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. (Icicle)

An Open Label Crossover Pharmacokinetic Trial of Aspirin Dry Powder Versus Aspirin Tablets and Aspirin Effervescent Tablets in Healthy Adult Subjects

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.

Study Overview

• Status: Completed
• Conditions: Pharmacology, Clinical
• Intervention / Treatment: Drug: Aspirin (Acetylsalicylic acid, BAYe4465); Drug: Aspirin (Acetylsalicylic acid, BAYe4465); Drug: Aspirin (Acetylsalicylic acid, BAYe4465)

• Study Type: Interventional
• Enrollment (Actual): 30
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • New Jersey
    • Hackensack, New Jersey, United States, 07601

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

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

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Aspirin dry powder; 500 mg Acetylsalicylic Acid (ASA) dry powder	Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One stick pack containing 500 mg acetylsalicylic acid dry powder; Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One tablet containing 500 mg acetylsalicylic acid; Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One effervescent tablet containing 500 mg acetylsalicylic acid
Active Comparator: Aspirin coated tablet; 500 mg ASA coated tablet	Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One stick pack containing 500 mg acetylsalicylic acid dry powder; Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One tablet containing 500 mg acetylsalicylic acid; Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One effervescent tablet containing 500 mg acetylsalicylic acid
Active Comparator: Aspirin effervescent tablet; 500 mg ASA effervescent tablet	Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One stick pack containing 500 mg acetylsalicylic acid dry powder; Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One tablet containing 500 mg acetylsalicylic acid; Drug: Aspirin (Acetylsalicylic acid, BAYe4465); One effervescent tablet containing 500 mg acetylsalicylic acid

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
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 Outcome Measures

Outcome Measure	Time Frame
Number of participants with Adverse Events as measure of safety and tolerability	Up to 5 weeks

Collaborators and Investigators

• Sponsor: Bayer

Study record dates

Study Major Dates

• Study Start: February 1, 2015
• Primary Completion (Actual): March 1, 2015
• Study Completion (Actual): March 1, 2015

Study Registration Dates

• First Submitted: March 14, 2015
• First Submitted That Met QC Criteria: March 14, 2015
• First Posted (Estimate): March 20, 2015

Study Record Updates

• Last Update Posted (Estimate): September 19, 2016
• Last Update Submitted That Met QC Criteria: September 16, 2016
• Last Verified: September 1, 2016

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Peripheral Nervous System Agents; Enzyme Inhibitors; Analgesics; Sensory System Agents; Anti-Inflammatory Agents, Non-Steroidal; Analgesics, Non-Narcotic; Anti-Inflammatory Agents; Antirheumatic Agents; Fibrinolytic Agents; Fibrin Modulating Agents; Platelet Aggregation Inhibitors; Cyclooxygenase Inhibitors; Antipyretics; Aspirin
• Other Study ID Numbers: 17494