Function rules – excipients for solid dosage
forms
The world of biopharma is undergoing a process
change.
Historically, the industry has been driven by
the
introduction of new molecular entities (NME).
In peak
years, such as 1996, the US FDA approved 53 NMEs,
giving the
industry huge possibilities for growth; however,
this number was
reduced to 25 NMEs (19 chemical and six biological)
in 2009,
presenting a new challenge for the innovation
pipeline.
Additionally, patents for industry blockbusters
are running out;
for example, the patent for the active pharmaceutical
ingredient
(API) in Pfizer’s Lipitor will expire in
June 2011.
So, where is additional innovation in the pharmaceutical
industry
coming from? One answer is in the formulation
of drugs.
Currently, the bioavailability of APIs is often
a limiting factor for
therapeutic success, which must be increased by
state-of-the-art
formulations and drug delivery systems. Meanwhile,
convenience
and ease of administration play important roles
in helping patients
make the best use of their medication and in targeting
patient
groups, such as children or patients with Parkinson’s
disease,
that have problems with standard formulations.
Functional excipients
The key driving factor in the challenges for new
formulations, especially solid ones, are functional
excipients. Functional excipients can help to
control dissolution and drug release while displaying
properties that help increase the productivity
in the manufacturing process. To make approval
of the final dosage form easier and more cost
effective, these improved properties are best
created by modifying known chemical entities.
Merck Millipore’s Parteck® product range
for direct
compressible excipients is the perfect example
for such functional
excipients. Proprietary particle engineering technology
leads to
advanced functionality, helping the formulation
of drugs without
the need for undergoing the complete registration
process for
novel excipients, which are costly – a pathway
usually only used
when there is a specific interaction with a certain
API is required.
All Parteck products show significantly higher
surface areas
than other excipients based on the same chemical
structure. In
addition to the long established Parteck M series
Mannitols and
Parteck Si series Sorbitols, Merck Millipore recently
introduced
two new products to the Parteck family.
Parteck ODT
Parteck ODT is an excipient for fast dissolving
and ODT
applications. It is unique in that the fast dissolution
times are
independent of compression force and tablet hardness,
giving both
formulation scientist and manufacturing manager
additional options. This means it is easier to
create small, hard tablets that
have short dissolution time; for example, paediatric
formulations
(Figure 1). Meanwhile, standard tablet hardness
can be achieved
by using lower compression force in the process
resulting in
higher productivity. Fast dissolution tablets
are often used in
applications such as painkillers, where fast release
is preferred.
Parteck ODT shows nearly instantaneous release
in the USP tests.
Parteck Mg DC is a directly compressible magnesium
carbonate. Commonly, such DC mineral salts are
made by
mixing salt with a binder such as starch, maltodextrin,
PVP or
HPMC. Again, advanced particle engineering made
it possible
to create a DC product without any additional
binder, giving
the scientist the possibility to work with higher
salt
concentration and a higher degree of freedom in
the
formulation, such as the option to create smaller
tablets.
Continuous improvement
The importance of functional excipients is steadily
growing
and demands for controlled release agents and
improved
bioavailability are increasing daily. Merck Millipore
will strive
to improve the Parteck product line and will address
the
needs of advanced formulations with its new inorganic
production plant at Darmstadt, creating products
adapted
to the challenges of today’s pharmaceutical
industry.
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Company profile
Merck
For further information, visit: www.merck.de
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