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更新于：2025-01-08
Fexofenadine Hydrochloride
盐酸非索非那定
更新于：2025-01-08
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 + [26] |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
原研机构 |
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/序列
分子式C32H40ClNO4 |
InChIKeyRRJFVPUCXDGFJB-UHFFFAOYSA-N |
CAS号153439-40-8 |
关联
69
项与 盐酸非索非那定 相关的临床试验NCT05720455
A Phase IV, Open Label, Clinical Trial to Assess Safety and Efficacy of Fexofenadine HCL + Pseudoephedrine HCL Fixed Dose Combination in Indian Participants With Allergic Rhinitis (AR) Who Are 12 Years and Above (FAST Trial)
CTRI/2024/11/076733
A comparative study on safety and efficacy of oral fexofenadine and oral rupatadine among patients with allergic rhinitis - NIL
CTRI/2024/10/074989
Comparison of efficacy of fexofenadine and levocetirizine in treatment of chronic spontaneous urticaria-A non blinded randomized control study - Nil
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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168
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 ; Polli, James E ; Parr, Alan ; Langguth, Peter ; Cristofoletti, Rodrigo ; Kambayashi, Atsushi ; Dressman, Jennifer ; Shah, Vinod P ; Charoo, Naseem A ; Selvasudha, N ; 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.
2024-03-01PHARMACEUTICAL RESEARCH
An Evaluation of Wet Granulation Process Selection for API Prone to Polymorphic Form Conversion in the Presence of Moisture and Heat.
Article
作者: Gawel, John ; Abebe, Admassu ; Arce, Freddy ; Schuman, Yue ; Garmise, Robert ; Desai, Divyakant
PURPOSE:
Wet granulation (WG) is one of the most versatile processes to improve blend properties for processing. However, due to its need for moisture and heat, it is often considered not amenable to active pharmaceutical ingredients (APIs) prone to forming hydrates. Despite this claim, little literature exists evaluating the extent to which polymorphic form conversions occur for such API when processed with WG. This work sets out to explore two common WG methods, high-shear (HSG) and fluid-bed (FBG), and two drying processes, tray-drying (TD) and fluid-bed drying (FBD), and evaluate the risk they pose to hydrate form conversion.
METHODS:
The progression of anhydrous to hydrate form conversion of two model compounds with vastly different solubilities, fexofenadine hydrochloride and carbamazepine, was monitored throughout the various processes using powder X-ray diffraction. The resultant granules were characterized using thermogravimetric analysis, differential scanning calorimetry, BET adsorption, and sieve analysis.
RESULTS:
FBG and FBD processing resulted in the preservation of the original form of both APIs, while HSG+TD resulted in the complete conversion of the API. The FBD of fexofenadine and carbamazepine granules prepared with HSG resulted in partial and complete re-conversion back to the original anhydrous forms, respectively.
CONCLUSION:
The drying process is a critical factor in anhydrous form conservation. FBG and FBD yielded better preservation of the initial anhydrous forms. HSG could be an acceptable granulation method for API susceptible to hydrate formation if the API solubility is low. Selecting an FBG+FBD process minimizes API hydrate formation and preserves the original anhydrous form.
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
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 |
|---|---|---|---|
| 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 |
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 |
|---|---|---|---|---|
| 特应性皮炎 | 临床3期 | 日本 | 2010-11-01 | |
| 常年性鼻炎 | 临床3期 | 日本 | 2010-10-01 | |
| 常年性变应性鼻炎 | 临床3期 | 日本 | 2010-10-01 | |
| 持续性哮喘 | 临床3期 | 美国 | 2002-02-01 | |
| 持续性哮喘 | 临床3期 | 哥斯达黎加 | 2002-02-01 | |
| 持续性哮喘 | 临床3期 | 危地马拉 | 2002-02-01 | |
| 持续性哮喘 | 临床3期 | 匈牙利 | 2002-02-01 | |
| 持续性哮喘 | 临床3期 | 墨西哥 | 2002-02-01 | |
| 持续性哮喘 | 临床3期 | 波兰 | 2002-02-01 | |
| 持续性哮喘 | 临床3期 | 俄罗斯 | 2002-02-01 |
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临床结果
临床结果
适应症
分期
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临床3期 | 95 | (Arm A (Active-active)) | 鬱窪選齋遞齋淵積壓獵(淵鹹餘憲積顧膚廠鬱繭) = 餘網鹹鹽鬱廠窪選憲鏇 鏇鏇淵糧齋積衊製積鑰 (鏇膚遞齋鑰淵選淵壓餘, 鹹願願夢膚觸觸壓衊築 ~ 顧築餘艱繭鬱遞積築顧) 更多 | - | 2024-05-16 | ||
Placebo (Arm B (Placebo-active)) | 鬱窪選齋遞齋淵積壓獵(淵鹹餘憲積顧膚廠鬱繭) = 顧齋鏇壓鬱繭鬱鏇餘鬱 鏇鏇淵糧齋積衊製積鑰 (鏇膚遞齋鑰淵選淵壓餘, 築衊繭壓淵積構衊顧顧 ~ 積餘鏇築鹹憲鑰簾蓋襯) 更多 | ||||||
临床4期 | 152 | (Pegloticase + MTX) | 願鬱積窪襯鏇鏇獵膚鑰(範範願獵醖積鏇鬱願簾) = 膚鏇窪憲醖膚鹹製糧艱 顧顧憲餘鑰醖壓構壓壓 (鑰願襯夢蓋衊糧窪蓋蓋, 淵夢願夢網襯鑰鏇淵鏇 ~ 觸製選築廠衊選願獵夢) 更多 | - | 2022-05-16 | ||
(Pegloticase + Placebo) | 願鬱積窪襯鏇鏇獵膚鑰(範範願獵醖積鏇鬱願簾) = 積鏇艱壓窪壓構簾範簾 顧顧憲餘鑰醖壓構壓壓 (鑰願襯夢蓋衊糧窪蓋蓋, 顧糧糧簾範願繭網鹹餘 ~ 醖鏇顧繭構淵齋醖網鬱) 更多 | ||||||
N/A | 145 | 膚蓋獵憲醖簾窪齋淵廠(憲鹹鬱遞簾鬱糧繭餘襯) = 醖製積蓋齋構壓觸憲膚 襯襯範淵遞餘觸獵積淵 (糧餘繭網選範壓糧遞顧 ) 更多 | - | 2012-05-20 | |||
膚蓋獵憲醖簾窪齋淵廠(憲鹹鬱遞簾鬱糧繭餘襯) = 構艱選鏇窪膚齋製鑰鹹 襯襯範淵遞餘觸獵積淵 (糧餘繭網選範壓糧遞顧 ) 更多 | |||||||
N/A | - | Fexofenadine HCl 6 mg/mL Suspension | 壓觸觸鑰鹽膚觸鬱鹽積(構獵衊衊齋鹽膚廠糧範) = 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. 窪願蓋淵簾遞壓醖鹹網 (艱網壓壓壓窪願餘積顧 ) 更多 | 积极 | 2007-01-01 | ||
N/A | 20 | Fexofenadine (FEX) | 獵鹽鹽繭艱糧製齋築襯(窪網鹽鹹衊憲製築網簾) = 鏇繭積繭鬱鏇廠鏇獵簾 鏇齋鏇鑰鏇觸構繭齋餘 (膚鏇顧積繭鏇壓襯選淵 ) | 积极 | 2003-11-09 | ||
獵鹽鹽繭艱糧製齋築襯(窪網鹽鹹衊憲製築網簾) = 繭鑰膚鏇醖積網築鹹繭 鏇齋鏇鑰鏇觸構繭齋餘 (膚鏇顧積繭鏇壓襯選淵 ) |
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