更新于：2024-09-21
Fexofenadine Hydrochloride
盐酸非索非那定
更新于：2024-09-21
概要
基本信息
简介非索非那定于1996年3月获得FDA批准，是一种令人费解的小分子药物，可作为H1受体拮抗剂。该药物阻碍组胺在H1受体的作用，减少呼吸超敏反应，荨麻疹，皮炎，瘙痒和其他皮肤病。非索非那定主要用于这些疾病，有助于缓解其症状。赛诺菲是非索非那定的神秘鼻祖组织，已在临床上得到广泛应用。尽管其广泛使用，但这种药物的具体作用机制尚不清楚。然而，非索非那定是治疗过敏和相关疾病的重要武器，尽管它可能导致嗜睡和口干以及其他副作用。非索非那定副作用的可变性和不精确的作用方式突出了进一步研究以充分理解药物作用机制的必要性。 |
药物类型 小分子化药 |
别名 Allegra 5%、Fexofenadine hydrochloride (JP17/USP)、Fexofenading Hydrochloride + [23] |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 英国 (1996-03-11), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C32H40ClNO4 |
InChIKeyRRJFVPUCXDGFJB-UHFFFAOYSA-N |
CAS号153439-40-8 |
关联
65
项与 盐酸非索非那定 相关的临床试验盐酸非索非那定干混悬剂人体生物等效性研究
Effect and Safety of Fexofenadine Hydrochloride vs Placebo in Patients With Acute Myocardial Infaction: A Randomized Clinical Trial
In vivo fasted-state bioequivalence study of Fexofenadine 120 mg tablet manufactured by Exir Pharmaceutical Co. compared to innovator product
100 项与 盐酸非索非那定 相关的临床结果
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100 项与 盐酸非索非那定 相关的转化医学
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100 项与 盐酸非索非那定 相关的专利（医药）
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165
项与 盐酸非索非那定 相关的文献（医药）2024-09-01JOURNAL OF PHARMACEUTICAL SCIENCES
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Fexofenadine
Article
作者: Abrahamsson, Bertil ; Langguth, Peter ; Polli, James E ; Parr, Alan ; Cristofoletti, Rodrigo ; Kambayashi, Atsushi ; Dressman, Jennifer ; Shah, Vinod P ; Selvasudha, N ; Charoo, Naseem A ; Mehta, Mehul ; Kath, Zahira Nala
In this monograph, the potential use of methods based on the Biopharmaceutics Classification System (BCS) framework to evaluate the bioequivalence of solid immediate-release (IR) oral dosage forms containing fexofenadine hydrochloride as a substitute for a pharmacokinetic study in human volunteers is investigated. We assessed the solubility, permeability, dissolution, pharmacokinetics, pharmacodynamics, therapeutic index, bioavailability, drug-excipient interaction, and other properties using BCS recommendations from the ICH, FDA and EMA. The findings unequivocally support fexofenadine's classification to BCS Class IV as it is neither highly soluble nor highly permeable. Further impeding the approval of generic equivalents through the BCS-biowaiver pathway is the reference product's inability to release ≥ 85 % of the drug substance within 30 min in pH 1.2 and pH 4.5 media. According to ICH rules, BCS class IV drugs do not qualify for waiving clinical bioequivalence studies based on the BCS, even though fexofenadine has behaved more like a BCS class I/III than a class IV molecule in pharmacokinetic studies to date and has a wide therapeutic index.
2024-03-13Chemical & pharmaceutical bulletin
Dissolution Profiles of Oral Disintegrating Tablet with Taste Masking Granule Polymer Coating in Biorelevant Bicarbonate Buffer
Article
作者: Sugano, Kiyohiko ; Higashino, Masaki
The current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra® as the reference formulation, and generic formulations A and B as the test formulations. Allegra®, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit® E, EUD-E), a basic polymer commonly used to mask the bitter taste of drugs. Both generic A and generic B have been known to be bioequivalent to Allegra®. The dissolution tests were conducted using a compendial paddle, with either bicarbonate (10 mM, pH 6.8) or phosphate buffer (25 mM, pH 6.8) as the dissolution media. A floating lid was employed to cover the surface of the bicarbonate buffer to prevent volatilization. Results indicated that in phosphate buffer, the dissolution profiles of Allegra and generic B significantly varied from that of generic A, whereas in the bicarbonate buffer, the dissolution profiles of Allegra, generic A, and generic B were comparable. These findings suggest that the use of bicarbonate buffer may offer a more precise prediction of human bioequivalence compared to phosphate buffer.
2024-02-01Georgian medical news
HISTOLOGICAL AND BIOCHEMICAL STUDY OF THE EFFECT OF FEXOFENADINE ON SALIVARY GLAND IN RATS.
Article
作者: Sarhat, E ; Mahmood, E ; Tawfeq, M ; Wadee, S
Fexofenadine is a newly introduced oral non-sedating agent used for allergic diseases. We sought to investigate the effects of the use of fexofenadine on the salivary gland of adult male albino rats. 30 adult male albino rats were classified randomly into 3 groups, as follows: Group A (control group) which consisted of 10 healthy rats. Group B (treated group) which consisted of 10 rats received FEX 5mg/kg/day, and Group C (treated group) which consisted of 10 rats received FEX 10mg/kg/day. Blood samples were obtained to assess serum levels of Thioredoxin reductase (TRX) and malondialdehyde (MDA). Salivary glands were removed and prepared for histological examination. This study showed that significantly (p<0.05) higher TRX and MDA levels were observed in group B and group C, compared to group A. The histological examination for salivary tissues revealed degenerative changes in serous cells of acini were present with deep pyknotic nuclei. Vacuolar cytoplasmic degeneration is also seen in other certain cells. Blood congestion was present in the intralobular blood vessels, particularly around the striated ducts. The glandular secretion duct contained mucus and serous secretion and the wall of the duct was surrounded by many WBCs with macrophage. Fexofenadine hydrochloride use induces remarkable histopathological changes with dose-dependent response and remarkably linked to elevation of oxidative stress markers.
100 项与 盐酸非索非那定 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 |
|---|---|---|---|
| 呼吸道过敏 | 美国 | 2011-01-24 | |
| 瘙痒 | 日本 | 2002-04-15 | |
| 慢性荨麻疹 | 美国 | 2000-02-25 | |
| 过敏性鼻炎 | 韩国 | 1998-05-04 | |
| 荨麻疹 | 澳大利亚 | 1997-01-10 | |
| 季节性过敏性鼻炎 | 英国 | 1996-03-11 |
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临床结果
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适应症
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临床3期 | 95 | (Arm A (Active-active)) | 獵廠襯餘網鬱憲選鑰夢(餘壓襯廠鏇構糧簾憲鏇) = 廠觸齋淵構糧壓壓衊餘 衊鏇築醖範遞鏇糧網壓 (獵鹹鏇遞壓壓築膚衊鹹, 蓋醖觸鹹壓獵鹹選鑰獵 ~ 觸鹽築蓋鑰遞簾糧醖鑰) 更多 | - | 2024-05-16 | ||
Placebo (Arm B (Placebo-active)) | 獵廠襯餘網鬱憲選鑰夢(餘壓襯廠鏇構糧簾憲鏇) = 獵鹹網簾鏇獵淵選衊襯 衊鏇築醖範遞鏇糧網壓 (獵鹹鏇遞壓壓築膚衊鹹, 鹹鏇構觸鏇窪鹽選築膚 ~ 餘網簾鹹淵廠製顧膚鑰) 更多 | ||||||
临床4期 | 152 | gout flare prophylaxis regimen+acetaminophen+methylprednisolone+fexofenadine+methotrexate+Pegloticase (Pegloticase + MTX) | 鹹艱鑰襯構鬱膚鹽餘廠(網構鹽蓋餘廠艱遞觸製) = 衊鏇鹹築鬱鑰遞鏇襯淵 糧鑰選蓋範衊鹽願鹹願 (獵鬱觸憲蓋鏇鏇鹽蓋製, 積鑰築齋廠積範鑰憲選 ~ 範願衊壓構繭廠構淵鑰) 更多 | - | 2022-05-16 | ||
(Pegloticase + Placebo) | 鹹艱鑰襯構鬱膚鹽餘廠(網構鹽蓋餘廠艱遞觸製) = 網網遞製淵鏇夢遞憲壓 糧鑰選蓋範衊鹽願鹹願 (獵鬱觸憲蓋鏇鏇鹽蓋製, 鹹壓衊築壓製襯獵積繭 ~ 艱鹽齋廠觸鹽窪鏇窪鹽) 更多 | ||||||
N/A | 145 | 製糧齋觸鏇顧襯廠壓廠(獵鏇餘膚選衊繭餘製鬱) = 膚夢鏇艱憲窪醖鏇繭餘 選鹽製餘積餘鹹衊壓遞 (積鑰鹹積積艱積簾構膚 ) 更多 | - | 2012-05-20 | |||
製糧齋觸鏇顧襯廠壓廠(獵鏇餘膚選衊繭餘製鬱) = 齋鹽衊鹹遞鬱憲淵鹹願 選鹽製餘積餘鹹衊壓遞 (積鑰鹹積積艱積簾構膚 ) 更多 | |||||||
N/A | - | Fexofenadine HCl 6 mg/mL Suspension | 鏇築獵醖網遞築憲顧簾(顧膚構鏇艱鏇願鑰獵鏇) = Ten treatment-emergent adverse events (TEAEs) occurred in seven subjects. No serious, one moderate intensity (pyrexia) and nine mild intensity TEAEs were reported. All TEAEs resolved without sequelae. 鹽壓製鬱衊鹹願築觸積 (鑰願遞蓋觸糧鬱網鹹憲 ) 更多 | 积极 | 2007-01-01 |
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