The Experts below are selected from a list of 966 Experts worldwide ranked by ideXlab platform
Akira Tsuji - One of the best experts on this subject based on the ideXlab platform.
-
application of muscle microdialysis to evaluate the concentrations of the fluoroquinolones Pazufloxacin and ofloxacin in the tissue interstitial fluids of rats
Journal of Pharmacy and Pharmacology, 2011Co-Authors: Harumi Araki, Naoko Ogake, Shinazburo Minami, Yasuo Watanabe, Hirokazu Narita, Ikumi Tamai, Akira TsujiAbstract:Muscle microdialysis has been used to determine the unbound concentrations of the fluoroquinolones, Pazufloxacin and ofloxacin, in tissue interstitial fluids (Cisf, u) of rats under steady state conditions. Cisf, u was estimated from the concentration in dialysate and the in-vitro permeability rate constant by the extrapolation method based on the clearance concept. Paper disks were inserted under the abdominal skin of rats, and the drug concentrations in the fluids penetrating into the disks (Cdisk) were measured and compared with Cisf, u. The Cisf, u of Pazufloxacin and ofloxacin in muscle were close to their unbound concentrations in the venous plasma; these were 75.3% and 77.1%, respectively, of the total concentrations in plasma at the steady state. The Cdisk of Pazufloxacin and ofloxacin were also close to their Cisf, u. These results indicate that the unbound concentrations of the fluoroquinolones in the tissue interstitial fluids were the same as those in the venous plasma. The disk insertion technique seems to be useful for evaluating drug concentrations in tissue interstitial fluid.
-
Possible involvement of P-glycoprotein in renal excretion of Pazufloxacin in rats.
European journal of pharmacology, 2004Co-Authors: Akemi Shimizu, Mika Miyoshi, Masami Sugie, Jun Ueyama, Takuji Yamaguchi, Toshinobu Sasaki, Kenzo Takagi, Mingji Jin, Ken-ichi Miyamoto, Akira TsujiAbstract:The present study aims to investigate whether Pazufloxacin, a new quinolone antimicrobial agent, is a substrate for P-glycoprotein in vitro, and whether it is excreted from kidney by P-glycoprotein and/or multidrug resistance-associated protein (Mrp2) in vivo. The in vitro experiments showed that the intracellular accumulation of Pazufloxacin in adriamycin-resistant human chronic myelogenous leukemia cells (K562/ADR) overexpressing P-glycoprotein was significantly lower than that in human chronic myelogenous leukemia cells (K562/S) not expressing P-glycoprotein. When rats received an intravenous injection of Pazufloxacin in combination with or without cyclosporine, cyclosporine significantly delayed the disappearance of Pazufloxacin from plasma and decreased the systemic clearance and volume of distribution at steady state of Pazufloxacin to 50% and 70% of the corresponding control values, respectively. Renal handling experiments revealed that the renal clearance of Pazufloxacin was 75% of that corresponding to the systemic clearance, suggesting that the main route of Pazufloxacin elimination is the kidney. Cyclosporine significantly increased the steady-state concentration of Pazufloxacin in plasma by decreasing the tubular secretion clearance and glomerular filtration rate. These results suggest the possibility that Pazufloxacin is excreted into the urine via P-glycoprotein. No significant differences in the renal and tubular secretion clearances of Pazufloxacin were observed between normal rats and Eisai hyperbilirubinemic rats (EHBR), which have a hereditary deficiency in Mrp2, indicating the lack of the involvement of Mrp2 in the renal excretion of Pazufloxacin. Sparfloxacin, a P-glycoprotein substrate, also significantly decreased the renal and tubular secretion clearances of Pazufloxacin, suggesting that Pazufloxacin and sparfloxacin share the same transporters, including P-glycoprotein. The present study at least suggests that Pazufloxacin is excreted into the urine via P-glycoprotein and some active drug transporters other than Mrp2.
Ye Wan-ping - One of the best experts on this subject based on the ideXlab platform.
-
Pharmacoeconomical Analysis of Pazufloxacin and Levofloxacin in Treatment of Urinary Tract Infection
Progress in Pharmaceutical Sciences, 2007Co-Authors: Ye Wan-pingAbstract:Objective:To analyze the cost-effectiveness of Pazufloxacin and levofloxacin in treatment of urinary tract infection. Methods: 70 cases with urinary infection were randomly divided into 2 groups,in which they were treated with Pazufloxacin and levofloxacin, respectively. The cost-effectiveness in two groups was analyzed and compared with each other by pharmacoeconomical methods. Results: There was no significant diffe-rence in therapeutic effect between two groups(P0.05),such as effective rates of 94.3% and 88.6%,bacterial clearance rates of 91.4% and 85.7% and undesired event rates of 5.71% and 8.57% in Pazufloxacin group and levofloxacin group.However,there was significant difference in cost-effectiveness ratio between two group,16.96 and 9.30 respectively in Pazufloxacin group and levofloxacin group (P0.05). Conclusion: Levofloxacin has cost-effective advantage over Pazufloxacin in the treatment of urinary tract infection.
Li Yang - One of the best experts on this subject based on the ideXlab platform.
-
Parmacokinetics of Pazufloxacin mesilate sodium chloride injection in Chinese healthy volunteers
The Chinese Journal of Clinical Pharmacology, 2005Co-Authors: Li YangAbstract:Objective To investigate the pharmacokinetics of Pazufloxacin mesilate sodium chloride injection in Chinese healthy volunteers. Methods Eight healthy volunteers were divided into 2 groups randomly by latin me-thod. The serum samples collected from the volunteers after injecting 300, 600 mg Pazufloxacin mesilate sodium chloride injection respectively by turns were determined by the HPLC method. The serum concentration were determined by the accompanity Pazufloxacin-serum concentration standard curve and the pharmacokinetic paraments were calculated by DAS sofeware. Results The following pharmacokinetic parameters were obtained:C max were (7.38± 0.85)and (18.36±2.39)mg·L -1, AUC 0-t were (31.34± 5.67)and (79.20±18.43)mg·h ·L -1, t 1/2β were (1.63±0.31)and (1.71±0.21)h,CL/F were (0.10±0.02)and(0.08± 0.01)L·kg·h -1, V/F were (0.23±0.03)and (0.19±0.05)L·kg -1.Conclusion The results indicated that the injection can be given 600 mg safely.
Jiro Fujita - One of the best experts on this subject based on the ideXlab platform.
-
Fujita J: In vitro activity of Pazufloxacin, tosufloxacin and other quinolones against Legionella species. J Antimicrob Chemother 2005, 56(6):1053-1057. doi:10.1186/1465-9921-11-158 Cite this article as: Morinaga et al.: Legionella pneumophila induce
2015Co-Authors: Futoshi Higa, Morikazu Akamine, Shusaku Haranaga, Masato Tohyama, Takashi Shinzato, Masao Tateyama, Michio Koide, Atsushi Saito, Jiro FujitaAbstract:Objectives: The activities of Pazufloxacin and tosufloxacin against Legionella spp. were evaluated in vitro and compared with those of other quinolones, macrolides and azithromycin. Methods: The conventional MICs were determined by the microbroth dilution method. Intracellular activities of drugs were evaluated by a cfu count. The minimal extracellular concentration inhibiting intracellular growth of bacteria (MIEC) was determined by a colorimetric cytopathic assay. Results: MICs of pazuloxacin and tosufloxacin at which 90 % (MIC90) of isolates are inhibited in 76 different Legionella spp. strains (38 ATCC strains and 38 clinical isolates) were 0.032 and 0.016 mg/L, whereas the MIC90s of levofloxacin, ciprofloxacin, garenoxacin, erythromycin, clarithromycin and azithromycin were 0.032, 0.032, 0.032, 2.0, 0.125 and 2.0 mg/L, respectively. Pazufloxacin and tosufloxacin at 4·MIC inhibited intracellulargrowthofLegionellapneumophilaSG1 (80-045strain), asdidotherquinolones, clarithromycin and azithromycin, whereas erythromycin at 4 · MIC did not. MIECs of Pazufloxacin, tosufloxacin, levo-floxacin, ciprofloxacin and garenoxacin for the strain were 0.063, 0.004, 0.016, 0.032 and 0.008 mg/L respectively, which were superior to those of macrolides and azithromycin. Pazufloxacin showed potent activity against three additional clinical isolates of L. pneumophila SG1, one clinical isolate each of L. pneumophila SG3 and SG5, as well as Legionella micdadei, Legionella dumoffii and Legionella long-beachae SG1. Conclusions: Pazufloxacin and tosufloxacin, as well as other quinolones, were more potent than macro-lides and an azalide. Present data warrant further study on the efficacy of these drugs in the treatment of Legionella infections
-
In vitro activity of Pazufloxacin, tosufloxacin and other quinolones against Legionella species
The Journal of antimicrobial chemotherapy, 2005Co-Authors: Futoshi Higa, Morikazu Akamine, Shusaku Haranaga, Masato Tohyama, Takashi Shinzato, Masao Tateyama, Michio Koide, Atsushi Saito, Jiro FujitaAbstract:Objectives: The activities of Pazufloxacin and tosufloxacin against Legionella spp. were evaluated in vitro and compared with those of other quinolones, macrolides and azithromycin. Methods: The conventional MICs were determined by the microbroth dilution method. Intracellular activities of drugs were evaluated by a cfu count. The minimal extracellular concentration inhibiting intracellular growth of bacteria (MIEC) was determined by a colorimetric cytopathic assay. Results: MICs of pazuloxacin and tosufloxacin at which 90% (MIC 90 ) of isolates are inhibited in 76 different Legionella spp. strains (38 ATCC strains and 38 clinical isolates) were 0.032 and 0.016 mg/L, whereas the MIC 90 s of levofloxacin, ciprofloxacin, garenoxacin, erythromycin, clarithromycin and azithromycin were 0.032, 0.032, 0.032, 2.0, 0.125 and 2.0 mg/L, respectively. Pazufloxacin and tosufloxacin at 4x MIC inhibited intracellular growth of Legionella pneumophila SG1 (80-045 strain), as did other quinolones, clarithromycin and azithromycin, whereas erythromycin at 4x MIC did not. MIECs of Pazufloxacin, tosufloxacin, levofloxacin, ciprofloxacin and garenoxacin for the strain were 0.063, 0.004, 0.016, 0.032 and 0.008 mg/L respectively, which were superior to those of macrolides and azithromycin. Pazufloxacin showed potent activity against three additional clinical isolates of L. pneumophila SG1, one clinical isolate each of L. pneumophila SG3 and SG5, as well as Legionella micdadei, Legionella dumoffii and Legionella long-beachae SG1. Conclusions: Pazufloxacin and tosufloxacin, as well as other quinolones, were more potent than macrolides and an azalide. Present data warrant further study on the efficacy of these drugs in the treatment of Legionella infections.
L I Tianyun - One of the best experts on this subject based on the ideXlab platform.
-
pharmacokinetics of multiple dose Pazufloxacin mesilate sodium chloride injection in chinese healthy volunteers
The Chinese Journal of Clinical Pharmacology, 2007Co-Authors: L I TianyunAbstract:Objective To evaluate the pharmacokinetics of multiple-dose Pazufloxacin mesilate sodium chloride injection in Chinese health volunteers. Methods The serum and urine samples of 12 healthy volunteer were collected after injecting 500mg Pazufloxacin mesilate sodium chloride injection for 7 days and were determined by HPLC method.Results The following pharmacokinetic parameters were calculated by DAS software, C_ max was (13.46±1.87) mg·L -1,C_ av was (2.72±0.36) mg·L -1,AUC_ ss was(32.70±4.28) mg·h·L -1,DF was 490.43%,FI was 98.15%.The 12 hour cumulative urinary excretionrates were 90%. Conclusion There were no body cumulation after injecting 500 mg Pazufloxacin mesilate sodium chloride twice per day for 7 days, the volunteers were safe.