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)|
|Journal||International journal of pharmaceutics|
|State||Published - Mar 15 2020|
Bibliographical noteFunding 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 ).
© 2020 Elsevier B.V.
PubMed: MeSH publication types
- Comparative Study
- Journal Article