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Objective: To evaluate the tolerability and pharmacokinetics of sitafloxacin fumarate injection in healthy Chinese volunteers.Methods:A total of 40 volunteers, half male and half female, were enrolled for single administration and multiple administrations of sitafloxacin fumarate injection. The single dose groups were further divided into 400 mg group and 500 mg group, and the tolerance was investigated. Multiple dose groups were divided into 300 mg (qd) group and 400 mg (qd) group to investigate the tolerability and pharmacokinetics. Adverse reactions were observed during the trial, and changes in vital signs, laboratory tests and other data were monitored to evaluate the safety and tolerability of the drug. The plasma concentrations of sitafloxacin were determined using HPLC-MS/MS, and its pharmacokinetic parameters were calculated and statistically analyzed.Results:No serious adverse events occurred during the trial. Main pharmacokinetic parameters of sitafloxacin after repeated administration are as follows: Cmax, AUC0-t, and AUC0-∞ are (2 913.00±436.63) μg·L-1, (18 368.93±4 141.28) h·μg·L-1 and (19 662.17±4 820.31) h·μg·L-1 in 300 mg (qd) group on day 1 of repeated administration; while (3 080.00±695.11) μg·L-1, (22 625.89±5 729.43) h·μg·L-1, and (22 990.68±5 866.94) h·μg·L-1 on day 7. The corresponding values are (4 590.00±894.67) μg·L-1, (24 113.91±5 030.12) h·μg·L-1 and (25 277.71±5 159.69) h·μg·L-1 in 400 mg (qd) group on day 1 of repeated administration; while (4 570.00±1 230.04) μg·L-1, (30 280.20±7 007.20) h·μg·L-1 and (30 586.30±7 055.85) h·μg·L-1 on day 7.Conclusion:Sitafloxacin fumarate injection is safe and well tolerated in Chinese healthy volunteers. The dynamic characteristics of multipledoses were nonlinear, without significant accumulation in patients of once-daily administration. There was no statistical significance in gender difference of main pharmacokinetic parameters within the same dose group.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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