• Biomolecules & Therapeutics
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• v.4 no.4
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• pp.378-384
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• 1996

In vitro activities of LB20304a were compared with those of grepafloxacin (OPC-17116), Q-35, ciprofloxacin, and sparfloxacin against 380 clinical isolates collected from general hospitals in 1996. LB 20304a was the most active agent against gram-positive strains including staphylococci, streptococci and enterococci. LB20304a was also very active against gram-negative bacteria and its activity was comparable to that of ciprofloxacin but better than those of grepafloxacin, Q-35 and sparfloxacin. The therapeutic effect of LB20304a was superior to those of sparfloxacin and ciprofloxacin against systemic infection by methicillin-resistant Staphylococcus aureus K283 (MRSA) in neutropenic mice. Against urinary tract infection induced by Escherichia coli 851E in mice, LB20304a was more active than sparfloxacin and ciprofloxacin. However, LB 20304a was slightly less active than that of ciprofloxacin against urinary tract infection by Pseudomonas aeruginosa 1912E, but better than that of sparfloxacin.

• Journal of Yeungnam Medical Science
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• v.15 no.2
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• pp.246-253
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• 1998

Sparfloxacin is a new synthetic quinolone antimicrobial developed at the Research Laboratories of Dainippon Pharmaceutical Co, Ltd. To evaluate the efficacy and safety of sparfloxacin in acute pulmonary infection, we administered sparfloxacina(100mg) twice in a day to 30 patients who had signs and symptoms of acute pulmonary infectious diseases regardless of their underlying lung disease for 7 days. The results were as follows: 1) A total 30 patients were enrolled in the trial. Among them, 24 cases(80%) had underlying lung problems such as chronic obstructive pulmonary disease(36.4%), bronchiectasis(36.4%), bronchial asthma(3.3%), or lung cancer(3.3%). 2) In 26 cases(86.6%), we observed effective improvement, and 4 cases(13.4%) show mildly effective improvement of symptoms and signs of respiratory infection. 3) In 23 cases(73.4%), we observed bacteriological eradication in culture or decreased the number of bacteria by Gram stain which found dominantly in previous Gram stain. 4) The significant side effect was not noted. The above results suggested that sparfloxacin was effective as a first line therapy in patients with acute respiratory infection.

• YAKHAK HOEJI
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• v.38 no.3
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• pp.265-273
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• 1994

ln vitro and in vivo antibacterial activities of DWQ-013(1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid), a new fluoroquinolone antibacterial agent, were compared with those of ciprofloxacin, sparfloxacin and ofloxacin against aerobic and anaerobic standard strains and clinical isolates. DWQ-013 had a broad spectrum and potent antibacterial activity against Gram-positive and Gram-negative bacteria. The antibacterial activity of DWQ-013 against Staphylococcus aureus was equal to that of sparfloxacin(SPFX) and superior to those of ciprofloxacin(CPFX). The antibacterial activity against Gram-negative bacteria was slightly lower than those of ciprofloxacin and sparfloxacin. MIC of DWQ-013 against Pseudomonas aeruginosa$(0.781{\sim}1.563\;{\mu}g/ml)$ was usually equal to that of sparfloxacin$(0.781\;{\mu}g/ml)$ and was inferior to that of ciprofloxacin$(0.098\;{\mu}g/ml)$. The number of viable cells was decreased rapidly after addition of DWQ-013 at concentration of $1{\sim}2$ folds of MIC.

• Bulletin of the Korean Chemical Society
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• v.33 no.1
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• pp.105-110
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• 2012

A europium (III)-sensitized, spectrofluorimetric (FL) method is presented for the determination of sparfloxacin (SPAR) using an anionic surfactant, sodium dodecyl benzene sulphonate (SDBS). The method is based on the strong fluorescence (FL) enhancement of SPAR after the addition of $Eu^{3+}$ ions as fluorescence probes. The experimental results indicated that the FL intensity of the SPAR-$Eu^{3+}$ system was enhanced markedly by SDBS. The maximum FL emission signal was obtained at about 615 nm when excited at 372 nm. The experimental conditions that affected the FL intensity of the SPAR-$Eu^{3+}$-SDBS system were optimized systematically. The enhanced FL intensity of the system exhibited a good linear relationship with the SPAR concentration over the range of $1.5{\times}10^{-9}-1.2{\times}10^{-7}mol\;L^{-1}$ with a correlation coefficient (r) of 0.9987. The limit of detection ($3{\delta}$) was $4.15{\times}10^{-10}mol\;L^{-1}$ with a relative standard deviation (RSD) of 1.65%. This method was successfully applied for the determination of SPAR in pharmaceuticals, and human serum and urine samples with higher sensitivity, wide dynamic range and better stability. The possible interaction mechanism of the system is also discussed in detail by ultraviolet absorption spectra and FL spectra.

• Journal of Life Science
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• v.16 no.5
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• pp.799-805
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• 2006

The in vitro activities of quinolones were determined with 36 strains of tetracycline- resistant, 39 strains of erythromycin-resistant, 21 strains of both resistant to tetracycline and erythromycin, and 27 strains of both susceptible to tetracycline and erythromycin of the M. pneumoniae isolates which have been isolated and classified in previous studies. The $MIC_{90}$ of moxifloxacin, levofloxacin, sparfloxacin, ofloxacin, ciprofloxacin, amikacin, and clarithromycin against 36 strains of tetracycline-resistant M. pneumoniae isolates were 0.125, 0.39, 0.125, 1.0, 1.0, 15.6, and $1.56\;{\mu}g/ml$, respectively. The $MIC_{90}$ against 39 strains of eryhtromycin-resistant M. pneumoniae isolates were 0.06, 0.39, 0.125, 1.0, 1.0, 15.6, and $25.0\;{\mu}g/ml$, respectively. The $MIC_{90}$ against 21 strains of both resistant to tetracycline and eryhtromycin of M. pneumoniae isolates were 0.125, 0.39, 0.125, 1.0, 1.0, 3.9, and $1.56\;{\mu}g/ml$, respectively. The $MIC_{90}$ against 27 strains of both susceptible to tetracycline and eryhtromycin of M. pneumoniae isolates were 0.125, 0.39, 0.125, 1.0, 1.0, 7.8, and $0.09\;{\mu}g/ml$, respectively. These result suggest that moxifloxacin, levofloxacin, and sparfloxacin of the quinolones might be promising antimicrobial agents for the treatment of tetracycline- and erythromycin-resistant M. pneumoniae infection. However, selection of ofloxacin, ciprofloxacin, and clarithromycin for the treatment of M. pneumoniae infection should be cautious decision with antimycoplasmal susceptibility test.

• Journal of Life Science
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• v.17 no.3 s.83
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• pp.435-443
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• 2007

Antimicrobial susceptibility test of the 116 strains of Mycoplasma pneumoniae isolates were performed by a broth micro-dilution method against to moxifloxacin, levofloxacin, sparfloxacin, ofloxacin, ciprofloxacin, clarithromycin minocycline, erythromycin, josamycin, and tetracycline. The initial-minimum inhibitory concentration (I-MIC) was evaluated as the lowest concentration of antimicrobial agents that prevented a color change in the medium at that time when the drug-free growth control, about 7 days after incubation, and the final-minimum inhibitory concentration (F-MIC) was defined a color change about 14 days after incubation. The evaluation to the drug-resistant M. pneumoniae isolates were determined the $MIC{\pm}1.0$ ${\mu}g/ml$ of each antimicrobial agent. According to the I-MIC, single drug-resistant M. pneumoniae strains to ciprofloxacin, ofloxacin, clarithromycin and erythromycin were 79.3, 53.5, 10.3, and 7.8%, respectively. Two kinds of drug-resistant M. pneumoniae strains to ofloxacin and ciprofloxacin, or ciprofloxacin and clarithromycin were 42.2 and 9.5%. Three kinds of drug-resistant M. pneumoniae strains to erythromycin, ofloxacin, and ciprofloxacin, or ofloxacin, ciprofloxacin and clarithromycin were 6.9 and 6.0% . According to the F-MIC, single drug-resistant M. pneumoniae strains to tetracycline, ciprofloxacin, ofloxacin, minocycline,erythromycin, josamycin, clarithromycin and sparfloxacin were 91.4, 91.4, 91.4, 89.7, 68.1, 52.6, 28.5, and 11.2%, respectively. The incidence of two kinds of drug-resistant M. pneumoniae strains were from 20.7% to 91.4%, three kinds of drug-resistant M. pneumoniae strains were from 28.5% to 89.7%, four kinds of drug-resistant M. pneumoniae strains were 2.6%, five kinds of drug-resistant M. pneumoniae were from 2.6% to 21.6%, six kinds of drug-resistant M. pneumoniae strains were from 0.9% to 24.1%, seven kinds of drug-resistant M. pneumoniae strains were from 0.9% to 2.6%, and eight kinds of drug-resistant M. pneumoniae strains were 1.7%. These results suggest that sparfloxacin, moxifloxacin and levofloxacin might be promising antimicrobial agents for the treatment of M. pneumoniae infection in Korea. However, most strains of M. pneumoniae isolates were single or multi-resistance pattern to the other tested antimicrobial agents. Therefore, tetracycline, minocycline, erythromycin, clarithromycin, and second-generation quinolones are more carefully used to patients with M. pneumoniae infection in Korea.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.52-59
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• 1996

The in vitro activity of LB20304 was evaluated against clinical isolates and compared with those of Q-35, ciprofloxacin, sparfloxacin, lomefloxacin and ofloxacin. LB20304 demonstrated 16-to 64-fold more potent activity than ciprofloxacin against gram-positive bacteria. LB20304 inhibited 90% of the isolates of methicillin-susceptible Staphylococcus aureus(MSSA) at a concentration of $0.016\mug/ml\; (MIC_{90}). MIC_{90}$ values of LB20304 against methicillin-resistant Staphylococcus aureus (MRSA), methicillin-susceptible Staphylococcus epidermidis (MSSE), methicillin-resistant S. epidermidis (MRSE) and Streptococcus pneumoniae were $2\mug/ml,\; 0.016\mug/ml,\; 0.5\mug/ml \;and\; 0.031\mug/ml,$ respectively. LB20304 was also very active against gram-negative bacteria. Against Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Pseudomonas aeruginosa and Acinetobacter calcoaceticus, $MIC_{90}s of\; LB20304 were\; 0.031\mug/ml,\; 0.25\mug/ml,\; 2\mug/ml,\; 8\mug/ml\; and\; 0.5\mug/ml$, respectively. Its activity was comparable to that of ciprofloxacin but much better than those of Q-35, sparfloxacin, ofloxacin and lomefloxacin. LB20304 also exhibited the most potent acitvity among quinolones tested against laboratory standard strains, ofloxacin-resistant strains, .betha.-lactamase-producing strains and anaerobic strains. The inhibitory effect$ (IC_{50)$ of LB20304 on DNA gyrase from Micrococcus luteus, determined by the supercoiling assay, was 8-fold more potent than that of ciprofloxacin. LB20304 did not induce topoisomerase-associated DNA cleavage even at a concentration of 10 mg/ml, although ciprofloxacin induced DNA cleavage at a concentration of 1 mg/ml.

• Journal of Life Science
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• v.15 no.3 s.70
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• pp.479-485
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• 2005

The 994 throat swabs obtained from 688 adults and 306 children patients with respiratory diseases were examined for Mycoplasma pneumoniae infection by culture method. Antimicrobial susceptibilities of the resulting 123 M. pneumoniae isolates were evaluated by testing minimum inhibitory concentrations (MICs) of erythromycin, minocycline, tetracycline, josamycin, sparfloxacin, ofloxacin, and ciprofloxacin by a broth micro-dilution method. The erythromycin resistant strains of M. pneumoniae was determined above $1.0{\mu}g/ml$ of MIC for erythromycin. The erythromycin resistant strains of M. pneumoniae was confirmed resistant gene mutation of the portions of genes 23S rRNA (domain II and V), and ribosomal protein 14 and L22 by PCR amplified and their nucleotide sequenses were compared to those of the susceptible strain M129. The isolation rate of M. pneumoniae was $12.9\%$ (89/688) for the adults and $11.1\%$ (34/306) for the children. The $MICs_{90}$ of the M. pneumoniae isolates were $0.12{\mu}g/ml$ for minocycline, $0.25{\mu}g/ml$ for sparfloxacin, $0.5{\mu}g/ml$ for ciprofloxacin, ofloxacin, and tetracycline, respectively, and $2.0{\mu}g/ml$ for josamycin and erythromycin, respectively. The isolation rate of erythromycin resistant M. pneumoniae from patients was $49.4\%\;(44/89)$ for the adults, $47.1\%\;(16/34)$ for children, and $48.8\%\;(60/123)$ for the total. No mutation could be detected in the ribosomal protein L22 region, but all strains were mutated in the ribosomal protein L4 as two point mutation M144V. Two point mutations in domain V of 23S rRNA were selected in the presense of erythromycin resistant M. pneumoniae isolates, such as one strain was G2057C mutant, two strains were A2059C mutants, three strains were C2611G mutants, four strains were A2058C mutants, five strains were A2058T mutants, twenty strains were A2059G mutants, and twenty-five strains were A2058G mutants, respectively. These results show that erythromycin was not the most active compound against M. pneumoniae infection in Korea and clinical studies of macrolides in human patients are demanded.

• Journal of fish pathology
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• v.9 no.2
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• pp.185-193
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• 1996

Extensive acquirement of drug resistance to traditional antibacterial agents poses a serious problem to eel aquaculturists. To collect the basic information for new drug development in the future, we assessed the in vitro antibacterial efficacy of 14 new quinolones with 75 isolates of Edwardsiella tarda from local aquaculture tanks of Anguilla japonica. Of all tested quinolones under development or marketed for human use, DU-6859 was most potent with its $MIC_{50}$ value of $0.05{\mu}g$/ml in broth microdilution assay. The drugs whose $MIC_{50}$ values ranged from 0.2 to $0.78{\mu}g$/ml were T-3762, Bay-y3118, ciprofloxacin, norfloxacin, ofloxcin and tosufloxacin. The weakest group of drugs, with their $MIC_{50}$ being 1.56-$3.13{\mu}g$/ml, were difloxacin, sparfloxacin, fleroxacin, Q-35, amifloxacin, lomefloxacin and enoxacin. The number of resistant strains, when arbitrarily defined with their MICs of $\geq6.25{\mu}g$/ml, was : 3 to T-3762, 3 to Bay-y3118, 44 to difloxacin, 16 to sparfloxacin, 13 to ciprofloxacin, 19 to fleroxacin, 36 to Q-35). 31 to amifloxacin, 5 to norfloxacin, 13 to ofloxacin, 31 to lomefloxacin, 41 to enoxacin, 12 to tosufloxacin and 0% to DU-6859, respectively. This information can be taken into consideration for the future development of fisheries antibacterial quinolones.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.57-63
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• 1997

Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.