Simultaneous improvement of physical stability, dissolution, bioavailability, and antithrombus efficacy of Aspirin and Ligustrazine through cocrystallization.
Simultaneous improvement of physical stability, dissolution, bioavailability, and antithrombus efficacy of Aspirin and Ligustrazine through cocrystallization.
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DOI：
10.1016/j.ijpharm.2022.121541
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发表时间：
2022-02
影响因子：
5.8
通讯作者：
Kairu Wang;Yanshuang Hao;Chenguang Wang;Xinghua Zhao;Xin He;Changquan Calvin Sun
中科院分区：
文献类型：
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作者：
Kairu Wang;Yanshuang Hao;Chenguang Wang;Xinghua Zhao;Xin He;Changquan Calvin Sun
合成并表征了一种新型的心血管药物阿司匹林（阿萨）和川芎嗪（TMP）1：1共晶。使用单晶X射线晶体学确定该药物-药物共晶体ASA-TMP的结构。ASA-TMP共晶表现出比TMP显著降低的升华倾向。重要的是，共结晶同时提高了两种母体药物的生物利用度。这表明，鉴于两种母体药物的协同药理作用，开发更有效的抗血栓形成药物治疗的可能性。
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.