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Metoprolol sustained release medicinal compositions and preparation method thereof

A slow-release composition and slow-release coating technology, which can be used in drug combinations, pharmaceutical formulations, drug delivery and other directions, and can solve problems such as changes

Active Publication Date: 2011-03-30
北京利龄恒泰药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the metoprolol microparticles or micropills prepared above all use silicon dioxide as the core, and the prepared micropills are further compressed into tablets. than, there will be a big change

Method used

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  • Metoprolol sustained release medicinal compositions and preparation method thereof
  • Metoprolol sustained release medicinal compositions and preparation method thereof
  • Metoprolol sustained release medicinal compositions and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 Different size micropills are coated with medicine and compare

[0038] Weigh 4g of HPMC (6cps), add water to soak overnight, and dissolve. Then add 200g of metoprolol tartrate raw material respectively, then add water, stir and dissolve in a heated state, and obtain the drug-containing coating solution.

[0039] Weigh and weigh 300g of 300μm~400μm, 400μm~500μm, 500μm~610μm, 610μm~750μm sucrose pellets respectively, and place them in the spray coating pan at the bottom of the fluidized bed. Keep at 45±2℃); air inlet pressure is 0.35bar; atomization pressure is 1.5bar; liquid spray rate is 3~5g / min (adjust at any time according to the fluidization state). When the sucrose core was in a fluidized state, the drug-containing coating solution was sprayed on the surface of the blank core by bottom spraying. After the application of the drug, the material continued to be fluidized at 45°C for 5 minutes to obtain the HPMC at different dosage levels. The drug-loaded...

Embodiment 2

[0042] Comparison of different binders in embodiment 2 active drug coating solution

[0043] Weigh 4g each of HPMC (6cps), PVP, and HPC, add water to soak, and dissolve. Then add 200g of metoprolol tartrate raw material, add water 200mL, heat and stir, dissolve, and obtain the coating solution containing medicine.

[0044] Weigh 300g of sucrose ball cores (26-35 mesh), place them in a fluidized bed bottom spray coating pan, set the inlet air temperature at 60°C (keep the temperature in the pot at 45±2°C); the inlet air pressure at 0.35 bar; the atomization pressure is 1.5bar; the spray rate is 3-5g / min (adjust at any time according to the fluidization state). When the sucrose core was in a fluidized state, the drug-containing coating solution was sprayed on the surface of the blank core by bottom spraying. After the application of the drug, the material continued to be fluidized at 45°C for 5 minutes to obtain the HPMC at different dosage levels. Drug-loaded pellets, weighed...

Embodiment 3

[0047] Embodiment 3 pellet active drug coating

[0048] Weigh 4g each of 6cps, 20cps, and 50cps HPMC, add water to soak, and dissolve. Then add 200g of metoprolol tartrate raw material, add water 200mL, heat and stir, dissolve, and obtain the coating solution containing medicine.

[0049] Weigh 300g of sucrose ball cores (26-35 mesh), place them in a fluidized bed bottom spray coating pan, set the inlet air temperature at 60°C (keep the temperature in the pot at 45±2°C); the inlet air pressure at 0.35 bar; the atomization pressure is 1.5bar; the spray rate is 3-5g / min (adjust at any time according to the fluidization state). When the sucrose core was in a fluidized state, the drug-containing coating solution was sprayed on the surface of the blank core by bottom spraying. After the application of the drug, the material continued to be fluidized at 45°C for 5 minutes to obtain the HPMC at different dosage levels. Drug-loaded pellets, weighed.

[0050] Table 3 The results of ...

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Abstract

The invention discloses a metoprolol tartrate extended release compound which comprises a. a hollow pill core; b. an active medicine layer containing metoprolol or medicine salt of the metoprolol and at least a bond, and the layer is positioned on the surface of the hollow pill core; c. a release coat layer containing acrylic acid resin NE30D and French chalks, and the release coat layer is positioned outside the active medicine layer. The invention also discloses a method of preparing the medicine compound.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical composition of metoprolol and a preparation method thereof. In particular, it relates to a slow-release pellet of metoprolol tartrate 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 tartrate (1-isopropylamino-3-[p-(2-methoxyethyl)phenoxy]-2-propanol L(+)-tartrate) (formula I) is the second generation It is a highly selective β1 receptor blocker for the heart, and is mainly used for the treatment of hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/138A61K9/00A61K47/02A61K47/38A61P9/12
Inventor 高春生黄健单利颜弘
Owner 北京利龄恒泰药业有限公司
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