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

A gentle and felodipine technology, applied in the field of medicine, can solve the problems of large fluctuation of blood pressure, many times of taking medicine, restricting the development of felodipine sustained-release tablets, etc., and achieves improved uniformity, good sustained-release effect, and stable sustained-release effect. Effect

Active Publication Date: 2018-02-23
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

[0042] The present invention also provides a preparation method of the felodipine sustained-release tablet described in the above technical scheme, comprising the following steps:

[0043] a) After mixing felodipine, dispersion matrix and solvent, cooling and drying are carried out successively to obtain felodipine solid dispersion; the dispersion matrix is ​​copovidone;

[0044] 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.

[0045] In the present invention, after mixing the felodipine, the dispersion matrix and the solvent, cooling and drying are carried out in sequence to obtain the 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 tho...

Embodiment 1

[0065](1) Mix 40g copovidone S630 with 200mL absolute ethanol, then add 5g felodipine bulk drug, and heat in a water bath at 70°C for 15min to obtain a dispersion solution of felodipine, then place the above solution on ice Cool in a bath for 12 hours, then dry in a vacuum oven at 50° C. for 36 hours to obtain a solid product, and finally crush the above solid product through an 80-mesh sieve to obtain a solid dispersion of felodipine.

[0066] (2) Felodipine solid dispersion obtained with 60g lactose, 30g microcrystalline cellulose, 2g micropowder silica gel, 4g magnesium stearate, 21g hydroxypropyl methylcellulose K250 and 42g hydroxypropyl 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).

[0067] (3) Adopt 25g Opadry coating powder to carry out coating, obtain felodipine sustained-release tablet product.

Embodiment 2

[0069] (1) Mix 40g of copovidone VA64 with 200mL of absolute ethanol, then add 5g of felodipine crude drug, and heat in a water bath at 70°C for 15min to obtain a dispersion solution of felodipine, then place the above solution on ice Cool in a bath for 10 hours, then dry in a vacuum oven at 55° C. for 30 hours to obtain a solid product, and finally crush the above solid product through an 80-mesh sieve to obtain a solid dispersion of felodipine.

[0070] (2) Felodipine solid dispersion obtained with 60g lactose, 30g microcrystalline cellulose, 2g micropowder silica gel, 4g magnesium stearate, 21g hydroxypropyl methylcellulose K250 and 42g 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).

[0071] (3) Adopt 25g Opadry coating powder to carry out coating, obtain felodipine sustained-release tablet p...

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Abstract

The invention provides a felodipine sustained release tablet and a preparation method thereof. The felodipine sustained release tablet is formed by mixing and tabletting felodipine solid dispersion, filler, lubricant and a sustained-release material. The felodipine sustained release tablet comprises felodipine solid dispersion, 60-160 weight parts of filler, 0.4-8 weight parts of lubricant and 30-90 weight parts of sustained-release material, wherein the felodipine solid dispersion comprises 2.5-10 weight parts of felodipine and 10-100 weight parts of dispersion matrix; the dispersion matrix is copovidone, and the sustained-release material is hydroxypropyl methylcellulose. Compared with the prior art, the felodipine sustained release tablet is evenly distributed through the solid dispersion, the uniformity of the felodipine sustained release tablet is improved; and through the interaction of the sustained-release material and the solid dispersion, the sustained-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): A61K9/22A61K47/38A61K47/32A61K31/4422A61P9/12
CPCA61K9/2027A61K9/2054A61K9/2866A61K31/4422
Inventor 蒲道俊李标徐志谦马宜雪徐洁赵强罗娟郑小锋
Owner XINAN PHARMA
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