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Composition capable of curing abnormal blood lipid

A technology for dyslipidemia and a composition is applied in the field of medical compositions for the treatment of dyslipidemia, which can solve the problems of unsatisfactory, unsatisfactory safety, unmaximized lipid-lowering effect, etc., and can increase HDL-C and improve blood lipids The effect of reaching the target rate and serum uric acid has no effect

Inactive Publication Date: 2013-06-05
内蒙古天衡医院管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Disadvantages of statins: (1) The lipid-lowering spectrum is relatively simple, mainly lowering LDL-C, and the effect on TG and HDL-C is weak
(4) High toxicity: mainly myotoxicity and hepatotoxicity [4] , with a dose-dependent increase in incidence
(5) 6% phenomenon: when the dose is doubled, the LDL-C lowering effect only increases by 6%
However, since simvastatin and niacin are not the drugs with the best lipid-lowering effect in the same class of drugs, the lipid-lowering effect has not been maximized, and the triple compound is still unsatisfactory
In addition, there are many adverse reactions (such as: flushing) mainly caused by niacin, which are poorly tolerated by patients and have a high discontinuation rate.
[0028] In summary, although the compound lipid-lowering drugs that have been marketed or have clinical reports have their own strengths, their lipid-lowering effects still have shortcomings, and their safety needs to be improved.

Method used

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  • Composition capable of curing abnormal blood lipid
  • Composition capable of curing abnormal blood lipid
  • Composition capable of curing abnormal blood lipid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1 tablet

[0075] 1. Prescription (based on 1000 tablets)

[0076]

[0077]

[0078] 2. Preparation process

[0079] (1) Grind acipimox, ezetimibe, and atorvastatin calcium through a 100-mesh sieve for later use.

[0080] (2) Mix acipimox, microcrystalline cellulose, and croscarmellose sodium in a wet granulator according to the prescription amount, stir at 600 rpm, and shear at 1200 rpm for about 10 minutes.

[0081] (3) Add an appropriate amount of 80% ethanol solution of 5% hydroxypropyl cellulose-SL to prepare a soft material, stir at 500 rpm, and shear at 1380 rpm for about 3 minutes.

[0082] (4) Granulate with a 24-mesh sieve, dry at 40° C., and then granulate with a 24-mesh sieve to obtain partial granules of acipimox.

[0083] (5) Ezetimibe, microcrystalline cellulose, heavy calcium carbonate, pregelatinized starch, croscarmellose sodium, and sodium lauryl sulfate are mixed in a wet granulator and stirred at 600 rpm Min, shear 1200 rpm, about ...

Embodiment 2

[0107] Example 2 tablet

[0108] 1. Prescription (based on 1000 tablets)

[0109]

[0110]

[0111] 2. Preparation process

[0112] (1) Grind acipimox, ezetimibe, and atorvastatin calcium through a 100-mesh sieve for later use.

[0113] (2) Mix acipimox, microcrystalline cellulose, and croscarmellose sodium in a wet granulator according to the prescription amount, stir at 600 rpm, and shear at 1200 rpm for about 10 minutes.

[0114] (3) Add an appropriate amount of 80% ethanol solution of 5% hydroxypropyl cellulose-SL to prepare a soft material, stir at 500 rpm, and shear at 1380 rpm for about 3 minutes.

[0115] (4) Granulate with a 24-mesh sieve, dry at 40°C, then granulate with a 24-mesh sieve, add magnesium stearate to obtain the granules of the acipimox part.

[0116] (5) Mix ezetimibe, microcrystalline cellulose, pregelatinized starch, croscarmellose sodium, and sodium lauryl sulfate in a wet granulator, stir at 600 rpm, and shear 1200 rpm, about 10 minutes.

...

Embodiment 3

[0137] Example 3 tablet

[0138] 1. Prescription (based on 1000 tablets)

[0139]

[0140]

[0141] 2. Preparation process

[0142] (1) Grind acipimox, ezetimibe, and atorvastatin calcium through a 100-mesh sieve for later use.

[0143] (2) Mix acipimox, microcrystalline cellulose, and croscarmellose sodium in a wet granulator according to the prescription amount, stir at 600 rpm, and shear at 1200 rpm for about 10 minutes.

[0144] (3) Add an appropriate amount of 80% ethanol solution of 5% hydroxypropyl cellulose-SL to prepare a soft material, stir at 500 rpm, and shear at 1380 rpm for about 3 minutes.

[0145] (4) Granulate with a 24-mesh sieve, dry at 40° C., then granulate with a 24-mesh sieve, and add a prescribed amount of magnesium stearate to obtain granules of the acipimox part.

[0146] (5) Ezetimibe, microcrystalline cellulose, pregelatinized starch, croscarmellose sodium, and sodium lauryl sulfate are mixed in a wet granulator, stirred at 600 rpm, and she...

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Abstract

The invention relates to a composition capable of curing abnormal blood lipid. The composition capable of curing the abnormal blood lipid comprises ezetimibe, atorvastatin calcium and acipimox. The range of weight ratios of the ezetimibe, the atorvastatin calcium and the acipimox in the composition is 5-10: 5-80: 250-1000, preferably 10: 10-40: 250-750 and optimally, 10: 10-20; 500-750. The composition capable of curing the abnormal blood lipid is strong in blood lipid regulating effect, comprehensive in function and little in side effect.

Description

technical field [0001] The invention relates to a pharmaceutical composition for treating dyslipidemia, in particular to a pharmaceutical composition containing ezetimibe, atorvastatin calcium and acipimox. Background technique [0002] 1. Introduction of hyperlipidemia [0003] Dyslipidemia, also known as hyperlipidemia, refers to the abnormal concentration of lipids or lipoprotein components in the circulation, high blood lipid levels, especially elevated low-density lipoprotein cholesterol (LDL-C), which is the cause of plaque formation. The main cause of atherosclerosis. The lipid content of plaques determines plaque stability and susceptibility to acute ischemic events. In the past 20 years, the morbidity and mortality of coronary heart disease and other cardiovascular diseases have gradually increased, becoming the leading cause of death among Chinese residents. It is closely related to abnormal blood lipid indicators such as LDL-C. For every 1% decrease in serum cho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4965A61P3/06A61K31/40A61K31/397
Inventor 狄媛吕玉珠杨敏张铁军唐亚坤刘俊轶
Owner 内蒙古天衡医院管理有限公司
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