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CompletedNCT01780233Updated Jan 31, 2013

Pharmacokinetic Study of Fentanyl 400 µg Sublingual Spray, Actiq® 400 µg Transmucosally, and Fentanyl Citrate Injection 100 µg Intravenously (iv)

A Phase 1 interventional study of Fentanyl 400 µg sublingual spray and Actiq® 400 µg transmucosally in Pain, sponsored by INSYS Therapeutics Inc. Completed at 1 site in United States. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2013-01-31.

Sponsored by INSYS Therapeutics Inc · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
40
Allocation
Randomized
Ages
18 Years to 55 Years
Sex
All
01

Study summary

The objective of this study was to compare the rate of absorption and bioavailability of fentanyl 400 µg sublingual spray, Actiq® 400 µg transmucosally, and fentanyl citrate injection 100 µg intravenously.

Read the detailed description

This was a Phase I, single-dose, open-label, randomized, 3-period, 3-treatment cross over study in which 21 healthy subjects received single doses of fentanyl 400 µg sublingual spray, Actiq® 400 µg transmucosally, and fentanyl citrate injection 100 µg intravenously following a 10-hour overnight fast. There was a 7 day washout period between treatments.

02

Conditions studied

  • Pain
03

In context

Lead sponsor

INSYS Therapeutics Inc is the lead sponsor of 45 studies on the registry; none are open to participants now.

Of its 5 completed or terminated interventional studies of FDA-regulated products, 3 (60%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 55 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  • Male or non-pregnant, non-breast-feeding female between the ages of 18-55 inclusive.
  • Body Mass Index (BMI) between 18-30 kg/m\^2, inclusive, and body weight of at least 60 kg (132 lbs).
  • Subject was healthy according to the medical history, laboratory results, and physical examination.

Exclusion criteria

Exclusion Criteria:

  • Had a presence or history of clinically significant cardiovascular, pulmonary, hepatic, renal, hematologic, gastrointestinal, endocrine, immunologic, dermatologic, neurologic, oncologic, or psychiatric disease or any other condition which, in the opinion of the Investigator would jeopardize the safety of the subject or the validity of the study results.
  • Had a clinically significant abnormal finding on the physical exam, medical history, electrocardiogram (ECG), or clinical laboratory results at screening.
  • Had a significant history of hypersensitivity to opioid analgesics, fentanyl or any related products, naltrexone, or severe hypersensitivity reactions (like angioedema) to any drugs.
  • Had a significantly abnormal diet during the 4 weeks preceding the first dose of study medication.
  • Had donated blood or plasma within 30 days prior to the first dose of study medication or during the course of this study.
  • Had participated in another clinical trial within 30 days prior to the first dose of study medication or during the course of this study.
  • Had used any over-the-counter (OTC) medication, including nutritional supplements, within 7 days prior to the first dose of study medication or during the course of this study.
  • Had used any prescription medication, except hormonal contraceptive or hormonal replacement therapy, within 14 days prior to the first dose of study medication or during the course of this study.
  • Had used enzyme altering drugs such as barbiturates, corticosteroids, phenothiazines, cimetidine, carbamazepine, etc, within 30 days prior to the first dose of study medication or during the course of this study.
  • Had used opioid analgesics within the last 30 days.
05

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
40 participants (actual)

Study arms

  • Experimental
    Fentanyl 400 µg sublingual spray + naltrexone 50 mg

    Patients received a single administration of 400 µg of fentanyl spray sublingually + naltrexone hydrochloride 50 mg orally.

    Drug: Fentanyl 400 µg sublingual spray · Drug: Naltrexone 50 mg

  • Active comparator
    Actiq® 400 µg transmucosally + naltrexone 50 mg

    Patients received a single administration of 400 µg of Actiq® transmucosally + naltrexone hydrochloride 50 mg orally.

    Drug: Actiq® 400 µg transmucosally · Drug: Naltrexone 50 mg

  • Active comparator
    Fentanyl citrate injection 100 µg iv + naltrexone 50 mg

    Patients received a single administration of 100 µg of fentanyl citrate intravenously + naltrexone hydrochloride 50 mg orally.

    Drug: Fentanyl citrate injection 100 µg intravenously · Drug: Naltrexone 50 mg

Interventions

  • DrugFentanyl 400 µg sublingual spray
  • DrugActiq® 400 µg transmucosally

    Actiq® 400 µg is a solid formulation of fentanyl citrate on a plastic stick that dissolves slowly in the mouth for absorption across the buccal mucosa.

    Also known as: fentanyl citrate

  • DrugFentanyl citrate injection 100 µg intravenously
  • DrugNaltrexone 50 mg

    Naltrexone hydrochloride was administered approximately 12 hours and 1 hour prior to and 12 hours after each dose of fentanyl to minimize the occurrence of unacceptable adverse effects (eg, decreased respiration, nausea) often associated with administration of fentanyl.

06

What researchers measure

Primary outcomes

  1. Time to reach the maximum drug concentration (Tmax) in plasma

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

Secondary outcomes

  1. Maximum drug concentration (Cmax) in plasma

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  2. Area under the plasma concentration-time curve from time-0 to the time of the last quantifiable concentration (AUClast)

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  3. Area under the plasma concentration-time curve from time-0 extrapolated to infinity (AUCinf)

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  4. Percentage of AUCinf based on extrapolation (AUCextrap)

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  5. Observed elimination rate constant (λz)

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  6. Observed terminal elimination half-life (T1/2)

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  7. Time of the last measurable concentration of drug (Tlast) in plasma

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

  8. Last quantifiable drug concentration (Clast) in plasma

    Time frame: Up to 60 minutes pre-dose to 36 hours post-dose

07

Study locations

1 site
  • CEDRA Clinical Research, LLC
    Austin, Texas 78759, United States
08

References and documents

Publications

  • Parikh N, Goskonda V, Chavan A, Dillaha L. Single-dose pharmacokinetics of fentanyl sublingual spray and oral transmucosal fentanyl citrate in healthy volunteers: a randomized crossover study. Clin Ther. 2013 Mar;35(3):236-43. doi: 10.1016/j.clinthera.2013.02.017. PubMed 23497761 ↗
09

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jan 31, 2013, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
10

Registry details

Key details

Study ID
NCT01780233
Lead sponsor
INSYS Therapeutics Inc
Responsible party
Sponsor
First posted
Jan 31, 2013
Start date
Apr 2007
Primary completion
May 2007
Completion
May 2007
Last update
Jan 31, 2013

Study contacts

Neha Parikh
study director · INSYS Therapeutics Inc
Frederick A. Bieberdorf, MD
principal investigator · CEDRA Clinical Research

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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This study is completed, as verified in Jan 2013. You cannot join it, but the record below documents what was studied.

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