Aspirin pulsed release pellets, its preparation and preparation method thereof

A technology of aspirin and pulse release, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as easy hydrolysis, unstable gastrointestinal tract, bleeding, and reduced antithrombotic efficacy

Inactive Publication Date: 2012-11-07
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The technical problem to be solved by the present invention is to overcome the problem that aspirin is easily hydrolyzed and unstable and causes gastrointestinal bleeding, while in the prior art, oral chewable tablets have the problem of stimulating the stomach and upper gastrointestinal tract, and enteric-coated tablets have excessive local concentration. High problem, prolonged dissolution time of sustain

Method used

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  • Aspirin pulsed release pellets, its preparation and preparation method thereof
  • Aspirin pulsed release pellets, its preparation and preparation method thereof
  • Aspirin pulsed release pellets, its preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Table 1 Embodiment 1 Aspirin pulse release micropellet each layer raw material composition ratio

[0078] category

Proportion

The composition ratio of each layer

[0079] blank core

11.4

\

drug layer

11.4

drug 30, povidone 60, tartaric acid 3, sodium lauryl sulfate 2, crospovidone 5

Isolation layer

2.2

Hydroxypropyl Methyl Cellulose 80, Macrogol 10, Talc 10

Regulatory release layer

25

Citric acid 30, enteric material 60, triethyl citrate 5, talcum powder 5

The protective layer

50

Sodium chloride 5, enteric-coated material 70, triethyl citrate 10, glyceryl monostearate 15

[0080] Table 2 is the specific type and dosage of each component in Table 1

[0081]

[0082] Note: The adjusted release layer and protective layer in the table are also listed in the raw material formula of pellets I, II and III

[0083] The structure of the aspirin pulse rel...

Embodiment 2

[0106] Table 3 Embodiment 2 Aspirin pulse release micropellet each layer raw material composition ratio

[0107] category

Proportion

The composition ratio of each layer

blank core

11.4

\

drug layer

11.4

Drug 50, Povidone 40, Tartaric Acid 3, Sodium Lauryl Sulfate 2, Crospovidone 5

Isolation layer

2.2

Hydroxypropyl Methyl Cellulose 85, Macrogol 5, Talc 15

Regulatory release layer

25

Citric acid 30, enteric material 60, triethyl citrate 5, talcum powder 5

The protective layer

50

Sodium chloride 0, enteric material 90, triethyl citrate 5, glyceryl monostearate 5

[0108] Table 4 is the specific type and dosage of each component in Table 3

[0109]

[0110]

[0111] Preparation:

[0112] 1. Drug-coated layer: same as in Example 1

[0113] 2. Packet isolation layer: same as embodiment 1

[0114] 3, bag regulating release layer: prepare I, II, III micropill with e...

Embodiment 3

[0119] Table 5 Embodiment 3 aspirin pulse release micropellet each layer raw material composition ratio

[0120] category

Proportion

The composition ratio of each layer

blank core

11.4

\

drug layer

11.4

drug 40, povidone 50, tartaric acid 1, sodium lauryl sulfate 4, crospovidone 5

Isolation layer

2.2

Hydroxypropyl Methyl Cellulose 85, Macrogol 5, Talc 15

Regulatory release layer

25

Citric acid 20, enteric material 60, triethyl citrate 5, talcum powder 15

The protective layer

50

Sodium chloride 0, enteric-coated material 80, triethyl citrate 5, glyceryl monostearate 15

[0121] Table 6 is the specific type and dosage of each component in Table 5

[0122]

[0123]

[0124] Preparation:

[0125] 1. Drug-coated layer: same as in Example 1

[0126] 2. Packet isolation layer: same as embodiment 1

[0127] 3, bag regulating release layer: prepare I, II, III micropill...

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Abstract

The invention discloses aspirin pulsed release pellets, its preparation and a preparation method thereof. The pellets comprise blank pellets, an aspirin-containing drug layer, an isolation layer, a regulation releasing layer and a protective layer. The regulation releasing layer contains polyprotic acid and/or its salt, anionic polymer salt, a plasticizer and an antiadherent. The anionic polymer salt is prepared by the following method: dissolving an enteric material, and using alkali to neutralize to a pH value greater than the enteric material dissolution pH value 0.1-3. The protective layer contains the enteric material, the plasticizer and the antiadherent. The enteric material is any one material selected from: an enteric material dissolved at pH value of 4.5-5.5 to prepare pellets I; an enteric material dissolved at pH value of 6.0-6.5 to prepare pellets II; or an enteric material dissolved at pH value of 7.0-8.0 to prepare pellets III. According to the preparation, local drug concentration will not be high, accumulation of the drug inside the body can be reduced, patient compliance can be improved, and stability inside the body can be raised. Therefore, bioavailability and the antithrombotic effect are raised.

Description

technical field [0001] The invention relates to an aspirin pulse release pellet, its preparation and a preparation method. Background technique [0002] Aspirin is a commonly used drug for cardiovascular diseases and has a huge consumption. At present, in our country, the incidence of cardiovascular and cerebrovascular diseases is increasing year by year. Among the drug prevention measures used, aspirin has shown excellent effects in primary and secondary prevention, which can reduce the incidence and death of myocardial infarction and stroke. risk. Aspirin not only gets attention in routine application, but also gradually expands its scope of application. On October 22, 2010, the famous medical journal "The Lancet" reported the case analysis of 18 years of British doctors, and found that long-term use of low-dose aspirin can reduce the chance of colon cancer by 24%, and the chance of dying from colon cancer by 35%; The 2006 AHA / ASA guidelines for the primary prevention o...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K31/616A61K47/38A61K47/32A61K47/34A61P9/10A61P35/00A61P1/00
Inventor 任麒孟建强
Owner SHANGHAI INST OF PHARMA IND
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