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Pharmaceutical compositions of allisartan Isoproxil or salts thereof with diuretics

A technology of alisartan medoxomil and composition, which is applied in the field of medicinal chemistry, can solve the problems of undisclosed dosage of diuretics, undisclosed dosage of diuretics, and inability to achieve the best therapeutic effect, etc., and achieves reduction of adverse drug reactions, simple steps, and improved The effect of the antihypertensive effect

Active Publication Date: 2019-06-04
SHENZHEN SALUBRIS PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]However, for people with severe hypertension and / or with multiple risk factors, target organ damage or clinical diseases, the administration of a single antihypertensive drug often cannot achieve the optimal For such patients, it is usually necessary to consider administering two or more antihypertensive drugs with different antihypertensive mechanisms
[0005] Chinese patent CN101822837A discloses a pharmaceutical composition of alisartan medoxomil or its salt and a diuretic, and discloses that the diuretic can be hydrochlorothiazide, chlorthalidone, indole Dapamide, meclothiazide, triamterene, spironolactone, furosemide, amiloride, torasemide, eplerenone, bumetanide, and the disclosure of alisartan medoxomil and its salts The dosage is 5mg to 800mg / person / day, more preferably 5mg-300mg / person / day, but the patent does not disclose the dosage of diuretics, as well as the matching range, optimal ratio and related experimental data that can achieve related synergistic effects; Similarly, Chinese patents CN101822836A and CN101822667A also disclose the pharmaceutical composition of alisartan medoxomil or its salt and diuretic, and disclose the dosage of alisartan medoxomil and its salt, but also do not disclose the dosage of diuretic, and can realize related synergy. Functional ratio range, optimal ratio and related experimental data

Method used

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  • Pharmaceutical compositions of allisartan Isoproxil or salts thereof with diuretics
  • Pharmaceutical compositions of allisartan Isoproxil or salts thereof with diuretics
  • Pharmaceutical compositions of allisartan Isoproxil or salts thereof with diuretics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 prepares alisartan medoxomil-indapamide pharmaceutical composition

[0024] Allisartan medoxomil (4.8 kg) was added in the V-shaped mixing cylinder, and indapamide (0.5 kg) was added, and after mixing for 60 minutes, the alisartan medoxomil-indapamide pharmaceutical composition with a mass ratio of 96:1 was obtained.

[0025] The same method can be used to prepare other alisartan medoxomil-indapamide pharmaceutical compositions with other mass ratios, such as alisartan medoxomil-indapamide pharmaceutical compositions with mass ratios of 48:1 and 300:1.

Embodiment 2

[0026] Embodiment 2 prepares alisartan medoxomil potassium-indapamide pharmaceutical composition

[0027] Allisartan medoxomil potassium (2.4 kg, calculated as allisartan medoxomil) was added in the V-type mixing cylinder, added indapamide (0.5 kg), and after mixing for 30 minutes, added allisartan medoxomil potassium (2.4 kg, calculated as allisartan medoxomil) ), after further mixing for 30 minutes, it is the alisartan medoxomil potassium-indapamide pharmaceutical composition that mass ratio is 96:1.

[0028] The same method can be used to prepare the other mass ratios of alisartan medoxomil potassium-indapamide pharmaceutical compositions, such as the alisartan medoxomil potassium-indapamide pharmaceutical compositions with mass ratios of 48:1 and 300:1.

Embodiment 3

[0029] Embodiment 3 prepares other alisartan medoxomil salt-indapamide pharmaceutical composition

[0030] The same method as in Example 1 or 2 can be used to prepare the pharmaceutical composition of other salts of alisartan medoxomil and indapamide, such as other salts of alisartan medoxomil and indapamide in mass ratios of 48:1, 96:1, and 300:1. Pharmaceutical compositions of dapamide.

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Abstract

The invention provides compositions of allisartan Isoproxil with pharmaceutical prospects and / or salts thereof with diuretics. By limiting the mass ratio of the allisartan Isoproxil and / or the salts thereof to the diuretics, the compositions are capable of realizing synergistic blood-pressure-reducing effects; moreover, the compositions are beneficial for improving the blood-pressure-reducing effects, thereby reducing adverse drug reactions.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular, the scheme relates to a pharmaceutical composition of alisartan medoxomil or its salt and a diuretic. Background technique [0002] Alisartan medoxomil (CAS: 947331-05-7), chemical name: 2-butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl -Methyl]-imidazole-5-carboxylic acid, 1-[(isopropoxy)-carbonyloxy]-methyl ester, trade name: Xinlitan, is a new type of angiotensin Ⅱ receptor antagonist . Chinese patent CN200680000397.8 discloses the structural formula of the allisartan medoxomil compound. The allisartan medoxomil is less toxic and has a better antihypertensive effect than similar products (such as losartan). Its antihypertensive effect. [0003] [0004] However, for the population with severe hypertension and / or with multiple risk factors, target organ damage or clinical disease, the administration of a single antihypertensive drug often cannot achieve the best the...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/4178A61P9/12A61K31/404
CPCA61K45/06A61K31/4178A61K31/404A61P9/12A61K2300/00
Inventor 颜杰孙晶超景小龙
Owner SHENZHEN SALUBRIS PHARMA
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