Metroprolol succinate sustained-release tablets and preparation method thereof

A technology of metoprolol succinate and sustained-release tablets, which can be applied in pharmaceutical formulations, medical preparations with inactive ingredients, cardiovascular system diseases, etc., and can solve problems such as sudden drug release, large environmental pollution, and solvent solvent residues , to achieve the effect of improving production efficiency

Inactive Publication Date: 2017-05-24
YAOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 1) In order to obtain the final product metoprolol succinate sustained-release tablets, the blank pellets first need to be coated with drugs to prepare drug-loaded pellets, and then coated with sustained-release materials to prepare sustained-release pellets, and then the sustained-release pellets are mixed with excipients Mixing, and finally tableting, the whole process takes a long time, the process is complicated, and the production cost is high;
[0006] 2) There is a risk of breakage during the tableting process of the sustained-release pellets, which may lead to sudden release of the drug;
[0007] 3) The coating liquid solvent used in the coating process is organic solvents such as dichloromethane and isopropanol. This solvent has certain toxicity, and the production process has relatively high environmental pollution and high production costs.
[0010] 1) Use the organic solvent ethanol as the wetting agent, there may be a risk of solvent residue in the product, and the solvent recovery is difficult, and it will pollute the environment to a certain extent during industrialized large-scale production;
[0011] 2) More intermediates are produced in the production process, and the process is more complicated;
[0013] i. The production process is more complex, time-consuming and costly;
[0014] ii. Organic solvents are used in the production process, and solvent recovery is difficult. Due to the large-scale use of organic solvents in the industrialized production process, there is a certain pollution to the environment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Metoprolol Succinate Extended Release Tablets

[0030] Material name percentage(%) Silica blank ball core 15.0 metoprolol succinate 19.0 Aqueous dispersion of ethyl cellulose (solid content) 7.2 Ethyl cellulose 37.2 Hydroxyethyl cellulose 18.6 Micropowder silica gel 3.0 total 100.0

[0031] According to the prescription ratio, weigh the prescription amount of silica blank pellet core (100~200μm), metoprolol succinate (d 0.9 =34μm), ethyl cellulose (d 0.9 =16μm), hydroxyethyl cellulose was premixed and set aside. At the same time, dilute the ethylcellulose aqueous dispersion to a concentration of 10-15% with purified water. Open the fluidized bed top spray one-step granulator, put the premixed material into the granulator, start the preheating step, preheat for a period of time, when the product temperature reaches 30℃~35℃, spray diluted ethyl alcohol The cellulose-based aqueous dispersion solution is used for g...

Embodiment 2

[0033] Metoprolol Succinate Extended Release Tablets

[0034] Material name percentage(%) Silica blank ball core 15.0 metoprolol succinate 19.0 Aqueous dispersion of ethyl cellulose (solid content) 7.2 Ethyl cellulose 37.2 Hydroxyethyl cellulose 18.6 Micropowder silica gel 3.0 total 100.0

[0035] In embodiment 2, prescription is identical with embodiment 1, and difference is that metoprolol succinate d 0.9 =12μm, ethyl cellulose d 0.9 = 8 μm, using the same preparation process as in Example 1 to granulate, the recovery rate in the granulation process was 90.1%, which was significantly lower than the recovery rate reported in Example 1, showing that it is very necessary to control the particle size of the material .

Embodiment 3

[0037] Metoprolol Succinate Extended Release Tablets

[0038] Material name percentage(%) Silica blank ball core 10.0 metoprolol succinate 19.0 Aqueous dispersion of ethyl cellulose (solid content) 8.0 Ethyl cellulose 41.0 Hydroxyethyl cellulose 20.5 Micropowder silica gel 1.5 total 100.0

[0039] Using the same preparation process in Example 1, the prepared sustained-release tablets were compared with the commercially available products of AstraZeneca for dissolution in vitro, f 2 =57, proving that the dissolution of the two is consistent.

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PUM

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Abstract

The invention relates to metroprolol succinate sustained-release tablets and a preparation method thereof. The sustained-release tablets comprise: a main medicine: metroprolol succinate; a sustained-release material: ethyecellulose; a pore-forming agent: hydroxyethyl cellulose; an adhesive: ethyecellulose aqueous dispersion; a filling agent: silicified microcrystalline cellulose; a flow aid: micropowder silica gel; a coating material: opadry II. The preparation method comprises the steps: mixing the main medicine and other auxiliary materials except for the flow aid and the coating material and performing one-step pelletization by a fluidized bed top-spray one-step pelletization process to obtain sustained-release granules; adding the flow aid into the sustained-release granules, mixing uniformly and tabletting; coating the compressed tablets with the opadry II to obtain the final sustained-release tablets.

Description

technical field [0001] The invention belongs to the field of oral sustained-release drug preparations, and relates to a metoprolol succinate sustained-release tablet and a preparation method thereof. Background technique [0002] Metoprolol succinate extended-release tablets are indicated for hypertension, angina pectoris, and symptom-stable chronic heart failure with abnormal left ventricular systolic function. This product was developed by British AstraZeneca, and it was launched in Europe and the United States in 1986. It can obtain 24-hour stable blood concentration of β after one administration. 1 The blocking effect greatly improves the therapeutic efficacy, so it is quickly accepted by the majority of clinicians and has become the most widely used β-blocker in the world. [0003] US Patent No. 4927640 discloses a preparation method of metoprolol succinate sustained-release tablets. In this patent, the fluidized bed coating technology is adopted. First, the raw mater...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/138A61K47/38A61K47/04A61P9/12A61P9/10A61P9/04
Inventor 朱锋曹呈勇刘丽
Owner YAOPHARMA CO LTD
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