1. This bioequivalence study demonstrates that the pharmacokinetic properties of gabapentin 500 mg and zolpidem tartrate 10 mg are unaffected when both treatments are taken simultaneously, compared with each drug taken alone, in healthy participants. |
2. Both treatments were well tolerated when taken alone and in combination, in a population of healthy participants. |
1 Introduction
2 Methods
2.1 Study Design
2.2 Participants
2.3 Analysis of Plasma Samples
2.4 Pharmacokinetic Parameters
2.5 Safety and Tolerability
2.6 Statistical Analyses
3 Results
3.1 Study Population
Characteristic | Number (%) or mean ± standard deviationa
|
---|---|
Male:female | 19:21 |
Age, years | 34.1 ± 8.1 |
Range | 18–45 |
Race | |
White | 24 (60) |
Black, non-Hispanic | 7 (18) |
Other | 9 (23) |
Weight (kg) | 68.3 ± 9.7 |
Range | 51.4–92.7 |
Body mass index (kg/m2) | 25.4 ± 2.7 |
Range | 20.7–32.1 |
3.2 Pharmacokinetic Analyses
Parameter (units) | Gabapentin + zolpidem (test) [mean (SD)] | Gabapentin (reference) [mean (SD)] | Ratio (%)a
| 90 % Confidence intervala
| |
---|---|---|---|---|---|
Lower | Upper | ||||
n
| 38 | 38 | |||
C
max (μg/mL) | 4.61 (1.11) | 4.72 (1.18) | 97.0 | 92.0 | 102.0 |
AUC0–tlqc (μg h/mL) | 52.5 (12.6) | 50.2 (12.1) | 104.0 | 98.8 | 109.0 |
AUC0–∞ (μg h/mL) | 53.4 (12.9) | 51.0 (12.4) | 104.0 | 99.0 | 109.0 |
t
max (h) | 4.63 (1.95) | 3.64 (1.17) | – | – | – |
t
½ (h) | 5.47 (1.06) | 5.49 (0.86) | – | – | – |
Parameter (units) | Zolpidem + gabapentin (test) [mean (SD)] | Zolpidem (reference) [mean (SD)] | Ratio (%)a
| 90 % Confidence intervala
| |
---|---|---|---|---|---|
Lower | Upper | ||||
n
| 38 | 37 | |||
C
max (ng/mL) | 154 (49.9) | 138 (43.9) | 111.0 | 104.0 | 118.0 |
AUC0–tlqc (ng h/mL) | 898 (381) | 842 (338) | 105.0 | 98.0 | 112.0 |
AUC0–∞ (ng h/mL) | 912 (386) | 854 (341) | 105.0 | 98.1 | 112.0 |
t
max (h) | 1.45 (0.94) | 1.84 (1.23) | – | – | – |
t
½ (h) | 3.47 (1.17) | 3.44 (1.21) | – | – | – |
3.3 Safety and Tolerability
Gabapentin | Zolpidem | Gabapentin + zolpidem | |
---|---|---|---|
Evaluable participants | 39 | 38 | 38 |
Participants [n (%)] reporting AEs | 1 (2.6) | 3 (7.9) | 1 (2.6) |
Participants [n (%)] withdrawing due to AEs | 0 (0) | 0 (0) | 0 (0) |
Participants [n (%)] with treatment-related AEsa
| 1 (2.6) | 3 (7.9) | 1 (2.6) |
Number of AEs | 1 | 4 | 2 |
Number of serious AEs | 0 | 0 | 0 |
Number of AEs by intensity | |||
Mild | 1 | 4 | 2 |
Moderate/severe | 0 | 0 | 0 |
Participants (n) reporting AE (by type) | |||
Dizziness | 0 | 1 | 1 |
Headache | 1 | 1 | 0 |
Vomiting | 0 | 1 | 0 |