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Pazufloxacin eardrops are a topical quinolone agent for the treatment of outer ear infection. The present study evaluated the pharmacokinetics and topical distribution of pazufloxacin eardrops by a sensitive LC-MS/MS method for determining pazufloxacin in plasma and otorrhea. Plasma and otorrhea samples were extracted by acetonitrile-induced protein precipitation and were subjected to liquid chromatography-tandem mass spectrometric analysis with an electrospray ionization interface. The samples were separated on an HSS T3 column (50 mm×2.1 mm, 1.8 μm). To avoid the matrix effect, gradient elution was performed with the mobile phase consisting of methanol and 1 mmol·L-1 ammonium acetate aqueous solution (0.1% formic acid). The ion transitions for pazufloxacin and pazufloxacin-d4 were m/z 319.1→281.2 and m/z 323.1→285.2, respectively, under the multiple reaction monitoring (MRM) mode. The method was linear in the range of 0.010 0 - 8.00 ng·mL-1 for pazufloxacin in plasma and 0.500 - 1 000 ng·mg-1 in otorrhea. The intra- and inter-day accuracy and precision for pazufloxacin in plasma and in otorrhea met acceptable criteria. The clinical trial was approved by the Society of Ethics and conducted in Nanjing First Hospital and Jiangsu Province Hospital. The validated methods were used in a systemic and topical pharmacokinetic study of 0.1% pazufloxacin eardrops in 3 patients with chronic suppurative otitis media.
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Objective To compare the clinical efficacy and safety following the topical application of pazufloxacin mesylate eye drops with levofloxacin eye drops (LOFX) for bacterial conjunctivitis.Methods A multicenter,randomized,investigator-masked,parallel-controlled clinical trial was performed.Five hundred and twenty eyes of 520 patients with bacterial conjunctivitis were enrolled from March to October 2008 in seven ophthalmic centers in China.The patients were randomized into trial group and control group in 3 ∶ 1 ratio with the 390 eyes in the trial group and 130 eyes in the control group.Pazufloxacin mesylate eye drops was topically used 4 times per day for consecutively 7-14 days in the trial group,and levofloxacin eye drops was used in the same way in the control group.Microbiological cultures for conjunctiva sac secretions and drug sensitive test were carried out before and at the end of the administration of eye drops.The signs and symptoms were observed and scored before treatment and 0,3,7 and 14days after treatment.The adverse events following the administration of the eye drops were evaluated and compared.Results The intention to treat analysis (ITT) showed that the cure rate was 59.38％ in the trial group and 60.47％ in the control group,with the effective rate 88.80％ and 86.05％,respectively,with an insignificant difference between the two groups (x2 =0.12,P =0.72).The clinically evaluable analysis (CE) exhibited that the cure rates were 63.48％ in the trial group and 63.87％ in the control group,with the effective rate 92.46％ and 88.24％,whichwas not significantly different between them (x2 =0.54,P=0.46).The modified-ITT analysis (mITT) showed that the cure rates were 60.57％ in the trial group and 62.07％ in the control group,with the effective rate 90.32％ and 88.51％,without significant difference between the two groups (P＞0.05).Based on microbiologically evaluable analysis (ME),the clinical cure rates were 63.71％ and 63.41％ in the trial group and control group,and the effective rates were 93.44％ and 90.24％,respectively.There was no significantly difference between the both groups (P＞0.05).In the trial group and control group,the bacterial eradication rate was 89.42％ and 90.80％ based on ITT,90.11％ and 92.77％ based on CE,respectively.There was no significant difference in incidences of adverse events following the administration of the drug between the trial group and control group,including ocular tolerance,burning sensation,pricking and itching (P =0.34).Conclusions The effectiveness and adverse response were resemble between Pazufloxacin mesylate eye drops and LOFV following the topical application for bacterial conjunctivitis,which indicate that Pazufloxacin mesylate eye drops is effective and safe.
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OBJECTIVE: To study the stability of Pazufloxacin Mesylate for Injection in two kinds of infusions.METHODS: The change of Pazufloxacin Mesylate for Injection in the appearance and the pH value within 12 h after mixing with fructose injection or 5% glucose and sodium chloride injection were investigated and the content of Pazufloxacin Mesylate was determined by HPLC.RESULTS: There was little change for the mixture in appearance,pH value and the content of Pazufloxacin Mesylate within 12 h.CONCLUSION: Pazufloxacin Mesylate for injection is stable within 12 h after mixing with Fructose injection or 5% Glucose and sodium chloride injection.
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OBJECTIVE:To study compatible stability of pazufloxacin mesilate for injection with three kinds of hemostatics in sodium chloride injection.METHODS:The changes of the mixtures in appearance,pH values,insoluble particles and the content of pazufloxacin mesilate within 8 hours after mixing of pazufloxacin injection with etamsylate,Vitamin K1 or aminomethylbenzoic at 25 ℃ under natural illumination in a simulated clinical common concentration were followed.RESULTS:There were no significant change in the appearance,pH value and the content of pazufloxacin mesilate within 8 hours after mixing of pazufloxacin mesilate for injection with aminomethylbenzoic injection or etamsylate injection;when mixed with Vitamin K1,there were no significant change in the appearance,pH and the content of pazufloxacin mesilate within 2 hours,but the insoluble particles was found to be unqualified after 1 hour of mixing,and white precipitate appeared after 4 hours and the content of pazufloxacin mesilate decreased to some degree.CONCLUSION:The mixture of pazufloxacin mesilate for injection and etamsylate or aminomethylbenzoic was stable within 8 hours at room temperature.The mixing of pazufloxacin mesilate for injection with Vitamin K1 should be conducted with caution.
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OBJECTIVE:To prepare pazufloxacin mesilate ophthalmic gel and to establish its quality control method.METHODS:The gel was prepared with pazufloxacin mesilate ophthalmic as principal agent and with PVA-124 as base material.The content of pazufloxacin mesilate was determined by HPLC and the stability of the gel was investigated as well.RESULTS:The prepared gel was yellowish liquid and its property fitted the description of Chinese Pharmacopeia(2005 edition).The linear range of pazufloxacin mesilate was 20.0～80.0 ?g?mL-1(r=0.999 9),and the average recovery was 98.67%(RSD=0.79%,n=3).No stratification was noted for the sample within 2-month storage under room temperature.CONCLUSION:The preparation technique of the pazufloxacin mesilate ophthalmic gel is simple and feasible,its quality control method is rapid and the determination result is accurate and reliable.
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0.05);the bacterial clearance rates of the 2 group were 100%.No adverse effects were found in both groups.CONCLUSION:Pazufloxacin injection was effective and safe in the treatment of bacterial infections of respiratory system or urinary system
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OBJECTIVE To study the antibacterial activity of pazufloxacin in vitro against bacteria isolated from(patients) with respiratory and urinary tract infection,compared with levofloxacin,ciprofloxacin,cefuroxime and(cefotaxime) to provide guideline for clinical application.METHODS The infected bacteria were identified by the(fully) automatic VITEK system.The susceptibility test was determined by MIC method and K-B disk diffusion method respectively.RESULTS The sensitivity of most Gram-negative bacteria to pazufloxacin was basically the same to levofloxacin,cefotaxime, etc.However,the sensitivity of Pseudomonas and Acinetobacter to(pazufloxacin) was higher than to other four antibiotics;the sensitivity of Gram-positive cocci,particularly(Streptococcus) to(pazufloxacin) was obviously lower than cephalosporins and no better than other quinolones.(CONCLUSIONS) The antibacterial activity of pazufloxacin in vitro against the bacteria isolated from patients with(respiratory) and urinary tract infection is comparatively strong,especially in the urinary system.Pazufloxacin has an excellent broad-(spectrum) and strong antibacterial activity.However,the antibacterial activity against Gram-positive cocci is(expected) to promote.
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OBJECTIVE: To valuate the antibiotic effects in vitro of Pazufloxacin combined with Cefoperazone/Sulbactam against 90 common pathogenic bacteria from hospital acquired infection. METHODS: The protocol was designed by checkerboard method. The MIC of two antibiotics alone or in combination against 90 strains (including 30 staphylococcus aureus, 30 Escherichia colis, 30 Pseudomonas aeruginosas) were detected by broth dilution method and the FIC index was calculated according to MIC values. RESULTS: The MIC of Pazufloxacin combined with cefoperazone/sulbactam against 90 strains was reduced significantly. The percentage of the FIC index maintained at less than 0.5, 0.5～1, 1～2, above 2 were 60.7%～80.0%, 20.0%～33.3%, 3.3%～6.6%, and 0% respectively. CONCLUSION: The antibiotic activity of Pazufloxacin combined with cefoperazone/sulbactam against 90 common iatrogenic strains from hospital acquired infection was enhanced significantly. Their antibacterial action in vitro was characterized by synergism and additive action instead of antagonistic effect.
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OBJECTIVE:To establish a RP-HPLC analytical method for the determination of pazufloxacin mesilate in human plasma and urine.METHODS:The plasma proteins were precipitated with methanol and the supernatant liquid ob-tained from the serum centrifugate was subjected to chromatographic analysis.The supernatant liquid obtained from the diluted urine centrifugate was subjected to sample introduction.The analytical column was Diamonsil C 18 ,the mobile phase consisted of acetonitrile-0.05mol/L potassium dihydrogen phosphate(containing1%tetrabutylammonium bromide)(8∶92,V/V)with a flow rate at1.4ml/min,excitation wavelength at320nm and emission wavelength at400nm.RESULTS:The linear range of pazufloxacin mesilate in both plasma and urine was31.25～10000ng/ml(r=0.9999).The relative recoveries of pazu-floxacin mesilate in human plasma and urine were97.77%～99.87%and98.31%～100.82%,respectively with RSD less than1.0%～3.0%.CONCLUSION:This method is accurate,reliable and simple and it is suitable for the pharmacokinetic study and routine monitoring of blood concentration of pazufloxacin mesilate.