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影响磺胺甲嗯唑-甲氧苄啶共晶形成的因素

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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(噁)唑片中含磺胺甲(噁)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(噁)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.
Factors Affecting the Formation of Sulfamethoxazole-trimethoprim Co-crystal
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.

sulfamethoxazoletrimethoprimco-crystalcompound sulfamethoxazole tabletantibacterial drug

陆纪宏、范珊珊、王强、刘相奎、沈裕辉

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浙江金华康恩贝生物制药有限公司,浙江金华 321016

中国医药工业研究总院上海医药工业研究院有限公司,上海 201203

磺胺甲(噁)唑 甲氧苄啶 共晶 复方磺胺甲(噁)唑片 抗菌药

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

2024

中国医药工业杂志
上海医药工业研究院,中国化学制药工业协会

中国医药工业杂志

CSTPCD
影响因子:0.487
ISSN:1001-8255
年,卷(期):2024.55(8)