Delving into the Latest Updates on Flurbiprofen Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Flurbiprofen Cataplasms, Flurbiprofen sodium (USP), 氟吡洛芬钠

+ [4]

Target

COX-2

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesNervous System Diseases+ [1]

Active Indication

Ankylosing SpondylitisOsteoarthritisPain+ [1]

Inactive Indication

MiosisOsteoarthritis, Knee

Originator Organization

Allergan Ltd. (Ireland)

Active Organization

Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.

Inactive Organization

Beijing Tide Pharmaceutical Co., Ltd.Allergan, Inc.Mikasa Seiyaku Co. Ltd.

Drug Highest PhaseApproved

First Approval Date

US (31 Dec 1986),

Miosis

Regulation-

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Structure

Molecular FormulaC15H13FO2

InChIKeySYTBZMRGLBWNTM-UHFFFAOYSA-N

CAS Registry5104-49-4

View All Structures (2)

[Translation] A single-center, open, randomized, single-dose, two-period, two-sequence, crossover bioequivalence study was conducted to evaluate the bioequivalence of the test preparation, flurbiprofen gel patch (specification: 40 mg) and the reference preparation (Zepsilon®) (specification: 40 mg) in healthy adult subjects under topical conditions.

主要目的：研究外用条件下单次给予受试制剂氟比洛芬凝胶贴膏（规格：40 mg，乐明药业（苏州）有限公司）与参比制剂氟比洛芬凝胶贴膏（泽普思®，规格：40 mg；日本三笠制药株式会社）在健康受试者体内的药代动力学特征，评价外用条件下给予两种制剂的生物等效性。次要目的：1、研究受试制剂氟比洛芬凝胶贴膏（规格：40 mg）和参比制剂氟比洛芬凝胶贴膏（泽普思®）（规格：40 mg）在健康受试者中的安全性。 2、研究受试制剂氟比洛芬凝胶贴膏（规格：40 mg）和参比制剂氟比洛芬凝胶贴膏（泽普思®）（规格：40 mg）在健康受试者中的黏附性。

[Translation]

Primary objective: To study the pharmacokinetic characteristics of the test preparation flurbiprofen gel patch (specification: 40 mg, Leming Pharmaceutical (Suzhou) Co., Ltd.) and the reference preparation flurbiprofen gel patch (Zepce®, specification: 40 mg; Mikasa Pharmaceutical Co., Ltd., Japan) in healthy subjects after a single administration under topical conditions, and to evaluate the bioequivalence of the two preparations under topical conditions. Secondary objectives: 1. To study the safety of the test preparation flurbiprofen gel patch (specification: 40 mg) and the reference preparation flurbiprofen gel patch (Zepce®) (specification: 40 mg) in healthy subjects. 2. To study the adhesion of the test preparation flurbiprofen gel patch (specification: 40 mg) and the reference preparation flurbiprofen gel patch (Zepce®) (specification: 40 mg) in healthy subjects.

Start Date10 Nov 2021

Sponsor / Collaborator

Lindmik Pharmaceutical (Suzhou) Co., Ltd.

100 Clinical Results associated with Flurbiprofen Sodium

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100 Translational Medicine associated with Flurbiprofen Sodium

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100 Patents (Medical) associated with Flurbiprofen Sodium

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49

Literatures (Medical) associated with Flurbiprofen Sodium

01 Jun 2024·Asian Journal of Pharmaceutical Sciences

Advancing ophthalmic delivery of flurbiprofen via synergistic chiral resolution and ion-pairing strategies

Article

Author: Wang, Yuequan ; Liu, Tong ; Jiang, Qikun ; Ma, Zhining ; He, Huiyang ; Hou, Xiaohong

Flurbiprofen (FB), a nonsteroidal anti-inflammatory drug, is widely employed in treating ocular inflammation owing to its remarkable anti-inflammatory effects. However, the racemic nature of its commercially available formulation (Ocufen®) limits the full potential of its therapeutic activity, as the (S)-enantiomer is responsible for the desired anti-inflammatory effects. Additionally, the limited corneal permeability of FB significantly restricts its bioavailability. In this study, we successfully separated the chiral isomers of FB to obtain the highly active (S)-FB. Subsequently, utilizing ion-pairing technology, we coupled (S)-FB with various counter-ions, such as sodium, diethylamine, trimethamine (TMA), and l-arginine, to enhance its ocular bioavailability. A comprehensive evaluation encompassed balanced solubility, octanol-water partition coefficient, corneal permeability, ocular pharmacokinetics, tissue distribution, and in vivo ocular anti-inflammatory activity of each chiral isomer salt. Among the various formulations, S-FBTMA exhibited superior water solubility (about 1-12 mg/ml), lipid solubility (1< lg P_ow < 3) and corneal permeability. In comparison to Ocufen®, S-FBTMA demonstrated significantly higher in vivo anti-inflammatory activity and lower ocular irritability (such as conjunctival congestion and tingling). The findings from this research highlight the potential of chiral separation and ion-pair enhanced permeation techniques in providing pharmaceutical enterprises focused on drug development with a valuable avenue for improving therapeutic outcomes.

01 Jun 2024·European review for medical and pharmacological sciences

Efficacy and safety of topical NSAIDs combined with physiotherapy for frozen shoulder: a randomized controlled trial.

Article

Author: Zhou, C-Q ; Mao, X-Z ; Chen, G-Y ; Li, H

OBJECTIVEFrozen shoulder is a prevalent condition among individuals in their middle and later years. Invasive therapy has shown promising results in the treatment of frozen shoulders, but its widespread adoption has been hampered by high costs and the need for advanced medical technology. As a result, patients with frozen shoulders often turn to non-steroidal anti-inflammatory drugs (NSAIDs) for symptomatic relief. However, the oral administration of NSAIDs can lead to troublesome adverse effects on the gastrointestinal, cardiovascular, and urinary systems. In contrast, topical NSAIDs have gained attention for their excellent efficacy and lower adverse effects in various chronic pain conditions. Therefore, our study aimed to investigate the efficacy and safety of topical NSAIDs in improving pain and mobility among patients with frozen shoulders.PATIENTS AND METHODSA total of 108 patients experiencing moderate to severe pain and mobility impairment due to frozen shoulder were enrolled in this study. The participants were randomly assigned to either the experimental group (n=72) or the control group (n=36). The experimental group received daily treatment with the loxoprofen hydrogel patch (LOX-P) in addition to basic rehabilitation physiotherapy. The control group was treated with flurbiprofen cataplasm (FLU-C) twice a day, along with rehabilitation physiotherapy. The primary endpoint for evaluating the efficacy of the two patches was the Constant-Murley score (CMS). Clinical symptom data, adverse events, and patient satisfaction were also recorded.RESULTSAfter 14 days of treatment, the effective rate was 66.67% (n=48) in the experimental group and 41.67% (n=15) in the control group. The overall difference in the effective rates was 25.00% (95% CI=5.20-42.52; p=0.013). The safety profiles of the two topical agents were similar, with only a few adverse events reported.CONCLUSIONSThe loxoprofen hydrogel patch demonstrates a significant ability to alleviate shoulder pain and restore shoulder function in the treatment of frozen shoulder, with minimal adverse reactions. Chictr.org.cn ID: ChiCTR2100052375.

01 May 2024·Pharmaceutical Research

Nonlinear Pharmacokinetics of Topical Flurbiprofen Gel in a Phase I Study Among Chinese Healthy Adults

Article

Author: Liu, Feiyan ; Xiao, Wending ; Cheng, Zeneng ; Xie, Feifan ; Zhu, Zhihong

INTRODUCTIONPDX-02 (Flurbiprofen sodium) is a topical nonsteroidal anti-inflammatory drug in gel formulation for local analgesia and anti-inflammation. A Phase I clinical trial was conducted to assess the safety, tolerability, and pharmacokinetics of single and multiple doses of PDX-02 gel in Chinese healthy adults.METHODSThe trial comprised three parts: (1) a single-dose ascending study with three dose levels (0.5%, 1% to 2% PDX-02 gel) applied on a 136 cm² skin area; (2) a multiple-dose study with either 1% or 2% PDX-02 gel applied on a 136 cm² skin area for 7 consecutive days; and (3) a high dose group with 2% PDX-02 gel on an 816 cm² skin area and a frequent multiple dose group with 2% PDX-02 gel on a 272 cm² skin area four times a day for 7 consecutive days. The safety, tolerability and pharmacokinetics of the PDX-02 gel were evaluated in each part.RESULTSA total of sixty participants completed the trial, with all adverse events recovered and all positive skin reaction being transient and recovered. The overall absorption of topical PDX-02 gel was slow with a mean peak time exceeding 9 h. The elimination rate remained consistent between dose groups. A less-than-dose-proportional nonlinear pharmacokinetics relationship was observed within the studied dose range, and this is likely due to the autoinduction of skin first-pass metabolism.CONCLUSIONThe topical PDX-02 gel showed favorable safety and tolerability in both single and multiple dosing studies, with a less-than-dose-proportional nonlinear pharmacokinetics observed.

100 Deals associated with Flurbiprofen Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D02290	Flurbiprofen Sodium	M01AE09 M02AA19 R02AX01 S01BC04	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Ankylosing Spondylitis	CN	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998
Osteoarthritis	CN	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998
Pain	CN	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998
Rheumatoid Arthritis	CN	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998