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A kind of rosuvastatin calcium tablet and preparation method thereof

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 formulation Problems such as product operation difficulties, to achieve the effect of good fluidity and compressibility, good stability and low cost

Active Publication Date: 2016-01-20
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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  • A kind of rosuvastatin calcium tablet and preparation method thereof
  • A kind of rosuvastatin calcium tablet and preparation method thereof
  • A kind of rosuvastatin calcium tablet and preparation method thereof

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 has an average particle size of 100μm.

[0037] Preparation method: First pass the rosuvastatin calcium raw material through a 100-mesh sieve, cross-linked povidone, lactose, microcrystalline cellulose, and magnesium stearate respectively through a 60-mesh sieve, and then pass the prescription amount of rosuvastatin calcium, Cross-linked povidone, lactose, and microcrystalline cellulose, mix well, then add the prescribed amount of magnesium stearate, mix well, press tablets, and coat with film.

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

[0039]

[0040] Remarks: ND = not detected (t...

Embodiment 2

[0041] Example 2: Rosuvastatin calcium tablets (screening for lactose)

[0042] Refer to the formulation and preparation method of Example 1, except that the lactose 90 replaced by 100 (average particle size 150μm), 70 (average particle size 212μm), Tablettose 80 (average particle size 180μm) or 100 (average particle size 150μm), the experimental results are as follows:

[0043]

[0044] It can be seen that different types of lactose have little effect on the dissolution of the drug and related substances, and have a slight impact on the difference in tablet weight. The weight difference of tablets obtained by spray-dried lactose is small, and the tablet weight obtained by granular lactose has a larger difference; The difference in tablet weight obtained by lactose with a larger diameter is smaller, but the difference in tablet weight obtained by all types of lactose is less than ±3.5%.

Embodiment 3

[0045] Example 3: Rosuvastatin calcium tablets (screening of microcrystalline cellulose)

[0046] Refer to the recipe composition and preparation method of Example 1, except that the microcrystalline cellulose Replace 302 with PH301 (average particle size 50μm), PH102 (average particle size 90μm), 90M (average particle size 100μm), LP200 (average particle size 190μm), 301 (average particle size 65μm) and 200 (average particle size 250μm), the experimental results are as follows:

[0047]

[0048] It can be seen that different types of lactose have little effect on the dissolution of the drug and related substances, and have a slight impact on the difference in tablet weight. Within the average particle size range of 90~250μm, the difference in tablet weight of the obtained rosuvastatin calcium tablets is <±1.5 %, but the difference in sheet weight obtained by all types of microcrystalline cellulose is less than ±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 -Yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, the structural formula is 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 to treat hypercholesterolemia, hyperlipoproteinemia and atherosclerosis Like sclerosis, it is superior to other statins on the market in reducing low-density lipoprotein (LDL-C) and raising high-density lipoprotein (HDL-C). It is well tolerated and safe, and is known as " Super statin". [0005] One disadvantage of rosuvastatin calcium is that under certain conditions, such as higher temperature, higher humidity, or ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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