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受中药复方制剂启发,由厚朴酚与川芎嗪制备得到的药物 - 药物共晶和共无定形物。

A drug-drug cocrystal and a co-amorphous form, prepared from honokiol and ligustrazine, inspired by Chinese patent medicine.

作者信息

Zhang Yanli, Liu Hui, Chen Zongxin, Meng Jialei, Li Yunfeng, Qi Luyao, Zhang Suiliang, Chen Xiaofeng, Lei Ming

机构信息

Seventh People's Hospital of Shanghai University of Traditional Chinese Medicine, 358 Datong Road, Shanghai, 200137, People's Republic of China.

Shanghai General Hospital affiliated to Shanghai Jiaotong University, 100 Haining Road, Shanghai, 200080, People's Republic of China.

出版信息

Acta Crystallogr B Struct Sci Cryst Eng Mater. 2023 Dec 1;79(Pt 6):519-524. doi: 10.1107/S2052520623008648. Epub 2023 Nov 15.

DOI:10.1107/S2052520623008648
PMID:37966478
Abstract

A drug-drug cocrystal created with two antithrombotic-active ingredients from herbs, honokiol (HON) and ligustrazine (TMP, 1:1), was synthesized and characterized. The structure of HON-TMP (1:1) was determined by single-crystal X-ray diffraction. Then co-amorphous HON-TMP was prepared by honey-assisted grinding, which was inspired by a grinding process for a Chinese patent medicine-Shijunzi honey pill. This co-amorphous drug-drug cocrystal (20% honey) exhibits improved solubility over HON and a significantly reduced sublimation tendency than TMP.

摘要

由两种具有抗血栓活性的草本成分厚朴酚(HON)和川芎嗪(TMP,1:1)制备的药物-药物共晶体被合成并进行了表征。通过单晶X射线衍射确定了HON-TMP(1:1)的结构。然后受中成药柿君子女蜜丸研磨工艺启发,采用蜂蜜辅助研磨法制备了共非晶态的HON-TMP。这种共非晶态药物-药物共晶体(含20%蜂蜜)相比厚朴酚具有更好的溶解性,相比川芎嗪升华趋势显著降低。

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引用本文的文献

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New Cocrystals of Ligustrazine: Enhancing Hygroscopicity and Stability.川芎嗪新共晶:提高吸湿性和稳定性。
Molecules. 2024 May 8;29(10):2208. doi: 10.3390/molecules29102208.