Pharmacology, Clinical
Conditions
Brief summary
To evaluate the bioavailability of a single oral dose of the Acetylsalicylic Acid containing dry powder 500 mg in comparison to the bioavailability of a single oral dose of aspirin tablets and aspirin effervescent tablets in healthy adults.
Interventions
One stick pack containing 500 mg acetylsalicylic acid dry powder
Sponsors
Bayer
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
* Healthy ,male and female subjects 18 to 55 years of age, inclusive * Body Mass Index (BMI) of approximately 18 to 30 kg/m2, and a total body weight \>50 kg (110 lbs) * Results of screening and clinical laboratory tests are within normal limits or considered not clinically significant by the Principal Investigator or Sponsor * Female subjects of childbearing potential must be using a medically acceptable form of birth control for at least 1 month prior to screening (3 months on oral contraceptives), e.g., oral or patch contraceptives, intrauterine device, intramuscular injection or double-barrier and have a negative pregnancy test at Screening and on Day 0 of each treatment period. Female subjects of nonchildbearing potential must be amenorrheic for at least 2 years or had a hysterectomy and/or bilateral oophorectomy.
Exclusion criteria
* History of hypersensitivity to acetylsalicylic acid (ASA), naproxen sodium, acetaminophen, other non-steroidal anti-inflammatory drugs (NSAIDs), and similar pharmacological agents or components of the products * History of gastrointestinal bleeding or perforation, including bleeding related to previous NSAID therapy. Active, or history of recurrent peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding). * Have taken ASA, ASA-containing products, acetaminophen or any other NSAID (OTC or prescription) seven days prior to dosing or during the Treatment Periods, other than study product * Loss of blood in excess of 500 mL within 56 days of the first dose of trial treatment (e.g., donation, plasmapheresis, or injury) * Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic disease, or malignancies * Positive alcohol or drug screen at Screening or on Day 0 of Treatment Periods 1,2 and 3 * Females who are pregnant or lactating
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Plasma concentration of Salicylic Acid (SA) characterized by AUC0-t /AUC0-∞ | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by AUC0-t | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by AUC0-∞ | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | AUC0-∞ : AUC from zero to infinity after single dose. |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by Cmax | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | Cmax: maximum drug concentration in plasma after single dose administration |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by tmax | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | tmax: time to reach maximum drug concentration in plasma after single (first) dose |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by λz (Kel) | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose | λz (Kel) : Apparent terminal rate constant, calculated from the slope of a log-linear regression of the unweighted data considering the last concentration-time points \> LLOQ |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by t1/2 | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by t lag | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | t lag : Lag-time (time delay between drug administration and first observed concentration above LLOQ (Lower limit of quantification) |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by Cmax/AUC0-∞ | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Acetyl salicylic Acid (ASA) characterized by MRT | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | MRT :Mean residence time (for extravascular and iv bolus administration) |
| Plasma concentration of Salicylic Acid (SA) characterized by AUC0-t | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Salicylic Acid (SA) characterized by AUC0-∞ | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | AUC0-∞ : AUC from zero to infinity after single dose |
| Plasma concentration of Salicylic Acid (SA) characterized by Cmax | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | Cmax: maximum drug concentration in plasma after single dose administration |
| Plasma concentration of Salicylic Acid (SA) characterized by tmax | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | tmax: time to reach maximum drug concentration in plasma after single (first) dose |
| Plasma concentration of Salicylic Acid (SA) characterized by λz (Kel) | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | λz (Kel) : Apparent terminal rate constant, calculated from the slope of a log-linear regression of the unweighted data considering the last concentration-time points \> LLOQ |
| Plasma concentration of Salicylic Acid (SA) characterized by t1/2 | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Salicylic Acid (SA) characterized by t lag | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | t lag : Lag-time (time delay between drug administration and first observed concentration above LLOQ |
| Plasma concentration of Salicylic Acid (SA) characterized by Cmax/AUC0-∞ | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
| Plasma concentration of Salicylic Acid (SA) characterized by MRT | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | MRT :Mean residence time (for extravascular and iv bolus administration) |
| Plasma concentration of Acetylsalicylic Acid (ASA) characterized by AUC0-t /AUC0-∞ | baseline (pre-dose), 5, 7.5, 10, 12.5, 15, 17.5, 20, 22.5, 25, 27.5, 30, 32.5, 35, 37.5, 40, 42.5, 45, 50, 55 minutes and 1, 1.25, 1.5, 1.75, 2, 3, 4, 5, 7, 9, 12 and 24 hours post-dose. | — |
Secondary
| Measure | Time frame |
|---|---|
| Number of participants with Adverse Events as measure of safety and tolerability | Up to 5 weeks |
Countries
United States
Outcome results
None listed