Reducing the Sublimation Tendency of Ligustrazine through Salt
Reducing the Sublimation Tendency of Ligustrazine through Salt
复制标题
盐降低川芎嗪的升华倾向
DOI：
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发表时间：
2020
期刊：
影响因子：
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通讯作者：
Changquan Calvin Sun
中科院分区：
文献类型：
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作者：
Shenye Hu;Chenguang Wang;Xin He （何欣）;Changquan Calvin Sun
通过阴离子交换反应合成了川芎嗪（四甲基吡嗪，TMP）与甜味剂糖精（SAC）和安赛蜜（ACS）的两种新盐。制备了新形式的单晶，并确定了它们的结构。测试了新盐对热和湿度的稳定性，并与商业盐酸盐和磷酸盐进行了比较。使用阿伦尼乌斯方程分析不同温度下的升华动力学。结果表明，TMP-ACS 的升华倾向和吸湿性显着降低，这使其成为比目前商业产品中使用的盐更适合开发具有可接受的货架稳定性的片剂的盐。
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.