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

COX

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

CN (01 Jan 1999),

InflammationPain

Regulation-

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Structure

Molecular FormulaC18H22Cl2N2O2

InChIKeyZQVZPANTCLRASL-UHFFFAOYSA-N

CAS Registry78213-16-8

主要目的：本试验旨在研究健康受试者单次空腹涂抹河南科伦药业有限公司持证、江苏知原药业股份有限公司生产的双氯芬酸二乙胺乳胶剂〔1%（20g：0.2g，以C14H10Cl2NNaO2计）〕的药代动力学特征；以GSK Consumer Healthcare Schweiz AG持证、GSK Consumer Healthcare SARL生产的双氯芬酸二乙胺乳胶剂〔扶他林®，1%（20g：0.2g，以C14H10Cl2NNaO2计）〕为参比制剂，比较两制剂中药动学参数Cmax、AUC0-t、AUC0-∞，评价两制剂的人体生物等效性。次要目的：观察健康受试者单次涂抹受试制剂和参比制剂后的安全性。

[Translation]

Primary objective: This study aims to study the pharmacokinetic characteristics of a single fasting application of diclofenac diethylamine emulsion [1% (20 g: 0.2 g, calculated as C14H10Cl2NNaO2)] by healthy subjects; using diclofenac diethylamine emulsion [Voltaren®, 1% (20 g: 0.2 g, calculated as C14H10Cl2NNaO2)] by GSK Consumer Healthcare Schweiz AG and produced by GSK Consumer Healthcare SARL as the reference preparation, to compare the pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ of the two preparations, and to evaluate the bioequivalence of the two preparations in humans. Secondary objective: To observe the safety of the test preparation and the reference preparation after a single application in healthy subjects.

Start Date04 Oct 2024

Sponsor / Collaborator

Henan Kelun Pharmaceutical Co., Ltd.

CTR20242855 / CompletedNot Applicable

双氯芬酸二乙胺乳胶剂人体生物等效性试验

[Translation] Bioequivalence study of diclofenac diethylamine emulsion in human body

采用单中心、随机、开放、三周期、部分重复交叉、单次给药设计，比较空腹给药条件下，福建品腾药业有限公司提供的双氯芬酸二乙胺乳胶剂[规格：1%（20 g：0.2 g），受试制剂]与GSK Consumer Healthcare Schweiz AG持证的双氯芬酸二乙胺乳胶剂[商品名：扶他林®，规格：1%（20 g：0.2 g），参比制剂]在中国健康人群中吸收程度和吸收速度的差异，评价空腹状态下使用两种制剂的生物等效性，并评价福建品腾药业有限公司提供的双氯芬酸二乙胺乳胶剂[规格：1%（20 g：0.2 g）]的安全性。

[Translation]

Methods A single-center, randomized, open-label, three-period, partially repeated crossover, single-dose design was used to compare the differences in absorption extent and rate between diclofenac diethylamine emulsion [specification: 1% (20 g: 0.2 g), test preparation] provided by Fujian Pinteng Pharmaceutical Co., Ltd. and diclofenac diethylamine emulsion [trade name: Voltaren®, specification: 1% (20 g: 0.2 g), reference preparation] certified by GSK Consumer Healthcare Schweiz AG in healthy Chinese people under fasting conditions, to evaluate the bioequivalence of the two preparations when used in the fasting state, and to evaluate the safety of diclofenac diethylamine emulsion [specification: 1% (20 g: 0.2 g)] provided by Fujian Pinteng Pharmaceutical Co., Ltd.

Start Date23 Aug 2024

Sponsor / Collaborator

Fujian Pinteng Pharmaceutical Co., Ltd.

CTR20242744 / CompletedNot Applicable

双氯芬酸二乙胺乳胶剂在健康受试者中的单中心、单次给药、随机、开放、两制剂、部分重复交叉、三周期生物等效性试验

[Translation] A single-center, single-dose, randomized, open-label, two-dose, partially repeated crossover, three-period bioequivalence study of diclofenac diethylamine emulsion in healthy subjects

主要目的:以丽彩甘肃西峰制药有限公司生产的双氯芬酸二乙胺乳胶剂(规格:2.32%(30g:0.696g，以CI8HClN202计))为受试制剂，以GlaxoSmithKline Consumer Healthcare(UK)Trading Limited的双氯芬酸二乙胺乳胶剂(规格:2.32%(30g:0.696g，以CI8H2ClN20计))为参比制剂，按生物等效性试验的有关规定，考察两制剂在健康人体内的生物等效性。次要目的:观察受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Main purpose: Diclofenac diethylamine emulsion (specification: 2.32% (30g: 0.696g, calculated as CI8HClN202)) produced by Licai Gansu Xifeng Pharmaceutical Co., Ltd. was used as the test preparation, and diclofenac diethylamine emulsion (specification: 2.32% (30g: 0.696g, calculated as CI8H2ClN20)) produced by GlaxoSmithKline Consumer Healthcare (UK) Trading Limited was used as the reference preparation. According to the relevant provisions of the bioequivalence test, the bioequivalence of the two preparations in healthy subjects was investigated. Secondary purpose: To observe the safety of the test preparation and the reference preparation in healthy subjects.

Start Date01 Aug 2024

Sponsor / Collaborator

Gansu Xifeng Pharmaceutical 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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112

Literatures (Medical) associated with Diclofenac Diethylamine

01 Dec 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.

04 Dec 2023·Molecular Pharmaceutics

Time-Dependent Differences in the Effects of Oleic Acid and Oleyl Alcohol on the Human Skin Barrier

Article

Author: Kopečná, Monika ; Kováčik, Andrej ; Boncheva Bettex, Mila ; Vávrová, Kateřina ; Hrdinová, Iva ; Opálka, Lukáš

Oleic acid and oleyl alcohol are commonly used permeation and penetration enhancers to facilitate topical drug delivery. Here, we aimed to better understand the mechanism of their enhancing effects in terms of their interactions with the human skin barrier using diclofenac diethylamine (DIC-DEA), a nonsteroidal anti-inflammatory drug for topical pain management. Oleic acid promoted DIC-DEA permeation through ex vivo human skin more rapidly than oleyl alcohol (both applied at 0.75%) due to fluidization of stratum corneum lipids as revealed by infrared spectroscopy. After 12 h, the effect of these enhancers on DIC-DEA permeation leveled off, fluidization was no longer evident, and skin permeabilization was mainly due to the formation of fluid enhancer-rich domains. Contrary to oleyl alcohol, oleic acid adversely affected two indicators of the skin barrier integrity, transepidermal water loss and skin electrical impedance. The content of oleyl alcohol in the stratum corneum was lower than that of oleic acid (even 12 h after the enhancers were removed from the skin surface), but it caused higher DIC-DEA retention in both epidermis and dermis compared to oleic acid. The effects of oleyl alcohol and oleic acid on DIC-DEA permeation and retention in the skin were similar after a single and repeated application (4 doses every 12 h). Thus, oleyl alcohol offers several advantages over oleic acid for topical drug delivery.

02 Nov 2023·Journal of AOAC International

Validation of an HPLC Method for the Determination of Diclofenac Diethylamine and Three of Its Impurities in a Gel Pharmaceutical Form

Article

Author: El Karbane, Miloud ; Elhamdaoui, Omar ; Bouatia, Mustapha ; Azougagh, Mohamed ; Laouni, Amine ; El Kacemi, Mounir ; Karrouchi, Khalid ; El Orche, Aimen

AbstractBackgroundMonitoring impurities in drug products is a principal requirement of pharmaceutical regulatory authorities all over the world to ensure drug safety. For this reason, there is a great need for analytical QC of dugs products.ObjectiveIn this study, a simple, efficient, and direct HPLC method was developed for the determination of three impurities of diclofenac.MethodsThe HPLC method was developed using a mobile phase which consisted of an HPLC grade mixture, acetonitrile–0.01M phosphoric acid adjusted to pH 2.3 (1 + 3, by volume).ResultsThe separation was performed in 15 min. The calibration curves of the three impurities were linear; the correlation coefficients were 0.999 at concentrations of 0.00015–0.003 µg/mL.ConclusionThe validation of this method shows that it meets all validation criteria. This shows the reliability of this method for the routine control of diclofenac impurities.HighlightsThe validation of a robust HPLC method for the determination of diclofenac impurities is of great importance for the pharmaceutical industry to control its products.

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	CN	-	01 Jan 1999
Pain	CN	-	01 Jan 1999

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Arthralgia	Phase 1	CN	Novartis Consumer Health SA	24 Oct 2019
Contusions	Phase 1	CN	Beijing Novartis Pharma Co. Ltd.	24 Oct 2019
Pain	Phase 1	CN	GSK Plc	24 Oct 2019
Contusions	Preclinical	CN	NOVARTIS CONSUMER HEALTH SCHWEIZ AG	24 Oct 2019
Contusions	Preclinical	CN	Novartis Consumer Health SA	24 Oct 2019
Osteoarthritis	Preclinical	CN	NOVARTIS CONSUMER HEALTH SCHWEIZ AG	24 Oct 2019
Osteoarthritis	Preclinical	CN	Novartis Consumer Health SA	24 Oct 2019
Osteoarthritis	Preclinical	CN	Beijing Novartis Pharma Co. Ltd.	24 Oct 2019
Osteoarthritis, Knee	Preclinical	DE	Novartis AG	01 Oct 2013
Ankle Injuries	Preclinical	DE	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	Ankle Injuries	302	Diclofenac diethylamine 2.32% gel	fpvozvdcrl(wlcetqrlhi): 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	qugmzzgjmq(vnyxatahqx) = nyeyfmrixj lzbsxdqmjd (krpznkxckr, wlyuaxphjx - gazgwpwbis) View more	-	12 Apr 2022
NCT01335724 (Pubmed \| BMC Musculoskelet Disord)	Phase 4	Neck Pain	72	Diclofenac diethylamine 1.16% gel	ltkgqrskkb(vbjwtniyot) = jxdxvisdmn prnsjpkqid (yvjmfnspwz ) View more	Positive	21 Aug 2013
				Placebo gel	ltkgqrskkb(vbjwtniyot) = pmkfkylcrr prnsjpkqid (yvjmfnspwz ) View more
NCT01335724 (CTgov)	Phase 4	Neck Pain	72	Diclofenac diethylamine 1.16% gel (Diclofenac Diethylamine 1.16% Gel)	tkmbexkjjh(vhocegmejr) = uglboildwl cpiygggsih (kamvrtvfeu, kkisbenlhc - ewkgitbjpr) View more	-	18 Jul 2012
				Placebo gel (Placebo Gel)	tkmbexkjjh(vhocegmejr) = iawvkaujma cpiygggsih (kamvrtvfeu, qkdsfiisah - awkttyjxaf) View more
NCT00955513 (CTgov)	Phase 3	Ankle Injuries	242	Diclofenac Diethylamine (Diclofenac Diethylamine Gel 2.32% Gel. Applied 2 Times a Day)	viahswelpl(ydxjntntxy) = xkmhusdfxp nsrvqvuljg (huffipgglm, rikcbsnzwb - gvmbwcfaju) View more	-	26 Jan 2011
				Diclofenac Diethylamine (Diclofenac Diethylamine Gel 2.32% Gel. Applied 3 Times a Day)	viahswelpl(ydxjntntxy) = sftxexacbt nsrvqvuljg (huffipgglm, mjhiitdajq - tvxmwsrkkz) View more