• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry >Facile syntheses of novel salts of a triazole antifungal agent with enhanced solubility
【24h】

Facile syntheses of novel salts of a triazole antifungal agent with enhanced solubility

机译：溶解性增强的三唑类抗真菌药新型盐的简便合成

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Acid addition salts of a triazole antifungal agent itraconazole were prepared with an aim to enhance the aqueous solubility and dissolution characteristics of the drug. Nitric, sulfuric, and p-toluenesulfonic acid addition salts (1a-c) were prepared using facile synthetic procedures. The solubility of the salts in water was found to be 24, 22, and 58 mg/mL, respectively, for 1a, 1b, and 1c, which is significantly higher than that of itraconazole (1 ng/mL). In addition to this, solubility of the salts in simulated gastric fluid (SGF) and other pharmaceutically used solvents such as ethanol and propylene glycol was also improved to a great extent. Also, it was observed that from 1a, 1b, and 1c, approximately 33, 26, and 45% drug was released in SGF in 3 h, whereas less than 10% drug was released from the free base form.
机译：制备三唑抗真菌剂伊曲康唑的酸加成盐，目的是增强药物的水溶性和溶解特性。使用简便的合成方法制备硝酸，硫酸和对甲苯磺酸加成盐（1a-c）。盐在水中的溶解度对于1a，1b和1c分别为24、22和58 mg / mL，这明显高于伊曲康唑的溶解度（1 ng / mL）。除此之外，还极大地提高了盐在模拟胃液（SGF）和其他可药用溶剂（例如乙醇和丙二醇）中的溶解度。同样，观察到从1a，1b和1c中，约有33、26和45％的药物在3小时内以SGF的形式释放，而少于10％的药物以游离碱形式释放。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号