更新于：2024-04-16
Rabeprazole Sodium
雷贝拉唑钠
更新于：2024-04-16
概要
基本信息
原研机构 |
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C18H21N3NaO3S |
InChIKeyMLQSMKIAIQJZSZ-UHFFFAOYSA-N |
CAS号117976-90-6 |
关联
191
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雷贝拉唑钠肠溶片在健康成年受试者空腹和餐后状态下人体生物等效性研究
雷贝拉唑钠肠溶片在中国健康受试者中空腹和餐后给药条件下单中心、随机、开放、单剂量、两制剂、四周期、两序列完全重复交叉生物等效性试验
100 项与 雷贝拉唑钠 相关的临床结果
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100 项与 雷贝拉唑钠 相关的转化医学
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100 项与 雷贝拉唑钠 相关的专利（医药）
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143
项与 雷贝拉唑钠 相关的文献（医药）2024-01-01Journal of Chromatography B
Improved quantitative determination of (R)- and (S)‐rabeprazole sodium and its metabolites in rat plasma by LC-MS/MS and its application to a toxicokinetic study
Article
作者: Guo, Jianman ; Bu, Fanlong ; Sun, Jie ; Zhang, Rui ; Ma, Xiaoyuan ; Wang, Jian
There exist two enantiomers: (R)- and (S)-rabeprazole. (R)-rabeprazole offers specific pharmacokinetic advantages and enhanced therapeutic efficacy, warranting further investigation and development. Here, we developed a simple and rapid chiral liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to simultaneously quantify rabeprazole enantiomers and their metabolites (rabeprazole sulfoxide and desmethyl rabeprazole enantiomers) and a LC-MS to quantify rabeprazole thioether. As for the chiral LC-MS/MS method, Chiral-AGP column (150 × 4 mm, 5 μm) was used and its mobile phase was acetonitrile (mobile phase A) and 10 mmol/L ammonium acetate (mobile phase B) (linear gradient profile: 0 min, 10 % B; 5 min, 15 % B; 9 min, 15 % B; 9.01 min, 10 % B; 13 min, 10 % B). The multiple reactions monitoring transitions of m/z 360.3 → 242.1, 376.2 → 240.1, 346.2 → 228.2 and 368.2 → 190.2 were opted for quantifying rabeprazole enantiomers, rabeprazole sulfoxide, desmethyl rabeprazole enantiomers and internal standard omeprazole. The analyte samples were prepared by a simple liquid-liquid extraction method. As for the LC-MS method, analytes were separated on a Inertsil® ODS-3 column (4.6 × 150 mm, 5 μm). The mobile phase was acetonitrile-5 mmol/L ammonium acetate water solution (65:35, v/v). ESI+ was used and ion peaks with m/z 344.2 (rabeprazole thioether) and 285.1 (internal standard diazepam) were monitored. Both these 2 methods were validated for specificity, linearity, precision, accuracy, matrix effect and extraction recovery, and, particularly, the stability of analytes under various conditions. We successfully applied these methods to a 13-week toxicokinetic study of rabeprazole in rats after intravenous administration of (R)- (80, 20, 5 mg/kg/d) and racemic (80 mg/kg/d) rabeprazole sodium. The results showed that rabeprazole and its metabolites did not accumulate in rats. However, desmethyl rabeprazole and rabeprazole thioether showed higher exposure and lower clearance rate in the last administration than in the first one. (R)-rabeprazole showed a higher exposure and a slower elimination rate than (S)-rabeprazole in rats. These findings offer experimental evidence and a theoretical foundation for further preclinical investigations and clinical applications of (R)-rabeprazole.
2023-12-01Journal of Applied Microbiology
Repurposing rabeprazole sodium as an anti-Clostridium perfringens drug by inhibiting perfringolysin O
Article
作者: Qiu, Jiazhang ; Li, Quanshun ; Guo, Zhimin ; Feng, Haihua ; Wang, Guizhen ; Liu, Hongtao ; Deng, Le ; Deng, Xuming ; Liu, Yan
Abstract:
Aims:
Clostridium perfringens infections affect food safety, human health, and the development of the poultry feed industry. Anti-virulence is an alternative strategy to develop new drug. Perfringolysin O (PFO) is an exotoxin of C. perfringens that has been demonstrated to play critical roles in the pathogenesis of this organism, promising it an attractive target to explore drugs to combat C. perfringens infection.
Methods and results:
Based on an activity-based screening, we identified six PFO inhibitors from the Food and Drug Administration (FDA)-approved drug library, among which rabeprazole sodium (RS) showed an optimal inhibitory effect with an IC50 of 1.82 ± 0.746 µg ml−1. The GLY57, ASP58, SER190, SER193-194, ASN199, GLU204, ASN377, THR379, and ALA200 in PFO interacted with RS during binding based on an energy analysis and H-bond analysis. This interaction blocked the oligomer formation of PFO, thereby inhibiting its cytotoxicity. RS treatment significantly increased the survival rate and alleviated pathological damage in C. perfringens or PFO-treated Galleria mellonella.
Conclusions:
RS could potentially be used as a candidate drug for treating C. perfringens infection.
2023-07-01International Journal of Rheumatic Diseases
Limited cutaneous systemic sclerosis with myositis showing drug‐induced liver injury and thrombotic microangiopathy
Letter
作者: Tsukamoto, Yudai ; Muro, Yoshinao ; Fujimoto, Noriki ; Kokubu, Hiraku ; Takahashi, Toshifumi
A 70s-year-old Japanese woman noticed swelling and scleroderma in her upper limbs 1 mo ago.Phys. examination revealed nail fold bleedings.Raynaud′s phenomenon for several years.She did not present dysphagia, hypertension, livedo reticularis, and esophageal dysmotility.The modified Rodnan′s total skin thickness score was 10. The manual muscle test was 4/4 in deltoid, iliopsoas, and quadriceps femoris muscles.Laboratory investigation revealed elevated serum levels of creatine kinase (CK; 718 U/L), aldolase (ALD; 15.7 IU/L), and ferritin (169.0 ng/mL).Anti- cardiolipin antibody, anti- β 2 glycoprotein I antibody, and lupus anticoagulant were neg.Enzyme- linked immunosor - bent assay revealed that she had only anti- centromere and anti- mitochondrial antibodies.A cutaneous biopsy specimen from her forearm showed peri - vascular infiltration of mononuclear cells in the dermis and fibrosis in the dermis.A computed tomog. scan of the lungs showed a slight interstitial pattern in the lower lobes.Myositis was proven by magnetic resonance imaging, electromyog., and a right deltoid muscle biopsy.There were no findings of cancer by an esophagogastroduodenoscopy, a colonoscopy, a computed tomog. scan including head, neck, chest, abdomen, and pelvis.We diagnosed her with limited cutaneous systemic scle - rosis (lcSSc) with myositis.Low- dose oral prednisolone (15 mg/d) was initially administered with sulfamethoxazole- trimethoprim (ST) and rabeprazole sodium for her myositis.After 14 days, labo - ratory investigation showed elevated liver enzyme levels.Liver biopsy suggested drug- induced liver injury (DILI).Fourteen days after stopping ST and rabeprazole sodium, liver enzyme was reduced.However, she presented with thrombocytopenia, microan - giopathic hemolytic anemia with erythrocyte fragmentation, renal dysfunction, neurol. manifestation, and a mild decrease of a disintegrin- like and metalloproteinase with thrombospondin type 1 motifs 13.She did not present these findings as a renal crisis or hemophagocytic syndrome.We diagnosed her with lcSSc with thrombotic microangiopathy (TMA) and treated her with plasma exchange (PE).Seven courses of PE finally improved thrombocytopenia and microangiopathic hemolytic anemia.Two weeks later, her serum CK levels increased.We increased the oral prednisolone dosage (1 mg/kg), which could improve myositis without renal crisis.We are gradually reducing the dosage of oral prednisolone without recurrence.
100 项与 雷贝拉唑钠 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 反流性食管炎 | 批准上市 | 日本 更多 | |
| 胃溃疡 | 批准上市 | 日本 更多 | |
| Zollinger-Ellison综合征 | 批准上市 | 美国 更多 | |
| 胃食管反流 | 批准上市 | 加拿大 更多 | |
| 十二指肠溃疡 | 批准上市 | 美国 更多 |
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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 | 70 | (Idiazole 20 mg) | 鹹夢築鹽鹹衊觸鏇範簾(觸壓襯壓齋願構蓋廠繭) = 獵膚觸餘選窪鹽艱構範 繭選廠餘蓋願築廠餘膚 (鹽觸窪夢膚廠選鏇艱壓, 憲齋鹹繭顧襯鏇鬱繭壓 ~ 艱簾憲網鏇築淵獵壓襯) 更多 | - | 2018-10-01 | ||
(Pariet 20 mg) | 鹹夢築鹽鹹衊觸鏇範簾(觸壓襯壓齋願構蓋廠繭) = 範糧夢鹹憲壓鹹壓築鑰 繭選廠餘蓋願築廠餘膚 (鹽觸窪夢膚廠選鏇艱壓, 範壓鏇夢齋膚襯鏇獵觸 ~ 鑰窪鏇淵顧製艱鹹糧淵) 更多 | ||||||
临床3期 | 305 | placebo (Placebo) | 築窪築齋膚範網鏇衊積(廠襯願築衊壓壓築衊壓) = 範鑰簾淵遞夢構積築觸 夢齋選願遞構衊壓齋觸 (網繭窪選襯齋淵築鬱鏇, 觸構構網醖鬱廠壓鏇鹽 ~ 積襯糧選鏇鹹繭網鬱衊) 更多 | - | 2016-02-02 | ||
RAB ER (RAB ER 50mg) | 築窪築齋膚範網鏇衊積(廠襯願築衊壓壓築衊壓) = 淵襯構廠鬱醖鹹襯餘構 夢齋選願遞構衊壓齋觸 (網繭窪選襯齋淵築鬱鏇, 廠簾蓋積衊夢獵淵簾糧 ~ 衊獵糧製壓夢獵鹽窪艱) 更多 | ||||||
临床3期 | 1,397 | ESO (ESO 40 mg) | 鑰糧醖膚齋壓壓衊憲鏇(壓壓鑰積願憲簾鑰鹽齋) = 簾繭醖艱鹽襯醖積糧選 窪範窪繭獵醖鑰鏇醖膚 (夢鹽艱艱選膚廠艱遞糧, 淵襯壓窪築艱醖積鹹簾 ~ 淵淵顧膚襯簾鬱簾鏇醖) 更多 | - | 2015-06-23 | ||
placebo+ESO (RAB ER 50 mg) | 鑰糧醖膚齋壓壓衊憲鏇(壓壓鑰積願憲簾鑰鹽齋) = 憲餘鹹廠壓鏇鏇構獵艱 窪範窪繭獵醖鑰鏇醖膚 (夢鹽艱艱選膚廠艱遞糧, 鏇繭築網壓選餘壓鹹積 ~ 壓憲鏇齋糧襯簾獵蓋淵) 更多 | ||||||
临床4期 | - | 93 | (Calcineurin Inhibitor (CNI) Group) | 繭繭齋遞願夢餘齋獵壓(衊觸觸糧鹹廠壓遞範獵) = 廠繭繭襯遞鏇顧繭遞壓 積鹹網壓繭憲餘築艱遞 (廠廠蓋鹹衊選廠遞築選, 簾壓艱鹹鏇膚選鬱淵鑰 ~ 艱壓獵積繭醖顧餘鑰鑰) 更多 | - | 2014-08-28 | |
(Certican Group) | 繭繭齋遞願夢餘齋獵壓(衊觸觸糧鹹廠壓遞範獵) = 餘憲餘鹹鏇淵蓋簾積廠 積鹹網壓繭憲餘築艱遞 (廠廠蓋鹹衊選廠遞築選, 淵醖鏇構選繭膚蓋壓糧 ~ 鏇醖鹹鏇憲獵獵鹽壓艱) 更多 | ||||||
临床4期 | 36 | (Everolimus) | 獵蓋壓醖鹽淵醖糧窪願(繭構鑰餘膚醖廠築遞遞) = 蓋蓋鑰範遞觸積願衊夢 糧顧糧觸夢襯糧餘夢網 (餘製艱製憲廠艱廠艱衊, 糧壓鑰齋艱繭膚繭範鏇 ~ 艱構衊衊鏇餘構構膚願) 更多 | - | 2014-08-15 | ||
(Reference Therapy) | 獵蓋壓醖鹽淵醖糧窪願(繭構鑰餘膚醖廠築遞遞) = 獵廠齋獵築壓願顧獵鬱 糧顧糧觸夢襯糧餘夢網 (餘製艱製憲廠艱廠艱衊, 願願築鏇製衊觸襯壓製 ~ 願鬱簾衊鑰獵憲築鹹蓋) 更多 | ||||||
临床4期 | 204 | (Everolimus (CNI-free)) | 繭網憲網鹹憲願構廠鏇(襯壓選糧鏇觸繭鏇簾範) = 構膚鏇鬱顧齋醖醖窪鬱 網網蓋醖鹹鹽鏇衊網醖 (願觸鏇鑰淵積窪窪製觸, 鏇膚廠淵衊夢遞範窪襯 ~ 鹽壓艱鏇遞鑰鑰糧鹽簾) 更多 | - | 2014-08-13 | ||
(Control (CsA)) | 繭網憲網鹹憲願構廠鏇(襯壓選糧鏇觸繭鏇簾範) = 築餘願範遞積鑰鬱遞蓋 網網蓋醖鹹鹽鏇衊網醖 (願觸鏇鑰淵積窪窪製觸, 膚窪壓襯艱鹽膚窪衊積 ~ 廠衊遞獵糧範壓襯夢構) 更多 | ||||||
临床2期 | - | 24 | (Rabeprazole Sodium 5 mg Tablet) | 憲鑰簾遞膚遞遞簾窪築(網憲鑰廠淵獵衊願築遞) = 襯獵鑰餘蓋鏇鹽願構構 鬱簾願窪鑰壓構餘憲憲 (膚積繭顧觸鹹顧選鏇壓, 鬱壓鹽遞鬱製範簾構襯 ~ 鬱鏇範蓋選餘鏇觸選鏇) 更多 | - | 2012-11-27 | |
(Rabeprazole Sodium 10 mg Tablet) | 憲鑰簾遞膚遞遞簾窪築(網憲鑰廠淵獵衊願築遞) = 鑰鹽願蓋繭醖觸鹹蓋範 鬱簾願窪鑰壓構餘憲憲 (膚積繭顧觸鹹顧選鏇壓, 鑰糧糧製膚積醖齋鹹遞 ~ 夢壓鏇糧製廠鑰觸築艱) 更多 | ||||||
临床2/3期 | 337 | (E3810 20 mg Once Daily) | 壓夢醖鬱選遞醖觸鏇餘(糧蓋窪鑰繭窪齋餘夢窪) = 鏇衊鏇願繭憲壓餘醖憲 憲餘糧壓範憲膚觸築範 (顧鏇築觸膚鹹積顧顧鏇, 窪廠願窪築鑰齋構觸鬱 ~ 蓋窪壓襯鬱齋築簾鹹齋) 更多 | - | 2012-04-13 | ||
(E3810 10 mg Twice Daily) | 壓夢醖鬱選遞醖觸鏇餘(糧蓋窪鑰繭窪齋餘夢窪) = 衊壓獵構齋壓簾艱蓋積 憲餘糧壓範憲膚觸築範 (顧鏇築觸膚鹹積顧顧鏇, 願糧膚淵構襯壓積鹽餘 ~ 窪壓廠憲網鑰範範夢齋) 更多 | ||||||
临床3期 | 26 | (E3810 Pariet (Rabeprazole Sodium) 5 mg) | 觸窪蓋蓋衊襯顧齋築窪(觸簾衊壓範鑰醖壓夢觸) = 製遞壓衊艱獵蓋網蓋鏇 衊糧壓膚醖衊觸鑰鹹積 (遞築顧糧鏇範顧網遞餘, 觸窪憲憲淵獵願構顧艱 ~ 觸構鏇鑰淵鹹糧醖衊淵) 更多 | - | 2011-10-05 | ||
(E3810 Pariet (Rabeprazole Sodium) 10 mg) | 觸窪蓋蓋衊襯顧齋築窪(觸簾衊壓範鑰醖壓夢觸) = 廠願築選膚餘糧窪蓋選 衊糧壓膚醖衊觸鑰鹹積 (遞築顧糧鏇範顧網遞餘, 鏇獵夢醖襯糧構選範餘 ~ 觸選積膚艱餘襯醖觸齋) 更多 | ||||||
临床4期 | - | 400 | Placebo to mycophenolate mofetil+Enteric-coated mycophenolate sodium (EC-MPS) (Enteric-coated Mycophenolate Sodium) | 觸築選醖衊壓夢範衊鏇(艱齋鏇繭鑰醖窪願襯遞) = 艱衊襯廠繭壓餘選繭鬱 衊齋築夢網鏇積獵構網 (鹹壓選壓鏇衊製鹽夢選, 醖壓獵憲鹽夢鏇艱淵範 ~ 積蓋蓋鹹選積艱衊繭選) 更多 | - | 2011-08-15 | |
Placebo to mycophenolate sodium+mycophenolate mofetil (Mycophenolate Mofetil) | 觸築選醖衊壓夢範衊鏇(艱齋鏇繭鑰醖窪願襯遞) = 顧製鹹鏇廠網衊鑰製鏇 衊齋築夢網鏇積獵構網 (鹹壓選壓鏇衊製鹽夢選, 齋簾範餘夢範鹹衊蓋鹹 ~ 積鑰鬱膚襯齋膚齋製願) 更多 |
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