Thermal investigation on hydrated co-amorphous systems of nicotinamide and prilocaine
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Thermal investigation on hydrated co-amorphous systems of nicotinamide and prilocaine. / Xu, Xiaoyue; Rades, Thomas; Grohganz, Holger.
In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 186, 2023, p. 1-6.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Thermal investigation on hydrated co-amorphous systems of nicotinamide and prilocaine
AU - Xu, Xiaoyue
AU - Rades, Thomas
AU - Grohganz, Holger
N1 - Funding Information: Xiaoyue Xu acknowledges the China Scholarship Council (Grant 202008420212) for financial support. Publisher Copyright: © 2023 The Author(s)
PY - 2023
Y1 - 2023
N2 - It is generally recognized that water, acting as a plasticizer, increases molecular mobility, leading to a decrease of the glass transition temperature (Tg) in amorphous systems. However, an anti-plasticizing effect of water was recently observed on prilocaine (PRL). This effect might be used in co-amorphous systems to moderate the plasticizing effect of water. Nicotinamide (NIC) can form co-amorphous systems with PRL. In order to investigate the effect of water on these co-amorphous systems, the Tgs and molecular mobility of hydrated co-amorphous NIC-PRL systems were compared with those of the respective anhydrous systems. Molecular mobility was estimated by considering the enthalpic recovery at the Tg using the Kohlrausch-Williams-Watts (KWW) equation. At molar ratios of NIC above 0.2, a plasticizing effect of water on co-amorphous NIC-PRL systems was observed with increasing the NIC concentration. In contrast, at molar ratios of NIC of 0.2 and below, water had an anti-plasticizing effect on the co-amorphous NIC-PRL systems, with increased Tgs and reduced mobility upon hydration.
AB - It is generally recognized that water, acting as a plasticizer, increases molecular mobility, leading to a decrease of the glass transition temperature (Tg) in amorphous systems. However, an anti-plasticizing effect of water was recently observed on prilocaine (PRL). This effect might be used in co-amorphous systems to moderate the plasticizing effect of water. Nicotinamide (NIC) can form co-amorphous systems with PRL. In order to investigate the effect of water on these co-amorphous systems, the Tgs and molecular mobility of hydrated co-amorphous NIC-PRL systems were compared with those of the respective anhydrous systems. Molecular mobility was estimated by considering the enthalpic recovery at the Tg using the Kohlrausch-Williams-Watts (KWW) equation. At molar ratios of NIC above 0.2, a plasticizing effect of water on co-amorphous NIC-PRL systems was observed with increasing the NIC concentration. In contrast, at molar ratios of NIC of 0.2 and below, water had an anti-plasticizing effect on the co-amorphous NIC-PRL systems, with increased Tgs and reduced mobility upon hydration.
KW - Anti-plasticizing effect of water
KW - Co-amorphous
KW - Glass transition
KW - Molecular mobility
KW - Prilocaine-nicotinamide
U2 - 10.1016/j.ejpb.2023.02.015
DO - 10.1016/j.ejpb.2023.02.015
M3 - Journal article
C2 - 36878408
AN - SCOPUS:85150066373
VL - 186
SP - 1
EP - 6
JO - European Journal of Pharmaceutics and Biopharmaceutics
JF - European Journal of Pharmaceutics and Biopharmaceutics
SN - 0939-6411
ER -
ID: 341261281