Development Of Uv-Spectrophotometric Method And Its Validation For Estimating Contents Of Prulifloxacin In Simulated Intestinal Fluid

This study was performed with an objective of developing and validating an UV-spectroscopic method for estimating contents of prulifloxacin in simulated intestinal fluid (SIF) i.e. phosphate- buffer media with a pH of 6.8 as per ICH guidelines. The λmax for prulifloxacin in phosphate- buffer media pH 6.8 was found to be 272 nanometer. The calibration curve of drug followed linearity in-between 1-9 μg/ml concentration range and correlation co-efficient value was found equal to 0.9995. We tested this proposed method onto the bulk and marketed pharmaceutical formulation (tablets) also in order to find out contents of drug. Using developed method for estimation of prulifloxacin in SIF, drug was found to be in-between 101.91 and 104.02 % in marketed tablets which shows a good agreement with that of the claimed level. Accuracy of developed method was established through recovery experimentation, performed for three spiked percent concentrations- 75%, 100%, and 125%. The % recovery was found to be in between 97.27 and 101.82%. Low values of % RSD supported accuracy as well as the reproducibility of developed method. Precision of developed method was established by good in-limit intraday and interday experimental variations and through repeatability tests. Values of % RSD less than 2 confirmed about precision of developed method. The ruggedness of the developed method was validated by performing drug estimation by two different performers. This proposed spectroscopic method has proved to be a rapid and successful method for routine analysis of prulifloxacin in simulated intestinal fluid.

Rapid europium-sensitized fluorescent determination of ulifloxacin,the active metabolite of prulifloxacin,in human serum and urine / 药物分析学报

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 enhanced 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

Rapid europium-sensitized fluorescent determination of ulifloxacin, the active metabolite of prulifloxacin, in human serum and urine / 药物分析学报

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 enhanced 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.

Determination of prulifloxacin active metabolite in human plasma and urine by RP-HPLC / 中国感染与化疗杂志

Objective To establish a RP-HPLC method for determining the concentration of prulifloxacin active metabolite in human plasma and urine.Methods The supernatant obtained by centrifugation after the sample was precipitated with methanol- acetonitrile (1:1) was chromatographically separated on a Diamonsil C_(18)(250 mm?4.6 mm,5?m) using a mobile phase con- sisting of acetonitrile and 0.05 mol/L potassium dihydrogen phosphate (pH2.2) containing 1% tetrabutylammonium bromide. The solutions of 20:80 (V/V) and 12:88 (V/V) at a flow rate of 1.0 mL/min and 1.6 mL/min were used for plasma and u- rine, respectively.Then the samples were assayed at wavelength of Ex 280 nm and Em 425 nm.Results The linear range for prulifloxacin active metabolite in plasma and urine were 0.005-5 mg/L (r=0.9999) and 0.05-5 mg/L(r=0.9999)with a low- er limit of quantitation of 0.002 mg/L and 0.01 rag/L, respectively.In plasma, the relative recovery ranged from 100.64% to 101.00% at the concentration of 5.00, 0.50 and 0.05 mg/L and within-day and between-day precisions were less than 2.5% and 4.6% respectively.Meanwhile, the relative recovery ranged from 97.20% to 100.20% at the concentration of 2.50, 0.50 and 0.10 mg/L in urine.The within-day and between-day precisions were lower than 1.3% and 4.3%, respectively.The method had been successfully used for the pharmacokinetic studies of a prulifloxacin formulation after oral administration to healthy volunteers.Conclusions The present method is simple, rapid, accurate, reproducible and suitable for the pharmacoki- netic study of prulifloxacin in humans.

Improvement in the Production Technology of Prulifloxacin / 中国药房

OBJECTIVE:To improve the production technology of prulifloxacin.METHODS:The primary synthetic process of prulifloxacin was improved from aspects of raw material,agents,reaction method,reaction condition etc by referring to literature together with our experience in and considerable experiments on the production of pruliflorxacin.RESULTS & CONCLUSIONS:The improved production technology of prulifloxacin is simple in operation,obtainable in raw material,high in yield and low in cost,it also meets the requirement on environmental protection,and which is thus suitable for the industrial production of prulifloxacin.

Pharmacokinetics of Prulifloxacin Capsules in Healthy Volunteers / 中国药房

OBJECTIVE:To study the pharmacokinetics of prulifloxacin capsules in Chinese healthy volunteers after single and multiple oral administration of prulifloxacin capsules.METHODS:A total of 12 healthy adult subjects were randomly grouped by 3? 3 Latin square,who were assigned to receive oral single dose of 132,264 and 528mg prulifloxacin capsules and multiple doses of 264mg prulifloxacin capsule for 6 days in succession.The blood concentration of NM394-the metabolite of Prulifloxacin was determined by HPLC at different time after oral administration of Prulifloxacin.The simulation and fitting,and computation of parameters were performed using DAS ver1.0 software.RESULTS:All 12 subjects had completed single oral administration test,with no adverse drug reactions appeared during the test.No prulifloxacin but its metabolite-NM394 was identified in the blood sample of subjects.The high,medium and low dosage groups were all fitted two-compartment model.The pharmacokinetics fitted first order kinetics process without gender difference.There was no accumulation and pharmacokinetic parameters change after multiple oral administration of prulifloxacin,suggesting prulifloxacin had no self-enzyme inhibition or induction.CONCLUSION:The established method is sensitive,accurate,reliable and specific,and it can meet the requirement of clinical pharmacokinetic trial.Its parameters are in line with literature reported abroad,with no gender difference among Chinese adults.

Study on in vitro antibacterial activity of prulifloxacin against pathogenic bacteria of respiratory tract and urinary tract infections / 重庆医科大学学报

Object:To study in vitro antibacterial activity of prulifloxacin against pathogenic bacteria of respiratory tract and urinary tract infections.Methods:The minimum inhibitory concentration(MIC) of prulifloxacin and levofloxacin against 221 pathogenic bacteria of respiratory tract and urinary tract infections was determined by agar dilution method.Results:MIC50,MIC90 and the susceptible rate of prulifloxacin were≤0.03~1?g/ml,0.5~4?g/ml and 67%~100%,respectively.Those of levofloxacin were 0.125~2?g/ml,0.5~8?g/ml and 61%~100%,respectively.MIC90 of prulifloxacin was half that of levofloxacin against Escherichia coli,Enterobacter cloacae,Pseudomonas aeruginosa and Moraxella catarrhalis.MIC90 of prulifloxacin was equal to that of levofloxacin against Klebsiella pneumoniae,Proteus spp,Staphlococcus epidermidis,Streptococcus pneumoniae and Enterococus faecalis.MIC90 of prulifloxacin was two times that of levofloxacin against Haemophilus influenzae and Staphylococcus aureus.Conclusion:Prulifloxacin had a broad-spectrum antibacterial activity against pathogenic bacteria of respiratory tract and urinary tract infections.