预约演示
更新于：2025-10-30
Betaxolol Hydrochloride
盐酸倍他洛尔
更新于：2025-10-30
概要
基本信息
药物类型 小分子化药 |
别名 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol、1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol、Betaxolol + [17] |
作用方式 拮抗剂 |
作用机制 β1-adrenergic receptor拮抗剂(β1-肾上腺素能受体拮抗剂) |
非在研适应症- |
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
5
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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1,595
项与 盐酸倍他洛尔 相关的文献（医药）2025-09-01JOURNAL OF CHROMATOGRAPHY A
Cationic separation of medium strong bases by electrophoretic focusing on inverse electromigration dispersion profile. Sensitive analysis of beta-blockers in blood and water with ESI-MS detection
Article
作者: Malá, Zdena ; Gebauer, Petr
Electrophoretic focusing on an inverse electromigration dispersion profile is a method where the migrating profile focuses and separates the analytes and transports them to the detector. Although so far only a few anionic and cationic electrolyte systems have been reported for this technique, it has proved its separation and concentration power and potential for sensitive and selective analyses of samples with complex matrices, typically without any pretreatment. To extend its applicability, there is need for the design of electrolyte systems covering other pH ranges and potential analyte groups. This work describes the first functional cationic system for electrophoretic focusing on inverse electromigration dispersion profile in the alkaline region, based on pentamethylenediamine and acetohydroxamic acid. Computer simulation and experiments have shown that the designed electromigration dispersion profile can be split into smaller sub-profiles to reach increased performance and selectivity. The practical applicability of the system is demonstrated on the analysis of beta-blockers in capillary blood via the dried blood spot technique in combination with electrospray-ionization mass-spectrometric detection. The method allows direct injection of aqueous dried blood spot extracts and sensitive determination of metoprolol and betaxolol in real samples with limits of detection at the 2 nM (500 ngL-1) level. Experiments with direct injection of spiked water samples show that the method can be used also for analysis of beta-blockers in waters with almost the same sensitivity.
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 ; Rui, Wen ; Rupenthal, Ilva D ; Liu, Li ; Shi, Yihan ; Xiao, Zhenping ; Huang, Ji ; Pan, Bowen ; Pan, Kangyiran ; Huang, Tianying ; Long, Qinqiang ; Hong, Yuexian ; Hou, Dongzhi ; He, Lin ; Li, Qinyu ; Teng, Xifeng
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 ; Liu, Huijuan ; Qi, Weixiao
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.
100 项与 盐酸倍他洛尔 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 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 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 青光眼 | 临床3期 | 美国 | 2003-01-01 |
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临床结果
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适应症
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临床3期 | 105 | 廠齋遞鏇窪繭蓋襯範網(獵獵繭艱鑰廠鏇壓構構) = 遞衊繭鹹齋獵積鏇範鹹 範窪衊齋鑰壓選窪壓鹽 (網顧觸壓餘淵淵醖糧廠 ) 更多 | - | 2009-08-01 | |||
Timolol maleate ophthalmic gel-forming solution 0.25% | 廠齋遞鏇窪繭蓋襯範網(獵獵繭艱鑰廠鏇壓構構) = 顧衊遞淵衊糧鏇鬱鹽鹹 範窪衊齋鑰壓選窪壓鹽 (網顧觸壓餘淵淵醖糧廠 ) 更多 |
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