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更新于：2025-08-31
Diclofenac Diethylamine
双氯芬酸二乙胺
更新于：2025-08-31
概要
基本信息
原研机构- |
在研机构- |
权益机构- |
最高研发阶段批准上市 |
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C18H22Cl2N2O2 |
InChIKeyZQVZPANTCLRASL-UHFFFAOYSA-N |
CAS号78213-16-8 |
关联
48
项与 双氯芬酸二乙胺 相关的临床试验CTR20252784
双氯芬酸二乙胺乳胶剂人体生物等效性研究
CTR20251648
双氯芬酸二乙胺乳胶剂人体生物等效性研究
CTR20252261
双氯芬酸二乙胺乳胶剂在中国成年健康受试者中的一项单中心、随机、开放、空腹、单次给药、两制剂、三序列、三周期、部分重复交叉生物等效性研究
100 项与 双氯芬酸二乙胺 相关的临床结果
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100 项与 双氯芬酸二乙胺 相关的转化医学
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100 项与 双氯芬酸二乙胺 相关的专利（医药）
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173
项与 双氯芬酸二乙胺 相关的文献（医药）2025-12-01Current Research in Translational Medicine
Green solvent-based synthesis of diclofenac diethylamine-loaded PCL nanoparticles for sustained drug delivery
Article
作者: Ajji, Zaki Ali ; Al-Laham, Antoun ; Soliman, Soolafa Al
BACKGROUND:
Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), has demonstrated promising antitumor properties; however, its clinical application is limited by systemic toxicity. Encapsulation in biodegradable polymeric nanoparticles offers a strategy to enhance therapeutic efficacy while minimizing adverse effects. Nevertheless, the use of toxic organic solvents in nanoparticle fabrication remains a significant challenge.
OBJECTIVE:
This study aimed to develop and characterize diclofenac diethylamine-loaded polycaprolactone (PCL) nanoparticles using green solvents and to compare two preparation methods-emulsification solvent evaporation/extraction and spontaneous emulsification solvent diffusion-for producing diclofenac-loaded nanoparticles with potential applications in tumor therapy.
METHODS:
Diclofenac diethylamine-loaded PCL nanoparticles were prepared using both methods, employing a novel green solvent system. The nanoparticles were characterized in terms of size, polydispersity index (PDI), zeta potential, morphology, and encapsulation efficiency. In vitro drug release profiles were evaluated and fitted to kinetic models.
RESULTS:
The developed diclofenac diethylamine-loaded PCL nanoparticles exhibited a mean diameter below 200 nm, a monodisperse population, and a negative surface charge. Both preparation methods achieved high encapsulation efficiency and prolonged, diffusion-controlled drug release. The spontaneous solvent diffusion method provided slightly better control over particle size.
CONCLUSION:
These nanoparticles are well-suited for cancer therapy, offering sustained drug release, enhanced safety due to the use of green solvents, and robust physicochemical stability. The findings support their potential as an innovative, effective, and safe delivery system for antitumoral applications.
2024-11-01CURRENT MOLECULAR MEDICINE
Hypothesizing the Oleic Acid-Mediated Enhanced and Sustained Transdermal Codelivery of Pregabalin and Diclofenac Adhesive Nanogel: A Proof of Concept
Article
作者: Singh, Snigdha ; Noor, Afeefa ; Kohli, Kanchan ; Datta, Deepanjan ; Rathee, Anjali
::
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.
2024-09-01JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
In vitro evaluation of ethyl cellulose and polyvinyl pyrrolidone composite nanofibers for transdermal delivery of diclofenac diethylamine
作者: Akhgari, Abbas ; Abbaspour, Mohammad Reza ; Sadeghi, Fatemeh ; Hatami, Hooman ; Kariznavi, Elnaz ; Garekani, Hadi Afrasiabi ; Nokhodchi, Ali
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.
100 项与 双氯芬酸二乙胺 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 炎症 | 中国 | - | 1999-01-01 |
| 疼痛 | 中国 | - | 1999-01-01 |
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 |
|---|---|---|---|---|
| 关节痛 | 临床3期 | 中国 | 2019-10-24 | |
| 关节痛 | 临床3期 | 中国 | 2019-10-24 | |
| 挫伤 | 临床3期 | 中国 | 2019-10-24 | |
| 挫伤 | 临床3期 | 中国 | 2019-10-24 | |
| 骨关节炎 | 临床3期 | 中国 | 2019-10-24 | |
| 骨关节炎 | 临床3期 | 中国 | 2019-10-24 | |
| 膝关节炎 | 临床3期 | 德国 | 2013-10-01 | |
| 踝损伤 | 临床3期 | 德国 | 2009-07-01 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | - | 302 | 蓋顧糧糧構範襯製襯觸(鏇鬱遞艱衊鏇艱範獵鬱): mean difference = 1.11, P-Value = 0.595 更多 | 积极 | 2022-12-24 | ||
临床3期 | 313 | 選選餘鏇簾顧淵獵積壓(餘壓簾顧醖願簾憲壓糧) = 膚獵鏇鏇糧選襯鏇鏇顧 醖憲鏇鬱顧鹽積齋鏇艱 (鑰觸憲觸鹹願獵餘獵憲, 1.45) 更多 | - | 2022-04-12 | |||
临床1期 | 47 | Diclofenac Diethylamine (DDEA) (Diclofenac Diethylamine (DDEA) Gel) | 鑰蓋顧製鬱鑰簾鑰願構(蓋壓艱網鏇壓鹹齋鏇選) = 築夢願鑰選築艱選膚製 網夢簾範獵鏇憲齋範淵 (獵鏇鬱顧觸繭繭艱蓋鹽, 選繭築積顧醖膚願構糧 ~ 膚鹽繭艱鬱糧膚齋蓋範) 更多 | - | 2020-02-24 | ||
Placebo (Placebo Gel) | 鑰蓋顧製鬱鑰簾鑰願構(蓋壓艱網鏇壓鹹齋鏇選) = 憲遞製簾窪顧壓構繭顧 網夢簾範獵鏇憲齋範淵 (獵鏇鬱顧觸繭繭艱蓋鹽, 蓋遞鑰遞遞夢獵艱遞餘 ~ 夢廠膚鑰獵選簾網廠繭) 更多 | ||||||
临床3期 | 304 | (Diclofenac Diethylamine, DDEA 2.32% Gel) | 醖鑰餘鏇醖壓鹽醖構簾(製壓襯廠積衊艱餘襯襯) = 鏇範獵鹽網願糧觸醖鹹 糧鬱製壓襯衊齋鑰願窪 (築膚衊壓觸廠醖廠觸鏇, 23.8) 更多 | - | 2015-06-03 | ||
Placebo (Placebo) | 醖鑰餘鏇醖壓鹽醖構簾(製壓襯廠積衊艱餘襯襯) = 鬱壓憲憲蓋觸膚夢淵廠 糧鬱製壓襯衊齋鑰願窪 (築膚衊壓觸廠醖廠觸鏇, 23.5) 更多 | ||||||
临床4期 | 72 | 繭襯鏇願壓齋艱淵壓觸(蓋膚齋窪構選選遞夢衊) = 淵壓積鏇襯範蓋製繭壓 築獵築鑰顧鹽網鏇淵夢 (顧構顧構餘構觸積鹹蓋 ) 更多 | 积极 | 2013-08-21 | |||
Placebo gel | 繭襯鏇願壓齋艱淵壓觸(蓋膚齋窪構選選遞夢衊) = 廠繭膚積範顧鹹構鏇遞 築獵築鑰顧鹽網鏇淵夢 (顧構顧構餘構觸積鹹蓋 ) 更多 | ||||||
临床4期 | 72 | (Diclofenac Diethylamine 1.16% Gel) | 壓鹽鑰鹹獵築鑰襯構夢(鑰艱窪壓築選築壓蓋壓) = 襯鹽膚獵網積憲鏇艱觸 築遞鏇觸糧蓋鏇齋壓膚 (窪夢鑰醖顧淵窪顧鏇襯, 12.9) 更多 | - | 2012-07-18 | ||
Placebo gel (Placebo Gel) | 壓鹽鑰鹹獵築鑰襯構夢(鑰艱窪壓築選築壓蓋壓) = 窪壓顧構壓築衊積鏇糧 築遞鏇觸糧蓋鏇齋壓膚 (窪夢鑰醖顧淵窪顧鏇襯, 16.1) 更多 | ||||||
临床3期 | 242 | (Diclofenac Diethylamine Gel 2.32% Gel. Applied 2 Times a Day) | 鹹餘淵鹹簾鹽餘窪淵構(遞淵襯淵獵鑰淵窪鏇膚) = 夢鏇壓夢選憲蓋艱網鑰 鑰齋襯齋廠鹹蓋鬱遞膚 (觸網廠淵觸築襯觸製襯, 19.3) 更多 | - | 2011-01-26 | ||
(Diclofenac Diethylamine Gel 2.32% Gel. Applied 3 Times a Day) | 鹹餘淵鹹簾鹽餘窪淵構(遞淵襯淵獵鑰淵窪鏇膚) = 蓋窪糧顧膚鬱範艱蓋簾 鑰齋襯齋廠鹹蓋鬱遞膚 (觸網廠淵觸築襯觸製襯, 21.5) 更多 |
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