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Nifedipine sustained-release tablet and preparation method thereof

A technology of nifedipine and nifedipine, applied in the field of medicine, can solve the problems of slow dissolution rate of nifedipine, slow release rate of slow control agent, inability to achieve complete release, etc., and achieve good fluidity and compressibility, good Disintegration effect, anti-triboelectric effect

Active Publication Date: 2014-11-12
JINAN LIMIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But present existing nifedipine slow-release tablet mostly has the following problems: (1) because nifedipine is a poorly soluble compound, the dissolution in water is extremely small, about 10-12 μ g / ml, so nifedipine stripping speed easily occurs The problem of being too slow; (2) In the treatment of slow control, some slow control agents have the problem that the release rate is too slow (complete release cannot be achieved within 24h), or the slow release is not stable, and the slow release effect is poor

Method used

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  • Nifedipine sustained-release tablet and preparation method thereof
  • Nifedipine sustained-release tablet and preparation method thereof
  • Nifedipine sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Based on the nifedipine sustained-release tablets made into 1000 tablets (each containing 20 mg of nifedipine),

[0031] Components and weight of the outer layer tablet: 5g of nifedipine, 10g of microcrystalline cellulose, 30g of spray-dried lactose (FlowLac100), 0.2g of sodium lauryl sulfate, 2.0g of copovidone (Plasdone S-630), micropowder Silica gel 1.0g, magnesium stearate 0.2g;

[0032] The composition and weight of the inner sheet: 15g of nifedipine, 100g of lactose, 45g of pregelatinized starch, 10g of hydroxypropyl cellulose (produced by Taian Ruitai Cellulose Co., Ltd.), 10g of sodium alginate, 10g of potassium alginate, poly Vitamin ketone (K30) 20g, PEG6000 2g, polyvinylpyrrolidone 2.0g, magnesium stearate 1.5g.

[0033] (1) Powder preparation of the outer layer tablet:

[0034] Grind microcrystalline cellulose, spray-dried lactose, copovidone, magnesium stearate and micronized silica gel to pass through an 80-mesh sieve, and set aside; mix nifedipine and s...

Embodiment 2

[0063] Based on the nifedipine sustained-release tablets made into 1000 tablets (each containing 20 mg of nifedipine),

[0064] Components and weight of the outer tablet: 5g of nifedipine, 12g of microcrystalline cellulose, 32g of spray-dried lactose, 0.25g of sodium lauryl sulfate, 2.5g of copovidone, 1.2g of micropowder silica gel, stearic acid Magnesium 0.3g;

[0065] Components and weight of the inner sheet: 15g of nifedipine, 110g of lactose, 50g of pregelatinized starch, 12g of hydroxypropyl cellulose (HPC), 12g of sodium alginate, 12g of potassium alginate, 22g of povidone, PEG6000 2.5g, polyvinylpyrrolidone 2.2g, magnesium stearate 1.8g.

[0066] Preparation method: dissolve nifedipine, povidone and PEG6000 in 600ml of absolute ethanol, and the rest are the same as in Example 1.

Embodiment 3

[0068] Based on the nifedipine sustained-release tablets made into 1000 tablets (each containing 20 mg of nifedipine),

[0069] Components and weight of the outer tablet: 5g of nifedipine, 8g of microcrystalline cellulose, 28g of spray-dried lactose, 0.15g of sodium lauryl sulfate, 1.5g of copovidone, 0.8g of micropowder silica gel, stearic acid Magnesium 0.1g;

[0070] Components and weight of the inner sheet: 15g of nifedipine, 90g of lactose, 40g of pregelatinized starch, 8g of hydroxypropyl cellulose (HPC), 8g of sodium alginate, 8g of potassium alginate, 18g of povidone, PEG6000 1.5g, polyvinylpyrrolidone 1.8g, magnesium stearate 1.2g.

[0071] Preparation method: dissolve nifedipine, povidone and PEG6000 in 400ml of absolute ethanol, and the rest are the same as in Example 1.

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Abstract

The invention discloses a nifedipine sustained-release tablet and a preparation method thereof. The nifedipine sustained-release tablet is a double-layer tablet, wherein the outer-layer tablet is prepared from the following raw materials: nifedipine, microcrystalline cellulose, spray-dried lactose, sodium dodecyl sulfate, copovidone, superfine silica powder and magnesium stearate by using a direct powder compression method; and the inner-layer tablet is prepared from the following raw materials: nifedipine, lactose, pregelatinized starch, hydroxypropyl cellulose, sodium alginate, potassium alginate, povidone, PEG6000, polyvinylpyrrolidone and magnesium stearate. The preparation method comprises the steps of preparing a nifedipine dispersoid from nifedipine, povidone and PEG6000 by using a solvent evaporation method; and then, carrying out wet granulation on the nifedipine dispersoid and other raw materials to prepare the inner-layer tablet. The outer-layer tablet of the nifedipine sustained-release tablet is prepared by using the direct powder compression method, so that disintegration is high, and the required blood concentration is rapidly reached within short time; and the inner-layer tablet formed by compounding the hydroxypropyl cellulose, sodium alginate and potassium alginate is used as a gel sustained-release framework and can be completely released within 24h.

Description

technical field [0001] The invention relates to a nifedipine sustained-release tablet and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Nifedipine is the first-generation calcium antagonist, an antihypertensive and angina pectoris drug, which was first developed and marketed by German Bayer Company in the 1970s. It was one of the best-selling drugs in the world in the mid-1980s. The drug is characterized by a rapid onset of action and a high peak / trough ratio, leading to neurohumoral activation. After years of clinical use, the curative effect of the drug has been affirmed, and nifedipine also has a strong price advantage, and has become one of the first-choice drugs for clinical treatment of hypertension and angina pectoris. [0003] Since the 1980s, it has been confirmed by medical practice that ordinary preparations of nifedipine reflexively cause increased heart rate and activate the sympathetic nervous system,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K31/4422A61K47/38A61K47/36A61K47/20A61P9/10A61P9/12
Inventor 秦怀国樊若男曹悦兴
Owner JINAN LIMIN PHARMA
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