Method for preparing tablet drug composition containing Rosuvastatin calcium

A technology of rosuvastatin calcium and its composition, which is applied in the field of preparation of rosuvastatin calcium pharmaceutical composition, can solve the problem that the stability of rosuvastatin calcium preparation and the pharmaceutical composition cannot reach the storage period Requirements, configure product operation difficulties and other issues, to achieve the effect of improving in vitro dissolution rate, improving bioavailability, and simple operation

Inactive Publication Date: 2011-04-13
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Method for preparing tablet drug composition containing Rosuvastatin calcium
  • Method for preparing tablet drug composition containing Rosuvastatin calcium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] Embodiment 1 (comparative embodiment)

[0118] Rosuvastatin Calcium 10-20g

[0119] Croscarmellose Sodium 30-60g

[0120] Microcrystalline Cellulose 100-200g

[0121] Lactose 100-240g

[0122] Pregelatinized starch 20-40g

[0123] Talc powder 1-2g

[0124] 5% povidone absolute ethanol solution appropriate amount

[0125] Coating powder 90-180g

[0126] Makes 1000 pieces

[0127] The preparation method goes through the following steps:

[0128] 1) Sift rosuvastatin calcium, microcrystalline cellulose, lactose, croscarmellose sodium, pregelatinized starch, and talcum powder separately, and set aside;

[0129] 2) Mix the raw and auxiliary materials evenly and set aside;

[0130] 3) Take 5% povidone anhydrous ethanol solution in 2), mix well, make 30-40 mesh granules, dry below 50°C, granulate, add lubricant, mix evenly, and compress into tablets;

[0131] 4) Put the sample prepared in 3) into the coating pan, coat it, and get it.

Embodiment 2

[0133] Composition 1

[0134] Rosuvastatin Calcium 20g

[0135] Beta Cyclodextrin 80g

[0136] Sodium hydroxide 0.02g

[0137] Composition 2

[0138] Croscarmellose Sodium 60g

[0139] Microcrystalline Cellulose 200g

[0140] Lactose 240g

[0141] Pregelatinized starch 40g

[0142] Talc powder 2g

[0143] 5% povidone absolute ethanol solution appropriate amount

[0144] Coating Composition

[0145] Coating powder 180g

[0146] Makes 1000 pieces

[0147] The preparation method goes through the following steps:

[0148] 1) Put rosuvastatin calcium, beta cyclodextrin, and sodium hydroxide in a mortar, add a small amount of water and grind it into a paste, dry it below 50°C, grind it into 80-100 mesh fine powder, and set aside;

[0149] 2) Sieve microcrystalline cellulose, lactose, croscarmellose sodium, pregelatinized starch, and talcum powder respectively, and set aside;

[0150] 3) Add the prescribed amount of excipient 2) into 1), mix well, and set aside;

[0151...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61K47/40A61P3/06
Inventor 黄欣
Owner TIANJIN HANRUI PHARMA
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