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.

NCT02394093 | Completed Phase 1

• 1 other identifier: 17494
• Study Type: interventional
• Target: 30
• Locations: 1 country
• Sites: 1

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.

Conditions

Pharmacology, Clinical

Outcome Measures

Primary Outcomes (20)

• 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-∞

  AUC0-∞ : AUC from zero to infinity after single dose.

  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 Cmax

  Cmax: maximum drug concentration in plasma after single dose administration

  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 tmax

  tmax: time to reach maximum drug concentration in plasma after single (first) dose

  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 λz (Kel)

  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

  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 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

  t lag : Lag-time (time delay between drug administration and first observed concentration above LLOQ (Lower limit of quantification)

  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 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

  MRT :Mean residence time (for extravascular and iv bolus administration)

  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-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-∞

  AUC0-∞ : AUC from zero to infinity after single dose

  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 Cmax

  Cmax: maximum drug concentration in plasma after single dose administration

  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 tmax

  tmax: time to reach maximum drug concentration in plasma after single (first) dose

  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 λz (Kel)

  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

  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 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

  t lag : Lag-time (time delay between drug administration and first observed concentration above LLOQ

  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 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

  MRT :Mean residence time (for extravascular and iv bolus administration)

  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 /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 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 Outcomes (1)

• Number of participants with Adverse Events as measure of safety and tolerability

  Up to 5 weeks

Study Arms (3)

Aspirin dry powder

EXPERIMENTAL

500 mg Acetylsalicylic Acid (ASA) dry powder

Drug: Aspirin (Acetylsalicylic acid, BAYe4465)

Aspirin coated tablet

ACTIVE COMPARATOR

500 mg ASA coated tablet

Drug: Aspirin (Acetylsalicylic acid, BAYe4465)

Aspirin effervescent tablet

ACTIVE COMPARATOR

500 mg ASA effervescent tablet

Drug: Aspirin (Acetylsalicylic acid, BAYe4465)

Interventions

Aspirin (Acetylsalicylic acid, BAYe4465) DRUG

One stick pack containing 500 mg acetylsalicylic acid dry powder

Aspirin dry powder

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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

Sponsors & Collaborators

• Bayer: lead

Study Sites (1)

Unknown Facility

Hackensack, New Jersey, 07601, United States

Location

MeSH Terms

Interventions

Aspirin

Intervention Hierarchy (Ancestors)

Salicylates; Hydroxybenzoates; Phenols; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; Hydrocarbons; Organic Chemicals

Study Officials

• Bayer Study Director

  Bayer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 14, 2015
• First Posted: March 20, 2015
• Study Start: February 1, 2015
• Primary Completion: March 1, 2015
• Study Completion: March 1, 2015
• Last Updated: September 19, 2016

Record last verified: 2016-09

Locations

US (1)