College of Veterinary Medicine, Hebei Agricultural University, Baoding, Hebei 071000, China.
College of Animal Science and Technology, Hebei Agricultural University, Baoding, Hebei 071000, China.
Int J Pharm. 2022 Mar 25;616:121541. doi: 10.1016/j.ijpharm.2022.121541. Epub 2022 Feb 3.
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.
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。