Drug-Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Xuejiao Li; Xinna Liu; Jianmin Song; Chenguang Wang; Jinhui Li; Lianchao Liu; Xin He; Xinghua Zhao; Changquan Calvin Sun

doi:10.1021/acs.cgd.1c00229

Drug-Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Xuejiao Li, Xinna Liu, Jianmin Song, Chenguang Wang, Jinhui Li, Lianchao Liu, Xin He, Xinghua Zhao, Changquan Calvin Sun

Pharmaceutics

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

15 Scopus citations

Abstract

The oral delivery of genistein (GEN) is hindered by its low bioavailability. The delivery of tetramethylpyrazine (TMP or ligustrazine) is faced with physical instability challenges due to its high sublimation tendency. We tackled respective challenges of the two drugs by forming a cocrystal. The GEN-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP and a significant enhancement in both the in vitro release rate and bioavailability in rats than GEN. Thus, cocrystallization simultaneously improves pharmaceutical properties of both parent drugs.

Original language	English (US)
Pages (from-to)	3461-3468
Number of pages	8
Journal	Crystal Growth and Design
Volume	21
Issue number	6
DOIs	https://doi.org/10.1021/acs.cgd.1c00229
State	Published - Jun 2 2021

Bibliographical note

Funding Information:
This work was supported by grants from the National Natural Science Foundation of China (Nos. 31872508 and 32002326) and Key Research grants of Hebei (19227505D). We acknowledge the Minnesota Supercomputing Institute at the University of Minnesota for providing resources that contributed to the research results reported within this manuscript. URL: http://www.msi.umn.edu

Publisher Copyright:
© 2021 American Chemical Society

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abstract = "The oral delivery of genistein (GEN) is hindered by its low bioavailability. The delivery of tetramethylpyrazine (TMP or ligustrazine) is faced with physical instability challenges due to its high sublimation tendency. We tackled respective challenges of the two drugs by forming a cocrystal. The GEN-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP and a significant enhancement in both the in vitro release rate and bioavailability in rats than GEN. Thus, cocrystallization simultaneously improves pharmaceutical properties of both parent drugs. ",

author = "Xuejiao Li and Xinna Liu and Jianmin Song and Chenguang Wang and Jinhui Li and Lianchao Liu and Xin He and Xinghua Zhao and Sun, {Changquan Calvin}",

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AU - Li, Xuejiao

AU - Liu, Xinna

AU - Song, Jianmin

AU - Wang, Chenguang

AU - Li, Jinhui

AU - Liu, Lianchao

AU - He, Xin

AU - Zhao, Xinghua

AU - Sun, Changquan Calvin

N1 - Funding Information: This work was supported by grants from the National Natural Science Foundation of China (Nos. 31872508 and 32002326) and Key Research grants of Hebei (19227505D). We acknowledge the Minnesota Supercomputing Institute at the University of Minnesota for providing resources that contributed to the research results reported within this manuscript. URL: http://www.msi.umn.edu Publisher Copyright: © 2021 American Chemical Society

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AB - The oral delivery of genistein (GEN) is hindered by its low bioavailability. The delivery of tetramethylpyrazine (TMP or ligustrazine) is faced with physical instability challenges due to its high sublimation tendency. We tackled respective challenges of the two drugs by forming a cocrystal. The GEN-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP and a significant enhancement in both the in vitro release rate and bioavailability in rats than GEN. Thus, cocrystallization simultaneously improves pharmaceutical properties of both parent drugs.

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Drug-Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

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