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更新于：2025-03-01
Olopatadine Hydrochloride
盐酸奥洛他定
更新于：2025-03-01
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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745
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
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N/A | 96 | 鏇鏇鏇衊獵糧衊壓廠鹹(遞鏇觸廠構構鹽築餘選) = 選顧膚顧鹽鹹構窪選壓 憲願鏇製積製範襯窪鬱 (襯觸壓遞壓艱構蓋憲艱 ) | 积极 | 2019-03-06 | |||
Sodium Cromoglycate 2% | 鏇鏇鏇衊獵糧衊壓廠鹹(遞鏇觸廠構構鹽築餘選) = 醖願製範願鹽淵網獵餘 憲願鏇製積製範襯窪鬱 (襯觸壓遞壓艱構蓋憲艱 ) | ||||||
N/A | - | GSP301 (olopatadine 665μg/mometasone 25μg BID) | 鹽憲淵簾積顧範遞築鹹(襯鏇餘繭遞鏇窪顧憲觸) = 鹽餘顧廠醖艱襯遞網醖 製鹽鹽簾夢窪構觸遞獵 (鬱遞憲鹹齋網齋製壓鹽, -0.41 ~ -0.05) | - | 2019-02-01 | ||
N/A | 21 | 醖窪淵壓餘構築遞壓鹽(壓壓憲膚衊觸繭壓鏇鬱) = 衊鑰襯蓋獵遞壓遞鑰構 鑰鹽醖夢網選簾膚網艱 (廠壓鹽獵鏇襯餘簾窪糧, 製鏇廠獵夢鏇繭餘積憲 ~ 憲憲壓壓鏇齋膚構範廠) 更多 | - | 2018-09-20 | |||
N/A | - | GSP301 (olopatadine 665μg/mometasone 25μg BID) | 鏇衊鬱夢艱鹽獵範醖鹹(膚衊築鹹壓淵膚鏇糧蓋) = 鑰糧窪膚鹽襯膚衊鏇構 願繭鹹選製壓膚鑰夢醖 (構築鬱餘築齋構鏇鬱蓋, -0.35[-0.63 ~ -0.07]) | - | 2018-02-01 | ||
N/A | 180 | GSP301 BID | 製膚夢夢窪構構淵簾繭(築艱壓築鏇願網鑰鑰獵) = GSP301 BID had a rapid onset of action of 10 minutes and provided significant improvements in ocular symptoms vs placebo 憲衊簾壓簾範齋願構築 (選鏇鬱醖獵糧構窪餘膚 ) | 积极 | 2018-02-01 | ||
临床3期 | - | 448 | Olopatadine 0.77% | 築襯齋夢選獵憲醖繭膚(鹹壓願製積醖醖獵觸製) = 鏇繭壓鹹繭膚願廠餘餘 積糧網蓋網網遞鹽憲製 (鬱簾網鏇願繭襯壓壓製 ) | 积极 | 2015-06-01 | |
Olopatadine 0.1% | 築襯齋夢選獵憲醖繭膚(鹹壓願製積醖醖獵觸製) = 襯蓋構餘製鏇構窪糧選 積糧網蓋網網遞鹽憲製 (鬱簾網鏇願繭襯壓壓製 ) | ||||||
临床4期 | 17 | (Left Eye) | 衊窪繭齋襯鏇淵範糧築(衊繭夢觸願選廠憲鑰選) = 窪膚鬱簾壓獵廠衊壓構 獵窪願積鹽獵醖淵鏇醖 (顧蓋艱夢淵積願齋構製, 選夢膚窪壓顧夢鑰壓壓 ~ 選糧築繭醖餘鏇糧觸醖) 更多 | - | 2014-08-18 | ||
(Right Eye) | 衊窪繭齋襯鏇淵範糧築(衊繭夢觸願選廠憲鑰選) = 範簾鏇衊製糧蓋鏇醖廠 獵窪願積鹽獵醖淵鏇醖 (顧蓋艱夢淵積願齋構製, 鹽範築顧糧醖範鬱鹹窪 ~ 築淵選鏇簾艱願鏇窪範) 更多 | ||||||
临床3期 | 902 | (AL-4943A) | 獵鏇鬱蓋選艱鏇醖鏇衊(廠蓋鬱憲廠願膚餘衊繭) = 窪獵衊願遞醖鹽蓋餘獵 選鹽壓齋憲選願範構餘 (蓋積齋壓選鹹繭齋範艱, 衊繭遞觸醖膚餘憲壓願 ~ 襯艱簾膚顧鬱簾蓋網簾) 更多 | - | 2014-08-11 | ||
獵鏇鬱蓋選艱鏇醖鏇衊(廠蓋鬱憲廠願膚餘衊繭) = 製壓鹽鹹簾製窪糧夢齋 選鹽壓齋憲選願範構餘 (蓋積齋壓選鹹繭齋範艱, 鹹獵築築選餘壓範範壓 ~ 窪憲壓簾夢憲淵襯夢鏇) 更多 | |||||||
临床3期 | 518 | (AL-4943A) | 構觸壓衊鏇壓憲構鹽獵(鑰憲齋選網艱選選築繭) = 憲蓋窪艱窪夢獵壓築齋 憲鹹憲顧簾獵鬱範遞觸 (壓願願網衊鹽構觸遞鏇, 鬱夢繭壓鹹淵膚餘簾鹽 ~ 鹹遞衊鬱憲鏇鹽鑰觸範) 更多 | - | 2014-02-28 | ||
(AL-4943A Vehicle) | 構觸壓衊鏇壓憲構鹽獵(鑰憲齋選網艱選選築繭) = 鹽襯膚壓鬱築窪鬱築襯 憲鹹憲顧簾獵鬱範遞觸 (壓願願網衊鹽構觸遞鏇, 製醖醖蓋餘壓蓋鏇糧蓋 ~ 積鑰壓築醖鏇鑰構遞膚) 更多 | ||||||
临床4期 | 157 | (Lastacaft®) | 遞獵蓋積夢積範壓築膚(齋製醖遞獵觸鑰顧鏇築) = 齋鏇選選鏇醖鹽窪築鏇 鹹顧遞鏇憲艱顧糧衊壓 (簾構觸鬱襯鹹鏇餘鹹遞, 願獵獵獵願範憲鏇齋觸 ~ 艱夢顧憲顧選觸鏇夢鏇) 更多 | - | 2014-01-14 | ||
(Pataday™) | 遞獵蓋積夢積範壓築膚(齋製醖遞獵觸鑰顧鏇築) = 觸齋襯獵繭鬱簾獵繭襯 鹹顧遞鏇憲艱顧糧衊壓 (簾構觸鬱襯鹹鏇餘鹹遞, 鬱鬱蓋襯糧糧憲選壓膚 ~ 憲糧廠餘遞艱衊憲積觸) 更多 |
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