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通过共结晶同时提高阿司匹林和川芎嗪的物理稳定性、溶解性能、生物利用度和抗血栓功效。

Simultaneous improvement of physical stability, dissolution, bioavailability, and antithrombus efficacy of Aspirin and Ligustrazine through cocrystallization.

机构信息

College of Veterinary Medicine, Hebei Agricultural University, Baoding, Hebei 071000, China.

College of Animal Science and Technology, Hebei Agricultural University, Baoding, Hebei 071000, China.

出版信息

Int J Pharm. 2022 Mar 25;616:121541. doi: 10.1016/j.ijpharm.2022.121541. Epub 2022 Feb 3.

Abstract

A novel 1:1 cocrystal between two cardiovascular drugs, aspirin (ASA) and ligustrazine (tetramethylpyrazine, TMP) has been synthesized and characterized. The structure of this drug-drug cocrystal, ASA-TMP, was determined using single crystal X-ray crystallography. The ASA-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP. Importantly, cocrystallization simultaneously improves bioavailability of both parent drugs. This suggests the possibility of developing a more effective antithrombosis drug therapy given the synergistic pharmacological effects of the two parent drugs.

摘要

一种新型的 1:1 共晶化合物由两种心血管药物,阿司匹林(ASA)和川芎嗪(四甲基吡嗪,TMP)合成并进行了表征。通过单晶 X 射线晶体学确定了这种药物共晶化合物 ASA-TMP 的结构。ASA-TMP 共晶的升华趋势明显低于 TMP。重要的是,共晶化同时提高了两种母体药物的生物利用度。鉴于两种母体药物的协同药理作用,这提示有可能开发出更有效的抗血栓形成药物治疗方法。

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