Novel composing prescription sustained-release preparation for treating high blood pressure and preparation method thereof

A technology of slow-release preparations and prescriptions, applied in the field of medicine, can solve problems such as patient discomfort, inaccurate dose control, and failure to achieve antihypertensive effects

Inactive Publication Date: 2008-05-28
BEIJING RUNDEKANG MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Both metoprolol and angiotensin II receptor antagonists can be used to treat hypertension. They have different action sites and methods to indirectly or directly play a role in lowering blood pressure. Clinically, doctors can choose according to their needs. Appropriate angiotensin II receptor antagonists and metoprolol are used in combination to achieve a synergistic effect, but often due to inaccurate dose control, it will bring discomfort to patients or fail to achieve the ideal antihypertensive effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Compound Metoprolol Eprosartan Tartrate Double-Layer Sustained Release Tablets

[0025] prescription:

[0026] components

content

Metoprolol tartrate

Eprosartan

HPMC-15M

EC

lactose

80% ethanol solution

microcrystalline cellulose

purified water

Talc powder

Co-made

100g

600g

80g

20g

30g

Appropriate amount

200g

Appropriate amount

Appropriate amount

1000 pieces

[0027] Preparation:

[0028] Pass metoprolol tartrate through a 100-mesh sieve, HPMC-15M, EC, and lactose pass through a 60-mesh sieve, mix the raw and auxiliary materials evenly, use 80% ethanol solution to make a soft material, granulate with a 16-mesh sieve, dry at 40°C, and use a 16-mesh sieve Whole the granules, add talcum powder and mix evenly, and set aside; in addition, mix eprosartan and microcrystalline cellulose evenly, ...

Embodiment 2

[0029] Example 2 Compound Metoprolol Irbesartan Tartrate Double-Layer Sustained Release Tablets

[0030] prescription:

[0031] components

content

Metoprolol tartrate

Irbesartan

HPMC-15M

HPMC-100M

sucrose

80% ethanol solution

lactose monohydrate

purified water

100g

150g

60g

15g

30g

Appropriate amount

80g

Appropriate amount

[0032] Micropowder silica gel

Co-made

Appropriate amount

1000 pieces

[0033] Preparation:

[0034] Pass metoprolol tartrate through a 100-mesh sieve, HPMC-15M, HPMC-100M, and sucrose pass through a 60-mesh sieve, mix the raw and auxiliary materials evenly, and use 80% ethanol solution to make a soft material, granulate with a 16-mesh sieve, dry at 40°C, and dry at 16 Mesh sieve for granulation, add some micropowder silica gel and mix evenly, and set aside; in addition, mix irbes...

Embodiment 3

[0035] Example 3 Compound metoprolol candesartan medoxomil tartrate film-coated sustained-release tablet

[0036] Prescription for Metoprolol Tartrate Tablets:

[0037] components

content

Metoprolol tartrate

microcrystalline cellulose

lactose

purified water

Co-made

100g

250g

75g

Appropriate amount

1000 pieces

[0038] Coating prescriptions containing candesartan cilexetil:

[0039] components

content

candesartan cilexetil

Ethyl cellulose

Acrylic RS100

Tween ~ 80

Talc powder

Anhydrous ethanol solution

4g

12g

15g

2g

4g

400ml

[0040] Preparation:

[0041] Pass metoprolol tartrate through a 100-mesh sieve, microcrystalline cellulose and lactose through a 60-mesh sieve, mix the raw and auxiliary materials evenly, make soft materials with appropriate amount of water, granulat...

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PUM

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Abstract

The invention relates to a sustained release preparation of a novel prescription for treating hypertension and the preparing method thereof. The novel prescription comprises a heart selective Beta1 receptor blocker metoprolol and an angiotensin II receptor antagonist (sartan drugs). The sustained release preparation consists of delayed release part and rapid release part, wherein the heart selective Beta1 receptor blocker metoprolol is the delayed release part, with first hour releasing 25-45%, fourth hour releasing 40-75% and eighth hour releasing over 75%; the angiotensin II receptor antagonist (sartan drugs) is the rapid release part, with 45 minutes dissolution over 75%. The composition has both rapid and prolonged action. The invention discloses in vitro drug release characteristics and preparation method thereof.

Description

technical field [0001] The invention relates to a sustained-release preparation of a new prescription for treating hypertension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Metoprolol is a selective β1 receptor blocker, which can block myocardial β1 receptors, slow down heart rate, inhibit cardiac contractility and atrioventricular conduction, reduce cardiac output and circulating blood flow, and reduce myocardial oxygen consumption ; It can also reduce the secretion of renin and aldosterone, reduce vascular tension, blood volume and blood pressure. It can be used to treat hypertension and angina pectoris, reduce the incidence of myocardial infarction, and reduce the mortality rate after myocardial infarction. One study confirmed the efficacy of metoprolol extended-release tablets in the treatment of hypertension. Methods: Thirty-eight hypertensive patients of Han and Han ethnic groups took metoprolol sustain...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/138A61K45/06A61P9/12A61K31/4184A61K31/41
Inventor 陈瑞晶
Owner BEIJING RUNDEKANG MEDICAL TECH CO LTD
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