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Metoprolol tartrate sustained-release tablet and preparation method thereof

A technology for metoprolol tartrate and sustained-release tablets, which is applied to pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problems of complicated preparation process, high production cost and difficult release curve. control and other problems, to achieve the effect of simple preparation method, avoiding toxic and side effects, and significant slow-release characteristics

Active Publication Date: 2013-11-13
CHONGQING GUOZHONG MEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has the following defects: 1. The prescription and preparation process of the prior art are relatively complicated, and the production cost is high, which is not conducive to industrial production; at the same time, because of the use of skeleton materials and the addition of various types of resistance auxiliary materials, the quality is not easy to control; 2. Due to the high viscosity and strong moisture absorption of slow-release framework materials, greasy and sticky phenomena are often prone to occur in the production process
3. The release curve of the existing metoprolol tartrate sustained-release tablets is not easy to control. Occasionally, the phenomenon of sudden release in the first period of time or the release rate in the first period of time cannot reach the metoprolol tartrate sustained-release tablet stipulated in the second part of the 2010 edition of the Pharmacopoeia. According to the standard requirements for release tablets, according to the 2010 edition of Pharmacopoeia Part II, the standards for metoprolol tartrate sustained-release tablets, the dissolution amount of each tablet at 1, 4 and 8 hours should be 25% to 45% of the labeled amount, respectively. 40%~75%, and over 75%

Method used

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  • Metoprolol tartrate sustained-release tablet and preparation method thereof
  • Metoprolol tartrate sustained-release tablet and preparation method thereof
  • Metoprolol tartrate sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Prepare Metoprolol Tartrate Extended Release Tablets as follows:

[0040] (1) Mix metoprolol tartrate: 30%, sustained-release matrix material: 25% hypromellose, and mix for 20min to 30min to obtain a mixed powder, wherein the model of hypromellose used is K4M ;

[0041] (2) add binding agent again in the mixed powder: with the 1.2% hydroxypropyl methylcellulose 20% soft material of the preparation of 85% ethanol solution, cross 18 mesh sieves and granulate, get wet granule;

[0042] (3) Dry the wet granules in a hot air circulation oven at 50°C to 60°C until the moisture content is ≤3% to obtain dry granules;

[0043] (4) Pass the dry granules through a 16-mesh sieve for granulation; put the dry granules and lubricants: 0.8% of magnesium stearate, 1.0% of micropowder silica gel, and mix them in a mixer, and the mixing time is about 20min to 30min;

[0044] (5) The dry granules mixed with the lubricant in step (4) are placed in a tablet press, and the pressure is adjus...

Embodiment 2

[0057] The addition amount of each raw material is: 35.0% of metoprolol tartrate, sustained-release matrix material: 20.0% of hypromellose, lubricant: 0.25% of magnesium stearate, 2.0% of micropowder silica gel, binder: 25.0%, film coating premix 2.75%, purified water 15.0%, the binder is 1.2% hydroxypropyl methylcellulose prepared with 95% ethanol solution, wherein the hydroxypropylmethylcellulose used The model of cellulose is K4M.

[0058] Its preparation method and release measurement method are the same as in Example 1.

[0059] The release measurement results are as follows:

[0060]

[0061] Finally, the release curve of this test was drawn by calculating the average release rate of the six samples in each period.

Embodiment 3

[0063] The addition amount of each raw material is: 40.0% of metoprolol tartrate, sustained-release matrix material: 25.0% of hydroxypropyl cellulose, lubricant: 2.5% of magnesium stearate, 0.1% of micropowder silica gel, binder: 15.0% %, film coating premix 1.4%, purified water 16.0%, and the binder is 1.2% hydroxypropyl methylcellulose prepared with 70% ethanol solution.

[0064] Its preparation method and release measurement method are the same as in Example 1.

[0065] The release measurement results are as follows:

[0066]

[0067] Finally, the release curve of this test was drawn by calculating the average release rate of the six samples in each period.

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Abstract

The invention provides a metoprolol tartrate sustained-release tablet and a preparation method thereof. The tablet is composed of the components of, by weight: 30-50% of metoprolol tartrate, 15-30% of a sustained-release framework material, 0.35-10.0% of a lubricant, 10.0-30.0% of an adhesive, 0.5-5.0% of a film coating premix, and 10.0-30.0% of purified water. Compared with prior art, the tablet and the method provided by the invention have the advantages of simple preparation method, low production cost, suitability for industrialized productions, no greasy and sticky phenomenon during a production process, and smooth release curve. With the tablet, a sudden release phenomenon of a first time period is prevented, and a phenomenon of unqualified release speed at a first time period is also prevented.

Description

technical field [0001] The invention relates to a metoprolol tartrate sustained-release tablet 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, improving active diastolic function, reducing energy requirements and increasing myocardial performance, c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/205A61K31/138A61K47/38A61P9/06A61P9/08
Inventor 李朝阳昝琼谈宗华李达富幸慧吴统选
Owner CHONGQING GUOZHONG MEDICAL
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