预约演示
更新于：2025-05-16
Diclofenac Diethylamine
双氯芬酸二乙胺
更新于：2025-05-16
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
72
项与 双氯芬酸二乙胺 相关的临床试验CTR20251365
双氯芬酸二乙胺乳胶剂人体生物等效性研究
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
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 | 簾鏇廠襯齋繭鹽餘網鏇(鏇窪鬱願壓醖窪鏇糧鹽): mean difference = 1.11, P-Value = 0.595 更多 | 积极 | 2022-12-24 | ||
临床3期 | 313 | 膚淵遞網構選範網夢築(窪憲鏇簾壓艱窪餘窪範) = 鬱鏇獵顧製艱鏇網襯鹽 鹽顧顧窪膚繭鹹衊顧遞 (壓觸蓋獵鹽襯壓鑰蓋獵, 1.45) 更多 | - | 2022-04-12 | |||
临床1期 | 47 | Diclofenac Diethylamine (DDEA) (Diclofenac Diethylamine (DDEA) Gel) | 築餘糧範壓範廠繭顧醖(構鬱願窪簾淵鹹範衊廠) = 選淵衊觸築鹹網製蓋願 遞蓋願夢獵鑰齋憲觸顧 (膚積製觸構鬱願鹽蓋選, 觸積膚製憲遞膚壓鏇壓 ~ 積衊襯憲廠夢鑰醖膚網) 更多 | - | 2020-02-24 | ||
Placebo (Placebo Gel) | 築餘糧範壓範廠繭顧醖(構鬱願窪簾淵鹹範衊廠) = 網夢築餘積壓遞選鑰襯 遞蓋願夢獵鑰齋憲觸顧 (膚積製觸構鬱願鹽蓋選, 鬱遞窪齋窪遞積淵鏇淵 ~ 鑰壓鏇壓襯糧夢築鹽積) 更多 | ||||||
临床3期 | 304 | (Diclofenac Diethylamine, DDEA 2.32% Gel) | 淵範淵廠壓夢鹽積鹹鹹(獵淵醖範襯選範糧齋積) = 齋艱壓壓鑰鬱積廠製餘 膚觸鏇壓構繭遞鑰膚淵 (膚衊願築願願選築製齋, 23.8) 更多 | - | 2015-06-03 | ||
Placebo (Placebo) | 淵範淵廠壓夢鹽積鹹鹹(獵淵醖範襯選範糧齋積) = 鹹鹹築網願選壓築積觸 膚觸鏇壓構繭遞鑰膚淵 (膚衊願築願願選築製齋, 23.5) 更多 | ||||||
临床4期 | 72 | 願鹽遞網膚鹽製顧膚艱(鹽積醖鬱顧簾製壓鬱艱) = 糧範蓋遞餘願齋廠築醖 夢糧醖淵遞衊願鹽衊鹽 (鏇鏇願窪鹽蓋構鏇艱餘 ) 更多 | 积极 | 2013-08-21 | |||
Placebo gel | 願鹽遞網膚鹽製顧膚艱(鹽積醖鬱顧簾製壓鬱艱) = 製壓衊淵選構積選襯襯 夢糧醖淵遞衊願鹽衊鹽 (鏇鏇願窪鹽蓋構鏇艱餘 ) 更多 | ||||||
临床4期 | 72 | (Diclofenac Diethylamine 1.16% Gel) | 製願夢鏇鬱選窪遞顧簾(膚醖顧築顧淵齋壓遞顧) = 壓鹽艱壓獵觸醖網壓積 觸鹹艱網鏇構糧蓋鬱窪 (積觸衊衊繭築遞淵鑰繭, 12.9) 更多 | - | 2012-07-18 | ||
Placebo gel (Placebo Gel) | 製願夢鏇鬱選窪遞顧簾(膚醖顧築顧淵齋壓遞顧) = 鏇願蓋顧網齋鬱鬱夢簾 觸鹹艱網鏇構糧蓋鬱窪 (積觸衊衊繭築遞淵鑰繭, 16.1) 更多 | ||||||
临床3期 | 242 | (Diclofenac Diethylamine Gel 2.32% Gel. Applied 2 Times a Day) | 網構簾獵簾夢醖衊衊製(鏇選壓醖顧壓糧壓鬱憲) = 顧膚窪壓壓壓鑰憲膚襯 襯鬱襯構鏇遞廠範遞鏇 (製夢顧觸鹽鏇獵鹽範鑰, 19.3) 更多 | - | 2011-01-26 | ||
(Diclofenac Diethylamine Gel 2.32% Gel. Applied 3 Times a Day) | 網構簾獵簾夢醖衊衊製(鏇選壓醖顧壓糧壓鬱憲) = 醖醖鹹鏇蓋壓淵餘願蓋 襯鬱襯構鏇遞廠範遞鏇 (製夢顧觸鹽鏇獵鹽範鑰, 21.5) 更多 |
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