Simultaneous taste-masking and oral bioavailability enhancement of Ligustrazine by forming sweet salts

Xinghua Zhao; Qiang Li; Chenguang Wang; Shenye Hu; Xin He; Changquan Calvin Sun

doi:10.1016/j.ijpharm.2020.119089

Simultaneous taste-masking and oral bioavailability enhancement of Ligustrazine by forming sweet salts

Xinghua Zhao, Qiang Li, Chenguang Wang, Shenye Hu, Xin He, Changquan Calvin Sun

Pharmaceutics

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

15 Scopus citations

Abstract

Ligustrazine (or Tetramethylpyrazine, TMP) is an active pharmaceutical ingredient that faces the challenges of bitter taste and low oral bioavailability by the commercial phosphate salt (TMP-Pho). We tackled these challenges by forming salts with two sweeteners, acesulfame (Acs) and saccharine (Sac). Both salts effectively masked the bitter taste of TMP. Compared to TMP-Pho, TMP-Sac shows 43% lower solubility and 11% lower permeability while TMP-Acs shows higher (two-fold) solubility but 24% lower permeability. Both TMP-Acs and TMP-Sac exhibited approximately 40% higher bioavailability through reducing the rate of TMP absorption. Thus, salt formation with both sweeteners simultaneously addressed the challenges brought about by the bitter taste and lower bioavailability of TMP.

Original language	English (US)
Article number	119089
Journal	International journal of pharmaceutics
Volume	577
DOIs	https://doi.org/10.1016/j.ijpharm.2020.119089
State	Published - Mar 15 2020

Bibliographical note

Funding Information:
This work was supported by grants from National Natural Science Foundation of China (No. 31872508 ), Natural Science Foundation of Hebei (No. C2017204085 ), and Key Research grants of Hebei ( 19227505D ).

Publisher Copyright:
© 2020 Elsevier B.V.

Keywords

Absorption
Bioavailability
Ligustrazine
Permeability
Solubility

PubMed: MeSH publication types

Comparative Study
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title = "Simultaneous taste-masking and oral bioavailability enhancement of Ligustrazine by forming sweet salts",

abstract = "Ligustrazine (or Tetramethylpyrazine, TMP) is an active pharmaceutical ingredient that faces the challenges of bitter taste and low oral bioavailability by the commercial phosphate salt (TMP-Pho). We tackled these challenges by forming salts with two sweeteners, acesulfame (Acs) and saccharine (Sac). Both salts effectively masked the bitter taste of TMP. Compared to TMP-Pho, TMP-Sac shows 43% lower solubility and 11% lower permeability while TMP-Acs shows higher (two-fold) solubility but 24% lower permeability. Both TMP-Acs and TMP-Sac exhibited approximately 40% higher bioavailability through reducing the rate of TMP absorption. Thus, salt formation with both sweeteners simultaneously addressed the challenges brought about by the bitter taste and lower bioavailability of TMP.",

keywords = "Absorption, Bioavailability, Ligustrazine, Permeability, Solubility",

author = "Xinghua Zhao and Qiang Li and Chenguang Wang and Shenye Hu and Xin He and Sun, {Changquan Calvin}",

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AU - Zhao, Xinghua

AU - Li, Qiang

AU - Wang, Chenguang

AU - Hu, Shenye

AU - He, Xin

AU - Sun, Changquan Calvin

N1 - Funding Information: This work was supported by grants from National Natural Science Foundation of China (No. 31872508 ), Natural Science Foundation of Hebei (No. C2017204085 ), and Key Research grants of Hebei ( 19227505D ). Publisher Copyright: © 2020 Elsevier B.V.

PY - 2020/3/15

Y1 - 2020/3/15

N2 - Ligustrazine (or Tetramethylpyrazine, TMP) is an active pharmaceutical ingredient that faces the challenges of bitter taste and low oral bioavailability by the commercial phosphate salt (TMP-Pho). We tackled these challenges by forming salts with two sweeteners, acesulfame (Acs) and saccharine (Sac). Both salts effectively masked the bitter taste of TMP. Compared to TMP-Pho, TMP-Sac shows 43% lower solubility and 11% lower permeability while TMP-Acs shows higher (two-fold) solubility but 24% lower permeability. Both TMP-Acs and TMP-Sac exhibited approximately 40% higher bioavailability through reducing the rate of TMP absorption. Thus, salt formation with both sweeteners simultaneously addressed the challenges brought about by the bitter taste and lower bioavailability of TMP.

AB - Ligustrazine (or Tetramethylpyrazine, TMP) is an active pharmaceutical ingredient that faces the challenges of bitter taste and low oral bioavailability by the commercial phosphate salt (TMP-Pho). We tackled these challenges by forming salts with two sweeteners, acesulfame (Acs) and saccharine (Sac). Both salts effectively masked the bitter taste of TMP. Compared to TMP-Pho, TMP-Sac shows 43% lower solubility and 11% lower permeability while TMP-Acs shows higher (two-fold) solubility but 24% lower permeability. Both TMP-Acs and TMP-Sac exhibited approximately 40% higher bioavailability through reducing the rate of TMP absorption. Thus, salt formation with both sweeteners simultaneously addressed the challenges brought about by the bitter taste and lower bioavailability of TMP.

KW - Absorption

KW - Bioavailability

KW - Ligustrazine

KW - Permeability

KW - Solubility

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Simultaneous taste-masking and oral bioavailability enhancement of Ligustrazine by forming sweet salts

Abstract

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