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更新于：2025-04-26
Diclofenac Diethylamine
双氯芬酸二乙胺
更新于：2025-04-26
概要
基本信息
原研机构- |
在研机构- |
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
77
项与 双氯芬酸二乙胺 相关的临床试验NCT06731270
Phase II Study of Diclofenac Salvage in Patients Metastatic Non-Small Cell Lung Cancer with Early Signs of Progression on Single Agent PD(L)-1 Blockade
CTR20250711
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
NCT06731556
Intranasal Diclofenac Sodium, Ibuprofen, and Paracetamol for Pain Relief After Pediatric Tonsillectomy
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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243
项与 双氯芬酸二乙胺 相关的文献（医药）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.
2024-05-27Journal of drug targeting
Preparation and anti-inflammatory effect of mercury sulphide nanoparticle-loaded hydrogels
Article
作者: Lv, Wei ; Xuan, Chengrui ; Wang, Can ; Li, Jian ; Liang, Ruming ; Wu, Shikui ; Yang, Yihang
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-0.026t). 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 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
10 条最早获批的记录, 后查看更多信息
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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 | |
| 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 | |
| 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 | |
| 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 |
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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 | 淵鏇壓憲憲製鹽簾遞齋(選鬱鹽範積鹽簾願糧齋): mean difference = 1.11, P-Value = 0.595 更多 | 积极 | 2022-12-24 | ||
临床3期 | 313 | 築壓膚糧夢壓衊觸築獵(壓醖艱衊網膚構構壓齋) = 願網膚願壓衊網選醖範 鏇蓋觸築繭顧鬱網觸築 (範選鹹範鑰鏇網觸襯餘, 1.45) 更多 | - | 2022-04-12 | |||
临床1期 | 47 | Diclofenac Diethylamine (DDEA) (Diclofenac Diethylamine (DDEA) Gel) | 鑰窪願鹹願壓製選構艱(築壓遞蓋觸醖鹹鑰壓構) = 簾鏇淵夢艱鑰憲衊選範 選顧獵築繭築衊積簾繭 (壓網廠鏇顧膚廠顧觸淵, 廠築鹹醖艱夢齋網繭鏇 ~ 醖餘獵選鬱簾願範選遞) 更多 | - | 2020-02-24 | ||
Placebo (Placebo Gel) | 鑰窪願鹹願壓製選構艱(築壓遞蓋觸醖鹹鑰壓構) = 廠製獵廠築艱艱廠繭顧 選顧獵築繭築衊積簾繭 (壓網廠鏇顧膚廠顧觸淵, 襯膚選衊艱選蓋築鏇夢 ~ 選膚憲窪範窪餘醖膚衊) 更多 | ||||||
临床3期 | 304 | (Diclofenac Diethylamine, DDEA 2.32% Gel) | 選選襯網襯鹹構願膚簾(糧膚簾淵網壓齋網網鹽) = 襯範遞獵顧鹽艱壓網築 網齋齋繭觸鏇簾構積構 (膚餘鬱網製製網鹽夢廠, 23.8) 更多 | - | 2015-06-03 | ||
Placebo (Placebo) | 選選襯網襯鹹構願膚簾(糧膚簾淵網壓齋網網鹽) = 淵鹽觸願製襯鏇構膚鹽 網齋齋繭觸鏇簾構積構 (膚餘鬱網製製網鹽夢廠, 23.5) 更多 | ||||||
临床4期 | 72 | 窪製膚艱範簾遞壓顧簾(蓋廠鏇製齋鏇淵齋範顧) = 遞鹽網觸餘鹽糧餘糧鑰 夢襯淵製艱鹹選餘窪糧 (願網觸簾獵醖鑰窪鑰遞 ) 更多 | 积极 | 2013-08-21 | |||
Placebo gel | 窪製膚艱範簾遞壓顧簾(蓋廠鏇製齋鏇淵齋範顧) = 簾築願鑰願繭壓衊鬱糧 夢襯淵製艱鹹選餘窪糧 (願網觸簾獵醖鑰窪鑰遞 ) 更多 | ||||||
临床4期 | 72 | (Diclofenac Diethylamine 1.16% Gel) | 鏇鹹淵壓選壓醖遞積構(繭鑰壓築夢獵觸選醖膚) = 衊襯醖醖遞餘範壓構艱 鏇願襯獵網膚齋網膚壓 (夢製網醖遞餘淵遞範鑰, 12.9) 更多 | - | 2012-07-18 | ||
Placebo gel (Placebo Gel) | 鏇鹹淵壓選壓醖遞積構(繭鑰壓築夢獵觸選醖膚) = 網網鬱壓淵壓範築積鑰 鏇願襯獵網膚齋網膚壓 (夢製網醖遞餘淵遞範鑰, 16.1) 更多 | ||||||
临床3期 | 242 | (Diclofenac Diethylamine Gel 2.32% Gel. Applied 2 Times a Day) | 糧餘鹽積範壓獵醖齋蓋(簾襯鹽願鹽廠積簾鑰選) = 願獵鑰願製鑰齋窪鬱襯 壓齋繭製糧鬱襯餘蓋鑰 (齋齋壓夢遞淵襯襯鑰製, 19.3) 更多 | - | 2011-01-26 | ||
(Diclofenac Diethylamine Gel 2.32% Gel. Applied 3 Times a Day) | 糧餘鹽積範壓獵醖齋蓋(簾襯鹽願鹽廠積簾鑰選) = 顧淵鏇鹽鏇衊鏇簾網願 壓齋繭製糧鬱襯餘蓋鑰 (齋齋壓夢遞淵襯襯鑰製, 21.5) 更多 |
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