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Etofenamate

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Chemical Structure| 30544-47-9 同义名 : -
CAS号 : 30544-47-9
货号 : A208669
分子式 : C18H18F3NO4
纯度 : 99%+
分子量 : 369.335
MDL号 : MFCD00242806
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(135.38 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(270.76 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties[3]. Etofenamate is an effective therapeutic option for the management of musculoskeletal disorders, such as blunt traumas, lumbago or osteoarthrosis[4]. The single dose of 1 g etofenamate is effective in the management of acute pain[5]. Molecules like etofenamate have a bioavailability of >20% and evidence for accumulation in synovial tissues, with efficacy demonstrated as improvement in pain and function in real-life studies of OA (osteoarthritis) patients[6]. In vivo activity in the rat paw edema inflammation model showed that SLN hydrogels containing lower doses of etofenamate (8.3 times lower) and ibuprofen (16.6 times lower) produced similar effects compared to the commercial formulations, while decreasing edema and inflammatory cell infiltration, and causing no histological changes in the epidermis[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00530387 Dermatitis, Photocontact Not Applicable Completed - United Kingdom ... 展开 >> Photobiology Unit, Ninewells Hospital, Dundee, Angus, United Kingdom, DD1 9SY 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.08mL

5.42mL

2.71mL
参考文献

[1]Fraga A, de Almeida M, et al. Intramuscular Etofenamate versus Diclofenac in the Relief of Renal Colic : A Randomised, Single-Blind, Comparative Study. Clin Drug Investig. 2003;23(11):701-6.

[2]Bender T, Bariska J, et al. Etofenamate levels in human serum and synovial fluid following iontophoresis. Arzneimittelforschung. 2001;51(6):489-92.

[3]Fraga A, de Almeida M, Moreira-da-Silva V, Sousa-Marques M, Severo L, Matos-Ferreira A, Campos-Pinheiro L, Reis M, Ribau U, Silveira P, Almeida L. Intramuscular Etofenamate versus Diclofenac in the Relief of Renal Colic : A Randomised, Single-Blind, Comparative Study. Clin Drug Investig. 2003;23(11):701-6

[4]Marinho ODS, Pereira A. Clinical Efficacy and Safety Profile of Topical Etofenamate in the Treatment of Patients with Musculoskeletal Disorders: A Systematic Review. Pain Ther. 2020 Dec;9(2):393-410

[5]Patiñio JL, Mejía SN, Ramos EQ. Efecto analgésico del etofenamato en el manejo de las lumbalgias agudas en urgencias [Etofenamate and the analgesic effect in the management of acute pain from spine in the emergency room]. Acta Ortop Mex. 2007 Sep-Oct;21(5):253-5. Spanish

[6]Rannou F, Pelletier JP, Martel-Pelletier J. Efficacy and safety of topical NSAIDs in the management of osteoarthritis: Evidence from real-life setting trials and surveys. Semin Arthritis Rheum. 2016 Feb;45(4 Suppl):S18-21

[7]Mancini G, Gonçalves LMD, Marto J, Carvalho FA, Simões S, Ribeiro HM, Almeida AJ. Increased Therapeutic Efficacy of SLN Containing Etofenamate and Ibuprofen in Topical Treatment of Inflammation. Pharmaceutics. 2021 Mar 3;13(3):328