Ceftobiprole medocaril (BAL5788) sodium is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens.
性状
Solid
体内研究(In Vivo)
Ceftobiprole medocaril (s.c.; 3 × q12h; total daily doses of BAL9141 equivalents, 2.1, 4.2, or 8.4 mg/kg) causes ten-day cumulative survival rates ranged from 57 to 100% for female Swiss albino mice (body weight, 20 to 22 g) infected Pen Cro Ctx strain P-15986.
Ceftobiprole medocaril (10, 40, 160 mg/kg; single dose; sc) has T 1/2 s from 20 min to 31 min, as the dose rose from 40 mg/kg to 160 mg/kg. The AUC/dose values for the escalating single doses ranges from 0.585 to 1.33, and the C max /dose values decreases from 1.08 to 0.90 in neutropenic thigh-infected mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
ClinicalTrial
参考文献
[1]. E Azoulay-Dupuis, et al. Efficacy of BAL5788, a prodrug of cephalosporin BAL9141, in a mouse model of acute pneumococcal pneumonia. Antimicrob Agents Chemother. 2004 Apr;48(4):1105-11.[2]. W A Craig, et al. In vivo pharmacodynamics of ceftobiprole against multiple bacterial pathogens in murine thigh and lung infection models. Antimicrob Agents Chemother. 2008 Oct;52(10):3492-6.
溶解度数据
In Vitro: DMSO : 250 mg/mL (350.81 mM; Need ultrasonic)配制储备液