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Slow-release pharmaceutical composition of metoprolol and preparation method of pharmaceutical composition

A technology of slow-release compositions and mixtures, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients. The effect of high drug rate and cost reduction

Active Publication Date: 2014-03-26
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Silicon dioxide is expensive, the drug loading rate is very low, and the release characteristics of the drug after tableting will change greatly compared with the coated granules

Method used

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  • Slow-release pharmaceutical composition of metoprolol and preparation method of pharmaceutical composition
  • Slow-release pharmaceutical composition of metoprolol and preparation method of pharmaceutical composition
  • Slow-release pharmaceutical composition of metoprolol and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1 Different particle size micropills are coated with medicine and this compares

[0058] Weigh 800g of metoprolol succinate raw material, add 1350ml of water, stir under heating, dissolve, obtain the coating solution containing medicine.

[0059] Weigh 100 μm to 200 μm, 200 μm to 350 μm, 400 μm to 610 μm, 610 μm to 750 μm sucrose pellet cores, and 200 μm to 350 μm silica pellet cores, respectively, and place them in the spray coating pan at the bottom of the fluidized bed, and set the inlet air temperature to 70°C (keep the temperature in the pot at 50±2°C); the air inlet pressure is 0.35bar; the atomization pressure is 1.5bar; the spray rate is 5-15g / min (adjust at any time according to the fluidization state). When the ball core is in a fluidized state, spray the drug-containing coating solution on the surface of the blank ball core by bottom spraying. After the drug application is completed, the material continues to be fluidized at 70°C for 5 minutes to o...

Embodiment 2

[0063] The release rate of the metoprolol succinate sustained-release pellets of different particle diameter blank sucrose ball cores is compared

[0064] prescription

[0065] Prescription of drug-loaded pellets:

[0066]

[0067] Slow-release coating formulation:

[0068] Ethyl cellulose (g) 200

[0069] HPC LF(g) 46

[0070] Preparation:

[0071] (1) Weigh 800g of metoprolol succinate raw material, add 1350ml of water, stir under heating at 60°C-70°C, dissolve, and pass through a 200-mesh sieve to obtain a drug-containing coating solution.

[0072]Weigh 200g of 100μm~200μm, 200μm~350μm, 400μm~610μm sucrose ball cores respectively, and place them in the spray coating pot at the bottom of the fluidized bed. ); the air inlet pressure is 0.35bar; the atomization pressure is 1.5bar; the spray rate is 5-15g / min (adjust at any time according to the fluidization state). When the sucrose core is in a fluidized state, spray the drug-containing coating solution on the surface...

Embodiment 3

[0078] Embodiment 3 Ethyl cellulose is different from HPC and the impact of this example on release

[0079] prescription

[0080] Prescription of drug-loaded pellets:

[0081] Metoprolol succinate (g): 800

[0082] Blank sucrose core (200~350m) (g): 200

[0083] Slow-release coating formulation:

[0084]

[0085]

[0086] Preparation:

[0087] (1) Weigh 800g of metoprolol succinate raw material, add 1350ml of water, stir under heating at 60°C-70°C, dissolve, and pass through a 200-mesh sieve to obtain a drug-containing coating solution.

[0088] Weigh 200g of 200μm ~ 350μm sucrose pellet core, put it in the fluidized bed bottom spray coating pot, set the inlet air temperature at 70°C (keep the temperature in the pot at 50±2°C); the inlet air pressure at 0.35bar ; The atomization pressure is 1.5bar; the spray rate is 5-15g / min (adjust at any time according to the fluidization state). When the sucrose core is in a fluidized state, spray the drug-containing coating s...

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Abstract

The invention discloses a metoprolol slow-release composition. The composition comprises: a, a blank sucrose pill core with the particle size of 200-350mu m; b, an active medicine layer containing metoprolol, wherein the active medicine layer is positioned on the surface of the blank pill core; and c, a slow-release coating layer containing ethyecellulose and hydroxypropylcellulose, wherein the slow-release coating layer is positioned outside the active medicine layer. The invention also discloses a method for preparing the pharmaceutical composition.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical composition of metoprolol and a preparation method thereof, in particular to a sustained-release pellet of metoprolol succinate and a preparation method thereof. Background technique [0002] Hypertension is one of the most common cardiovascular diseases in the world today, with a prevalence of about 10%. Some developed countries even reach 20%. There are about 600 million people with high blood pressure in the world. my country has now become a country with a high incidence of hypertension, and the incidence has been rising with a relatively large number of cases in the past 20 years. Metoprolol succinate (1-isopropylamino-3-[p-(2-methoxyethyl)phenoxy]-2-propanol L(+)-succinate) (formula I) is the The second-generation β1 receptor blocker is highly selective for the heart, and is mainly used for the treatment of hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/138A61K47/38A61P9/12
CPCA61K9/5078A61K31/138A61K9/5042A61P9/00A61P9/12
Inventor 高春生单利陈小平王玉丽杨美燕林韶辉
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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