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Diclofenac salt of tramadol

A technology of diclofenac and tramadol, applied in the preparation of organic compounds, active ingredients of anhydride/acid/halide, medical preparations containing active ingredients, etc., can solve the problem of difficult to obtain diclofenac aqueous injection solution, low solubility, etc. question

Inactive Publication Date: 2013-03-13
YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aqueous injectable solutions of diclofenac are difficult to obtain due to its low solubility in water

Method used

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  • Diclofenac salt of tramadol
  • Diclofenac salt of tramadol
  • Diclofenac salt of tramadol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Embodiment 1. Obtaining the method for tramadol-diclofenac (1: 1) co-crystal

[0080] A solution of tramadol free base (22 g, 83.5 mmol) in 50 mL of dichloromethane was added to a stirred solution of diclofenac free acid (24.7 g, 83.4 mmol) in 50 mL of ethyl acetate. The mixture was heated until dissolved, then the solvent was evaporated under vacuum to yield a white amorphous solid. The amorphous solid was dissolved in 350 mL of acetonitrile, then heated to 75°C with stirring for 1 hour. The supernatant was cooled to room temperature to produce a white precipitate. The obtained precipitate was filtered off and dried by oven to afford a crystalline white solid (43.6 g, 93.2% yield) of diclofenac salt with a 1:1 ratio of tramadol.

[0081] The crystalline form of the diclofenac salt of tramadol was characterized by a powder XRD profile having X-ray powder diffraction peaks selected from the group consisting of: at about 11.0°, 19.0°, 20.5° and 20.8° ± 0.2° 2Θ. In this...

Embodiment 2

[0082] Example 2. Identification of Diclofenac Salt (1:1) of Tramadol

[0083] The diclofenac salt of tramadol of Example 1 (1:1 ratio) was identified by the following analysis.

[0084] NMR

[0085] The proton nuclear magnetic resonance (NMR) analysis record of the sample of embodiment 1 is by Bruker Avance II 400Ultrashield NMR in deuterated chloroform (CDCl 3 ) is obtained.

[0086] Diclofenac with Tramadol: 1 H NMR (400MHz, CDCl 3 )δ8.12 (br, 1H, proton of protonated tertiary amine), 7.31 (d, J=8.0Hz, 1H), 7.25 (t, J=8.0Hz, 1H), 7.22 (dd, J=6.0, 1.6 Hz, 1H), 7.09(br, 1H), 7.03(td, J=7.6, 1.6Hz, 1H), 6.98(d, J=8.0Hz, 1H), 6.93(t, J=8.0Hz, 1H), 6.86(td, J=7.6, 1.2Hz, 1H), 6.75(dd, J=8.0, 2.4Hz, 1H), 6.49(dd, J=7.6, 1.2Hz, 1H), 3.80(s, 3H), 3.75( s, 2H), 2.72(dd, J=13.2, 8.0Hz, 1H), 2.29(s, 6H), 2.25(dd, J=13.2, 2.0Hz, 1H), 1.94-2.00(m, 1H), 1.82 -1.86(m, 1H), 1.52-1.79(m, 6H), 1.24-1.31(m, 1H) 13 C NMR (100MHz, CDCl 3 )δ177.64,159.63,149.65,142.88,138.33,130.70,129....

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Abstract

The present invention relates to a compound of diclofenac-tramadol salt in 1:1 ratio and a pharmaceutical formulation comprising such compound. The present invention also relates to a method for treating a patient with moderate to moderately severe pain. The method comprises: identifying a patient suffering from moderate to moderately severe pain with pain intensity scale of 5-9, and administering to said patient the diclofenac-tramadol salt, in an effective amount. The method is particularly useful in treating postoperative pain after Cesarean, postoperative pain after non-Cesarean surgeries, cancer pain, osteoarthritis pain, or rheumatoid arthritis pain.

Description

technical field [0001] The present application relates to compounds having a diclofenac-tramadol salt in a 1:1 ratio. The present invention also relates to the efficacy of said compounds in the treatment of moderate to severe pain, such as post-surgical pain (e.g., after cesarean section or other surgical procedures), cancer pain, and pain associated with erosive osteoarthritis and rheumatoid arthritis. application. Background technique [0002] According to its physical cause, pain can be divided into 3 categories: nociceptive, neurological, and mixed. [0003] Nociceptive pain is usually caused by nociceptive stimuli, such as heat and cutting that directly result in damage or injury to the body or tissues. Nociceptive pain can be further divided into two categories based on where the pain begins: somatic pain and visceral pain. Somatic pain arises in bones, joints, muscles, skin, or connective tissue in direct contact with an external noxious stimulus. Visceral pain ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/195A61K31/185A61K31/135A61P35/00A61P19/10
CPCC07C217/74C07C2101/14A61K31/135C07C229/42A61K31/196A61P19/10A61P25/00A61P29/00A61P35/00C07C2601/14A61K2300/00A61K31/185A61K31/195C07C211/55C07C211/63
Inventor 陈佳慧黄毓梁龚亮仁颜铭钟
Owner YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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