Rosuvastatin calcium oral drug composition

Abstract

The invention relates to a rosuvastatin calcium oral drug composition and a preparation method thereof. The rosuvastatin calcium oral drug composition is characterized by comprising the following components in proportion: 10-80mg of rosuvastatin calcium, 20-160mg of hydroxypropyl betadex, 5-40mg of meglumine, 2-16mg of sodium sulfite, 100-800mg of lactose, 50-400mg of microcrystalline cellulose, 20-160mg of croscarmellose sodium, 2-16mg of magnesium stearate and a proper amount of 80 percent ethanol solution. The preparation method comprises the following steps of: dissolving hydroxypropyl betadex, meglumine and magnesium stearate into a proper amount of 80% ethanol solution; adding rosuvastatin calcium and mixing until the rosuvastatin calcium is completely dissolved; evenly mixing lactose, microcrystalline cellulose and croscarmellose sodium for later use; quantitatively adding the solution into an evenly-mixed accessory for pelletization; and obtaining a finished product by drying, palletizing, totally mixing, checking an intermediate body, pressing into pieces, coating and packing. The prepared rosuvastatin calcium tablet has good stability and high bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to an oral pharmaceutical composition of rosuvastatin calcium and a preparation method thereof. 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 liver protein production and increasing the expression of low...

AI Technical Summary

Problems solved by technology

[0023] One disadvantage of rosuvastatin calcium is that in some cases, it is easily degraded in high-temperature, high-humidity and light environments, and the main products formed are lactone degradation products, oxidative degradation products and light degradation products, resulting in The operation is difficult, and the prepared pharmaceutical composition cannot meet the requirement of storage period. This instability is determined by itself. The β, δ-hydroxyl groups on the heptenoic acid chain in the Rosuvastatin calcium molecule Stable, in which 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

[0030] 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. Degradation products, oxidative degradation products, and photodegradation products are no longer increased, which can ensure the stability of long-term storage, thus solving the problem that has been plagued by the stability of rosuvastatin calcium preparations

Images