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Metoprolol slow-release tablet and preparation method thereof

A torolol sustained-release tablet and a torolol tablet technology are applied in the field of medicine, and can solve the problems of sudden drug release, reducing the efficacy of metoprolol, affecting the stable release rate of the active drug of metoprolol, and the like. The effect of avoiding drug burst release and reducing the degree of fragmentation

Active Publication Date: 2012-08-08
华益泰康药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, when the tablet is compressed, the strong mechanical external force is easy to crush the drug-containing pellets coated with the sustained-release layer, exposing the active drug inside, and affecting the concentration of the active drug of metoprolol in the sustained-release tablet. Stable release rate, resulting in drug burst release
Although some anti-compression excipients are added to the existing tablets during tablet compression, the phenomenon of drug burst release still occurs
As a result, the drug cannot be released stably, reducing the efficacy of metoprolol

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: Preparation of metoprolol sustained-release tablet of the present invention

[0047] 1. Formula

[0048] See Table 1.

[0049] Table 1 Formulation

[0050]

[0051] 2. Preparation method

[0052] To prepare medicated pellets:

[0053] Dissolve the prescribed amount of HPMC E5 and metoprolol succinate in water, add microcrystalline cellulose PH-F20JP and crystalline cellulose to the solution under stirring to disperse them, and set aside.

[0054] Weigh the prescribed amount of sucrose pellets and place them in the fluidized bed. After starting the instrument and setting the experimental parameters, after the temperature of the material reaches the set material temperature, spray the liquid with the bottom spray method. The experimental parameters are: the diameter of the nozzle is 0.5mm, the air inlet temperature is 55-60°C, the material temperature is 30-45°C, and the atomization pressure is 0.15-0.20MPa.

[0055] Package isolation layer:

[0056...

Embodiment 2

[0069] Embodiment 2: Preparation of metoprolol sustained-release tablet of the present invention

[0070] 1. Formula

[0071] See Table 2.

[0072] Table 2 Formulation

[0073]

[0074]

[0075] 2. Preparation method

[0076] To prepare medicated pellets:

[0077] Take an appropriate amount of water in a beaker, heat it to 70-80°C, add the prescribed amount of HPMC E5 into the water and stir to disperse it. After cooling down, wait until HPMC E5 is completely dissolved, add metoprolol succinate, microcrystalline cellulose PH101 and HPMC K4M according to the prescription amount in the table, mix well and place in a wet granulator, set the speed of the stirring paddle at 200-250 rpm The speed of the cutting knife is 2000-3000 rpm, and after dry mixing, an appropriate amount of purified water is gradually added to make a soft material.

[0078] The prepared soft material was transferred to an extruder and extruded into strips with a diameter of 0.4 mm, and the screw sp...

Embodiment 3

[0093] Embodiment 3: Preparation of metoprolol sustained-release tablet of the present invention

[0094] 1. Formula

[0095] See Table 3.

[0096] Table 3 Formulation

[0097]

[0098]

[0099] 2. Preparation method

[0100] To prepare medicated pellets:

[0101] Dissolve the prescribed amount of HPMC E5 and metoprolol succinate in water, add microcrystalline cellulose PH-F20JP and crystalline cellulose to the solution under stirring to disperse them, and set aside.

[0102] Weigh the prescribed amount of microcrystalline cellulose pellets and place them in the fluidized bed. After starting the instrument and setting the experimental parameters, after the material temperature reaches the set material temperature, spray the liquid and apply the medicine by bottom spraying. The experimental parameters are: the diameter of the nozzle is 0.5mm, the air inlet temperature is 55-60°C, the material temperature is 30-45°C, and the atomization pressure is 0.15-0.20MPa.

[0103...

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Abstract

The invention relates to the technical field of pharmaceutics and discloses a metoprolol slow-release tablet and a preparation method thereof. The preparation method provided by the invention comprises the following steps: preparing a metoprolol active drug and a first plastic material into a pastille pill; obtaining slow-release pastille pill by coating a slow-release layer; and tabletting together with a tablet agent containing at least 90wt% of second plastic material. During the process of preparing the metoprolol slow-release tablet according to the invention, the specific material is added to the active drug and the tablet accessory, so that the crushing degree of the slow-release pastille pill is relieved, the stable releasing of the active drug of the slow-release tablet is ensured and the sudden releasing phenomenon of the drug is avoided.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a metoprolol sustained-release tablet and a preparation method thereof. Background technique [0002] Metoprolol, chemically known as 1-isopropylamino-3-[p-(2-methoxyethyl)phenoxy]-2-propanol, is a highly selective beta1-receptor for the heart Retardant, structural formula is as follows: [0003] [0004] Hypertension has become one of the major diseases threatening human health, and studies have shown that metoprolol can effectively treat hypertension, and long-term use can significantly reduce the risk of death in patients with heart failure. It is one of the first choices of antihypertensive drugs. In addition, metoprolol can also be used for symptoms such as angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, and cardiac neurosis. [0005] At present, metoprolol widely used in China is mainly metoprolol ta...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/138A61K47/38A61P9/12A61P9/04A61P9/10A61P9/00A61P9/06A61P25/00A61P5/16
Inventor 诸弘刚谭海松何燕妮赵兰敏张松琼黎继清徐艳
Owner 华益泰康药业股份有限公司
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