Trial Outcomes & Findings for Study to Assess the Absorption and Tolerability of Intranasal Ketorolac Tromethamine and to Assess the Effects of Oxymetazoline Hydrochloride and Fluticasone Propionate on the Absorption and Tolerability of Intranasal Ketorolac Tromethamine in Participants With Allergic Rhinitis (NCT NCT01365650)

NCT ID: NCT01365650

Last Updated: 2018-03-06

Results Overview

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

24 participants

Primary outcome timeframe

Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

Results posted on

2018-03-06

Participant Flow

December 18, 2007 through February 15, 2008; Medical Clinic

After subjects had given their informed consent, subjects were required to pass a screening visit within 3 weeks prior to study drug administration.

Participant milestones

Participant milestones
Measure
Symptomatic Allergic Rhinitis
Treatment A: Single intranasal (i.n.) dose of Ketorolac tromethamine (KT) 30 mg (one 15 mg spray into each nostril) on day 1 of Period 1 followed by a 2-7 day washout interval Treatment B: Single i.n. dose of oxymetazoline hydrochloride (OH) followed 30 minutes later by a single i.n. dose of KT 30 mg (one 15 mg spray into each nostril) of Period 2 followed by a 2-7 day washout interval Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of KT 30 mg (one 15 mg spray into each nostril) on day 1 of Period 3
Treatment A
STARTED
24
Treatment A
COMPLETED
24
Treatment A
NOT COMPLETED
0
Treatment B
STARTED
24
Treatment B
COMPLETED
24
Treatment B
NOT COMPLETED
0
Treatment C
STARTED
24
Treatment C
COMPLETED
24
Treatment C
NOT COMPLETED
0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Study to Assess the Absorption and Tolerability of Intranasal Ketorolac Tromethamine and to Assess the Effects of Oxymetazoline Hydrochloride and Fluticasone Propionate on the Absorption and Tolerability of Intranasal Ketorolac Tromethamine in Participants With Allergic Rhinitis

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
All Study Participants
n=24 Participants
Treatment A: Single intranasal (i.n.) dose of Ketorolac tromethamine (KT) 30 mg (one 15 mg spray into each nostril) on day 1 of Period 1 followed by a 2-7 day washout interval Treatment B: Single i.n. dose of oxymetazoline hydrochloride (OH) followed 30 minutes later by a single i.n. dose of KT 30 mg (one 15 mg spray into each nostril) of Period 2 followed by a 2-7 day washout interval Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of KT 30 mg (one 15 mg spray into each nostril) on day 1 of Period 3
Age, Categorical
<=18 years
0 Participants
n=5 Participants
Age, Categorical
Between 18 and 65 years
22 Participants
n=5 Participants
Age, Categorical
>=65 years
2 Participants
n=5 Participants
Age, Continuous
42.6 years
STANDARD_DEVIATION 16.3 • n=5 Participants
Sex: Female, Male
Female
9 Participants
n=5 Participants
Sex: Female, Male
Male
15 Participants
n=5 Participants
Region of Enrollment
Australia
24 participants
n=5 Participants

PRIMARY outcome

Timeframe: Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Outcome measures

Outcome measures
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 Participants
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 Participants
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 Participants
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
Cmax (the Maximum Observed Plasma Concentration)
1630.223 ng/mL
Standard Deviation 653.599
1729.393 ng/mL
Standard Deviation 684.055
1617.810 ng/mL
Standard Deviation 766.328

PRIMARY outcome

Timeframe: Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Outcome measures

Outcome measures
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 Participants
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 Participants
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 Participants
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
Tmax (the Time to Maximum Concentration)
1.000 hours
Interval 0.25 to 2.0
1.250 hours
Interval 0.75 to 2.05
0.875 hours
Interval 0.25 to 4.0

PRIMARY outcome

Timeframe: Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Outcome measures

Outcome measures
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 Participants
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 Participants
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 Participants
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
AUC 0-t (the Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to the Last Quantifiable Time Point Post-dose)
9001.8 ng*h/mL
Standard Deviation 4011.2
9310.3 ng*h/mL
Standard Deviation 3200.2
8794.3 ng*h/mL
Standard Deviation 4188.2

PRIMARY outcome

Timeframe: Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Outcome measures

Outcome measures
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 Participants
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 Participants
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 Participants
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
AUC 0-∞ (the AUC From Time Zero to Infinity, Where Possible)
9906.9 ng*h/mL
Standard Deviation 4347.0
9959.1 ng*h/mL
Standard Deviation 3294.8
9445.4 ng*h/mL
Standard Deviation 4308.2

PRIMARY outcome

Timeframe: Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Outcome measures

Outcome measures
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 Participants
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 Participants
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 Participants
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
t1/2z (the Terminal Half-life, Where Possible)
5.583 hours
Standard Deviation 1.929
5.172 hours
Standard Deviation 1.582
5.216 hours
Standard Deviation 1.958

PRIMARY outcome

Timeframe: Blood samples for PK analyses were obtained at pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 15 and 24 hours post administration of ketorolac tromethamine

PK analysis by standard model was performed by a pharmacokineticist using model-independent analysis methods in WinNonlin Professional. Actual blood sampling times for ketorolac assay were converted to a time from dosing (elapsed time). Elapsed times were listed by subject for each time, together with individual plasma concentrations of ketorolac.

Outcome measures

Outcome measures
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 Participants
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 Participants
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 Participants
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
MRT (the Mean Residence Time)
7.241 hours
Standard Deviation 2.235
6.861 hours
Standard Deviation 2.037
7.088 hours
Standard Deviation 2.488

Adverse Events

Single i.n. Dose of 30 mg Ketorolac Tromethamine

Serious events: 0 serious events
Other events: 17 other events
Deaths: 0 deaths

Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a

Serious events: 0 serious events
Other events: 22 other events
Deaths: 0 deaths

Seven Days of Treatment With i.n. Fluticasone Propionate

Serious events: 0 serious events
Other events: 17 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
Single i.n. Dose of 30 mg Ketorolac Tromethamine
n=24 participants at risk
Treatment A: Single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 1.
Single i.n. Dose of Oxymetazoline Hydrochloride Followed by a
n=24 participants at risk
Treatment B: Single i.n. dose of oxymetazoline hydrochloride followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) 30 minutes later on Day 1 of Period 2.
Seven Days of Treatment With i.n. Fluticasone Propionate
n=24 participants at risk
Treatment C: Seven days of treatment with i.n. fluticasone propionate (between Periods 2 and 3) followed by a single i.n. dose of 30 mg ketorolac tromethamine (one 15 mg spray into each nostril) on day 1 of Period 3.
Eye disorders
Lacrimation increased
12.5%
3/24 • Number of events 3 • 3 months
0.00%
0/24 • 3 months
8.3%
2/24 • Number of events 2 • 3 months
Gastrointestinal disorders
Nausea
0.00%
0/24 • 3 months
12.5%
3/24 • Number of events 4 • 3 months
0.00%
0/24 • 3 months
Infections and infestations
Urinary tract infection
8.3%
2/24 • Number of events 2 • 3 months
0.00%
0/24 • 3 months
8.3%
2/24 • Number of events 2 • 3 months
Nervous system disorders
Dizziness
8.3%
2/24 • Number of events 2 • 3 months
4.2%
1/24 • Number of events 1 • 3 months
4.2%
1/24 • Number of events 1 • 3 months
Nervous system disorders
Headache
12.5%
3/24 • Number of events 3 • 3 months
12.5%
3/24 • Number of events 3 • 3 months
8.3%
2/24 • Number of events 2 • 3 months
Respiratory, thoracic and mediastinal disorders
Cough
4.2%
1/24 • Number of events 1 • 3 months
4.2%
1/24 • Number of events 1 • 3 months
8.3%
2/24 • Number of events 2 • 3 months
Respiratory, thoracic and mediastinal disorders
Sneezing
4.2%
1/24 • Number of events 1 • 3 months
8.3%
2/24 • Number of events 2 • 3 months
0.00%
0/24 • 3 months
Respiratory, thoracic and mediastinal disorders
Throat irritation
33.3%
8/24 • Number of events 8 • 3 months
4.2%
1/24 • Number of events 1 • 3 months
20.8%
5/24 • Number of events 5 • 3 months
Respiratory, thoracic and mediastinal disorders
Nasal discomfort
45.8%
11/24 • Number of events 12 • 3 months
75.0%
18/24 • Number of events 18 • 3 months
58.3%
14/24 • Number of events 14 • 3 months

Additional Information

David Bregman, M.D., Ph.D.

Luitpold Pharmaceuticals, Inc.

Phone: 610-650-4200

Results disclosure agreements

  • Principal investigator is a sponsor employee
  • Publication restrictions are in place