Pharmacokinetics and Safety of Topical Administration of Brimonidine Tartrate Ophthalmic Solution 0.025%.

A Prospective, Single-Center, Open-Label, Study of the Plasma Pharmacokinetics and Safety Following Topical Administration of Brimonidine Tartrate Ophthalmic Solution 0.025% Used Four Times Daily in Healthy, Adult Subjects.

To characterize the plasma pharmacokinetics and safety profile of brimonidine following a single dose and 4 times per day (QID) dosing of brimonidine tartrate ophthalmic solution 0.025% for 7 days in healthy, adult subjects.

Study Overview

• Status: Completed
• Conditions: Hyperemia
• Intervention / Treatment: Drug: Brimonidine tartrate

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

Contacts and Locations

Study Locations

• United States
  • New York
    • Rochester, New York, United States, 14609
      • Bausch & Lomb, Incorporated

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:

• have ocular health within normal limits.
• have blood (hematology, blood chemistry) and urine analysis within normal limits.
• have a body weight within 15% of ideal weight

Exclusion Criteria:

• have known contraindications or sensitivity to the use of any of the investigational drug(s) or their components, or any other medications required by the protocol;
• have any active systemic or ocular disorder other than refractive disorder.
• have presence of any abnormality of the lids, ocular surface, or lacrimal duct system that in the Investigator's opinion could affect ophthalmic drop absorption.
• have a history of chronic alcohol consumption.
• consume alcohol and/or caffeine or xanthine containing products within 48 hours prior to dosing at Visit 1 or anticipated use during the study.
• have a history of tobacco, nicotine, or nicotine containing product use within the last year prior to Visit 2;
• have significant weight change (over 10 pounds) within the 60 days prior to Visit 2;
• have blood donation or equivalent blood loss of 450 ml or more, within 60 days prior to Visit 2;
• have an abnormal blood pressure (defined as ≤ 90 or ≥ 160 (systolic) measured in mmHg or ≤ 60 or ≥ 100 (diastolic) measured in mmHg);
• have intraocular pressure (IOP) that is less than 5 mmHg or greater than 22 mmHg or have a normal IOP with a diagnosis of glaucoma.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Screening
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Brimonidine tartrate; One drop of brimonidine tartrate ophthalmic solution 0.025% in each eye once at Visit 2 (Day 1) then four times daily (QID) approximately 4 hours apart at Visit 3 (Day 2) through day 6, and then once at Visit 4 (Day 7).	Drug: Brimonidine tartrate

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Plasma Levels	Blood samples will be collected for the determination of brimonidine in plasma at the specified time points on Day 1.	Day 1 (Visit 2)
Plasma Levels	Blood samples will be collected for the determination of brimonidine in plasma at the specified time points on Day 2.	Day 2 (Visit 3)
Plasma Levels	Blood samples will be collected for the determination of brimonidine in plasma at the specified time points on Day 7.	Day 7 (Visit 4)
Plasma Levels	Blood samples will be collected for the determination of brimonidine in plasma at the specified time points on Day 8.	Day 8 (Visit 5)

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Visual Acuity	Visual acuity testing should be done with best correction at 10ft	Baseline (Visit 1)
Slit Lamp Biomicroscopy	Lid and lid margin erythema and swelling, conjunctival erythema/hyperemia and chemosis will be graded on a scale of 0 - 4. with 0=normal and 4=marked. Half grade measurements will be accepted for erythema/hyperemia.	Baseline (Visit 1)
Intraocular Pressure	Intraocular Pressure measured at baseline Day 8 (Visit 5)	Day 8 (Visit 5)
Hematology and Blood Chemistry Analysis	Blood samples will be collected for hematology and blood chemistry parameters at Baseline (Visit 1)	Baseline (Visit 1)
Urinalysis	Urine sample will be collected for urinalysis at Baseline (Visit 1)	Baseline (Visit 1)
Visual Acuity	Visual acuity testing should be done with best correction at 10ft	Day 1 (Visit 2)
Visual Acuity	Visual acuity testing should be done with best correction at 10ft	Day 7 (Visit 4)
Visual Acuity	Visual acuity testing should be done with best correction at 10ft	Day 8 (Visit 5)
Slit Lamp Biomicroscopy	Lid and lid margin erythema and swelling, conjunctival erythema/hyperemia and chemosis will be graded on a scale of 0 - 4. with 0=normal and 4=marked. Half grade measurements will be accepted for erythema/hyperemia.	Day 1 (Visit 2)
Slit Lamp Biomicroscopy	Lid and lid margin erythema and swelling, conjunctival erythema/hyperemia and chemosis will be graded on a scale of 0 - 4. with 0=normal and 4=marked. Half grade measurements will be accepted for erythema/hyperemia.	Day 7 (Visit 4)
Slit Lamp Biomicroscopy	Lid and lid margin erythema and swelling, conjunctival erythema/hyperemia and chemosis will be graded on a scale of 0 - 4. with 0=normal and 4=marked. Half grade measurements will be accepted for erythema/hyperemia.	Day 8 (Visit 5)
Intraocular Pressure	Intraocular Pressure measured at baseline (Visit 1)	Baseline (Visit 1)
Hematology and Blood Chemistry Analysis	Blood samples will be collected for hematology and blood chemistry parameters at Day 8 (Visit 5)	Day 8 (Visit 5)
Urinalysis	Urine sample will be collected for urinalysis at Day 8 (Visit 5)	Day 8 (Visit 5)

Collaborators and Investigators

• Sponsor: Bausch & Lomb Incorporated
• Collaborators: ORA, Inc.
• Investigators: Study Director: Joseph Ciolino, MD, ORA, Inc.

Study record dates

Study Major Dates

• Study Start (Actual): February 1, 2014
• Primary Completion (Actual): March 1, 2014
• Study Completion (Actual): April 1, 2014

Study Registration Dates

• First Submitted: January 16, 2014
• First Submitted That Met QC Criteria: January 16, 2014
• First Posted (Estimate): January 20, 2014

Study Record Updates

• Last Update Posted (Actual): April 28, 2017
• Last Update Submitted That Met QC Criteria: April 27, 2017
• Last Verified: April 1, 2017

More Information

Terms related to this study

• Keywords: Ocular Redness
• Additional Relevant MeSH Terms: Cardiovascular Diseases; Vascular Diseases; Hyperemia; Physiological Effects of Drugs; Adrenergic Agents; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Antihypertensive Agents; Adrenergic alpha-2 Receptor Agonists; Adrenergic alpha-Agonists; Adrenergic Agonists; Brimonidine Tartrate
• Other Study ID Numbers: 863/13-100-0007