

e-0

0

BASF offers more than cGMP quality and supply safety: technical expertise. Our technical service is always at your side. BASF wishes to create a prosperous and sustain-able future with you as our customer – and partner.

BASF AktiengesellschaftFine Chemicals DivisionPharma Solutions67056 LudwigshafenGermany

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

Pharma Solutions by BASF

Documents

Kollicoat IR White 2