Medicinal composition of amlodipine and atorvastatin calcium and its preparation method

Abstract

The invention relates to a medicinal composition by taking amlodipine and atorvastatin calcium as active components, the medicinal composition comprises amlodipine, atorvastatin calcium, a filler, a disintegrant and a lubricant; the active components are composed of 2-20 parts of amlodipine and 5-120 parts of atorvastatin calcium; the amlodipine is a maleic acid amlodipine hydrate crystal. The molecular formula of the maleic acid amlodipine hydrate crystal is C24H29C1N2O9.1.5H2O. The amlodipine in the medicinal composition has the advantages of fast effectiveness and stability, and is capable of steadily releasing the drug effect in 24 hours, the medicinal composition has strong synergy, accumulation and complementary effects, and the bioavailability is high.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition with amlodipine and atorvastatin calcium as active ingredients and a preparation method thereof. Background technique [0002] Amlodipine, Chinese alias: 6-methyl-2-(2-aminoethoxy)methyl-4-(2-chlorophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid Ethyl ester, English name: Amlodipine, molecular formula: C 20 h 25 ClN 2 O 5 . It can be used for hypertension, alone or in combination with other antihypertensive drugs, and can also be used for patients with stable angina. Dihydropyridine calcium channel blockers (CCBs), as first-line antihypertensive drugs, selectively block voltage-dependent Ca 2+ Channel, relaxes vascular smooth muscle, reduces peripheral resistance, and lowers blood pressure. The characteristics of this class of drugs are that they do not reduce the blood flow of important organs such as the heart, brain and kidney...

AI Technical Summary

Problems solved by technology

[0006] 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 within 6 to 12 hours, and the overall level of blood concentration is low, especially the initial blood concentration after administration is very low. -The peak blood concentration can be reached in 2 hours, and the drug effect is fast. The time difference between the two drugs reaching the peak blood concentration after simultaneous administration is far away, and the synergistic, cumulative and complementary effects are very limited

For example, Chinese patent CN102000075A discloses a pharmaceutical composition of amlodipine and atorvastatin calcium anhydrate, which has lower impurities and degradation products, but amlodipine and atorvastatin calcium The plasma concentration-time curves of the anhydrous substances have not changed, and amlodipine still has a slow onset of action, and the synergistic effect of the two is very limited

[0007] 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. After administration according to the dose required by the normal human body, the initial blood concentration is very low, and its synergy with atorvastatin calcium, accumulation, Complementarity is very limited

Disclosed a kind of composition of atorvastatin and levamlodipine maleate as Chinese patent CN101224205A, this composition has good stability and dissolution rate, but, after administration of this composition, levamlodipine The plasma concentration-time curve of dipine salt has not changed, and the onset of amlodipine is slow, 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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