Method for preparing aspirin enteric-coated tablet for removing fever, easing pain and resisting inflammation

一种阿司匹林、抗炎药物的技术，应用在医药领域，能够解决用药不方便、水杨酸中毒反应、胃黏膜损伤等问题，达到降低胃肠道不良反应、低游离水杨酸含量的效果

Inactive Publication Date: 2016-10-12
苗怡文
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 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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  • Method for preparing aspirin enteric-coated tablet for removing fever, easing pain and resisting inflammation
  • Method for preparing aspirin enteric-coated tablet for removing fever, easing pain and resisting inflammation
  • Method for preparing aspirin enteric-coated tablet for removing fever, easing pain and resisting inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] The preparation of embodiment 1 aspirin compound

[0047] (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;

[0048] (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;

[0049] (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.

[0050] The obtained aspirin compound was measured by powder X-ray powd...

Embodiment 2

[0051] The preparation of embodiment 2 aspirin compounds

[0052] (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;

[0053] (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;

[0054] (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.

[0055] The obtained aspirin co...

Embodiment 3

[0056] The preparation of embodiment 3 aspirin compounds

[0057] (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;

[0058] (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;

[0059] (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.

[0060] The obtained aspirin compound was measured ...

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Abstract

The invention belongs to the technical field of medicines and relates to a method for preparing an aspirin enteric-coated tablet for removing fever, easing pain and resisting inflammation. An aspirin compound provided by the invention has a new crystal form and is different from aspirin reported in the prior art. Tests discover that compared with the aspirin enteric-coated tablet in the prior art, the aspirin enteric-coated tablet prepared by the method has relatively low free salicylic acid content, and the increase of the free salicylic acid content is not obvious along with the prolonging of the storage time, so that the untoward effects of the medicine to the gastrointestinal tract are greatly reduced.

Description

[0001] This application is an invention patent application filed by the applicant Miao Yiwen (the name of the invention is: an antipyretic, analgesic, anti-inflammatory drug compound and its preparation method, the application number is: 2015102160635, and the application date is: April 30, 2015 day) divisional application. technical field [0002] The invention belongs to the technical field of medicines, and relates to a method for preparing aspirin enteric-coated tablets for antipyretic, analgesic and anti-inflammatory drugs. Background technique [0003] 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 ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/616A61P29/00A61P7/02C07C69/157C07C67/52
CPCA61K9/2059A61K9/284A61K9/2866A61K31/616C07B2200/13C07C67/48C07C67/52C07C69/157
Inventor 于美莉
Owner 苗怡文
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