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Study on the solubilization of telmisartan by forming cocrystals with aromatic carboxylic acids

Journal 2021 · IF 3.545 · 23(27): 4871-4878 · 发表于 2021 年 5 月 28 日
作者: Guojia Yu,Xinjian Chen,Lichao He,Xiangrong Li,Zhiyong Zhou,Zhongqi Ren
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摘要

The solubility of insoluble telmisartan (TEL) was improved by forming new cocrystal forms with several aromatic carboxylic acids. All solid forms showed three dissolution modes: TEL–HBA achieved the maximum release equilibrium within 30 min and maintained a stable and efficient dissolution level within 6 h. TEL–3-HBA and TEL–2,5-DHBA showed a slowly declining trend over time up to 6 h. TEL–3,5-DHBA conformed to the “spring and parachute” model. The TEL–HBA mixture was the most stable and was selected for further thermodynamic study, which found a 1 : 1 complexation with HCl (0.1 M) solution.

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