Amlodipine and olmesartan medoxomil pharmaceutical composition and preparation method thereof

Abstract

The invention relates to an amlodipine and olmesartan medoxomil pharmaceutical composition and a preparation method thereof. The amlodipine and olmesartan medoxomil pharmaceutical composition comprises the following components in parts by weight: 2.5-10 parts of amlodipine, 20-40 parts of olmesartan medoxomil, 5-50 parts of compressible starch, 10-60 parts of microcrystalline cellulose, 15-40 parts of low-substituted hydroxypropyl cellulose, 10-45 parts of cross-linked polyvinylpyrrolidone, 1-5 parts of essence and 1-3 parts of magnesium stearate, wherein the amlodipine is an amlodipine maleate hydrate crystal. The pharmaceutical composition has the advantages of rapider and stable acting, strong synergism, accumulation and complementation effects, and high bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an amlodipine olmesartan medoxomil medicinal composition and a preparation method thereof. Background technique [0002] Olmesartan, Chinese alias: 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[2'-(tetrazol-5-yl)phenyl]phenyl]methylimidazole -5-Carboxylic acid, English name: Olmesartan Medoxomil, molecular formula: C 24 h 26 N 6 o 3 , molecular weight: 446.5, the structural formula is as follows: [0003] [0004] Olmesartan medoxomil is a new angiotensin II receptor antagonist (ARB) drug launched in China in August 2006. Olmesartan medoxomil is the latest member of the angiotensin II receptor antagonist (ARB) class of drugs. It is a prodrug that can be rapidly and completely hydrolyzed into the active metabolite olmesartan after entering the gastrointestinal tract And its absorption is not affected by food. Because olmesartan medoxomil is not metabolized by the ...

AI Technical Summary

Problems solved by technology

[0010] In the prior art, amlodipine and amlodipine salts (such as amlodipine maleate, amlodipine besylate, amlodipine mesylate, etc.) are almost insoluble in water and are slowly absorbed in the human body. The peak blood concentration is reached in 6-12 hours, and the overall level of blood drug concentration is low, especially the initial blood concentration after administration is very low, the drug has a very slow onset and slow action; while olmesartan medoxomil is administered 1-2 hours after administration Reach the peak concentration of the blood concentration, the drug has a rapid onset of action, and the time difference between the two drugs when they reach the peak blood concentration after simultaneous administration is far away, and the synergistic, cumulative and complementary effects are very limited

Disclosed as Chinese patent CN101766609A is a kind of compound preparation that is made up of amlodipine besylate, olmesartan medoxomil and auxiliary material, because the blood drug concentration-time curve of amlodipine and olmesartan medoxomil does not change respectively, ammonia Clodipine still works slowly, and the synergistic, additive and complementary effects of the two are very limited

[0011] In addition, in order to improve the bioavailability of amlodipine salt, the prior art uses the amlodipine salt of the racemate to be split into levamlodipine salt. After the administration of levamlodipine salt, although the bioavailability is somewhat However, the time to reach the peak blood concentration is still 6-12 hours, and the onset of effect is slow. The initial blood concentration after administration according to the dose required by the normal human body is very low, and its synergy, accumulation and complementarity with olmesartan medoxomil very limited

Chinese patent CN101416966A discloses a novel pharmaceutical composition for the treatment of hypertension, specifically related to levamlodipine and olmesartan medoxomil, and levamlodipine includes pharmaceutically acceptable salts, including besylate, malay However, after administration of the pharmaceutical composition, the plasma concentration-time curve of levamlodipine salt does not change, amlodipine takes effect slowly, and the synergistic effect of the two is very limited

And, amlodipine salt is split into levamlodipine salt, which increases the production process, and in the process of splitting, there is loss of dexamlodipine salt and the introduction of impurities, which greatly increases the cost of medicine

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