Texture analyzer evaluation of ODTs.
USP's disintegration test method is well established to differentiate traditional tablets' disintegration time, but it does not
reflect the disintegration environment of ODTs, which typically has a small amount of water available. To mimic the ODTs disintegrating
or softening process in an oral cavity, a method was developed on a texture analyzer to monitor the disintegrating process
of ODTs in 2 mL of deionized water.
Figure 8: Tablet disintegration process demonstrated by texture analyzer.
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Figure 8 compares tablet disintegration process between ODTs that contain 2% Ac-Di-Sol and ODTs that contains 5% PVP XL-10
from the texture analyzer, in commonly used ODT hardness ranges. The three graphs are for tablets that were compressed at
4kN, 6kN, and 8kN, respectively. Each graph shows the probe travel distance as a function of tablet immersion time in shallow
water. The plateau portion of each curve indicates the tablet was cohesive enough to withstand the slight compressive force
before it further disintegrated. The steep vertical portion of each curve indicates that the tablet had disintegrated further
and the probe distance increased in search of the target force. The test came to an end when the probe touched the bottom
of the weighing boat.
One interesting finding from this texture analyzer study was that 2% Ac-Di-Sol and 5% PVP XL-10 provided different ODT disintegration
patterns. Ac-Di-Sol-containing tablets showed an alternative in plateau and vertical portion on the disintegration curve,
indicating a gradual softening or disintegration process. On the other hand, PVP XL-10-containing tablets displayed an initial
longer portion of plateau followed by a big vertical portion, indicating an initial delay in tablet softening or disintegration,
followed by a sudden tablet softening or disintegration. This finding partially explained the triangle-mouthfeel study results.
For example, in the triangle study, out of the total panelists that made the correct judgment, 80% commented that Ac-Di-Sol
containing ODTs provided a preferred mouthfeel to PVP XL-10 containing ODTs such as a smoother mouthfeel with faster disintegration
for Ac-Di-Sol-containing ODTs. This difference could be attributed to the gradual disintegration pattern of Ac-Di-Sol-containing
ODTs.
Conclusion
The selection of superdisintegrants is critical to ensure rapid tablet disintegration of ODTs that were prepared from the
DC process. This study showed that all three types of commercial superdisintegrants, XL-CMC, crospovidone, and SSG, can be
used in ODT applications at common ODT tablet-hardness ranges. An optimal use level was identified for each superdisintegrant,
which is 2% for Ac-Di-Sol, 5% for PVP XL-10, 5% for Kollidon CL-SF, and 5% for Glycolys. Ac-Di-Sol is the most effective among
all three types of superdisintegrant. It achieved rapid tablet disintegration time at the lowest use level and it more effectively
disintegrated harder tablets. In general, ODTs that contain 2% Ac-Di-Sol had the same mouthfeel as ODTs that contain 5% PVP
XL-10; however, 2% Ac-Di-Sol and 5% PVP XL-10 disintegrated tablets in different pattern when only a small amount of water
was available such as in the oral cavity.
Yeli Zhang* is a senior research associate, Amy Wrzesinski is an associate chemist, Marley Moses is a research technician, and Holly Bertrand is a research chemist, all in the pharmaceutical department of FMC, 801 PrincetonSouth Corporate Center, Ewing, NJ 08628,
tel. 609.963.6236, fax 609.963.6241, yeli.zhang@fmc.com
.
*To whom all correspondence should be addressed.
Submitted: Dec. 16, 2009. Accepted: Mar. 8, 2010.
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