Pain
Conditions
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.
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.
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.
Sponsors
INSYS Therapeutics Inc
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
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
* 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.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Time to reach the maximum drug concentration (Tmax) in plasma | Up to 60 minutes pre-dose to 36 hours post-dose |
Secondary
| Measure | Time frame |
|---|---|
| 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 |
| Maximum drug concentration (Cmax) in plasma | 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 |
| Observed elimination rate constant (λz) | Up to 60 minutes pre-dose to 36 hours post-dose |
Countries
United States
Outcome results
None listed