Method for preparing tablet drug composition containing Rosuvastatin calcium

Abstract

The invention relates to a method for preparing a tablet drug composition containing Rosuvastatin calcium. The preparation forms of the drug composition can be administered to the patients safely and the stability of Rosuvastatin calcium and the absorbability in gastrointestinal tract can be improved. Specifically, the invention relates to a method for preparing the drug composition containing amorphous Rosuvastatin calcium and beta-cyclodextrin. The method is characterized by grinding Rosuvastatin calcium and beta-cyclodextrin under alkaline condition, drying and crashing to obtain (80-100)-mesh fine powder, mixing the fine powder with appropriate auxiliary materials, preparing granules, carrying out tabletting and carrying out coating, thus preparing the drug composition. The in vitro release of the composition is improved to a greater degree, thus improving the bioavailability; and the composition can effectively treat hyperlipidemia, is convenient to take orally, covers the bad taste and is fast to disintegrate and absorb and convenient to carry.

Description

technical field [0001] The invention relates to a preparation method of a rosuvastatin calcium pharmaceutical composition. Dispersing rosuvastatin calcium in beta cyclodextrin can greatly increase the release rate in vitro, thereby improving the bioavailability. Background technique [0002] Rosuvastatin Calcium (Rosuvastatin Calcium), chemical name: bis-[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl) )amino]-pyrimidin-5-yl](3R,5R)-3,5-dihydroxyhept-6-enoic acid] calcium salt (2:1). [0003] Its structural formula is: [0004] [0005] Molecular formula: (C 22 h 27 FN 3 o 6 S) 2 Ca [0006] Molecular weight: 1001.13 [0007] Pharmacological type: Rosuvastatin is a 3-hydroxy-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, so it can reduce the cholesterol level in plasma. [0008] Mechanism of action: Rosuvastatin can selectively inhibit the rate-limiting enzyme HMG-CoA reductase in the synthesis of cholesterol in the liver, reducing live...

AI Technical Summary

Problems solved by technology

[0018] One disadvantage of rosuvastatin calcium is that in some cases, it is easily degraded in high temperature, high humidity and light environment, and the main product formed is lactone Degradation products, oxidative degradation products and photodegradation products, which make it difficult to configure the product, and the prepared pharmaceutical composition cannot meet the storage period requirements. This instability is determined by itself. Rosuvastatin The β, δ-hydroxyl groups on the heptenoic acid chain in the calcium molecule are very stable. Among them, the hydroxyl group adjacent to the carbon-carbon double bond is easily oxidized into a ketone functional group, and can also undergo intramolecular ring closure to form a lactone

[0025] In order to solve the above problems, the inventor has explored through a large number of experiments for a long time, surprisingly found a new pharmaceutical composition of rosuvastatin calcium, which Under the conditions of preparation, storage and high humidity, the degradation products of lactone, oxidative degradation and light degradation of the composition no longer increase, which can ensure the stability of long-term storage, thereby solving the problem of stability of rosuvastatin calcium preparations. sexual problems

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