Metoprolol sustained-release tablet and preparation method thereof

A technology for torolol sustained-release tablets and sustained-release tablets, which are applied in directions such as pharmaceutical formulations, medical preparations containing active ingredients, and pill delivery, can solve the problems of complex processes, long process time, low production efficiency, and the like, and achieve simplification. The preparation process, the process operation are simple, and the production efficiency is high.

Inactive Publication Date: 2015-04-22
田武
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 1. The preparation of the sustained-release pellets includes two steps of adding drug to the core and coating the sustained-release coating. The process of applying the drug to the core takes a long time, resulting in low production efficiency
[0007] 2. Sustained-release pellets may be crushed during the tableting process, resulting in the risk of sudden drug release
[0008] 3. Toxic solvents are used when coating the controlled release layer, which is not conducive to the control of drug safety
[0009] 4. Due to its own preparation process, if machines such as high-speed high-shear mixers and grinding equipment are used in the preparation process, the preparation process will be long, the pro...

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] prescription

[0046]

[0047]

[0048] Preparation Process:

[0049] (1) Mix the active ingredients metoprolol succinate, hydroxypropyl cellulose K4M Premium, povidone K29 / 32 and magnesium stearate in the proportion of the above formula and mix them evenly;

[0050] (2) Using dry granulation to compress the mixture into granules;

[0051] (3) Collect the granules and fine powder. As for the mixer, add the prescribed amount of hydroxypropyl cellulose K100 Premium LV CR, micro-powder silica gel (Aerosil 200 Pharma), and magnesium stearate, and mix well.

[0052] (4) Press into tablets as required;

[0053] (5) The tablet core is coated, and the weight gain of the coating is controlled at about 5%.

Embodiment 2

[0055] prescription

[0056]

[0057]

[0058] Preparation Process:

[0059] (1) Mix the active ingredients metoprolol succinate, hydroxypropyl cellulose K100M Premium, povidone K29 / 32 and magnesium stearate in the proportion of the above-mentioned formula amount and stir evenly;

[0060] (2) Using dry granulation to compress the mixture into granules;

[0061] (3) Collect the granules and fine powder. As for the mixer, add the prescribed amount of hydroxypropyl cellulose K100 Premium LV CR, micro-powder silica gel (Aerosil 200 Pharma), and magnesium stearate, and mix well.

[0062] (4) Press into tablets as required;

[0063] (5) The tablet core is coated, and the weight gain of the coating is controlled at about 5%.

Embodiment 3

[0065] prescription

[0066]

[0067]

[0068] Preparation Process:

[0069] (1) Mix the active ingredients metoprolol succinate, hydroxypropyl cellulose K15M Premium, and magnesium stearate in the proportion of the above formula and mix them evenly;

[0070] (2) Using 10% povidone K29 / 32 aqueous solution as a binder, wet granulation is used to make the mixture into granules;

[0071] (3) After the granules are dried at 60°C, the granules are sized at 24 mesh, and the granules and fine powder are collected. As for the mixer, add the prescribed amount of hydroxypropyl cellulose K100 Premium LV CR, pre-crossed starch, and micronized silica gel (Aerosil 200 Pharma), magnesium stearate, mix well.

[0072] (4) Press into tablets as required;

[0073] (5) The tablet core is coated, and the weight gain of the coating is controlled at about 5%.

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PUM

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Abstract

The invention discloses a metoprolol sustained-release tablet and a preparation method thereof. The metoprolol sustained-release tablet contains an effective component metoprolol. The preparation method comprises the following steps: firstly, pelletizing medicines and one part of auxiliary materials; then mixing the prepared particles with other sustained-release auxiliary materials, and pressing to form tablet cores; and finally wrapping the tablet cores with a layer of sustained-release coating, so as to form a release curve of which the drug releasing rate is close to zero level and the drug releasing time can reach over 20 hours.

Description

Technical field [0001] The invention relates to a sustained-release tablet containing metoprolol as a drug ingredient and a preparation method thereof. The prepared sustained-release preparation can well control the early release of the drug, and the sustained-release effect is close to zero-order release, and the sustained release can reach More than 20 hours. Background technique [0002] Metoprolol succinate is a cardiovascular system drug used for high blood pressure; angina pectoris; chronic heart failure with stable symptoms with abnormal left ventricular systolic function. Metoprolol is a selective β1 receptor blocker. It is one of the commonly used drugs for the treatment of hypertension, coronary heart disease, chronic heart failure and arrhythmia. The dose required for metoprolol to act on cardiac β1 receptors is lower than the dose required for β2 receptors on peripheral blood vessels and bronchus to act, so the selectivity of metoprolol is dose-dependent. Since the ...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K9/36A61K31/138A61P9/00
Inventor 田武
Owner 田武
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