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A kind of sustained-release medicine of metoprolol and preparation method thereof

A technology for slow-release drugs and drugs, which is applied in the directions of drug combinations, pharmaceutical formulations, and non-active ingredients medical preparations, can solve the problems of high price of silicon dioxide and low drug application rate, and saves the cost of preparations and the drug application rate. The effect of high rate and cost reduction

Active Publication Date: 2016-12-21
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 be greatly changed compared with coated granules

Method used

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  • A kind of sustained-release medicine of metoprolol and preparation method thereof
  • A kind of sustained-release medicine of metoprolol and preparation method thereof
  • A kind of sustained-release medicine of metoprolol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Comparison of drug coating on pellets with different particle sizes

[0060] Weigh 800g of metoprolol succinate raw material, add 1350ml of water, stir under heating, dissolve, obtain the coating solution containing medicine.

[0061] 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, the drug-containing coating solution is sprayed on the surface of the blank ball core by bottom spraying. After the drug application is completed, the material is continuously fluidized at 70°C for 5 minutes to obtain su...

Embodiment 2

[0064] Example 2 Comparison of the release rate of metoprolol succinate sustained-release pellets with blank sucrose cores of different particle sizes

[0065] prescription

[0066] Prescription of drug-loaded pellets:

[0067]

[0068] Slow-release coating formulation:

[0069] Ethyl cellulose (g) 200

[0070] HPC LF(g) 46

[0071] Preparation:

[0072] (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.

[0073]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 su...

Embodiment 3

[0079] Example 3 Effect of different ratios of ethyl cellulose and HPC on release

[0080] prescription

[0081] Prescription of drug-loaded pellets:

[0082] Metoprolol succinate (g): 800

[0083] Blank sucrose core (200~350μm) (g): 200

[0084] Slow-release coating formulation:

[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 sucrose pellets with a diameter of 200 μm to 350 μm, place them in a fluidized bed bottom spray coating pan, 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 solution on...

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Abstract

The invention discloses a metoprolol slow-release medicine, which comprises: a. a blank sucrose ball core; b. an active drug layer containing metoprolol, which is located on the surface of the blank ball core; c. A sustained-release coating layer of cellulose-based and hyprolose, which is located on the outside of the active drug layer. The invention also discloses a method for preparing the metoprolol slow-release medicine.

Description

technical field [0001] The invention relates to a sustained-release medicine 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 in a relatively large proportion 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 cardiomyopathy, aortic dissection, a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/138A61K47/38A61P9/12
CPCA61K9/5042A61K9/5078A61K31/138A61P9/00A61P9/12
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