TABLE 3.
Pharmacokinetic Assessments of Metformin Showing Parameters of Metformin for Various Dose Cohorts Computed Using Noncompartmental Analysisa
| Dose, mg | Tmax, Hours | Cpmax, ng/mL | AUC (0–4 Hours), ng/mL*Hour | |||||
|---|---|---|---|---|---|---|---|---|
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| Dose Cohort | Day -7 or Day -14 | Day 1 | Day -7 or Day -14 | Day 1 | Day -7 or Day -14 | Day 1 | Day -7 or Day -14 | Day 1 |
|
| ||||||||
| 1 | 500 bid | 1000 bid | 2.5 ± 1.2 (6 patients) | 4 (2 patients) | 1647 ± 551 (6 patients) | 2045 ± 1022 (2 patients) | 4828 ± 1469 (6 patients) | 6181 ± 4340 (2 patients) |
| 2 | 500 bid | 850 tid | 1.9 ± 0.9 (9 patients) | 2.7 ± 1.2 (3 patients) | 1139 ± 386 (9 patients) | 2030 ± 550 (3 patients) | 3572 ± 1323 (9 patients) | 6354 ± 2050 (3 patients) |
| 3 | 500 bid | 1000 tid | 2.4 ± 0.9 (5 patients) | 2 (3 patients) | 1215 ± 483 (5 patients) | 2585 ± 1007 (3 patients) | 3633 ± 1460 (5 patients) | 8499 ± 3032 (3 patients) |
Abbreviations: AUC, area under the curve, bid, twice daily; Cpmax, maximum (or peak) serum concentration; tid, three times a day; Tmax, time at which the maximum (or peak) serum concentration is observed.
For analysis, serial blood samples were collected at 0, 0.5, 1, 2, 4, and 24 hours after the administration of metformin on day -7 or day -14 and day 1. Metformin plasma levels were quantitated using a Liquid chromatography–mass spectrometry method.
a
Data are shown as the mean ± SD.