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

doi:10.1016/j.ijpharm.2022.121541

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

Pharmaceutics

Research output: Contribution to journal › Article › peer-review

31 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 language	English (US)
Article number	121541
Journal	International journal of pharmaceutics
Volume	616
DOIs	https://doi.org/10.1016/j.ijpharm.2022.121541
State	Published - 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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10.1016/j.ijpharm.2022.121541

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

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.",

keywords = "Antithrombosis, Aspirin, Bioavailability, Cocrystal, Ligustrazine",

author = "Kairu Wang and Yanshuang Hao and Chenguang Wang and Xinghua Zhao and Xin He and Sun, \{Changquan Calvin\}",

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: {\textcopyright} 2022 Elsevier B.V.",

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doi = "10.1016/j.ijpharm.2022.121541",

language = "English (US)",

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TY - JOUR

T1 - Simultaneous improvement of physical stability, dissolution, bioavailability, and antithrombus efficacy of Aspirin and Ligustrazine through cocrystallization

AU - Wang, Kairu

AU - Hao, Yanshuang

AU - Wang, Chenguang

AU - Zhao, Xinghua

AU - He, Xin

AU - Sun, Changquan Calvin

N1 - 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.

PY - 2022/3/25

Y1 - 2022/3/25

N2 - 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.

AB - 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.

KW - Antithrombosis

KW - Aspirin

KW - Bioavailability

KW - Cocrystal

KW - Ligustrazine

UR - https://www.scopus.com/pages/publications/85124258558

UR - https://www.scopus.com/pages/publications/85124258558#tab=citedBy

U2 - 10.1016/j.ijpharm.2022.121541

DO - 10.1016/j.ijpharm.2022.121541

M3 - Article

C2 - 35124115

AN - SCOPUS:85124258558

SN - 0378-5173

VL - 616

JO - International journal of pharmaceutics

JF - International journal of pharmaceutics

M1 - 121541

ER -

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

Abstract

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