Antipyretic analgesic anti-inflammatory aspirin composition tablet

A technology of aspirin and anti-inflammatory drugs, applied in the field of medicine, can solve the problems of inconvenient medication, salicylic acid poisoning reaction, gastrointestinal bleeding, etc., achieve low free salicylic acid content, and reduce the effect of gastrointestinal adverse reactions

Inactive Publication Date: 2016-01-13
QINGDAO HUAZHICAO PHARMA CO LTD
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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 anti-inflammatory aspirin composition tablet
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  • Antipyretic analgesic anti-inflammatory aspirin composition tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of aspirin crystals

[0030] (1) Grind the crude aspirin, pass it through a 60-mesh sieve, and then add it to a mixed solution of ether and chloroform whose volume is 8 times the weight of aspirin. The volume ratio of ether and chloroform is 2:3, 130 rpm / min stirring for 10 minutes;

[0031] (2) Add ethanol with a volume 3 times the weight of aspirin under stirring at 90 rpm, and raise the temperature to 30°C at the same time;

[0032] (3) After adding the solution, let it stand still for 3 hours, add distilled water at 0°C with a volume 8 times the weight of aspirin dropwise under the condition of stirring at 150 rpm, and finish adding dropwise at a uniform speed within 2 hours;

[0033] (4) After the dropwise addition, cool down to -15°C, continue to stir at a stirring rate of 110 rpm for 2 hours, let stand for 1 hour to precipitate crystals, filter, wash, and vacuum dry to obtain aspirin crystals.

[0034] The X-ray powder diffraction pat...

Embodiment 2

[0035] Example 2: Preparation of aspirin tablets

[0036] Prescription: 5 parts by weight of aspirin prepared in Example 1, 7.3 parts by weight of microcrystalline cellulose, 5.4 parts by weight of lactose, 3 parts by weight of sodium starch glycolate, 0.15 parts by weight of nicotinamide, and 0.3 parts by weight of povidone K30, 4 parts by weight of 95% ethanol, and 0.4 parts by weight of magnesium trisilicate.

[0037] Preparation:

[0038] (1) Processing of raw and auxiliary materials: sieve aspirin to 100 mesh, sieve carboxymethyl starch sodium and nicotinamide to 80 mesh;

[0039] (2) Weighing: Weighing according to the prescription;

[0040] (3) Adhesive preparation: dissolve the prescribed amount of povidone K30 in 95% ethanol and set aside;

[0041] (4) Granulation: Add aspirin, microcrystalline cellulose, lactose, carboxymethyl starch sodium, and nicotinamide into the wet mixing granulator, dry mix for 10 minutes, add the prepared binder, wet mix and cut 150 -18...

Embodiment 3

[0046] Example 3: Preparation of aspirin tablets

[0047] Prescription: 5 parts by weight of aspirin prepared in Example 1, 7.4 parts by weight of microcrystalline cellulose, 5.5 parts by weight of lactose, 4 parts by weight of sodium starch glycolate, 0.2 parts by weight of nicotinamide, and 0.4 parts by weight of povidone K30, 5 parts by weight of 95% ethanol, and 0.5 parts by weight of magnesium trisilicate.

[0048] Preparation:

[0049] (1) Processing of raw and auxiliary materials: sieve aspirin to 100 mesh, sieve carboxymethyl starch sodium and nicotinamide to 80 mesh;

[0050] (2) Weighing: Weighing according to the prescription;

[0051] (3) Adhesive preparation: dissolve the prescribed amount of povidone K30 in 95% ethanol and set aside;

[0052] (4) Granulation: Add aspirin, microcrystalline cellulose, lactose, carboxymethyl starch sodium, and nicotinamide into the wet mixing granulator, dry mix for 10 minutes, add the prepared binder, wet mix and cut 150 -180...

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PUM

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Abstract

The invention discloses an antipyretic analgesic anti-inflammatory aspirin composition tablet and belongs to the technical field of medicine. A composition is prepared from aspirin, microcrystalline cellulose, lactose, carboxymethyl starch sodium, nicotinamide, povidone K30, 95% ethyl alcohol and magnesium trisilicate. The aspirin is a novel crystalline compound and is different from aspirin reported in the prior art, and an X-ray powder diffraction pattern shown as figure 1 is obtained by means of measurement with Cu-Kalpha rays. Through experiments, compared with an aspirin tablet in the prior art, the tablet prepared from the novel aspirin crystalline compound has the advantages that the tablet contains low free salicylic acid content, the content of the free salicylic acid is increased unobviously along with storage time prolongation, and adverse effect of the tablet on the gastrointestinal tract is lowered greatly.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to an antipyretic, analgesic and anti-inflammatory drug aspirin composition tablet. 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, inhibits platelet function, has no dose-related effect, and can quickly achieve the inhibitory effect 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 and 75-150 mg / day for secondary prevention. [0003] There are two main problems in the existing...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/616C07C69/157A61P29/00
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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