TY - JOUR
T1 - Reducing the Sublimation Tendency of Ligustrazine through Salt Formation
AU - Hu, Shenye
AU - Wang, Chenguang
AU - He, Xin
AU - Sun, Changquan Calvin
N1 - Publisher Copyright:
Copyright © 2020 American Chemical Society.
PY - 2020/3/4
Y1 - 2020/3/4
N2 - Two new salts of ligustrazine (tetramethylpyrazine, TMP) with the sweeteners saccharine (SAC) and acesulfame (ACS) have been synthesized through the anion exchange reaction. Single crystals of the new forms were prepared, and their structures were determined. The stability of the new salts against heat and humidity was tested and compared to the commercial hydrochloride and phosphate salts. The sublimation kinetics at various temperatures was analyzed using the Arrhenius equation. The results indicated that TMP-ACS exhibits significantly reduced sublimation tendency and hygroscopicity, which make it a more suitable salt for developing a tablet with acceptable shelf stability than the salts currently used in commercial products.
AB - Two new salts of ligustrazine (tetramethylpyrazine, TMP) with the sweeteners saccharine (SAC) and acesulfame (ACS) have been synthesized through the anion exchange reaction. Single crystals of the new forms were prepared, and their structures were determined. The stability of the new salts against heat and humidity was tested and compared to the commercial hydrochloride and phosphate salts. The sublimation kinetics at various temperatures was analyzed using the Arrhenius equation. The results indicated that TMP-ACS exhibits significantly reduced sublimation tendency and hygroscopicity, which make it a more suitable salt for developing a tablet with acceptable shelf stability than the salts currently used in commercial products.
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U2 - 10.1021/acs.cgd.9b01704
DO - 10.1021/acs.cgd.9b01704
M3 - Article
AN - SCOPUS:85080076000
SN - 1528-7483
VL - 20
SP - 2057
EP - 2063
JO - Crystal Growth and Design
JF - Crystal Growth and Design
IS - 3
ER -