A kind of metoprolol tartrate crystal, pharmaceutical composition containing the crystal and preparation method thereof

A technology of metoprolol tartrate and composition, which is applied in the fields of metoprolol tartrate crystals and pharmaceutical compositions containing the crystals and their preparation, and can solve the problems affecting the dissolution rate of tablets and the large amount of magnesium stearate used , to achieve the effects of superior drug efficacy, quality improvement, and improved drug efficacy

Active Publication Date: 2020-05-22
ZHUHAI TONGYUAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The amount of magnesium stearate in the pharmaceutical composition is too large, and magnesium stearate is a hydrophobic auxiliary material, and the amount of magnesium stearate will affect the dissolution rate of the tablet

Method used

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  • A kind of metoprolol tartrate crystal, pharmaceutical composition containing the crystal and preparation method thereof
  • A kind of metoprolol tartrate crystal, pharmaceutical composition containing the crystal and preparation method thereof
  • A kind of metoprolol tartrate crystal, pharmaceutical composition containing the crystal and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 2～5

[0060]

Embodiment 1

[0063] prescription:

[0064]

[0065] Preparation Process:

[0066] (1) Weigh hypromellose, disperse evenly with ethanol, add purified water, stir until the liquid is uniform and transparent, cool, and use it as an adhesive for subsequent use;

[0067] (2) Take metoprolol tartrate, starch, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch according to the prescription ratio, and metoprolol tartrate→starch→2 / 3 of the prescription amount of sodium carboxymethyl starch → The sequence of low-substituted hydroxypropyl cellulose is uniformly mixed by the method of equal increment to obtain mixed powder;

[0068] (3) Add binder to the mixed powder described in step (2), obtain soft material by wet granulator, and then make granules, then boil and dry, sieve and granulate to obtain dry granules;

[0069] (4) take silicon dioxide, magnesium stearate by prescription ratio, join in the dry granule described in step (3) together with the carboxymethyl starch sodiu...

Embodiment 2

[0072] prescription:

[0073]

[0074] Preparation Process:

[0075] (1) Weigh hypromellose, disperse evenly with ethanol, add purified water, stir until the liquid is uniform and transparent, cool, and use it as an adhesive for subsequent use;

[0076] (2) Take metoprolol tartrate, starch, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch according to the prescription ratio, and metoprolol tartrate→starch→2 / 3 of the prescription amount of sodium carboxymethyl starch → The sequence of low-substituted hydroxypropyl cellulose is uniformly mixed by the method of equal increment to obtain mixed powder;

[0077] (3) Add binder to the mixed powder described in step (2), obtain soft material by wet granulator, and then make granules, then boil and dry, sieve and granulate to obtain dry granules;

[0078] (4) take silicon dioxide, magnesium stearate by prescription ratio, join in the dry granule described in step (3) together with the carboxymethyl starch sodiu...

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PUM

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a metoprolol tartrate crystal, pharmaceutical composition containing the crystal and preparation methods of the metoprolol tartrate crystal and the pharmaceutical composition. The metoprolol tartrate crystal has the chemical structural formula shown in the description. The characteristic peak of an X-ray powder diffraction spectrum obtained through Cu-K alpha ray measurement is shown when 2 theta is 10.65 degrees, 12.98 degrees, 14.28 degrees, 15.03 degrees, 15.89 degrees, 16.93 degrees, 18.13 degrees, 19.45degrees, 20.43 degrees, 20.87 degrees, 21.66 degrees, 22.39 degrees, 23.20 degrees, 23.62 degrees and 24.06 degrees. The pharmaceutical composition containing the crystal is prepared from, in percentage by weight, 21%-45% of the metoprolol tartrate crystal, 36%-53% of starch, 6%-8% of low-substituted hydroxypropyl cellulose, 7%-11% of sodium carboxymethyl starch, 4%-6% of silicon dioxide, 1% of magnesium stearate and a proper amount of hydroxypropyl methylcellulose. Compared with the prior art, the obtained pharmaceutical composition has better solubility and excellent efficacy.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a metoprolol tartrate crystal, a pharmaceutical composition containing the crystal and a preparation method thereof. Background technique [0002] Metoprolol tartrate is a cardioselective beta-blocker without endogenous sympathomimetic activity, which can inhibit the excessive release of catecholamines in the circulatory system, upregulate the receptors of cardiomyocytes, and restore their sensitivity, Inhibit the excessively activated renin-angiotensin-aldosterone system, dilate peripheral blood vessels, and reduce water and sodium retention. Reduce cardiac preload and postload, and at the same time prevent cardiomyocyte hypertrophy and utilize antioxidants. It can improve myocardial energy metabolism and effectively inhibit sympathetic nerve excitation after medication. Reducing excessive heart rate, allowing adequate diastolic filling of the ventricles, improvi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C217/32C07C213/10C07C59/255C07C51/43A61K9/20A61K31/138A61K47/38A61K47/36A61K47/04A61K47/12A61P9/06
CPCA61K9/2009A61K9/2013A61K9/2054A61K9/2059C07B2200/13C07C51/43C07C59/255C07C213/10C07C217/32
Inventor 陈敏黄毅吴忠虹黄宁刘辉
Owner ZHUHAI TONGYUAN PHARMA CO LTD
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