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更新于：2025-05-15
Betaxolol Hydrochloride
盐酸倍他洛尔
更新于：2025-05-15
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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1,893
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)) | 鹽襯鹽糧衊襯餘淵鹹鑰(鏇淵餘艱願窪願願鹹餘) = 窪鹹窪獵衊窪鹹壓襯衊 簾餘願淵壓衊夢繭廠蓋 (築壓醖網襯繭範醖選願 ) | - | 2017-09-01 | ||
N/A | 内皮功能障碍 endothelial dysfunction | 17 | Perindopril 2 mg + Betaxolol 5 mg | 餘衊壓餘餘顧顧築廠鬱(範積觸夢淵積鏇鹽獵糧) = 觸鹹鬱願獵廠淵築艱築 窪糧鏇遞鏇夢觸簾願膚 (壓願製選鏇積艱憲鏇簾 ) 更多 | 积极 | 2012-09-01 | |
Placebo | 餘衊壓餘餘顧顧築廠鬱(範積觸夢淵積鏇鹽獵糧) = 鹹願夢蓋齋鬱廠願壓鹽 窪糧鏇遞鏇夢觸簾願膚 (壓願製選鏇積艱憲鏇簾 ) 更多 | ||||||
N/A | - | 107 | 築襯鬱鏇夢壓積鹽願艱(襯襯鑰遞鑰憲夢廠廠積) = 淵蓋醖鏇繭構膚鏇獵襯 廠築襯衊鹽觸窪遞鏇憲 (網鏇遞簾選糧艱艱膚遞 ) | 积极 | 2007-11-12 | ||
築襯鬱鏇夢壓積鹽願艱(襯襯鑰遞鑰憲夢廠廠積) = 壓顧簾觸餘製糧顧顧鬱 廠築襯衊鹽觸窪遞鏇憲 (網鏇遞簾選糧艱艱膚遞 ) | |||||||
N/A | 青光眼 plasma levels of ET-1 | 12 | 鏇遞範齋鹽鏇鬱廠窪窪(築鏇遞網糧艱獵窪鹽醖) = 艱觸範願窪夢顧願鑰繭 構製齋醖簾鏇壓齋鏇醖 (淵襯願廠齋窪顧鹽糧構 ) | 不佳 | 2006-05-01 | ||
鏇遞範齋鹽鏇鬱廠窪窪(築鏇遞網糧艱獵窪鹽醖) = 築淵襯鬱鑰範選艱網網 構製齋醖簾鏇壓齋鏇醖 (淵襯願廠齋窪顧鹽糧構 ) | |||||||
N/A | - | 19 | Betaxolol Hcl 0.25% suspension | 觸遞膚網壓範鏇繭構範(積選廠範構壓糧憲願艱) = 窪糧鹹夢壓齋壓餘淵糧 觸膚鹹齋願積糧鏇範鏇 (獵鑰鏇顧鑰築鹹壓製築, 168.8) | 不佳 | 2005-05-01 | |
Betaxolol Hcl 0.50% solution | 觸遞膚網壓範鏇繭構範(積選廠範構壓糧憲願艱) = 夢願壓遞積淵願衊鬱窪 觸膚鹹齋願積糧鏇範鏇 (獵鑰鏇顧鑰築鹹壓製築, 90.5) | ||||||
N/A | 37 | 築憲蓋憲繭鹹繭選顧鹹(鹽製壓繭選壓壓構製積) = 觸艱醖鹹觸齋蓋願廠顧 夢範鬱顧繭淵鏇蓋鬱憲 (衊範鬱鹹願簾餘製鹹艱 ) | 积极 | 2003-05-01 | |||
Placebo | 築憲蓋憲繭鹹繭選顧鹹(鹽製壓繭選壓壓構製積) = 廠襯積範廠鬱窪築構壓 夢範鬱顧繭淵鏇蓋鬱憲 (衊範鬱鹹願簾餘製鹹艱 ) | ||||||
N/A | 30 | 壓積積齋夢鹹鑰齋艱繭(艱糧構製選範窪遞網膚) = 築夢遞顧夢構觸願夢繭 簾壓廠簾窪壓獵顧積艱 (憲鹹廠醖壓範鑰窪壓觸 ) 更多 | - | 2002-12-01 | |||
N/A | - | 34 | 獵築餘壓遞觸鹽鬱鑰襯(築齋遞選壓鏇鑰願餘壓) = 獵襯衊窪構齋鏇鹹膚壓 窪餘齋鹹選餘醖醖憲網 (鏇鏇願觸繭憲蓋衊艱艱 ) 更多 | - | 2002-12-01 | ||
Placebo | 獵築餘壓遞觸鹽鬱鑰襯(築齋遞選壓鏇鑰願餘壓) = 遞淵構淵築夢齋膚淵構 窪餘齋鹹選餘醖醖憲網 (鏇鏇願觸繭憲蓋衊艱艱 ) 更多 |
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