DRUG DELIVERY & FORMULATION

Masking the taste of

fast-disintegrating
tablets
A new co-polymer coating overcomes the challenge of masking the taste
of fast-disintegrating tablets.

Röhm GmbH & Co KG

F ast-disintegrating tablets are a convenient dos-

age form for many applications – but they are
challenging to formulate if the active substance
especially when giving nasty-tasting medicine to
children. However, there are much more effective
and controllable ways of “locking in” the unpleasant
has an unpleasant taste. A new copolymer coat- taste of a drug, such as coating tablets with a taste-
ing enables the formulation of fast-disintegrating, free protective coating.
taste-masked tablets – thereby giving better patient e oral route is still the most convenient
compliance. and appropriate way to take most medicines and
Röhm Pharma Polymers is a business line within – without efforts to hide it – a bad taste can seri-
the Business Unit, Specialty Acrylics, of Degussa ously reduce levels of patient compliance, thereby
AG (Düsseldorf, Germany) – a world-leader in the lowering therapeutic efficacy. An unpleasant-tast- An unpleasant-
field of specialty chemicals. e business line origi- ing active substance needs to be “masked” for only tasting active
nated within the Röhm & Haas company, founded a relatively short period of time in the mouth and substance needs
by Dr Otto Röhm and his partner Otto Haas throat (from seconds to minutes), but even this to be “masked” for
nearly one hundred years ago. e long history requires a highly effective coating for good results. only a relatively
of Röhm Pharma Polymers has endowed it with e methacrylate copolymer, EUDRAGIT® E PO short period of
a deep understanding of pharmaceutical methods (E POwder) is very suitable for this purpose, show- time in the mouth
that enables it to enter into fruitful partnerships ing excellent taste-masking properties even at low and throat…
with pharmaceutical companies to develop novel film thicknesses; it can also be used to coat difficult
oral dosage forms. dosage forms, such as multiparticulate fast-disinte-
grating tablets.
Taste-masking
In the film Mary Poppins, Julie Andrews sang Fast-disintegrating tablets
that “...a spoonful of sugar helps the medicine go Fast-disintegrating tablets, made up of numerous
down...” – and this has long been folk wisdom, small subunits, are modern dosage forms that are

Innovations in Pharmaceutical Technology 109

DRUG DELIVERY & FORMULATION

Figure 1. Scanning electron microscope view of the three paracetamol grades used in coating tests.

Figure 2. Fluid bed coating of ‘dense powder’ grade paracetamol with EUDRAGIT® E PO.

well accepted by patients. ey are preferred when 1) Preparation of the wetting agent, polymer, and
it is necessary to give a large dose of a drug, involv- plasticiser suspension,
ing a tablet weight above 1 gram, as swallowing 2) Separate preparation of pigment / glidant sus-
such a large tablet is not feasible. Even for lower pension, and
tablet weights, they are of particular benefit to 3) e combination of 1) and 2).
patients with swallowing problems, such as children
or older people. Mixing SDS (sodium dodecyl sulphate),
Fast-disintegrating tablets break down in a very EUDRAGIT® E PO and stearic acid gives
short time, often within less than one minute. a clear, slightly yellowish colloidal solution.
Disintegration can take place in a glass of water Homogenisation can be performed by using either
(dispersible tablets), or in the mouth. In the latter an impeller mixer or a high-shear mixer (for exam-
case, water is not always needed, which is helpful ple, Ultra Turrax). A high-shear mixer is recom-
for people when travelling. mended, because of the shorter preparation time
It is challenging It is challenging to taste-mask multiparticulate (30-60 minutes versus 4-6 hours for an impeller
to taste-mask dosage forms, as every subunit (which may be gran- mixer). e process ends when the colloidal solu-
multiparticulate ules, pellets, micro-tablets or even drug crystals) tion is obtained.
dosage forms, as must be completely covered in order to ensure good During the dissolution process, the polymer
every subunit… taste-masking. EUDRAGIT® E PO is well-suited chains become hydrated. As hydration proceeds,
must be completely for this purpose and shows excellent taste-masking viscosity increases to a maximum and then falls
covered in order properties – even at coating densities of only 1-2 back to its original level. e final colloidal
to ensure good mg/cm2 that add little to the total tablet weight. solution of low viscosity can be easily handled
taste-masking. in the spraying process. For convenience in pro-
Preparation procedure duction, the colloidal solution can be prepared
EUDRAGIT® E PO spray suspensions used for in advance and stored for a few days before the
coating are simple to prepare. Starting with the coating procedure. Data on file at Röhm show
polymer powder (E POwder), preparation involves that the solution has a storage stability of up to
three main steps: eight days.

110 Innovations in Pharmaceutical Technology

 DRUG DELIVERY & FORMULATION

Fine-particle coating Multiparticulate tablets

To demonstrate the suitability of EUDRAGIT® When compressing coated particles into tablets, it
E PO for fine-particle coating, three different is important that the film coating is not damaged
quality grades of paracetamol were studied. by compression forces, otherwise the taste-mask-
ese grades differ in particle shape and particle ing functionality will be lost. is was tested by
size distribution, and thus specific surface area coating ‘special granular’ paracetamol with either
(Figure 1). Film coating was performed in a 15% or 30% EUDRAGIT® E PO, followed by
Unilab-5-TJ fluid bed coater (Hüttlin) and the compression in an eccentric press (Korsch, EKO)
drug crystals were coated to a 30% polymer into tablets with 60-80N hardness. e content
weight gain. of coated particles in the tablet was 40% and 48%
ere were no changes in specific surface area respectively.
for the “dense powder” and “special granular” e integrity of the film-coating was tested by
grades. is means that the crystals were coated dissolution in buffer pH 6.8. is buffer is highly
without agglomeration. Agglomeration effects were discriminating because solubility of the film-coating
observed, however, with the “fine crystal” grade. is low, but solubility of the drug is high under these
is is because the needle shape of these crystals conditions. Film damage is, therefore, easy to detect.
makes them unsuitable for coating. For the 15% formulation, there was a slightly
Scanning electron microscopy of the “dense increased release-rate for the coated particles, as
powder” grade showed that the surfaces of the compared with the compressed tablet; for the for-
single particles were completely covered, with film mulation with a 30% coating, no difference between
thicknesses between 12 and 70 µm (Figure 2). the coated particles and the compressed tablet could
ese are reasonable values for taste-masking be detected (Figure 3). is means that there was no
purposes. significant film damage from compression in either
Taste-masking investigations with the “special formulation.
granular” grade coated with EUDRAGIT® E PO
showed a good ‘mouth feeling’. Effective taste- The solution for better taste-masking
masking was obtained with just a 15% polymer ese experiments with paracetamol show that
weight gain; with a 30% polymer application, the EUDRAGIT® E PO provides a highly effective and The coating
average duration of taste-masking was doubled. convenient solution to the challenge of taste-masking solution is easy to
Despite this effective taste-masking, dissolution fine particles and multiparticulate, fast-disintegrating prepare, stable and
profiles of all paracetamol grades were unaffected tablets. e coating solution is easy to prepare, stable non-hazardous in
by film coating, as verified with both buffer pH and non-hazardous in use, and adds only minimally use, and adds only
5.8 (which is the USP dissolution medium for to the final tablet weight. Surely, it provides a much minimally to the
paracetamol tablets) and 0.1 N HCl. better solution than taking “a spoonful of sugar”? final tablet weight.

Figure 3. Dissolution rate of paracetamol from coated particles before and after compression into tablets.

Innovations in Pharmaceutical Technology 111