Marbofloxacin

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Chemical Structure| 115550-35-1 同义名 : 马波沙星
CAS号 : 115550-35-1
货号 : A352968
分子式 : C17H19FN4O4
纯度 : 98+%
分子量 : 362.36
MDL号 : MFCD00864820
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Topo II
描述 Marbofloxacin is a third generation fluoroquinolone and orally active antimicrobial agent, which has a broad spectrum bactericidal activity and good efficacy. [3]. Marbofloxacin is a fluoroquinolone antibiotic and highly effective treatment for respiratory diseases. The minimum inhibitory concentration (MIC, 1 μg/ml in TSB, 2 μg/ml in serum), minimum bactericidal concentration (MBC, 4 μg/ml in TSB, 4 μg/ml in serum), and mutant prevention concentration (2.56 μg/ml in TSB) for marbofloxacin against Streptococcus suis (HB2). In serum, by inhibitory sigmoid Emax modeling, the AUC0-24h/MIC values for marbofloxacin against HB2 were 25.23 (bacteriostatic), 35.64 (bactericidal), and 39.71 (elimination) h[4]. MBF is a concentration-dependent drug and the AUC/MIC ratio is the best PK/PD predictor for its efficacy. The MBF dosage of 4 mg/kg appeared to produce an appropriate value of the PK-PD surrogate that predicts antibacterial success for disease caused by susceptible bacteria[5]. All strains tested of E. coli (MIC90 = 0.06 μg/ml) and S. aureus (MIC90 = 0.25 μg/ml) were susceptible to marbofloxacin. PK/PD analysis suggests that the therapeutic regimen of marbofloxacin could be effective for infections caused by E. coli strains in animals between 3 and 80 days, with a CFR for Cmax /MIC > 10 of 100% and for AUC24 /MIC > 125 of 99.99%[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.80mL

2.76mL

1.38mL

27.60mL

5.52mL

2.76mL
参考文献

[1]Voermans M, van Soest JM, et al. Clinical efficacy of intravenous administration of marbofloxacin in a Staphylococcus aureus infection in tissue cages in ponies. J Vet Pharmacol Ther. 2006 Dec;29(6):555-60.

[2]Vouldoukis I, Rougier S, et al. Canine visceral leishmaniasis: comparison of in vitro leishmanicidal activity of marbofloxacin, meglumine antimoniate and sodium stibogluconate. Vet Parasitol. 2006 Jan 30;135(2):137-46.

[3]Voermans M, van Soest JM, van Duijkeren E, Ensink JM. Clinical efficacy of intravenous administration of marbofloxacin in a Staphylococcus aureus infection in tissue cages in ponies. J Vet Pharmacol Ther. 2006 Dec;29(6):555-60

[4]Lei Z, Liu Q, Yang B, Khaliq H, Cao J, He Q. PK-PD Analysis of Marbofloxacin against Streptococcus suis in Pigs. Front Pharmacol. 2017 Nov 20;8:856

[5]Poapolathep S, Laovechprasit W, Giorgi M, Monanunsap S, Klangkaew N, Phaochoosak N, Kongchandee P, Poapolathep A. Pharmacokinetics of marbofloxacin in Green sea turtles (Chelonia mydas) following intravenous and intramuscular administration at two dosage rates. J Vet Pharmacol Ther. 2020 Mar;43(2):215-221

[6]Rubio-Langre S, Aguilar-Sola S, Lorenzutti AM, San Andrés MI, De Lucas JJ, Litterio NJ. Pharmacokinetic evaluation of marbofloxacin after intravenous administration at different ages in llama crias, and pharmacokinetic/pharmacodynamic analysis by Monte Carlo simulation. J Vet Pharmacol Ther. 2018 Dec;41(6):861-870