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A kind of felodipine sustained-release tablet and preparation method thereof

A felodipine and gentle technology, applied in the direction of non-active ingredient medical preparations, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problem of large blood pressure fluctuations, frequent medications, and restrictions on the development of felodipine sustained-release tablets and other problems, to achieve the effect of improving uniformity, good sustained release effect, sustained release effect and stability

Active Publication Date: 2018-10-16
XINAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, felodipine ordinary tablets and sustained-release tablets are mainly on the market, and the ordinary tablets need to be taken 2 to 3 times a day. Although this preparation can achieve the effect of lowering blood pressure, it has a large fluctuation in blood pressure due to the frequent taking of the medicine; Therefore, sustained-release tablets are more recognized and concerned by people.
[0006] However, the slow-release tablets currently available on the market have the problem of poor release and uniformity, which limits the development of felodipine sustained-release tablets.

Method used

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  • A kind of felodipine sustained-release tablet and preparation method thereof
  • A kind of felodipine sustained-release tablet and preparation method thereof
  • A kind of felodipine sustained-release tablet and preparation method thereof

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preparation example Construction

[0043] The present invention also provides a preparation method of the felodipine sustained-release tablet described in the above technical scheme, comprising the following steps:

[0044] A) cooling after mixing felodipine with the dispersed dispersion matrix after melting, obtains felodipine solid dispersion; Described dispersion matrix is ​​polyethylene glycol;

[0045] b) compressing the felodipine solid dispersion, filler, lubricant and slow-release material after mixing to obtain a felodipine sustained-release tablet; the slow-release material is hydroxypropyl methylcellulose.

[0046] In the present invention, felodipine is mixed with the molten dispersion matrix and then cooled to obtain a felodipine solid dispersion. In the present invention, the felodipine is the main ingredient; the source of the felodipine is not particularly limited in the present invention, and commercially available products well known to those skilled in the art can be used. In the present inv...

Embodiment 1

[0067] (1) Heat 50g of polyethylene glycol 6000 in a water bath at 70°C until it is completely melted, then add 5g of felodipine crude drug and mix, then cool in an ice bath for 12 hours to obtain a completely embrittled solid product, and finally pulverize Cross 80 mesh sieves to obtain felodipine solid dispersion.

[0068](2) Combine the obtained felodipine solid dispersion with 48g lactose, 12g mannitol, 20g microcrystalline cellulose, 2g micropowder silica gel, 4g magnesium stearate, 21g hydroxypropyl methylcellulose K250 and 42g hydroxypropyl methylcellulose Methylcellulose K750 is added in the mixer, stirred at 4r / min for 30min, finally adopts tablet press to carry out tabletting, tabletting parameter is φ 9mm, hardness 6kg, obtains felodipine slow-release tablet (1000).

[0069] (3) Adopt 25g Opadry coating powder to carry out coating, obtain felodipine sustained-release tablet product.

Embodiment 2

[0071] (1) Heat 30g of polyethylene glycol 10000 in a water bath at 70°C until it is completely melted, then add 5g of felodipine bulk drug and mix, then cool in an ice bath for 12 hours to obtain a completely embrittled solid product, and finally pulverize Cross 80 mesh sieves to obtain felodipine solid dispersion.

[0072] (2) Felodipine solid dispersion obtained with 68g lactose, 32g microcrystalline cellulose, 2g micropowder silica gel, 4g magnesium stearate, 18g hydroxypropyl methylcellulose K250 and 45g hydroxypropyl methylcellulose K750 is added in the mixer, stirred at 3r / min for 30min, finally adopts tablet press to carry out tabletting, tabletting parameter is φ 9mm, hardness 6kg, obtains felodipine slow-release tablet (1000).

[0073] (3) Adopt 25g Opadry coating powder to carry out coating, obtain felodipine sustained-release tablet product.

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Abstract

The invention provides a felodipine sustained release tablet and a preparation method of the felodipine sustained release tablet. The felodipine sustained release tablet is prepared by mixing felodipine solid dispersion with a filling agent, a lubricating agent and a sustained-release material, and then tabletting; specifically, the felodipine sustained release tablet is prepared from the following components in parts by weight: the felodipine solid dispersion (containing 2.5-10 parts of felodipine and 10-100 parts of dispersion substrate), 60-160 parts of the filling agent, 0.4-8 parts of the lubricating agent, and 30-90 parts of the sustained-release material, wherein the dispersion substrate adopts polyethylene glycol, and the sustained-release material adopts hydroxypropyl methyl cellulose. Compared with the prior art, the felodipine sustained release tablet provided by the invention has the advantages that the uniform distribution is realized through the solid dispersion, so that the uniformity of the felodipine sustained release tablet is improved, and meanwhile through the interaction between the sustained-release material and the solid dispersion, the slow-release effect of the felodipine sustained release tablet is good and stable.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a felodipine sustained-release tablet and a preparation method thereof. Background technique [0002] Felodipine, the chemical name is 2,6-dimethyl-4-(2,3-dichlorophenyl)-1,4-dihydro-3,5-pyridine dicarboxylic acid methyl ethyl ester, the English name is FELODIPINE , the molecular formula is C 18 h 19 Cl 2 NO 4 , the molecular weight is 384.25, and the chemical structural formula is as follows: [0003] [0004] Felodipine is a dihydropyridine calcium antagonist with a high degree of vascular selectivity, and has the effect of significantly lowering blood pressure and total peripheral boost. Targeting certain parts of the vascular system to increase blood flow in these parts, such as coronary vessels and cerebrovascular, commonly used drugs include nifedipine, amlodipine, felodipine, etc. Felodipine has a negative effect on the myocardium Very small, long-term applicati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/28A61K31/4422A61K47/38A61K47/10A61P9/12
CPCA61K9/0002A61K9/2031A61K9/2054A61K9/2866A61K31/4422
Inventor 李标蒲道俊徐志谦马宜雪余春梅罗娟向俭杨秀丽
Owner XINAN PHARMA
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