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

NCT ID: NCT01780233

Last Updated: 2013-01-31

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 40 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2007-04-30
• Study Completion Date: 2007-05-31

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.

Conditions

Pain

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: CROSSOVER
• Primary Study Purpose: TREATMENT
• Blinding Strategy: NONE

Study Groups

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.

Group Type: EXPERIMENTAL

Fentanyl 400 µg sublingual spray

Intervention Type: DRUG

Naltrexone 50 mg

Intervention Type: DRUG

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.

Actiq® 400 µg transmucosally + naltrexone 50 mg

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

Group Type: ACTIVE_COMPARATOR

Actiq® 400 µg transmucosally

Intervention Type: DRUG

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.

Naltrexone 50 mg

Intervention Type: DRUG

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.

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.

Group Type: ACTIVE_COMPARATOR

Fentanyl citrate injection 100 µg intravenously

Intervention Type: DRUG

Naltrexone 50 mg

Intervention Type: DRUG

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.

Interventions

Fentanyl 400 µg sublingual spray

Intervention Type: DRUG

Actiq® 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.

Intervention Type: DRUG

Fentanyl citrate injection 100 µg intravenously

Intervention Type: DRUG

Naltrexone 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.

Intervention Type: DRUG

Other Intervention Names

fentanyl citrate

Eligibility Criteria

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

• 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.

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 55 Years
• Eligible Sex: ALL
• Accepts Healthy Volunteers: Yes

Sponsors

INSYS Therapeutics Inc

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Neha Parikh

Role: STUDY_DIRECTOR

INSYS Therapeutics Inc

Frederick A. Bieberdorf, MD

Role: PRINCIPAL_INVESTIGATOR

CEDRA Clinical Research

Locations

CEDRA Clinical Research, LLC

Austin, Texas, United States

Countries

United States

References

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.

Reference Type: DERIVED

PMID: 23497761 (View on PubMed)

Other Identifiers

INS-06-003

Identifier Type: -

Identifier Source: org_study_id