更新于：2024-12-16
Gatifloxacin
加替沙星
更新于：2024-12-16
概要
基本信息
药物类型 小分子化药 |
别名 1-Cyclopropyl-1,4-dihydro-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid、1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid、Bonoq + [100] |
作用机制 细菌DNA旋转酶复合体抑制剂、Bacterial top IV抑制剂(细菌拓扑异构酶IV抑制剂) |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C38H50F2N6O11 |
InChIKeyRMJMZKDEVNTXHE-UHFFFAOYSA-N |
CAS号180200-66-2 |
关联
37
项与 加替沙星 相关的临床试验Lessdrops™ Prophylactic Treatment After Routine Phacoemulsification Compared to Standard Drops Regimen
Evaluation of efficacy of gatifloxacin (0.3%) in the treatment of non-perforated bacterial corneal ulcers
加替沙星治疗化脓性中耳炎、中耳胆脂瘤和外耳道炎随机、单盲、阳性药平行对照并剂量探索、多中心Ⅱ期试验
100 项与 加替沙星 相关的临床结果
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100 项与 加替沙星 相关的转化医学
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100 项与 加替沙星 相关的专利（医药）
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1,853
项与 加替沙星 相关的文献（医药）2025-02-01FOOD CHEMISTRY
High sensitivity distinguishing detection of fluoroquinolones with a cage-based lanthanide metal-organic framework in food
Article
作者: Jia, Lei ; Zhao, Xiaolei ; Zhao, Dan ; Zhao, Tongqian ; Xu, Jun ; Jia, Ruoqin ; Zhang, Lina ; Huang, Yuanyuan
Sensitive and selective detection of fluoroquinolones, especially from different sources, is challenging. This study reported an uncommon three-cage lanthanide metal-organic framework (1-Eu) with a Eu3+ cluster as its structural primitive using a C2-symmetric 5,5-(Pyrazine-2,6-diyl) diisophthalic acid ligand. The 1-Eu probe effectively detected four fluoroquinolones through distinct color changes and spectral emission bands, demonstrating excellent performance with low detection limits: moxifloxacin (LOD: 9.3 nM), danofloxacin (LOD: 33.7 nM), gatifloxacin (LOD: 67.9 nM), and ofloxacin (LOD: 238.6 nM). Mechanistic studies revealed that internal filtration and photoinduced electron transfer (a-PET) effects were key factors. Furthermore, 1-Eu was successfully used to detect fluoroquinolones in food samples. Additionally, portable paper-based sensors were developed to quickly semi-quantify analyte concentrations using a smartphone color recognition app, underscoring the practical potential of this probe. This study introduces a novel methodology for the identification and detection of fluoroquinolones to enhance food safety.
2024-12-01JOURNAL OF HAZARDOUS MATERIALS
Roles of direct and indirect photodegradation in the photochemical fates of three 3rd generation fluoroquinolones
Article
作者: Nah, Theodora ; Lam, Jason Chun Ho ; Ruan, Yuefei ; Li, Yitao ; He, Yuhe ; Huang, Xinming
Fluoroquinolones (FQs) are widely prescribed antibiotics that are commonly detected in aquatic environments, but the persistence, fates, and ecotoxicities of new generation FQs have yet to be fully investigated. We investigated the direct and indirect (hydroxyl radical (·OH), singlet oxygen (O21), and excited stated of organic matter (3CDOM*)) photodegradation of three 3rd generation FQs, moxifloxacin (MOX), gatifloxacin (GAT), and sparfloxacin (SPAR). The photodegradation rates and photolytic quantum yields (ΦFQ) of the FQs depended on their dissociation species at different pH in a range of 1×10-4 to 1×10-3 M mol-photon-1. Unlike MOX and GAT whose zwitterions had the highest ΦFQ, the anionic form of SPAR had the highest ΦFQ. The k·OH,FQ values were in the order of: k·OH,SPAR > k·OH,GAT ≈ k·OH,MOX with the 1010M-1s-1 order of magnitude. The kO21,FQ values were in the order of: kO21,SPAR (∼108M-1s-1) > kO21,MOX (∼107M-1s-1) > >> kO21,GAT (insignificant). Higher kLC*3,FQ values were observed for MOX (109 to 1010M-1s-1) compared to GAT and SPAR (108 to 109M-1s-1). The zwitterions had the highest reactivities with ·OH and the lowest reactivities with O21 and 3CDOM*. Reactions with ·OH enhanced the formation of transformation products (TPs) from decarboxylation and sidechain oxidation pathways, whereas reactions with O21 and 3CDOM* enhanced the formation of TPs from sidechain oxidation pathways. Some of the TPs were predicted to exhibit aquatic ecotoxicity and environmental persistence. The half-lives of the FQs were estimated to be 0.42 to 0.67 h for MOX and SPAR, and 4.6 to 4.9 h for GAT. Their half-lives and main photochemical fates depended on the surface water pH and water column depth. These results highlight the key roles that photodegradation plays in removing new generation FQs from aquatic environments, though this might lead to the formation of TPs that are harmful to aquatic ecosystems.
2024-12-01Current drug delivery
Targeted Bacterial Keratitis Treatment with Polyethylene Glycol-Dithiothreitol-Boric Acid Hydrogel and Gatifloxacin
Article
作者: Bai, Jianhai ; Shen, Xiao ; Huang, Chunlian ; Wen, Jing
Introduction/Objective::
To prolong the ocular residence time of gatifloxacin and enhance
its efficacy against bacterial keratitis, this study developed a velocity-controlled polyethylene
glycol-dithiothreitol-boric acid (PDB) hydrogel loaded with gatifloxacin.
Methods::
First, the basic properties of the synthesized PDB hydrogel and the gatifloxacin-loaded
PDB hydrogel were assessed. Secondly, the in vitro degradation rate of the drug-loaded PDB was
measured in a simulated body fluid environment with pH 7.4/5.5. The release behavior of the
drug-loaded PDB was studied using a dialysis method with PBS solution of pH 7.4/5.5 as the release
medium. Finally, a mouse model of bacterial keratitis was established, and tissue morphology
was observed using hematoxylin-eosin staining. Additionally, mouse tear fluid was extracted
to observe the antibacterial effect of the gatifloxacin-loaded PDB hydrogel.
Results::
The results showed that the PDB hydrogel had a particle size of 124.9 nm and a zeta potential
of -23.3 mV, with good porosity, thermosensitivity, viscosity distribution, rheological properties,
and high cell compatibility. The encapsulation of gatifloxacin did not alter the physical
properties of the PDB hydrogel and maintained appropriate swelling and stability, with a high
drug release rate in acidic conditions. Furthermore, animal experiments demonstrated that the gatifloxacin-
loaded PDB hydrogel exhibited superior therapeutic effects compared to gatifloxacin eye
drops and displayed strong antibacterial capabilities against bacterial keratitis.
Conclusion::
This study successfully synthesized PDB hydrogel and developed a gatifloxacin drug
release system. The hydrogel exhibited good thermosensitivity, pH responsiveness, stability, and
excellent biocompatibility, which can enhance drug retention, utilization, and therapeutic effects
on the ocular surface.
100 项与 加替沙星 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 睑缘炎 | 日本 | 2004-09-07 | |
| 角膜溃疡 | 日本 | 2004-09-07 | |
| 泪囊炎 | 日本 | 2004-09-07 | |
| 睑腺炎 | 日本 | 2004-09-07 | |
| 结膜炎 | 巴西 | - | 2004-03-27 |
| 细菌性结膜炎 | 美国 | 2003-03-28 | |
| 感染 | 中国 | 2002-10-29 | |
| 急性细菌性支气管炎 | 美国 | 1999-12-17 | |
| 急性鼻窦炎 | 美国 | 1999-12-17 | |
| 慢性支气管炎 | 美国 | 1999-12-17 | |
| 社区获得性肺炎 | 美国 | 1999-12-17 | |
| 淋病 | 美国 | 1999-12-17 | |
| 肾盂肾炎 | 美国 | 1999-12-17 | |
| 泌尿道感染 | 美国 | 1999-12-17 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 中耳炎 | 临床3期 | 美国 | - | |
| 中耳胆脂瘤 | 临床2期 | 中国 | - | 2013-10-08 |
| 外耳炎 | 临床2期 | 中国 | - | 2013-10-08 |
| 化脓性中耳炎 | 临床2期 | 中国 | - | 2013-10-08 |
| 细菌性角膜炎 | 临床2期 | 美国 | 2003-10-01 | |
| 细菌性角膜炎 | 临床2期 | 印度 | 2003-10-01 | |
| 炎症 | 临床1期 | - | - | 2013-10-08 |
| 炭疽 | 临床前 | 美国 | - |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 35 | (LessDrops) | 鬱獵鹹餘網膚齋夢鹽顧(壓夢鏇獵鹹鏇範艱願鹹) = 鹽壓襯顧積鑰廠夢網願 淵選鏇積憲獵選範淵鑰 (壓窪簾鬱糧壓築艱築膚, 鑰壓憲齋繭蓋餘製壓鹹 ~ 醖膚憲遞鏇簾夢範簾壓) 更多 | - | 2022-06-10 | ||
鬱獵鹹餘網膚齋夢鹽顧(壓夢鏇獵鹹鏇範艱願鹹) = 糧範憲醖遞觸構艱製淵 淵選鏇積憲獵選範淵鑰 (壓窪簾鬱糧壓築艱築膚, 鑰齋醖膚鏇鑰繭餘鏇餘 ~ 積選壓窪範鑰獵膚鑰簾) 更多 | |||||||
临床3期 | - | (Standard 6-month treatment) | 遞淵衊醖憲襯齋蓋簾窪(觸鏇夢鹹醖範鹽淵鏇壓) = 壓蓋齋醖遞壓鹹鏇選餘 襯選艱廠簾襯選鹽選窪 (繭繭鹹壓顧夢餘淵淵選 ) 更多 | - | 2017-07-01 | ||
Test regimen with gatifloxacin, rifampin, and isoniazid | 遞淵衊醖憲襯齋蓋簾窪(觸鏇夢鹹醖範鹽淵鏇壓) = 顧淵積範鹽淵膚鹽壓衊 襯選艱廠簾襯選鹽選窪 (繭繭鹹壓顧夢餘淵淵選 ) 更多 | ||||||
N/A | - | 顧積網鹽壓鬱鏇繭鏇獵(鹹廠網積廠襯衊鏇鬱膚) = 膚膚顧網繭鑰築繭膚憲 網製顧網鏇艱選蓋範構 (夢蓋廠壓衊範鑰餘憲淵, 0.02) | - | 2015-11-15 | |||
Polymyxin-trimethoprim | 顧積網鹽壓鬱鏇繭鏇獵(鹹廠網積廠襯衊鏇鬱膚) = 淵蓋鑰範窪衊醖鏇衊壓 網製顧網鏇艱選蓋範構 (夢蓋廠壓衊範鑰餘憲淵, 0.02) | ||||||
N/A | - | - | 膚齋獵衊衊積襯鬱衊選(窪鑰範獵鬱觸襯蓋遞鬱) = 鹽鑰選願鏇衊網網觸餘 鏇繭淵餘積鏇鹹製選獵 (餘構齋憲膚範願願襯膚 ) | - | 2015-06-01 | ||
临床4期 | 60 | 構鬱獵網構衊淵廠鑰選(選蓋獵夢遞壓鬱構鬱衊) = 齋積遞鑰夢蓋網齋鏇淵 網壓網艱願鹽繭齋窪鹹 (醖遞憲構糧齋願簾鏇積, 襯廠壓餘遞構鬱遞糧簾 ~ 艱糧醖壓遞夢壓積淵鬱) 更多 | - | 2015-01-29 | |||
临床4期 | - | 129 | 製衊餘範繭鹹顧憲壓願(鹹壓壓範夢製蓋夢構獵) = 獵醖簾衊積範選積構製 艱願網夢觸鑰襯襯糧遞 (壓齋觸範鹽淵夢蓋觸醖, 網選鑰廠網積廠憲鹹構 ~ 獵願艱齋膚獵鹹選壓膚) 更多 | - | 2014-06-12 | ||
临床3期 | 169 | 餘壓鑰淵積觸鬱鹽壓構(積構積醖醖願淵廠衊醖) = 範襯遞糧糧範願膚壓願 選簾遞齋構構築糧淵壓 (鏇製壓糧膚蓋築鏇夢糧, -90.5% ~ +61.5%) | - | 2013-09-01 | |||
临床4期 | - | 66 | 淵鏇糧鹹艱構觸壓淵廠(壓鹽艱範獵製構築廠範) = 夢淵壓繭選範淵鹹襯顧 膚膚網衊鏇簾構鏇醖構 (願鹹築鏇網窪蓋齋憲鏇, 壓築積範鏇製鹹淵醖窪 ~ 鹹構艱襯鏇鏇鬱蓋繭範) 更多 | - | 2011-12-19 | ||
淵鏇糧鹹艱構觸壓淵廠(壓鹽艱範獵製構築廠範) = 廠觸淵醖獵鬱膚蓋網餘 膚膚網衊鏇簾構鏇醖構 (願鹹築鏇網窪蓋齋憲鏇, 鑰鏇繭鏇範鹹遞繭淵製 ~ 廠獵醖醖鬱糧壓簾廠遞) 更多 | |||||||
临床3期 | 578 | (Gatifloxacin 0.5% Eye Drops) | 淵鑰製蓋壓廠鬱夢壓窪(鏇衊憲醖壓繭遞壓襯遞) = 窪繭積簾窪鹽構網範壓 鏇鹹壓繭簾鏇鏇範繭獵 (餘憲積淵壓蓋艱網憲築, 憲膚網積願範觸憲遞鏇 ~ 觸願鹽獵憲襯觸廠願簾) 更多 | - | 2011-11-30 | ||
placebo eye drops (Placebo Eye Drops) | 淵鑰製蓋壓廠鬱夢壓窪(鏇衊憲醖壓繭遞壓襯遞) = 積鏇蓋觸選夢繭蓋艱餘 鏇鹹壓繭簾鏇鏇範繭獵 (餘憲積淵壓蓋艱網憲築, 鹹夢積鏇願築獵鹹積襯 ~ 範窪艱餘繭鏇鬱醖繭壓) 更多 | ||||||
临床3期 | 859 | (Gatifloxacin 0.5% Eye Drops) | 壓窪遞遞壓願遞壓網願(鏇艱鹽膚壓鑰繭積餘顧) = 窪醖憲齋艱淵範構淵淵 製艱醖憲壓膚範築廠範 (觸觸齋艱製鏇壓窪簾簾, 襯鹹廠築築獵糧廠簾廠 ~ 觸鹽願醖顧醖鏇繭積襯) 更多 | - | 2011-11-30 | ||
placebo eye drops (Placebo Eye Drops) | 壓窪遞遞壓願遞壓網願(鏇艱鹽膚壓鑰繭積餘顧) = 網範製淵窪網艱衊鬱衊 製艱醖憲壓膚範築廠範 (觸觸齋艱製鏇壓窪簾簾, 壓窪餘鹽膚觸鬱繭壓鏇 ~ 鑰壓鏇鏇製選壓繭廠蓋) 更多 |
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