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drug combination of nep inhibitor and its application

A technology of inhibitors and drugs, applied in the field of biomedicine, can solve problems such as blood reduction

Active Publication Date: 2019-11-22
SHANGHAI HANSOH BIOMEDICAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is now known that angiotensin receptor blockers (ARBs, angiotensin II antagonists) work by preventing angiotensin II from binding to its receptors on blood vessel walls, resulting in a decrease in blood

Method used

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  • drug combination of nep inhibitor and its application
  • drug combination of nep inhibitor and its application
  • drug combination of nep inhibitor and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] components Composition per unit (mg) composition(%) compound 1 calcium salt 25 62.2％ microcrystalline cellulose 7 17.4％ Low-substituted hydroxypropyl cellulose 5 12.4％ Crospovidone 2 5.0％ talcum powder 0.4 1.0％ colloidal silica 0.2 0.5％ Magnesium stearate 0.6 1.5％ total 40.2 100％

[0063] The magnesium stearate, colloidal silicon dioxide and microcrystalline cellulose are first sieved through a 30-mesh sieve. The above mixture, active ingredient compound 1 calcium salt polymorph, cross-linked polyvinylpyrrolidone and povidone were then mixed in a hopper mixer for about 120 revolutions. The mixture was pressed using a roller press with a pressure of 30 kN. After pressing, the mixture was ground using a grinder and sieved through a 18 mesh sieve to obtain the final internal phase or granules. Fill the granules into capsules to make capsules.

[0064] The dissolution test that gained capsule is car...

Embodiment 2

[0066] components Composition per unit (mg) composition(%) compound 1 calcium salt 123 35.1 Valsartan 98 28 microcrystalline cellulose 61 17.41 Low-substituted hydroxypropyl cellulose 43.5 12.44 Crospovidone 17.5 4.98 colloidal silica 1.75 0.5 Magnesium stearate 5.25 1.5 total weight 350 100

[0067] Firstly, the active ingredient compound 1 calcium salt and valsartan were sieved through a 40-mesh sieve. The microcrystalline cellulose and crospovidone were added to the active ingredient, and the mixture was sieved through a 20-mesh sieve. The mixture was then mixed and rotated about 100 revolutions in a hopper mixer. Then add the low-substituted hydroxypropyl cellulose and colloidal silicon dioxide into the hopper mixer, and make it rotate for 100 revolutions and finally add the magnesium stearate. The powder mixture is then compressed into tablets.

[0068] The tablet that embodiment 2 is prepared is ...

Embodiment 3

[0071]

[0072]

[0073] The magnesium stearate, colloidal silicon dioxide and microcrystalline cellulose are first sieved through a 30-mesh sieve. The above mixture, active ingredients compound 1 and valsartan, crospovidone and povidone were then mixed in a hopper mixer for about 120 revolutions. The mixture was pressed using a roller press with a pressure of 30 kN. After pressing, the mixture was ground using a grinder and sieved through a 18 mesh sieve to obtain the final internal phase or granules. Fill the granules into capsules to make capsules.

[0074] The capsules prepared in Example 3 are placed under different conditions respectively, and the stability of the preparation is investigated, and the results are as shown in the table:

[0075]

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Abstract

Disclosed are a pharmaceutical composition comprising a neutral endopeptidase (NEP) inhibitor and a use thereof in the preparation of a drug for treating and preventing diseases associated with NEP. The composition comprises: (i) (9R,11S)-11-([1,1'-biphenyl]-4-ylmethyl)-2,6,9-trimethyl-4,8,13-trioxo-3,5,7-trioxa-12-azahexadecane-16-acid (compound 1) or a pharmaceutical salt thereof, and / or (ii) an angiotensin II antagonist or a pharmaceutical salt thereof, and / or (iii) an angiotensin-converting enzyme inhibitor, and (iv) a pharmaceutically acceptable carrier.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a drug combination of NEP inhibitors and an application thereof. Background technique [0002] Essential hypertension is a polygenic disease that cannot be completely controlled by a single treatment. In 2000, approximately 3,330 million adults in economically developed countries and approximately 65 million (one in three adults) in the United States had hypertension. Chronic and uncontrolled hypertensive vascular disease will eventually lead to pathological changes in target organs such as heart and kidney. Sustained high blood pressure can also lead to an increased incidence of stroke. The nature of hypertensive vascular disease is therefore multifactorial. Therefore, in some cases, drugs with different mechanisms of action can be used in combination for the control of hypertension and the cardiovascular complications caused by hypertension. [0003] The patent CN2014...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/216A61K31/351A61K31/4015A61K31/54A61K31/4178A61K31/40A61K31/44A61P9/12A61P9/04A61P13/12A61P3/10
CPCA61K31/216A61K31/351A61K31/40A61K31/4015A61K31/4178A61K31/44A61K31/54
Inventor 包如迪王娟娟
Owner SHANGHAI HANSOH BIOMEDICAL
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