Pharmacokinetics
Conditions
Keywords
pharmacokinetics, area under curve, time to maximum concentration
Brief summary
Determine whether the amount of drug absorbed is different if the tablet is placed under the tongue, placed between the cheek and gum, or swallowed.
Interventions
DRUGTreatment A: Sufentanil IV
Sufenta IV (50 mcg/mL) 15 mcg push over 1 minute (IV)
DRUGTreatment B: Sufentanil NanoTab Sublingual
Single Sufentanil NanoTab 15 mcg given sublingually (SL)
DRUGTreatment C: Sufentanil NanoTab Buccal
Treatment C: Single Sufentanil NanoTab 15 mcg given buccally (BU)
DRUGTreatment D: Sufentanil NanoTab Oral
Single Sufentanil NanoTab 15 mcg swallowed (PO)
Sponsors
Talphera, Inc
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* body mass index 18 - 30
Exclusion criteria
* pregnant females * smokers * pulmonary disease * sleep apnea
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| AUC (0 - Inf) | 24 hours | total amount of sufentanil absorbed |
| Cmax | 24 hours | maximum plasma concentration |
| Tmax | 24 hours | time to maximum plasma concentration |
| CST 1/2 | 24 hours | time for maximum plasma concentration to decrease by 50% |
Countries
United States
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Treatment A, Followed by Treatment B, C and D in Random Order Treatment A: Sufenta IV (50 mcg/mL) 15 mcg push over 1 minute (IV) Treatment B: Single Sufentanil NanoTab 15 mcg given sublingually (SL) Treatment C: Single Sufentanil NanoTab 15 mcg given buccally (BU) Treatment D: Single Sufentanil NanoTab 15 mcg swallowed (PO) Sequence 1: A, B, C, D Sequence 2: A, B, D, C Sequence 3: A, C, B, D Sequence 4: A, C, D, B Sequence 5: A, D, B, C Sequence 6: A, D, C, B A 48-hour washout period separated each treatment period. The washout began with the start of dosing. | 25 |
| Total | 25 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 | FG003 | FG004 | FG005 |
|---|---|---|---|---|---|---|---|
| Overall Study | Withdrawal by Subject | 1 | 0 | 1 | 1 | 0 | 0 |
Baseline characteristics
| Characteristic | Treatment A, Followed by Treatment B, C and D in Random Order |
|---|---|
| Age, Categorical <=18 years | 0 Participants |
| Age, Categorical >=65 years | 0 Participants |
| Age, Categorical Between 18 and 65 years | 25 Participants |
| Age, Continuous | 29.8 years STANDARD_DEVIATION 7.7 |
| Region of Enrollment United States | 25 participants |
| Sex: Female, Male Female | 12 Participants |
| Sex: Female, Male Male | 13 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk |
|---|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — | — / — |
| other Total, other adverse events | 8 / 25 | 4 / 24 | 5 / 24 | 3 / 23 |
| serious Total, serious adverse events | 0 / 25 | 0 / 24 | 0 / 24 | 0 / 23 |
Outcome results
Primary
AUC (0 - Inf)
total amount of sufentanil absorbed
Time frame: 24 hours
Population: A The number of subjects (n) in Treatment D was less than the total 22 subjects for the following PK parameters: AUC 0-inf (n=18).
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Sufentanil IV | AUC (0 - Inf) | 273.8 h.pg/mL | Standard Deviation 61.1 |
| Sufentanil NanoTab Buccal | AUC (0 - Inf) | 212.5 h.pg/mL | Standard Deviation 57 |
| Sufentanil NanoTab Sublingual | AUC (0 - Inf) | 163.4 h.pg/mL | Standard Deviation 52.5 |
| Sufentanil NanoTab Oral | AUC (0 - Inf) | 24.9 h.pg/mL | Standard Deviation 14.1 |
Primary
Cmax
maximum plasma concentration
Time frame: 24 hours
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Sufentanil IV | Cmax | 445.1 pg/mL | Standard Deviation 312 |
| Sufentanil NanoTab Buccal | Cmax | 58.9 pg/mL | Standard Deviation 25.7 |
| Sufentanil NanoTab Sublingual | Cmax | 40.6 pg/mL | Standard Deviation 14.8 |
| Sufentanil NanoTab Oral | Cmax | 4.3 pg/mL | Standard Deviation 3.8 |
Primary
CST 1/2
time for maximum plasma concentration to decrease by 50%
Time frame: 24 hours
Population: The number of subjects (n) in Treatment D was less than the total 22 subjects for the following PK parameters: CST½ (n=16).
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Sufentanil IV | CST 1/2 | 0.14 hours |
| Sufentanil NanoTab Buccal | CST 1/2 | 2.28 hours |
| Sufentanil NanoTab Sublingual | CST 1/2 | 2.50 hours |
| Sufentanil NanoTab Oral | CST 1/2 | 2.00 hours |
Primary
Tmax
time to maximum plasma concentration
Time frame: 24 hours
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Sufentanil IV | Tmax | 0.07 hours |
| Sufentanil NanoTab Buccal | Tmax | 0.85 hours |
| Sufentanil NanoTab Sublingual | Tmax | 0.83 hours |
| Sufentanil NanoTab Oral | Tmax | 1.11 hours |