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Medicinal salt with local narcosis and antiphlogosis activity and its prepn process

A technology of local anesthetics and medicinal salts, applied in the field of new medicinal salts, can solve problems such as difficulty in obtaining diclofenac aqueous injection, low solubility, etc.

Inactive Publication Date: 2004-04-07
YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aqueous injection of diclofenac is difficult to obtain due to its relatively low solubility in water

Method used

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  • Medicinal salt with local narcosis and antiphlogosis activity and its prepn process
  • Medicinal salt with local narcosis and antiphlogosis activity and its prepn process
  • Medicinal salt with local narcosis and antiphlogosis activity and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Preparation of diclofenac salt of lidocaine via lidocaine free base and diclofenac free acid

[0078] Element

Weight (g) or Volume (ml)

Lidocaine free base

23.434g

Diclofenac Free Acid

29.615g

ethanol

120mL

[0079] method 1:

[0080] Lidocaine free base (23.434 g) was dissolved in 20 mL of alcohol. Diclofenac free acid (29.615 g) was dissolved in 100 mL of ethanol. The dissolved solutions of lidocaine free base and diclofenac free acid were mixed well. Ethanol was removed by natural evaporation (even if the sample evaporated naturally), reduced pressure or vacuum concentration or drying under nitrogen atmosphere until completely dry to obtain the diclofenac salt of lidocaine in Example 1.

[0081] Method 2:

[0082] Lidocaine free base (23.434 g) and diclofenac free acid (29.615 g) were mixed well and then added to 120 mL of ethanol. Alternatively, lidocaine free base and diclofenac free acid are added sequen...

Embodiment 2

[0084] Preparation of diclofenac salt of lidocaine via lidocaine free base and diclofenac free acid

[0085] Element

Weight (g) or Volume (ml)

Lidocaine free base

2.3434g

Diclofenac Free Acid

2.9615g

ethanol

120mL

[0086] method 1:

[0087] Lidocaine free base (2.3434 g) was dissolved in 20 mL of ethanol. Diclofenac free acid (2.9615 g) was dissolved in 100 mL of ethanol with optional heating to facilitate dissolution. The dissolved solutions of lidocaine free base and diclofenac free acid were mixed. Ethanol was removed by natural evaporation, decompression or vacuum concentration or drying under nitrogen atmosphere until the sample was completely dry to obtain the diclofenac salt of lidocaine in Example 2.

[0088] Method 2:

[0089]Lidocaine free base (2.3434 g) and diclofenac free acid (2.9615 g) were mixed well and then added to 120 mL of ethanol. Alternatively, lidocaine free base and diclofenac free acid are ad...

Embodiment 3

[0091] Preparation of diclofenac salt of lidocaine via lidocaine free base and diclofenac free acid

[0092] Element

Weight (g) or Volume (ml)

Lidocaine free base

23.434g

Diclofenac Free Acid

29.615g

Isopropanol

120mL

[0093] method 1:

[0094] Lidocaine free base (23.434 g) was dissolved in 20 mL of isopropanol. Diclofenac free acid (29.615 g) was dissolved in 100 mL of isopropanol with optional heating to facilitate dissolution. The dissolved solutions of lidocaine and diclofenac were mixed. The isopropanol was removed by natural evaporation, reduced pressure or vacuum concentration or drying under nitrogen atmosphere until completely dry to obtain the diclofenac salt of lidocaine in Example 3.

[0095] Method 2:

[0096] Lidocaine free base (23.434 g) and diclofenac free acid (29.615 g) were mixed and then added to 120 mL of isopropanol. Alternatively, add lidocaine free base and diclofenac free acid sequentially t...

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PUM

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Abstract

The present invention provides with local narcosis and antiphlogosis activity, and the optimal salt is diclofenac salt of lidocaine. Diclofenac acid is one kind of non-steroid anti-inflammatory drug (NSAID), and lidocaine is one kind of local anaesthetic, with diclofenac acid and / or lidocaine being replaceable with other NSAID and / or other local anaesthetic separately. The medicinal salt is crysalline compound dissimilar to NSAID and lidocaine obviously, as DSC, TGA, HPLC and FTIR show. The medicinal salt is especially suitable for local treatment and injection outside gastrointestinal tract to treat local pain including muscle pain, joint pain, pain related to herpes, wound pain, etc.

Description

technical field [0001] The present invention relates to a new group of pharmaceutically acceptable salts, each having local anesthetic and anti-inflammatory activity. The preferred pharmaceutically acceptable salt in this group is the diclofenac salt of lidocaine. Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID). Lidocaine is a local anesthetic. Other NSAIDs (except salicylic acid derivatives of NSAIDs) can be used in place of diclofenac, and / or other local anesthetics can be used in place of lidocaine. The pharmaceutically acceptable salts of the present invention are physically and chemically distinct from NSAIDs alone or local anesthetics alone. The pharmaceutically acceptable salts of the present invention are particularly suitable for topical treatment or parenteral injection to treat localized pain in patients, including but not limited to muscle pain, arthralgia, pain associated with herpes infection, and / or wound pain (such as surgical surgical pain or b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/08A61K9/107A61K9/70A61K31/167A61K31/196A61K31/407A61K45/06A61P23/02A61P29/00C07C229/42C07C237/04C07D487/04
CPCY10S514/97C07D487/04A61K31/167C07C229/42C07C237/04A61K31/196A61K45/06A61P23/02A61P29/00A61K2300/00
Inventor 李芳裕陈善炯陈炳崑蔡瓊如易延陵
Owner YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD
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