Pharmacokinetics Study of Zolpidem Hemitartarate Orodispersible Tablet 1.75 mg Formulation

Pharmacokinetics Study of Zolpidem Hemitartarate Orodispersible Tablet 1.75 mg Formulation, With Fasting and Postprandial Administration, in Male and Female Healthy Volunteers, Produced by Biolab Sanus Farmacêutica Ltda

The purpose of this study is to evaluate the pharmacokinetics of the new formulation of zolpidem hemitartarate orodispersible tablet 1.75 mg in male and female healthy volunteers.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: zolpidem hemitartarate 1.75 mg - Sequency 1; Drug: zolpidem hemitartarate 1.75 mg - Sequency 2

Detailed Description

This is a phase I study of zolpidem hemitartarate orodispersible tablet 1.75 mg in fasting and postprandial administration. Sample size is 28 healthy volunteers, male and female, aged from 18 to 50 years old.

This is an open-label, randomized, crossover study. Each volunteer will be randomized to one of the following sequencies:

Sequency 1: zolpidem hemitartarate 1.75 mg in fasting (period 1) and zolpidem hemitartarate 1.75 mg postprandial (period 2) Sequency 2: zolpidem hemitartarate 1.75 mg postprandial (period 1) and zolpidem hemitartarate 1.75 mg in fasting (period 2) Formulation will be administered in a single dose, orally in each period. Trial volunteers will be admitted in two different periods of 36 hours each, when investigational product will be administered and blood samples will be collected at pre-determined periods of time up to 24 hours for pharmacokinetics evaluation.

Primary objective is to evaluate the pharmacokinetics of the new formulation of zolpidem hemitartarate orodispersible tablet 1.75 mg in healthy volunteers. As a secondary objective, it will be evaluated if there is any pharmacokinetics difference between genders.

• Study Type: Interventional
• Enrollment (Actual): 28
• Phase: Phase 1

Contacts and Locations

Study Locations

• Brazil
  • SP
    • Bragança Paulista, SP, Brazil, 12916-900
      • UNIFAG - Unidade Integrada de Farmacologia e Gastroenterologia

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male or female volunteers, aged from 18 to 50 years old (women cannot be pregnant or in breastfeeding period and should be committed to use an effective contraceptive method during the study)
• Body mass index (BMI) greater than or equal to 18.5 and less than or equal to 29.9 kg/m2
• Good health conditions and without significant diseases, according to best medical judgment, according to medical history, blood pressure and heart rate measurements, pulse, temperature, physical examination, electrocardiogram (ECG) and complementary laboratory tests
• Ability to understand the nature and objectives of the trial, including risks and adverse events, willingness to cooperate with the researcher and proceed according to all study requirements, which shall be confirmed by informed consent form signature.

Exclusion Criteria:

• Known hypersensitivity to the investigational product (Zolpidem) or chemically related compounds
• History or presence of hepatic or gastrointestinal diseases, or other condition that interferes with drug absorption, distribution, excretion or metabolism
• Maintenance therapy with any drugs, except oral contraceptives
• History of hepatic, kidney, lungs, gastrointestinal, epileptic, hematologic, psychiatric, cardiologic or allergic diseases of any etiology , that requires pharmacological treatment or considered as clinically relevant by the investigator
• Electrocardiographic findings that at investigator discretion are not recommended for study participation
• Deviations on screening laboratory results that are considered clinically relevant by the investigator
• Smoking
• Intake of more than five cups of coffee or tea per day
• History of abusive use of drugs and alcohol
• Use of regular medication two weeks prior to study enrollment or use of any medications one week prior to study enrollment
• Hospitalization for any reason up to 8 weeks prior to start of first period of trial treatment
• Treatment within 3 months prior to the start of trial treatment, with any drug with known and well-established toxic potential to major organs
• Participation in any pharmacokinetics trial with more than 300 mL of blood draw or administration of any experimental drug within 12 months prior to trial treatment start
• Donation or loss of 450 mL or more of blood within 3 months prior to trial enrollment or donation of more than 1500 mL of blood within 12 months prior to the trial treatment start
• Positive result for the BHCG urine test, performed by female volunteers
• Positive results for the detection of abusive drugs at urine exam
• Result higher than 0.1 mg/L for the etilometer exam
• Any condition, according to investigator's best judgment, that prevents the subject to participate in the trial

Study Plan

How is the study designed?

Design Details

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

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Sequency 1; zolpidem hemitartarate 1.75 mg in fasting (period 1) and zolpidem hemitartarate 1.75 mg postprandial (period 2)	Drug: zolpidem hemitartarate 1.75 mg - Sequency 1; zolpidem hemitartarate 1.75 mg in fasting (period 1) and zolpidem hemitartarate 1.75 mg postprandial (period 2)
Experimental: Sequency 2; zolpidem hemitartarate 1.75 mg postprandial (period 1) and zolpidem hemitartarate 1.75 mg in fasting (period 2)	Drug: zolpidem hemitartarate 1.75 mg - Sequency 2; zolpidem hemitartarate 1.75 mg postprandial (period 1) and zolpidem hemitartarate 1.75 mg in fasting (period 2)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Elimination rate constant (Ke)	24 hours
Maximum serum concentration (Cmax)	24 hours
Time to reach maximum (peak) plasma concentration following drug administration (tmax)	24 hours
Area under the curve (0-last)	24 hours
Area under the curve (0-inf)	24 hours
Half life (t1/2)	24 hours
Volume of distribution (Vd)	24 hours
Clearance (C)	24 hours

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of adverse events	60 days
Intensity of adverse events	60 days

Collaborators and Investigators

• Sponsor: Biolab Sanus Farmaceutica
• Investigators: Principal Investigator: José Pedrazzoli Júnior, PhD, UNIFAG - Unidade Integrada de Farmacologia e Gastroenterologia

Study record dates

Study Major Dates

• Study Start (Actual): July 5, 2017
• Primary Completion (Actual): February 22, 2018
• Study Completion (Actual): February 22, 2018

Study Registration Dates

• First Submitted: June 23, 2016
• First Submitted That Met QC Criteria: June 24, 2016
• First Posted (Estimate): June 27, 2016

Study Record Updates

• Last Update Posted (Actual): June 8, 2018
• Last Update Submitted That Met QC Criteria: June 7, 2018
• Last Verified: June 1, 2018

More Information

Terms related to this study

• Keywords: pharmacokinetics; Healthy Volunteers
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Central Nervous System Depressants; Hypnotics and Sedatives; GABA Agents; Sleep Aids, Pharmaceutical; GABA-A Receptor Agonists; GABA Agonists; Zolpidem
• Other Study ID Numbers: JPJ15/16

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No