TY - JOUR
T1 - The natural bile acid surfactant sodium taurocholate (NaTC) as a coformer in coamorphous systems
T2 - Enhanced physical stability and dissolution behavior of coamorphous drug-NaTc systems
AU - Gniado, Katarzyna
AU - MacFhionnghaile, Pól
AU - McArdle, Patrick
AU - Erxleben, Andrea
N1 - Publisher Copyright:
© 2017 Elsevier B.V.
PY - 2018/1/15
Y1 - 2018/1/15
N2 - The amorphization of 18 different drugs on milling with one mole equivalent sodium taurocholate (NaTC) was investigated. In all cases the X-ray powder pattern showed an amorphous halo after milling at room temperature or after cryomilling and 14 of the 18 coamorphous drug-NaTC systems were physically stable for between one to eleven months under ambient storage conditions. In three cases, namely carbamazepine-NaTC, indomethacin-NaTC and mefenamic acid-NaTC, significant dissolution advantages over the crystalline drugs were observed, both for the freshly prepared samples and after storage for seven months. To understand the increased physical stability, infrared-, near-infrared and Raman spectroscopic studies were carried out. The effectiveness of NaTC as a coformer in a diverse range of coamorphous systems is attributed to its awkward molecular shape that hampers recrystallization and phase separation and its propensity to form a range of similar, yet different drug-coformer hydrogen bonding arrangements.
AB - The amorphization of 18 different drugs on milling with one mole equivalent sodium taurocholate (NaTC) was investigated. In all cases the X-ray powder pattern showed an amorphous halo after milling at room temperature or after cryomilling and 14 of the 18 coamorphous drug-NaTC systems were physically stable for between one to eleven months under ambient storage conditions. In three cases, namely carbamazepine-NaTC, indomethacin-NaTC and mefenamic acid-NaTC, significant dissolution advantages over the crystalline drugs were observed, both for the freshly prepared samples and after storage for seven months. To understand the increased physical stability, infrared-, near-infrared and Raman spectroscopic studies were carried out. The effectiveness of NaTC as a coformer in a diverse range of coamorphous systems is attributed to its awkward molecular shape that hampers recrystallization and phase separation and its propensity to form a range of similar, yet different drug-coformer hydrogen bonding arrangements.
KW - Amorphous
KW - Crystallization inhibition
KW - Dissolution studies
KW - Spectroscopy
UR - https://www.scopus.com/pages/publications/85032910873
U2 - 10.1016/j.ijpharm.2017.10.049
DO - 10.1016/j.ijpharm.2017.10.049
M3 - Article
SN - 0378-5173
VL - 535
SP - 132
EP - 139
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -