TABLE 6.
Penetration of the new fluoroquinolones and ciprofloxacin into selected fluids and tissues
| Site | Tissue to serum or fluid to serum ratio (reference) | ||||
|---|---|---|---|---|---|
| Ciprofloxacin (sampling time 1 to 6 h postdose) | Grepafloxacin (sampling time 2 to 5 h postdose) | Levofloxacin (sampling time 1 to 6 h postdose) | Sparfloxacin (sampling time 2 to 6 h post dose) | Trovafloxacin (sampling time 2 to 6 h postdose) | |
| Aqueous humour | 0.13 (139) | ND | 0.23 (118)† | 0.22 (154) | ND |
| Cerebrospinal fluid | 0.37 (106)* | ND | 0.16 (118) | 0.25 (154) 0.36 (154)* |
0.2 (155)‡ |
| Gall bladder | |||||
| Tissue | ND | 6.22 (147)* | 1.42 (118,152) | 7.1 (154)*,§ | ND |
| Bile | 5.08 (139) | 56.4 (147)* | 5.92 (118,152) | 9.6 (154)¶ | ND |
| Inflammatory (blister) fluid | 1.17 (145) | 1.81 (148) | 0.96 (153)* | 1.17 (145) | 0.64 (156) |
| Male genital tissues | |||||
| Epididymis | ND | 4.88 (149) | 1.22 (118) | ND | ND |
| Testis | ND | 4.95 (149) | 1.63 (118) | ND | ND |
| Prostate | |||||
| Prostatic fluid | 2.26 (106) | 1.23 (150) | ND | 1.5 (154) | ND |
| Tissue | 1.86 (139) | 3.60 (149) | 1.28 (118) | 1.4 (154)¶ | 0.96 (157)* |
| Respiratory tract | |||||
| Alveolar macrophages | 14.3 (146)*,** | 123.07 (151)* | ND | 41.3 (146)** | 13.32 (158) 24.10 (158)* |
| Bronchial mucosa | 1.7 (146)*,** | 2.85 (151)* | ND | 3.3 (146)** | 1.07 (158) 1.12 (158)* |
| Epithelial lining fluid | 1.9 (146)*,** | 12.30 (151)* | ND | 11.9 (146)** | 2.27 (158) 5.85 (158)* |
| Skin | 1.9 (139) | ND | 1.14 (118) | 1.2 (154) | ND |
Specific dosages and sampling times for all of the above data were not provided due to lack of space – see appropriate reference for further details (found in bracks beside values). No data were available for clinafloxacin, gatifloxacin and moxifloxacin, hence they were excluded from this table. Inflammatory fluid to serum ratio was determined by taking the ratio of the area under the plasma concentration time curve values (sampling time not applicable). All others were determined by taking the ratio of tissue concentration to serum concentration (or the ratio of the mean tissue concentration to the mean serum concentration).
Multiple doses of the fluoroquinolone were administered to subjects before sample was taken. All other data were collected after a single administration of the study drug.
Sampling time of 2 to 9 h postdose.
Sampling time of 1 to 24 h postdose.
Sampling time of 18 h postdose.
Sample taken at peak concentration reached in the plasma/serum (Cmax) (time not specified in reference).
Sampling time not specified. ND No data