Benexate, a drug used clin. as a defensive type anti-ulcer agent, has poor soly. and a bitter taste. To improve its soly., 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 prepn. and evaluation of the physicochem. properties of the novel salts benexate saccharinate monohydrate and benexate cyclamate whose crystal structures were detd. by single-crystal X-ray structure anal. These novel salts showed higher soly. and faster dissoln. profiles that were assocd. 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. [on SciFinder(R)]
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