Medicinal composition for treating cerebrovascular disease

A composition and cardiovascular technology, applied in cardiovascular system diseases, drug combination, drug delivery, etc., can solve the problems of affecting coronary artery perfusion, accelerating myocardial cell apoptosis, and having no therapeutic effect, so as to achieve low therapeutically effective dose and reduce Myocardial oxygen consumption, the effect of reducing angioedema and dry cough

Inactive Publication Date: 2008-04-30
BEIJING JINCHENG TAIER PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When used to treat angina-type coronary heart disease, its current clinical dosage is 16 mg per day. The therapeutic effect is obvious, but it also has side effects. Perfusion, causing reflex tachycardia, clinical symptoms manifested as chest tightness, headache, back pain, etc.
[0004] In the prior art, there is no attempt or related report on the combined use of bisoprolol and candesartan to treat cardiovascular diseases, and there is no related report that the combined use of the two has outstanding therapeutic effects

Method used

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  • Medicinal composition for treating cerebrovascular disease
  • Medicinal composition for treating cerebrovascular disease
  • Medicinal composition for treating cerebrovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] According to the following formula, it is pressed with the production process of the tablet, and the dispersible tablet meeting the quality standard is obtained:

[0052] Recipe 1

[0053] Bisoprolol Fumarate 3g Candesartan Medoxil 4g

[0054] Microcrystalline Cellulose 100g Cross-linked PVP 60g

[0055] Poloxamer 9g PVP 3g

[0056] Ethanol 80ml Magnesium stearate 1.2g

[0057]

[0058] 180.2g

[0059] Made into 1000 pieces, each weighing 0.18g

[0060] Recipe 2

[0061] Bisoprolol Fumarate 2.5g Candesartan Medoxil 3.5g

[0062] Microcrystalline Cellulose 120g Cross-linked PVP 50g

[0063] Poloxamer 9g PVP 3g

[0064] Ethanol 80ml Magnesium stearate 1.2g

[0065]

[0066] 189.2g

[0067] Made into 1000 pieces, each weighing 0.19g

[0068] Recipe 3

[0069]...

Embodiment 2

[0100] Embodiment 2: the acute toxicity research of compound preparation

[0101] Test drug : Compound dispersible tablet containing 3 mg of bisoprolol fumarate (equivalent to 2.5 mg of bisoprolol), 4.2 mg of candesartan cilexetil (equivalent to 3 mg of candesartan)

[0102] high dose: Each rabbit is administered once a day, and the dosage is equivalent to 5.76mg of the drug ingredient, with an average of 2.4mg / kg, which is 20 times the dosage for humans;

[0103] medium dose : Each rabbit is administered once a day, and the dosage is equivalent to 2.88mg of the drug ingredient, with an average of 1.2mg / kg, which is 9.5 times the dosage for humans;

[0104] low dose : Each rabbit is administered once a day, and the dosage is equivalent to 1.44mg of the drug ingredient, with an average of 1.2mg / kg, which is 3.8 times the dosage for humans;

[0105] negative control : blank supplementary tablet of compound dispersible tablet, which does not contain drug ingredients,

...

Embodiment 3

[0113] Embodiment 3: the long-term toxicity study of the topical administration of compound preparation

[0114] Test drug : same as embodiment 2

[0115] high dose : Each rat is given a single dose of 1.152 mg of drug ingredients, with an average of 4.8 mg / kg, which is 40 times the amount used by humans;

[0116] medium dose : Each rat is given a single dose of 0.576 mg of drug ingredients, with an average of 2.4 mg / kg, which is 20 times the amount used by humans;

[0117] low dose : Each rat is given a single dose of 0.288 mg of drug ingredients, with an average of 1.2 mg / kg, which is 10 times the amount used by humans;

[0118] The weight of rats is 0.236~0.264kg

[0119] Three doses were administered once a day, observed continuously for 30 days, and repeated the test three times. As a result, the whole body of the animal had no obvious changes; the anatomical observations were executed by dislocation, and there were no significant changes in kidney, liver, liver ...

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Abstract

A composite medicine in the various forms for treating cardiovascular disease such as coronary heat disease, hypertension, etc is prepared from bisoprolol and candesartan in the mole ratio of 1: (1-2).

Description

field of invention [0001] The invention relates to a pharmaceutical composition, in particular to a pharmaceutical composition for treating cardiovascular diseases, which uses bisoprolol and candesartan as active ingredients. Background technique [0002] Bisoprolol is a selective β1-adrenergic receptor blocker, a highly selective β1-receptor blocker, without intrinsic sympathomimetic activity and membrane stabilizing effect, and inhibits by competing with adrenergic β1-receptors The cardiovascular effects of catecholamines result in a decrease in cardiac contractility and contraction velocity, slowing conduction and heart rate, reducing myocardial oxygen consumption, and improving myocardial exercise endurance. It is clinically used to treat hypertension and heart failure coronary heart disease; when used to lower blood pressure, its current clinical dosage is 5 mg per day, and the antihypertensive effect is relatively obvious, but it is still not very ideal, and there are ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/41A61K31/138A61K9/20A61K9/48A61K9/14A61K9/08A61K9/10A61P9/00
Inventor 杨军
Owner BEIJING JINCHENG TAIER PHARMA CO LTD
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