Epinephrine Inhalation Aerosol USP, a HFA-MDI Study for Assessment of Pharmacokinetics
Primary Purpose
Asthma, Bronchospasm, Wheezing
Status
Completed
Phase
Phase 1
Locations
United States
Study Type
Interventional
Intervention
Epinephrine Inhalation Aerosol, HFA
Epinephrine Inhalation Aerosol
Sponsored by
About this trial
This is an interventional treatment trial for Asthma focused on measuring asthma, bronchospasm, wheezing, shortness of breath
Eligibility Criteria
Inclusion Criteria:
- Generally healthy at screening;
- No clinically significant respiratory, cardiovascular and other systemic or organic illnesses;
- Body weight ≥ 50 kg for men and ≥ 45 kg for women,
- Sitting blood pressure ≤ 135/90 mm Hg;
- Demonstrating negative HIV, HBsAg and HCV-Ab screen tests;
- Women of child-bearing potential must be non-pregnant, non-lactating, and practicing a clinically acceptable form of birth control;
- Properly consented
- Other criteria apply
Exclusion Criteria:
- A smoking history of ≥10 pack-years, or having smoked within 6 months;
- Upper respiratory tract infections within 2 wk, or lower respiratory tract infection within 4 wk, prior to Screening;
- Any current or recent respiratory conditions that might significantly affect pharmacodynamic response to the study drugs;
- Known intolerance or hypersensitivity to the study MDI ingredients;
- Having been on other investigational studies, or donated blood, in the last 30 days;
- Other Criteria Apply
Sites / Locations
- Amphastar Site 0035
Arms of the Study
Arm 1
Arm 2
Arm Type
Experimental
Active Comparator
Arm Label
Epinephrine Inhalation Aerosol, HFA
Epinephrine Inhalation Aerosol, CFC
Arm Description
Experimental treatment of 10 inhalations of 125 mcg epinephrine base propelled by HFA 134a
Epinephrine Inhalation Aerosol, CFC propelled, 220 mcg/inhalation , 10 inhalations
Outcomes
Primary Outcome Measures
Baseline Concentration (C0) of Total Epinephrine
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at Baseline (prior to dosing) in each treatment period following a specified washout period (3-14 days), and were analyzed using an established analysis method. Baseline concentration (C0) is the concentration of epinephrine measured in the plasma at this time point.
Peak Concentration (Cmax) of Total Epinephrine From Time Zero to 6 Hours Post-dose
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Peak (maximum) concentration (Cmax) is the highest concentration of epinephrine measured in plasma during the treatment period.
Area Under the Curve From Time Zero to 6 Hours Post-dose (AUC[0-6]) for Total Epinephrine
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Area under the curve from time zero to 6 hours post-dose (AUC[0-6]) was calculated using the trapezoidal rule.
Time to Reach Peak Concentration (Tmax) for Total Epinephrine
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Tmax is the amount of time it takes for epinephrine to reach peak concentration in plasma during the treatment period.
Half-life (t1/2) of Total Epinephrine
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Half-life (t1/2) is the amount of time it takes for epinephrine to decrease to half the peak concentration in plasma during the treatment period.
Concentration vs. Time for Total Epinephrine From Time Zero to 6 Hours Post-dose
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method.
Secondary Outcome Measures
Full Information
NCT ID
NCT01188577
First Posted
August 24, 2010
Last Updated
June 27, 2017
Sponsor
Amphastar Pharmaceuticals, Inc.
1. Study Identification
Unique Protocol Identification Number
NCT01188577
Brief Title
Epinephrine Inhalation Aerosol USP, a HFA-MDI Study for Assessment of Pharmacokinetics
Official Title
Epinephrine Inhalation Aerosol USP, an HFA-MDI CLINICAL STUDY-B2 FOR ASSESSMENT OF PHARMACOKINETICS (A Randomized, Evaluator-Blind, Single-Dose, Two Arm, Crossover, PK Study in Healthy Volunteers)
Study Type
Interventional
2. Study Status
Record Verification Date
June 2017
Overall Recruitment Status
Completed
Study Start Date
August 2010 (undefined)
Primary Completion Date
September 2010 (Actual)
Study Completion Date
January 2011 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Sponsor
Name of the Sponsor
Amphastar Pharmaceuticals, Inc.
4. Oversight
Data Monitoring Committee
No
5. Study Description
Brief Summary
This study examines the pharmacokinetic profile of Armstrong's proposed Epinephrine Inhalation Aerosol USP, an HFA-MDI (E004), using a stable isotope deuterium-labeled epinephrine (epinephrine-d3) to differentiate the administered drug from the endogenous epinephrine, in healthy male and female adult volunteers. The current study is designed for a more thorough evaluation of the E004 Pharmacokinetics. Safety of E004 will also be evaluated, under augmented dose conditions.
Detailed Description
E004 is formulated with epinephrine free base as the active ingredient, and hydrofluoroalkane (HFA-134a) as the propellant.
In order to differentiate the inhaled epinephrine from the fluctuating background of endogenous epinephrine 1, a stable-isotope deuterium (2H) labeled epinephrine (epinephrine-d3) preparation will be used to formulate E004 inhalers, denoted as E004-d3. PK of E004 at 125 mcg of epinephrine-d3 per inhalation, will be compared to that of the currently marketed, non-labeled, Epinephrine-CFC MDI as the Reference Control (220 mcg per inhalation).
This study is a randomized, evaluator-blind, single dose, two-arm, crossover, PK study, to be conducted in ~18 healthy, male and female, adult volunteers. PK will be studied using E004-d3 at 125 mcg per inhalation (Arm T). A currently marketed, non-labeled, Epinephrine CFC-MDI will be used as a Reference Control (Arm C).
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
Asthma, Bronchospasm, Wheezing, Shortness of Breath
Keywords
asthma, bronchospasm, wheezing, shortness of breath
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1, Phase 2
Interventional Study Model
Crossover Assignment
Masking
ParticipantCare ProviderOutcomes Assessor
Allocation
Randomized
Enrollment
23 (Actual)
8. Arms, Groups, and Interventions
Arm Title
Epinephrine Inhalation Aerosol, HFA
Arm Type
Experimental
Arm Description
Experimental treatment of 10 inhalations of 125 mcg epinephrine base propelled by HFA 134a
Arm Title
Epinephrine Inhalation Aerosol, CFC
Arm Type
Active Comparator
Arm Description
Epinephrine Inhalation Aerosol, CFC propelled, 220 mcg/inhalation , 10 inhalations
Intervention Type
Drug
Intervention Name(s)
Epinephrine Inhalation Aerosol, HFA
Other Intervention Name(s)
HFA epinephrine inhalation aerosol, 125 mcg/inhalation
Intervention Description
10 inhalations of epinephrine inhalation aerosol, 125 mcg/inhalation
Intervention Type
Drug
Intervention Name(s)
Epinephrine Inhalation Aerosol
Other Intervention Name(s)
Primatene Mist, Epinephrine Inhalation Aerosol, USP
Intervention Description
Epinephrine Inhalation Aerosol, 220 mcg/ inhalation, 10 inhalations
Primary Outcome Measure Information:
Title
Baseline Concentration (C0) of Total Epinephrine
Description
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at Baseline (prior to dosing) in each treatment period following a specified washout period (3-14 days), and were analyzed using an established analysis method. Baseline concentration (C0) is the concentration of epinephrine measured in the plasma at this time point.
Time Frame
0 to 30 minutes prior to dosing
Title
Peak Concentration (Cmax) of Total Epinephrine From Time Zero to 6 Hours Post-dose
Description
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Peak (maximum) concentration (Cmax) is the highest concentration of epinephrine measured in plasma during the treatment period.
Time Frame
Pre-dose to 6 hours post-dose
Title
Area Under the Curve From Time Zero to 6 Hours Post-dose (AUC[0-6]) for Total Epinephrine
Description
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Area under the curve from time zero to 6 hours post-dose (AUC[0-6]) was calculated using the trapezoidal rule.
Time Frame
Pre-dose to 6 hours post-dose
Title
Time to Reach Peak Concentration (Tmax) for Total Epinephrine
Description
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Tmax is the amount of time it takes for epinephrine to reach peak concentration in plasma during the treatment period.
Time Frame
Pre-dose to 6 hours post-dose
Title
Half-life (t1/2) of Total Epinephrine
Description
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method. Half-life (t1/2) is the amount of time it takes for epinephrine to decrease to half the peak concentration in plasma during the treatment period.
Time Frame
Pre-dose to 6 hours post-dose
Title
Concentration vs. Time for Total Epinephrine From Time Zero to 6 Hours Post-dose
Description
Patient PK blood samples were taken from a vein in a hand or arm via indwelling heparin-anticoagulated IV catheters, or by venipunctures at 0 (baseline), 2, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 45, 60, 90, 120, 240, and 360 minutes post-dose in each treatment period and were analyzed using an established analysis method.
Time Frame
Pre-dose to 6 hours post-dose
10. Eligibility
Sex
All
Minimum Age & Unit of Time
18 Years
Maximum Age & Unit of Time
30 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
Generally healthy at screening;
No clinically significant respiratory, cardiovascular and other systemic or organic illnesses;
Body weight ≥ 50 kg for men and ≥ 45 kg for women,
Sitting blood pressure ≤ 135/90 mm Hg;
Demonstrating negative HIV, HBsAg and HCV-Ab screen tests;
Women of child-bearing potential must be non-pregnant, non-lactating, and practicing a clinically acceptable form of birth control;
Properly consented
Other criteria apply
Exclusion Criteria:
A smoking history of ≥10 pack-years, or having smoked within 6 months;
Upper respiratory tract infections within 2 wk, or lower respiratory tract infection within 4 wk, prior to Screening;
Any current or recent respiratory conditions that might significantly affect pharmacodynamic response to the study drugs;
Known intolerance or hypersensitivity to the study MDI ingredients;
Having been on other investigational studies, or donated blood, in the last 30 days;
Other Criteria Apply
Overall Study Officials:
First Name & Middle Initial & Last Name & Degree
Medical Director
Organizational Affiliation
Amphastar Pharmaceuticals, Inc.
Official's Role
Study Director
Facility Information:
Facility Name
Amphastar Site 0035
City
Cypress
State/Province
California
ZIP/Postal Code
90630
Country
United States
12. IPD Sharing Statement
Citations:
PubMed Identifier
2019665
Citation
Pinnas JL, Schachtel BP, Chen TM, Roseberry HR, Thoden WR. Inhaled epinephrine and oral theophylline-ephedrine in the treatment of asthma. J Clin Pharmacol. 1991 Mar;31(3):243-7. doi: 10.1002/j.1552-4604.1991.tb04969.x.
Results Reference
background
PubMed Identifier
16400891
Citation
Hendeles L, Marshik PL, Ahrens R, Kifle Y, Shuster J. Response to nonprescription epinephrine inhaler during nocturnal asthma. Ann Allergy Asthma Immunol. 2005 Dec;95(6):530-4. doi: 10.1016/S1081-1206(10)61014-9.
Results Reference
background
PubMed Identifier
3780129
Citation
Warren JB, Doble N, Dalton N, Ewan PW. Systemic absorption of inhaled epinephrine. Clin Pharmacol Ther. 1986 Dec;40(6):673-8. doi: 10.1038/clpt.1986.243.
Results Reference
background
PubMed Identifier
10919679
Citation
Cripps A, Riebe M, Schulze M, Woodhouse R. Pharmaceutical transition to non-CFC pressurized metered dose inhalers. Respir Med. 2000 Jun;94 Suppl B:S3-9.
Results Reference
background
PubMed Identifier
10936150
Citation
Dickinson BD, Altman RD, Deitchman SD, Champion HC. Safety of over-the-counter inhalers for asthma: report of the council on scientific affairs. Chest. 2000 Aug;118(2):522-6. doi: 10.1378/chest.118.2.522.
Results Reference
background
PubMed Identifier
11061773
Citation
Simons FE, Gu X, Johnston LM, Simons KJ. Can epinephrine inhalations be substituted for epinephrine injection in children at risk for systemic anaphylaxis? Pediatrics. 2000 Nov;106(5):1040-4. doi: 10.1542/peds.106.5.1040.
Results Reference
background
PubMed Identifier
10535697
Citation
Kushner DJ, Baker A, Dunstall TG. Pharmacological uses and perspectives of heavy water and deuterated compounds. Can J Physiol Pharmacol. 1999 Feb;77(2):79-88.
Results Reference
background
PubMed Identifier
9616533
Citation
Bondesson E, Friberg K, Soliman S, Lofdahl CG. Safety and efficacy of a high cumulative dose of salbutamol inhaled via Turbuhaler or via a pressurized metered-dose inhaler in patients with asthma. Respir Med. 1998 Feb;92(2):325-30. doi: 10.1016/s0954-6111(98)90116-0.
Results Reference
background
PubMed Identifier
32423275
Citation
Kerwin EM, Marrs T, Luo MZ, Zhang JY. Pharmacokinetic Study of Epinephrine Hydrofluoroalkane (Primatene MIST) Metered-Dose Inhaler. J Aerosol Med Pulm Drug Deliv. 2020 Oct;33(5):282-287. doi: 10.1089/jamp.2019.1577. Epub 2020 May 18.
Results Reference
derived
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Epinephrine Inhalation Aerosol USP, a HFA-MDI Study for Assessment of Pharmacokinetics
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