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Antipyretic, analgesic and anti-inflammatory medicine compound and preparation method thereof

An anti-inflammatory drug and compound technology, applied in the field of medicine, can solve the problems of inconvenient medication, salicylic acid poisoning, gastrointestinal bleeding, etc., and achieve the effects of low free salicylic acid content and reducing gastrointestinal adverse reactions

Active Publication Date: 2015-07-08
启东市和洪农副产品专业合作社
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There are two main problems in the existing aspirin preparations: easily hydrolyzed to produce salicylic acid and cause gastrointestinal bleeding
Although people have improved the dosage form, such as adding suppositories to avoid contact between the drug and the gastrointestinal tract, it is extremely inconvenient to use the drug; Some of the tablets will leak, which will stimulate the stomach and cause damage to the gastric mucosa; if the content of free salicylic acid in the enteric-coated tablets is high, it will cause salicylic acid poisoning, which has not been fundamentally solved question

Method used

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  • Antipyretic, analgesic and anti-inflammatory medicine compound and preparation method thereof
  • Antipyretic, analgesic and anti-inflammatory medicine compound and preparation method thereof
  • Antipyretic, analgesic and anti-inflammatory medicine compound and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0033] The preparation of embodiment 1 aspirin compound

[0034] (1) Add the aspirin crude product to a mixed solution of absolute ethanol, ethyl acetate, and cyclohexane whose volume is 5 times the weight of aspirin, and the volume ratio of absolute ethanol, ethyl acetate, and cyclohexane is: 4.5: 1.5:1, heat up to 35°C, stir until completely dissolved;

[0035] (2) In a sound field with a frequency of 25KHz and an output power of 40W, add a mixed solution of ether and water whose volume is 10 times the weight of aspirin while stirring. The volume ratio of ether and water is 1:3.5, and the stirring speed is 150 rpm / min, adding speed is 80ml / min;

[0036] (3) After adding the mixed solution of ether and water, under a sound field with a frequency of 15KHz and an output power of 10W, cool down to 0-2°C at a rate of 2°C / hour, grow crystals for 3 hours, wash, and dry in vacuum to obtain aspirin compound.

[0037] The obtained aspirin compound was measured by powder X-ray powd...

Embodiment 2

[0038] The preparation of embodiment 2 aspirin compounds

[0039](1) Add the aspirin crude product to a mixed solution of absolute ethanol, ethyl acetate, and cyclohexane whose volume is 6 times the weight of aspirin, and the volume ratio of absolute ethanol, ethyl acetate, and cyclohexane is: 4.5: 1.5:1, heat up to 40°C, stir until completely dissolved;

[0040] (2) In a sound field with a frequency of 27.5KHz and an output power of 50W, add a mixed solution of ether and water whose volume is 12.5 times the weight of aspirin while stirring. The volume ratio of ether and water is 1:3.5, and the stirring speed is 205 rev / min, adding speed is 100 ml / min;

[0041] (3) After adding the mixed solution of ether and water, under a sound field with a frequency of 17.5KHz and an output power of 15W, the temperature was lowered to 0-2°C at a rate of 3°C / hour, the crystal was grown for 4.5 hours, washed, and dried in vacuum to obtain Aspirin compound.

[0042] The obtained aspirin com...

Embodiment 3

[0043] The preparation of embodiment 3 aspirin compounds

[0044] (1) Add the aspirin crude product to a mixed solution of absolute ethanol, ethyl acetate, and cyclohexane whose volume is 7 times the weight of aspirin, and the volume ratio of absolute ethanol, ethyl acetate, and cyclohexane is: 4.5: 1.5:1, heat up to 45°C, stir until completely dissolved;

[0045] (2) In a sound field with a frequency of 30KHz and an output power of 60W, add a mixed solution of ether and water whose volume is 15 times the weight of aspirin while stirring. The volume ratio of ether and water is 1:3.5, and the stirring speed is 260 rpm / min, adding speed is 120ml / min;

[0046] (3) After adding the mixed solution of ether and water, under a sound field with a frequency of 20KHz and an output power of 20W, the temperature is lowered to 0-2°C at 4°C / hour, the crystal is grown for 6 hours, washed, and dried in vacuum to obtain aspirin compound.

[0047] The obtained aspirin compound was measured ...

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Abstract

The invention belongs to the technical field of medicine, and relates to an antipyretic, analgesic and anti-inflammatory medicine compound and a preparation method thereof, in particular to a novel aspirin compound and a preparation method thereof. The aspirin compound has the X-ray powder diffraction spectrum shown in drawing 1. The aspirin compound is a novel crystal form aspirin compound which is different from aspirin reported in the prior art. Experiments show that compared with aspirin enteric coated tablets in the prior art, enteric coated tablets prepared through the novel crystal form aspirin compound have the low free salicylic acid concentration, the free salicylic acid concentration of the enteric coated tablets prepared through the novel crystal form aspirin compound is not obviously increased while the storage time is prolonged, and adverse gastrointestinal tract effects of medicine are greatly reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to an antipyretic, analgesic and anti-inflammatory drug compound and a preparation method thereof, in particular to a novel aspirin compound and a preparation method thereof. Background technique [0002] Aspirin (aspirin), also known as acetylsalicylic acid, is one of the three classic drugs in history. It is an anti-inflammatory drug for pain and is a standard preparation for comparing and evaluating other drugs. Since the 1960s, pharmacological studies have shown that aspirin persistently inactivates COX-1 activity and inhibits platelet function without dose-related effects, and the inhibitory effect can be quickly achieved at a very low concentration (nmol / L), that is, it has a clear anticoagulant effect Blood effect, so it can be used as a drug to prevent blood clots. The "Chinese Expert Consensus" recommends a long-term dose of aspirin of 75-100 mg / day for primary prevention a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/157C07C67/52C07C67/48A61K31/616A61P29/00A61P19/02A61P7/02A61P19/04
CPCA61K9/2059A61K9/284A61K9/2866A61K31/616C07B2200/13C07C67/48C07C67/52C07C69/157
Inventor 于美莉
Owner 启东市和洪农副产品专业合作社