Single nitrate isosorbide delayed-release tablets

A technology of isosorbide dinitrate and sustained-release tablets, which is applied in the field of medicine, can solve the problems of reduced curative effect, low effective dose, and difficulty in controlling the onset of angina pectoris in the morning, so as to prevent myocardial ischemia, reduce body load, and eliminate drug resistance Effect

Inactive Publication Date: 2008-02-06
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the dosage forms of isosorbide mononitrate include tablets, capsules, etc. After oral administration, the blood drug concentration rises rapidly to 400ng / ml, which greatly exceeds the minimum effective dose (100ng / ml), causing patients to experience severe headache, Nausea, vomiting, circulatory collapse and other side effects, the incidence rate is about 14%
In addition, the effective action time of the drug can only last for 6 hours, and it needs to be taken three times a day. Not only is it difficult to control the onset of angina pectoris in the morning, but also when it is taken for a long time, tolerance often occurs and the curative effect is reduced.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Isosorbide Mononitrate 40g

[0020] HPMC-4M 80g

[0021] 8% PVP absolute ethanol solution 20g

[0022] Lactose 12g

[0023] Magnesium stearate 0.4g

[0024] Preparation process: Isosorbide mononitrate passes through a 100-mesh sieve, HPMC-4M passes through a 80-mesh sieve, weighs the prescribed amount of isosorbide mononitrate, lactose, and HPMC-4M, mixes them evenly, and adds an appropriate amount of 8% PVP absolute ethanol solution to prepare Granules, dried at 60°C, sieved with a 16-mesh sieve to dry the granules, adding the prescribed amount of magnesium stearate to the dry granules, mixing them evenly, and pressing them into 1000 tablets.

Embodiment 2

[0026] Isosorbide Mononitrate 40g

[0027] HPMC-4M 128g

[0028] 8% PVP absolute ethanol solution 56g

[0029] Lactose 12g

[0030] Magnesium stearate 0.4g

[0031] The preparation process is the same as in Example 1.

Embodiment 3

[0033] Isosorbide Mononitrate 40g

[0034] HPMC-15M 100g

[0035] 8% PVP95% ethanol solution 25g

[0036] Lactose 12g

[0037] Magnesium stearate 0.4g

[0038] The preparation process is the same as in Example 1.

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PUM

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Abstract

A slow-releasing tablet of isosorbide mononitrate for treating coronary heart disease and angina pectoris is prepared proportionally from isosorbide mononitrate, slow releasing agent, adhesive, filler and lubricant through proportional mixing, granulating, and tabletting.

Description

technical field [0001] The invention relates to a sustained-release tablet, in particular to an isosorbide mononitrate sustained-release tablet for treating coronary heart disease and angina pectoris, and belongs to the field of medicine. Background technique [0002] Isosorbide mononitrate is a commonly used drug for treating coronary heart disease and angina pectoris. It was first developed by Boehringer Mannheim Gnb.h in Germany and launched in the market in 1981. It has been clinically used for many years and has a definite curative effect. Its main mechanism of action is to expand venous volume vessels and peripheral resistance vessels, reduce cardiac preload and postload, and reduce myocardial oxygen consumption. The drug has the characteristics of high bioavailability, small individual differences, long half-life, and remarkable curative effect, and is better than indigestion and nitroglycerin in the prevention of coronary heart disease and angina pectoris. [0003] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/34A61K9/22A61P9/10
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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