Sarpogrelate Drug Interaction

A Randomized, Open-label, Three-sequence, Three-period Crossover Study to Investigate The Effect of Anplag on the Disposition of Betaloc in Healthy Male Volunteers

This is a randomized, open-label, single & multiple-dose, three-sequence, three-period crossover study to investigate the effect of sarpogrelate hydrochloride on the disposition of metoprolol tartrate in healthy male volunteers

Study Overview

• Status: Completed
• Conditions: Hypertension; Peripheral Artery Disease
• Intervention / Treatment: Drug: Sarpogrelate pretreatment; Drug: Sarpogrelate; Drug: Metoprolol

Detailed Description

Eligibility for participation of this study will be determined from demographic information, medical history, physical examination, electrocardiogram (ECG) and clinical laboratory tests within 4 weeks before study drug administration. Subjects suitable for this study will be admitted to the Clinical Trial Center of Ajou University Medical Center on the day before dosing (Day -1).

On Day 1, Subjects will be dosed study drug (metoprolol tartrate 100 mg once a day only, or metoprolol tartrate 100 mg once a day with sarpogrelate hydrochloride 100 mg three times a day, sarpogrelate hydrochloride 100 mg three times a day pretreatment for three days and metoprolol tartrate 100 mg once a day with sarpogrelate hydrochloride 100 mg three times a day).

Pharmacokinetic samplings and blood pressure/pulse rate measurement will be done upto 12 hours after metoprolol tartrate 100 mg dosing.

After one week of washout period (Day 8), Subjects will be dosed study drug by crossover manner, and pharmacokinetic samplings and blood pressure/pulse rate measurement will be done upto 12 hours after metoprolol tartrate 100 mg dosing.

After one week of washout period (Day 15), Subjects will be dosed study drug by crossover manner, and pharmacokinetic samplings and blood pressure/pulse rate measurement will be done upto 12 hours after metoprolol tartrate 100 mg dosing.

• Study Type: Interventional
• Enrollment (Anticipated): 9
• Phase: Phase 1

Contacts and Locations

Study Locations

• Korea, Republic of
  • Gyeonggi
    • Suwon, Gyeonggi, Korea, Republic of, 433-721
      • Ajou University School of Medicine

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 45 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects aged 20 - 45 years
• With in 20% of ideal body weight, {Ideal body weight=[height(cm)-100]*0.9}
• Agreement with written informed consent

Exclusion Criteria:

• Clinically significant cardiovascular, pulmonary, hepatic, renal, hematologic, gastrointestinal disease or mental disorder (Past history or present)
• Inadequate result of laboratory test (especially, AST/ALT > 1.25 x UNL, Total bilirubin > 1.5 x UNL)
• Positive reaction in the HBs Ag, anti-HCV Ab, anti-HIV Ab, VDRL test
• Taking OTC(Over the counter)medicine including oriental medicine within 7 days
• Clinically significant allergic disease (Except for mild allergic rhinitis and dermatitis seems to be not need for medication)
• Subject with known for hypersensitivity reaction to Metoprolol or Sarpogrelate
• Previous whole blood donation within 60 days or component blood donation within 30 days
• Previous participation of other trial within 90 days
• Continued taking caffeine (caffeine > 5 cup/day), drinking (alcohol > 30 g/day) and severe heavy smoker (cigarette > 1/2 pack per day)
• An impossible one who participates in clinical trial by investigator's decision including for reason of laboratory test result

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Sarpogrelate pretreatment and Metoprolol; Sarpogrelate hydrochloride 100 mg pretreatment three times a day for three days and Metoprolol Tartrate 100 mg once a day with Sarpogrelate hydrochloride 100 mg three times a day	Drug: Sarpogrelate pretreatment; Sarpogrelate hydrochloride 100 mg pretreatment three times a day for three days; Drug: Sarpogrelate; Sarpogrelate hydrochloride 100 mg three times a day; Drug: Metoprolol; Metoprolol Tartrate 100 mg once a day
ACTIVE_COMPARATOR: Sarpogrelate and Metoprolol; Metoprolol Tartrate 100 mg once a day with Sarpogrelate hydrochloride 100 mg three times a day	Drug: Sarpogrelate; Sarpogrelate hydrochloride 100 mg three times a day; Drug: Metoprolol; Metoprolol Tartrate 100 mg once a day
ACTIVE_COMPARATOR: Metoprolol only; Metoprolol Tartrate 100 mg once a day	Drug: Metoprolol; Metoprolol Tartrate 100 mg once a day

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Plasma concentration of Metoprolol and metabolites	Cmax (maximal plasma concentration) and AUC (area under the time-concentration curve) will be calculated from pharmacokinetic samplings	upto 12 hours after Metoprolol Tartrate 100 mg dosing

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Blood pressure and pulse rate changes	Blood pressure and pulse rate measurement with Dash 5000 patient monitoring system (GE Healthcare, USA) at 0 (before Metoprolol Tartrate 100 mg dosing), 1, 2, 3, 4, 5, 6, 8, 10, 12 hours after Metoprolol Tartrate 100 mg dosing	Upto 12 hours after Metoprolol Tartrate 100 mg dosing

Collaborators and Investigators

• Sponsor: Ajou University School of Medicine

Study record dates

Study Major Dates

• Study Start: December 1, 2013
• Primary Completion (ACTUAL): January 1, 2014
• Study Completion (ACTUAL): December 1, 2014

Study Registration Dates

• First Submitted: March 25, 2014
• First Submitted That Met QC Criteria: March 25, 2014
• First Posted (ESTIMATE): March 27, 2014

Study Record Updates

• Last Update Posted (ESTIMATE): February 25, 2015
• Last Update Submitted That Met QC Criteria: February 23, 2015
• Last Verified: February 1, 2015

More Information

Terms related to this study

• Keywords: Pharmacokinetics; Pharmacodynamics; Drug-drug interaction
• Additional Relevant MeSH Terms: Cardiovascular Diseases; Vascular Diseases; Arteriosclerosis; Arterial Occlusive Diseases; Atherosclerosis; Peripheral Vascular Diseases; Peripheral Arterial Disease; Physiological Effects of Drugs; Adrenergic beta-Antagonists; Adrenergic Antagonists; Adrenergic Agents; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Anti-Arrhythmia Agents; Antihypertensive Agents; Autonomic Agents; Peripheral Nervous System Agents; Fibrinolytic Agents; Fibrin Modulating Agents; Platelet Aggregation Inhibitors; Serotonin Agents; Serotonin Antagonists; Sympatholytics; Adrenergic beta-1 Receptor Antagonists; Metoprolol; Sarpogrelate
• Other Study ID Numbers: DDI-102