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Anti-angina pharmaceutical composition containing nicorandil

A technology of nicorandil and composition, applied in the field of anti-angina pectoris pharmaceutical composition and preparation thereof, can solve the problems of accelerating blood flow and anticoagulation, cavity, anus and gastrointestinal tract ulcers, ulcers and the like

Inactive Publication Date: 2015-12-02
XIAN HANFENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] But, because nicorandil has the effect of nitrates, there are also some side effects of nitrates. At the same time, it has been reported that nicorandil can cause ulcers in the mouth, anus and gastrointestinal tract in recent years. Studies have shown that ulcers The rate is concentration-dependent. When the daily dose of nicorandil is greater than 40mg, the incidence of ulcer, intestinal fistula and intestinal perforation is greatly increased. The above metabolites cannot be fully integrated into the pool of niacin and niacinamide in the human body and overflow, causing accelerated blood flow and anticoagulation in the blood, resulting in ulcers

Method used

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  • Anti-angina pharmaceutical composition containing nicorandil

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0045] Experimental Example 1: Study on the anti-angina pectoris effect of the pharmaceutical composition of beta-receptor blocker and nicorandil in the angina pectoris model of conscious rabbits.

[0046] 1. Experimental animals and experimental groups: 150 male big-eared white rabbits (provided by the Fourth Military Medical University) were selected for the experiment, with a body mass of (2.2±0.1) kg. Randomly divided into 15 groups, 10 in each group. Grouped as follows:

[0047] (1) Normal control group: the same volume of 0.5% CMC was given by intragastric administration;

[0048] (2) Model control group: the same volume of 0.5% CMC was given by intragastric administration;

[0049] (3) Comparative example group 1 (nicorandil): 0.5mg / kg, mixed with 0.5% CMC and administered into the stomach;

[0050] (4) Comparative example group 2 (propranolol): 1mg / kg, mixed with 0.5% CMC and administered orally;

[0051] (5) Comparative example group 3 (sotalol): 2 mg / kg, mixed wi...

experiment example 2

[0069] Experimental Example 2: The protective effect of the pharmaceutical composition of beta-receptor blocker and nicorandil on myocardial ischemia-reperfusion injury in rats.

[0070] 1. Experimental animals and experimental groups: 150 male SD rats (provided by the Fourth Military Medical University) were selected for the experiment, with a body mass of (250±20) kg. Randomly divided into 15 groups, 10 in each group. Grouped as follows:

[0071] (1) Normal control group: the same volume of 0.5% CMC was given by intragastric administration;

[0072] (2) Model control group: the same volume of 0.5% CMC was given by intragastric administration;

[0073] (3) Comparative example group 1 (nicorandil): 1 mg / kg, mixed with 0.5% CMC and administered into the stomach;

[0074] (4) Comparative example group 2 (propranolol): 2mg / kg, mixed with 0.5% CMC and administered orally;

[0075] (5) Comparative example group 3 (sotalol): 4 mg / kg, mixed with 0.5% CMC and administered orally; ...

Embodiment 1

[0092] Embodiment 1: the preparation of compound pharmaceutical composition 1 (tablet) (in 1000 pieces)

[0093] Tablet prescription:

[0094] Nicorandil

5g

Propranolol

10g

lactose

90g

microcrystalline cellulose

80g

Sodium carboxymethyl starch

5g

Micropowder silica gel

0.5g

Talc powder

2.5g

[0095] Coating prescription

[0096] Opadry Coating Powder 4g

[0097] Purified water 45g

[0098] Preparation:

[0099] (1) Weigh Nicorandil and Propranolol in the prescribed amount, pulverize them through an 80-mesh sieve, and mix them uniformly by using the method of equal increments.

[0100] (2) Weigh microcrystalline cellulose, lactose, micropowder silica gel, sodium carboxymethyl starch and talcum powder in prescription quantities, pulverize through a 60-mesh sieve, and mix well.

[0101] (3) Mix (1) and (2) uniformly to obtain an intermediate.

[0102] (4) Check the intermediate content, ca...

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Abstract

The invention discloses an anti-angina pharmaceutical composition containing nicorandil. The anti-angina pharmaceutical composition comprises the nicorandil, beta receptor blocker and pharmaceutically acceptable excipients. The pharmaceutical composition has the advantages that the pharmaceutical composition has good angina and myocardial ischemia resisting effects, drug resistance cannot be caused easily, various adverse reactions of single medicine use can be overcome, toxic and side effects are lowered, and the pharmaceutical composition shows good synergistic effect in angina resisting and the treatment of myocardial ischemia.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a nicorandil-containing antiangina pharmaceutical composition and a preparation method thereof. Background technique [0002] Angina pectoris is a clinical syndrome mainly characterized by paroxysmal chest pain or chest discomfort caused by coronary insufficiency, myocardial acute, temporary ischemia and hypoxia. It is characterized by paroxysmal chest squeezing pain, which may be accompanied by other symptoms. The pain is mainly located at the back of the sternum and can radiate to the precordium and left upper limb. The cause is the accumulation of metabolites due to myocardial hypoxia. These substances stimulate the local sympathetic nerve endings in the heart, and the residence is sent to the brain by the afferent nerve through the lower cervical and upper thoracic sympathetic ganglia and the corresponding spinal cord segment. Discomfort in the area of ​​skin where the spinal nerves ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K45/06A61K31/455A61K31/165A61P9/10
Inventor 安龙王汝涛陈涛王惟娇赵熠郭树攀朱银静
Owner XIAN HANFENG PHARMA
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