Abstract
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.
Highlights
The pharmaceutical field has recently shown enormous interest in improving the solubilities and dissolution rates of poorly soluble drugs
Study, we explored explored benexate benexate
The solid–state properties of these new crystals were measured by Powder X-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and TG and compared to benexate hydrochloride monohydrate, the
Summary
The pharmaceutical field has recently shown enormous interest in improving the solubilities and dissolution rates of poorly soluble drugs. Many techniques for the same have been widely reported in the literature, including solid dispersion, particle size reduction, development of various nanoparticulate delivery systems, and complexation with cyclodextrin derivatives [1,2,3,4,5,6,7,8]. The preparation of nanoparticulate delivery is a cutting-edge technique to improve the bioavailability of poorly soluble drug materials
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