Delving into the Latest Updates on Diclofenac Diethylamine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Diclofenac Diethylamine Emulgel, Diclofenac Diethylamine Gel, Diethylamine Diclofenate

+ [6]

Target

COXs

Action

inhibitors

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

InflammationPain

Inactive Indication

Ankle InjuriesArthralgiaContusions+ [2]

Originator Organization-

Active Organization-

Inactive Organization

GSK Plc

Novartis AGNOVARTIS CONSUMER HEALTH SCHWEIZ AG

+ [2]

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 1999),

InflammationPain

Regulation-

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Structure/Sequence

Molecular FormulaC18H22Cl2N2O2

InChIKeyZQVZPANTCLRASL-UHFFFAOYSA-N

CAS Registry78213-16-8

主要研究目的：考察空腹单次外用受试制剂双氯芬酸二乙胺乳胶剂（规格：1%[20g: 0.2g]，华益泰康药业股份有限公司生产，海南天盛保和生物科技有限公司提供）与参比制剂双氯芬酸二乙胺乳胶剂（商品名：扶他林®，规格：1%[20g: 0.2g]，GSK Consumer Healthcare Schweiz AG持证，GSK Consumer Healthcare SARL生产，海南天盛保和生物科技有限公司提供）在中国成年健康受试者体内的药代动力学特征，评价空腹状态下外用两种制剂的生物等效性。次要研究目的：评价空腹单次外用受试制剂和参比制剂在中国成年健康受试者中的安全性。

[Translation]

Main study objectives: To investigate the pharmacokinetic characteristics of the single-dose topical test preparation diclofenac diethylamine emulsion (specification: 1% [20g: 0.2g], produced by Huayi Taikang Pharmaceutical Co., Ltd., provided by Hainan Tiansheng Baohe Biotechnology Co., Ltd.) and the reference preparation diclofenac diethylamine emulsion (trade name: Voltaren®, specification: 1% [20g: 0.2g], licensed by GSK Consumer Healthcare Schweiz AG, produced by GSK Consumer Healthcare SARL, provided by Hainan Tiansheng Baohe Biotechnology Co., Ltd.) in healthy adult Chinese subjects, and to evaluate the bioequivalence of the two topical preparations in the fasting state. Secondary study objectives: To evaluate the safety of the single-dose topical test preparation and the reference preparation in healthy adult Chinese subjects.

Start Date25 Feb 2025

Sponsor / Collaborator

Hainan Tiansheng Baohe Biotechnology Co., Ltd.

NCT06731556

/ CompletedPhase 3IIT

Intranasal Diclofenac Sodium, Ibuprofen, and Paracetamol for Pain Relief After Pediatric Tonsillectomy

This study aims to evaluate the efficacy and safety of intranasal Diclofenac Sodium, intranasal Ibuprofen, and intranasal Paracetamol for pain control following tonsillectomy in pediatric patients.

Start Date15 Dec 2024

Sponsor / Collaborator

Bezmialem Vakif University

CTR20244293

/ Active, not recruitingNot Applicable

双氯芬酸二乙胺乳胶剂在中国健康人群中外用条件下单次给药的人体生物等效性临床试验方案

[Translation] A human bioequivalence clinical trial protocol for a single-dose topical administration of diclofenac diethylamine emulsion in healthy Chinese people

主要目的：以持证商为GSK Consumer Healthcare Schweiz AG 的双氯芬酸二乙胺乳胶剂，规格：1%（20g:0.2g，以双氯芬酸钠计））为参比制剂，以青岛百洋制药有限公司研发的双氯芬酸二乙胺乳胶剂（1%（20g:0.2g，以双氯芬酸钠计））为受试制剂，评价两种制剂在中国健康受试者中外用条件下的生物等效性。次要目的：1）评价受试制剂与参比制剂在中国健康受试者中的安全性；2）评价受试制剂与参比制剂对中国健康受试者的皮肤反应性。

[Translation]

Primary objective: To evaluate the bioequivalence of the two preparations under topical conditions in healthy Chinese subjects, using diclofenac diethylamine emulsion (specification: 1% (20g:0.2g, calculated as diclofenac sodium)) from GSK Consumer Healthcare Schweiz AG as the reference preparation and diclofenac diethylamine emulsion (1% (20g:0.2g, calculated as diclofenac sodium)) developed by Qingdao Baiyang Pharmaceutical Co., Ltd. as the test preparation. Secondary objectives: 1) To evaluate the safety of the test preparation and the reference preparation in healthy Chinese subjects; 2) To evaluate the skin reactivity of the test preparation and the reference preparation in healthy Chinese subjects.

Start Date13 Dec 2024

Sponsor / Collaborator

Qingdao Guofeng Group Huayang Parmaceutical Co. Ltd.

100 Clinical Results associated with Diclofenac Diethylamine

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100 Translational Medicine associated with Diclofenac Diethylamine

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100 Patents (Medical) associated with Diclofenac Diethylamine

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246

Literatures (Medical) associated with Diclofenac Diethylamine

01 Nov 2024·Current Molecular Medicine

Hypothesizing the Oleic Acid-Mediated Enhanced and Sustained Transdermal Codelivery of Pregabalin and Diclofenac Adhesive Nanogel: A Proof of Concept

Article

Author: Noor, Afeefa ; Kohli, Kanchan ; Rathee, Anjali ; Datta, Deepanjan ; Singh, Snigdha

:Pregabalin (PG) and diclofenac diethylamine (DEE) are anti-inflammatory molecules that are effective in relieving inflammation and pain associated with musculoskeletal disorders, arthritis, and post-traumatic pain, among others. Intravenous and oral delivery of these two molecules has their limitations. However, the transdermal route is believed to be an alternate viable option for the delivery of therapeutic molecules with desired physicochemical properties. To this end, it is vital to understand the physicochemical properties of these drugs, dosage, and strategies to enhance permeation, thereby surmounting the associated constraints and concurrently attaining a sustained release of these therapeutic molecules when administered in combination. The present work hypothesizes the enhanced permeation and sustained release of pregabalin and diclofenac diethylamine across the skin, entrapped in the adhesive nano-organogel formulation, including permeation enhancers. The solubility studies of pregabalin and diclofenac diethylamine in combination were performed in different permeation enhancers. Oleic acid was optimized as the best permeation enhancer based on in vitro studies. Pluronic organogel containing pregabalin and diclofenac diethylamine with oleic acid was fabricated. Duro-Tak® (87-2196) was added to the organogel formulation as a pressure-sensitive adhesive to sustain the release profile of these two therapeutic molecules. The adhesive organogel was characterized for particle size, scanning electron microscopy, and contact angle measurement. The HPLC method developed for the quantification of the dual drug showed a retention time of 3.84 minutes and 9.69 minutes for pregabalin and diclofenac, respectively. The fabricated nanogel adhesive formulation showed the desired results with particle size and contact angle of 282 ± 57 nm and ≥120⁰, respectively. In vitro studies showed the percentage cumulative release of 24.90 ± 4.65% and 33.29 ± 4.81% for pregabalin and diclofenac, respectively. In order to accomplish transdermal permeation, the suggested hypothesis of fabricating PG and DEE nano-organogel in combination with permeation enhancers will be a viable drug delivery method. In comparison to a traditional gel formulation, oleic acid as a permeation enhancer increased the penetration of both PG and DEE from the organogel formulation. Notably, the studies showed that the use of pressure-sensitive adhesives enabled the sustained release of both PG and DEE.Therefore, the results anticipated the hypothesis that the transdermal delivery of adhesive PG and DEEbased nanogel across the human skin can be achieved to inhibit inflammation and pain.

01 Sep 2024·Journal of Drug Delivery Science and Technology

In vitro evaluation of ethyl cellulose and polyvinyl pyrrolidone composite nanofibers for transdermal delivery of diclofenac diethylamine

Author: Abbaspour, Mohammad Reza ; Hatami, Hooman ; Nokhodchi, Ali ; Kariznavi, Elnaz ; Akhgari, Abbas ; Sadeghi, Fatemeh ; Garekani, Hadi Afrasiabi

Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prominent painkiller and anti-inflammatory drugs with gastrointestinal (GI) adverse effects.Transdermal drug delivery systems (TDDS) could overcome GI adverse effects associated with oral ingestion of NSAIDs as well as maintaining a prolonged release of the drug.The main aim of this study was to prepare and investigate diclofenac diethylamine (DDA) loaded nanofibers made of Et cellulose (EC) and polyvinyl pyrrolidone K90 (PVP) using electrospinning.The impact of penetration enhancers such as nerolidol and farnesol on release profiles through cellophane membranes and other characteristics of nanofibers were also investigated.Based on release studies, some formulations were selected for release examination through rate skin using Franz diffusion cells.To gain insight about potential interactions between drug and polymers FTIR, DSC, and XRD analyses were performed.Morphol. examination was also conducted using SEM (SEM).Morphol. studies showed that nanofibers made of EC only are greater in the mean diameter than other nanofibers while other formulations were not significantly different from each other regardless of the presence of penetration enhancers.EC nanofibers had the lowest elastic modulus and tensile strength and most elongation at break which makes them the least tough and most flexible nanofibers among all the formulations.The addition of PVP increased the toughness and decreased the flexibility of nanofibers.The addition of nerolidol did not alter the mech. properties of nanofibers significantly, while the addition of farnesol increased elastic modulus, tensile strength, and elongation at break significantly in a concentration-dependent manner.EC nanofibers had the lowest release rate and lowest total cumulative release content while the addition of PVP significantly improved both of these features.In release studies through cellophane membrane, the addition of 5 % of penetration enhancer slightly increased the release rate while did not significantly alter cumulative release while the addition of 10 % farnesol notably increased the release rate and total cumulative released content.Release studies through rat skin were in accordance with cellophane membrane studies and the formulation with 10 % farnesol had the most release rate and total cumulative release and these findings confirm the pos. effect of penetration enhancers.DSC thermogram showed an amorphous state of the drug in fibers and this was supported by XRD results.The FTIR results confirmed that no chem. interaction between the drug and other formulation components has occurred and no new compounds have been formed.Based on these results, the utilization of DDA-loaded PVP and EC nanofibers in conjunction with a penetration enhancer showed significant potential for application in transdermal patches.

27 May 2024·Journal of Drug Targeting

Preparation and anti-inflammatory effect of mercury sulphide nanoparticle-loaded hydrogels

Article

Author: Liang, Ruming ; Wu, Shikui ; Lv, Wei ; Li, Jian ; Yang, Yihang ; Wang, Can ; Xuan, Chengrui

We successfully prepared mercury sulphide nanoparticle hydrogels by physical encapsulation method. The successfully prepared mercuric sulphide nanoparticle hydrogel was a zinc folate hydrogel, which showed an obvious porous structure with interconnected and uniformly distributed pores and a pore size range of about 20 μm. The maximum drug loading of the hydrogels was 3%, and the in vitro cumulative release degree was in accordance with the first-order kinetic equation Mt = 149.529 (1 - e^-0.026^t). The particles in mercuric sulphide nanoparticle hydrogels significantly down-regulated the expression of the cell surface co-stimulatory molecule CD86 (p < .0001). Meanwhile, the inflammatory response was regulated through the NF-κB pathway in LPS-induced inflammatory cells. Later, it was observed that mercuric sulphide nanoparticle hydrogels could significantly counteract the inflammatory and immune models through a mouse ear swelling model, a rat foot-plantar swelling model and a rheumatoid arthritis model. This design targets the immunomodulatory, and anti-inflammatory effects through nanocomposite hydrogel technology. It reduces the drawbacks of low mercury utilisation and susceptibility to accumulation of toxicity. It aims to provide an experimental basis for the development of mercuric sulphide and the treatment of inflammatory and immune-related diseases.HighlightsMercury sulphide nanoparticle hydrogel has an optimal mercury sulphide nanoparticle content of 2%, is structurally homogeneous and stable, and does not exhibit significant liver or kidney toxicity.Mercuric sulphide nanoparticle hydrogel exerts anti-inflammatory effects in cells and rats, and regulates the expression of macrophage surface molecules and factors related to the NF-κB pathway.Mercuric sulphide nanoparticle hydrogel improves the condition of ankle synovial joints in a rat model of rheumatoid arthritis.

100 Deals associated with Diclofenac Diethylamine

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External Link

KEGG	Wiki	ATC	Drug Bank
D07817	Diclofenac Diethylamine	M02AA15 D11AX18 M01AB05 S01BC03	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Inflammation	China	-	01 Jan 1999
Pain	China	-	01 Jan 1999

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Arthralgia	Phase 2	China	NOVARTIS CONSUMER HEALTH SCHWEIZ AG	24 Oct 2019
Arthralgia	Phase 2	China	Beijing Novartis Pharma Co. Ltd.	24 Oct 2019
Arthralgia	Phase 2	China	Novartis Consumer Health SA	24 Oct 2019
Contusions	Phase 2	China	Beijing Novartis Pharma Co. Ltd.	24 Oct 2019
Contusions	Phase 2	China	Novartis Consumer Health SA	24 Oct 2019
Osteoarthritis	Phase 2	China	NOVARTIS CONSUMER HEALTH SCHWEIZ AG	24 Oct 2019
Osteoarthritis	Phase 2	China	Novartis Consumer Health SA	24 Oct 2019
Osteoarthritis	Phase 2	China	Beijing Novartis Pharma Co. Ltd.	24 Oct 2019
Osteoarthritis, Knee	Phase 2	Germany	Novartis AG	01 Oct 2013
Ankle Injuries	Phase 2	Germany	Novartis AG	01 Jul 2009

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04052620 (Pubmed)	Phase 3	-	302	Diclofenac diethylamine 2.32% gel	oglwhqvabv(eojjoyfkyu): mean difference = 1.11, P-Value = 0.595 View more	Positive	24 Dec 2022
				Diclofenac diethylamine 1.16% gel
NCT04052620 (CTgov)	Phase 3	Pain \| Ankle Injuries	313	Diclofenac diethylamine 1.16% gel	aczygnmhfb(pqzdbgcuhe) = gvaycsprnu xhmouvhafo (jxhacnvnrv, otuihuwuer - qojkiccvmo) View more	-	12 Apr 2022
NCT01967550 (CTgov)	Phase 3	Osteoarthritis, Knee	304	diclofenac diethylamine, DDEA 2.32% gel (Diclofenac Diethylamine, DDEA 2.32% Gel)	yffnxxekre(fiqyckwzlg) = oooqiimeha ytjtaklvmm (kmxuhcbins, mdvuadfpoo - ncabgnawqq) View more	-	03 Jun 2015
				Placebo (Placebo)	yffnxxekre(fiqyckwzlg) = frtudiwouc ytjtaklvmm (kmxuhcbins, jgxtgdwzkl - abrbsweppf) View more
NCT01335724 (Pubmed \| BMC Musculoskelet Disord)	Phase 4	Neck Pain	72	Diclofenac diethylamine 1.16% gel	vitnuaaljf(yiagfmkscv) = ohchesivxt sgejibhzfr (gqtotaufzp ) View more	Positive	21 Aug 2013
				Placebo gel	vitnuaaljf(yiagfmkscv) = rqlrgrywnv sgejibhzfr (gqtotaufzp ) View more
NCT01335724 (CTgov)	Phase 4	Neck Pain	72	Diclofenac diethylamine 1.16% gel (Diclofenac Diethylamine 1.16% Gel)	wqfjoobgvh(wxvzkntufd) = fbeauipbtw zfdakonasx (jzbkozpccl, xrklwdyqxr - rganzrzzyk) View more	-	18 Jul 2012
				Placebo gel (Placebo Gel)	wqfjoobgvh(wxvzkntufd) = foinelunau zfdakonasx (jzbkozpccl, yjfqtzynxl - dkqynqyeif) View more
NCT00955513 (CTgov)	Phase 3	Ankle Injuries	242	Diclofenac Diethylamine (Diclofenac Diethylamine Gel 2.32% Gel. Applied 2 Times a Day)	gvpbmaoqmk(eoqmbtqhta) = crhyipabsg oxgnwbwlay (zcnekgifvl, stvutgoqxr - dxkidpbqdg) View more	-	26 Jan 2011
				Diclofenac Diethylamine (Diclofenac Diethylamine Gel 2.32% Gel. Applied 3 Times a Day)	gvpbmaoqmk(eoqmbtqhta) = qfcpsuamvb oxgnwbwlay (zcnekgifvl, pwdbibxils - bjgmnkhpqe) View more