Medicinal composition containing clopidogrel and aspirin and application thereof to preparation of medicaments for treating acute non-disabling cerebrovascular diseases

A technology of aspirin and clopidogrel, applied in drug combinations, medical preparations containing active ingredients, cardiovascular system diseases, etc., can solve problems such as unsatisfactory effects, inconvenience, and heavy burden on patients, and achieve simple and convenient compliance Effect

Active Publication Date: 2011-07-20
BEIJING TIANTAN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] 1. The treatment method is single and the effect is not ideal;
[0012]2. The use of infusion therapy is heavy on the patient and inconvenient

Method used

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  • Medicinal composition containing clopidogrel and aspirin and application thereof to preparation of medicaments for treating acute non-disabling cerebrovascular diseases
  • Medicinal composition containing clopidogrel and aspirin and application thereof to preparation of medicaments for treating acute non-disabling cerebrovascular diseases
  • Medicinal composition containing clopidogrel and aspirin and application thereof to preparation of medicaments for treating acute non-disabling cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Compound matrix sustained-release tablet of embodiment 1 aspirin and clopidogrel bisulfate

[0024] Aspirin 75mg

[0025] Clopidogrel 75mg

[0026] Hypromellose 150mg

[0027] Lactose 50mg

[0028]Magnesium stearate 3~6mg

[0029] Proper amount of hypromellose ethanol solution

[0030] Preparation process: crush aspirin, clopidogrel, and hydroxypropylmethylcellulose, a matrix sustained-release material, and sieve. 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.

[0031] Determination of the release rate of sustained-release ta...

Embodiment 2

[0034] Example 2 Observational study of combined application of antiplatelet drugs in patients with TIA and minor ischemic stroke

[0035] (1) A randomized double-blind study design is adopted:

[0036] 1. Inclusion criteria for observational studies of combined use of antiplatelet drugs in patients with TIA and minor ischemic stroke:

[0037] 1) Adults, male or female, aged ≥ 40 years;

[0038] 2) Non-disabling ischemic stroke (NIHSS ≤ 3 points on admission), and the study drug can be used within 24 hours of symptom onset. The time to symptom onset was defined as "the time when it last appeared normal".

[0039] 3) Those with medium-to-high risk of stroke (ABCD at admission 2 Patients with TIA (focal cerebral or retinal ischemia-induced neurological dysfunction, which completely disappears within 24 hours) with a score ≥ 4), and the study drug can be used within 24 hours of symptom onset. The time to symptom onset was defined as "the time when it last appeared normal".

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PUM

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Abstract

The invention discloses a medicinal composition containing clopidogrel and aspirin. The medicinal composition is characterized by comprising the clopidogrel and the aspirin serving as active ingredients, wherein the medicinal composition is prepared in the dose unit that every unit dose of preparation contains 75mg of active ingredients; and both ingredients exist in a free state or pharmaceutically acceptable salt forms. The invention discloses application of the composition to preparation of medicaments for treating an acute non-disabling cerebrovascular disease. The invention has the advantages that: 1, a patient can be easily and conveniently treated by using an oral medicament and has high compliance; and 2, compared with single use of aspirin, the technical scheme of the invention is of great benefit to the patient with the acute non-disabling cerebrovascular diseases without increasing the bleeding rate.

Description

technical field [0001] The present invention relates to the subject of the present invention is a novel combination of active ingredients consisting of clopidogrel and aspirin with antiplatelet aggregation activity, and the use of pharmaceutical compositions containing them. Background technique [0002] Clopidogrel is a platelet aggregation inhibitor. ATC classification is: BO1AC / 04. Clopidogrel also selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GP111b / 111a complex, thereby inhibiting aggregation to platelets, clopidogrel Gray must be biotransformed to inhibit platelet aggregation. 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. [0003] Aspirin, also known as acetylsalicylic acid, has antipyretic, analgesi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/616A61K31/4365A61P9/10A61P7/02
Inventor 王拥军赵性泉王伊龙周永
Owner BEIJING TIANTAN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV
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