更新于：2024-12-06
(S)-Ornidazole Disodium Phosphate
磷酸左奥硝唑酯二钠
更新于：2024-12-06
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2021-05-26), |
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C7H13ClN3NaO7P |
InChIKeySAJKYPFJKUEHSG-QYCVXMPOSA-N |
CAS号1030019-20-5 |
关联
11
项与 磷酸左奥硝唑酯二钠 相关的临床试验注射用[14C]磷酸左奥硝唑酯二钠在中国健康成年男性受试者体内的物质平衡研究
一项评价注射用磷酸左奥硝唑酯二钠在腹腔感染手术患者中的药代动力学试验
一项评价注射用磷酸左奥硝唑酯二钠在不同程度肾功能不全受试者中的药代动力学和安全性的开放、平行、单次给药的临床试验
100 项与 磷酸左奥硝唑酯二钠 相关的临床结果
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100 项与 磷酸左奥硝唑酯二钠 相关的转化医学
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100 项与 磷酸左奥硝唑酯二钠 相关的专利（医药）
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3
项与 磷酸左奥硝唑酯二钠 相关的文献（医药）2015-12-01Chemico-biological interactions2区 · 医学
Effects of the ornidazole enantiomers on the central nervous system: Involvement of the GABAA receptor
2区 · 医学
Article
作者: Chen, Ke ; Ji, Hui ; Sun, Ji-Hong ; Wei, Ting-Ting ; Wang, Zhi-Qiang ; Han, Lu-Wei
This is the preliminary study of the sedative and muscle relaxation activity of ornidazole enantiomers, which are widely used in the treatment of susceptible protozoal infections and anaerobic bacterial infections. Adverse effects on the central nervous system (CNS) are the main side effects of ornidazole during its clinical application. The aim of this study was to compare the different central inhibitory effects between S-(-) ornidazole and R-(+) ornidazole in mice and clarify the possible mechanisms. In the present study, central effects of ornidazole were evaluated by open-field test and rota-rod test, and such effects were reversed by pre-treatment with flumazenil (i.p., 10 mg/kg) suggesting that ornidazole exhibits such action by interacting with the GABAergic system. Then, the functional difference between S-(-) ornidazole and R-(+) ornidazole was further explored by evaluating the contents of glutamate (Glu) and γ-aminobutyric acid (GABA) in the brain, and Western blot was used to measure glutamic acid decarboxylase (GAD65/67) expression in the mice cerebral cortex. We found that R-(+) ornidazole mediated an increase in GABA level while decreased the level of glutamate through upregulation of GAD65/67 in the cerebral cortex. Taken together, our study suggests that R-(+) ornidazole mediate stronger central inhibitory effects than S-(-) ornidazole through interaction with the GABAergic system.
2014-08-01Journal of chromatography. B, Analytical technologies in the biomedical and life sciences3区 · 医学
Enantioselective HPLC determination and pharmacokinetic study of secnidazole enantiomers in rats
3区 · 医学
Article
作者: Liu, Dongqin ; Du, Jiangbo ; Zhang, Yifan ; Chen, Yao ; Zhong, Dafang ; Chen, Xiaoyan
Secnidazole is a long-lasting nitroimidazole antimicrobial agent that is used as racemic mixture in clinical settings. We developed and validated an enantioselective high-performance liquid chromatography method to determine secnidazole enantiomers in rat plasma. Secnidazole enantiomers and S-(-)-ornidazole (internal standard) were extracted from 50 μL of rat plasma using diethyl ether-dichloromethane (3:2, v/v). Baseline resolution (Rs=2.45) was achieved within 7.0 min on a Chiral-AGP column (150 mm × 4.0mm, 5 μm) at 20°C. The mobile phase consisted of 10mM ammonium acetate-methanol (96:4, v/v) and was delivered at a flow rate of 0.5 mL/min with ultraviolet detection at 318 nm. The method was linear over the concentration range 0.500-100 μg/mL for both enantiomers. The lower limit of quantification was 0.500 μg/mL for both enantiomers. The relative standard deviation values for intra- and inter-day precision were 0.8-8.6 and 1.8-8.2% for S-(+)-secnidazole and R-(-)-secnidazole, respectively. The relative error values of accuracy ranged from -7.8 to 1.1% for S-(+)-secnidazole and from -7.3 to -0.1% for R-(-)-secnidazole. The method was successfully used to determine the pharmacokinetic properties of secnidazole enantiomers in rats after administration of the racemate and individual enantiomers. The pharmacokinetic results indicate that the disposition of secnidazole enantiomers is not stereoselective and chiral inversion and enantiomer-enantiomer interaction do not occur in rats.
2013-12-01Journal of pharmaceutical and biomedical analysis3区 · 医学
Enantioselective determination of ornidazole in human plasma by liquid chromatography–tandem mass spectrometry on a Chiral-AGP column
3区 · 医学
Article
作者: Yifan Zhang ; Dafang Zhong ; Xiaoyan Chen ; Zhiyu Ma ; Jiangbo Du ; Ting Wang
A rapid, sensitive, and enantioselective method was developed and validated for determination of ornidazole enantiomers in human plasma by liquid chromatography-tandem mass spectrometry. Ornidazole enantiomers were extracted from 100μl of plasma using ethyl acetate. Baseline chiral separation (Rs=2.0) was obtained within 7.5min on a Chiral-AGP column (150mm×4.0mm, 5μm) using an isocratic mobile phase of 10mM ammonium acetate/acetic acid (100/0.01, v/v). Stable isotopically labeled R-(+)-d5-ornidazole and S-(-)-d5-ornidazole were synthesized as internal standards. Acquisition of mass spectrometric data was performed in multiple reaction monitoring mode via positive electrospray ionization, using the transitions of m/z 220→128 for ornidazole enantiomers, and m/z 225→128 for d5-ornidazole enantiomers. The method was linear in the concentration range of 0.030-10.0μg/ml for each enantiomer. The lower limit of quantification for each enantiomer was 0.030μg/ml. The relative standard deviation values of intra- and inter-day precision were 1.8-6.2% and 1.5-10.2% for R-(+)-ornidazole and S-(-)-ornidazole, respectively. The relative error values of accuracy ranged from -4.5% to 1.2% for R-(+)-ornidazole and from -5.4% to -0.8% for S-(-)-ornidazole. The validated method was successfully applied to a stereoselective pharmacokinetic study of ornidazole after oral administration of 1000mg racemic ornidazole.
100 项与 磷酸左奥硝唑酯二钠 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 |
|---|---|---|---|
| 细菌感染 | 中国 | 2021-05-26 |
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 |
|---|---|---|---|---|
| 牙龈炎 | 申请上市 | 中国 | 2019-08-15 | |
| 腹腔感染 | 申请上市 | 中国 | 2019-08-15 | |
| 脓毒症 | 申请上市 | 中国 | 2019-08-15 | |
| 子宫内膜炎 | 临床3期 | 中国 | 2023-02-07 | |
| 盆腔腹膜炎 | 临床3期 | 中国 | 2023-02-07 | |
| 输卵管炎 | 临床3期 | 中国 | 2023-02-07 | |
| 输卵管-卵巢脓肿 | 临床3期 | 中国 | 2023-02-07 | |
| 厌氧菌感染 | 临床2期 | 中国 | 2018-05-15 | |
| 厌氧菌感染 | 临床2期 | 中国 | 2018-05-15 | |
| 妇科感染 | 临床1期 | 中国 | 2014-06-11 |
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