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影响磺胺甲(口恶)唑-甲氧苄啶共晶形成的因素

Factors Affecting the Formation of Sulfamethoxazole-trimethoprim Co-crystal

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【作者】 陆纪宏范珊珊王强刘相奎沈裕辉

【Author】 LU Jihong;FAN Shanshan;WANG Qiang;LIU Xiangkui;SHEN Yuhui;Zhejiang Jinhua CONBA Bio-pharm.Co., Ltd.;Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry;

【通讯作者】 沈裕辉;

【机构】 浙江金华康恩贝生物制药有限公司中国医药工业研究总院上海医药工业研究院有限公司

【摘要】 药物共晶在改善难溶性药物溶解和溶出方面有广阔的应用前景。复方磺胺甲(口恶)唑片中含磺胺甲(口恶)唑和甲氧苄啶,这2种活性药物成分可能形成共晶。经过与标准样品对比,确定该现象存在于片剂中。该文继续探讨了制剂工艺中水分含量、压力和温度这3个因素对磺胺甲(口恶)唑-甲氧苄啶共晶形成的影响。结果显示,水分可诱导共晶形成;温度升高至128℃后才会形成共晶;压力对共晶的形成无影响。2种活性药物成分形成的共晶,晶体结构稳定,提高了片剂的抗压性。

【Abstract】 Drug co-crystal had a promising application in improving the solubility and dissolution of poorly water-soluble drugs. The compound sulfamethoxazole tablets contain two active pharmaceutical ingredients: sulfamethoxazole and trimethoprim, which may form co-crystal. In this paper, the existence of the co-crystal in the tablets had been confirmed by comparison with the standard samples. Then, three influence factors introduced in the formulation process, namely water content, pressure and temperature, on the formation of sulfamethoxazole-trimethoprim co-crystal was investigated. The results showed that water content was the key parameter for the formation of the co-crystal, whereas the co-crystal was formed only when the temperature reached above 128 ℃. Pressure was proved to have no effect on the formation of the co-crystal. The formed co-crystal had a stable crystal structure, which improved the compression resistance of the tablets.

【基金】 上海市2023年度“科技创新行动计划”专业技术服务平台项目(23DZ2292600)
  • 【文献出处】 中国医药工业杂志 ,Chinese Journal of Pharmaceuticals , 编辑部邮箱 ,2024年08期
  • 【分类号】TQ460.1
  • 【下载频次】9
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