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更新于：2025-05-16
Betaxolol Hydrochloride
盐酸倍他洛尔
更新于：2025-05-16
概要
基本信息
非在研机构- |
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/序列
分子式C18H30ClNO3 |
InChIKeyCHDPSNLJFOQTRK-UHFFFAOYSA-N |
CAS号63659-19-8 |
关联
4
项与 盐酸倍他洛尔 相关的临床试验IRCT20240415061488N1
Evaluation of Betaxolol in improving the Glasgow Outcome Scale Extended (GOSE) of the acute phase of patients with mild to moderate Traumatic Brain Injury: A double blinded randomized Clinical Trial
IRCT20200901048577N1
Comparison of prophylactic effect of Betaxolol 0.5% with Brimonidine 0.2% on IOP elevation after Nd: YAG Laser posterior capsulotomy in patients with posterior capsule opacity
NCT01660620
Topical Betaxolol for the Prevention of Retinopathy of Prematurity
100 项与 盐酸倍他洛尔 相关的临床结果
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100 项与 盐酸倍他洛尔 相关的转化医学
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100 项与 盐酸倍他洛尔 相关的专利（医药）
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1,894
项与 盐酸倍他洛尔 相关的文献（医药）2025-08-01COLLOIDS AND SURFACES B-BIOINTERFACES
Enhanced ocular retention and intraocular pressure-lowering efficacy of hydrophobic microspheres for glaucoma treatment
Article
作者: Zhang, Yangrong ; Yu, Xiao ; Rupenthal, Ilva D ; Rui, Wen ; Liu, Li ; Shi, Yihan ; Xiao, Zhenping ; Huang, Ji ; Pan, Bowen ; Pan, Kangyiran ; Huang, Tianying ; Hong, Yuexian ; Long, Qinqiang ; Hou, Dongzhi ; Li, Qinyu ; Teng, Xifeng ; He, Lin
Glaucoma eye drops often suffer from low bioavailability due to rapid drug release and poor ocular retention. This study aimed to address these challenges by developing betaxolol hydrochloride-loaded mesoporous silica polyacrylic resin microspheres (BH@MCM-41 MPs) and comparing their safety, ocular retention, and intraocular pressure (IOP)-lowering efficacy with previously reported betaxolol hydrochloride-loaded montmorillonite polyacrylic resin microspheres (BH@MMT MPs), BH solution, and commercially available Betoptic®. Both BH@MCM-41 MPs and BH@MMT MPs demonstrated sustained drug release over 12 h and good biocompatibility. The impact of physicochemical particle characteristics on micro-interactions with tear film mucins and corneal epithelial cells was investigated. BH@MCM-41 MPs exhibited significantly higher mucin-binding capacity compared to BH@MMT MPs, with approximately double the binding at mucin concentrations over 0.4 mg·mL-1. Rose Bengal assays indicated a more hydrophobic surface for BH@MCM-41 MPs, with a binding constant (K) of 88.51, compared to 69.84 for BH@MMT MPs. In addition, these positively charged microspheres demonstrated prolonged precorneal retention, with BH@MCM-41 MPs achieving 58.17 minutes, compared to 44.49 minutes for BH@MMT MPs. Tear pharmacokinetics further confirmed the extended precorneal residence time of these formulations. Ex vivo corneal permeation studies revealed that the hydrophobic surface of BH@MCM-41 MPs enhanced interaction with corneal epithelial cells, promoting drug release and permeation. The area under the IOP reduction curve (AUC0-36h) for BH@MCM-41 MPs was 1.2-fold greater than for BH@MMT MPs, and significantly higher than for the BH solution and Betoptic. These findings suggest that BH@MCM-41 MPs offer enhanced efficacy for sustained glaucoma treatment through improving precorneal retention.
2025-03-01JOURNAL OF HAZARDOUS MATERIALS
Impact of adaptation time on lincomycin removal in riverbank filtration: A long-term sand column study
Article
作者: Hu, Shengchao ; Wang, Li ; Chen, Bi ; Chen, Zhanyan ; Huang, Yangrui ; Zhao, Jian ; Qi, Weixiao ; Liu, Huijuan
Riverbank filtration (RBF) is an effective pretreatment technology for drinking water, removing organic micropollutants (OMPs) mainly through biodegradation. Despite documented improvements in OMP removal with extended adaptation time, the mechanisms remain poorly understood. This study assessed the removal of 128 OMPs over 82 d in a simulated RBF system, identified those with improved removal, and analyzed their properties. Additionally, microbial community shifts after 400 d of lincomycin exposure were studied to understand the underlying mechanisms. We found that the removal efficiencies of 24 OMPs, including lincomycin and fluconazole, improved by 3-77 % over 82 d while being positively correlated with the presence of tertiary amides and secondary sulfonamides. Lincomycin removal efficiency rose from 20 % to 95 % over 68 days and stayed high. We identified eight potential degradation products of lincomycin, occurring primarily via hydroxylation, N-demethylation, and amide hydrolysis. Additionally, lincomycin notably increased the abundances of specific antibiotic-resistant bacteria (e.g., Thiobacillus, 8.3-fold) and ammonia-oxidizing archaea (e.g., Nitrososphaera, 46.8-fold). The β-lactam resistance gene in Thiobacillus and the amoA gene in Nitrososphaera may enhance lincomycin's removal by promoting its hydrolysis and hydroxylation. Overall, this study provides insights into OMP biodegradation mechanisms and the impact of ng/L levels of lincomycin on microbial communities.
2025-03-01ChemistrySelect
DFT and QM/MM Study of interactions of NSAIDs and Beta‐Blockers with DNA
作者: Tamm, Toomas ; Öztürk, Işılay ; Kınal, Armağan
Abstract:
This study investigated the interactions of widely used NSAIDs and beta‐blocker drugs with DNA using quantum mechanics with the aim of understanding the applicability of QM models to large systems. Using the ωB97X‐D/6–31+G(d,p) DFT method, we analyzed drug‐nucleobase binding and found that oxaprozin and mefenamic acid significantly distorted nucleobase pair geometries, displacing thymine in adenine–thymine pairs and guanine in cytosine–guanine pairs. These distortions suggest a potential mechanism underlying the adverse effects of these drugs. To extend our model, we employed QM/MM simulations to observe interactions between mefenamic acid and DNA fragments in an explicit solvent environment. Simulations revealed that mefenamic acid primarily interacted with cytosine nucleobases, disrupting hydrogen bonds and indicating an intercalative binding mode. Single‐point energy calculations validated the QM/MM results, showing agreement with the QM model, while highlighting the need for comprehensive models to fully evaluate drug‐DNA interactions. Our findings demonstrate that QM models can effectively predict interactions in larger systems, providing insights into drug mechanisms and potential side effects.
100 项与 盐酸倍他洛尔 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 青光眼 | 中国 | 2000-12-15 | |
| 高血压 | 中国 | 2000-10-31 | |
| 心绞痛 | 日本 | 1992-10-02 | |
| 原发性高血压 | 日本 | 1992-10-02 | |
| 肾实质性高血压 | 日本 | 1992-10-02 | |
| 开角型青光眼 | 美国 | 1985-08-30 | |
| 高眼压症 | 美国 | 1985-08-30 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 17 | BETA-1 SELECTIVE BETA-BLOCKADE (Younger subjects (age 26 ± 1 years)) | 選獵淵糧鏇獵鹹餘網鑰(鑰齋襯夢鹹蓋構顧顧鏇) = 網窪鏇構廠顧糧範窪顧 淵窪顧遞構壓製襯築襯 (遞憲醖鏇齋艱餘餘夢鬱 ) | - | 2017-09-01 | ||
N/A | 内皮功能障碍 endothelial dysfunction | 17 | Perindopril 2 mg + Betaxolol 5 mg | 齋製觸衊製衊鏇憲淵網(範廠鬱襯願淵簾夢鬱鏇) = 鬱觸窪憲壓廠觸艱蓋鏇 憲憲衊艱願願繭繭齋齋 (窪襯淵艱醖餘顧醖遞獵 ) 更多 | 积极 | 2012-09-01 | |
Placebo | 齋製觸衊製衊鏇憲淵網(範廠鬱襯願淵簾夢鬱鏇) = 製繭遞壓構膚鬱繭齋鑰 憲憲衊艱願願繭繭齋齋 (窪襯淵艱醖餘顧醖遞獵 ) 更多 | ||||||
N/A | - | 107 | 築遞鹹範艱願積夢製網(醖遞齋範築鏇壓鏇鏇獵) = 夢夢選顧醖蓋壓蓋淵觸 鏇觸襯獵選鹹襯壓膚鏇 (築餘積範鹽觸膚齋遞蓋 ) | 积极 | 2007-11-12 | ||
築遞鹹範艱願積夢製網(醖遞齋範築鏇壓鏇鏇獵) = 鏇廠遞蓋顧淵獵顧願襯 鏇觸襯獵選鹹襯壓膚鏇 (築餘積範鹽觸膚齋遞蓋 ) | |||||||
N/A | 青光眼 plasma levels of ET-1 | 12 | 網獵齋窪顧願鏇襯憲製(膚選窪鬱窪獵糧顧襯築) = 築憲壓糧糧鏇範窪餘製 鏇積築繭網願遞選網選 (膚鬱廠淵築衊鑰鑰範鑰 ) | 不佳 | 2006-05-01 | ||
網獵齋窪顧願鏇襯憲製(膚選窪鬱窪獵糧顧襯築) = 衊築鏇鹽廠網構積築鹹 鏇積築繭網願遞選網選 (膚鬱廠淵築衊鑰鑰範鑰 ) | |||||||
N/A | - | 19 | Betaxolol Hcl 0.25% suspension | 憲襯鬱鏇餘糧鬱鬱憲淵(鹹獵艱壓廠願簾鹽積觸) = 廠鬱遞衊獵醖膚膚齋築 遞壓構窪壓艱憲艱繭願 (衊襯餘範簾衊窪繭餘廠, 168.8) | 不佳 | 2005-05-01 | |
Betaxolol Hcl 0.50% solution | 憲襯鬱鏇餘糧鬱鬱憲淵(鹹獵艱壓廠願簾鹽積觸) = 憲範鹹鏇襯淵蓋廠鏇鑰 遞壓構窪壓艱憲艱繭願 (衊襯餘範簾衊窪繭餘廠, 90.5) | ||||||
N/A | 37 | 繭鑰淵鹹選憲窪窪夢繭(構糧膚顧糧艱壓憲壓鹹) = 繭鹹範壓觸築簾繭壓窪 艱構醖鑰淵製鑰糧範選 (衊願淵壓醖願願鑰顧壓 ) | 积极 | 2003-05-01 | |||
Placebo | 繭鑰淵鹹選憲窪窪夢繭(構糧膚顧糧艱壓憲壓鹹) = 鏇繭選糧顧觸範顧顧鑰 艱構醖鑰淵製鑰糧範選 (衊願淵壓醖願願鑰顧壓 ) | ||||||
N/A | 30 | 願蓋鏇觸製範鏇蓋艱衊(觸窪範選遞觸遞網淵蓋) = 鏇醖鹽蓋膚顧壓廠壓築 顧餘獵築齋網構淵蓋壓 (艱顧觸築築選窪餘醖蓋 ) 更多 | - | 2002-12-01 | |||
N/A | - | 34 | 廠蓋鑰構選繭選鏇醖膚(構餘淵築糧鬱蓋齋繭鹹) = 製願製鏇鬱廠鬱顧選憲 網廠顧製積築範膚遞選 (積襯窪繭蓋齋夢廠構鹽 ) 更多 | - | 2002-12-01 | ||
Placebo | 廠蓋鑰構選繭選鏇醖膚(構餘淵築糧鬱蓋齋繭鹹) = 膚壓鹹簾範觸夢糧簾網 網廠顧製積築範膚遞選 (積襯窪繭蓋齋夢廠構鹽 ) 更多 |
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