Amlodipine and fosinopril sodium medical composition and preparation method thereof

Abstract

The invention relates to an amlodipine and fosinopril sodium medical composition, which comprises the following components in parts by weight: 5 to 10 parts of amlodipine, 10 to 40 parts of fosinopril sodium, 5 to 50 parts of compressible starch, 10 to 60 parts of microcrystalline cellulose, 15 to 40 parts of low-substitution hydroxy propyl cellulose, 10 to 45 parts of crospolyvinylpyrrolidone, and 1 to 3 parts of magnesium stearate, wherein the amlodipine is a maleic amlodipine hydrate crystal, and the molecular formula of the maleic amlodipine hydrate crystal is C24H29ClN2O9.1.5H2O. The medical composition has stable and quick action, stable and durable effect and high bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a medicinal composition of amlodipine and fosinopril sodium and a preparation method thereof. Background technique [0002] Fosinopril, Chinese alias: 4-cyclohexyl-1-[[[2-methyl-1-(1-propionyloxy)propoxy](4-phenylbutyl)phosphinyl]acetyl] -L-proline, English name: Fosinopril, molecular formula: C 30 h 46 NO 7 P, molecular weight: 563.66. Fosinopril is a new phosphorus-containing angiotensin-converting enzyme inhibitor (ACEI) drug that was launched in China in 2007. As a prodrug, it has a weak direct inhibitory effect on ACE, but it is slowly and incompletely absorbed after oral administration, and is rapidly transformed into the more active diacid metabolite fosinoprilat. Fosinoprilat inhibits ACE activity through the combination of secondary phosphate groups and zinc ions in the active site of ACE. The inhibitory effect of this drug on ACE produces the followin...

AI Technical Summary

Problems solved by technology

[0005] 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, and the drug has a very slow onset and slow action; while fosinopril sodium takes 5-7 hours after administration. Reaching the peak concentration of blood concentration, the drug has a slow onset of action, and the pharmaceutical composition with amlodipine or amlodipine salt and fosinopril sodium as active ingredients has a slow onset and slow effect after administration

Chinese patent CN101653440A discloses a composition containing amlodipine salt and pril-like drugs. This patent does not specifically disclose the composition and composition of the excipients in the pharmaceutical composition with amlodipine and fosinopril sodium as active ingredients. In addition, those skilled in the art know that, compared with amlodipine, the solubility and temperature stability of these amlodipine salts are slightly improved, but they are still slightly soluble or even insoluble , is not easily absorbed in the human body. Generally speaking, the time for amlodipine salt to reach the peak blood concentration is still 6-12 hours, and the medicinal composition still takes effect slowly after administration.

[0006] In addition, in order to improve the bioavailability of amlodipine salt, the prior art adopts the method of splitting racemic amlodipine or its salt into levamlodipine or its salt, after administration of levamlodipine or its salt, Although the bioavailability has been improved, the time to reach the peak blood concentration is still 6 to 12 hours, and the onset of action is slow. After administration according to the dose required by the normal human body, the initial blood concentration is very low. Slow onset of action after administration of sodium medicinal compositions

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

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