Benexate, a drug used clinically as a defensive type anti-ulcer agent, has poor solubility\nand a bitter taste. To improve its solubility, a crystal engineering approach was proposed with the\nformation of novel salts using an artificial sweetener as a salt co-former. This was also expected to\naddress the bitter taste of the drug. In this work, we report on the preparation and evaluation of the\nphysicochemical properties of the novel salts benexate saccharinate monohydrate and benexate\ncyclamate whose crystal structures were determined by single-crystal X-ray structure analysis.\nThese novel salts showed higher solubility and faster dissolution profiles that were associated\nwith the occurrence of local layered-like structures. They also showed better moisture uptake profiles\nand were classified as non-hygroscopic materials. Therefore, benexate saccharinate monohydrate\nand benexate cyclamate expedited the development of sweet pharmaceutical salts of benexate with\nimproved performances.
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