August 2004
Supersedes issue dated January 2004
MEMP 030723e-02/Page 1 of 12
Excipients
s
Contract Manufacturing
Value Added
MEMP 030723e-02 August 2004 Page of 12 Kollicoat® EMM 30 D
Contents
Page
1 Introduction 3
1.1 General Information 3
1.2 Chemical structure 3
1.3 Trivial names 3
1.3 Commercial formulation 3
4 Storage 11
5 Stability 11
6 PBG No. 11
7 Packaging 11
MEMP 030723e-02 August 2004 Page of 12 Kollicoat® EMM 30 D
1 Introduction
1.1 General Information Kollicoat® EMM 30 D is a copolymer based on ethyl acrylate and methyl
methacrylate. It has a neutral character. The polymer is suitable for the produc
tion of sustained-release formulations and transdermal therapeutic systems. It
has a strong, pH-independent sustained-release effect.
Moreover, it can also be used for taste masking.
1.3 Trivial names Polyacrylate dispersion 30% (Ph. Eur.), Ethyl Acrylate-Methyl Methacrylate
Copolymer Emulsion (JPE)
1.4 Commercial formulation Kollicoat® EMM 30 D is an aqueous dispersion with a 30% solids content.
The cloudy white, low-viscosity product has a weak, characteristic odour.
Solubility Kollicoat® EMM 30 D can be mixed with water in any proportion while retaining
its cloudy white appearance. Mixing the product with acetone, ethanol or isopropyl
alcohol at a ratio of 1 : 5 results in a weakly opalescent, viscous solution. When
organic solvents are added, the polymer initially precipitates out; however, it
redissolves on addition of more solvent. Kollicoat® EMM 30 D is not soluble in
diluted alkaline solutions. The cloudy white appearance of the dispersion is preserved.
Film formation When the product is poured out onto a glass plate, a clear film is formed after
evaporation of the water.
Viscosity Viscosity is determined according to DIN EN ISO 3219 at a shear rate of 250 s-1
and 23 °C.
MEMP 030723e-02 August 2004 Page of 12 Kollicoat® EMM 30 D
Coagulate content 100 g of the substance is filtered through a 90 µm screen. The residue is dried
to constant weight in the drying cabinet at 105°.
Microbial status The test of microbial status is carried out according to Ph. Eur., Category 3.
If not specified otherwise, the determination methods are taken from the current
European Pharmacopoeia.
2.3 Pharmacopoeias Kollicoat® EMM 30 D meets the requirements of the monograph Polyacrylate
Dispersion 30% (Ph. Eur.) and Ethyl Acrylate-Methyl Methacrylate Copolymer
Dispersion (JPE).
Kollicoat® EMM is a soft polymer, which makes the use of a plasticizer unnecessary.
The product forms very flexible, extensible films.
The layer thickness should not fall below 1.5 mg/cm2 ( approximately 15 µm),
since otherwise film defects and bursting may be expected.
Kollicoat® EMM 30 D is a polymer with relatively high tack. Auxiliary agents are
necessary to reduce the tack and to improve processing when it is processed as
a coating.
Previously, talc was generally used for this purpose. More recent studies have
shown that the use of fine microcrystalline cellulose or hydroxypropyl methylcellu
lose can greatly reduce the tack. At the same time, the inlet air temperature and
the spraying rate can be increased, which makes it possible to noticeably accel
erate the coating process. At the same time, these substances have the advan
tage that they can also act as a pore-forming agent and give stable release char
acteristics throughout the storage time.
MEMP 030723e-02 August 2004 Page of 12 Kollicoat® EMM 30 D
Influence of various auxiliary agents on release control and tack
Formulation No. 2 is the most suitable because of its very low tack.
3.2 Propranolol sustained-
release pellets
Composition of the pellets: 20% propranolol-HCl, 51.7% Avicel® PH 101, 25.8% lactose,
2.5% Kollidon® VA 64
Composition of the The formulation is designed for 3 kg pellets (diameter 0.7–1.4 mm)
spray suspension
Parts by weight Proportion
[g] [%]
Polymer suspension
Kollicoat® EMM 30 D 895.5 39.3 (11.8 polymer)
Pharmacoat 603 ®
16.1 0.7
Water 501.2 42.5
Pigment suspension
Kollidon® 30 11.4 0.5
Titanium dioxide 11.4 0.5
Sicovit® Red 30 11.4 0.5
Talc 136.7 6.0
Water 694.3 10.0
2278.0 100.0
Pigment suspension:
Spray suspension:
The pigment suspension is introduced into the polymer suspension with stirring.
The mixture must be stirred in order to prevent sedimentation during the spray
ing process.
The coating weight of 3 mg/cm2 in this case was calculated from the surface
area of the above pellets. Since the particle size distribution and the surface
structure influence the required polymer quantity, a calculation of the surface
area is recommended in order to estimate the quantity to be applied.
Release of propranolol sustained-release pellets
MEMP 030723e-02 August 2004 Page of 12 Kollicoat® EMM 30 D
3.3 Ibuprofen sustained-
release pellets
Composition of the pellets: 60.0% ibuprofen, 2.5% Kollidon® VA 64, 37.5% Avicel® PH 101
Composition of the spray The formulation is designed for 2.3 kg pellets (* 0.7–1.5 mm)
suspension
Parts by weight Proportion
[g] [%]
Polymer suspension
Kollicoat® EMM 30 D 540.2 32.50 ( 9.75 polymer)
Pharmacoat 603
®
12.5 0.75
Avicel PH 105
®
74.8 4.50
Water 785.2 47.25
Pigment suspension
Kollidon® 30 8.3 0.5
Titanium dioxide 8.3 0.5
Sicovit Red 30
®
8.3 0.5
Talc 58.2 3.5
Water 166.2 10.0
1662 100.0
As the ibuprofen pellets become highly charged during coating, the coater must
be well earthed.
MEMP 030723e-02 August 2004 Page of 12 Kollicoat® EMM 30 D
3.4 Production of caffeine
sustained-release granules
Composition of the spray The formulation is designed for 500 g granules (diameter 0.6–1.8 mm)
suspension
Parts by weight Proportion
[g] [%]
Polymer suspension
Kollicoat® EMM 30 D 237.25 32.5
( 9.75 polymer)
Pharmacoat 603
®
5.48 0.75
Avicel PH 105
®
32.85 4.50
Water 344.92 47.25
Pigment suspension
Kollidon® 30 3.65 0.5
Titanium dioxide 3.65 0.5
Sicovit Red 30
®
3.65 0.5
Talc 25.55 3.5
Water 73.00 10.0
730.00 100.0
The spray suspension is prepared in the same way as the previous formulation.
MEMP 030723e-02 August 2004 Page 10 of 12 Kollicoat® EMM 30 D
3.5 General notes for the Due to the different solubilities of the active ingredients and the different release
production of a spray rates they give as a result, the choice of pore-forming agent is very important in
suspension the production of spray suspensions. The figures shown in the chart are based
on our experience.
3.6 Additional applications Kollicoat® EMM 30 D can be used as an odour, taste or moisture barrier, or to
protect active ingredients against interaction with other substances (protective
coating, subcoating).
By granulating active ingredients in a fluidized bed, for instance, and subse
quent compressing, it is possible to produce matrix sustained-release tablets.
The production of transdermal systems is also possible.
MEMP 030723e-02 August 2004 Page 11 of 12 Kollicoat® EMM 30 D
5. Stability At least 18 months in the unopened original containers at room temperature.
Under the effects of heat or frost as well as foaming, aqueous dispersions can
form coagulates which make them unsuitable for further use. Since the product
has a neutral pH, care must be taken not to introduce contamination into the
product, due to the risk of microbial growth. Opened containers must be used
up as quickly as possible, or preserved with sodium hypochlorite solution
(5 ppm active chlorine).
Note The data contained in this publication are based on our current knowledge
and experience. In view of the many factors that may affect processing and
application of our product, these data do not relieve processors from carrying
out their own investigations and tests; neither do these data imply any guarantee
of certain properties, nor the suitability of the product for a specific purpose.
Any descriptions, drawings, photographs, data, proportions, weights etc. given
herein may change without prior information and do not constitute the agreed
contractual quality of the product. It is the responsibility of the recipient of our
products to ensure that any proprietary rights and existing laws and legislation
are observed.
August 2004
MEMP 030723e-02 August 2004 Page 12 of 12 Kollicoat® EMM 30 D
BASF Aktiengesellschaft
Fine Chemicals Division - Pharma Solutions - 67117 Limburgerhof - www.pharma-solutions.basf.com