Table 2.
Pharmacokinetic parameters of ibandronate in serum and urine after administration of ibandronate
| Subjects | Administration | AUCinf (ng h/mL) | C max or C 5min (ng/mL) | T max (h) | t 1/2 (h) | CL (mL/min) | CLr (mL/min) | Fe (%) | |||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Type | Number | Route | Number | Dose (mg) | |||||||
| Healthy postmenopausal women | 8 | Oral | 1 | 20 | 31.2 ± 13.3 | 9.02 ± 3.88 | 0.980 ± 0.457 | 14.4 ± 7.50 | – | 59.4 ± 6.79 | 0.542 ± 0.184 |
| 8 | 1 | 50 | 76.9 ± 31.2 | 24.3 ± 9.93 | 1.00 ± 0.472 | 20.4 ± 4.98 | – | 59.4 ± 9.18 | 0.551 ± 0.257 | ||
| 8 | 1 | 100 | 168 ± 76.5 | 47.2 ± 27.4 | 1.19 ± 0.869 | 21.5 ± 7.66 | – | 115 ± 39.9 | 1.08 ± 0.473 | ||
| 8 | 1 | 150 | 329 ± 156 | 86.0 ± 46.1 | 1.19 ± 0.572 | 23.0 ± 6.68 | – | 61.8 ± 14.1 | 0.850 ± 0.549 | ||
| Postmenopausal women with osteoporosis | 6 | Oral | 1 | 20 | 33.6 ± 15.9 | 12.9 ± 5.60 | 0.750 ± 0.274 | 9.59 ± 7.34 | – | 38.3 ± 8.08 | 0.407 ± 0.248 |
| 6 | 4 | 20 | 50.2 ± 39.5 | 16.6 ± 11.5 | 0.917 ± 0.204 | 21.3 ± 2.34 | – | – | – | ||
| 6 | 1 | 50 | 96.3 ± 60.8 | 36.5 ± 33.9 | 0.837 ± 0.261 | 16.0 ± 3.86 | – | 40.8 ± 8.28 | 0.479 ± 0.336 | ||
| 6 | 4 | 50 | 99.6 ± 41.5 | 31.2 ± 12.9 | 0.750 ± 0.274 | 19.6 ± 7.38 | – | – | – | ||
| 6 | 1 | 100 | 288 ± 126 | 96.0 ± 52.1 | 0.917 ± 0.204 | 15.9 ± 3.38 | – | 36.0 ± 4.62 | 0.631 ± 0.320 | ||
| 6 | 4 | 100 | 227 ± 70.7 | 111 ± 96.3 | 0.750 ± 0.274 | 16.1 ± 5.03 | – | – | – | ||
| 6 | 1 | 150 | 764 ± 486 | 272 ± 201 | 0.917 ± 0.204 | 17.0 ± 4.00 | – | 34.4 ± 8.17 | 1.08 ± 0.810 | ||
| 6 | 4 | 150 | 754 ± 415 | 254 ± 172 | 1.08 ± 0.492 | 18.9 ± 3.15 | – | – | – | ||
| Postmenopausal women with osteopenia | 10 | i.v. | 1 | 0.25 | 74.4 ± 9.80 | 60.5 ± 7.80 | – | 18.7 ± 1.73 | 56.8 ± 6.90 | 34.3 ± 4.60 | 59.6 ± 4.49 |
| 10 | 1 | 0.5 | 137 ± 16.3 | 117 ± 18.8 | – | 18.5 ± 1.67 | 61.7 ± 7.10 | 34.8 ± 6.80 | 55.4 ± 6.88 | ||
| 10 | 1 | 1.0 | 240 ± 22.7 | 186 ± 36.2 | – | 18.5 ± 0.950 | 70.1 ± 7.30 | 43.9 ± 7.41 | 61.7 ± 9.69 | ||
| 10 | 1 | 2.0 | 541 ± 95.9 | 388 ± 72.3 | – | 18.9 ± 1.99 | 63.3 ± 10.7 | 41.9 ± 9.78 | 64.6 ± 7.92 | ||
Estimates are mean ± SD
AUC inf area under the concentration–time curve from 0 to infinity, C max maximum concentration, C 5min concentration at 5 min after administration, T max time to reach maximum concentration, t 1/2 half-life, CL clearance, CLr renal clearance, Fe fraction of administered dose excreted in urine up to 48 or 72 h postdose