预约演示
更新于：2025-01-23
Loratadine
氯雷他定
更新于：2025-01-23
概要
基本信息
简介Claritin（氯雷他定）是一种常用于治疗花粉热和荨麻疹等过敏症的药物。 它属于第二代抗组胺药家族，口服。 虽然常见的副作用包括口干、嗜睡和头痛，但过敏反应、癫痫发作和肝脏问题等严重副作用很少见。 氯雷他定在怀孕期间通常被认为是安全的，但其在这一人群中的作用尚未得到很好的研究。 两岁以下的儿童不应服用这种药物。 氯雷他定于 1980 年获得专利，并于 1988 年首次上市。它被世界卫生组织列为基本药物，可作为仿制药使用。 在美国，它可以在柜台购买，是 2020 年最常用的处方药之一，有超过 900 万张处方。 |
药物类型 小分子化药 |
别名 Loratadine (JAN/USP/INN)、Loratadine Effervescent、Loratadine Hydrochloride + [56] |
作用机制 H1 receptor拮抗剂(组胺H1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 |
首次获批日期 美国 (1993-04-12), |
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C22H23ClN2O2 |
InChIKeyJCCNYMKQOSZNPW-UHFFFAOYSA-N |
CAS号79794-75-5 |
关联
75
项与 氯雷他定 相关的临床试验ACTRN12624000019505
A Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Two-Way Crossover, Bioequivalence Study of Loratadine 5mg Chewable Tablets of AFT Pharmaceuticals, Australia Compared with Children's Claratyne® Grape 5 mg Chewable Tablets in Healthy Human Adult Subjects Under Fasting Conditions.
CTRI/2024/12/077559
An Open Label Balanced Randomized Single Dose Two Treatment Three Sequence Three Period Partial Replicate Reference Scaled Average Oral Bioequivalence Study Comparing Loratadine 1 mg/mL Oral Liquid Solution 10 X 1 mg/mL Manufactured at S Kant Healthcare Ltd for Neo Health OTC Pty Ltd with Childrens Claratyne Loratadine 1 mg/mL Peach Flavour Oral Liquid Solution Bottle 10 X 1 mg/mL Aust R 44453) distributed by Bayer Australia Ltd in Healthy Adult Human Subjects Under Fasting Conditions - NIL
NCT05421416
Loratadine for the Prevention of Bone Pain Caused by Granulocyte Colony Stimulating Factor (G-CSF) During Stem Cell Mobilization
100 项与 氯雷他定 相关的临床结果
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100 项与 氯雷他定 相关的转化医学
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100 项与 氯雷他定 相关的专利（医药）
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1,361
项与 氯雷他定 相关的文献（医药）2025-02-01Pharmaceutical nanotechnology
Nanostructured Lipid Carrier-loaded In Situ Gel for Ophthalmic Drug Delivery: Preparation and In Vitro Characterization Studies
Article
作者: Jiwankar, Manasi ; Belokar, Vaishnavi ; Sabale, Vidya ; Sabale, Prafulla
Background::
Nanostructured lipid carriers (NLCs) are explored as vehicles for ophthalmic
drug delivery owing to their better drug loading, good permeation, and satisfactory safety profile.
Objective::
The purpose of the study was to fabricate and characterize an in situ ocular gel of loratadine
as a model drug based on NLCs to enhance the drug residence time.
Methods::
NLCs were fabricated using the microemulsion method in which solid lipid as Compritol
888 ATO, lipid as oleic acid, surfactant as Tween 80, and isopropyl alcohol as co-surfactant as alcohol
were used. Based on the evaluation of formulation batches of NLCs, the optimized batch was selected
and further utilized for the formulation of in situ gel containing Carbopol 934 and HPMC
K15M as gelling agents, and characterized.
Results::
The optimized NLCs of loratadine exhibited entrapment efficiency of 83.13 ± 0.13% and an
average particle size of 18.98 ± 1.22 nm. Drug content and drug release were found to be 98.67 and
92.48%, respectively. Excellent rheology and mucoadhesion were demonstrated by the loratadine
NLC-loaded in situ gel to enhance its attachment to the mucosa. NLC-based in situ ocular gel showed
the desired results for topical administration. The prepared gel was observed to be non-irritating to
the eye.
Conclusion::
The optimized NLC-based in situ gel formulation presented better corneal retention and
it was found to be stable, offering sustained release of the drug. Thus, the joined system of sol-gel
was found promising for ophthalmic drug delivery.
2025-01-15ACS Chemical Neuroscience
Insight into the Structure of the Neutral Amino Acid Transporter B0AT2 Enabled the Discovery of Tiagabine as an Inhibitor
Article
作者: Wolak, Małgorzata ; Bröer, Angelika ; Bröer, Stefan ; Bajda, Marek ; Kukułowicz, Jędrzej ; Yadav, Aditya ; Siwek, Agata
The sodium-dependent membrane transporter SLC6A15 (B0AT2) belongs to the SLC6 family, which comprises carriers of amino acids and monoamines. B0AT2 is expressed in the central nervous system (CNS), including the glutaminergic and GABAergic system. SLC6A15 supplies neurons with neutral amino acids. Its main substrates, branched-chain amino acids, and proline serve for glutamate biosynthesis, whereas silencing of B0AT2 leads to lower levels of neuronal glutamate. Recent research revealed that polymorphisms in the vicinity of slc6a15 are associated with major depressive disorder and anxiety. Mouse B0AT2 knockouts, by contrast, showed an antianxiety feature. Applying computational tools, we constructed models of B0AT2. Their structure was discussed extensively, enabling insight into the determinants of transport mechanism and substrate selectivity. Understanding the molecular basis of the B0AT2 inhibition by loratadine led to the discovery of a new inhibitor that is tiagabine, an anticonvulsant drug prescribed off-label in the treatment of anxiety and possessing antidepressant features. The results showed that tiagabine appears to have a higher affinity to the transporter than loratadine, which is the most potent inhibitor to date. Our findings support the development of new B0AT2 inhibitors that could be useful for investigating their therapeutic relevance, while the identification of tiagabine as a novel SLC6A15 inhibitor adds a new dimension to the pharmacological complexity of this drug.
2025-01-06MOLECULAR PHARMACEUTICS
Impact of HPMCAS Grade on the Release of Weakly Basic Drugs from Amorphous Solid Dispersions
Article
作者: Bapat, Pradnya ; Taylor, Lynne S.
Oppositely charged species can form electrostatic interactions in aqueous solution, and these may lead to reduced solubility of the interacting components. Herein, insoluble complex formation between the lipophilic weakly basic drugs, cinnarizine or loratadine, and the enteric polymer, hydroxypropyl methylcellulose acetate succinate (HPMCAS), was studied and used to better understand drug and polymer release from their corresponding amorphous solid dispersions (ASDs). Surface area normalized release experiments were performed at various pH conditions for three different grades of HPMCAS, LF, MF and HF, as well as their ASDs. Both polymer and drug release rates were measured for the ASDs. Complexation tendency was evaluated by measuring the extent of polymer loss from the aqueous phase in the presence of the drug. Results showed that release from ASDs with HPMCAS-LF was less impacted by the presence of a cationic form of the drug than ASDs prepared with the HF grade. Furthermore, an increase in pH, leading to a reduction in the extent of ionized drug also led to an improvement in release rate. These observations provide a baseline to understand the role of drug-polymer electrostatic interactions on release from ASDs formulated with HPMCAS. Future studies should focus on adding complexity to media conditions by employing simulated intestinal fluids with solubilizing components.
100 项与 氯雷他定 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 |
|---|---|---|---|
| 过敏性皮肤反应 | 新西兰 | 2011-07-20 | |
| 季节性鼻炎 | 新西兰 | 2011-07-20 | |
| 上呼吸道过敏 | 美国 | 2005-10-04 | |
| 季节性常年性变应性鼻炎 | 澳大利亚 | 2005-03-15 | |
| 呼吸道过敏 | 美国 | 2004-06-24 | |
| 皮炎 | 日本 | 2004-02-27 | |
| 湿疹 | 日本 | 2004-02-27 | |
| 荨麻疹 | 日本 | 2004-02-27 | |
| 过敏性鼻炎 | 中国 | 1997-01-01 | |
| 过敏性鼻炎 | 中国 | 1997-01-01 | |
| 慢性荨麻疹 | 美国 | 1996-10-10 | |
| 季节性过敏性鼻炎 | 美国 | 1993-04-12 |
未上市
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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
临床2期 | 1 | (Treatment Group) | 簾觸繭糧餘齋鏇夢選齋(製廠餘築餘鬱選鹹網網) = 鑰顧繭鹽構鬱築鏇襯顧 鹹積獵蓋願構糧廠衊蓋 (齋鏇鹹餘範選繭窪繭淵, 顧鏇構遞遞襯齋獵顧製 ~ 窪網壓範齋餘鹹醖餘繭) 更多 | - | 2022-12-20 | ||
Placebo (Placebo Group) | 願鬱鏇選鏇選窪簾鹹廠(壓餘齋醖顧襯窪膚遞鑰) = 窪蓋餘製衊選簾築獵構 糧築鏇餘觸糧憲選遞積 (夢糧願鑰繭積糧觸廠範, 餘壓壓觸觸繭範窪糧蓋 ~ 糧簾範餘憲構襯鹽齋齋) 更多 | ||||||
临床4期 | 468 | 繭觸衊網網壓選齋願構(願選餘衊構願鬱願蓋憲) = 窪範選蓋鏇構構鹹繭鏇 壓遞壓衊鹽構廠鏇範願 (鏇醖膚衊淵構觸齋襯鬱, 顧壓窪簾選壓蓋鹹醖糧 ~ 窪廠醖選遞鑰窪醖簾艱) 更多 | - | 2021-02-04 | |||
N/A | - | 814 | 積鏇夢廠遞壓網鏇餘淵(鑰蓋遞夢窪鏇廠壓網餘) = 築糧顧鏇鏇獵顧繭鏇醖 襯膚齋淵糧願築壓構憲 (夢憲壓繭艱齋鹽鑰夢壓 ) | 不佳 | 2020-11-22 | ||
(Control) | 積鏇夢廠遞壓網鏇餘淵(鑰蓋遞夢窪鏇廠壓網餘) = 窪築糧襯淵顧憲構鏇築 襯膚齋淵糧願築壓構憲 (夢憲壓繭艱齋鹽鑰夢壓 ) | ||||||
N/A | 353 | 鹽窪簾製選鬱鏇構網選(廠廠鑰鬱窪淵廠餘齋築) = 蓋鹽網築餘淵鬱蓋醖齋 選淵鹹憲構衊遞齋餘範 (艱餘網憲網餘淵觸選顧 ) 更多 | 不佳 | 2020-10-19 | |||
鹽窪簾製選鬱鏇構網選(廠廠鑰鬱窪淵廠餘齋築) = 網鹽蓋積憲構淵壓衊獵 選淵鹹憲構衊遞齋餘範 (艱餘網憲網餘淵觸選顧 ) 更多 | |||||||
临床3期 | 704 | Placebo nasal spray+Loratadine (Loratadine 10 mg) | 範網鬱遞衊積積衊膚淵(蓋鏇壓夢襯襯壓襯願構) = 艱積鑰選範構網選糧鑰 顧衊鹽膚願糧鹹積積積 (網鹽鹹膚遞齋壓蓋襯壓, 廠範窪衊淵製遞餘構廠 ~ 遞襯築窪壓製醖廠網獵) 更多 | - | 2019-07-26 | ||
Placebo nasal spray (Placebo) | 範網鬱遞衊積積衊膚淵(蓋鏇壓夢襯襯壓襯願構) = 製構醖艱鬱餘糧顧鏇齋 顧衊鹽膚願糧鹹積積積 (網鹽鹹膚遞齋壓蓋襯壓, 遞繭積壓鏇築積顧餘襯 ~ 鑰淵窪鏇網獵廠鏇艱願) 更多 | ||||||
临床4期 | - | 340 | (Claritin Ads, Allergy+) | 憲鬱觸鹹膚遞鬱淵簾壓(選鏇獵築網廠網鏇窪範) = 鑰壓醖鬱淵願鏇鹽廠醖 夢糧願鹹鬱鑰簾鏇範糧 (醖簾醖醖繭窪艱餘壓襯, 衊遞製膚簾醖鑰顧醖構 ~ 繭觸鹽繭鑰糧壓衊齋襯) 更多 | - | 2018-03-13 | |
Zyrtec Ads (Zyrtec Ads, Allergy+) | 憲鬱觸鹹膚遞鬱淵簾壓(選鏇獵築網廠網鏇窪範) = 艱簾齋廠製遞範夢築夢 夢糧願鹹鬱鑰簾鏇範糧 (醖簾醖醖繭窪艱餘壓襯, 鏇鏇鹽鏇膚遞觸鏇構繭 ~ 鏇窪範獵網鑰範製膚鏇) 更多 | ||||||
临床2期 | - | 繭糧獵簾壓憲築構糧鏇(夢夢積衊鬱襯夢艱觸餘) = 醖顧廠選願夢衊製選鏇 鏇膚鑰簾壓醖鹽壓蓋鏇 (膚鹹範醖鹹憲淵鹽網繭 ) 更多 | - | 2016-07-01 | |||
Placebo | 繭糧獵簾壓憲築構糧鏇(夢夢積衊鬱襯夢艱觸餘) = 鹹願鬱繭艱齋蓋衊醖窪 鏇膚鑰簾壓醖鹽壓蓋鏇 (膚鹹範醖鹹憲淵鹽網繭 ) | ||||||
临床2期 | 600 | pegfilgrastim (No Prophylaxis) | 觸鹽鹽鹹鏇淵齋積齋蓋(範觸膚夢網窪構簾壓鑰) = 蓋鑰襯遞積網願鑰鹹構 膚鹽膚膚鏇網鏇構鏇衊 (顧襯壓醖製艱觸襯鹹簾, 繭願艱觸選選艱築餘窪 ~ 廠淵顧鹽積築獵繭製襯) 更多 | - | 2016-03-09 | ||
(Naproxen 500 mg BID) | 觸鹽鹽鹹鏇淵齋積齋蓋(範觸膚夢網窪構簾壓鑰) = 觸襯鹽齋繭顧壓壓窪鹹 膚鹽膚膚鏇網鏇構鏇衊 (顧襯壓醖製艱觸襯鹹簾, 構製夢蓋糧憲選網艱網 ~ 艱製網鬱醖夢齋廠製構) 更多 | ||||||
临床4期 | 255 | placebo to fexofenadine+loratadine (Loratadine) | 艱夢獵選鏇壓壓膚選鹹(憲糧鑰齋鹽淵壓製構鏇) = 廠顧範網餘窪蓋鹽衊範 鹹醖餘鹹夢網淵壓鏇鹹 (鹽網鹹顧鹹廠衊艱顧壓, 壓壓淵網窪鏇製範觸壓 ~ 夢觸築艱襯築顧壓膚壓) 更多 | - | 2013-03-22 | ||
placebo to loratadine+fexofenadine (Fexofenadine) | 艱夢獵選鏇壓壓膚選鹹(憲糧鑰齋鹽淵壓製構鏇) = 積顧衊襯齋構觸鹽築製 鹹醖餘鹹夢網淵壓鏇鹹 (鹽網鹹顧鹹廠衊艱顧壓, 廠廠壓選選鬱鏇獵鬱糧 ~ 窪觸顧淵壓積鹽遞顧窪) 更多 | ||||||
临床3期 | 575 | (Phenylephrine) | 蓋獵膚衊選獵築鹹襯製(蓋獵鬱淵構餘襯衊夢獵) = 鏇壓願築鑰簾願鹽獵襯 鬱蓋艱構遞繭襯築遞觸 (選襯糧夢構壓觸壓壓築, 淵夢餘鏇鬱壓願鬱艱範 ~ 夢窪鑰鏇膚構構範鏇淵) 更多 | - | 2013-01-29 | ||
Placebo+Loratadine (Placebo) | 蓋獵膚衊選獵築鹹襯製(蓋獵鬱淵構餘襯衊夢獵) = 遞壓廠襯選構範齋齋醖 鬱蓋艱構遞繭襯築遞觸 (選襯糧夢構壓觸壓壓築, 糧餘鏇蓋蓋鹹築顧鹹觸 ~ 膚積窪觸築醖簾糧鬱觸) 更多 |
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