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

A slow-release preparation and high blood pressure technology, applied in the field of medicine, can solve the problems of patients' discomfort, failure to achieve antihypertensive effect, and inaccurate dose control

Inactive Publication Date: 2008-07-09
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 the...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Compound metoprolol tartrate and eprosartan double-layer sustained-release tablets

[0027] prescription:

[0028] Component

Content

Metoprolol tartrate

Eprosartan

HPMC-15M

100g

600g

80g

[0029] EC

Lactose

80% ethanol solution

Microcrystalline cellulose

purified water

Talc

Co-made

20g

30g

Right amount

200g

Right amount

Right amount

1000 pieces

[0030] Preparation:

[0031] Pass metoprolol tartrate through a 100-mesh sieve, HPMC-15M, EC, and lactose through a 60-mesh sieve, mix the raw and auxiliary materials uniformly, and use 80% ethanol solution to make soft materials, sieve for granulation on the 16th, dry at 40℃, sieve on the 16th Whole granules, add talc powder and mix evenly, and then mix eprosartan and microcrystalline cellulose uniformly, make soft material with purified water, and prepare quick-release granules of basically the same size by the same method. The above two...

Embodiment 2

[0032] Example 2 Compound Metoprolol Tartrate Irbesartan Double-layer Sustained Release Tablet

[0033] prescription:

[0034] Component

Content

Metoprolol tartrate

Irbesartan

HPMC-15M

HPMC-100M

Sucrose

80% ethanol solution

Lactose monohydrate

purified water

Micronized silica gel

Co-made

100g

150g

60g

15g

30g

Right amount

80g

Right amount

Right amount

1000 pieces

[0035] Preparation:

[0036] Pass metoprolol tartrate through a 100-mesh sieve, HPMC-15M, HPMC-100M, and sucrose through a 60-mesh sieve, mix the raw and auxiliary materials evenly, use 80% ethanol solution to make soft material, 16-mesh sieve for granulation, dry at 40℃, 16 The granules are sieved through a mesh, and part of the micro-powdered silica gel is added and mixed uniformly for use. In addition, irbesartan and lactose monohydrate are mixed uniformly, and purified water is used to make soft materials, and the same method is used to prepare quic...

Embodiment 3

[0037] Example 3 Compound metoprolol candesartan cilexetil tartrate film-coated sustained-release tablet

[0038] Metoprolol tartrate core prescription:

[0039] Component

Content

Metoprolol tartrate

Microcrystalline cellulose

Lactose

purified water

Co-made

100g

250g

75g

Right amount

1000 pieces

[0040] Coating prescription containing candesartan cilexetil:

[0041] Component

Content

Candesartan cilexetil

Ethyl cellulose

Acrylic resin RS100

Tween~80

Talc

Absolute ethanol solution

4g

12g

15g

2g

4g

400ml

[0042] Preparation:

[0043] 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 a soft material with an appropriate amount of water, granulate with a 20-mesh sieve, dry, sizing on an 18-mesh sieve, and press to tablet. Standby; place ethyl cellulose and acrylic resin RS10...

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PUM

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Abstract

The invention relates to a sustained-release preparation with novel composition for curing high blood pressure and a preparation method thereof. The novel composition consists of a cardiac selective Beta1 blocker metoprolol and an angiotensin II receptor antagonist (sartans). The sustained-release preparation consists of a sustained release section and a fast release section, wherein, the cardiac selective Beta1 blocker metoprolol is the sustained release section and the angiotensin II receptor antagonist (sartans) is the immediate-release section. The cardiac selective Beta1 blocker metoprolol releases 25 percent to 45 percent in the first hour, 40 percent to 75 percent in the fourth hour, and above 75 percent in the eighth hour; while the angiotensin II receptor antagonist (sartans) releases above 75 percent after 45 min. The invention has quick and long-lasting effect, and discloses the vitro release characteristics and preparation method of the sustained-release preparation.

Description

Technical field [0001] The invention relates to a sustained-release preparation of a new prescription for treating hypertension and a preparation method thereof, and belongs 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 tone, 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. A study confirmed the efficacy of metoprolol sustained-release tablets in the treatment of hypertension. Methods: 38 patients with hypertension in Han and Han ethnic groups took Metoprolol sustained-release tabl...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K9/22A61K9/52A61K31/41A61K31/4178A61K31/4184A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P9/12A61K31/137
Inventor 陈瑞晶
Owner BEIJING RUNDEKANG MEDICAL TECH CO LTD
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