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

Phase 1

Completed

• Conditions: Pain
• Interventions: Drug: Actiq® 400 µg transmucosally; Drug: Fentanyl 400 µg sublingual spray; Drug: Fentanyl citrate injection 100 µg intravenously; Drug: Naltrexone 50 mg

• Registration Number: NCT01780233
• Lead Sponsor: INSYS Therapeutics Inc

Brief 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.

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.

Study Timeline

• Study Start: 2007-04
• Primary Completion: 2007-05
• Study Completion: 2007-05
• Status Verified: 2013-01
• Study First Submitted: 2013-01-28
• Study First Submitted QC: 2013-01-28
• Last Update Submitted: 2013-01-28
• Study First Posted: 2013-01-31
• Last Update Posted: 2013-01-31

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 40

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.

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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.

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Actiq® 400 µg transmucosally + naltrexone 50 mg	Actiq® 400 µg transmucosally	Patients received a single administration of 400 µg of Actiq® transmucosally + naltrexone hydrochloride 50 mg orally.
Fentanyl 400 µg sublingual spray + naltrexone 50 mg	Fentanyl 400 µg sublingual spray	Patients received a single administration of 400 µg of fentanyl spray sublingually + naltrexone hydrochloride 50 mg orally.
Fentanyl 400 µg sublingual spray + naltrexone 50 mg	Naltrexone 50 mg	Patients received a single administration of 400 µg of fentanyl spray sublingually + naltrexone hydrochloride 50 mg orally.
Actiq® 400 µg transmucosally + naltrexone 50 mg	Naltrexone 50 mg	Patients received a single administration of 400 µg of Actiq® transmucosally + naltrexone hydrochloride 50 mg orally.
Fentanyl citrate injection 100 µg iv + naltrexone 50 mg	Fentanyl citrate injection 100 µg intravenously	Patients received a single administration of 100 µg of fentanyl citrate intravenously + naltrexone hydrochloride 50 mg orally.
Fentanyl citrate injection 100 µg iv + naltrexone 50 mg	Naltrexone 50 mg	Patients received a single administration of 100 µg of fentanyl citrate intravenously + naltrexone hydrochloride 50 mg orally.

Primary Outcome Measures

Name	Time	Method
Time to reach the maximum drug concentration (Tmax) in plasma	Up to 60 minutes pre-dose to 36 hours post-dose

Secondary Outcome Measures

Name	Time	Method
Maximum drug concentration (Cmax) in plasma	Up to 60 minutes pre-dose to 36 hours post-dose
Area under the plasma concentration-time curve from time-0 to the time of the last quantifiable concentration (AUClast)	Up to 60 minutes pre-dose to 36 hours post-dose
Area under the plasma concentration-time curve from time-0 extrapolated to infinity (AUCinf)	Up to 60 minutes pre-dose to 36 hours post-dose
Percentage of AUCinf based on extrapolation (AUCextrap)	Up to 60 minutes pre-dose to 36 hours post-dose
Observed elimination rate constant (λz)	Up to 60 minutes pre-dose to 36 hours post-dose
Observed terminal elimination half-life (T1/2)	Up to 60 minutes pre-dose to 36 hours post-dose
Time of the last measurable concentration of drug (Tlast) in plasma	Up to 60 minutes pre-dose to 36 hours post-dose
Last quantifiable drug concentration (Clast) in plasma	Up to 60 minutes pre-dose to 36 hours post-dose

Trial Locations

Locations (1)

CEDRA Clinical Research, LLC; 🇺🇸 Austin, Texas, United States