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Multi-cascade antihypertensive drug composition containing folic acid

A composition and drug technology, applied in the field of pharmacy, can solve problems such as hypokalemia, short half-life of CCB, inconvenience for patients, etc., and achieve the effects of preventing stroke, enhancing protection, and delaying stroke

Inactive Publication Date: 2017-01-11
SHENZHEN AUSA PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the short half-life of some CCBs, the first-pass effect is relatively large, so the number of doses is more, causing inconvenience to patients
In 2003, the European Society of Cardiology reported that in 9 pilot studies including 67435 randomized patients, the efficacy of CCB and traditional drugs were compared, and the evaluation indicators included total mortality, cardiovascular mortality, all cardiovascular events, myocardial infarction and For all prognostic indicators including heart failure, no obvious advantage of CCB was found in the results, which is related to the limited antihypertensive effect of CCB alone
Long-term use of the above-mentioned ARBs can easily lead to hyperkalemia, while thiazide diuretics have natriuretic, diuretic and potassium-excreting effects, and long-term use can easily cause hypokalemia

Method used

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  • Multi-cascade antihypertensive drug composition containing folic acid
  • Multi-cascade antihypertensive drug composition containing folic acid
  • Multi-cascade antihypertensive drug composition containing folic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: Preparation of Compound Amlodipine 5mg / Valsartan 80mg / Indapamide 2.5mg / Folic Acid 0.4mg

[0054] prescription:

[0055]

[0056] Preparation Process:

[0057] (1) Take the prescribed amount of amlodipine, valsartan, indapamide, and folic acid, pass through a 100-mesh sieve, and mix them uniformly by the method of equal increments;

[0058] (2) Other auxiliary materials are passed through a 100-mesh sieve and dried at 75°C for 2 hours;

[0059] (3) Mix the microcrystalline cellulose, starch and carboxymethyl starch sodium according to the prescription amount, and then mix them with the mixed raw material drugs in equal increments;

[0060] (4) Make soft materials with an appropriate amount of 5% povidone K-30, granulate with a 24-mesh sieve, granulate with a 20-mesh sieve, and dry at 40-45°C;

[0061] (5) Add an appropriate amount of magnesium stearate to the dry granules, mix them evenly, and compress them into tablets after content determination.

Embodiment 2

[0062] Example 2: Preparation of Compound Amlodipine 5mg / Irbesartan 150mg / Indapamide 2.5mg / Folic Acid 0.4mg

[0063] prescription:

[0064]

[0065] Preparation Process:

[0066] (1) Take the prescribed amount of amlodipine, irbesartan, indapamide, and folic acid, pass through a 100-mesh sieve, and mix them uniformly by the method of equal increments;

[0067] (2) Other auxiliary materials are passed through a 100-mesh sieve and dried at 75°C for 2 hours;

[0068] (3) Mix the microcrystalline cellulose, starch and carboxymethyl starch sodium according to the prescription amount, and then mix them with the mixed raw material drugs in equal increments;

[0069] (4) Make soft materials with an appropriate amount of 5% povidone K-30, granulate with a 24-mesh sieve, granulate with a 20-mesh sieve, and dry at 40-45°C;

[0070] (5) Add an appropriate amount of magnesium stearate to the dry granules, mix them evenly, and compress them into tablets after content determination.

Embodiment 3

[0071] Example 3: Preparation of Compound Nicardipine 65mg / Telmisartan 20mg / Hydrochlorothiazide 10mg / Folic Acid 0.8mg

[0072] prescription:

[0073]

[0074] Preparation Process:

[0075] (1) Get the nicardipine, telmisartan, hydrochlorothiazide, folic acid of prescription quantity, after crossing 100 mesh sieves, mix uniformly by the method of equal increments for subsequent use;

[0076] (2) Other auxiliary materials are passed through a 100-mesh sieve and dried at 75°C for 2 hours;

[0077] (3) mix the microcrystalline cellulose, starch, carboxymethyl starch sodium according to the prescription amount and then mix with the mixed raw material drug in equal increments;

[0078] (4) Make soft material with an appropriate amount of 5% povidone K-30, granulate with 24 mesh sieve, granulate with 20 mesh sieve, and dry at 40-45°C;

[0079] (5) Add an appropriate amount of magnesium stearate to the dry granules, mix them evenly, and compress them into tablets after content d...

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PUM

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Abstract

The invention relates to a drug composition. The drug composition consists of an effective treating amount of calcium antagonist (CCB), an angiotensin II receptor blocker (ARB), a thiazide diuretic, a folic acid compound and a pharmaceutically acceptable carrier, wherein the content of the CCB is 2-240 mg, the content of the ARB is 4-600 mg, the content of the thiazide diuretic is 0.625-25 mg, and the content of the folic acid compound is 0.4-0.4 mg. The drug composition has the advantages that the drug composition can effectively improve the treatment effect of reducing blood pressure of class-2 and class-3 hypertensive patients, strengthen the effect of protecting target organs of the patients and reduce the occurrence risk of cerebral apoplexy complications caused by high blood pressure. In addition, the drug composition can be conveniently taken by patients, the treatment compliance is greatly improved, and the medical costs can be also reduced.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing calcium antagonist (CCB), angiotensin II receptor blocker (ARB), thiazide diuretic and folic acid, which is used for treating moderate and severe hypertension, preventing and delaying Stroke caused by high blood pressure. The present invention belongs to the field of pharmacy. Background technique [0002] Essential hypertension is a major factor leading to coronary heart disease, stroke, congestive heart failure and kidney damage. At present, the prevalence of hypertension in my country has risen to 27.2%, and it is estimated that there are about 300 million patients. The main therapeutic goal of treating hypertensive patients is to minimize the overall risk of cardiovascular complications and death. Drugs to lower blood pressure can effectively reduce the morbidity and mortality of cardiovascular complications. [0003] Drugs currently used to lower blood pressure mainly include calc...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/519A61P9/12A61P9/10
CPCA61K45/06A61K31/519A61K2300/00
Inventor 于多张磊徐希平刘平王滨燕
Owner SHENZHEN AUSA PHARM CO LTD
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