Water is generally regarded as a universal plasticizer
of amorphous
drugs or amorphous drug-containing systems. A decrease in glass-transition
temperature (T
g) is considered the general
result of this plasticizing effect. A recent study exhibits that water
can increase the T
g of amorphous prilocaine
(PRL) and thus shows an anti-plasticizing effect. The structurally
similar drug lidocaine (LID) might show similar interactions with
water, and thus an anti-plasticizing effect of water is hypothesized
to also occur in amorphous LID. However, the influence of water on
the T
g of LID cannot be determined directly
due to the very low stability of LID in the amorphous form. It is
possible to predict the T
g of LID from
a co-amorphous system of PRL–LID using the Gordon–Taylor
equation. Interactions were observed between PRL and LID based on
the deviations between the experimental T
gs and the T
gs calculated by the conventional
use of the Gordon–Taylor equation. A modified use of the Gordon–Taylor
equation was applied using the optimal co-amorphous system as a separate
component and the excess drug as the other component. The predicted T
g of fully hydrated LID could thus be determined
and was found to be increased by 0.9 ± 0.7 K compared with the T
g of water-free amorphous LID. It could be shown
that water exhibited a small anti-plasticizing effect on LID.
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