Patient-friendly ODTs
Many tablets are hard to swallow: they are bitter tasting, disintegrate
slowly and do not take effect for about an hour after administration. One
company has worked to successfully overcome these challenges.
Several marketed products,
which are typically
immediate-release dosage
forms, exhibit a rapid-onset of
action with a Tmax of about an
hour. Actives in many of these
marketed products are bitter to
a varying degree, and the ability
to mask poor drug taste with
traditional flavours and sugars
is limited.
Overcoming the problem of
poor taste with extremely bitter
drugs makes the development
of patient-friendly, orally
disintegrating tablets (ODTs)
particularly challenging. A
major objective at Eurand is
to develop ODTs that
achieve the desired plasma
concentration profiles for
poorly tasting therapeutic
agents while maintaining
effective taste-masking
properties and acceptable
‘mouthfeel’ so that the ODTs
are bioequivalent to referencelisted
IR drug products.
Taste-masking
Eurand’s Microcaps®
technology efficiently and
uniformly coats drug particles
with polymeric membranes of
varying thickness and porosity.
The membranes create an inert
barrier between the drug and
the tastebuds. However, the
very act of taste-masking
results in slower dissolution
and hence release of the
drug for absorption.
The modified Microcaps
technology enables preparation
of drug particles with
taste-masking membranes
comprising gastrosoluble
agents (for example, calcium
carbonate or Eudragit E100
polymer), which rapidly dissolve
in the acid environment of
the stomach, thereby creating
micro-channels for dissolved
drug to pass through. This
permits more rapid release of
the active ingredient.
Rapid disintegration
Eurand’s AdvaTab® technology
is a direct compression
technology that incorporates
taste-masked microparticles
of poor-tasting drugs with
proprietary quick dissolving
microgranules and flavours/
sweeteners into tablets in which
taste-masked drug particles are
homogeneously dispersed in
the tablet matrix. The resulting
ODT disintegrates quickly
(typically within 30 seconds)
in the mouth without water,
forming a smooth, easy-to
swallow suspension.
These tablets exhibit excellent
physical robustness and as
such are suitable for packaging
in bottles and push-through
blisters as well as rapid
disintegration/dissolution
properties, thus achieving
bioequivalence to a reference
listed IR drug product
(see graph).
Immediate release
While the orally administered
pharmaceutical dosage form
passes through the human
gastrointestinal tract exhibiting
varying pHs, the drug should
be solubilised/released from the
dosage form and be available
in solution form at or near the
site for absorption to occur.
Moreover, the transit time of
dosage form varies depending
on the dosage form size and
fast/fed conditions. The rate
at which the drug goes into a
solution and is released from
a dosage form is important to
the kinetics of drug absorption.
Many therapeutic agents are
most effective when made
available at constant rates, at
ascending rates or at no-release
for several hours followed by
sustained-release profiles or a
bimodal-release profile.
Eurand’s Diffucaps®
technology involves the
preparation of immediate
release beads with one or more
layers of functional polymers
and finished dosage forms, hard
gelatin capsules, conventional
or orally disintegrating tablets,
comprising one or more coated
bead populations (IR beads
and/or coated sustained or
enteric release beads, and/or
TPR beads). Such a dosage
form exhibits a composite
drug-release profile mimicking
the target profile suitable for
a once-daily dosing regimen.
The resulting absorption of
therapeutic agents generally
results in desired plasma
concentrations leading
to maximum efficacy and
minimum toxic side effects. end
For more
information, visit:
www.eurand.com.
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