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

Research output: Contribution to journalArticlepeer-review

5 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 languageEnglish (US)
Article number119089
JournalInternational journal of pharmaceutics
Volume577
DOIs
StatePublished - 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
  • Journal Article

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