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

Kairu Wang, Yanshuang Hao, Chenguang Wang, Xinghua Zhao, Xin He, Changquan Calvin Sun

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

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.

Original languageEnglish (US)
Article number121541
JournalInternational journal of pharmaceutics
Volume616
DOIs
StatePublished - Mar 25 2022

Bibliographical note

Funding Information:
This work was supported by grants from the National Natural Science Foundation of China (Nos. 32002326 and 32172898 ) and Key Research grants of Hebei ( 19227505D ), China. We thank the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing the resources that contributed to the research results reported within this paper ( http://www.msi.umn.edu ).

Publisher Copyright:
© 2022 Elsevier B.V.

Keywords

  • Antithrombosis
  • Aspirin
  • Bioavailability
  • Cocrystal
  • Ligustrazine

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