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Bioequivalence Study of Ticagrelor Tablet in Healthy Volunteers
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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.
Keywords
- Bassand JP, Hamm CW, Ardissino D, Boersma E, Budaj A, Fernández-Avilés F, Fox KA, Hasdai D, Ohman EM, Wallentin L, Wijns W. Guidelines for the diagnosis and treatment of non-ST-segment elevation acute coronary syndromes: The Task Force for the Diagnosis and Treatment of Non-ST-Segment Elevation Acute Coronary Syndromes of the European Society of Cardiology. European heart journal. 2007 Jun 14;28(13):1598-660.
- National Institute for Clinical Excellence (NICE). Post myocardial infarction secondary prevention in primary and secondary care for patients following a myocardial infarction: full guideline. May 2007. Available athttp://www.nice.org.uk/nicemedia/pdf/CG48FullGuideline.pdf.
- Gurbel PA, Bliden KP. Durability of platelet inhibition by clopidogrel. American Journal of Cardiology. 2003 May 1; 91(9):1123-5.
- Angiolillo DJ, Fernandez-Ortiz A, Bernardo E, Alfonso F, Macaya C, Bass TA, Costa MA. Variability in individual responsiveness to clopidogrel: clinical implications, management, and future perspectives. Journal of the American College of Cardiology. 2007 Apr 10;49(14):1505-16.
- Wiviott SD, Braunwald E, McCabe CH, Montalescot G, Ruzyllo W, Gottlieb S, Neumann FJ, Ardissino D, De Servi S, Murphy SA, Riesmeyer J. Prasugrel versus clopidogrel in patients with acute coronary syndromes. New England Journal of Medicine. 2007 Nov 15;357(20):2001-15.
- Roffman DS. Developments in oral antiplatelet agents for the treatment of acute coronary syndromes: Clopidogrel, prasugrel, and ticagrelor. Journal of pharmacy practice. 2016 Jun;29(3):239-49.
- Nilsson L, Van Giezen JJ, Greasley PJ. Evidence for distinct ligand binding sites on recombinant human P2Y12 receptors.
- Storey RF, Husted S, Harrington RA, Heptinstall S, Wilcox RG, Peters G, Wickens M, Emanuelsson H, Gurbel P, Grande P, Cannon CP. Inhibition of platelet aggregation by AZD6140, a reversible oral P2Y12receptor antagonist, compared with clopidogrel in patients with acute coronary syndromes. Journal of the American College of Cardiology. 2007 Nov 6;50(19):1852-6.
- James S, Åkerblom A, Cannon CP, Emanuelsson H, Husted S, Katus H, Skene A, Steg PG, Storey RF, Harrington R, Becker R. Comparison of ticagrelor, the first reversible oral P2Y12 receptor antagonist, with clopidogrel in patients with acute coronary syndromes: rationale, design, and baseline characteristics of the PLATelet inhibition and patient Outcomes (PLATO) trial. American heart journal. 2009 Apr 1;157(4):599-605.
- Food and Drug Administration. Guidance for industry Statistical approaches to Establishing Bioequivalence. 2001.
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