Reducing the Sublimation Tendency of Ligustrazine through Salt Formation

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Abstract

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.

Original languageEnglish (US)
Pages (from-to)2057-2063
Number of pages7
JournalCrystal Growth and Design
Volume20
Issue number3
DOIs
StatePublished - Mar 4 2020

Bibliographical note

Funding Information:
We thank Victor G. Young, Jr. and the X-ray Crystallographic Laboratory at 192 Kolthoff Hall, Department of Chemistry, University of Minnesota, for providing crystallographic solutions of TMP-SAC and TMP-ACS. This work was supported by grants from National Natural Science Foundation of China (No.31872508), Natural Science Foundation of Hebei (No.C2017204085) and Key Research grants of Hebei (19227505D).

Publisher Copyright:
Copyright © 2020 American Chemical Society.

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