Triamterene-furosemide salt: structural aspects and physicochemical evaluation
文献类型：期刊论文
| 作者 | Peng, Bo; Wang, Jian-Rong ; Mei, Xuefeng
|
| 刊名 | ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE CRYSTAL ENGINEERING AND MATERIALS
 |
| 出版日期 | 2018-12 |
| 卷号 | 74页码:738-741 |
| 关键词 | triamterene furosemide drug-drug salt solubility intrinsic dissolution rate (IDR) |
| ISSN号 | 2052-5206 |
| DOI | 10.1107/S2052520618013185 |
| 文献子类 | Article |
| 英文摘要 | Furosemide (Fur) is a BCS class IV diuretic drug with low bioavailability due to its poor solubility and poor membrane permeability. Triamterene (Tri) is a potassium-sparing diuretic with low bioavailability due to its poor solubility. Here, a novel drug-drug salt composed of Tri and Fur was successfully synthesized. Tri-Fur was comprehensively characterized with single-crystal X-ray and powder X-ray diffraction techniques, thermogravimetric analysis, differential scanning calorimetry and dynamic vapor sorption. The apparent equilibrium solubility (in pH 2.0 buffer) of Tri-Fur is improved compared with Fur and a physical mixture of Tri with equimolar Fur by 15.3-fold and 12.2-fold enhancements, respectively. Its intrinsic dissolution rate (in pH 2.0 buffer) is also higher than for a Fur component with an enhancement of 9.5-fold. This study provides a valuable insight into the formation of dual pharmaceutical salts and demonstrates that Tri-Fur can be a potential alternative formulation. |
| WOS关键词 | PHARMACEUTICAL COCRYSTALS ; SOLUBILITY ; POLYMORPHISM ; PERMEABILITY ; IMPROVE ; DRUGS |
| 资助项目 | Shanghai Natural Science Foundation[18ZR1447900] ; Youth Innovation Promotion Association CAS[2016257] ; CAS Key Technology Talent Program[00000000] ; SANOFI-SIBS Scholarship[00000000] |
| WOS研究方向 | Chemistry ; Crystallography |
| 语种 | 英语 |
| WOS记录号 | WOS:000452796800025 |
| 出版者 | INT UNION CRYSTALLOGRAPHY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279478]  |
| 专题 | 药物质量控制与固体化学研究中心 |
| 通讯作者 | Mei, Xuefeng |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, 555 Zu Chong Zhi Rd,Zhangjiang High Tech Pk, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Peng, Bo,Wang, Jian-Rong,Mei, Xuefeng. Triamterene-furosemide salt: structural aspects and physicochemical evaluation[J]. ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE CRYSTAL ENGINEERING AND MATERIALS,2018,74:738-741. |
| APA | Peng, Bo,Wang, Jian-Rong,&Mei, Xuefeng.(2018).Triamterene-furosemide salt: structural aspects and physicochemical evaluation.ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE CRYSTAL ENGINEERING AND MATERIALS,74,738-741. |
| MLA | Peng, Bo,et al."Triamterene-furosemide salt: structural aspects and physicochemical evaluation".ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE CRYSTAL ENGINEERING AND MATERIALS 74(2018):738-741. |
入库方式： OAI收割
来源：上海药物研究所
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