This is a Phase 1 Relative Bioavailability Study Comparing The Pharmacokinetics Of Aramchol Meglumine (AM) Granules For Oral Suspension To Aramchol Free Acid (AA) 300 mg Tablets In Healthy Volunteers
A single center, 3-period, open-label, crossover study in healthy male and female volunteers who will receive 2 single doses of Aramchol meglumine (AM) and 1 single dose of Aramchol free acid (AA) under fasting conditions. A single 400 mg dose of Aramchol meglumine (AM; Test 1) will be administered to all study subjects in Period 1. The second dose of Aramchol meglumine (AM) will be between 200 mg and 800 mg and will be selected after review of the pharmacokinetics (PK) from Period 1. In Periods 2 and 3, study subjects will be randomized 1:1 to receive the second dose of Aramchol meglumine (AM; Test 2) in one period and a 300 mg tablet of Aramchol free acid (AA; Reference) in the other period. Each product will be given under fasting conditions. The study periods will be separated by a wash-out period of at least 14 days.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
16
Aramchol meglumine is a salt form of Aramchol free acid
Aramchol free acid is a fatty acid-bile acid conjugate
Diagnostic & Consultative Centre 'Ascendent' Ltd.
Sofia, Bulgaria
Cmax of Aramchol
Observed maximal concentration after administration
Time frame: 8 days 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
AUClast of Aramchol
Area under the concentration/time curve to the last measurable concentration, calculated by the trapezoidal rule from time 0 h to last observed concentration at time t
Time frame: 8 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
AUCinf of Aramchol
Area under the concentration/time curve, from time 0 h extrapolated to infinity
Time frame: 8 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
Tmax of Aramchol
Observed time point of maximal concentration
Time frame: 24 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
λz of Aramchol
Terminal rate constant in both study periods
Time frame: 8 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
t½ of Aramchol
Plasma concentration half-life
Time frame: 24 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
CL/F of Aramchol
Clearance per fraction of bioavailability
Time frame: 24 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
VZ/F of Aramchol
Volume of distribution per fraction of bioavailability
Time frame: 24 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.
%AUCextrap of Aramchol
The percentage of the area under the concentration-time curve (%AUC) that is extrapolated beyond the last observed data point
Time frame: 24 days. 19 blood samples were drawn in each study period: within 10 minutes pre-dose and 2, 3, 4, 6, 8, 10, 12,14, 18, 24, 30, 36, 48 (Day 3), 72 (Day 4), 96 (Day 5), 120 (Day 6), 144(Day 7), 168 hours (Day 8) post-dose.