Download Film Coating for Taste-masking of Pediatric Oral Solid

Case Study
Film Coating for Taste-masking of
Pediatric Oral Solid Dosage Forms
Use of Surelease® and Opadry® in the Development of a Paediatric Form of Raltegravir for the
European Union
Raltegravir is anti-retroviral drug, developed by Merck Sharp & Dome (MSD) for the treatment
of human immunodeficiency virus (HIV-1) and marketed under the trade name ISENTRESS.
The product was first presented as a 400 mg film coated tablet and granted a marketing
authorization, valid throughout the European Union in December 2007 for the treatment of
HIV-1 infection in adults.
Subsequently MSD decided to develop a paediatric formulation of the drug designed to be suitable for
children from the age of two years, for whom the 400mg tablet was not appropriate. For clinical reasons it
was decided that two strengths were needed, 25mg and 100mg.
The active substance, raltegravir, has an intense bitter taste and hence the taste masking of this material
was seen as an essential part of the development program. Several taste-masking options were evaluated
by coating the raltegravir granules prior to processing into the final dosage form. The chosen option was to
use a coating comprised of Surelease® (E-7-19040), aqueous ethylcellulose dispersion, in combination with a
hypromellose based Opadry® product. Insoluble in water, ethylcellulose acts as the taste-masking agent by
delaying the release of the drug in the mouth, while Opadry is used as a pore-former in the coating, which
allows immediate release of the drug once in the stomach.
MSD considered a range of different dosage forms for the finished medicinal product including orally
disintegrating tablets and chewable tablets. Based on dissolution data and patient questionnaires the
decision was made to go forward with a chewable tablet. The final chewable tablet also contains a flavour
system in case chewing causes some breakdown of the taste-mask coating.
In the EU, the paediatric form of Isentress gained a positive opinion from the Committee for
Medicinal Products for Human use in October 2012, for use in children from the age of 2 years.
Note: In the US, there is also a version of Isentress for oral suspension, which also includes Surelease. This
product is licenced for patients at least 4 weeks of age and weighing over 3kg.
Further information on the use of Film Coating for Taste-masking applications can be found at:
http://www.colorcon.com/products-formulation/all-products/film-coatings/sustained-release/surelease
The information contained herein, to the best of Colorcon, Inc.’s knowledge is true and accurate. Any recommendations or
suggestions of Colorcon, Inc. with regard to the products provided by Colorcon, Inc. are made without warranty, either implied or
expressed, because of the variations in methods, conditions and equipment which may be used in commercially processing the
products, and no such warranties are made for the suitability of the products for any applications that you may have disclosed.
Colorcon, Inc. shall not be liable for loss of profit or for incidental, special or consequential loss or damages.
Colorcon, Inc. makes no warranty, either expressed or implied, that the use of the products provided by Colorcon, Inc., will
not infringe any trademark, trade name, copyright, patent or other rights held by any third person or entity when used in the
customer’s application.
© BPSI Holdings LLC, 2014.
For more information, contact your Colorcon representative or call:
The information contained in this document is proprietary to
Colorcon, Inc. and may not be used or disseminated
inappropriately.
North America
+1-215-699-7733
All trademarks, except where noted, are property
of BPSI Holdings LLC.
Europe/Middle East/Africa
Asia Pacific
Latin America
+44-(0)-1322-293000
+65-6438-0318
+65-6438-0318
+54-11-4552-1565+54-11-5556-7700
You can also visit our website at www.colorcon.com
Film Coating for Pediatric Formulations
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