Delving into the Latest Updates on Dexibuprofen with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(+)-(S)-p-isobutylhydratropic acid, (2S)-2-(4-isobutylphenyl)propanoic acid, (S)-α-methyl-4-(2-methylpropyl)benzeneacetic acid

+ [17]

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesSkin and Musculoskeletal Diseases+ [1]

Active Indication

InflammationHeadacheBack Pain+ [7]

Inactive Indication

Acute PainAnalgesiaAnesthesia+ [1]

Originator Organization-

Active Organization

Overseas Pharmaceuticals Ltd.

Gebro Pharma GmbH

Beijing Join Chain Medicine Co., Ltd.

+ [2]

Inactive Organization

Aponia Laboratories, Inc.

Drug Highest PhaseApproved

First Approval Date

CH (28 Apr 1998),

Rheumatic Diseases

RegulationPriority Review (CN)

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Structure

Molecular FormulaC13H18O2

InChIKeyHEFNNWSXXWATRW-JTQLQIEISA-N

CAS Registry51146-56-6

The main purpose of the study is to evaluate the pharmacokinetic differences between JC002 and the control formulation in the postprandial state and the effect of a high-fat meal on pharmacokinetics. The secondary purpose of the study is to study the safety of the test formulation and the control formulation in healthy adult subjects.

Start Date24 Jul 2024

Sponsor / Collaborator

Beijing Jiacheng Biomedical Technology Development Co., Ltd

CTR20240968 / Active, not recruitingNot Applicable

JC002比较药代动力学临床试验

[Translation] JC002 comparative pharmacokinetic clinical trial

主要研究目的：评价空腹状态下JC002药代动力学的特性。次要研究目的：评价JC002服用口感与已上市对照制剂是否存在差异；并观察JC002在健康成人受试者中的安全性。

[Translation]

The main purpose of the study is to evaluate the pharmacokinetic characteristics of JC002 in the fasting state. The secondary purpose of the study is to evaluate whether the taste of JC002 is different from that of the marketed control preparation; and to observe the safety of JC002 in healthy adult subjects.

Start Date10 Apr 2024

Sponsor / Collaborator

Beijing Jiacheng Biomedical Technology Development Co., Ltd

CTR20231623 / Active, not recruitingNot Applicable

JC001生物等效性试验（高剂量组）

[Translation] JC001 bioequivalence study (high dose group)

验证高剂量JC001与800mg布洛芬注射液BE等效

[Translation]

Verify the BE equivalence between high-dose JC001 and 800mg ibuprofen injection

Start Date25 Jun 2023

Sponsor / Collaborator

Beijing Join Chain Medicine Co., Ltd.

[+1]

100 Clinical Results associated with Dexibuprofen

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100 Translational Medicine associated with Dexibuprofen

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100 Patents (Medical) associated with Dexibuprofen

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312

Literatures (Medical) associated with Dexibuprofen

01 Nov 2024·International Journal of Biological Macromolecules

Ionic liquid supported hydrogel–lipase biocatalytic systems in asymmetric synthesis of enantiomerically pure S-ibuprofen

Article

Author: Jesionowski, Teofil ; Szada, Daria ; Biadasz, Andrzej ; Degórska, Oliwia ; Zdarta, Jakub ; Nghiem, Long Duc ; Fu, Qiang

Novel hydrogel biocatalysts with immobilized lipase, stabilized by ionic liquids (ILs) of different hydrophobicity, were synthesized and evaluated. Variations of the time of immobilization and ratio of substrates during hydrogel synthesis were considered to obtain the most stable biocatalyst with the highest activity. Physicochemical characterization proved the success of the hydrogel synthesis and enzyme deposition on the surface of the support. Nevertheless, the key objective was to produce a biocatalyst for further application in ibuprofen methyl ester resolution, with the aim of obtaining an enantiomerically pure product. The hydrogel biocatalysts obtained in the presence of 5 wt% ILs after 8 h of immobilization achieved the highest activity recovery of 62 %. After 10 reaction cycles, enzymatic activity was still above 60 %, and the negative effect of pH and temperature on the activity of immobilized lipase was much lower than in the case of the free enzyme. After application of the catalyst in the resolution of ibuprofen methyl ester, the enantiomeric excess and conversion rate of the process were obtained for the dynamic kinetic resolution in isooctane. A conversion rate of 95 % was achieved due to the stabilization of the biocatalyst with IL and its resulting high catalytic activity. The study thus provides the pharmaceutical industry with a new potential approach with a strong scientific foundation.

13 Sep 2024·Pharmaceutical Development and Technology

Dexibuprofen enteric film-coated tablets: design, characterization and pharmacokinetic analysis in human volunteers

Article

Author: Dawaba, Hamdy M. ; Hanif, Anas M. ; Alam, Shazia ; Dawaba, Aya M. ; Aslam, Nousheen ; Rehman, Abdul ; Bushra, Rabia ; Sayed, Ossama M.

OBJECTIVEThis study aimed to develop a stable and scalable enteric film-coated tablet for the gastric irritant dexibuprofen.METHODSUtilizing direct compression with super-disintegration (crospovidone), the optimal core batches were coated with Opadry white seal coat and enterically coated with Eudragit^®L100 with pigment (Talc), demonstrating a 12% weight increase; release and integrity were assessed using specific pH buffers and SEM, with stability testing confirming a six-month shelf life at 40 °C and 75% RH.RESULTSThe optimized formulation achieved 99.87% release in phosphate buffer within 60 min, maintained integrity for 120 min in acidic conditions, and exhibited superior bioavailability compared to Innovifen with relative bioavailability ≈of 121% and elevated C_max (18.35 µg/ml compared to 11.1 µg/ml).CONCLUSIONThese results highlight the potential of this formulation to enhance patient safety and efficacy through delayed enteric technology and fast intestinal release.

01 Aug 2024·Journal of Pharmaceutical and Biomedical Analysis

Transacylation and hydrolysis of the acyl glucuronides of ibuprofen and its α-methyl-substituted analogues investigated by 1H NMR spectroscopy and computational chemistry: Implications for drug design

Article

Author: Stachulski, Andrew V ; Athersuch, Toby J ; Richards, Selena E ; Johnson, Caroline H ; Nicholson, Jeremy K ; Wilson, Ian D ; Lindon, John C ; Bradshaw, Peter R

Drugs and drug metabolites containing a carboxylic-acid moiety can undergo in vivo conjugation to form 1-β-O-acyl-glucuronides (1-β-O-AGs). In addition to hydrolysis, these conjugates can undergo spontaneous acyl migration, and anomerisation reactions, resulting in a range of positional isomers. Facile transacylation has been suggested as a mechanism contributing to the toxicity of acyl glucuronides, with the kinetics of these processes thought to be a factor. Previous ¹H NMR spectroscopic and HPLC-MS studies have been conducted to measure the degradation rates of the 1-β-O-AGs of three nonsteroidal anti-inflammatory drugs (ibufenac, R-ibuprofen, S-ibuprofen) and a dimethyl-analogue (termed here as "bibuprofen"). These studies have also determined the relative contributions of hydrolysis and acyl migration in both buffered aqueous solution, and human plasma. Here, a detailed kinetic analysis is reported, providing the individual rate constants for the acyl migration and hydrolysis reactions observed in buffer for each of the 4 AGs, together with the overall degradation rate constants of the parent 1-β-O-AGs. Computational modelling of the reactants and transition states of the transacylation reaction using density functional theory indicated differences in the activation energies that reflected the influence of both substitution and stereochemistry on the rate of transacylation/hydrolysis.

100 Deals associated with Dexibuprofen

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External Link

KEGG	Wiki	ATC	Drug Bank
D03715	Dexibuprofen	M01AE14	DB09213

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Inflammation	KR	Gebro Pharma GmbH	31 Dec 2007
Headache	AR	-	16 Apr 2007
Back Pain	AR	-	02 Apr 2007
Musculoskeletal Pain	AR	-	01 Apr 2007
Dysmenorrhea	GB	-	14 Mar 2007
Fever	CN	Hubei Biocause Heilen Pharmaceutical Co., Ltd.	01 Jan 2001
Osteoarthritis	CN	-	01 Jan 2001
Rheumatoid Arthritis	CN	-	01 Jan 2001
Pain	CH	-	21 May 1998
Rheumatic Diseases	CH	-	28 Apr 1998

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Anesthesia	Phase 1	CN	Beijing Join Chain Medicine Co., Ltd.	16 Nov 2020
Anesthesia	Phase 1	CN	Zhongshan Union Weihua Pharmaceutical Co. Ltd.	16 Nov 2020
Analgesia	Phase 1	CN	Zhongshan Union Weihua Pharmaceutical Co. Ltd.	25 Jul 2018
Analgesia	Phase 1	CN	Beijing Join Chain Medicine Co., Ltd.	25 Jul 2018
Fever	Phase 1	CN	Beijing Join Chain Medicine Co., Ltd.	25 Jul 2018
Fever	Phase 1	CN	Zhongshan Union Weihua Pharmaceutical Co. Ltd.	25 Jul 2018
Acute Pain	Phase 1	US	Aponia Laboratories, Inc.	12 Jan 2018
Myalgia	Phase 1	US	Aponia Laboratories, Inc.	01 Jan 2015

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03852459 (CTgov)	Phase 2	Acute Pain \| Myalgia	251	S-Ibuprofen (Active Arm)	vjkqyrcilo(nnydjvxvql) = lmzjsmjaig kpecunnsmr (dgryojqlti, uidgcgoerj - iewmbywqrj) View more	-	25 Jan 2022
				Vehicle (Placebo Arm)	vjkqyrcilo(nnydjvxvql) = rkvcipugtg kpecunnsmr (dgryojqlti, oxsbihqkob - upmrqdpcwv) View more