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Metoprolol sustained-release dropping pill and preparation method thereof

A technology for sustained-release dripping pills and angina pectoris, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of allergic reactions or adverse reactions, manufacturing and medical costs of injections High, short drug action time and other problems, to achieve the effect of improving left ventricular ejection fraction and exercise tolerance, reducing the incidence rate, and reducing the number of hospitalizations

Inactive Publication Date: 2008-09-24
北京博智绿洲医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to reasons such as preparation technology, there are problems such as long dissolution time, low dissolution rate, poor absorption, hepatic and intestinal first-pass effect and low bioavailability after taking tablets or capsules, which affect the efficacy of the drug and directly affect the outcome of the treatment
The metoprolol dropping pill preparation of prior art production, though overcome the defective that above-mentioned dosage form produces, have quick effect, absorption fast, and advantages such as high bioavailability, but there is uneven dispersion of medicine, drug release is unstable, and medicine Defects such as short action time
[0007] Injections are often prone to allergic reactions or adverse reactions, etc., but also have the disadvantages of difficult operation, great pain for patients, high manufacturing and medical costs, and heavy economic burden for patients.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Based on the total weight of 100g, weigh the matrix PEG4000 40%, PEG6000 20%, PEG10000 10%, stearic acid 10%, glyceryl monostearate 7%, Tween-80 3%, raw material metoprolol 10% ; Place the matrix in a heating container to heat and stir to melt, add the corresponding proportion of metoprolol, stir well, then add Tween-80 and stir evenly, under the condition of heat preservation, melt the molten or mixed liquid medicine Drop into the condensate column filled with simethicone, in which the temperature when heated and melted is 70°C, the temperature of the upper part of the condensate is 20°C, and the temperature of the bottom is -4°C; take it out after forming,

[0042] The obtained product has a 2-hour cumulative release percentage of 30%-51%, a 6-hour cumulative release percentage of 52%-74%, a 10-hour cumulative release percentage of 75%-100%, and good roundness.

Embodiment 2

[0044] Based on the total weight of 100g, weigh the matrix PEG4000 20%, PEG6000 20%, PEG10000 4.5%, stearic acid 20%, glyceryl monostearate 10%, Tween-80 0.5%, raw material metoprolol 25% Place the matrix in a heating container and heat it and stir it to melt, add the corresponding proportion of metoprolol, stir well, then add Tween-80 and stir evenly, under the condition of heat preservation, put the melted or mixed medicine The liquid drops into the condensation column filled with simethicone oil, where the temperature when heated and melted is 65°C, the temperature of the upper part of the condensate is 30°C, and the temperature of the bottom is -1°C; take it out after forming,

[0045] The obtained product has a cumulative release percentage of 25%-47% in 2 hours, a cumulative release percentage of 55%-67% in 6 hours, and a cumulative release percentage of 85%-93% in 10 hours, and has good roundness.

Embodiment 3

[0047] Based on the total weight of 100g, weigh the matrix PEG4000 50%, PEG6000 10%, PEG10000 10%, stearic acid 5%, glyceryl monostearate 5%, Tween-80 2%, raw material metoprolol 18% Place the matrix in a heating container and heat it and stir it to melt, add the corresponding proportion of metoprolol, stir well, then add Tween-80 and stir evenly, under the condition of heat preservation, put the melted or mixed medicine The liquid drops into the condensation column filled with simethicone oil, where the temperature when heated and melted is 65°C, the temperature of the upper part of the condensate is 30°C, and the temperature of the bottom is 0°C; take it out after forming,

[0048] The obtained product has a 2-hour cumulative release percentage of 63%-71%, a 6-hour cumulative release percentage of 76%-87%, a 10-hour cumulative release percentage of 77%-100%, and good roundness.

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PUM

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Abstract

The invention relates to a fast-effect slow-release sustained-release metoprolol dropping pill used for treating hypertension, angina, the maintenance therapy after myocardial infarction and hyperthyroidism and the preparation method thereof, and aims to supplement the deficiency of the prior art and provide a sustained-release metoprolol dropping pill. The sustained-release metoprolol dropping pill is added with a hydrophobic framework capable of sustaining drug release and tween-80 playing the role of solubilization on the basis of the existing dropping pill technology, thereby overcoming the defects in the prior art effectively and having the advantages of even drug distribution, full release, long release time, reduced frequency of drug taking for patients and high bioavailability simultaneously.

Description

technical field [0001] The invention relates to a metoprolol sustained-release dripping pill capable of rapid effect and sustained drug release for the treatment of hypertension, angina pectoris, maintenance therapy after myocardial infarction, arrhythmia, hyperthyroidism and the like and a preparation method thereof. Background technique [0002] Metoprolol——trade name: Betaloc; English name: Metoprolol; [0003] Chemical name: 2-(±)-1-(isopropylamino)-3-[p-(2-methoxyethyl)phenoxy]-2-propanol [0004] Metoprolol is a second-generation β-blocker that selectively blocks β 1 Receptor, more selective for heart than blood vessels, for bronchial β 2 Receptor blocking effect is far less than propranolol, no endogenous sympathomimetic activity. Therefore, it is very suitable for the treatment of hypertension, angina pectoris, arrhythmia, myocardial infarction and certain cardiomyopathy. (1) Hypertension: especially suitable for mild and moderate hypertension. This product can ...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/138A61K47/34A61K47/38A61P9/10A61P9/12A61K47/10A61K47/14
Inventor 曲韵智
Owner 北京博智绿洲医药科技有限公司
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