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Compound antihypertensive preparation and application thereof

A technology of inhibitors and high blood pressure, applied in the field of medicine, can solve the problems of target organ protection not being correspondingly enhanced, angioneural edema, abnormal blood potassium, etc., to reduce the probability of abnormal blood potassium, enhance the protective effect, Strengthen the effect of synergistic antihypertensive effect

Active Publication Date: 2015-07-01
XIAN HANFENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Clinically, the compound drug composed of low-dose thiazide diuretics such as hydrochlorothiazide and ACEI has outstanding synergistic antihypertensive performance, and ACEI can also inhibit the renin-angiotensin system (RAS) activation and Partially offset the side effects of hypokalemia, but long-term use may still cause problems such as cough, abnormal blood potassium, and vascular nerve edema
In addition, the protective effect of such compounds on target organs has not been correspondingly enhanced, on the contrary, it may be weakened due to the influence on lipid metabolism

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

[0036] Embodiment 1: the preparation of compound pharmaceutical composition 1 (tablet) (in 1000 pieces)

[0037]

[0038] Preparation:

[0039] Pass the prescribed amount of enalapril and metofazon through a 80-mesh sieve; lactose, microcrystalline cellulose, pregelatinized starch, and sodium carboxymethyl starch through a 60-mesh sieve, and mix evenly by the method of equal increments. Add 50% ethanol to make a soft material, granulate with a 18-mesh screen, dry the wet granules at 40°C, and granulate with an 18-mesh screen. Add magnesium stearate and mix well. Detect the content of the semi-finished product, calculate the weight of the tablet, press the tablet machine to tablet, and store it in the dark. Each of the prepared compound tablets contains 10 mg enalapril and 0.5 mg metorfazon.

Embodiment 2

[0040] Embodiment 2: the preparation of compound pharmaceutical composition 2 (tablet) (in 1000 pieces)

[0041]

[0042]

[0043] Preparation Process:

[0044] Pass the prescribed amount of enalapril and metorfazon through a 80-mesh sieve; lactose, microcrystalline cellulose, pregelatinized starch, sodium carboxymethyl starch and calcium hydrogen phosphate through a 60-mesh sieve, and use the equal-increasing method well mixed. Then add magnesium stearate and mix well. Detect the content of the semi-finished product, calculate the weight of the tablet, press the tablet machine to tablet, and store it in the dark. Each of the prepared compound tablets contains 20 mg enalapril and 0.25 mg metorfazon.

Embodiment 3

[0045] Embodiment 3: the preparation of compound pharmaceutical composition 3 (capsules) (in 1000 grains)

[0046]

[0047] Preparation Process:

[0048] Sieve the main ingredient through 80-mesh sieve and the auxiliary materials through 60-mesh sieve respectively, and set aside. Weigh 5g of enalapril and 1g of Metorfazon and mix them uniformly according to the method of equal increase, add lactose, microcrystalline cellulose, crospovidone and sodium lauryl sulfate respectively according to the prescription amount, Mix evenly, add 5% povidone ethanol solution to make a soft material, granulate with a 20-mesh sieve, and dry at 40°C. After the granules are dried, the granules are sized through a 20-mesh sieve, then magnesium stearate is added, and mixed evenly. The content of the semi-finished product is detected, the filling amount is calculated, and the No. 3 capsule is used to fill it. Each capsule contains 5mg of enalapril and 1mg of metorfazon.

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PUM

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Abstract

The invention provides a pharmaceutical composition for treating hypertension. The pharmaceutical composition comprises (1) an angiotensin-converting enzyme inhibitor, (2) furosemide metolazone (former name: metolazone), and (3) pharmaceutically acceptable auxiliary materials, wherein the weight ratio of the angiotensin-converting enzyme inhibitor to the metolazone is (10-40) to (0.5-1). By combination of the angiotensin-converting enzyme inhibitor and the metolazone, the synergistic hypotensive action is reinforced; the protection effect on target organs, especially kidneys are enhanced; the probability of serum potassium abnormity is lowered; the compliance of patients is improved; the population of medication is expanded; and the pharmaceutical composition is suitable for severe and intractable hypertension, especially secondary hypertension caused by kidney damages.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a pharmaceutical composition in which angiotensin-converting enzyme inhibitors and metolazone (formerly known as metolazone) are active ingredients and an application thereof. Background technique [0002] Hypertension is one of the most common cardiovascular diseases at present. Inadequate treatment can easily lead to stroke, myocardial infarction, heart failure, chronic kidney disease and other complications, with high disability and fatality rates, consuming a lot of medical resources and social wealth. Bring a great burden to the family and society. Therefore, the main goal of hypertension treatment is to minimize the overall risk of cardiovascular complications and death, and to treat all reversible cardiovascular risk factors, target organ damage, and other coexisting clinical diseases. [0003] Currently, drugs for the treatment of hypertension include calcium channel blockers (C...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/517A61K38/05A61K31/55A61P9/12
Inventor 郭树攀陈涛王汝涛
Owner XIAN HANFENG PHARMA