Influence of Water on Amorphous Lidocaine
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Influence of Water on Amorphous Lidocaine. / Xu, Xiaoyue; Grohganz, Holger; Rades, Thomas.
In: Molecular Pharmaceutics, Vol. 19, No. 9, 2022, p. 3199–3205.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Influence of Water on Amorphous Lidocaine
AU - Xu, Xiaoyue
AU - Grohganz, Holger
AU - Rades, Thomas
PY - 2022
Y1 - 2022
N2 - 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(g)s and the T(g)s 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.
AB - 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(g)s and the T(g)s 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.
KW - co-amorphous
KW - glass transition
KW - molecular interaction
KW - anti-plasticizing effect
KW - lidocaine
U2 - 10.1021/acs.molpharmaceut.2c00339
DO - 10.1021/acs.molpharmaceut.2c00339
M3 - Journal article
C2 - 35876141
VL - 19
SP - 3199
EP - 3205
JO - Molecular Pharmaceutics
JF - Molecular Pharmaceutics
SN - 1543-8384
IS - 9
ER -
ID: 318528304