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Compound antihypertensive preparation and application thereof

A technology of high blood pressure and receptor antagonists, applied in pill delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., to achieve the effect of reducing adverse reactions, improving compliance, and widening the population of patients

Inactive Publication Date: 2015-12-02
XIAN LIBANG ZHAOXIN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent does not mention the drug users. We know that candesartan may worsen liver function in patients with liver dysfunction. It should be used with caution in clinical practice, and it should also be used with caution in patients with severe renal impairment

Method used

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  • Compound antihypertensive preparation and application thereof
  • Compound antihypertensive preparation and application thereof
  • Compound antihypertensive preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: Antihypertensive Effect Experiment of Triple Drug Combination on Hypertension in Spontaneously Hypertensive Rats

[0048] 1. Experimental animals and experimental groups

[0049] 190 spontaneously hypertensive male rats, weighing 250g±20g, were randomly divided into 19 groups, 10 rats in each group, after being fed for one week.

[0050] (1) Model control group: intragastric administration of the same volume of normal saline;

[0051] (2) Metolazone group: 0.05mg / kg / d

[0052] (3) Hydrochlorothiazide: 1.2mg / kg / d

[0053] (4) Valsartan group: 7.5mg / kg / d

[0054] (5) Olmesartan group: 4mg / kg / d

[0055] (6) Amlodipine group: 1mg / kg / d

[0056] (7) Lacidipine group: 0.4mg / kg / d

[0057] (8) Felodipine group: 0.5mg / kg / d

[0058] (9) Metolazone + valsartan + amlodipine: 0.05mg / kg / d+7.5mg / kg / d+1mg / kg / d

[0059] (10) Metolazone + valsartan + lacidipine: 0.05mg / kg / d+7.5mg / kg / d+0.4mg / kg / d

[0060] (11) Metolazone + valsartan + felodipine: 0.05mg / kg / d+7.5mg / kg / d+...

Embodiment 2

[0075] Example 2: Compared with the triple drug combination containing hydrochlorothiazide, the triple drug combination of the present invention has an antihypertensive effect on spontaneously hypertensive rats and an experiment on kidney damage

[0076] 1. Experimental animals and experimental groups

[0077] 120 spontaneously hypertensive male rats, weighing 250g±20g, were randomly divided into 12 groups, 10 rats in each group, after being fed for one week.

[0078] (1) Metolazone + valsartan + amlodipine: 0.05mg / kg / d+7.5mg / kg / d+1mg / kg / d

[0079] (2) Metolazone + valsartan + lacidipine: 0.05mg / kg / d+7.5mg / kg / d+0.4mg / kg / d

[0080] (3) Metolazone + valsartan + felodipine: 0.05mg / kg / d+7.5mg / kg / d+0.5mg / kg / d

[0081] (4) Metolazone + Olmesartan + Amlodipine: 0.05mg / kg / d+4mg / kg / d+1mg / kg / d

[0082] (5) Metolazone + Olmesartan + Lacidipine: 0.05mg / kg / d+4mg / kg / d+0.4mg / kg / d

[0083] (6) Metolazone + Olmesartan + Felodipine: 0.05mg / kg / d+4mg / kg / d+0.5mg / kg / d

[0084] (7) Hydrochlorot...

Embodiment 3

[0126] Embodiment 3, the preparation of compound pharmaceutical composition 3 (tablet) (in 1000 pieces)

[0127] Tablet prescription:

[0128]

[0129] Coating prescription:

[0130] Opadry Coating Powder 9g

[0131] Purified water 60g

[0132] Preparation:

[0133] (1) Weigh the prescribed amount of valsartan, metolazone, and amlodipine, pulverize them through an 80-mesh sieve, and mix them uniformly by using the method of equal increments.

[0134] (2) Weigh the microcrystalline cellulose, starch, croscarmellose sodium, and micropowder silica gel of the prescribed amount, pulverize them through a 60-mesh sieve, and mix them evenly.

[0135] (3) Mix (1) and (2) evenly, add 95% ethanol to make a soft material, granulate with an 18-mesh sieve, and dry at 50°C.

[0136] (4) After the granules are dried, the granules are sized through a 20-mesh sieve, then magnesium stearate is added, and the mixture is evenly mixed to obtain an intermediate.

[0137] (5) Check the inter...

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Abstract

The invention provides a pharmaceutical composition for treating hypertension. The pharmaceutical composition is characterized by comprising (1) angiotensin II receptor blocker, (2) diuretic metolazone, (3) calcium channel blocker and (4) pharmaceutically acceptable adjuvant materials, wherein the weight ratio among the angiotensin receptor blocker, the metolazone and the calcium channel blocker is 2-200:0.5-5:2-50. The pharmaceutical composition for treating hypertension has the advantages that the pharmaceutical composition combines the angiotensin receptor blocker, the metolazone and the calcium channel blocker, and accordingly, synergetic antihypertensive effect is enhanced, adverse reaction is reduced and compliance of patients is improved; the pharmaceutical composition is wide in application range and can be also used for patients suffering from severe renal damage; the pharmaceutical composition is applicable to mild and moderate essential hypertension, particularly secondary hypertension caused by renal damage.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical composition with an angiotensin II receptor antagonist, metolazone and a calcium ion antagonist as active ingredients and an application thereof. Background technique [0002] With the rapid growth of my country's economy and drastic changes in people's lifestyles, cardiovascular disease has become the biggest killer threatening human health. Hypertension is one of the most common cardiovascular diseases and has become a major public health problem worldwide. According to statistics from the national health department, by the end of 2010, the number of hypertensive patients in my country has reached 200 million, and more than 3 million people are added every year. Hypertension is a clinical syndrome characterized by elevated systemic arterial systolic blood pressure (SBP) and / or diastolic blood pressure (DBP), especially the damage to target organs such as the heart, bra...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/517A61K9/28A61P9/12A61P9/10
Inventor 张婉直惠民权安龙陈涛余惟平王汝涛
Owner XIAN LIBANG ZHAOXIN BIOTECH CO LTD
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