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Felodipine sustained-release tablet and preparation technology thereof

A felodipine and gentle technology, applied in the field of sustained-release tablets, can solve the problems of unfavorable environmental protection, complicated preparation process, gastrointestinal irritation, etc., and achieve the effect of slow and stable drug release, simple preparation process and rapid drug release

Active Publication Date: 2015-07-08
CHANGZHOU NO 4 PHARMA FACTORY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process of this invention is complex, the use of a large amount of surfactants causes gastrointestinal irritation, and the use of organic solvents such as chloroform is not conducive to environmental protection

Method used

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  • Felodipine sustained-release tablet and preparation technology thereof
  • Felodipine sustained-release tablet and preparation technology thereof
  • Felodipine sustained-release tablet and preparation technology thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Solid dispersion

[0029]

[0030] (2) Sustained-release pellets

[0031] Solid dispersion 75g

[0032] Ethylcellulose 15g

[0033] Hydroxypropyl Cellulose 1.5g

[0034] (3) Felodipine Sustained Release Tablets (4000 Tablets)

[0035]

[0036] Preparation Process:

[0037] ①Add felodipine and copovidone to absolute ethanol, stir to dissolve, add polacrilin potassium, stir, ultrasonically uniform, dry under reduced pressure to remove solvent, and obtain felodipine immediate-release solid dispersion;

[0038] 2. Get the felodipine immediate-release solid dispersion prepared in step 1. and add it in the fluidized bed, spray coating at the bottom with ethylcellulose ethanol solution containing porogen, to prepare slow-release coated pellets;

[0039] ③Weigh the felodipine immediate-release solid dispersion and sustained-release coated pellets in proportion, mix them evenly with microcrystalline cellulose, sodium carboxymethyl starch, and magnesium stearate, a...

Embodiment 2

[0041] (1) Solid dispersion

[0042]

[0043]

[0044] (2) Sustained-release pellets

[0045] Solid dispersion 120g

[0046] Ethyl cellulose 30g

[0047] Hydroxypropyl Cellulose 6g

[0048] (3) Felodipine Sustained Release Tablets (4000 Tablets)

[0049]

[0050] Preparation Process:

[0051] ①Add felodipine and copovidone to absolute ethanol, stir to dissolve, add polacrilin potassium, stir, ultrasonically uniform, dry under reduced pressure to remove solvent, and obtain felodipine immediate-release solid dispersion;

[0052] 2. Get the felodipine immediate-release solid dispersion prepared in step 1. and add it in the fluidized bed, spray coating at the bottom with ethylcellulose ethanol solution containing porogen, to prepare slow-release coated pellets;

[0053]③ Weigh the felodipine immediate-release solid dispersion and sustained-release coated pellets in proportion, mix them evenly with lactose, pregelatinized starch, crospovidone, and magnesium stearate, ...

Embodiment 3

[0055] (1) Solid dispersion

[0056]

[0057] (2) Sustained-release pellets

[0058] Solid dispersion 165g

[0059] Ethylcellulose 39.5g

[0060] Hydroxypropyl Cellulose 7.8g

[0061] (3) Felodipine Sustained Release Tablets (4000 Tablets)

[0062]

[0063] Preparation Process:

[0064] ①Add felodipine and copovidone to absolute ethanol, stir to dissolve, add polacrilin potassium, stir, ultrasonically uniform, dry under reduced pressure to remove solvent, and obtain felodipine immediate-release solid dispersion;

[0065] 2. Get the felodipine immediate-release solid dispersion prepared in step 1. and add it in the fluidized bed, spray coating at the bottom with ethylcellulose ethanol solution containing porogen, to prepare slow-release coated pellets;

[0066] ③ Weigh the felodipine immediate-release solid dispersion and sustained-release coated pellets in proportion, mix them with microcrystalline cellulose, starch, croscarmellose sodium, and magnesium stearate, an...

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Abstract

The invention discloses a felodipine sustained-release tablet and a preparation technology thereof. According to the preparation technology of the felodipine sustained-release tablet, fast-release solid dispersions, sustained-release micro-pills and pharmaceutically acceptable accessories are mixed and the mixture is compressed to obtain the preparation. The fast-release solid dispersions comprise felodipine, copovidone and polacrilin potassium; the sustained-release micro pills are obtained by coating the fast-release solid dispersions with the ethyl cellulose film with a pore-forming agent. The sustained-release tablet disclosed by the invention has the advantages of fast early-stage releasing speed and slow and stable later-stage releasing speed, so that the drug can be completely released and an effective blood drug concentration can be maintained for a long time; the felodipine sustained-release tablet is high in bioavailability, simple in preparation technology and applicable to industrial mass production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a solid oral preparation, in particular to a sustained-release tablet containing felodipine and a preparation process thereof. Background technique [0002] Felodipine is a third-generation dihydropyridine calcium antagonist, which is used to treat hypertension by inhibiting the influx of extracellular calcium in arteriolar smooth muscle and reducing peripheral vascular resistance. Felodipine is white to pale yellow crystal or crystalline powder, odorless and tasteless; unstable when exposed to light. Soluble in acetone, methanol or ethanol, almost insoluble in water, the chemical name is (±)-2,6-dimethyl-4-(2,3-dichlorophenyl)-1,4-dihydro- Methyl 3,5-pyridinedicarboxylate, molecular formula C 18 h 19 Cl 2 NO 4 , the molecular weight is 384.26, and the structural formula is as follows: [0003] [0004] Currently, felodipine is available i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/32A61K47/38A61K31/4422A61P9/12
Inventor 贾红瑞
Owner CHANGZHOU NO 4 PHARMA FACTORY
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