eBook: Formulation Technologies and Strategies for Successful New Product Development - 38

sodium stearyl fumarate, 3% trimyristin, 1% Parteck®
LUB MST magnesium stearate, or 5% polyethylene
glycol 6000) in placebo formulations, no significant
effect on disintegration behavior was observed. As a
result, formulators have greater flexibility to resolve
specific formulation problems.
Disintegration and drug release tests for tablets
including Parteck® ODT excipient and different
model APIs have also been evaluated.11
In one
example,
Figure 3. Morphology of Parteck® ODT excipient before compression.
This type of polyol excipient typically shows a
great deal of wear of the granulated particles upon
mechanical stress. The morphology of the Parteck®
ODT material remains unchanged after mixing and
compression, however, resulting in a very large
specific surface area of the tablet matrix of up to
3.5 m²/g.8,10
One benefit is the minimization of the wear of
tableting equipment. Also, such an exceptionally
large surface area can adsorb large quantities of
small API particles well and prevent de mixing during
the manufacturing process. Indeed, up to 50% API
can be directly compressed with Parteck® ODT,
compared with a typical content of approximately
20-30%. Water uptake and disintegration of the
tablet matrix are also enhanced. Clearly, both the
superdisintegrant and the unique surface structure
of the binder are responsible for fast disintegration
of the overall product.
In addition, the Parteck® ODT system does not exhibit
any sensitivity toward different lubricants. When
added to a randomly chosen set of lubricants (2%
two Parteck® ODT drug formulations
(Tables 3 and 4) with paracetamol of different grades
and sources were used to investigate drug release
kinetics in vitro.
Notably, after 10 minutes more than 95% of the API
in the two formulations was released with Parteck®
ODT as directly compressible excipient. In addition,
friability at a very low compression force (e.g., 5 kN)
of < 0.4% was achieved (data not shown), allowing
for the manufacture of extremely robust tablets
that can survive processing and handling during
manufacture, packaging, and use.
In another example with sildenafil as the API,
disintegration times were found to be well within
the range expected for ODT applications, and
good tablet hardnesses and low tablet friabilities
were observed even at low compression forces.
Importantly, producing hard and stable tablets did
not cause the disintegration time to suffer. As can be
seen in Figure 4, the disintegration time remained
constant over a wide range of tablet strengths.
This attribute is a major difference from some ODT
excipient systems on the market, which display fast
disintegration only for rather soft tablets.
38

eBook: Formulation Technologies and Strategies for Successful New Product Development

Table of Contents for the Digital Edition of eBook: Formulation Technologies and Strategies for Successful New Product Development