Solubility Improvement of Benexate through Salt Formation Using Artificial Sweetener.
Solubility Improvement of Benexate through Salt Formation Using Artificial Sweetener.
复制标题
DOI：
10.3390/pharmaceutics10020064
复制
发表时间：
2018-05-26
期刊：
影响因子：
5.4
通讯作者：
Uekusa H
中科院分区：
文献类型：
--
作者：
Dwichandra Putra O;Umeda D;Fujita E;Haraguchi T;Uchida T;Yonemochi E;Uekusa H
贝奈克酯是一种临床上用作防御型抗溃疡药物，其溶解性差且有苦味。为了提高其溶解性，提出了一种晶体工程方法，即使用一种人工甜味剂作为盐共形成物来形成新型盐。这也有望解决该药物的苦味问题。在这项工作中，我们报道了新型盐贝奈克酯糖精酸盐一水合物和贝奈克酯环己基氨基磺酸盐的制备以及其物理化学性质的评估，它们的晶体结构通过单晶X射线结构分析确定。这些新型盐显示出更高的溶解性和更快的溶出曲线，这与局部层状结构的出现有关。它们还显示出更好的吸湿曲线，并被归类为非吸湿性材料。因此，贝奈克酯糖精酸盐一水合物和贝奈克酯环己基氨基磺酸盐加速了具有改进性能的贝奈克酯甜味药物盐的开发。
Benexate, a drug used clinically as a defensive type anti-ulcer agent, has poor solubility and a bitter taste. To improve its solubility, a crystal engineering approach was proposed with the formation of novel salts using an artificial sweetener as a salt co-former. This was also expected to address the bitter taste of the drug. In this work, we report on the preparation and evaluation of the physicochemical properties of the novel salts benexate saccharinate monohydrate and benexate cyclamate whose crystal structures were determined by single-crystal X-ray structure analysis. These novel salts showed higher solubility and faster dissolution profiles that were associated with the occurrence of local layered-like structures. They also showed better moisture uptake profiles and were classified as non-hygroscopic materials. Therefore, benexate saccharinate monohydrate and benexate cyclamate expedited the development of sweet pharmaceutical salts of benexate with improved performances.
登录
查看更多内容
影响因子：
--
作者：
MURANUSHI, N;YOSHIDA, M;YAMADA, H
通讯作者：
YAMADA, H
影响因子：
4.6
作者：
Ainurofiq, Ahmad;Mauludin, Rachmat;Yonemochi, Etsuo
通讯作者：
Yonemochi, Etsuo
DOI：
10.1254/jjp.72.183
发表时间：
1996-10-01
期刊：
JAPANESE JOURNAL OF PHARMACOLOGY
影响因子：
--
作者：
Hori, Y;Odaguchi, K;Mizui, T
通讯作者：
Mizui, T
影响因子：
3.8
作者：
IWASAKI, T;MATSUNAGA, K
通讯作者：
MATSUNAGA, K
影响因子：
5.8
作者：
Ohara, T;Kitamura, S;Terada, K
通讯作者：
Terada, K