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Metoprolol tartrate tablet and preparation method thereof

A technology for metoprolol tartrate and torolol tablets, which is applied in the directions of pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. The effect of strong viscosity and simple ingredients

Pending Publication Date: 2021-02-19
北京中科利华医药研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The solubility of metoprolol tartrate in water is very large, and the actual measurement can reach 1.5g / mL. However, most of the traditional wet granulation uses lactose or lactose mixed with other materials such as microcrystalline cellulose and mannitol as fillers, but lactose will Maillard reaction occurs with the amino group of metoprolol to generate brown or even black macromolecular substance melanoidin or melanoidin, which makes the final metoprolol tartrate tablets contain related substances and increases impurities

Method used

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  • Metoprolol tartrate tablet and preparation method thereof
  • Metoprolol tartrate tablet and preparation method thereof
  • Metoprolol tartrate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] A kind of preparation method of metoprolol tartrate sheet, concrete steps are:

[0035] (1) Weighing raw materials: Internal addition: 20 mg of metoprolol tartrate, 305 mg of povidone K, 60 mg of microcrystalline cellulose, 4 mg of sodium carboxymethyl starch, 15 mg of water (wetting agent); external addition: sodium carboxymethyl starch 4mg, micropowder silica gel 1.5mg, magnesium stearate 1mg, spare;

[0036] (2) Granulation:

[0037] First, mix povidone K30 and sodium carboxymethyl starch evenly, then add metoprolol tartrate and microcrystalline cellulose, put the material in a wet granulator for mixing and stirring at 30Hz (420rpm), shear at 20Hz (1120rpm )) 5 minutes, take 3 samples from each position of the upper, middle and lower positions of the mixed material in the wet granulation pot, each about 1 mg, a total of 9 samples are sent for analysis and inspection, and the mixing uniformity is measured. Granulate; add water to the mixed material (control the time...

Embodiment 2

[0042] A kind of preparation method of metoprolol tartrate sheet, concrete steps are:

[0043] (1) Weighing raw materials: Internal addition: 30 mg of metoprolol tartrate, 306 mg of povidone K, 75 mg of microcrystalline cellulose, 6 mg of sodium carboxymethyl starch, 20 mg of water (wetting agent); external addition: sodium carboxymethyl starch 7mg, micropowder silica gel 4mg, magnesium stearate 3mg, spare;

[0044] (2) Granulation:

[0045]First, mix povidone K30 and sodium carboxymethyl starch evenly, then add metoprolol tartrate and microcrystalline cellulose, put the material in a wet granulator for mixing and stirring at 30Hz (420rpm), shear at 20Hz (1120rpm )) 5 minutes, take 3 samples from each position of the upper, middle and lower positions of the mixed material in the wet granulation pot, each about 1 mg, a total of 9 samples are sent for analysis and inspection, and the mixing uniformity is measured. Granulate; add water to the mixed material (control the time of...

Embodiment 3

[0050] A kind of preparation method of metoprolol tartrate sheet, concrete steps are:

[0051] (1) Weighing raw materials: Internal addition: Metoprolol tartrate 25mg, povidone K305.5mg, microcrystalline cellulose 72.5mg, sodium carboxymethyl starch 5mg, water (wetting agent) 19mg; external addition: carboxymethyl Sodium starch starch 5mg, micropowder silica gel 2.4mg, magnesium stearate 1.8mg, spare;

[0052] (2) Granulation:

[0053] First, mix povidone K30 and sodium carboxymethyl starch evenly, then add metoprolol tartrate and microcrystalline cellulose, put the material in a wet granulator for mixing and stirring at 30Hz (420rpm), shear at 20Hz (1120rpm )) 5 minutes, take 3 samples from each position of the upper, middle and lower positions of the mixed material in the wet granulation pot, each about 1 mg, a total of 9 samples are sent for analysis and inspection, and the mixing uniformity is measured. Granulate; add water to the mixed material (control the time of addi...

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Abstract

The invention discloses a metoprolol tartrate tablet. The tablet is prepared from the following raw materials in parts by weight: 20-30 parts of metoprolol tartrate, 60-75 parts of microcrystalline cellulose, 9-12 parts of a disintegrating agent I and 15-20 parts of water which are internally added; and 4-7 parts of a disintegrating agent II and 2.5-7 parts of a lubricating agent which are externally added. According to the metoprolol tartrate tablet and a preparation method thereof provided by the invention, the composition of the raw materials in the formula is reduced, the standard of quality requirements is met, the generation of related substances is reduced, and a preparation is purer and safer; the preparation is simple in auxiliary material components, operation is convenient, prepared granules are good in flowability and high in viscosity resistance, sticking cannot be caused during tabletting, the drug stability can be improved, and the bitterness of a main drug is covered, the release degree of the tablet is not influenced; and the method is suitable for industrial production and has a relatively high application value.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a metoprolol tartrate tablet and a preparation method thereof. Background technique [0002] Metoprolol tartrate belongs to class 2A, β1-blockers without partial agonistic activity (cardioselective β-blockers). It has selective blocking effect on β1-receptor, no PAA (partial agonistic activity), no membrane stabilizing effect. Its blocking effect on β-receptor is about equal to that of propranolol (PP), and its selectivity to β1-receptor is slightly inferior to that of atenolol. The effects of metoprolol on the heart, such as slowing heart rate, inhibiting contractility, reducing self-discipline and delaying atrioventricular conduction time, are similar to those of propranolol and atenolol (AT). The effect of blood pressure and heart rate is also similar to that of PP and AT. Its contraction effect on blood vessels and bronchial smooth muscle is weaker than...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/32A61K47/36A61K47/12A61K47/04A61K31/138A61P9/12A61P9/10A61P9/00A61P9/06A61P5/16A61P25/00
CPCA61K9/2095A61K9/2054A61K9/2059A61K9/2027A61K9/2013A61K9/2009A61K31/138A61P9/12A61P9/10A61P9/00A61P9/06A61P5/16A61P25/00
Inventor 杨玲王登才路梦莹黄文艺王丛笑
Owner 北京中科利华医药研究院有限公司
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