Bioequivalence Study of Ticagrelor Tablet in Healthy Volunteers
Abstract
Aim: To evaluate the comparative oral bioavailability of single dose of Tigemac® Tablets 90 mg (Ticagrelor
manufactured by Macleods Pharmaceuticals Ltd., India) with Brilinta® Tablets 90 mg (Ticagrelor manufactured
by AstraZeneca Pharmaceuticals LP, USA) in healthy, adult, human volunteers under fasting condition.
Additionally, safety and tolerability of test and reference products were also evaluated.
Methods: This was an open label, balanced, analyst blind, randomized, two-treatment, two-period, twosequence,
single dose, crossover bioequivalence study with 7 days wash out period in 24 healthy, adult,
human volunteers. The study compared oral bioavailability of two formulations Tigemac® (Test Product)
versus Brilinta® (Reference product) in a single dose administered in fasting condition.
Results: The 90% confidence intervals for the ratio (Test/Reference) of Cmax and AUC0-48 for Tigemac® tablet
were within the acceptable limits of bioequivalence 80.00% - 125.00%. The ratios (T/R) of Cmax and
AUC0-48 for ticagrelor were found to be 96.88% and 101.84% respectively. Similarly, the ratios (T/R) of Cmax
and AUC0-48 for ticagrelor active metabolite (deshydroxyethoxy ticagrelor [ARC124910XX]) were found to be
104.03% and 105.77% respectively. The highest intra subject C.V. for ticagrelor was observed to be 14.95%.
No adverse event occurred during the study period while two adverse events were reported during post
study assessments. Both test and reference products were safe and well tolerated in fasting condition.
Conclusion: Tigemac® the test formulation was found to bioequivalent with the reference product Brilinta® in
healthy, adult, human volunteers under fasting condition.
Registration: 35-5/WZ-2017/BE EXP/Macleods-12
Conflict of Interest: All authors have authored this manuscript in the capacity of paid employees of Macleods
Pharmaceuticals Limited. Mumbai, India.
Funding Source: Macleods Pharmaceuticals Limited, Mumbai, India.
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