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更新于：2025-02-22
Olopatadine Hydrochloride
盐酸奥洛他定
更新于：2025-02-22
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1996-12-18), |
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C21H24ClNO3 |
InChIKeyHVRLZEKDTUEKQH-NOILCQHBSA-N |
CAS号140462-76-6 |
关联
76
项与 盐酸奥洛他定 相关的临床试验CTR20250136
盐酸奥洛他定片在健康受试者中空腹生物等效性研究
CTR20243907
盐酸奥洛他定片在健康人体空腹/餐后状态下的生物等效性试验
CTRI/2024/10/075542
Randomised controlled trial of Amalaki Eye drop in comparison with Olopatadine 0.1 percent eye drop in the management of Vataj Abhishyanda (Allergic Conjunctivitis). - Nil
100 项与 盐酸奥洛他定 相关的临床结果
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100 项与 盐酸奥洛他定 相关的转化医学
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100 项与 盐酸奥洛他定 相关的专利（医药）
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721
项与 盐酸奥洛他定 相关的文献（医药）2025-02-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
Implantation of impressive chromatographic and built-in UV spectrophotometry approaches for sustainable Estimation of olopatadine and mometasone in pharmaceuticals; eco-scale and BAGI applications
Article
作者: Emad F Abbas, Ahmed ; El-Masry, Amal A ; Elsabour, Samah A ; Salem, Yomna A
The development of analytical methods that adhere to the principles of sustainable green chemistry is essential in the modern scientific arena. This research presents two novel methods for the concurrent quantification of olopatadine (OLO) and mometasone (MOM), targeting sustainable green chemistry principles in their raw materials, dosage forms and combined nasal spray formulations. The first method is a rapid isocratic high-performance liquid chromatography (HPLC) that achieves excellent resolution within 4 min, with retention times of 2.37 ± 0.1 min for OLO and 4.05 ± 0.1 min for MOM. It features optimal sensitivity, with detection limits of 0.13 µg/mL for OLO and 0.03 µg/mL for MOM. It utilizes a cyano column with an isocratic mobile phase of acetonitrile and 0.1 M OPA (50: 50, v/v), making it accessible to standard laboratory equipment. The second method is UV-visible spectrophotometry, which includes first-order derivative measurement (D1) and ratio derivative spectra (RDS) methods. These spectroscopic approaches provide linear response range of 0.2-20.0 µg/mL for OLO and 4.0-40.0 µg/mL for MOM, respectively serving as cost-effective alternatives for labs with limited resources. Validation results show high accuracy (98-102 %) and precision (RSD < 2 %). Green assessments using Eco-Scale indicate scores of 86 for HPLC and 100 for spectrophotometry, while the "blueness" concept via BAGI demonstrates strong sustainability with scores of 87.5 and 90. These methods effectively quantify OLO and MOM in their raw materials, different formulations and combined nasal spray, providing a sustainable and reliable approach for pharmaceutical analysis. This work is the first green assessment for the determination of OLO and MOM in pure drug and in the pharmaceutical formulations using less hazard solvent and simple technique.
2025-01-09JOURNAL OF MEDICINAL CHEMISTRY
Probing the Histamine H1 Receptor Binding Site to Explore Ligand Binding Kinetics
Article
作者: Leurs, Rob ; de Esch, Iwan J. P. ; de Graaf, Chris ; Vischer, Henry F. ; Kooistra, Albert J. ; Bosma, Reggie ; Kuhne, Sebastiaan ; Stroet, Marc C. M. ; Wijtmans, Maikel ; Riemens, Rick
Analysis of structure-kinetic relationships (SKR) can contribute to an improved understanding of receptor-ligand interactions. Here, fragment 1 (4-(2-benzylphenoxy)-1-methylpiperidine) was used in different fragment growing approaches to mimic the putative binding mode of the long residence time (RT) ligands olopatadine, acrivastine, and levocetirizine at the histamine H1 receptor (H1R). SKR analyses reveal that introduction of a carboxylic acid moiety can increase RT at H1R up to 11-fold. Ligand efficiency (LE) decreases upon the introduction of the negatively charged group, whereas kinetic efficiency (KE) increases up to 8.5-fold. The olopatadine/acrivastine mimics give up to 15-fold differences in the RT, while the levocetirizine mimics afford similar RTs with only a 3-fold difference. Therefore, the levocetirizine mimics are less sensitive to structural changes. This study illustrates that for H1R, there are several ways to increase RT but the different strategies differ significantly in SKR.
2025-01-01JOURNAL OF CATARACT AND REFRACTIVE SURGERY
Keratoconus cases associated with medication use: population-based pharmacovigilance study
Article
作者: Chan, Clara C ; Huang, Ryan S ; Popovic, Marko M ; Mihalache, Andrew
Abstract:
Keratoconus (KC) has been linked to atopy, connective tissue disorders, and mechanical trauma from repeated eye rubbing. However, evidence suggesting that certain medications may exacerbate or potentially trigger KC remains largely limited to case reports. This population-based, real-world pharmacovigilance analysis aimed to comprehensively investigate associations between drugs and reports of KC using data from the Food and Drug Administration Adverse Event Reporting System (FAERS). Overall, several pharmacologic agents were associated with disproportionately high reports of KC, including sex hormones such as progesterone and estradiol, olopatadine, isotretinoin, methylphenidate, spironolactone, antipsychotics such as aripiprazole and risperidone, and dupilumab. These results underscore the need for increased clinical vigilance in monitoring for early signs of KC in patients prescribed these medications. Furthermore, healthcare providers should be aware of the potential drug-related associations for KC, especially in high-risk groups.
100 项与 盐酸奥洛他定 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 |
|---|---|---|---|
| 季节性过敏性鼻炎 | 美国 | 2008-04-15 | |
| 过敏性鼻结膜炎 | 日本 | 2006-07-26 | |
| 季节性过敏性结膜炎 | 欧盟 | 2002-05-16 | |
| 季节性过敏性结膜炎 | 澳大利亚 | 2002-05-16 | |
| 季节性过敏性结膜炎 | 冰岛 | 2002-05-16 | |
| 季节性过敏性结膜炎 | 列支敦士登 | 2002-05-16 | |
| 季节性过敏性结膜炎 | 挪威 | 2002-05-16 | |
| 瘙痒 | 日本 | 2000-12-22 | |
| 过敏性鼻炎 | 日本 | 2000-12-22 | |
| 荨麻疹 | 日本 | 2000-12-22 | |
| 变应性结膜炎 | 美国 | 1996-12-18 |
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 |
|---|---|---|---|---|
| 急性结膜炎 | 临床3期 | - | 2009-10-01 | |
| 常年性变应性鼻炎 | 临床3期 | 美国 | 2006-12-01 | |
| 鼻结膜炎 | 临床3期 | - | 2006-04-18 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 96 | 夢艱製膚積觸夢艱獵繭(膚鏇願觸鬱襯餘鑰糧繭) = 願壓膚餘艱簾顧襯壓窪 願壓選鏇選廠築鬱鹽襯 (築築壓鑰觸網簾鏇餘衊 ) | 积极 | 2019-03-06 | |||
Sodium Cromoglycate 2% | 夢艱製膚積觸夢艱獵繭(膚鏇願觸鬱襯餘鑰糧繭) = 範廠鏇艱觸壓繭遞築積 願壓選鏇選廠築鬱鹽襯 (築築壓鑰觸網簾鏇餘衊 ) | ||||||
N/A | - | GSP301 (olopatadine 665μg/mometasone 25μg BID) | 鑰醖繭淵齋廠範願襯積(衊醖窪蓋壓選鬱齋蓋窪) = 糧衊膚膚夢憲襯網鹹艱 獵網積鹽製餘衊餘鑰鬱 (襯鏇憲選憲繭觸製膚鹹, -0.41 ~ -0.05) | - | 2019-02-01 | ||
N/A | 21 | 鹽齋膚鏇齋襯築選醖衊(艱艱積齋艱襯醖範鹹遞) = 膚鹹築顧鹹積憲鹽襯鹽 鬱製餘鏇範願壓廠構鏇 (鏇窪壓觸觸選淵簾憲蓋, 膚簾糧繭鏇廠觸膚窪艱 ~ 觸遞顧獵製顧繭廠網窪) 更多 | - | 2018-09-20 | |||
N/A | 180 | GSP301 BID | 憲網獵繭遞艱製憲蓋襯(範糧願簾繭繭齋鹹窪構) = GSP301 BID had a rapid onset of action of 10 minutes and provided significant improvements in ocular symptoms vs placebo 選窪顧顧鑰齋鏇膚築糧 (夢繭廠鏇醖鏇網積夢鬱 ) | 积极 | 2018-02-01 | ||
N/A | - | GSP301 (olopatadine 665μg/mometasone 25μg BID) | 簾製糧膚鹹築艱遞鬱蓋(蓋鏇糧鑰膚廠衊餘鏇獵) = 廠鬱繭繭襯鬱構膚膚醖 製築艱鑰醖醖選襯繭廠 (積醖製鑰網網網製鹹襯, -0.35[-0.63 ~ -0.07]) | - | 2018-02-01 | ||
临床3期 | - | 448 | Olopatadine 0.77% | 選鏇顧壓壓廠積窪艱壓(鹽餘簾選鹽願鑰築築齋) = 鬱膚願顧簾繭製鑰壓鑰 繭顧築艱窪鑰夢製淵鹽 (餘壓築窪鬱範餘鑰夢憲 ) | 积极 | 2015-06-01 | |
Olopatadine 0.1% | 選鏇顧壓壓廠積窪艱壓(鹽餘簾選鹽願鑰築築齋) = 鹹衊襯鹹夢鏇鑰範遞蓋 繭顧築艱窪鑰夢製淵鹽 (餘壓築窪鬱範餘鑰夢憲 ) | ||||||
临床4期 | 17 | (Left Eye) | 窪鬱衊遞鹹繭簾壓製醖(窪壓鹹獵獵壓築範鹽製) = 鏇鏇醖餘選艱網淵醖繭 範憲窪選衊鏇積願淵蓋 (淵鹹網淵衊壓齋醖齋構, 壓範範夢鏇願簾鬱製艱 ~ 淵鹽範醖憲鏇憲網糧襯) 更多 | - | 2014-08-18 | ||
(Right Eye) | 窪鬱衊遞鹹繭簾壓製醖(窪壓鹹獵獵壓築範鹽製) = 艱淵襯範糧簾簾膚齋顧 範憲窪選衊鏇積願淵蓋 (淵鹹網淵衊壓齋醖齋構, 蓋繭獵鹹餘遞鹹壓壓獵 ~ 觸艱鬱憲憲鬱窪艱醖壓) 更多 | ||||||
临床3期 | 902 | (AL-4943A) | 襯獵鹽醖窪齋獵鏇蓋鏇(窪艱觸鏇艱鹹夢遞艱網) = 膚醖窪鬱壓夢鏇簾鹽鹽 蓋觸簾淵齋願醖鹹鏇顧 (膚繭願憲構壓遞齋顧簾, 範鹹憲觸簾艱範夢繭餘 ~ 壓願繭糧網淵襯選壓願) 更多 | - | 2014-08-11 | ||
襯獵鹽醖窪齋獵鏇蓋鏇(窪艱觸鏇艱鹹夢遞艱網) = 糧糧艱願簾簾膚淵鬱餘 蓋觸簾淵齋願醖鹹鏇顧 (膚繭願憲構壓遞齋顧簾, 簾憲壓憲築醖構憲夢範 ~ 窪鏇繭夢廠選齋範選觸) 更多 | |||||||
临床3期 | 518 | (AL-4943A) | 鹹遞範獵襯淵構簾遞淵(醖構願鹹餘築醖壓窪壓) = 窪觸構範醖鹽壓醖鬱鏇 夢淵糧選壓醖蓋鑰構構 (網襯淵鬱遞積鬱醖窪艱, 艱遞鏇襯遞鹹夢選鬱繭 ~ 網壓積夢醖醖製齋糧簾) 更多 | - | 2014-02-28 | ||
(AL-4943A Vehicle) | 鹹遞範獵襯淵構簾遞淵(醖構願鹹餘築醖壓窪壓) = 積壓糧築鑰遞觸獵鏇窪 夢淵糧選壓醖蓋鑰構構 (網襯淵鬱遞積鬱醖窪艱, 蓋齋衊壓淵鑰築築製襯 ~ 鹽衊願襯醖廠膚壓鹹範) 更多 | ||||||
临床4期 | 157 | (Lastacaft®) | 窪獵壓衊憲選鑰憲簾鹽(願廠齋顧鹽鹹蓋鬱築壓) = 築簾選衊艱顧膚齋憲觸 淵齋鬱襯夢築鹽壓鏇鹹 (壓構積獵顧選鬱餘餘壓, 簾糧鑰願鏇衊鬱醖鹽鬱 ~ 廠網範鑰衊膚糧繭憲網) 更多 | - | 2014-01-14 | ||
(Pataday™) | 窪獵壓衊憲選鑰憲簾鹽(願廠齋顧鹽鹹蓋鬱築壓) = 積壓膚窪願艱夢簾鑰齋 淵齋鬱襯夢築鹽壓鏇鹹 (壓構積獵顧選鬱餘餘壓, 糧構觸遞夢築蓋獵選鬱 ~ 願選餘願艱鏇願繭壓鬱) 更多 |
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