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Prulifloxacin, a broad-spectrum quinolone antibiotic, exhibits three distinct crystal forms, each with different bioavailability and therapeutic properties. It is imperative to assess and control the proportion of each crystal form during the production of raw materials and preparations. Therefore, it is necessary to establish an analytical method that can determine the content of each crystal form in the ternary polycrystalline mixtures. In this study, prulifloxacin crystal forms were analyzed and quantitatively measured using Raman spectroscopy. First, three pure crystal forms of prulifloxacin were prepared under different crystallization conditions and mixed into ternary mixtures at the designed proportions. Subsequently, the ternary mixed crystal samples were analyzed using a Raman microscope.Then run a partial least squares regression analysis to establish a PLS quantitative model using the average spectra data, and a non-negative least squares analysis to establish an area percentage quantitative model using Raman imaging data.The method validation results showed that the two models successfully predicted the proportion of each crystal form within the prulifloxacin polycrystalline mixtures, with a prediction accuracy of less than ± 10 %. Raman spectroscopy was thus established as an effective method for crystal form analysis and quantitative measurement of prulifloxacin. [Display omitted] • Studied the percentage of each crystal form of prulifloxacin by Raman technology. • Established a PLS quantitative model using Raman spectra. • Established an area percentage quantitative model using Raman imaging maps. • The method validation results showed that both models were precise and accurate. [ABSTRACT FROM AUTHOR]

Prulifloxacin is a chemotherapeutic antibiotic of Fluor quinolone drug used to treat a various urinary tract infections. It has short half-life, makes the sustained release (SR) forms extremely advantageous. Sustained release tablets results in increased bioavailability. The purpose of the present study was to develop a sustain release matrix drug delivery system (SR) containing Prulifloxacin as a model drug by using various proportions of polymers such as HPMC E15, HPMC K15. The sustained release formulations of Prulifloxacin were prepared by direct compression method. Optimization of formulation was done by studying effect of drug to polymer ratio on drug release. FT-IR studies indicated absence of any interaction between Prulifloxacin, polymers (HPMC E15 and HPMC K15) and excipients. Ten formulations were prepared and Formulation F8 possesses good drug release property. The tablets were also evaluated for its hardness, friability and other In-vitro evaluation tests. All parameters complied with IP limits. Drug release was diffusion controlled and followed Zero order kinetics. Non-Fickian diffusion was the drug release mechanism for all the tablets formulated. [ABSTRACT FROM AUTHOR]

Highly sensitive and rapid method for the determination of prulifloxacin (PUFX) has been developed on the basis of ion association reaction of PUFX, Y(III) and eosin Y (EY). In pH 6.5 BR buffer medium, PUFX reacts with Y(III) to form a 2:1 cationic chelate which further reacts with EY to form 2:1 ion-association complex. As a result, not only the spectra of absorption are changed, but quenching of fluorescence and significant enhancement of resonance Rayleigh scattering (RRS) is observed. Furthermore, a new RRS spectrum would appear, and the maximum RRS wavelength was located at about 375 nm. The fluorescence quenching (FQ) and enhanced RRS intensity were directly proportional to the PUFX concentration in the ranges of 1.5 - 7.6 μg mL-1 and 0.004 - 3.0 μg mL-1 with detection limits 8.5 ng mL-1 and 1.1 ng mL-1, respectively. The optimum conditions of RRS method and the effects of coexisting substances on the reaction were investigated. In addition the composition of ion-association complexes, the reaction mechanism, the energy transfer between absorption, fluorescence and RRS and reasons for RRS enhancement were discussed. The methods were applied to the determination of PUFX in pharmaceutical samples with satisfactory results. [ABSTRACT FROM AUTHOR]

The chronic course and evolution of chronic obstructive pulmonary disease (COPD) is often characterized by periods of exacerbation of symptoms, which have a negative impact on the quality of life of patients, as well as on the evolution of COPD, and represent a significant cause of medical intervention and hospitalization. Very few data are available on the efficacy of rescue antibiotics in patients with acute exacerbation of COPD (AECOPD) unresponsive to previous treatment. The aim of this study was to evaluate the efficacy of two fluoroquinolones in AECOPD previously treated without success. The FADOI-FLOR study is a randomized, single-blind, non-inferiority comparison between levofloxacin and prulifloxacin. Primary end-point was “therapeutic success” at Day 10 of treatment, defined as disappearance of signs/symptoms or decrease of at least three points of a global score of symptomatology (maximum score = 15). 258 patients were enrolled (128 levofloxacin and 130 prulifloxacin), in 25 centers. A very high proportion of patients in the two groups had therapeutic success at Day-10 (levofloxacin 93.0% vs prulifloxacin 96.7%, population intention-to-treat; 94.6% vs 99.1%, population per-protocol). Earlier therapeutic success (within 7 days) was achieved in 32.0% and 36.2% of patients receiving levofloxacin or prulifloxacin, respectively. At 3-month follow-up, re-exacerbations occurred in 17.8% of patients treated with levofloxacin and 14.2% of those receiving prulifloxacin (p= 0.44). In conclusion, fluoroquinolones are very effective in the treatment of AECOPD resistant to other antibiotics. [ABSTRACT FROM PUBLISHER]

A novel sensitive analytical method based on the use of a semi-automatic microextraction by packed sorbents (MEPS) techniques combined with ultra high-performance liquid chromatography (UHPLC) with PDA detection has been developed and validate for the analysis of ulifloxacin, the active metabolite of prulifloxacin using danofloxacin as internal standard in human plasma and urine. Different experimental parameters were optimized and validated according to international guidelines. Complete separation of the analytes was achieved with a Waters BEH C 18 (50 × 2.1 mm I.D., 1.7 μm particle size) analytical column, a mixture of 10 mM ammonium acetate (pH 3.0) (A) with and acetonitrile (B) both containing 1% triethylamine were used as mobile phase, at a flow rate of 0.6 mL/min in gradient elution, and detection wavelength of 272 nm. This method is linear in concentration range of 0.02–10.0 μg/mL for plasma and urine, respectively. The limit of quantitation was 20 ng/mL for the two fluids. The recoveries of the method were 95% for ulifloxacin in human plasma and urine and 95.5% for the internal standard. Intra- and inter- assay precision and accuracy for ulifloxacin were lower than 10% at all tested concentrations. The proposed method was successfully applied to measure plasma and urine concentrations of ulifloxacin in patients suffering from Peripheral Arterial Disease and for pharmacokinetics study. [ABSTRACT FROM AUTHOR]

The determination of antibiotics in biological samples is compromised by their interaction with proteins. It is showed here that the water resistant zeolite imidazolate framework 67 (ZIF-67) represents a useful sorbent for solid-phase extraction (SPE) of fluoroquinolones (FQs) from biological samples. ZIF-67 is unique in possessing permanent nanoscale porosity and a high surface area. As a result, it efficiently excludes proteins from the inner network but can well adsorb small organic molecules. Its extraction capacity for FQs exceeds that of isostructural ZIF-8, probably due to high affinity for Co(II) ions in ZIF-67. The findings were exploited to design a method for the analysis of FQs, which were extracted from bio-samples by ZIF-67 via SPE. Following elution of the absorbed FQs with NaOH/methanol, they were quantified by HPLC with diode array detection. The assay has a wide linear range that extends from 3.9 to 4000 μg⋅kg‾, with detection limits between 1.2 and 2.9 μg⋅kg‾. The method was successfully applied to the determination of FQs in manure. [Figure not available: see fulltext.] [ABSTRACT FROM AUTHOR]

A new and specific HPLC–DAD method for the direct determination of Prulifloxacin and its active metabolite, Ulifloxacin, in human plasma has been developed. Plasma samples were analysed after a simple solid phase extraction (SPE) clean-up using a new HILIC stationary phase based high-performance liquid chromatography (HPLC) column and an ammonium acetate buffer (5 mM, pH 5.8)/acetonitrile (both with 1% Et3N,v/v) mobile phase in isocratic elution mode, with Danofloxacin as the internal standard. Detection was performed using DAD from 200 to 500 nm and quantitative analyses were carried out at 278 nm. The LOQ of the method was 1 μg/mL of the cited analytes and the calibration curve showed a good linearity up to 25 μg/mL. For both analytes the precision (RSD%) and the trueness (bias%) of the method fulfil with International Guidelines. The method was applied for stability studies, at three QC concentration levels, in human plasma samples stored at different temperature of + 25, + 4 and −20 °C in order to evaluate plasma stability profiles. [ABSTRACT FROM AUTHOR]

Introduction and hypothesis: This multicentre, randomised, non-blinded, parallel group study is designed to assess the null hypothesis that a 3-month prophylactic schedule with fosfomycin is not inferior to prulifloxacin in reducing the number of urinary tract infection episodes during and after prophylaxis in female patients with recurrent urinary tract infections (rUTIs). Methods: One hundred and fifty-two patients with rUTIs who were candidates for prophylaxis therapy were enrolled and randomised to prulifloxacin (group 1) or fosfomycin (group 2). The prophylaxis regimen included a single dose of fosfomycin (one 3-g cachet) per week, or a single dose (600 mg) of prulifloxacin (one tablet) a week for 12 weeks. The inclusion criteria were female patients over 18 years, urine culture responsiveness to drugs at patient recruitment and history of rUTI. Exclusion criteria were pregnancy and counter-indications to this drug therapy. Patients were prospectively randomised. Check-ups were scheduled at 2 weeks, 1 month and 3 months from the beginning of the study and 3, 6, and 12 months after suspension of the therapy. The primary end-points were the reduction of the number of UTIs (negative urine culture) during and after prophylaxis. Results: Final data analysis included 67 patients in group 1 and 57 in group 2. Nine out of 76 patients (group 1) and 19 out of 76 (group 2) dropped out. UTI episodes were significantly reduced in number compared with before prophylaxis ( p < 0.0001) at all study end-points in both groups. No significant differences were found in disease-free duration, as achieved by the two therapy groups (log-rank test; p = 0.41), in the reduction of UTI episodes during and after prophylaxis, in the adverse effects or improved quality of life. Conclusions: Both drugs provided adequate prophylaxis in patients with rUTIs, with no difference in efficacy. [ABSTRACT FROM AUTHOR]

Urinary tract infections are one of the most common reasons for antimicrobial prescriptions, however urine cultures are often unavailable and the choice of antibiotics is therefore empiric. The ideal antimicrobial agent must have specific pharmacokinetic and pharmacodynamic characteristics and an adequate spectrum of activity in order to obtain the potential eradication of the pathogen from the site of infection, minimizing the risk of recurrences and ensuring the best safety profile. There are several factors to be considered in the therapy choice: the type of infection, the increasing presence of extended-spectrum beta-lactamase (ESBL) producing bacteria showing resistance to most antibiotics and the problem of the bacterial internalization, that is a frequent cause of treatment failure and early recurrences. Prulifloxacin is a recent oral fluoroquinolone antibiotic approved in several European countries for the treatment of lower urinary tract infections and shows some interesting advantages in comparison with other antibiotics. [ABSTRACT FROM AUTHOR]

A new, simple, safe, accurate and reproducible spectrophotometric analytical method was developed for the estimation of Prulifloxacin, from its tablet dosage form. In the present investigation, 2.0 M Sodium benzoate solution also known as Neuberg's hydrotropic salt was employed as hydrotropic solubilizing agent to solubilize poorly water-soluble drug Prulifloxacin for its spectrophotometric analysis. The primary objective of the present investigation was to employ this hydrotropic solution to extract the drug from its dosage form, precluding the use of costlier organic solvents. Aqueous solubilities of this selected model drug was to a great extent in 2.0 M sodium benzoate solutions. Various organic solvents like methanol, chloroform, ethanol, acetonitrile, hexane and toluene are widely used to conduct the spectrophotometric analysis, but higher cost and toxicity prevents their frequent use. The results of the analysis were validated statistically and by recovery studies. The ? max was observed at 296nm. The drug follows Beer's law in concentration range of 15-60 mcg/ml with coefficient correlation value of 0.992. The mean percent recovery was 100.49%. [ABSTRACT FROM AUTHOR]

ABSTRACT A simple spectrofluorimetric method is described for the determination of DNA, based on its enhancement of the fluorescence intensity of prulifloxacin (PUFX)-Tb3+. The luminescence intensity of the PUFX-Tb3+ complex increased up to 10-fold after adding DNA. The excitation and emission wavelengths were 345 and 545 nm, respectively. Under optimum conditions, variations in the fluorescence intensity showed a good linear relationship with the concentration of hsDNA in the range of 3.0 × 10-9 to 1.0 × 10-6 g/mL, with a correlation coefficient ( R) of 0.997, and the detection limit was 2.1 × 10-9 g/mL. The method was successfully applied to the determination of DNA in synthetic samples, and recoveries were in the range 97.3-102.0%. The mechanism of fluorescence enhancement of the PUFX-Tb3+ complex by DNA is also discussed. The mechanism may involve formation of a ternary complex mainly by intercalation binding together with weak electrostatic interaction, which will increase the energy transition from ligand to Tb3+, increasing the rigidity of the complex, and decreasing the radiationless energy loss through O-H vibration of the H2O molecule in the PUFX-Tb3+ compl+osed method is not only more robust and friendly to the environment, but also of relatively higher sensitivity. Copyright © 2013 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

The aim of the study was to compare the efficacy and safety of singledose prulifloxacin vs. single-dose pefloxacin in the treatment of patients with acute uncomplicated urinary tract infections. Two hundred and thirty-one female out-patients were considered microbiologically evaluable and randomly treated with 600 mg prulifloxacin (116 patients) or 800 mg pefloxacin (115 patients). The most commonly isolated uropathogen at baseline was Escherichia coli (71.4%), followed by Proteus mirabilis (10.8%) and Klebsiella pneumoniae (7.8%). Five-seven days posttreatment, the eradication rate was 97.4% and 92.2% in the prulifloxacin and pefloxacin group, respectively. The one-tailed 95% confidence interval analysis showed the equivalence of treatments. Four weeks from treatment no relapses, reinfections or superinfections were observed. The clinical success rates were 92.2% in the prulifloxacin and 84.3% pefloxacin groups. The safety profile was very good with both drugs. The results of the study make it possible to consider prulifloxacin a possible therapeutic option in patients with acute uncomplicated UTIs.

Abstract: Rationale: Antimicrobial therapy of chronic bronchitis exacerbations in patients with severe chronic obstructive pulmonary disease (COPD) is based on empiric antibiotic treatment. Objectives: To evaluate the efficacy of prulifloxacin versus levofloxacin therapy in severe COPD patients with exacerbations of chronic bronchitis. Methods: This study involved a multicenter, parallel, double-blind, randomized clinical trial. Patients aged 40 years or older, smokers, or ex-smokers (>10 pack-years) with spirometrically confirmed severe COPD (FEV1 ≤ 50% predicted and FEV1/FVC ratio < 0.7) and diagnosed with an acute exacerbation of chronic bronchitis were enrolled in the study. Patients were randomized to receive prulifloxacin 600 mg once a day or levofloxacin 500 mg once a day for 7 days. Measurements and main results: The primary outcome measure was clinical assessment at the TOC visit (7–10 days after the end of treatment) of signs and symptoms of exacerbation, namely sputum purulence, sputum volume, dyspnoea, cough and body temperature assessed through semi-quantitative scales. The ITT population included 346 (174 prulifloxacin, 172 levofloxacin) out of 351 treated subjects. A total of 161 patients with prulifloxacin (92.5%) and 166 with levofloxacin (96.5%) were considered cured at TOC (the difference in the percentage of cured patients was −3.98 with 95%CI of −8.76; 0.79). At the 6-month follow-up, the rates of patients with no relapse of AECB were higher than 95% in both the prulifloxacin and levofloxacin groups. Conclusions: Both prulifloxacin and levofloxacin showed efficacy rates higher than 90% in the treatment of severe COPD patients with exacerbations of chronic bronchitis, with no statistically significant differences between the two antibiotics. The long-term follow-up confirmed a very low incidence of relapse, endorsing the appropriateness of this therapeutic approach. EUDRACT no. 2006-004167-56. [Copyright &y& Elsevier]

Abstract: A novel HPLC method for the simultaneous determination of Prulifloxacin, Ulifloxacin, its process impurities in a tablets formulation and Enrofloxacin, used as Internal Standard, is developed. The separation was successfully carried out with a new stationary phase, HILIC, under isocratic elution mode using ammonium acetate buffer (5mM, pH 5.8) and acetonitrile (12:88, v/v) at a flow rate of 1.0mL/min. Column was thermostated at 25°C (±1°C) and 20μL were injected for the analysis. Calibration curves were linear in the investigated range with correlation coefficient better than 0.9880, while the limit of quantifications ranged from 0.25 to 5μg/mL, depending from the analyte. The within and between batch precision (RSD%) values ranged from 0.11% to 13.9% while within and between batch trueness (bias%) values ranged from 14.0% to −11.3%. This method for the direct determination and quantification of process impurities in pharmaceutical formulations is suitable for routine analyses in quality control laboratories and was applied to evaluate for the first time, the presence and the quantities of cited analytes in commercially available formulation. [Copyright &y& Elsevier]

Abstract: This experiment was designed to investigate correlation among 28-days repeated oral dose toxicity, toxicokinetics and tissue distribution data of ulifloxacin (active metabolite of prulifloxacin) in Wistar albino rats. Prulifloxacin was administered for 28-days in rats at 0, 100, 200, 400mg/kg/day followed by 14-days recovery period. Simultaneously different toxicokinetic parameters and tissue distributions of ulifloxacin was examined by LC–MS/MS method. Plasma levels and tissue concentrations of ulifloxacin were increased with dose-related manner. Ulifloxacin was also distributed to many tissues, and concentration in lungs nearly equivalent to the plasma concentration. Based on these results it was concluded that long-term repeated dose of prulifloxacin may produce different blood parameters abnormality, liver damage, stomach ulcer, joint damage and dysfunction of lungs in rats which relates to high tissue distribution and accumulation of ulifloxacin in these tissues. These findings help in management of prulifloxacin induced adverse effects by appropriate dose selection in clinical practice. [Copyright &y& Elsevier]

Background: Prulifloxacin is a promising fluoroquinolone antibiotic. A multicentre, double-blind, randomized clinical study was designed to evaluate its efficacy and safety compared to that of levofloxacin for the treatment of respiratory and urinary infections of Chinese patients. Methods: A total of 267 patients were enrolled and each was randomly assigned to either the treatment or the control group. Prulifloxacin 264.2 mg (equivalent to ulifloxacin 200 mg) b.i.d. or levofloxacin hydrochloride 200 mg b.i.d. was administered orally for 5-14 days according to a patient's condition. The clinical response, bacterial eradication and incidence of adverse events were evaluated. Results: Two hundred and forty-three patients completed the study. For the modified intention-to-treat population, the cure and effective rates were 45.53 and 82.93% in the prulifloxacin group and 49.18 and 83.61% in the levofloxacin group. For the per-protocol analysis population, the cure and effective rates were 45.90 and 83.61% in the prulifloxacin group and 49.59 and 83.47% in the levofloxacin group. The bacterial eradication rates were 96.59 and 95.35%, and the drug-related adverse event rates were 7.87 and 5.51% in the prulifloxacin and levofloxacin group, respectively. The cure rate and efficacy rate of respiratory and urinary tract infections of the levofloxacin group were better than those of the prulifloxacin group. However, the difference between the 2 groups was not statistically significant (p > 0.05). Conclusion: Prulifloxacin is as effective and well tolerated as levofloxacin in the treatment of respiratory and urinary tract infections. Copyright © 2012 S. Karger AG, Basel [ABSTRACT FROM AUTHOR]

Abstract: A rapid, specific and novel gradient LC–MS method has been developed and validated for the identification and characterization of stressed degradation products (DPs) of prulifloxacin (PF) using liquid chromatography combined with quadrupole time-of-flight electrospray ionization tandem mass spectrometry (LC/Q–TOF–ESI-MS/MS). PF was subjected to hydrolytic (acidic, alkaline and neutral), oxidation, photolytic and thermal stress, as per ICH guidelines Q1A (R2). The drug showed extensive degradation in hydrolytic and oxidative, while it was stable to thermal and photolytic stress conditions. In total, 13 DPs were formed and the chromatographic separation of drug and its DPs was achieved on a C-18 column (4.6×250mm, 5μm) using gradient elution method. All the DPs have been identified and characterized using MS n experiments and accurate mass measurements. The LC–MS method was validated with respect to specificity, linearity, accuracy, precision and robustness. [Copyright &y& Elsevier]

Fluoroquinolones are broad-spectrum antibiotics increasingly utilized as empirical or prophylactic therapy in the management of cancer patients. We evaluated the effects of newer generation fluoroquinolones on the level of gastrointestinal (GI) colonization by Candida albicans in a previously established mouse model. Adult male Crl:CD1 (ICR) BR mice were fed chow containing Candida albicans or regular chow. The mice fed the Candida chow had their gut colonized by the yeast. Both groups were subsequently given levofloxacin, moxifloxacin, prulifloxacin or normal saline for 10 days. Stool cultures were performed immediately before, at the end, and one week after discontinuation of treatment to determine the level of intestinal yeast colonization. Candida-colonized mice treated with fluoroquinolones had substantially higher yeast counts in their stools than control mice fed Candida containing chow but treated with saline. Mice fed regular chow and treated with the study antibiotics or saline did not have any Candida in their stools. Dissemination of Candida to internal organs was not observed in any animal. In conclusion, we have shown that all fluoroquinolones tested induced substantial increases in the murine intestinal concentration of C. albicans. [ABSTRACT FROM AUTHOR]

Abstract: Prulifloxacin is a fluoroquinolone antibiotic that has been approved in several European countries for the treatment of lower urinary tract infections and exacerbations of chronic bronchitis. In this review, PubMed and Scopus databases were searched for potential uses of prulifloxacin beyond respiratory and urinary tract infections. Nine individual articles (eight randomised controlled trials and one cohort study) were regarded as eligible for inclusion in the review. Three of the studies were double-blinded, whilst six were open-label trials. Three studies referred to the treatment of patients with chronic bacterial prostatitis (CBP), one to prophylaxis of patients undergoing transrectal prostate biopsy, one to prophylaxis of women undergoing surgical abortion, two to patients with traveller''s diarrhoea, one to diabetic patients with soft tissue infections or osteomyelitis, and one to improving tolerance of Bacillus Calmette–Guérin (BCG) instillations in patients with bladder cancer. Regarding CBP, prulifloxacin was non-inferior to its comparators, with a trend towards better microbiological outcomes at follow-up. Regarding traveller''s diarrhoea, prulifloxacin resulted in better clinical and microbiological outcomes compared with placebo. Finally, prulifloxacin decreased the adverse events associated with BCG instillations in patients with bladder cancer, without affecting cancer recurrence rates. In summary, prulifloxacin appears to be a promising agent for the treatment of bacterial prostatitis and traveller''s diarrhoea. [Copyright &y& Elsevier]

The main objective of this paper is to investigate the pharmacokinetics of NM394 (an active metabolite of prulifloxacin) and evaluate the dose relationship and accumulation characteristics after single and multiple doses of prulifloxacin. Thirty healthy volunteers were given 132 mg, 264 mg, and 528 mg of prulifloxacin capsules in a randomized test corresponding to low, medium and high groups for single dose trial. With one-week washout period, 264 mg of prulifloxacin capsules were given to eight volunteers of the medium group for multiple doses trial. The concentration of NM394 in serum was determined by a sensitive HPLC method and its pharmacokinetic parameters were analyzed by DAS2.0.1 and evaluated by SPSS statistic software (version 13.0). Various parameters were determined. Numerical experiments show that the pharmacokinetic parameters of NM394 displayed first order linear pharmacokinetic character. There are no big differences in pharmacokinetic characteristics of NM394 between single and multiple doses. Almost no significant accumulation of drugs is observed after multiple doses of 264 mg per day for 7 d and chronopharmacokinetics were first observed. [ABSTRACT FROM AUTHOR]

Abstract: A new fluorescent method was developed based on the ulifloxacin-europium (III)-sodium dodecylbenzene sulfonate system for the determination of ulifloxacin, the active metabolite of prulifloxacin. Sodium dodecylbenzene sulfonate formed a ternary complex with ulifloxacin-europium (III) and significantly enhaneed the characteristic fluorescence of europium (III). The enhanced fluorescence intensity showed a good linear relationship with the concentration of ulifloxacin in the range of 5.0×10−8 – 2.0×10−6M with a detection limit of 2.0×10−10 M (3σ). This method is rapid and sensitive, and has been successfully applied to the determination of ulifloxacin in human urine and serum samples. [Copyright &y& Elsevier]

Abstract: Prulifloxacin is a kind of new oral taking antibiotic of fluoroquinolone. Conjugation reaction of prulifloxacin with trypsin in Britton–Robinson buffer solution of pH 7.96 was analyzed by UV–vis spectrophotometry and fluorescence spectrometry. The intrinsic fluorescence of trypsin was strongly quenched by prulifloxacin. This effect was rationalized in terms of a static quenching procedure. The binding parameters have been evaluated by fluorescence quenching methods. Negative values ΔG 0 for the formation of prulifloxacin–trypsin complex implied that both hydrogen bonds and hydrophobic interactions might play a significant role in prulifloxacin binding to trypsin. The binding distance deduced from the efficiency of energy transfer was 0.84nm for prulifloxacin–trypsin. Furthermore, association constants and binding mechanism were successfully derived from the fluorescence spectra. UV–vis detections supported a change in the secondary structure of proteins caused by the interaction of prulifloxacin with trypsin. [Copyright &y& Elsevier]

Abstract: The interaction between prulifloxacin, a kind of new oral taking antibiotic and pepsin, a kind of enzyme in the stomach has been investigated in vitro under a simulated physiological condition by different spectroscopic methods. The intrinsic fluorescence of pepsin was strongly quenched by prulifloxacin. This effect was rationalized in terms of a static quenching procedure. The binding parameters have been evaluated by fluorescence quenching methods. The negative value of ΔG 0 reveals that the binding process is a spontaneous process. The binding distance R between donor (pepsin) and acceptor (prulifloxacin) was obtained according to the Förster''s resonance energy transfer theory and found to be 0.95nm. The results obtained herein will be of biological significance in pharmacology and clinical medicine. [Copyright &y& Elsevier]

A novel chemiluminescence method was proposed for the determination of prulifloxacin. The method was based on the chemiluminescence reaction of the KMnO4-Na2S2O3-PUFX system sensitized by Tb3+. Under the optimum conditions, the chemiluminescence intensity was proportional to the concentration of the PUFX within the range of 5.0 × 10-8 ∼ 1.0 × 10-5 mol L-1, and the detection limit was 8.0 × 10-9 mol L-1. The proposed method was applied to the analysis of PUFX in tables, serum, and urine samples with satisfactory results. The possible mechanism of this sensitized CL reaction was also discussed. [ABSTRACT FROM AUTHOR]

The interaction between bovine serum albumin (BSA) and prulifloxacin was investigated by ultraviolet spectrophotometer (UV) and fluorescence spectroscopy in this paper. Two-dimensional (2D) correlation spectroscopy was applied to the analysis of fluorescence spectra. The results of spectroscopic measurements suggested that prulifloxacin (PL) have a strong ability to quench the intrinsic fluorescence of bovine serum albumin through static quenching procedure. Thermodynamic parameter enthalpy changes (ΔH) and entropy changes (ΔS) were calculated. Owing to the spectral resolution enhancement in 2D correlation spectroscopy, the structure change of prulifloxacin can be observed. [ABSTRACT FROM AUTHOR]

OBJECTIVE To determine whether the new fluoroquinolone prulifloxacin might improve tolerance to Bacillus Calmette-Guérin (BCG) intravesical therapy in patients with bladder cancer. PATIENTS AND METHODS A series of 72 patients with intermediate- or high-risk nonmuscle-invasive bladder cancer were enrolled in this prospective, randomized, open-label, controlled clinical trial performed at a single tertiary care institution. After complete transurethral resection, patients were randomized to receive induction treatment with BCG and three capsules of prulifloxacin 600 mg or no prophylactic treatment (control group). Adverse events (AEs) were self-recorded by the patients after each instillation and classified by the investigator according to a classification grid considering account duration and intensity. Cystoscopy findings at 3 and 6 months were also recorded. RESULTS There was no significant difference in baseline symptoms between the groups. Overall, there was a significant decrease in the percentage of patients with at least one AE between instillations in prulifloxacin-treated group. The proportion of patients with moderate to severe AEs after the fourth instillation was significantly less in the prulifloxacin-treated group. There was a significant effect of prulifloxacin on the need for anti-tuberculosis treatment. More patients in the control group stopped or delayed the full induction course of BCG instillations (34% vs 19%, P = 0.04). Recurrence rates were not affected by prulifloxacin treatment. CONCLUSION Prulifloxacin reduces the incidence of moderate to severe AEs from BCG intravesical therapy in patients with nonmuscle-invasive bladder cancer, improving compliance to the induction BCG course. These preliminary findings warrant further clinical research. [ABSTRACT FROM AUTHOR]

Abstract: We report the results of a prospective randomised study to evaluate the therapeutic effect of Serenoa repens, Urtica dioica (ProstaMEV®), quercitin and curcumin (FlogMEV®) extracts associated with prulifloxacin in patients affected by chronic bacterial prostatitis (CBP). From a whole population of 284 patients, 143 patients affected by CBP [National Institutes of Health (NIH) class II prostatitis] were enrolled. All patients received prulifloxacin 600mg daily for 14 days, in accordance with antibiogram results. Patients were split into two groups: Group A received prulifloxacin associated with ProstaMEV® and FlogMEV®; Group B received only antibiotic therapy. Microbiological and clinical efficacies were tested by two follow-up visits at 1 month and 6 months, respectively. Quality of life (QoL) was measured using the NIH Chronic Prostatitis Symptom Index (CPSI) and International Prostatic Symptom Score (IPSS) questionnaires. Group A comprised 106 patients and Group B comprised 37 patients. One month after treatment, 89.6% of patients who had received prulifloxacin associated with ProstaMEV® and FlogMEV® did not report any symptoms related to CBP, whilst only 27% of patients who received antibiotic therapy alone were recurrence-free (P <0.0001). Significant differences were found between groups in terms of symptoms and QoL (P <0.0001 for both). Six months after treatment, no patients in Group A had recurrence of disease whilst two patients in Group B did. Questionnaire results demonstrated statistically significant differences between groups (all P <0.001). The association of S. repens, U. dioica (ProstaMEV®), quercitin and curcumin (FlogMEV®) extracts is able to improve the clinical efficacy of prulifloxacin in patients affected by CBP. [Copyright &y& Elsevier]

Prulifloxacin, the lipophilic prodrug of ulifloxacin, is a new oral fluoroquinolone with a broad spectrum of in vitro activity against various Gram-positive and Gramnegative microorganisms. Currently, it is the most potent in vitro fluoroquinolone against Escherichia coli and Pseudomonas aeruginosa, and also has the lowest potential of inducing the emergence of resistant strains for these bacteria. It exhibits good penetration in target tissues and fluids, and possesses a long half-life, thus allowing for once-daily administration. Prulifloxacin has been successfully tested in Phase III randomized, controlled trials including patients with acute exacerbations of chronic bronchitis, uncomplicated and complicated urinary tract infections, and chronic bacterial prostatitis. Results are awaited from recently completed and ongoing Phase III randomized, placebo-controlled studies testing prulifloxacin for the treatment of traveler's diarrhea. Prulifloxacin has an acceptable toxicity profile, comparable to that of other fluoroquinolones, with gastric disturbances, diarrhea, nausea and skin rash of mild-to-moderate severity being the most frequent adverse events. Additional research is needed to further elucidate the promising role of prulifloxacin in the treatment of infections sustained by multidrug-resistant pathogens and to consolidate the wide spectrum of activity from a clinical standpoint. [ABSTRACT FROM AUTHOR]

Determination of thiourea by terbium(III)/ prulifloxacin sensitized potassium permanganate-sulfite chemiluminescence with quenching method. The reaction between KMnO 4 and Na 2 SO 3 brought only weak chemiluminescence, but the chemiluminescence increased sharply in the presence of sensitizer Tb3+/ PUFX. Addition of thiourea can prevent the reaction between KMnO 4 and Na 2 SO 3 , thus the chemiluminescence intensity was significantly decreased. A chemiluminescence quenching method can be established for thiourea detection. [Display omitted] • The KMnO 4 -Na 2 SO 3 system chemiluminescence increased sharply in the presence of sensitizer Tb3+/ PUFX. • The sensitized chemiluminescence can be selectively quenched by thiourea. • A method for determination of thiourea was established. Based on the thiourea quenching of the chemiluminescence of Tb3+/ prulifloxacin (PUFX) sensitized KMnO 4 -Na 2 SO 3 system, a convenient and rapid chemiluminescence method for the determination of thiourea was proposed. The reaction between KMnO 4 and Na 2 SO 3 brought only weak chemiluminescence, but the chemiluminescence increased sharply in the presence of sensitizer Tb3+/ PUFX. Addition of thiourea can prevent the reaction between KMnO 4 and Na 2 SO 3 , thus the chemiluminescence intensity was significantly decreased. Under the optimum conditions, the calibration graphs for thiourea were linear in the range of 1.0 × 10-7 to 4.0 × 10-5 mol•L-1. The limit of detection was 6.4 × 10-8 mol•L-1. The method was applied satisfactorily to the determination of thiourea in tap water, lake water and rice noodles and the spiked recoveries were between 104.7 ~ 113.4%. The possible mechanism of sensitization and quenching was also proposed. [ABSTRACT FROM AUTHOR]

A selective molecular imprinting-chemiluminescence sensor is developed for the determination of prulifloxacin by using a prulifloxacin-imprinted polymer as recognition material and the cerium(IV)/sodium thiosulfate/prulifloxacin chemiluminescence reaction as the detection system. The linear response range of the sensor is from 8.0 × 10-8 to 7.0 × 10-6 mol L-1 with a detection limit of 2.0 × 10-8 mol L-1. The relative standard deviation for 5.0 × 10-7 mol L-1 prulifloxacin solution is 1.3% (n = 7). This sensor has been applied to the determination of prulifloxacin in urine samples, and the results obtained are satisfactory. [ABSTRACT FROM AUTHOR]

A terbium-sensitized fluorescence spectrophotometry method using an anionic surfactant, sodium dodecyl benzene sulphonate (SDBS), was developed for the determination of prulifloxacin (PUFX). It was found that SDBS significantly enhanced the fluorescence intensity of the PUFX-Tb3+ complex (about 13-fold). The optimal experimental conditions were determined as follows: excitation and emission wavelengths of 290 nm and 545 nm, pH 8.0, 4.0 × 10-5 mol L-1 terbium(III), and 4.0 × 10-4 mol L-1 SDBS. The enhanced fluorescence intensity of the system (ΔF) showed a good linear relationship with the concentration of PUFX over the range 6.0 × 10-8 to 2.0 × 10-6mol L-1 with a correlation coefficient of 0.9991. The detection limit (S/N = 3) was determined as 8.5 × 10-9 mol L-1. This method has been successfully applied for the determination of PUFX in pharmaceuticals and human urine/serum samples. Compared with most other methods reported, the rapid and simple procedure proposed here offered higher sensitivity, wider linear range, and good stability. The luminescence mechanism of the system was also discussed in detail. In the fluorescence system of PUFX-Tb3+-SDBS, SDBS acted not only as the surfactant but also as the energy donor. [ABSTRACT FROM AUTHOR]