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Rosuvastatin calcium tablet and preparation process thereof

A technology for rosuvastatin calcium and a preparation process is applied in the field of rosuvastatin calcium-containing tablets and the preparation process thereof, and can solve the problems of stable rosuvastatin calcium tablets, high fluidity requirements, and poor particle size. Uniformity and other problems, to achieve the effect of easy industrialized large-scale production, solving the release stability, and simple preparation process

Inactive Publication Date: 2015-08-19
KUNMING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This invention does not fundamentally solve the stability problem of rosuvastatin calcium. Since all the excipients have relatively high hygroscopicity, the degradation products will still increase significantly during storage.
At the same time, direct compression has high requirements on the fluidity of excipients, and excipients suitable for direct compression are generally expensive; moreover, rosuvastatin calcium has strong adsorption, and the most obvious defect of direct compression is poor content uniformity
However, the unevenness of dry granulation particles will lead to problems such as large differences in tablet weight, uneven hardness, and rapid dissolution.
[0013] In summary, the prior art has failed to provide a rosuvastatin calcium tablet with good stability, stable dissolution, few side effects, and simple preparation process.

Method used

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  • Rosuvastatin calcium tablet and preparation process thereof
  • Rosuvastatin calcium tablet and preparation process thereof
  • Rosuvastatin calcium tablet and preparation process thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034]

[0035] Preparation process: The prescription quantity weighed rosuvastatin calcium, polystyrene maleic anhydride copolymer, and poloxamer 407 through a 100-mesh sieve, added to absolute ethanol, suspended, and dried under reduced pressure at 40°C to remove ethanol. The dry matter is passed through a 80-mesh sieve, mixed evenly with the prescribed amount of hydroxypropyl methylcellulose, sodium alginate, and microcrystalline cellulose passed through a 100-mesh sieve, then mixed with magnesium stearate, and compressed into tablets.

Embodiment 2

[0037]

[0038]

[0039] Preparation process: The prescription quantity weighed rosuvastatin calcium, polystyrene maleic anhydride copolymer, and poloxamer 407 through a 100-mesh sieve, added to absolute ethanol, suspended, and dried under reduced pressure at 40°C to remove ethanol. The dried product is passed through a 80-mesh sieve, mixed evenly with the prescribed amount of hydroxypropyl methylcellulose, sodium alginate, and starch passed through a 100-mesh sieve, then mixed with calcium stearate, and compressed into tablets.

Embodiment 3

[0041]

[0042] Preparation process: The prescription quantity weighed rosuvastatin calcium, polystyrene maleic anhydride copolymer, and poloxamer 407 through a 100-mesh sieve, added to absolute ethanol, suspended, and dried under reduced pressure at 40°C to remove ethanol. The dried product is passed through an 80-mesh sieve, mixed evenly with the prescribed amount of hydroxypropyl methylcellulose, sodium alginate, and mannitol passed through a 100-mesh sieve, then mixed with sodium stearate fumarate, and compressed into tablets.

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Abstract

The invention discloses a rosuvastatin calcium tablet and a preparation process thereof, and belongs to chemical medicinal preparations. The rosuvastatin calcium tablet is formed by uniformly mixing rosuvastatin calcium solid dispersions with pharmaceutically-acceptable accessories and then carrying out direct compression, the rosuvastatin calcium solid dispersions are obtained by suspending rosuvastatin calcium, a polystyrene maleic anhydride copolymer and poloxamer 407 in absolute ethyl alcohol and drying to remove ethyl alcohol, the rosuvastatin calcium solid dispersions are uniformly mixed with the other pharmaceutically-acceptable accessories, and then the direct compression is carried out. According to the rosuvastatin calcium tablet and the preparation process thereof, the problem of release of the rosuvastatin calcium is successfully solved, and the dissolution stability of the rosuvastatin calcium is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a pharmaceutical preparation, in particular to a tablet containing rosuvastatin calcium and a preparation process thereof. Background technique [0002] Rosuvastatin Calcium is a white amorphous powder, slightly soluble in water and methanol, very slightly soluble in ethanol. Rosuvastatin calcium is a hydrophilic compound with an oil-water partition coefficient (octanol / water) of 0.13 at pH 7. The chemical name is bis-[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidin-5-yl]( 3R,5S)-3,5-Hydroxyhept-6-enoic acid] calcium salt (2:1), the molecular formula is (C 22 h 27 FN 3 o 6 S) 2 Ca, the structural formula is as follows: [0003] [0004] Pharmacological type: Rosuvastatin calcium is a 3-hydroxy-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, so it can reduce the cholesterol level in plasma. [0005...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K31/505A61K9/20A61K47/38A61K47/36A61P3/06
Inventor 李洋朱海燕
Owner KUNMING MEDICAL UNIVERSITY
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