A Bioequivalence Study of Film-coated Tablet and Dry Syrup 1% Form for E2020 in Healthy Japanese Adult Males

The purpose of this study is to confirm bioequivalence between E2020 dry syrup 1% form (0.5 g), given either with 200 mL of water or suspended in 20 mL of water, and E2020 film-coated tablet (5 mg) in Japanese healthy adult males.

Study Overview

• Status: Completed
• Conditions: Healthy Adult
• Intervention / Treatment: Drug: Donepezil Hydrochloride; Drug: Donepezil Hydrochloride; Drug: Donepezil Hydrochloride

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Tokyo
    • Sumida-ku, Tokyo, Japan

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 44 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria

Those who meet all below criteria are eligible to enroll in this study;

1. Those who provide consent by their own will.
2. Male subjects aged between ≥ 20 years and < 45 years old at the time of obtaining informed consent and non-smoker (subjects who have not been smoking for at least 4 weeks prior to study treatment)
3. BMI at screening is 18.5 kg/m2 or above and less than 25.0 kg/m2
4. Those who are willing to and can comply with the conditions described in the study protocol.

Exclusion Criteria

Those who meet any of the below criteria will be excluded from the study.

1. Any significant medical illness that required intervention within 8 weeks before treatment, or any medical history of clinically significant infectious diseases within 4 weeks before treatment.
2. Those who had any psychiatric, GI tract, hepatic, renal, respiratory, endocrine, hematological, neurological, cardiovascular diseases or congenital metabolic disorders within 4 weeks before study drug administration that may have an impact on the evaluation of the drug.
3. Subjects who have any medical history of GI, hepatic, or renal surgery (e.g. excision of liver, kidney or GI tract) that may have an impact on pharmacokinetics of the drug.
4. Subjects who have any history of medically significant allergy to medications or foods, and those who currently have any symptoms of seasonal
5. Subjects whose weight changes were more than 10% from the screening phase to study drug administration.
6. Those with clinical abnormal symptoms, medical history of organ dysfunction, subjective symptoms, objective findings, vital signs, and abnormal EKG or clinical laboratory test values, which need medical intervention.
7. Corrected change in QT wave (QTc) interval of > 450 msec with 12-lead EKG at screening or study drug administration.
8. Subjects who are positive for hepatitis B surface antigen (HBs antigen), hepatitis C (HCV) antibody, or serologic test for syphilis (STS).
9. Subjects who are suspected with or who has a history of drug or alcohol abuse, or positive urine screen for drugs of abuse or exhalation alcohol test at screening or baseline.
10. Subjects who consumed caffeine-containing food or beverages within 72 hours before study drug administration.
11. Exposure to any supplements or herbs (including Chinese medicine), or beverages (e.g. alcohol or grapefruit-containing beverages, within 2 weeks of study drug administration.
12. Exposure to St. John's wort containing medications within 4 weeks of study drug administration.
13. Use of any prescription drugs within 4 week before study drug administration.
14. Use of any OTC medications within 2 week before study drug administration.
15. Subjects who enrolled in another clinical trial and exposed to any investigational drug within 16 weeks of study enrollment.
16. Subjects who received blood infusion within 12 weeks, those who had blood drawn 400 mL or more within 12 weeks, 400 mL, or 200 mL or more within 4 weeks, or sampling of a component of the blood within 2 week of study drug administration.
17. Subjects who performed extreme exercises or exhausting labors (more than 1 hr/day or 5 day/week) within 2 weeks before hospitalization.
18. Any subject who, or whose partner, does not want to take highly reliable contraceptive measures until the end of the post-treatment examination.
19. Subjects who are inappropriate to participate in the study, as judged by the investigator or subinvestigator

Study Plan

How is the study designed?

Design Details

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

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: 2	Drug: Donepezil Hydrochloride; Drug E2020 film-coated tablet: E2020 film-coated tablet (5mg) orally administered in a single dose with 200 mL water.; Drug: Donepezil Hydrochloride; Drug E2020 dry syrup 1% form (suspended): E2020 dry syrup 1% (0.5 g) will be orally administered in a single dose after suspended in 20 ml water.; Drug: Donepezil Hydrochloride; Drug E2020 dry syrup 1% form: E2020 dry syrup 1% (0.5 g) will be orally administered in a single dose with 200 mL water.
Active Comparator: 1	Drug: Donepezil Hydrochloride; Drug E2020 film-coated tablet: E2020 film-coated tablet (5mg) orally administered in a single dose with 200 mL water.; Drug: Donepezil Hydrochloride; Drug E2020 dry syrup 1% form (suspended): E2020 dry syrup 1% (0.5 g) will be orally administered in a single dose after suspended in 20 ml water.; Drug: Donepezil Hydrochloride; Drug E2020 dry syrup 1% form: E2020 dry syrup 1% (0.5 g) will be orally administered in a single dose with 200 mL water.
Active Comparator: 3	Drug: Donepezil Hydrochloride; Drug E2020 film-coated tablet: E2020 film-coated tablet (5mg) orally administered in a single dose with 200 mL water.; Drug: Donepezil Hydrochloride; Drug E2020 dry syrup 1% form (suspended): E2020 dry syrup 1% (0.5 g) will be orally administered in a single dose after suspended in 20 ml water.; Drug: Donepezil Hydrochloride; Drug E2020 dry syrup 1% form: E2020 dry syrup 1% (0.5 g) will be orally administered in a single dose with 200 mL water.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
PK Parameter Cmax, calculated from plasma E2020 concentration by a non-compartmental analysis, will be evaluated.	Up to 168 hrs after administration
PK Parameter AUC (0-168), calculated from plasma E2020 concentration by a non-compartmental analysis, will be evaluated.	Up to 168 hrs after administration

Collaborators and Investigators

• Sponsor: Eisai Co., Ltd.
• Investigators: Study Director: Hiroki Shimizu, Eisai Co., Ltd.

Study record dates

Study Major Dates

• Study Start: March 1, 2011
• Primary Completion (Actual): May 1, 2011
• Study Completion (Actual): May 1, 2011

Study Registration Dates

• First Submitted: January 6, 2012
• First Submitted That Met QC Criteria: January 9, 2012
• First Posted (Estimate): January 10, 2012

Study Record Updates

• Last Update Posted (Estimate): January 10, 2012
• Last Update Submitted That Met QC Criteria: January 9, 2012
• Last Verified: January 1, 2012

More Information

Terms related to this study

• Keywords: Bioequivalence; Healthy Subjects; Donepezil
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Cholinergic Agents; Enzyme Inhibitors; Nootropic Agents; Cholinesterase Inhibitors; Donepezil
• Other Study ID Numbers: E2020-J081-033

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No