Evaluation of Pharmacokinetics Profiles and Bactericidal Activity of Zabofloxacin (Bacteriocide)

Phase I Study of Pharmacokinetics and Bacteriocidal Activity

Phase I clinical study to compare the pharmacokinetic profiles and bactericidal activity of Zabofloxacin 183mg, 367mg and Levofloxacin 250mg after oral administration in healthy volunteer

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Zabofloxacin 183mg; Drug: Levofloxacin 250mg; Drug: Zabofloxacin 367mg

Detailed Description

A Randomized, open label, single dose, crossover phase I clinical study to compare the pharmacokinetic profiles and bactericidal activity of Zabofloxacin 183mg, 367mg and Levofloxacin 250mg after oral administration in healthy volunteer

• Study Type: Interventional
• Enrollment (Actual): 18
• Phase: Phase 1

Contacts and Locations

Study Locations

• Korea, Republic of
  • Jeollabuk-do
    • Jeonju, Jeollabuk-do, Korea, Republic of, 561-712
      • Chonbuk National University Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 19 years to 65 years (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• A healthy adult within the range of 19 to 65 years old at the time of screening
• Body Mass Index(BMI)=17.5~30.5kg/m2, one with weight of more than 55kg (BMI= kg/(m)2)
• Congenital or chronic diseases within the last three years, there is no medical examination results of popular characters with no psychotic symptoms or findings
• Doctor checks conducted hematology, blood chemistry, urinalysis and laboratory tests, including an electrocardiogram(EKG) performed during screening tests such as a suitable test subjects who judged
• The purpose of the test participants prior to testing, information, and to hear about the free will fully explain to participate in this study, according to the Institutional Review Board(IRB)-approved consent form signed by the parties in writing

Exclusion Criteria:

• One with clinically significant blood, kidneys, endocrine, respiratory, gastrointestinal, urinary, cardiovascular, hepatic, psychiatric, neurological or allergic disease (but ,except for untreated seasonal allergies of asymptomatic at the time of administration) with medical history or evidence
• One with gastrointestinal disease(Such as esophageal stricture or achalasia of the esophagus disease, Crohn disease) to affect drug absorption or surgery(but, excluding simple appendectomy or hernia surgery) with medical history
• Alanine Aminotransferase(ALT) or Aspartate Aminotransferase(AST) > 2 times the upper limit of the normal range
• Within 6 months, 210 g / week of alcohol in excess of a history of regular characters (beer (5%) 1 cup (250 mL) = 10 g, soju(20%) 1 cup (50 mL) = 8 g, Wine (12%) 1 cup (125 mL) = 12 g)
• Take part in other clinical trials within two months
• Systolic Blood Pressure(SBP) ≥ 140 mmHg or Diastolic Blood Pressure (DBP) ≥ 90 mmHg
• The great history of alcohol or drug abuse within 1 year
• Taking medication of drug-metabolizing enzymes that are known to significantly induce or inhibit within 30 days
• More than 20 cigarettes a day smoker
• Taking medication of a prescription drug or nonprescription within 10 days,
• Within two months the whole blood donation have, within one month of the apheresis donation have
• Participate in clinical trials to test drug administration and may be at increased risk due to interpretation of test results, or may interfere with severe supply / chronic medical or mental condition or abnormal laboratory test values in character
• Pregnant women and lactating mothers
• Described lifestyle in this protocol can comply with or can not
• One with other investigator judge to unsuitable

Study Plan

How is the study designed?

Design Details

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

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: A Group; 1st oral administration of Zabofloxacin 183mg, 2nd oral administration of Zabofloxacin 367mg and 3rd oral administration of Levofloxacin 250mg	Drug: Zabofloxacin 183mg; Zabofloxacin 183mg single dose; Other Names: Zabolante 183mg; Drug: Levofloxacin 250mg; Levofloxacin 250mg single dose; Other Names: Cravit; Drug: Zabofloxacin 367mg; Zabofloxacin 367mg single dose; Other Names: Zabolante 367mg
EXPERIMENTAL: B Group; 1st oral administration of Zabofloxacin 367mg, 2nd oral administration of Levofloxacin 250mg and 3rd oral administration of Zabofloxacin 367mg	Drug: Zabofloxacin 183mg; Zabofloxacin 183mg single dose; Other Names: Zabolante 183mg; Drug: Levofloxacin 250mg; Levofloxacin 250mg single dose; Other Names: Cravit; Drug: Zabofloxacin 367mg; Zabofloxacin 367mg single dose; Other Names: Zabolante 367mg
EXPERIMENTAL: C Group; 1st oral administration of Levofloxacin 250mg, 2nd oral administration of Zabofloxacin 183mg and 3rd oral administration of Zabofloxacin 367mg	Drug: Zabofloxacin 183mg; Zabofloxacin 183mg single dose; Other Names: Zabolante 183mg; Drug: Levofloxacin 250mg; Levofloxacin 250mg single dose; Other Names: Cravit; Drug: Zabofloxacin 367mg; Zabofloxacin 367mg single dose; Other Names: Zabolante 367mg

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax and AUC	Maximum of Concentration(Cmax) Area Under Plasma Concentration-Time Curve(AUC)	Predose(0), 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic Profile of Plasma	Maximum drug concentration time(Tmax) Half-time(t1/2) Apparent renal clearance(CL/F) Apparent volume of distribution(Vz/F) Mean of Retention Time(MRT)	Predose(0), 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 hours
Pharmacokinetic Profile of Urine	Umax, Cumulative Amount Excreted(Ae), Fraction of the dose excreted unchanged(fe), Renal Clearance(CLr), Urinary Hydrogen exponent(Urinary pH)	Predose(-12-0), 0-6, 6-12, 12-24, 24-36, 48-72, 72-96, 96-120 hours
Bactericidal Activity Profile of Urine	Urinary Bactericidal Titers(UBT) Area under the UBT-versus-time curve(AUBT)	Predose(-12-0), 0-6, 6-12, 12-24, 24-36, 48-72, 72-96, 96-120 hours

Collaborators and Investigators

• Sponsor: Dong Wha Pharmaceutical Co. Ltd.

Study record dates

Study Major Dates

• Study Start: May 1, 2014
• Primary Completion (ACTUAL): August 1, 2014
• Study Completion (ACTUAL): September 1, 2014

Study Registration Dates

• First Submitted: July 11, 2014
• First Submitted That Met QC Criteria: August 6, 2014
• First Posted (ESTIMATE): August 8, 2014

Study Record Updates

• Last Update Posted (ESTIMATE): June 29, 2015
• Last Update Submitted That Met QC Criteria: June 25, 2015
• Last Verified: February 1, 2015

More Information

Terms related to this study

• Keywords: healthy
• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Nucleic Acid Synthesis Inhibitors; Enzyme Inhibitors; Antineoplastic Agents; Topoisomerase II Inhibitors; Topoisomerase Inhibitors; Anti-Bacterial Agents; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 CYP1A2 Inhibitors; Anti-Infective Agents, Urinary; Renal Agents; Levofloxacin; Ofloxacin; Fluoroquinolones
• Other Study ID Numbers: DW224-I-7