Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0235290 (
bitter taste
)
1,408
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
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
.
...
PMID:Simultaneous taste-masking and oral bioavailability enhancement of Ligustrazine by forming sweet salts. 3200 Dec 92
