Safety and Efficacy of Balofox (Balofloxacin) in the Treatment of Uncomplicated Urinary Tract Infections in Adults (BUTA Study).

Objective: To evaluate the safety and efficacy of Balofox (Balofloxacin) in the treatment of Uncomplicated Urinary Tract Infections in Adults. Design: Open, prospective, noncomparative, observational, multi-center, post-marketing study. Setting: 248 physicians across India in clinical and hospital settings. Patients: A total of 3511 patients of either sex above 18 years of age with laboratory and/or clinical diagnosis of urinary tract infection were administered Balofox (Balofloxacin) orally two times daily for 5-7 days. Respiratory system abnormalities, cardiovascular abnormalities, nervous system abnormalities and abdominal symptoms were seen in 554 patients. Body temperature, abdominal pain and burning during micturation were recorded at baseline and then on days 2, 3, 4, 5 and 6. Global assessment was done by physician independently at the end of therapy on a 4-point Likert scale. Results: Of the 8063 patients enrolled in the study with, 6977 patients had urinary tract infection, but data of 3466 patients was excluded from analysis due to insufficient data and an intention-to-treat analysis done for efficacy on 3511 patients. The body temperature reduced from 102.12°F at baseline to 99.03°F on day 3 (p<0.0001), and upto 97.72 on day 6 (p<0.0001). The scores for abdominal pain and burning during micturation also significantly (p<0.05) reduced on days 2, 3, 5, & 6 from baseline. The commonly reported adverse events were nausea (5.95%), headache (1.85%), vomiting (1.77%), vertigo and giddiness (1.62%), hyperacidity (1.05%). For global assessment of response to therapy, more than 95% doctors reported the response to therapy as good. More than 90% of doctors reported the tolerability of the drug to be good. Conclusion: Balofox is safe and effective in the management of uncomplicated urinary tract infection in adults.

Farmacocinética plasmática de la balofloxacina en terneros / Farmacocinética plasmática de balofloxacin em bezerros / Plasma pharmacokinetic of balofloxacin in calves

Los parámetros farmacocinéticos de absorción y disposición de balofloxacina se determinaron en terneros hembras raza holando-argentino (n = 6), luego de una dosis única de 5 mg/kg administrada en bolo intravenoso y subcutáneo, en un diseño cruzado de tratamiento. El analito se determinó en muestras de plasma por método microbiológico de difusión en agar utilizando como microorganismo detector una solución de esporas de Bacillus subtilis BGA y medio de cultivo Antibiotic Nº 1. Las concentraciones plasmáticas de balofloxacina en función del tiempo se analizaron por el modelo cinético no compartimental utilizando el software PK Solution 2.0. Los parámetros farmacocinéticos obtenidos fueron para la vía intravenosa: t1/2  = 2.3 ± 1.1 h; Cltotal área= 10.2 ± 3.4 ml/min/kg; Vdárea= 1.8 ± 0.3 L/kg; ABCárea= 551.3 ± 247.0 g/min/ml. Excepto para CltotaL área y ABCárea, los valores obtenidos para la administración intravenosa difirieron significativamente de los obtenidos del ensayo por vía subcutánea (p<0.05), para el cual se obtuvo un Cmáx= 1.3 ± 0.4 g/ml, con un tmáx= 51 ± 12.1 minutos y una biodisponibilidad cercana al 98%. El valor de Vdárea superior a 1 l/kg obtenido con ambas vías de aplicación indica buena capacidad para difundir a territorios extravasculares y tejidos.

Pharmacokinetic parameters of absorption and disposition of balofloxacin were determined in female Holando-Argentinean calves (n = 6), after a 5 mg/kg single dose, administered as both intravenous and subcutaneous bolus, in a crossed-over design treatment. The analyte was determined in plasma samples by microbiological method in agar diffusion, using a Bacillus subtilis BGA spore solution as microorganism detector in agar Antibiotic Nº 1. The plasmatic concentrations of balofloxacin based on the time were analyzed by a non compartimental kinetic model using software PK Solution 2.0. The intravenous pharmacokinetic parameters obtained were: t1/2β= 2.3 ± 1.1 h; Cltotal area= 10.2 ± 3.4 ml/min/kg; Vdárea= 1.8 ± 0.3 L/kg; and AUCárea= 551.3 ± 247.0 μg/min/ml. Except for Cltotal area and AUCarea, the values obtained for the intravenous administration significantly differed from the obtained ones for the subcutaneous route (p<0.05), for which Cmax= 1.3 ± 0.4 μg/ml, tmax= 51 ± 12.1 minutes and bioavailability values close to 98% were obtained. The Vdarea value was superior to 1 l/kg for both routes of application and indicates good capacity to spread to extravascular area and tissues.

Os parâmetros farmacocinéticos de absorção e eliminação dos balofloxacin foi determinada nos bezerros Holando-argentina (n = 6), depois de uma dose única de 5 mg/kg, uma vez que ambos foram administrados em bolus por via intravenosa e subcutânea, em um design de tratamento cruzado. O analito foi determinado em amostras de plasma por método microbiológico de difusão em ágar, utilizando uma solução de esporos de microorganismo Bacillus subtilis BGA como detector em ágar antibiótica Nº 1. As concentrações plasmáticas de balofloxacin com base no tempo não foram analisados por um modelo de cinética compartimental usando software PK Solução 2,0. O parâmetros farmacocinéticos da via intravenosa obtidos foram: t1/2 β = 2.3 ± 1.1 h; Cltotal área = 10.2 ± 3.4 ml / min / kg; Vdárea = 1.8 ± 0.3 l/kg; e AUCárea = 551,3 ± 247,0 μg/min/ml. Exceto para Cltotal área e AUCárea, os valores obtidos para a administração intravenosa diferiu significativamente do obtido para a via subcutânea, (p<0,05), para a qual Cmax = 1.3 ± 0.4 μ g/ml, tmax = 51 ± 12.1 minutos e biodisponibilidade perto de 98% foram obtidos. O valor Vdarea foi superior a 1 l/kg para ambas as vias de aplicação e indica uma boa capacidade de propagação de espaço extravascular e tecidos.

Balofloxacin and levofloxacin in the treatment of 215 cases of bacterial infections in urinary system lower respiratory tract / 重庆医科大学学报

0.05).Conclusion:Balofloxacin is as effective and well-tolerated as levofloxacin for the treatment of bacterial infections in urinary system respiratory tract.

A Multi-center Study to Evaluate the Efficacy and Safety of Balofloxacin and Ofloxacin for Patients with Uncomplicated Urinary Tract Infection / 대한비뇨기과학회지

PURPOSE: Balofloxacin is a new fluoroquinolone antibiotic that has potent, broad-spectrum, antimicrobial activity and a good safety profile during preclinical study. The aim of this study was to evaluate the efficacy and safety of balofloxacin in comparison with those of ofloxacin for uncomplicated urinary tract infections. MATERIALS AND METHODS: Patients randomly received oral balofloxacin at 100mg twice a day or oral ofloxacin at 200mg twice a day for 5 days at a ratio of 2:1. Efficacy was assessed by the eradication rate of baseline pathogens and clinical outcome of the objective disease. Safety was assessed by adverse events, changes in laboratory tests and vital signs. RESULTS: The bacteriological efficacy rate was 83.9%(99/118) in the balofloxacin group and 88.4%(61/69) in the ofloxacin group. In the equivalence test using 15% as the standard, clinically acceptable difference value of efficacy, balofloxacin was equivalent to ofloxacin [95% CI: -14.6% to 5.5%]. The bacteriological evaluation of the case whose baseline pathogen was susceptible to the study drug was 96.6%(84/87) for the balofloxacin group and 92.6%(50/54) for the ofloxacin group [95% CI: -4.0% to 11.9%], thereby demonstrating equivalence; as did the relatively high clinical success rates of 99.2% and 95.7%, respectively. The adverse event rate and the drug-related adverse event rate for the balofloxacin group was significantly lower than that of the ofloxacin group(p=0.036, 0.031). Neither unusual laboratory findings nor abnormal vital signs were reported for either group and there were no significant differences between the treatment groups. CONCLUSIONS: Twice daily administration of 100mg balofloxacin is as effective as twice daily administration of 200mg ofloxacin for the treatment of uncomplicated urinary tract infections. With regard to safety, balofloxacin was confirmed to be safer than ofloxacin.

Pharmacokinetics of Balofloxacin Tablets in Chinese Healthy Volunteers / 中国药房

OBJECTIVE:To study the pharmacokinetics of balofloxacin tablets in Chinese healthy volunteers.METHODS:A single dose of 100 or 200 mg balofloxacin tablets were given to 12 healthy volunteers in a randomized crossover design.Concentrations of balofloxacin in plasma and urine were determined by HPLC with data processed by DAS(drug and statistics)software.RESULTS:After administration of balofloxacin 100 mg and 200 mg,the Cmax were(0.970?0.245)?g?mL-1 and(1.849?0.466)?g?mL-1;the tmax were(1.25?1.10)h and(1.24?0.81)h;the t1/2 were(7.14?1.01)h and(7.11?0.72)h;the AUC0～36 were(7.309?1.368)?g?h?mL-1 and(15.214?1.727)?g?h?mL-1;AUC0～∞ were(7.531?1.386)?g?h?mL-1 and(15.695?1.762)?g?h?mL-1;the accumulative eliminating rates within 36 h in urine were(64.47?11.56)% and(63.24?11.93)%,respectively.CONCLUSION:The pharmacokinetics of balofloxacin in healthy volunteer after oral administration was characterized by high peak concentration and long half life.The method is sensitive,accurate,reliable and specific,and can satisfy the requirements for pharmaceutical study.