Oral enteric preparation containing Grel drugs and aspirin

Abstract

The invention relates to a novel oral enteric preparation which is composed of 0.1-1000mg of Grel drugs, or medically acceptable salts, ester or derivatives, 37.5-325mg of aspirin and at least one medically acceptable load, wherein the Grel drugs, or medically acceptable salts, esters or derivatives are clopidogrel, prasugrel, brilinta, sarpogrelate, ozagrel, anagrelide, pamicogrel, or medically acceptable salts, ester or derivatives, preferably, clopidogrel sulfate. The oral enteric preparation is used for curing acute coronary syndrome (ACS), angor pectoris, stroke, myocardial infarction or cardia cerebrovascular diseases of patients. According to the oral enteric preparation, adverse reactions such as functional gastrointestinal disorders, nausea, vomit, gastritis, concealed hemorrhage, ulcer exacerbation and gastrointestinal bleeding caused by strong stimulus of aspirin to stomach can be avoided.

Description

technical field

[0001] The present invention relates to a novel oral enteric-coated preparation, which consists of 0.1-1000mg of gray drug or its pharmaceutically acceptable salt or ester or its derivative, 37.5-325mg of aspirin and at least one pharmaceutically acceptable The composition of the carrier is used for preventing, delaying the progress or treating patients with acute coronary syndrome, angina pectoris, stroke, myocardial infarction, ischemic disease or cardiovascular and cerebrovascular diseases, and belongs to the field of medical technology. Background technique

[0002] Cardiovascular disease, including coronary heart disease, stroke or peripheral vascular disease, is the main cause of human death. Cardiovascular disease has been the first cause of death in my country since 1990. The 2008 "Statistical Bulletin on China's Health Development" shows that the number of deaths caused by cardiovascular disease has accounted for 40.27% of the total number of deaths ...

Examples

Embodiment 1

[0132] Example 1: Enteric-coated tablet comprising clopidogrel bisulfate and aspirin

[0133] 1.1. Preparation of tablet core: direct compression method

[0134] Name of raw material

Dose 1 (mg)

Dose 2 (mg)

Clopidogrel bisulfate

97.875

97.875

aspirin

75.00

150.00

corn starch

30.50

30.50

Mannitol

198.215

113.835

Micropowder silica gel

2.05

2.05

microcrystalline cellulose

60.80

60.80

tartaric acid

9.38

18.76

Carboxymethyl Starch Sodium

15.00

15.00

hydrogenated castor oil

8.08

8.08

stearic acid

3.10

3.10

Sheet weight

500

500

[0135] Preparation:

[0136] (A) Pass various solid raw and auxiliary materials through 80-100 mesh sieves respectively, and set aside;

[0137] (B) the clopidogrel bisulfate of prescription quantity and micropowder silica gel...

Embodiment 2

[0145] Example 2: Enteric-coated tablet comprising clopidogrel bisulfate and aspirin

[0146] 2.1. Preparation of tablet core: direct compression method

[0147] Name of raw material

[0148] The preparation method of the tablet core is the same as in Example 1, with citric acid replacing tartaric acid.

[0149] 2.2. Preparation of enteric-coated tablets:

[0150] Name of coating excipients

[0151] Talc powder

[0152] Preparation method: take hypromellose phthalate and add about 200g of purified water, stir well; add phthalate and talcum powder in the remaining purified water, homogenize in a homogenizer for 45 minutes; suspend the above talcum powder The solution is slowly poured into the aqueous dispersion of hypromellose phthalate, and stirred slowly for 30 minutes; the prepared coating solution is filtered through an 80-mesh screen; 80°C, tablet bed temperature 30-35°C, atomization pressure 1.5bar, coating pan rotation speed 15-25 rpm, sam...

Embodiment 3

[0153] Example 3: Enteric-coated tablet comprising clopidogrel bisulfate and aspirin

[0154] 3.1. Preparation of tablet core: direct compression method

[0155] Name of raw material

[0156] The preparation method of tablet core is the same as embodiment 1.

[0157] 3.2. Preparation of enteric-coated tablets:

[0158] Name of coating excipients

[0159] Preparation method: Take acrylic resin Eudragit L and add about 200g of purified water, stir well; add PEG6000 and talcum powder in the remaining purified water, homogenize in a homogenizer for 45 minutes; slowly pour the above talcum powder suspension into acrylic resin Eudragit L In the water dispersion, stir slowly for 30 minutes; filter the prepared coating solution through an 80-mesh sieve; add 500g of tablet cores to the coating pan, adjust the inlet air temperature to 80°C, the tablet bed temperature to 30-35°C, and atomize The pressure is 1.5 bar, the rotating speed of the coating pan is 15-25 rpm...

technical field

[0001] The present invention relates to a novel oral enteric-coated preparation, which consists of 0.1-1000mg of gray drug or its pharmaceutically acceptable salt or ester or its derivative, 37.5-325mg of aspirin and at least one pharmaceutically acceptable The composition of the carrier is used for preventing, delaying the progress or treating patients with acute coronary syndrome, angina pectoris, stroke, myocardial infarction, ischemic disease or cardiovascular and cerebrovascular diseases, and belongs to the field of medical technology. Background technique

[0002] Cardiovascular disease, including coronary heart disease, stroke or peripheral vascular disease, is the main cause of human death. Cardiovascular disease has been the first cause of death in my country since 1990. The 2008 "Statistical Bulletin on China's Health Development" shows that the number of deaths caused by cardiovascular disease has accounted for 40.27% of the total number of deaths ...

Examples

Embodiment 1

[0132] Example 1: Enteric-coated tablet comprising clopidogrel bisulfate and aspirin

[0133] 1.1. Preparation of tablet core: direct compression method

[0134] Name of raw material

Dose 1 (mg)

Dose 2 (mg)

Clopidogrel bisulfate

97.875

97.875

aspirin

75.00

150.00

corn starch

30.50

30.50

Mannitol

198.215

113.835

Micropowder silica gel

2.05

2.05

microcrystalline cellulose

60.80

60.80

tartaric acid

9.38

18.76

Carboxymethyl Starch Sodium

15.00

15.00

hydrogenated castor oil

8.08

8.08

stearic acid

3.10

3.10

Sheet weight

500

500

[0135] Preparation:

[0136] (A) Pass various solid raw and auxiliary materials through 80-100 mesh sieves respectively, and set aside;

[0137] (B) the clopidogrel bisulfate of prescription quantity and micropowder silica gel...

Embodiment 2

[0145] Example 2: Enteric-coated tablet comprising clopidogrel bisulfate and aspirin

[0146] 2.1. Preparation of tablet core: direct compression method

[0147] Name of raw material

[0148] The preparation method of the tablet core is the same as in Example 1, with citric acid replacing tartaric acid.

[0149] 2.2. Preparation of enteric-coated tablets:

[0150] Name of coating excipients

[0151] Talc powder

[0152] Preparation method: take hypromellose phthalate and add about 200g of purified water, stir well; add phthalate and talcum powder in the remaining purified water, homogenize in a homogenizer for 45 minutes; suspend the above talcum powder The solution is slowly poured into the aqueous dispersion of hypromellose phthalate, and stirred slowly for 30 minutes; the prepared coating solution is filtered through an 80-mesh screen; 80°C, tablet bed temperature 30-35°C, atomization pressure 1.5bar, coating pan rotation speed 15-25 rpm, sam...

Embodiment 3

[0153] Example 3: Enteric-coated tablet comprising clopidogrel bisulfate and aspirin

[0154] 3.1. Preparation of tablet core: direct compression method

[0155] Name of raw material

[0156] The preparation method of tablet core is the same as embodiment 1.

[0157] 3.2. Preparation of enteric-coated tablets:

[0158] Name of coating excipients

[0159] Preparation method: Take acrylic resin Eudragit L and add about 200g of purified water, stir well; add PEG6000 and talcum powder in the remaining purified water, homogenize in a homogenizer for 45 minutes; slowly pour the above talcum powder suspension into acrylic resin Eudragit L In the water dispersion, stir slowly for 30 minutes; filter the prepared coating solution through an 80-mesh sieve; add 500g of tablet cores to the coating pan, adjust the inlet air temperature to 80°C, the tablet bed temperature to 30-35°C, and atomize The pressure is 1.5 bar, the rotating speed of the coating pan is 15-25 rpm...

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