• YAKHAK HOEJI
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• v.38 no.6
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• pp.763-769
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• 1994

Bifidobacterium bifidum, one strain of medical preparation being on the market for human intestinal disorders, was sensitive to rifampicin and fluoroquinolones. If this preparation is taken with rifampicin and fluoroquinolones, its therapeutic effect can't be expected. Serial passage of B. bifidum RFR61, which was obtained by MNNG mutation method, on agar with 2-fold minimal inhibitory concentration of ofloxacin produced B. bifidum OFR9 with minimal inhibitory contentrations of fluoroquinolones up to $4{\sim}256-fold$ higher than that for the original strain. B. bifidum OFR9 produced almost the same amount of organic acid as parental strain. This strain showed growth inhibitory activity against E. coli NM522, Shigella dysenteriae ATCC9752 and E. coli 078. No inactivations of rifampicin and ofloxacin by this resistant mutant strain were found.

• Journal of the Korean Chemical Society
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• v.57 no.5
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• pp.574-590
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• 2013

A new solid complexes of Ti(IV), Y(III) and Ce(IV) have been synthesized with ofloxacin. The formulae and structure of the complexes have been proposed in the light of analytical, spectral ($^1H$ NMR, IR and UV-Visible), magnetic, molar conductivities and thermal studies. The complexes are soluble in DMSO-$d_6$ and DMF. The measured molar conductance values indicate that, the three complexes are electrolyte in nature. The results support the formation of the complexes and indicated that ofloxacin reacts as a bidentate ligand chelate to the metal ion through the pyridone oxygen and one carboxylato oxygen. The kinetic parameters of thermogravimetric and its differential have been evaluated by using Coats Redfern (CR) and Horowitz-Metzeger (HM) methods. The thermodynamic data reflect the thermal stability for all complexes. The metal- ligand binding of the Ti(IV), Y(III) and Ce(IV) complexes is predicted using density funcational theory at the B3LYP-CEP-31G level of theory and total energy, dipole moment estimation of different Ti(IV), Y(III) and Ce(IV) ofloxacin structures. The biological activities of the ofloxacin, inorganic salts and their metal complexes were assayed against different bacterial species.

• Korean journal of dermatology
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• v.56 no.10
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• pp.624-627
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• 2018

Allergic contact dermatitis is an inflammatory condition associated with periorbital erythema, edema, and pruritus. The periorbital skin is relatively thin compared with the skin over other facial areas; therefore, it is vulnerable to allergen penetration and may show a variety of cutaneous manifestations. Recently, vision enhancement surgery is a widely performed procedure, and the prevalence of senile cataract and glaucoma is increasing. The prevalence of periocular allergic contact dermatitis is increasing secondary to the growing use of topical ophthalmic medications. Several studies in Korea have reported periocular allergic contact dermatitis secondary to the use of topical ophthalmic medications including latanoprost ($Latano^{(R)}$), fluorometholone ($Tolon^{(R)}$), polymyxin B ($Terramycin^{(R)}$), atropine sulfate ($Atropine^{(R)}$), neomycin sulfate ($Cambison^{(R)}$), and befunolol hydrochloride ($Bentos^{(R)}$), among others. However, ofloxacin ($Effexin^{(R)})$-induced allergic contact dermatitis has not been reported in the domestic and/or foreign literature. We report a case of periocular allergic contact dermatitis secondary to the use of ofloxacin ophthalmic ointment.

• 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.

• Genomics & Informatics
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• v.16 no.3
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• pp.44-51
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• 2018

Fluoroquinolone (FQ) antibiotics are an important class of synthetic antibacterial agents. These are the most extensively used drugs for treating bacterial infections in the field of both human and veterinary medicine. Herein, the antibacterial and pharmacological properties of four fluoroquinolones: lomefloxacin, norfloxacin, ciprofloxacin, and ofloxacin have been studied. The objective of this study was to analyze the antibacterial characteristics of the different fluoroquinolones. Also, the pharmacological properties of the compounds including the Lipinski rule of five, absorption, distribution, metabolism, and excretion, LD50, drug likeliness, and toxicity were evaluated. We found that among all four FQ molecules, ofloxacin showed the highest antibacterial activity through in silico assays with a strong interaction (-38.52 kJ/mol) with the antibacterial target protein (topoisomerase-II DNA gyrase enzyme). The pharmacological and pharmacokinetic analysis also showed that the compounds ciprofloxacin, ofloxacin, lomefloxacin and norfloxacin have good pharmacological properties. Notably, ofloxacin was found to possess an IGC50 (concentration needed to inhibit 50% growth) value of $0.286{\mu}g/L$ against the Tetrahymena pyriformis protozoa. It also tested negative for the Ames toxicity test, showing its non-carcinogenic character.

• Journal of Pharmaceutical Investigation
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• v.35 no.1
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• pp.45-50
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• 2005

The purpose of the present study was designed to evaluate the bioequivalence of two ofloxacin tablets, Tarivid (Jeil Pharm. Co., Ltd.) and Favid (ILHWA Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four normal male volunteers, $23.67{\pm}3.12$ year in age and $68.50{\pm}7.23$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After four tablets containing 100 mg of ofloxacin were orally administered, blood was taken at predetermined time intervals and concentrations of ofloxacin in plasma were determined using HPLC. Pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$ and $C_{max}$ and untransformed $T_{max}$. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals for the log transformed data were acceptance range of log 0.8 to log 1.25 (e.g., $log0.94{\sim}log1.04\;and\;log0.90{\sim}log1.07\;for\;AUC_t\;and\;C_{max}$, respectively). The major parameters, $AUC_t$, and $C_{max}$, met the criteria of KDFA for bioequivalence indicating that Favid tablet is bioequivalent to Tarivid tablet.

• YAKHAK HOEJI
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• v.43 no.1
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• pp.124-127
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• 1999

Bifidobacterium infantis K-525 isolated from healthy Korean was susceptible to rifampicin and fluoroquinolones and resistant to other antituberculosis agents. When the preparation of this strain is taken as a therapeutics for human intestinal disorders with rifampicin or fluoroquinolones, its therapeutic effect can not be expected. So, B, infantis RFR-525 resistant to rifampicin was obtained by treating the parent B. infantis 525 with N-methyl-N'-nitro-N-nitrosoguanidine. B. infantis OFR-525 was produced by serial passage of B. infantis RFR-525 on agar with 2-fold minimal inhibitory concentration of ofloxacin. B. infantis OFR-525 was resistant to antituberculosis agents and fluoroquinolones up to 4∼128 fold higher than that for the original strain. The resistance of B. infantis OFR-525 against rifampicin and ofloxacin was maintained in vivo and in vitro. Conclusively, B. infantis OFR-525 can be regarded as a promising strain which can be developed as the preparation for the treatment of the intestinal disorders of the tuberculosis patients under rifampicin and ofloxacin therapy.

• Applied Microscopy
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• v.36 no.2
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• pp.93-99
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• 2006

Gemifloxacin is a synthetic fluoroquinolone antimicrobial agent that exhibits potent activity against most Gram-negative and Gram-positive organisms, and has a comparatively low chondrotoxic potential in immature animals. This study examined the effects of gemifloxacin on the Achilles tendons in immature Sprague-Dawley rats treated by oral intubation once daily for 5 consecutive days from postnatal week 4 onward at doses of 0 (vehicle), and 600mg/kg body weight Ofloxacin was used for comparison. The Achilles tendon sperimens were examined by electron microscopy. In comparison with the vehicle-treated controls, there were ultrastructural changes in all samples from the gemifloxacin- and ofloxacin-treated rats. Degenerative changes were observed in the tenocytes, and the cells that detached from the extracellular matrix were recognizable. The degree of degenerative changes and the number of degenerated cells in the Achilles tendon were significantly higher in the treated group than in the control group. Moreover, among the quinolone treated groups, these findings were more significant in the ofloxacin treated group, and less significant in the gemifloxacin treated group. It is unclear what these findings mean with respect to the possible risk ill juvenile patients treated with gemifloxacin or other quinolones. However, these results show that gemifloxacin causes fewer changes in the connective tissue structures.

• Bulletin of the Korean Chemical Society
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• v.29 no.11
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• pp.2103-2108
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• 2008

• YAKHAK HOEJI
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• v.41 no.4
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• pp.450-455
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• 1997

The preparation of Bacillus coagulans is used as a therapeutics for human intestinal disorders. However, the bacterium in the preparation is very susceptible to rifampic in and fluoroquinolones. When the preparation is taken with rifampicin or fluoroquinolones, its therapeutic effect can not be expected. So B. coagulans RFR17 resistant to rifampicin was obtained by treating the parent B. coagulans with N-methyl-N'-nitro-N-nitrosoguanidine. B. coagulans OFR17 was produced by serial passage of B. coagulans RFR17 on agar with 2-fold minimal inhibitory concentration of ofloxacin or ciprofloxacin. B. coagulans OFR17 was resistant to fluoroquinolones up to 16~64 fold higher than that for the original strain. B. coagulans OFR17 also exhibited identical characteristics with the parent strain when they were tested for lactic acid production and growth inhibition of E. coli MB4-01 and Shigella sonnei MB4-10411. From in vitro test, it was also identified that rifampicin and ofloxacin are not inactivated by certain factors of B. coagulans OFR17. Conclusively, B. coagulans OFR17 can be regarded as a promising strain which can be developed as the preparation for the treatment of the intestinal disorders of the tuberculosis patients under rifampicin and ofloxacin therapy.