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Compound sustained-release preparation of aspirin and clopidogrel or pharmaceutically acceptable salt thereof

A sustained-release preparation, clopidogrel technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., to achieve the effects of reducing drug concentration, avoiding peak and valley phenomena, and avoiding nausea

Inactive Publication Date: 2010-05-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] At present, there are no products or related reports on the market that make the compound composition of aspirin and clopidogrel or its salts into sustained-release preparations

Method used

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  • Compound sustained-release preparation of aspirin and clopidogrel or pharmaceutically acceptable salt thereof
  • Compound sustained-release preparation of aspirin and clopidogrel or pharmaceutically acceptable salt thereof
  • Compound sustained-release preparation of aspirin and clopidogrel or pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0044] The compound matrix sustained-release tablet of example 1 aspirin and clopidogrel bisulfate

[0045] Aspirin 75mg

[0046] Clopidogrel Bisulfate 97.875mg

[0047] Hypromellose 150mg

[0048] Lactose 50mg

[0049] Magnesium stearate 3~6mg

[0050] Proper amount of hypromellose ethanol solution

[0051] Preparation process: aspirin, clopidogrel bisulfate, and hydroxypropylmethylcellulose, a matrix slow-release material, are pulverized and sieved. Weigh the prescribed amount of aspirin, clopidogrel hydrogen sulfate and mix them with hypromellose and lactose respectively, then add the ethanol solution of hypromellose respectively, mix to make soft material, and granulate with 24-30 nylon sieve. Ventilate and dry at a temperature of 40°C to 50°C for 1.5 to 2.5 hours, granulate, then mix aspirin sustained-release granules and clopidogrel bisulfate sustained-release granules, add magnesium stearate, and compress into tablets to obtain.

[0052] Determination of the relea...

example 2

[0053] Example 2 Compound aspirin / clopidogrel double-layer matrix sustained-release tablet

[0054] Aspirin extended-release portion:

[0055] Aspirin 150mg

[0056] HPMC K4M 110mg

[0057] Citric acid 7.5mg

[0058] Talc powder 10mg

[0059] Appropriate amount of PVP ethanol solution

[0060] Clopidogrel extended-release fraction:

[0061] Clopidogrel 75mg

[0062] Pregelatinized starch 40mg

[0063] HPMC K15M 70mg

[0064] Magnesium stearate 6~8mg

[0065] Appropriate amount of PVP ethanol solution

[0066] Preparation process: aspirin slow-release part: weigh the prescribed amount of aspirin, HPMC K4M , citric acid, and set aside; clopidogrel slow-release part: the prescribed amount of clopidogrel bisulfate, pregelatinized starch, HPMC K15M Mix evenly and set aside; add PVP ethanol solution to the aspirin slow-release part and clopidogrel slow-release part respectively, mix to make a soft material, granulate with 24-30 nylon sieve, and ventilate an...

example 3

[0068] Example 3 Compound aspirin / clopidogrel bisulfate double-layer matrix sustained-release tablet

[0069] Aspirin 150mg

[0070] HPMC K15M 100mg

[0071] Citric acid 5mg

[0072] Talc powder 8mg

[0073] Clopidogrel Bisulfate 97.875mg

[0074] Microcrystalline Cellulose 20mg

[0075] Pregelatinized starch 60mg

[0076] Crospovidone (PVPP) 15mg

[0077] Zinc stearate 3~6mg

[0078] Preparation process: aspirin, HPMC K15M , citric acid, and talcum powder were mixed uniformly by equal increment method, and set aside; the prescribed amount of clopidogrel bisulfate, pregelatinized starch, microcrystalline cellulose, PVPP zinc stearate were uniformly mixed by equal increment method , ready for use; first pre-compress the aspirin slow-release part, then pour into the clopidogrel bisulfate immediate-release part, press into tablets, and obtain.

[0079] Determination of the release rate of sustained-release tablets: according to the first method of dissolut...

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PUM

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Abstract

The invention relates to a sustained-release preparation of a compound composite, in particular to a compound sustained-release preparation of aspirin and clopidogrel or an pharmaceutically acceptable salt thereof, comprising a basic remedy, an auxiliary material with sustained-release function and other auxiliary materials, wherein the mass ratio of the basic remedy to the auxiliary material with the sustained-release function is 1:0.01-1:20, and the mass ratio of the aspirin to the clopidogrel or the acceptable salt thereof is 0.1:1-10:1. The compound composite is used for preventing and treating diseases caused by platelet aggregation, and the sustained-release preparation prepared by the compound composite can reduce stimulation effect of medicaments on the gastrointestinal tract, improves patient compliance, avoids peak valley phenomenon in the blood after common preparations are taken, lowers the occurrence of adverse reaction, and enhances medication safety and curative effect, thereby achieving stable effects with sustainable action.

Description

Technical field: [0001] The invention relates to a sustained-release preparation of a compound composition, that is, a compound sustained-release preparation of aspirin and clopidogrel or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique: [0002] Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPlllb / llla complex, thereby inhibiting platelet aggregation. In addition to ADP, clopidogrel also inhibits platelet aggregation induced by other agonists by blocking the expansion of platelet activation caused by released ADP. Clopidogrel does not inhibit the activity of phosphodiesterase. Clopidogrel acts by irreversibly modifying platelet ADP receptors. [0003] Clopidogrel, molecular formula: C 16 h 16 ClNO 2 S, molecular weight: 321.82, chemical structure as follows: [0004] [0005] product name Clopidogre...

Claims

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Application Information

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IPC IPC(8): A61K31/616A61K31/4365A61K9/22A61K9/52A61P7/02
Inventor 王东凯王玉李翔
Owner SHENYANG PHARMA UNIVERSITY
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