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Metoprolol tartrate matrix sustained-release tablet

A technology of metoprolol tartrate and matrix slow-release materials, which is applied in the direction of sugar-coated pills, pill delivery, endocrine system diseases, etc. It can solve the problems of decreased drug release, affecting drug release, cumbersome process, etc., and achieves good linearity and low cost. , The effect of low process requirements

Active Publication Date: 2011-04-13
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] It can be seen from Fig. 1 in vitro release curve in this article that the drug release is basically constant at 0-10 hours, and the release rate is about 0.052 / h. However, at 10-12 hours, the drug release is less than 5%, and the drug release rate is less than 0.025 / h. obvious downward trend
[0023] In addition, the compression of the three-layer tablet requires the use of a three-layer tablet press, and its process is cumbersome. At present, there are few three-layer tablet presses that can be used for industrial production at home and abroad. In the article, S.M.Al-Saidan et al. use a single-layer tablet press The three-layer tablet is compressed manually by the machine, and the compression force between the layers and the compressed density significantly affect the release of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Embodiment 1 metoprolol tartrate contains the double-layer tablet of control layer

[0077] 1) Prescription composition

[0078] drug layer

[0079]

[0080] Regulatory layer

[0081]

[0082] 2) Preparation process:

[0083] Drug layer:

[0084]1. Take the prescribed amount of metoprolol tartrate, hypromellose K4M, hypromellose K15M, micropowder silica gel and stearic acid and mix evenly;

[0085] 2. 10% PVP k30 85% ethanol solution to make soft materials, pass through a 20-mesh sieve to make wet granules;

[0086] 3. Dry at 40°C, pass through a 20-mesh sieve for granulation;

[0087] 4. Add the prescribed amount of magnesium stearate and mix well. Theoretical tablet weight: 189.5mg

[0088] Regulatory layer:

[0089] 1. Take the prescribed amount of hydroxypropyl methylcellulose K4M, micropowder silica gel, and stearic acid and mix evenly;

[0090] 2. 10% PVP k30 85% ethanol solution to make soft materials, pass through a 20-mesh sieve to make wet granu...

Embodiment 2

[0101] Embodiment 2 Metoprolol tartrate contains the double-layer tablet and single-layer tablet contrast of control layer

[0102] Prescription: See Table 8 below

[0103] Preparation process: with embodiment 1

[0104] According to the United States Pharmacopoeia USP30 Metoprolol Succinate Sustained-release Tablet Standard, the release results are shown in Table 9 below, and all data are the average values ​​of 6 samples from the same batch.

[0105] Table 8 Example 2 prescription

[0106]

[0107] *(Klucel MF)

[0108] ▲(Klucel HF)

[0109] ◆(kollicoat SR)

[0110] ★Adhesive: 10% PVP K30 85% ethanol solution

[0111] Table 9 release results

[0112]

[0113] In this example, the comparison between the double-layer tablet containing metoprolol tartrate containing the regulating layer and the traditional single-layer tablet shows that on the basis of the single-layer tablet that releases too fast in the early stage, adding an appropriate regulating layer can obtai...

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Abstract

The invention provides a novel metoprolol tartrate-containing matrix sustained-release tablet, i.e. a metoprolol tartrate matrix sustained-release tablet with a regulation layer. The novel double-layer matrix sustained-release tablet with the regulation layer is prepared by adding the regulation layer on the basis of the traditional metoprolol tartrate matrix sustained-release tablet, can release medicines uniformly in 24 hours, overcomes the defects of the metoprolol tartrate sustained-release tablet in the prior art, and has the advantages of ideal release effect, simple process and low cost.

Description

technical field [0001] The invention relates to a novel matrix sustained-release tablet containing metoprolol tartrate, in particular to a metoprolol tartrate matrix sustained-release tablet with a regulating layer, which can be sustained-release for 24 hours. Background technique [0002] Metoprolol is a β1-receptor blocker without partial agonist activity (cardioselective β-receptor blocker), used for the treatment of hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, main Arterial dissection, arrhythmia, hyperthyroidism, cardiac neurosis, etc., have also been found to be useful in the treatment of heart failure in recent years. [0003] Metoprolol itself has low solubility in water, which affects its bioavailability. Therefore, the metoprolol preparations currently on the market are mainly its salts, such as metoprolol tartrate, metoprolol succinate etc., the dosage forms include ordinary tablets, sustained-release tablets, controlled-rele...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/28A61K31/138A61P9/12A61P9/10A61P9/06A61P9/00A61P9/04A61P5/16
Inventor 姜庆伟梁希刘全志杨文斌
Owner 北京天衡药物研究院有限公司
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