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Eplerenone oral solid preparation and preparation method therefor

A technology of eplerenone and solid preparations, applied in the field of medicine, can solve problems such as unfavorable water penetration and tablet disintegration, reduce liquid surface tension, increase insoluble drugs, etc., and achieve excellent preparation technical effects, solubility and The effect of dissolution enhancement

Inactive Publication Date: 2017-12-12
NANJING CAVENDISH BIO ENG TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] US2003236236A1 and CN101152187A disclose a method for increasing insoluble drugs by adding surfactants, including polysorbate, polyoxyethylene fatty acid ester, sorbitan fatty acid, and poloxamer, although its dissolution rate and bioavailability are improved, However, compared to drugs that are easily wetted by water, the addition of surfactants unnecessarily reduces the surface tension of the liquid, which is not conducive to water penetration and tablet disintegration

Method used

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  • Eplerenone oral solid preparation and preparation method therefor
  • Eplerenone oral solid preparation and preparation method therefor
  • Eplerenone oral solid preparation and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Eplerenone dispersible tablet or orally disintegrating tablet

[0052] prescription:

[0053]

[0054]

[0055] Preparation:

[0056] Wherein, the preparation method of eplerenone-polyvinylpyrrolidone compound:

[0057] a. Dissolve polyvinylpyrrolidone in ethanol, add eplerenone, and stir until dissolved under heating;

[0058] b. The solution of step a is granulated in one step by fluidized bed spray drying;

[0059] The preparation method of described dispersible tablet or capsule comprises:

[0060] (1) Grind the eplerenone-polyvinylpyrrolidone composite solid dispersion powder obtained by spray granulation with lactose, microcrystalline cellulose, and croscarmellose sodium, pass through a 40-mesh sieve and mix, add stearin Magnesium acid mixed evenly;

[0061] (2) Dry the mixed powder in an oven at 55°C until the drying loss is less than 2%, take it out and pass through a 40-mesh sieve, and press it into tablets. The tablet has a hardness of 5-10kg and a ...

Embodiment 2

[0063] Eplerenone Capsules

[0064] Components and dosage:

[0065]

[0066] Wherein, the preparation method of eplerenone-polyvinylpyrrolidone compound:

[0067] a. Dissolve polyvinylpyrrolidone in ethanol, add eplerenone, and stir until dissolved under heating;

[0068] b. The solution of step a is granulated in one step by fluidized bed spray drying;

[0069] The preparation method of described capsule comprises:

[0070] (1) The eplerenone-polyvinylpyrrolidone composite solid dispersion powder obtained by spray granulation is ground with lactose, microcrystalline cellulose, croscarmellose sodium and silicon dioxide, and mixed through a 40-mesh sieve ;

[0071] (2) Dry the mixed powder in an oven at 60°C until the drying loss is less than 2%, take it out and pass through a 40-mesh sieve, and fill it into capsules. The weight of the content of each capsule is about 170mg.

Embodiment 3

[0073] Eplerenone Tablets

[0074] prescription:

[0075]

[0076] Preparation:

[0077] Wherein, the preparation method of eplerenone-polyvinylpyrrolidone compound:

[0078] a. Dissolve polyvinylpyrrolidone in ethanol, add eplerenone, and stir until dissolved under heating;

[0079] b. The solution of step a is granulated in one step by fluidized bed spray drying;

[0080] The preparation method of described tablet comprises:

[0081] (1) Mix the eplerenone-polyvinylpyrrolidone composite solid dispersion powder obtained by spray granulation with lactose, microcrystalline cellulose, and hydroxypropyl cellulose evenly, add ethanol-made soft material, and pass the soft material through 40 mesh Sieve wet granules

[0082] (2) Place the wet granules in an oven at 55°C and dry until the loss on drying is less than 2%, take them out, pass through a 40-mesh sieve for granulation;

[0083] (3) Add croscarmellose sodium and magnesium stearate to the dry granules, mix well, and...

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Abstract

The invention discloses an eplerenone oral solid preparation. The eplerenone oral solid preparation comprises an eplerenone-polyvinylpyrrolidone compound, wherein the eplerenone-polyvinylpyrrolidone compound is prepared by the steps of a, dissolving polyvinylpyrrolidone into ethyl alcohol or acetone, adding eplerenone, and performing heating and dissolving to obtain a clear solution; and b, performing spraying and drying on the clear solution obtained in the step a by adopting a fluidized bed, and then performing one-step palletizing to obtain the oral solid preparation. In addition, the invention also discloses a preparation method for the oral solid preparation. The dissolution rate of the eplerenone oral solid preparation is greater than 90% in 10min.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to an eplerenone oral solid preparation and a preparation method thereof. Background technique [0002] Eplerenone, the chemical name is (7α, 11α, 17α)-9,11-epoxy-17-hydroxy-3-oxo-pregna-4-ene-7,21-dicarboxylic acid, γ-lactone, 7-methyl ester, its chemical structural formula is as shown in (1): [0003] [0004] Eplerenone is an oral highly selective aldosterone receptor antagonist (SAB), which can block the action of the renin-angiotensin-aldosterone system (RAAS) by competitively inhibiting aldosterone and mineralocorticoid receptors Binding, antagonizing the binding of aldosterone to mineralocorticoid receptors in epithelial (such as kidney) and non-epithelial (such as heart, blood vessels, and brain) tissues plays an important role in regulating the function of the human cardiovascular system. Therefore, eplerenone can effectively control high blood pressur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K47/32A61K31/585A61P9/12A61P9/10
CPCA61K9/0056A61K9/2027A61K9/2095A61K9/4866A61K31/585
Inventor 许永翔
Owner NANJING CAVENDISH BIO ENG TECH
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