Table 2.
NCA PK parameters estimates in kidneys of CMS/CMS-E2 and formed colistin/colistin B in rats.
| Drug | Dosage (mg·kg CBA) | Tmax (h) | Cmax (µg/g) | Kidney/plasma ratio of Cmax | AUC0 − inf or AUClast (µg·h/g) | Kidney/plasma ratio of AUC0 − inf | t1/2 (min) | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| CMS/CMS-E2 | Colistin/colistin B | CMS/CMS-E2 | Colistin/colistin B | CMS/CMS-E2 | Colistin/colistin B | CMS/CMS-E2 | Colistin/colistin B | CMS/CMS-E2 | Colistin/colistin B | CMS/CMS-E2 | Colistin/colistin B | ||
| CMS | 10 | 2 | 2 | 64.2 ± 38.1 | 10.4 ± 3.13 | 3.00 | 13.7 | 162* | 64.7 | 5.24 | 31.6 | – | 72.6 |
| 20 | 4 | 6 | 281 ± 92.8 | 53.6 ± 11.0 | 7.11 | 12.7 | 1620 | 603 | 10.9 | 26.1 | 61.8 | 374 | |
| CMS-E2 | 20 | 2 | 4 | 105 ± 25.3 | 17.6 ± 6.79 | 5.50 | 15.4 | 289 | 81.5* | 7.80 | 19.7 | 33.6 | – |
| 40 | 4 | 10 | 379 ± 85.5 | 148 ± 32.8 | 7.44 | 20.1 | 2496 | 1406* | 11.0 | 39.6 | 121 | – | |
*The value was AUClast. CMS colistin methanesulphonate, CMS-E2 colistin B methanesulphonate, CBA colistin base activity, Tmax time of maximum observed concentration, Cmax maximum observed concentration, AUC0 − inf area under the concentration-time curve to infinite time, AUClast area under the curve from time 0 to last measurable concentration, t1/2 terminal half-life.