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Metoprolol slow-release microsphere, slow-release medical composition and preparation method of metoprolol slow-release microsphere

A slow-release microsphere and microsphere technology, applied in the field of medicine, can solve the problems of complex prescription process, poor controllability, short sustained-release time, etc., and achieve the effects of strong controllability, low cost and high encapsulation rate

Inactive Publication Date: 2013-07-10
广州万泽医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition, there is also a report of a slow-release pharmaceutical composition of metoprolol sustained-release pellets and a preparation method thereof. This method also follows the fluidized bed coating, wrapping a drug layer and a slow-release layer on the blank core, and finally carrying out Aging, in order to achieve the purpose of stable drug release for 12 hours, the sustained release time is short, and the prescription process is complicated and the controllability is poor

Method used

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  • Metoprolol slow-release microsphere, slow-release medical composition and preparation method of metoprolol slow-release microsphere
  • Metoprolol slow-release microsphere, slow-release medical composition and preparation method of metoprolol slow-release microsphere
  • Metoprolol slow-release microsphere, slow-release medical composition and preparation method of metoprolol slow-release microsphere

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Embodiment 1

[0055] The metoprolol sustained-release microspheres of the present embodiment are prepared from 40wt% of the pharmaceutical active ingredient and 60wt% of the sustained-release material, the pharmaceutical active ingredient is metoprolol hydrochloride, and the sustained-release material 65 wt% ethyl cellulose with 35 wt% Eudragit RS 100. The specific composition of the slow-release microspheres is: 4g of metoprolol hydrochloride, 3.9g of ethyl cellulose and 2.1g of Eudragit RS 100. Sustained-release microspheres and excipients are mixed with a mass ratio of 25: 1 to prepare a pharmaceutical composition. The excipients are 0.2 g each of magnesium stearate and silicon dioxide. The specific preparation method includes the following steps:

[0056] (1) prepare organic solvent, described organic solvent is the mixed solution of ethyl acetate: ethanol=8: 2 (v / v);

[0057] (2) Add the medicinal active ingredient and sustained-release material in proportion to the mixed solution of ...

Embodiment 2

[0062] The metoprolol sustained-release microspheres of the present embodiment comprise 8wt% of pharmaceutically active ingredients and 92wt% of sustained-release materials, wherein the pharmaceutically active ingredients are metoprolol succinate, and the sustained-release materials It is 75 wt% ethyl cellulose and 25 wt% polyaminomethacrylate. The specific composition of the metoprolol sustained-release microspheres is: 0.8 g of metoprolol succinate, 6.9 g of ethyl cellulose and 2.3 g of Eudragit RL 100 as sustained-release materials. Metoprolol sustained-release microspheres and excipients prepare the metoprolol sustained-release microspheres pharmaceutical composition with a mass ratio of 50:1, wherein the excipients are magnesium stearate, talcum powder, 0.1g, the specific preparation method comprises the following steps:

[0063] (1) prepare organic solvent, described organic solvent is the mixed solution of chloroform: ethanol=8: 2 (v / v);

[0064] (2) Add the medicinal...

Embodiment 3

[0069] The metoprolol sustained-release microspheres of the present embodiment comprise 20wt% of the pharmaceutically active ingredient and 80wt% of the sustained-release material, wherein the pharmaceutically active ingredient is metoprolol tartrate, and the sustained-release material is 71 wt% ethyl cellulose and 29 wt% polyaminomethacrylate. The specific composition of the microspheres is: 2g of metoprolol tartrate and 5.68g of ethylcellulose and 2.32g of Eudragit RS100. The release microspheres and excipients are mixed in a mass ratio of 10:1 to prepare a pharmaceutical composition containing sustained release microspheres. The excipients are 0.8 g of BASF, magnesium stearate, and silicon dioxide. 0.1g, the specific preparation method comprises the following steps:

[0070] (1) prepare organic solvent, described organic solvent is 80% (v / v) ethanol solution;

[0071] (2) Add the medicinal active ingredient and sustained-release material in proportion to the solution obta...

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Abstract

The invention provides metoprolol slow-release microsphere, slow-release medical composition and a preparation method of the metoprolol slow-release microsphere. The metoprolol slow-release microsphere comprises 8-40wt% of active pharmaceutical ingredients and 60-92wt% of slow-release materials, wherein the active pharmaceutical ingredients contain metoprolol succinate, metoprolol tartrate or metoprolol hydrochloride, and the slow-release materials include 65-75wt% of ethyl cellulose and 25-35wt% of poly amino methacrylate. The active pharmaceutical ingredients and the slow-release materials are dissolved in an organic solvent to prepare microsphere, then the microsphere and an excipient are mixed to be pressed into tablets or manufactured into capsules to achieve the slow-release medicalcomposition containing the metoprolol slow-release microsphere. The medical composition is simple in prescription, low in toxicity, high in package rate, strong in controllability, good in reproducibility and low in cost.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a metoprolol sustained-release microsphere, a sustained-release pharmaceutical composition containing the sustained-release microsphere and a preparation method thereof. Background technique [0002] Metoprolol is a selective β1 receptor blocker, commonly used its tartrate, succinate and hydrochloride, is a very water-soluble drug. Since it was successfully developed in Sweden in 1969, it was successfully launched in the market under the trade name of Betaloc in 1975. It has been widely used in the treatment of various cardiovascular diseases such as hypertension, angina pectoris, arrhythmia, myocardial infarction and heart failure. . [0003] Since the selective effect of metoprolol on β1 is dose-dependent, ordinary tablets are likely to cause excessively high peak blood concentration, which will lead to its effect on β2, causing side effects on lung function and blood sugar. Therefore...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/138A61K47/38A61P9/04A61P9/06A61P9/10A61P9/12
Inventor 吴传斌周玥鋆温新国付寒潘昕
Owner 广州万泽医药科技有限公司
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