Property: Light Yellow Crystalline Powder,New type of animal dedicated fluoroquinolone drugs. Marbofloxacin is a new type of fluoroquinolone antibiotic, by inhibiting bacterial DNA transcription to inhibit the growth of bacteria, the gram-negative bacteria, gram-positive bacteria and mycoplasma have antibacterial activity. Ma Bo effect through oral and injected drugs were able to absorb good, low toxic and side effect.

Pharmacokinetics: absorption was rapid and complete after administration and injection, plasma protein binding rate was low, tissue distribution was wide, and it was well distributed in kidney, liver, lung and skin. The oral bioavailability of pregnant sows and cats was about 80%, and that of calves was more than 100%. All the tissue concentrations detected were higher than those in plasma. Some of them were metabolized into inactive metabolites such as N-demethylation MBF and N-oxygen MBF in the liver. The main excretion pathway was the kidney, and the canine excreted 3045% of the prototype drug in urine. Intramuscular injection and subcutaneous administration of fowl (intramuscular injection), broiler (intramuscular injection), sows (intramuscular injection) were 4.33, 5.265.74 and 10 h, respectively, and the effective blood concentration was maintained for a longer period of time after intramuscular injection and subcutaneous injection, respectively, for 14 h and 13 h.

Application: Fluoroquinolone antibiotic, used for treatment of deep and superficial skin infection, urinary tract infection, the cat's skin and soft tissue infection, acute upper respiratory tract infection. Used for sensitive bacteria caused by cattle, pigs, dogs, cats, respiratory tract, the digestive tract, urinary tract, skin infections, etc. For cattle, sheep mastitis mastitis and pigs - metritis - no milk syndrome are malignant.

Usage :Used for sensitive bacteria caused by cattle, pigs, dogs, cats, respiratory tract, the digestive tract, urinary tract, skin infections, etc. For cattle, sheep mastitis mastitis and pigs - metritis - no milk syndrome are malignant.

Table 1: Mean pharmacokinetic parameters following intravenous administration of marbofloxacin to 6 adult beagle dogs at a dosage of 2.5 mg/lb.

Parameter	Estimate ± SD* n=6
Total body clearance, (mL/h•kg)	94 ± 8
Volume of distribution at steady state, Vss, (L/kg)	1.19 ± 0.08
AUC0-inf (μg•h/mL)	59 ± 5
Terminal plasma elimination half-life, t1/2(h)	9.5 ± 0.7

* SD = standard deviation

Table 2: Mean pharmacokinetic parameters following oral administration of marbofloxacin tablets to adult beagle dogs at a nominal dosage of 1.25 mg/lb or
2.5 mg/lb and to cats at 2.5 mg/lb.†

 

 

Parameters	Dog Estimate ± SD* (1.25 mg/lb) n=6	Dog Estimate ± SD* (2.5 mg/lb) n=6	Cat Estimate ± SD* (2.5 mg/lb) n=7
Time of maximum concentration, Tmax(h)	1.5 ± 0.3	1.8 ± 0.3	1.2 ± 0.6
Maximum concentration, Cmax, (μg/mL)	2.0 ± 0.2	4.2 ± 0.5	4.8 ± 0.7
AUC0-inf (μg•h/mL)	31.2 ± 1.6	64 ± 8	70 ± 6
Terminal plasma elimination half-life, t1/2(h)	10.7 ± 1.6	10.9 ± 0.6	12.7 ± 1.1

† mean actual dosages administered to dogs were 1.22 mg/lb and 2.56 mg/lb, respectively, and the mean
actual dosage administered to cats was 2.82 mg/lb.
* SD = standard deviation

Figure 2: Mean plasma concentrations (µg/mL) following single oral administration of marbofloxacin to adult beagle dogs at dosages of 1.25 mg/lb or 2.5 mg/lb.

* See Table 4 in Microbiology section for MIC data.

Figure 3: Mean plasma concentrations (µg/mL) following single oral administration of marbofloxacin to adult cats at a dosage of 2.5 mg/lb.

* See Table 5 in Microbiology section for MIC data.

Table 3a: Tissue distribution following a single oral administration of marbofloxacin tablets to adult beagle dogs at a dosage of 1.25 mg/lb*.

Tissue	Marbofloxacin 2 hours (n=4)	Concentrations 18 hours (n=4)	(μg/g ± SD) 24 hours (n=4)
bladder	4.8 ± 1.1	2.6 ± 1.5	1.11 ± 0.19
bone marrow	3.1 ± 0.5	1.5 ± 1.5	0.7 ± 0.2
feces	15 ± 9	48 ± 40	26 ± 11
jejunum	3.6 ± 0.5	1.3 ± 1.0	0.7 ± 0.3
kidney	7.1 ±1.7	1.4 ± 0.5	0.9 ± 0.3
lung	3.0 ± 0.5	0.8 ± 0.2	0.57 ± 0.19
lymph node	5.5 ± 1.1	1.3 ± 0.3	1.0 ± 0.3
muscle	4.1 ± 0.3	1.0 ± 0.3	0.7 ± 0.2
prostate	5.6 ± 1.4	1.8 ± 0.6	1.1 ± 0.4
skin	1.9 ± 0.6	0.41 ± 0.13	0.32 ± 0.08

* SD = standard deviation

Table 3b: Tissue distribution following a single oral administration of marbofloxacin tablets to adult beagle dogs at a dosage of 2.5 mg/lb.

Tissue	Marbofloxacin 2 hours (n=4)	Concentrations 18 hours (n=4)	(μg/g ± SD*) 24 hours (n=4)
bladder	12 ± 4	6 ± 7	1.8 ± 0.4
bone marrow	4.6 ± 1.5	1.28 ± 0.13	0.9 ± 0.3
feces	18 ± 3	52 ± 17	47 ± 28
jejunum	7.8 ± 1.1	2.0 ± 0.3	1.1 ± 0.3
kidney	12.7 ±1.7	2.7 ± 0.3	1.6 ± 0.2
lung	5.48 ± 0.17	1.45 ± 0.19	1.0 ± 0.2
lymph node	8.3 ± 0.7	2.3 ± 0.5	2.03 ± 0.06
muscle	7.5 ± 0.5	1.8 ± 0.3	1.20 ± 0.12
prostate	11 ± 3	2.7 ± 1.0	2.0 ± 0.5
skin	3.20 ± 0.33	0.705 ± 0.013	0.46 ± 0.09

* SD = standard deviation

 

Microbiology

The primary action of fluoroquinolones is to inhibit the bacterial enzyme, DNA gyrase. In susceptible organisms, fluoroquinolones are rapidly bactericidal at relatively low concentrations. Marbofloxacin is bactericidal against a broad range of gram-negative and gram-positive organisms. The minimum inhibitory concentrations (MICs) of pathogens isolated in clinical field studies performed in the United States were determined using National Committee for Clinical Laboratory Standards (NCCLS) standards, and are shown in Tables 4 and 5.

Table 4. MIC Values* (μg/mL) of marbofloxacin against pathogens isolated from skin, soft tissue and urinary tract infections in dogs enrolled in clinical studies conducted during 1994–1996.

Organism	No. of Isolates	MIC50	MIC90	MIC Range
Staphylococcus intermedius	135	0.25	0.25	0.125-2
Escherichia coli	61	0.03	0.06	0.015-2
Proteus mirabilis	35	0.06	0.125	0.03-0.25
Beta-hemolytic Streptococcus, (not Group A or Group B)	25	1	2	0.5-16
Streptococcus, Group D enterococcus	16	1	4	0.008-4
Pasteurella multocida	13	0.015	0.06	≤0.008-0.5
Staphylococcus aureus	12	0.25	0.25	0.25-0.5
Enterococcus faecalis	11	2	2	1-4
Klebsiella pneumonia	11	0.06	0.06	0.01-0.06
Pseudomonas spp.	9	**	**	0.06-1
Pseudomonas aeruginosa	7	**	**	0.25-1

* The correlation between in vitro susceptibility data (MIC) and clinical response has not been
determined.
** MIC50 and MIC90 not calculated due to insufficient number of isolates.

Table 5: MIC Values* (μg/mL) of marbofloxacin against pathogens isolated from
skin and soft tissue infections in cats enrolled in clinical studies conducted in 1995
and 1998.

Organism	No. of Isolates	MIC50	MIC90	MIC Range
Pasteurella multocida	135	0.03	0.06	≤0.008-0.25
Beta-hemolytic Streptococcus	22	1	1	0.06-1
Staphylococcus aureus	21	0.25	0.5	0.125-1
Corynebacterium spp.	14	0.5	1	0.25-2
Staphylococcus intermedius	11	0.25	0.5	0.03-0.5
Enterococcus faecalis	10	2.0	2.0	1.0-2.0
Escherichia coli	10	0.03	0.03	0.015-0.03
Bacillus spp.	10	0.25	0.25	0.125-0.25