| 杨洁,刘浩,李姗姗,等.复方新诺明有效成分的晶体结构及共晶研究[J].安徽医药,2021,25(11):2136-2139. |
| 复方新诺明有效成分的晶体结构及共晶研究 |
| Research on the co-crystal and structures of the effective constituents in radonil |
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| DOI：10.3969/j.issn.1009-6469.2021.11.004 |
| 中文关键词: 甲氧苄氨嘧啶，磺胺甲 ??唑复方合剂 粉末衍射 晶体结构 共晶 抗菌药物 |
| 英文关键词: Trimethoprim,sulfamethoxazole drug combination Powder diffraction Crystal structure Co-crystal Antibacterial agents |
| 基金项目:国家自然科学基金( 31800802)；陕西省自然科学基金( 2019JM-152)；研究生创新种子基金( CX2020258)；大学生创新创业训练计划项目( S201910699420，S202010699055) |
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| 中文摘要: |
| 目的研究复方新诺明中有效成分磺胺甲 ??唑(SMZ)的单晶结构，研究其与甲氧苄啶( TMP)的共晶现象，为开发共晶新剂型提供实验支持。方法采用加溶剂研磨法制备 SMZ和 TMP的共晶粉末，利用反射法测定红外光谱，采用差示扫描量热法(DSC)测定熔点，通过粉末 X射线衍射( PXRD)研究晶型。通过溶剂挥发法得到 SMZ的单晶，利用 X射线单晶衍射仪测定其晶体结构。结果 SMZ的单晶属于单斜晶系，空间点群为 C2/c，晶胞参数 a=1.620 9(10)nm，b=0.552 7(3)nm，c=2.595 5(16) nm，每个晶胞中有 8个分子。共晶粉末的熔点为 187.78 ℃，介于 SMZ的熔点 170.92 ℃和 TMP的熔点 201.96 ℃之间。与单独组分相比较，红外图谱的指纹区发生明显变化， PXRD产生新的 X射线粉末衍射峰。结论 SMZ的单晶属于 E型结构， SMZ和 TMP通过研磨可以形成共晶，共晶现象引起红外、熔点和衍射峰的明显变化，研究结果为开发药物共晶新剂型提供实验基础。 |
| 英文摘要: |
| Objective The crystal structure of sulfamethoxazole which was the main effective constituent of Radonil was obtained and researched. The co-crystal phenomena between sulfamethoxazole (SMZ) and trimethoprim (TMP) were studied to obtain more experimental data for developing new dosage forms.Methods The co-crystals of SMZ and TMP were prepared by trituration with solvent.The infrared spectroscopy, melting point and crystal form of SMZ, TMP, and co-crystals were investigated by attenuated total reflectance FT-IR, differential scanning calorimetry and powder X-ray diffraction. The single crystal of SMZ was obtained from methanol bysolvent evaporation method. The crystal structure of SMZ was tested by X-ray single crystal diffractometer.Results The crystal of SMZ was monoclinic, space group C2/c, with a=1.620 9(10) nm, b=0.552 7(3) nm, c=2.595 5(16) nm, eight molecular in one cell unit. The melting point of the co-crystal was 187.78 ℃ which was between the SMZ (170.92 ℃) and the TMP (201.96 ℃). Comparing with the SMZ and TMP, the FT-IR of co-crystals in the molecular fingerprint region had some significant difference. The new X-ray powder diffraction peaks were found from the co-crystals.Conclusion The configuration of SMZ single crystal structure was E conformation. The co-crystal can be obtained by trituration. Some significant difference in FT-IR, melting point and diffraction peaks were introduced by co-crystal phenomenon. These results will provide an experimental basis for the development of new drug co-crystals dosage forms. |
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