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Oral solid preparation of eplerenone and preparation method thereof

A solid preparation, eplerenone technology, applied in the field of medicine, can solve problems such as poor dissolution, and achieve the effects of high dissolution and excellent bioavailability

Active Publication Date: 2019-06-25
NANJING CAVENDISH BIO ENG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present inventor has developed a kind of oral solid preparation of eplerenone, has avoided using hydrophilic binding agent and non-ionic surfactant, and has overcome the problem of poor dissolution rate of eplerenone oral solid preparation

Method used

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  • Oral solid preparation of eplerenone and preparation method thereof
  • Oral solid preparation of eplerenone and preparation method thereof
  • Oral solid preparation of eplerenone and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Eplerenone Tablets

[0040] (1) Suspension prescription and preparation method (API+SDS)

[0041]

[0042] Dissolve the prescribed amount of sodium lauryl sulfate in the prescribed amount of purified water. After completely dissolving, add the prescribed amount of eplerenone to suspend in the solution, stir at 40°C for 1 hour, and then ultrasonicate the suspension for 1 hour.

[0043] (2) Premix

[0044]

[0045] The prescription amount of microcrystalline cellulose, anhydrous lactose and croscarmellose sodium are uniformly mixed to obtain a premix.

[0046] (3) Granulation drying and sizing

[0047] Slowly and evenly add the suspension obtained in (1) into the premix to make a soft material, pass through a 40-mesh sieve to granulate. Dry in an air blast oven at 55±5°C until the moisture is within 2% to 3%. The granules are taken out, passed through an 80-mesh sieve, and sized to obtain dry granules.

[0048] (4) total mix

[0049] Add 1.5 mg / tablet of magne...

Embodiment 2

[0055] Eplerenone Tablets

[0056] (1) Suspension prescription and preparation method (API+SDS)

[0057]

[0058] Dissolve the prescribed amount of sodium lauryl sulfate in the prescribed amount of purified water. After completely dissolving, add the prescribed amount of eplerenone to suspend in the solution, stir at 40°C for 1 hour, and then ultrasonicate the suspension for 1.5 hours .

[0059] (2) Premix

[0060]

[0061] The prescription amount of microcrystalline cellulose, lactose monohydrate and croscarmellose sodium are uniformly mixed to obtain a premix.

[0062] (3) Granulation drying and sizing

[0063] Slowly and evenly add the suspension obtained in (1) into the premix to make a soft material, pass through a 40-mesh sieve to granulate. Dry in a fluidized bed at 50-70°C until the water content is in the range of 2%-3%. The granules are taken out, passed through an 80-mesh sieve and sized to obtain dry granules.

[0064] (4) total mix

[0065] Add 1.0mg / ta...

Embodiment 3

[0071] Eplerenone Tablets

[0072] (1) Suspension prescription and preparation method (API+SDS)

[0073]

[0074] Dissolve the prescribed amount of sodium lauryl sulfate in the prescribed amount of purified water. After completely dissolving, add the prescribed amount of eplerenone to suspend in the solution, stir at 40°C for 1 hour, and then ultrasonicate the suspension for 1.5 hours .

[0075] (2) Premix

[0076]

[0077] The prescription amount of microcrystalline cellulose, lactose monohydrate and croscarmellose sodium are uniformly mixed to obtain a premix.

[0078] (3) Granulation drying and sizing

[0079] Slowly and evenly add the suspension obtained in (1) into the premix to make a soft material, pass through a 40-mesh sieve to granulate. Dry in a fluidized bed at 50-70°C until the water content is in the range of 2%-3%. The granules are taken out, passed through an 80-mesh sieve and sized to obtain dry granules.

[0080] (4) total mix

[0081] Add the ex...

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Abstract

The invention discloses an oral solid preparation of eplerenone. The oral solid preparation is composed of, by weight percentage, 10%-35% of eplerenone, 0.5%-5% of sodium lauryl sulfate, 50%-80% of filler, 3%-10% of disintegrant and 0.1%-1.8% of lubricant. In addition, a preparation method is also disclosed. The oral solid preparation overcomes the problem of poor dissolution of an oral solid preparation of eplerenone, and has excellent bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, relates to 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 formula (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 pressure,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/585A61K47/38A61P9/12
Inventor 许永翔赵新慧
Owner NANJING CAVENDISH BIO ENG TECH