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Gatifloxacin Sesquihydrate

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Chemical Structure| 180200-66-2 同义名 : AM-1155 sesquihydrate;BMS-206584 sesquihydrate;PD135432 sesquihydrate
CAS号 : 180200-66-2
货号 : A152235
分子式 : C38H50F2N6O11
纯度 : 95%
分子量 : 804.83
MDL号 : MFCD22373645
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Gatifloxacin (Sesquihydrate) is an antibiotic of the fourth-generation fluoroquinolone family. Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin[3]. Gatifloxacin possessed potent activity (MIC, 0.39 microg/ml) against the NorA-overproducing strain S. aureus NY12, the norA transformant, which was slightly lower than that against the parent strain SA113[4]. Ocular inserts of gatifloxacin were prepared successfully by using solvent casting method for sustained drug delivery. The cross-linked and Eudragit RL-100 coated ocular insert of gatifloxacin provides better in vitro drug release and sustained upto 11h[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.24mL

0.25mL

0.12mL

6.21mL

1.24mL

0.62mL

12.42mL

2.48mL

1.24mL

参考文献

[1]Pantel A, Petrella S, et al. Extending the definition of the GyrB quinolone resistance-determining region in Mycobacterium tuberculosis DNA gyrase for assessing fluoroquinolone resistance in M. tuberculosis. Antimicrob Agents Chemother. 2012 Apr;56(4):1990-6.

[2]Khurana G, Arora S, Pawar PK. Ocular insert for sustained delivery of gatifloxacin sesquihydrate: Preparation and evaluations. Int J Pharm Investig. 2012;2(2):70–77

[3]Jensen H, Zerouala C, Carrier M, Short B. Comparison of ophthalmic gatifloxacin 0.3% and ciprofloxacin 0.3% in healing of corneal ulcers associated with Pseudomonas aeruginosa-induced ulcerative keratitis in rabbits. J Ocul Pharmacol Ther. 2005;21(1):36–43

[4]Fukuda H, Hori S, Hiramatsu K. Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998;42(8):1917–1922