• 약학회지
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• 제38권6호
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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.

• 대한화학회지
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• 제57권5호
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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.

• 대한피부과학회지
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• 제56권10호
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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.

• 생명과학회지
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• 제17권3호통권83호
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• pp.435-443
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• 2007

호흡기질환 환자의 상기도 도말물로 부터 분리 동정된 M. pneumoniae 116균주의 moxifloxacin, levofloxacin, sparfloxacin, ofloxacin, ciprofloxacin, clarithromycin minocycline, erythromycin, josamycin, and tetracycline에 대한 감수성 검사를 실시하였다. 각 항생물질에 대한 저항성 균주의 기준은 $MIC{\pm}1.0$ ${\mu}g/ml$ 로 하였으며, 초기 MIC와 최종 MIC를 구분하여 다제 저항성 균주의 분포를 분석하였다. 초기 MIC의 결과로 분리된 균주의 단일 약제에 대한 저항성은 ciprofloxacin이 79.3%, ofloxacin이 53.5%, clarithromycin이 10.3%, erythromycin이 7.8%이었으며, 2가지 약제에 저항성은 ofloxacin과 ciprofloxacin이 42.2%, ciprofloracin과 clarithromycin이 9.5%이었으며, 3가지 약제에 저항성은 erythromycin, ofloxacin과 ciprofloxacin이 6.9%, ofloxacin, ciprofloxacin과 clarithromycin이 6.0%이었다. 최종 MIC의 결과로 분리균의 단일 약제에 대한 저항성은 tetracycline, ciprofloxacin, ofloxacin이 각각 91.4%, minocycline이 89.7%, erythromycin이 68.1%, josamycin이 52.6%, clarithromycin이 28.5%, sparfloxacin이 11.2%이었으며, 2가지 약제에 저항성인 균의 분포는 $20.7{\sim}91.4%$, 3가지약제에 저항성인 규의 분포는 &28.5{\sim}89.7%$, 4가지 약제에 저항성인 균의 분포는 2.6%, 5가지 약제에 저항성인 균은 $2.6{\sim}21.6%$, 6가지 약제에 저항성인 균은 $0.9{\sim}24.1%$이었으며, 7가지 약제에 저항성인 균은 $0.9{\sim}2.6%$이었으며, 8종류 약제에 저항성인 균도 1.7%있었다. 이상의 결과로 국내에서 분리된 M. pneumoniae 균주는 적게는 1-4 종류의 항생제에, 많게는 5-8 종류의 항생제에 저항성인 균주가 있으므로 마이코플라스마폐렴 환자를 치료할때는 macrolide계나 quinolone계의 항생제 선택에 신중을 기하여야 하며, 가급적이면 항생제 감수성 검사를 실시하여 적절한 항생제를 선택함으로써 저항성균의 출현율을 줄일 수 있고 효율적인 치료도 할 수 있도록 하여야 할 것으로 생각된다.

• Genomics & Informatics
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• 제16권3호
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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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• 제35권1호
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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.

• 약학회지
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• 제43권1호
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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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• 제36권2호
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• pp.93-99
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• 2006

Gemifloxacin은 대부분의 G(-) 세균들과 G(+) 세균들에 대해 강한 활성을 나타내며 미성숙동물에서 비교적 낮은 연골독성 가능성을 가진 합성 fluoroquinolone계 항생제이다. 본 연구는 미성숙 SD계 랫드의 아킬레스건에 gemifloxacin이 미치는 영향을 평가하기 위해 gemifloxacin을 생후 4주 후부터 0(vehicle), 600mg/kg body weight 용량으로 5일 동안 매일 한번씩 경구투여를 하여 ofloxacin과 비교하였다. 아킬레스건의 형태학적 변화를 투과전자현미경을 이용하여 관찰한 결과 부형제만 처치한 대조군과 비교하였을 때, gemifloxacin과 ofloxacin을 처치한 랫드로부터 채취한 샘플에서 초미세구조의 변화가 관찰되었다. quinolone을 처치한 군의 tenocyte에서는 다양한 퇴행성 변화가 관찰되었고, 세포외기질에서 분리된 세포들이 존재하였는데 이는 ofloxacin을 처치한 그룹에서 특히 높았고 gemifloxacin을 처치한 그룹에서는 매우 낮았다. 따라서, gemifloxacin이 아킬레스건과 같은 결합조직 구조물들의 퇴행성 변화를 보다 적게 야기한다는 것을 보여준다.

• Bulletin of the Korean Chemical Society
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• 제29권11호
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• pp.2103-2108
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• 2008

• 약학회지
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• 제41권4호
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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.