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Slow-release medicinal preparation for treating heart diseases

A sustained-release drug and sustained-release preparation technology, which is applied in the field of sustained-release pharmaceutical preparations and metoprolol sustained-release drugs, can solve the problems of poor sustained-release effect, unsatisfactory demand, and low drug load, and achieve good results. The effect of application prospect, simple preparation method and controllable carrier pore size

Inactive Publication Date: 2016-05-11
BEIJING HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, in the current drug loading method, the inner and outer pores of the silica carrier used are all mesoporous materials.
After the drug enters the surface pores of the carrier, there is not enough mass transfer driving force to realize the further loading of the drug, so that the final loading of the drug is not high, and the sustained release effect is not good, which cannot meet the needs

Method used

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  • Slow-release medicinal preparation for treating heart diseases
  • Slow-release medicinal preparation for treating heart diseases
  • Slow-release medicinal preparation for treating heart diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] One. Preparation of metoprolol tartrate sustained-release preparation

[0037] (1) Preparation of spherical mesoporous silica nanoparticles (MCM-41)

[0038] Place the three-neck flask in a water bath at 80°C, measure 240 ml of deionized water and 1.75 ml of NaOH solution with a concentration of 2 mol / L, and then add 0.5 g of cetyl ammonium bromide. After stirring, after the solution was clarified, 0.3 ml of mesitylene was added according to the molar ratio of tetraethyl orthosilicate (TEOS) to mesitylene (TMB) being 0.2. After stirring for 5 min, 2.5 ml of ethyl orthosilicate was added dropwise. After stirring for 2 hours, it was naturally cooled to obtain a white suspension, which was filtered with suction, washed with deionized water three times, and dried in a vacuum oven at 60°C. Put the obtained white powder into 200 ml of ammonium nitrate ethanol solution with a concentration of 1 g / ml and reflux at 80°C for 8 hours, filter with suction, wash with ethanol for 3...

Embodiment 2

[0044] One. Preparation of metoprolol tartrate sustained-release preparation

[0045] (1) Preparation of spherical mesoporous silica nanoparticles (MCM-41)

[0046] The three-neck flask was placed in a water bath at 80°C, 240 ml of deionized water and 1.75 ml of NaOH solution with a concentration of 2 mol / L were measured, and then 0.5 g of cetyl ammonium bromide was added. After stirring, after the solution is clarified, 0.6 ml of mesitylene is added according to the molar ratio of tetraethyl orthosilicate (TEOS) to mesitylene (TMB) being 0.4. After stirring for 5 min, 2.5 ml of ethyl orthosilicate was added dropwise. After stirring for 2 hours, it was naturally cooled to obtain a white suspension, which was filtered by suction, washed three times with deionized water and twice with ethanol, and the obtained sample was dried in a vacuum oven at 60°C. Put the obtained white powder into 200 ml of ammonium nitrate ethanol solution with a concentration of 1 g / ml and reflux at 80...

Embodiment 3

[0052] One. Preparation of metoprolol tartrate sustained-release preparation

[0053] (1) Preparation of spherical mesoporous silica nanoparticles (MCM-41)

[0054] The three-neck flask was placed in a water bath at 80°C, 240 ml of deionized water and 1.75 ml of NaOH solution with a concentration of 2 mol / L were measured, and then 0.5 g of cetyl ammonium bromide was added. After stirring, after the solution was clarified, 0.9 ml of mesitylene was added according to the molar ratio of tetraethyl orthosilicate (TEOS) to mesitylene (TMB) being 0.6. After stirring for 5 min, 2.5 ml of ethyl orthosilicate was added dropwise. After stirring for 2 hours, it was naturally cooled to obtain a white suspension, which was filtered by suction, washed three times with deionized water and twice with ethanol, and the obtained sample was dried in a vacuum oven at 60°C. Put the obtained white powder into 200 ml of ammonium nitrate ethanol solution with a concentration of 1 g / ml and reflux at ...

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Abstract

The invention relates to a slow-release medicinal preparation for treating heart diseases, especially to a metoprolol slow-release medicinal preparation with mesoporous silica as a carrier, belonging to the field of pharmacy. The slow-release medicinal preparation for treating heart diseases is composed of metoprolol and mesoporous silica nanoparticles. The invention has the following advantages: the preparation method is simple, and the bore diameter of the carrier is controllable; Compared with common preparations, the metoprolol tartrate low-release preparation provided by the invention has the advantages of slower, more sustainable and more stable in-vitro release; the metoprolol tartrate low-release preparation can guarantee control of attack by high blood pressure and myocardial ischemia around the clock; so the metoprolol tartrate low-release preparation has good clinical application prospects.

Description

technical field [0001] The invention relates to a slow-release drug preparation for treating heart disease, in particular to a metoprolol slow-release drug with mesoporous silicon dioxide as a carrier, and belongs to the field of pharmacy. Background technique [0002] With the improvement of people's living standards in our country and the simultaneous growth of sub-healthy people, the latest data in 2011 shows that there are more than 200 million people with high blood pressure in my country, but 70% don't know they are sick, and die every year due to cardiovascular and cerebrovascular diseases About 3 million people, half of which are related to high blood pressure, and cardiovascular and cerebrovascular diseases tend to be younger at an unexpected speed, increasing the number of patients. Most hypertension has no known cause and is a lifelong condition. Long-term and effective implementation of antihypertensive drug therapy is one of the main ways to improve the quality ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/138A61K47/04A61P9/12A61P9/10
Inventor 刘德平吴亚贞贾晓云林元华蔡晴
Owner BEIJING HOSPITAL
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