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

Pain Clinical Trial

Official title:

A Single-dose Crossover Study of Fentanyl Sublingual Spray 400 Mcg Versus Actiq® 400 Mcg Versus Fentanyl Citrate Injection (iv) 100 Mcg Under Fasted Conditions

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT01780233
• Other study ID #: INS-06-003
• Status: Completed
• Phase: Phase 1
• First received: January 28, 2013
• Last updated: January 28, 2013
• Start date: April 2007
• Est. completion date: May 2007

Study information

• Verified date: January 2013
• Source: INSYS Therapeutics Inc
• Contact: n/a
• Is FDA regulated: No
• Health authority: United States: Food and Drug Administration
• Study type: Interventional

Clinical Trial 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.

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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 40
• Est. completion date: May 2007
• Est. primary completion date: May 2007
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Both
• Age group: 18 Years to 55 Years

Eligibility

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.

Study Design

Allocation: Randomized, Endpoint Classification: Pharmacokinetics Study, Intervention Model: Crossover Assignment, Masking: Open Label, Primary Purpose: Treatment

Related Conditions & MeSH terms

• Pain

Intervention

Drug:
• Fentanyl 400 µg sublingual spray

• 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.
• Fentanyl citrate injection 100 µg intravenously

• 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.

Locations

Country	Name	City	State
United States	CEDRA Clinical Research, LLC	Austin	Texas

Sponsors (1)

Lead Sponsor	Collaborator
INSYS Therapeutics Inc

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Time to reach the maximum drug concentration (Tmax) in plasma		Up to 60 minutes pre-dose to 36 hours post-dose	No
Secondary	Maximum drug concentration (Cmax) in plasma		Up to 60 minutes pre-dose to 36 hours post-dose	No
Secondary	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	No
Secondary	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	No
Secondary	Percentage of AUCinf based on extrapolation (AUCextrap)		Up to 60 minutes pre-dose to 36 hours post-dose	No
Secondary	Observed elimination rate constant (?z)		Up to 60 minutes pre-dose to 36 hours post-dose	No
Secondary	Observed terminal elimination half-life (T1/2)		Up to 60 minutes pre-dose to 36 hours post-dose	No
Secondary	Time of the last measurable concentration of drug (Tlast) in plasma		Up to 60 minutes pre-dose to 36 hours post-dose	No
Secondary	Last quantifiable drug concentration (Clast) in plasma		Up to 60 minutes pre-dose to 36 hours post-dose	No