Healthy
Conditions
Brief summary
Study conducted to determine and compare the relative bioavailability of two solid oral formulations (reference versus test) of the non-fixed combination of Ticagrelor 90 mg (Brilinta by AstraZeneca S.A. de C.V.) + Acetylsalicylic Acid 100 mg (ASPIRINA JUNIOR by Bayer de México S.A. de C.V.) administered concomitantly versus the fixed-dose combination of Ticagrelor 90 mg / Acetylsalicylic Acid 100 mg manufactured by Laboratorios Silanes S.A. de C.V.
Detailed description
Prospective, longitudinal, open-label, single-dose per period, two treatments two periods, crossover, balanced, randomized study with a 7-day washout period in 20 plus 4 (24) healthy research subjects of both genders, under fasting conditions. In order to establish characterization of the pharmacokinetic parameters Cmax, Tmax, T1/2, Ke, (AUC 0-t) and the (AUC 0-\ ) when administered as a single dose of the non-fixed combination of Ticagrelor 90 mg (Brilinta by AstraZeneca S.A. de C.V.) + Acetylsalicylic Acid 100 mg (ASPIRINA JUNIOR by Bayer de México S.A. de C.V.) as a reference formulation and the fixed-dose combination of Ticagrelor 90 mg/ Acetylsalicylic Acid 100 mg as the test formulation manufactured by Laboratorios Silanes S.A. de C.V.
Interventions
DRUGA1: Ticagrelor / Acetylsalicylic acid in fixed dose combination capsule. (Laboratorios Silanes S.A. de C.V.)
Formula: 90 mg/ 100 mg Pharmaceutical Form: Capsule Dosage: 1 capsule (90 mg/ 100mg) Administration way: oral
DRUGA2: Ticagrelor (BRILINTA®, AstraZeneca S.A. de C.V.) A3: Acetylsalicylic Acid (ASPIRINA JUNIOR®, Bayer de México S.A. de C.V.)
A2: Pharmaceutical Form: Tablet Formula: 90 mg Dosage: 1 tablet of 90 mg Administration way: oral A3: Pharmaceutical Form: Tablet Formula: Each tablet contains 100 mg Dosage: 1 tablet of 100 mg Administration way: oral
Sponsors
Laboratorios Silanes S.A. de C.V.
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Subjects who have given informed consent in writting * Subjects of both genders aged between 18 and 55 years, mexicans, with no background of hypersensitivity or allergies to the drugs under study or related drugs. * Subjects with no background of using anticoagulants of any kind. * Subjects with no background of hepatitis B and/or C. * Vital signs within normal limits, according to international guidelines recorded during selection. * Electrocardiographic trace without evidence of conduction disorders, with RR, PR, QRS, and QT ranges and ST segment values within physiological limits. * Body mass index between 18.0 - 27.0 (kg/m2). * Negative drug abuse test for both men and women. * Negative pregnancy test for women. * All women who agree to participate in the study and who use some form of contraception barrier method such as male or female condoms, copper intrauterine devices (IUDs), or male or female sterilization. * No background of food allergies. * No background of medication use for 14 consecutive days or less than 9 half-lives of the last dose administered of the indicated medication prior to the start of the study. * Background of participation in clinical studies similar to this one within a period of 3 months prior to the study. * No presence of Hepatitis B surface antigens or antibodies against Hepatitis C, HIV, and VDRL core proteins. * No background of alcohol consumption during the study selection period. * No background of donating or losing 450 mL or more of blood within 60 days prior to the study.
Exclusion criteria
* Individuals with hypersensitivity to ticagrelor, acetylsalicylic acid, or any of their components. * Subjects with background of use of anticoagulants. * Subjects with background of hepatitis B and/or C. * Vital signs outside normal limits, according to international guidelines recorded during selection. * Electrocardiogram showing evidence of conduction disturbances, with RR, PR, QRS, and QT intervals and ST segment values within physiological limits. * Body mass index below 18.0 (kg/m2) or above 27.0 (kg/m2). * During the medical history process, the subject indicated background of abuse and dependence on alcohol, psychoactive substances, and chronic use of medications. * Positive drug abuse test for both men and women. * Positive pregnancy test for women. * Background of food allergies. * Background of participation in clinical studies similar to the present study within a period of less than 3 months prior to the study. * Presence of Hepatitis B surface antigens or antibodies against Hepatitis C, HIV, and VDRL core proteins. * Health assessment other than healthy, determined by the results of questioning, physical examination, laboratory tests: blood count, blood chemistry to assess liver and kidney function, fasting lipids and glucose, general urine test, and serology for hepatitis B and C, VDRL, HIV, and electrocardiogram. * In a subordinate relationship with the company or researcher.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Determine Cmax. | Baseline, 0.16, 0.33, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, 24.0 and 48.0 hours. | Evaluate the pharmacokinetics profile of the fixed dose Ticagrelor/Acetylsalicylic Acid employing the maximum observed concentration following the treatment (Cmax), obtained graphically, from the plasma concentration profile with respect to time. |
| Determine AUC 0-t. | Baseline, 0.16, 0.33, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, 24.0 and 48.0 hours. | Evaluate the pharmacokinetics profile of the fixed dose Ticagrelor/Acetylsalicylic Acid employing the area under the curve from time zero to the last measurable concentration (AUC 0-t) using the linear trapezoidal method. |
| Determine AUC 0-inf. | Baseline, 0.16, 0.33, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, 24.0 and 48.0 hours. | Evaluate the pharmacokinetics profile of the fixed dose Ticagrelor/Acetylsalicylic Acid employing the area under the curve from time zero to infinity calculated (AUC 0-inf). |
| Determine Tmax. | Baseline, 0.16, 0.33, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, 24.0 and 48.0 hours. | Evaluate the pharmacokinetics profile of the fixed dose Ticagrelor/Acetylsalicylic Acid employing the time of the maximum measured concentration (tmax) obtained graphically from the plasma concentration profile with respect to time. |
| Determine Ke. | Baseline, 0.16, 0.33, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, 24.0 and 48.0 hours. | Evaluate the pharmacokinetics profile of the fixed dose Ticagrelor/Acetylsalicylic Acid employing the elimination rate (Ke) estimated from the terminal linear portion of the plasma concentration profile with respect to time (on a semi-log scale). |
| Determine T1/2. | Baseline, 0.16, 0.33, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 4.50, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, 24.0 and 48.0 hours. | Evaluate the pharmacokinetics profile of the fixed dose Ticagrelor/Acetylsalicylic Acid employing the half time elimination (t1/2) by the quotient of Ln(2) Ke. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Determine the frequency of occurrence of adverse events | 1, 2, 9 and 11 days. | The percentage of frequency of appearance of each adverse event was evaluated. |
| Adverse events | 1, 2, 9 and 11 days. | Any adverse event were classified by severity, treatment and its relationship with the study drug was evaluated. |
Countries
Mexico
Contacts
PRINCIPAL_INVESTIGATORSusana Tera - Ponce, Dr.
Centro de Estudios Científicos y Clínicos Pharma S.A. de C.V.
Outcome results
None listed