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Carboxyl contained NSAIDS (nonsteroidal anti-inflammatory drugs) salt

An antipyretic and analgesic drug and an antipyretic and analgesic technology are applied in the salt field of carboxyl-containing non-steroidal antipyretic and analgesic drugs, and can solve the problems of water insolubility, large toxic and side effects, drug resistance and the like

Inactive Publication Date: 2007-05-30
陈文展
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the gastrointestinal side effects of NSAIDs currently used clinically are relatively common, so medicinal chemists at home and abroad have been committed to finding new anti-inflammatory drugs with high efficiency and low toxicity
[0003] Existing non-steroidal antipyretic and analgesic drugs have been used for many years, and their safety has been verified, but each has some problems, such as insolubility in water, low bioavailability, long-term use, large toxic and side effects, and drug resistance.

Method used

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  • Carboxyl contained NSAIDS (nonsteroidal anti-inflammatory drugs) salt
  • Carboxyl contained NSAIDS (nonsteroidal anti-inflammatory drugs) salt
  • Carboxyl contained NSAIDS (nonsteroidal anti-inflammatory drugs) salt

Examples

Experimental program
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Effect test

Embodiment 1

[0016] Embodiment 1: the preparation of saprofen acid tromethamine salt

[0017] In a 500ml dry and clean three-neck flask, add 30g of serprofen acid and 300ml of anhydrous benzene, heat and stir until completely dissolved, add 13g of tromethamine under the state of complete dissolution, heat and reflux the mixture for 3 hours, TLC thin layer identification reaction completely (developing solvent: ethyl acetate: ethanol: glacial acetic acid = 5:5:0.5), slightly cool the mixture and add 200ml of absolute ethanol, put the mixture in the refrigerator to fully cool, filter the precipitated white crystals with suction, and use a small amount of cold The solid was washed with anhydrous ether. Vacuum drying at 80°C to obtain 29g of serprofen acid tromethamine salt, yield 87.9%, mp: 186-188°C, product verified by four major spectra: uv: maximum absorption at 254nm, maximum absorption at 289nm .

Embodiment 2

[0018] Embodiment 2: the preparation of aclofenac tromethamine salt

[0019] In a 250ml three-necked flask, add 50g of aclofenac to 200ml of methanol. Under the condition of avoiding light, stir and heat up to 30°C, and the mixture dissolves. At this time, add 38g of trometamol, stir until the reaction is clear, and react for 8 hours , TLC identified that the reaction was complete (developing agent: n-hexane: acetone: glacial acetic acid = 10:5:0.2), after the reaction was completed, 60 ml of ether was added, and the mixture was cooled to obtain a white crystalline powder. The solid was filtered by suction and washed with a small amount of ether. Vacuum drying at 50°C yielded 79g, the yield was 89.8%, mp: 110-111°C, the product was confirmed by four major spectra: UV: maximum absorption at 286nm.

Embodiment 3

[0020] Embodiment 3: Solubility experiment of aclofenac tromethamine salt

[0021] Take aclofenac tromethamine salt respectively as shown in Table 1, add corresponding solvents respectively, shake vigorously for 5 seconds every 5 minutes, observe after 30 minutes, the results are shown in Table 1:

[0022] Table 1: Solubility test of aclofenac tromethamine salt

[0023]

[0024] 0.1mol / ml

[0025] The experimental results show that: after the salt formation of aclofenac and tromethamine, it is easily soluble in water, 0.1mol / ml hydrochloric acid, 0.1mol / ml sodium hydroxide, slightly soluble in acetone and ethanol, and insoluble in ether.

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Abstract

Disclosed are non-steroidal analgesic and analgesic anti-inflammatory agents containing carboxyl including sodium, calcium, zinc, magnesium, N-n-octylgucamine, Arginine, Lycine or Trometamol salts of Loxoprofen, Ketoprofen, Pranoprofen, Tiaprofenic acid, Butibufen, Omolofen, epoxy indene acid, Lobuprofen, Clofenamic acid, Clonixin, Fenoprofen, Benorilate, Flurbiprofen, Alminoprofen, Bucloxic acid, Sulindac, Zidometacin, Acemetacin, Ketorolac, Risedronic acid, Sulindac, Lonaprofen, aspirin, Florfenicol, tiaprofenic acid, overall evaluation shows that trometamol salts are the best choice in terms of physicochemical properties, solvability, stability, local irritation, blood vessel irritation, and bioavailability for oral administration.

Description

Technical field: [0001] The invention relates to a carboxyl-containing non-steroidal antipyretic and analgesic salt, a preparation method and application thereof. Background technique: [0002] Inflammation is the most important basic pathological process. When inflammation occurs, local manifestations of redness, swelling, heat, pain and dysfunction may appear, accompanied by systemic symptoms such as elevated body temperature and changes in the number of peripheral blood cells. For the treatment of inflammation, people used glucocorticoid steroidal anti-inflammatory drugs (steroidal anti-inflammatory drugs, SAIDs) in the early days. However, early use can lead to dependence. And it is easy to cause side effects such as adrenal cortex function decline. In the late 1950s, research on nonsteroidal anti-inflammatory drugs (nonsteroidal anti-inflammatory drugs, NSAIDs) was turned, and it rapidly developed into a kind of treatment with many varieties, large quantities, and exc...

Claims

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Application Information

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IPC IPC(8): A61K31/19A61K31/381A61K31/60A61K45/00A61P29/00
Inventor 陈文展
Owner 陈文展
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