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Rosuvastatin calcium tablet and preparation method thereof

A technology of rosuvastatin calcium and tablet cores, which is applied in the field of medicine, can solve the problems that the pharmaceutical composition cannot meet the storage period requirements, the pharmaceutical composition cannot be legally implemented, and the operation of the product is difficult to configure, so as to achieve excellent quality and stability Sexuality, rapid release, and the effect of solving stability problems

Active Publication Date: 2015-03-11
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] 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 lactone degradation products, oxidative degradation products and photodegradation products product, thus causing difficulty in configuring the product, and the prepared pharmaceutical composition cannot meet the storage period requirements. This instability is determined by itself. The heptenoic acid chain in the rosuvastatin calcium molecule β, δ-hydroxyl is 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
The defect of this patent is that there is no micro-powder silica gel with a pharmaceutical registration license in China, which leads to the fact that the pharmaceutical composition cannot be legally implemented in the country and cannot be industrialized

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] (1) Prescription:

[0086] Tablet prescription:

[0087]

[0088] Prescription of coating solution: dosage of 1000 tablets

[0089] Opadry 6.75g

[0090] Add purified water to 45g

[0091] (2) Preparation method:

[0092] ① Pass rosuvastatin calcium, crospovidone, and calcium hydrogen phosphate through an 80-mesh sieve, microcrystalline cellulose-lactose (1:3) compound through a 60-mesh sieve, and magnesium stearate through a 100-mesh sieve, spare.

[0093] ② Take rosuvastatin calcium, microcrystalline cellulose-lactose (1:3) complex, crospovidone, and calcium hydrogen phosphate that meet the requirements and mix them in a mixer for 45 minutes.

[0094] ③ Add magnesium stearate to the product obtained in step ② and mix evenly, measure the content of the main ingredient, determine the weight of the tablet, and compress it under the conditions of ambient temperature 18°C ​​and humidity 45%, and the compression pressure is 15-35kN.

[0095] ④Put the tablet prepare...

Embodiment 2

[0098] (1) Prescription:

[0099] Tablet prescription:

[0100]

[0101] Prescription of coating solution: dosage of 1000 tablets

[0102] Opadry 6.75g

[0103] Add purified water to 45g

[0104] (2) Preparation method:

[0105] ① Pass rosuvastatin calcium, crospovidone, and calcium hydrogen phosphate through an 80-mesh sieve, microcrystalline cellulose-lactose (1:3) compound through a 60-mesh sieve, and magnesium stearate through a 100-mesh sieve, spare.

[0106] ② Take rosuvastatin calcium, microcrystalline cellulose-lactose (1:3) compound, and crospovidone that meet the requirements and mix them evenly in a mixer.

[0107]③ Add magnesium stearate to the product obtained in step ② and mix evenly, measure the content of the main ingredient, determine the weight of the tablet, and press it under the conditions of ambient temperature 18°C ​​and humidity 60%, and the tableting pressure is 15-35kN.

[0108] ④Put the tablet prepared in step ③ into a coating pan for coatin...

Embodiment 3

[0111] (1) Prescription:

[0112] Tablet prescription:

[0113]

[0114] Prescription of coating solution: dosage of 1000 tablets

[0115] Opadry 6.75g

[0116] Add purified water to 45g

[0117] (2) Preparation method:

[0118] ① Pass rosuvastatin calcium, low-substituted hydroxypropyl cellulose, and tricalcium phosphate through a 80-mesh sieve, microcrystalline cellulose-lactose (1:3) compound through a 60-mesh sieve, and silicon dioxide through a 100-mesh sieve ,spare.

[0119] ② Take rosuvastatin calcium, microcrystalline cellulose-lactose (1:3) compound, and low-substituted hydroxypropyl cellulose that meet the requirements and mix them evenly in a mixer.

[0120] ③ Add silicon dioxide to the product obtained in step ② and mix evenly, measure the content of the main ingredient, determine the weight of the tablet, and press it under the conditions of ambient temperature 26°C and humidity 60°C, and the tableting pressure is 30-35kN.

[0121] ④Put the tablet prepare...

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Abstract

The invention provides a rosuvastatin calcium pharmaceutical composition and a preparation method thereof. A rosuvastatin calcium tablet comprises a tablet core and a film coating, and is characterized in that the tablet core is formed by taking rosuvastatin calcium as a pharmaceutical active ingredient and a pharmaceutically auxiliary material; the pharmaceutically auxiliary material contains a microcrystalline cellulose-lactose compound, calcium hydrophosphate, polyvinylpolypyrrolidone and magnesium stearate. A direct powder compression method is adopted for tabletting to prepare a rosuvastatin calcium preparation, so that the stability, dissolution speed and content uniformity of the medicine are improved; the rosuvastatin calcium tablet is simple in technology and low in cost, and is suitable for large-scale production.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a tablet of rosuvastatin calcium and a preparation process thereof. Background technique [0002] Hyperlipidemia refers to abnormal fat metabolism or operation in the human body, and the contents of total cholesterol (TC), triacylglycerol (TG), LDL-C and very low-density lipoprotein cholesterol (VLDL-C) in plasma Exceeding the normal standard, in addition, the level of high-density lipoprotein cholesterol (HDL-C) in the plasma is too low, which also belongs to the category of dyslipidemia. [0003] 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: [0004] [0005] Molecular formula: (C 22 h 27 FN 3 O6 S )2Ca [0006] Molecular weight: 1001.13 [0007] Pharmacological type: Rosuvastatin calcium is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K9/36A61K31/505A61K47/04A61K47/38A61K47/26A61P3/06
Inventor 曲继广杨帆刘芳菊赵晓雷程彦超张微微李彪关珊孙晓业曹柳
Owner SHIJIAZHUANG NO 4 PHARMA
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