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Cholesterol uptake inhibitor and vitamin-B composition and application thereof

A composition and cholesterol technology, applied in the field of pharmacy, to achieve the effects of convenience in taking medicine, improving curative effect and reducing medical expenses

Active Publication Date: 2013-12-04
SHENZHEN AUSA PHARM CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the pathological mechanism of atherosclerosis has not yet been fully elucidated, most scholars support the theory of "endothelial injury response", that is, early arterial intima injury is the result of subsequent lipid infiltration, fibroproliferative reaction and atheromatous plaque formation. Base

Method used

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  • Cholesterol uptake inhibitor and vitamin-B composition and application thereof
  • Cholesterol uptake inhibitor and vitamin-B composition and application thereof
  • Cholesterol uptake inhibitor and vitamin-B composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1. Preparation of Ezetimibe 10mg / Folic Acid 0.8mg Tablets

[0025] Recipe composition:

[0026]

[0027]Made into 1000 pieces

[0028] Preparation method: crush the raw and auxiliary materials through an 80-mesh sieve, and dry for later use. Take 10g of ezetimibe and 0.8g of folic acid and mix evenly according to the method of equal increase, add 25g of sodium carboxymethyl starch, 115g of microcrystalline cellulose, and 80g of calcium hydrogen phosphate, mix evenly according to the method of equal increase, and add an appropriate amount of binder 10% povidone aqueous solution to make soft material, 30 mesh granulation, drying at 40-45°C for 3 hours; 30 mesh granulation, finally adding 1% magnesium stearate and mixing, after content determination, tableting and packaging. Pay attention to avoiding light during the preparation process. After the finished product passes the inspection, it will be packaged in aluminum-plastic blisters and stored away from ligh...

Embodiment 2

[0029] Example 2. Preparation of Ezetimibe 10mg / 5-Methyltetrahydrofolate 0.2mg Capsules

[0030] Recipe composition:

[0031]

[0032] Make 1000 capsules

[0033] Preparation method: crush the raw and auxiliary materials through an 80-mesh sieve, and dry for later use. Take 10g of ezetimibe and 0.2g of 5-methyltetrahydrofolate and mix them uniformly according to the method of equal increase, add 80g of starch, 40g of microcrystalline cellulose, and 40g of sodium carboxymethyl starch, mix evenly, and make it with 50% ethanol Soft material, granulate with 20 mesh sieve, dry at 60°C for about 2 hours, granulate with 20 mesh sieve, control the water content of the granules to 2-3%, mix the dried granules with 1% magnesium stearate in the prescribed amount evenly, The semi-finished product is tested, its content is determined, and it is packed into hollow capsules to obtain 1000 capsules. Protect from light during preparation. After the finished pr...

Embodiment 3

[0034] Example 3. Ezetimibe glucuronide 15 mg / calcium leucovorin 1 mg / vitamin B 6 Preparation of 5.0 mg granules

[0035] Recipe composition:

[0036]

[0037] Make 1000 bags

[0038] Preparation method: crush the raw materials and auxiliary materials through a 120-mesh sieve, take 15 g of ezetimibutol glucuronide, 1.0 g of calcium leucovorin, and vitamin B 6 5g, 800g of lactose, 40g of starch, 5g of gum arabic, 2g of sweet orange essence, 5g of polyethylene glycol, 27g of sodium carboxymethyl starch, sieved, mixed evenly to make a soft material, granulated, dried at 40-60°C, containing The water content is about 3%, it is taken out, granulated, and filled into granules according to the conventional method. Each bag of the prepared compound tablet contains 15 mg of ezetimibutol glucuronide, 1 mg of calcium leucovorin, vitamin B 6 5.0mg.

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Abstract

The invention relates to cholesterol uptake inhibitor and vitamin-B composition and applications thereof. Preferably, Ezetimibe serves as the selective cholesterol uptake inhibitor, 1-30mg; vitamin-B is folates, vitamin B6 or vitamin B12, 0.01-50mg. The invention further provides the application of the composition in the preparation of drugs for treating hypercholesteremia and preventing atherosclerosis. The cholesterol uptake inhibitor and vitamin-B composition has the advantages that the composition is better in cholesterol reduction and is able to protect blood vessel endothelium to effectively prevent atherosclerosis accordingly; clinical application benefit of the composition is significantly better than that of the sole use of the selective cholesterol update inhibitor; in addition, the composition is convenient for patients to take, and costs in medical treatment are reduced.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing a selective cholesterol absorption inhibitor and B vitamins, in particular to a pharmaceutical composition for treating hypercholesterolemia, preventing atherosclerosis formation and related diseases. The present invention belongs to the field of pharmacy. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the main causes of human death, including coronary atherosclerotic heart disease (referred to as coronary heart disease, myocardial infarction is its severe type) and stroke, the latter is also mostly caused on the basis of cerebral arteriosclerosis. Arteriosclerosis is a non-inflammatory disease of the arteries, which can thicken and harden the arterial wall, lose elasticity, and narrow the lumen. Atherosclerosis is the most important type (85% of coronary heart disease is caused by coronary artery porridge. caused by sclerosis). Dyslipidemia, especi...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61P3/06A61P9/10A61P9/14
Inventor 张磊陈光亮王存芳徐希平
Owner SHENZHEN AUSA PHARM CO LTD
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