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Rosuvastatin calcium tablet and preparation method

A technology of rosuvastatin calcium and tablet cores, which is applied in the field of rosuvastatin calcium tablets and its preparation, can solve the problem that the pharmaceutical composition cannot meet the storage period requirements, the stability of rosuvastatin calcium tablets decreases, and the preparation Problems such as product operation difficulties, to achieve the effect of good fluidity and compressibility, good stability and low cost

Active Publication Date: 2013-01-09
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] A disadvantage of rosuvastatin calcium is that it is easily degraded under certain conditions, such as higher temperature, higher humidity, or light conditions, and the main products formed are (3R, 5S) lactone degradation products and oxidation product, which makes the preparation of the product difficult, and the prepared pharmaceutical composition does not meet the storage period requirements
Experiments have found that the stability of rosuvastatin calcium tablets prepared with micro-powdered silica gel from certain manufacturers is reduced; moreover, when the content of micro-powdered silica gel in the prescription is large, powder throwing will occur during tablet compression, resulting in a large difference in tablet weight

Method used

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  • Rosuvastatin calcium tablet and preparation method
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  • Rosuvastatin calcium tablet and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Rosuvastatin Calcium Tablets

[0034] Prescription composition (1000 tablets)

[0035]

[0036] Remarks: Lactose 90 average particle size 160μm; microcrystalline cellulose 302 average particle size 100μm.

[0037]Preparation method: first pass the rosuvastatin calcium raw material through a 100-mesh sieve, crospovidone, lactose, microcrystalline cellulose, and magnesium stearate respectively pass through a 60-mesh sieve, and then pass the prescribed amount of rosuvastatin calcium, Crospovidone, lactose, and microcrystalline cellulose are mixed evenly, and then magnesium stearate is added in the prescribed amount, mixed evenly, compressed into tablets, and film-coated.

[0038] Results: The tableting process was smooth, the tablet surface was smooth, and the difference in tablet weight was <±1.5%; the tablet surface was smooth and complete after coating. The dissolution rate of samples and related substances are as follows:

[0039]

[0040] Note:...

Embodiment 2

[0041] Embodiment 2: Rosuvastatin calcium tablet (screening to lactose)

[0042] With reference to embodiment 1 prescription composition and preparation method, just lactose 90 is replaced with 100 (average particle size 150μm), 70 (average particle size 212μm), Tablettose 80 (average particle size 180μm) or 100 (average particle size 150 μm), the experimental results are as follows:

[0043]

[0044] It can be seen that different types of lactose have little effect on drug dissolution rate and related substances, but slightly affect the difference in tablet weight. The difference in tablet weight obtained by using spray-dried lactose is small, and the difference in tablet weight obtained by using granular lactose is relatively large; The difference in tablet weight obtained by lactose with a larger diameter is small, but the difference in tablet weight obtained by all types of lactose is <±3.5%.

Embodiment 3

[0045] Embodiment 3: Rosuvastatin calcium tablet (screening to microcrystalline cellulose)

[0046] With reference to embodiment 1 prescription composition and preparation method, just microcrystalline cellulose 302 is replaced with PH 301 (average particle size 50μm), PH 102 (average particle size 90μm), 90M (average particle size 100μm), LP200 (average particle size 190μm), 301 (average particle size 65μm) and 200 (average particle size 250 μm), the experimental results are as follows:

[0047]

[0048] It can be seen that different types of lactose have little effect on drug dissolution rate and related substances, but slightly affect the difference in tablet weight. Within the average particle size range of 90-250 μm, the difference in tablet weight of the obtained rosuvastatin calcium tablets is <±1.5 %, but the differences in tablet weights obtained from the types of microcrystalline cellulose used were all <±3.5%.

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Abstract

The invention relates to a rosuvastatin calcium tablet and a preparation method, the tablet is composed of a tablet core and a coating layer, the tablet core is composed of rosuvastatin calcium, lactose, microcrystalline cellulose, a disintegrating agent and a lubricant, the lactose is spray dried lactose or particle lactose, and the microcrystalline cellulose is flowing steam dried microcrystalline cellulose or spray dried microcrystalline cellulose. The rosuvastatin calcium tablet is not required for adding a stabilizing agent or aerosil or preparing to a special preparation, the rosuvastatin calcium preparation with good stability, excellent dissolution and content uniformity can be obtained by a direct tabletting technology, and the method of the invention has the advantages of simple technology and low cost, and is suitable for large scale production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a rosuvastatin calcium tablet and a preparation method thereof. Background technique [0002] Rosuvastatin calcium, chemical name bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5 -base]-(3R, 5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, the structural formula is as shown in formula 1: [0003] [0004] Rosuvastatin calcium is a potent 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCoA reductase) inhibitor, which can be used in the treatment of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis It is better than other statins on the market in terms of lowering low-density lipoprotein (LDL-C) and raising high-density lipoprotein (HDL-C), and has good tolerance and safety. Super statin". [0005] A disadvantage of rosuvastatin calcium is that it is easily degraded under certain conditions, such as higher tempe...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/30A61K31/505A61P3/06A61P9/10
Inventor 赫玉霞白敏杜旭召陈素锐王蒙吴欢欢金晓利刘英帝陈亚平郝卫华
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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