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Metoprolol fumarate sustained-release tablet and preparation method thereof

A technology of fumaric acid beauty and sustained-release tablets, which is applied in the directions of pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., to achieve the effects of convenient medication, reduced medication frequency, and good patient compliance.

Active Publication Date: 2012-02-22
SHANDONG YONGJU MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Metoprolol fumarate is commonly used clinically in three specifications of 95mg / tablet, 190mg / tablet, and 285mg / tablet. There is no raw material drug and preparation of metoprolol fumarate in my country.

Method used

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  • Metoprolol fumarate sustained-release tablet and preparation method thereof
  • Metoprolol fumarate sustained-release tablet and preparation method thereof
  • Metoprolol fumarate sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] 1. The total amount of 1000 tablets is prepared from the following raw materials, and the sustained-release tablets are taken at intervals of 24 hours:

[0053] Main drug: skeleton material: blocker: wetting agent: lubricant: glidant = 95g: 300g: 50g: 300g: 4.02g: 8.375g;

[0054] *In addition to the main drug, other raw materials are collectively referred to as "excipients", the same below.

[0055] The main drug is metoprolol fumarate, provided by Shandong Qidu Pharmaceutical Co., Ltd.

[0056] The specification of the skeleton material is viscosity K 15~100M Hydroxypropyl Methyl Cellulose (English: Hydroxypropyl Methyl Cellulose is called for short: HPMC), commercially available commodity, U.S. Dow Chemical Company manufactures (viscosity K 15~100M , after conversion into the legal dosage unit, the viscosity K 15M Equivalent to the legal measurement unit of 13 ~ 18mPa s; viscosity K 100M It is equivalent to the legal measurement unit of 80~120mPa·s. )

[0057] ...

Embodiment 2

[0100] A total of 1000 tablets are prepared from the raw materials of the following proportioning ratio, and the sustained-release tablets are taken at intervals of 24 hours:

[0101] Main drug: skeleton material: blocker: wetting agent: lubricant: glidant = 95g: 100g: 30g: 100g: 2.68g: 5.025g;

[0102] Raw materials, auxiliary materials, preparation methods and test results are all equal or close to those of Example 1 except for the change in dosage.

Embodiment 3

[0104] A total of 1000 tablets are prepared from the raw materials of the following proportioning ratio, and the sustained-release tablets are taken at intervals of 24 hours:

[0105] Main drug: skeleton material: blocker: wetting agent: lubricant: glidant = 95g: 200g: 40g: 200g: 3.35g: 6.70g;

[0106] The skeleton material is set to a viscosity specification of K 100M Hydroxypropyl methylcellulose;

[0107] All the other materials, auxiliary materials, preparation methods and test results are equal to or close to those in Example 1 except for the change in dosage.

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Abstract

A metoprolol fumarate sustained-release tablet and a preparation method thereof. The sustained-release tablet with a total amount of 1000 tablets and an administration interval of 24 h is prepared by the following components: 95 g of metoprolol fumarate used as a main drug; 100-300 g of hydroxypropyl methyl cellulose used as a skeletal material; 30-50 g of ethyl cellulose or low-permeability acrylic resin used as a retarding agent; 100-300 g of 85% ethanol used as a wetting agent; 2.68 g-4.02 g of magnesium stearate used as a lubricant, and 5.025-8.375 g of talcum powder used as a flow aid. The main drug is well mixed firstly with the retarding agent and then with the skeletal material; a soft material and granules are prepared by he wetting agent; the granules are dried and sized; the lubricant and the flow aid are added for tabletting; when the tablet is qualified after examination, the metoprolol fumarate sustained-release tablet is obtained. After administration, the drug is released slowly; not only the everyday administration frequency is decreased, which is convenient for drug administration of clinical doctors and patients, but also the blood concentration of the drug is stable; no peak-valley phenomenon is generated; the toxic and side effect is decreased to a lowest level; and the patient compliance is good.

Description

technical field [0001] The invention relates to metoprolol fumarate sustained-release tablets and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Metoprolol Fumarate Sustained Release Tablets, English name Metoprolol Fumarate Sustained Release tablets; chemical name (±) 1-(isopropylamino)-3-[p-(2-methoxyethyl)-phenoxy] -2-Propanol fumarate. [0003] With the aging of the population, the incidence of cardiovascular disease has increased sharply, which has plagued people for a long time. Hypertension, angina pectoris, arrhythmia and heart failure (heart failure) are the most common clinical cardiovascular diseases with extremely high incidence rates. [0004] Classical theory holds that the contractility of a failing heart decreases, and increasing myocardial contractility is beneficial to patients with heart failure, so inotropic drugs have always been regarded as an effective treatment for patients with hea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/138A61K31/194A61K47/38A61P9/04A61P9/06A61P9/10A61P9/12
Inventor 李后涛李洁崔美兰白臣生牛海岗
Owner SHANDONG YONGJU MEDICAL TECH