Metroprolol succinate sustained release tablet and preparation method thereof

A technology of metoprolol succinate and sustained-release tablets, which can be used in pharmaceutical formulations, cardiovascular system diseases, drug combinations, etc., and can solve the problems of weak reproducibility and consistency of drug release rules

Inactive Publication Date: 2018-01-19
北京华素制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The sustained-release tablets in this application do not use multi-unit microparticles or pellet systems, but use the mixture of hydroxypropylmethylcellulose and carbomer as the sustained-release retardation material. The reproducibility and consistency are far weaker than the multi-unit microparticle or pellet system, because the drug release behavior of the microparticle or pellet system is the sum of the drug release behavior of the individual pellets that make up a dose, and individual pellets vary due to the preparation process. Introduced defects are not expected to seriously affect the drug release behavior of the whole tablet dosage form

Method used

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  • Metroprolol succinate sustained release tablet and preparation method thereof
  • Metroprolol succinate sustained release tablet and preparation method thereof
  • Metroprolol succinate sustained release tablet and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0040] The present invention also provides a preparation method of metoprolol succinate sustained-release tablet, which comprises the following steps: S1, using metoprolol succinate, drug-loaded pellet coating binder, purified water and alcohol Prepare the drug-loaded pellet coating solution with a neutral solvent, and coat the drug-loaded pellet coating solution on the surface of the blank core to obtain the drug-loaded pellet; S2. Using the coating material for sustained-release pellet coating, causing Pore ​​agent, plasticizer, anti-adhesive agent, purified water and alcoholic solvent to prepare sustained-release pellet coating liquid, coating the drug-loaded pellet surface prepared in S1 with the sustained-release pellet coating liquid, Obtain the sustained-release pellets; S3, prepare the coating liquid for protecting the pellets by using the coating material for coating the pellets, the adhesive for coating the pellets and purified water, and coat the coating liquid for t...

Embodiment 1～ Embodiment 2

[0076] prescription:

[0077]

[0078] The assay method of release adopts USP40, according to the second method device of dissolution assay (Chinese Pharmacopoeia 2015 edition), with 1000ml phosphate buffer (pH=6.8) as solvent, rotating speed is 50 revolutions per minute, operate according to law, after 1 Hours, 4 hours, 8 hours and 20 hours, the eluate was taken and measured by HPLC (the same below).

[0079] result:

[0080]

Embodiment 3～ Embodiment 7

[0082] prescription:

[0083]

[0084]

[0085] result:

[0086] Release(%)

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PUM

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Abstract

The invention belongs to the technical field of drug preparations, and relates to a Metoprolol succinate sustained release tablet and a preparation method thereof. The sustained release tablet includes a tablet film coating material and a tablet core coated with the coating, the tablet core comprises a pellet and accessories, the pellet comprises, from the inside to the outside, a blank pill core,a drug-loading coating layer, a sustained release coating layer and a protective coating layer, the drug-loading coating layer comprises Metoprolol succinate and a drug-loading pellet coating adhesive, the sustained release coating layer comprises a sustained release pellet coating layer coating material, a pore forming agent, a plasticizer and an anti adhesion agent, the protective coating layerincludes a protection pellet coating adhesive, the accessories include a filler, a disintegrating agent and a lubricating agent. The sustained layer of the release tablet is externally wrapped with the protective layer, and the problems of slow release ability reduction and unqualified content uniformity caused by excess fluidity and the like due to the damage of the sustained release layer can be solved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a metoprolol succinate sustained-release tablet and a preparation method of the metoprolol succinate sustained-release tablet. Background technique [0002] Metoprolol is a commonly used drug for the treatment of hypertension, coronary heart disease, chronic heart failure and arrhythmia, which can inhibit cardiac β 1 receptors and peripheral vascular and bronchial beta 2 Receptors act on β 1 The blocking effect of the receptor is strong, and it has a strong effect on β 2 The blocking effect of the receptor is extremely weak, and the receptor selectivity is more significant, and this selectivity is closely related to the dosage. Since metoprolol has effect on cardiac beta 1 Receptor effects require lower doses than peripheral vascular and bronchial beta 2 The dose required to produce an effect on the receptor, so low doses of metoprolol can selectively act o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/26A61K31/138A61K47/38A61P9/12A61P9/10A61P9/04A61P9/06
Inventor 龙永鹏翟海燕姚文静魏淑冬边玢董国明
Owner 北京华素制药股份有限公司
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