Study on Cocrystal and Salt of Triamterene to Improve Solubility

来源 :2014年中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会 | 被引量 : 0次 | 上传用户:qq121450500
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  Triamterene is potassium-sparing diuretics widely used in cardiovascular medications, while poor solubility restrict its application and induce low bioavailability.In our research, two salts of TAT with mandelic acid(5) and saccharin(6), as well as a few crystal phases including benzoic acid, tartaric acid, Methyl gallate were synthesized by suspend or grinding.The new crystal phases were characterized by single crystal X-ray diffraction, powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analyses.The solubility of TAT is improved, and the apparent solubility values of TAT/mandelate salt and TAT/saccharinate salt monohydrate in the phosphate buffer of pH 6.8 are approximately 3.2 and 1.2 times as large as that of TAT.
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