StabEthycelFilmCoat HdOut.QXD - FMC BioPolymer
StabEthycelFilmCoat HdOut.QXD - FMC BioPolymer
StabEthycelFilmCoat HdOut.QXD - FMC BioPolymer
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be Registered U.S. Patent & Trademark Office and<br />
in other countries: <strong>FMC</strong> logo, Aquacoat, The Science<br />
of Formulation, and The Science of Formulation Mark.<br />
© <strong>FMC</strong> Corporation. All rights reserved.<br />
<strong>FMC</strong> <strong>BioPolymer</strong><br />
THE SCIENCE OF FORMULATION<br />
POSTER SESSION<br />
The stability of ethylcellulose film coatings<br />
containing PG alginate or carrageenan<br />
Author: Dr. Juergen Siepmann,<br />
University of Lille et al.<br />
Controlled Release Society 2007<br />
Presented by: Dr. Juergen Siepmann,<br />
University of Lille et al.<br />
www.fmcbiopolymer.com<br />
pharm_info@fmc.com<br />
2007-ECD.01.0607 Printed in USA RS
THE STABILITY OF ETHYLCELLULOSE FILM COATINGS<br />
CONTAINING PG ALGINATE OR CARRAGEENAN<br />
Susanne Muschert, 1 Florence Siepmann, 1 Bruno Leclercq, 2 Brian Carlin, 3 Juergen Siepmann 1<br />
1<br />
College of Pharmacy, JE 2491, University of Lille, 3, Rue du Prof. Laguesse, 59006 Lille, France<br />
2<br />
<strong>FMC</strong> <strong>BioPolymer</strong>, Avenue Mounier 83, 1200 Brussels, Belgium<br />
3<br />
<strong>FMC</strong> <strong>BioPolymer</strong>, US Route 1 & Plainsboro Road, Princeton, NJ 08543, USA<br />
Introduction<br />
Ethylcellulose-based film coatings offer an effective means to control drug<br />
release from solid oral dosage forms [1,2] . The use of aqueous polymer dispersions<br />
presents major advantages compared to organic solutions, including<br />
reduced processing times. However, the obtained film coatings might show<br />
further coalescence during long term storage, resulting in decreasing drug<br />
release rates. The aim of this study was to identify an easy tool to improve<br />
long term stability of polymeric film coatings from aqueous dispersions.<br />
Objectives<br />
• To identify appropriate additives for the aqueous ethylcellulose dispersion<br />
Aquacoat ® ECD, that do not cause flocculation of the coating formulation<br />
and improve the storage stability of coated pellets.<br />
• To monitor the efficiency of these novel film coatings via open long term<br />
storage trials under ambient and stress conditions.<br />
Experimental<br />
Theophylline beads were coated with an aqueous ethylcellulose dispersion<br />
(Aquacoat ECD) containing small amounts of propylene glycol alginate (PG<br />
alginate) or carrageenan in a fluidized bed. The pellets were cured for 1 or<br />
2 d at 60°C, or for 1 or 2 d at 60°C and 75% relative humidity (RH) (followed<br />
by 1 d at 60°C for drying). Drug release was measured in 0.1 M HCl as well<br />
as in phosphate buffer pH 7.4 using the USP paddle apparatus. Potential<br />
changes in the release patterns during 6 months open storage under<br />
ambient as well as stress conditions [“room temperature and ambient RH”<br />
and “40°C and 75%RH”] were monitored.<br />
Results and Discussion<br />
Figure 1: Theophylline release from pellets coated with ethylcellulose:PG alginate 90:10 blends in 0.1<br />
M HCl before (dotted curves) and after (solid curves) 6 open months storage at: (a) room temperature,<br />
and (b) 40°C and 75% RH (coating level: 20%, the curing conditions are indicated in the figures).<br />
Figure 2: Theophylline release from pellets coated with ethylcellulose:PG alginate 90:10 blends in<br />
phosphate buffer pH 7.4 before (dotted curves) and after (solid curves) 6 open months storage at: (a)<br />
room temperature, and (b) 40°C and 75% RH (coating level: 20%, the curing conditions are indicated<br />
in the figures).<br />
Figure 3: Theophylline release from pellets coated with ethylcellulose:carrageenan 90:10 blends in<br />
0.1M HCl before (dotted curves) and after (solid curves) 6 open months storage at (a) room temperature,<br />
and (b) 40°C and 75% RH (coating level: 20%, the curing conditions are indicated in the figures).<br />
Figure 4: Theophylline release from pellets coated with ethylcellulose:carrageenan 90:10 blends in<br />
phosphate buffer pH 7.4 before (dotted curves) and after (solid curves) 6 open months storage at (a)<br />
room temperature, and (b) 40°C and 75% RH (coating level: 20%, the curing conditions are indicated<br />
in the figures).<br />
Figure 5: Theophylline release from pellets coated with ethylcellulose:carrageenan 95:5 blends in 0.1M<br />
HCl before (dotted curves) and after (solid curves) 6 open months storage at (a) room temperature, and<br />
(b) 40°C and 75% RH (coating level: 20%, the curing conditions are indicated in the figures).<br />
Figure 6: Theophylline release from pellets coated with ethylcellulose: carrageenan 95:5 blends in<br />
phosphate buffer pH 7.4 before (dotted curves) and after (solid curves) 6 months storage at (a) room temperature,<br />
and (b) 40°C and 75% RH (coating level: 20%, the curing conditions are indicated in the figures).<br />
Conclusions<br />
The PG alginate and carrageenan containing ethylcellulose coatings are not<br />
as stable as the previously investigated ethylcellulose: PVA-PEG graft<br />
copolymer systems [3] , but further work is required to determine process and<br />
material contributions.<br />
References<br />
1. J.W. McGinity Aqueous Polymeric Coatings for Pharmaceutical Dosage Forms, II (1997).<br />
2. P. Schultz et al. J. Control. Release 47, 181 (1997).<br />
3. S. Muschert et al. 3rd Pharmaceutical Sciences World Meeting (PSWC 2007),<br />
Amsterdam, The Netherlands.<br />
www.fmcbiopolymer.com<br />
www.univ-lille2.fr.
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