Atorvastatin calcium tablet and preparation method thereof

A technology for atorvastatin calcium and tablets, applied in the field of tablets containing atorvastatin calcium and its preparation, capable of solving the gastrointestinal irritation of surfactants, aggravating gastrointestinal irritation, and insufficient dissolution rate, etc. problems, to achieve the effect of improving drug solubility, reducing stomach discomfort, and solving stability problems

Active Publication Date: 2015-01-28
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Atorvastatin calcium has poor stability and is sensitive to humidity, heat and low pH conditions, especially in low pH conditions, it is easy to degrade
Atorvastatin calcium has poor solubility in acidic environment, after testing, commercially available ( Pfizer) in pH1.2 hydrochloric acid medium 10min dissolution rate is less than 60%
However, the problem caused by a large amount of disintegrants is that it is easy to absorb moisture, which leads to the degradation of atorvastatin calcium
Furthermore, a certain amount of sodium lauryl sulfate is added to the formula to improve the dissolution rate in vitro, but the addition of surfactants will cause gastrointestinal irritation
[0011] Chinese patent CN102309462A provides a kind of atorvastatin calcium tablet, which adopts dry secondary granulation technology, the process is relatively complicated, the stability is poor, and it cannot be completely dissolved in acid
The invention uses slightly acidic lactose and highly hygroscopic crospovidone, which will lead to the degradation of atorvastatin calcium
[0014] Chinese patent CN101791297B discloses an orally disintegrating atorvastatin calcium tablet and a preparation method thereof to prepare atorvastatin calcium tasteless microcapsules, but the process is complicated and the dissolution is not fast
[0016] Chinese patent CN 102139115B discloses the cyclodextrin inclusion compound of atorvastatin and the preparation method of its oral solid preparation. The sulfobutyl-β-cyclodextrin used is high in moisture, which easily leads to the degradation of atorvastatin calcium
The preparation process of both is relatively complicated, and a large amount of surfactant is used, which aggravates the irritation to the gastrointestinal tract
[0018] In summary, in the prior art, a kind of atorvastatin calcium tablet with good stability and high dissolution rate has not been provided.

Method used

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  • Atorvastatin calcium tablet and preparation method thereof
  • Atorvastatin calcium tablet and preparation method thereof
  • Atorvastatin calcium tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] (1) Atorvastatin calcium coated pellets

[0038]

[0039] (2) Atorvastatin Calcium Tablets

[0040]

[0041] Preparation Process:

[0042] (1) Dissolve atorvastatin calcium in methanol, add polacrilin potassium IRP-88 fine powder, ultrasonicate for 1h, frequency 26.4kHz, dry under reduced pressure at 50°C to remove solvent, pulverize, and pass through a 100-mesh sieve to obtain atorvastatin calcium Vastatin calcium solid dispersion;

[0043] (2) Swell Carbomer 971P in water completely, add triethanolamine to adjust the pH to 9.0, add the atorvastatin calcium solid dispersion prepared in step (1) and stir evenly, and spray dry to obtain atorvastatin calcium pellets ;

[0044] (3) Dissolve acrylic resin IV and ethyl cellulose in absolute ethanol as a coating liquid, and carry out fluidized bed bottom spray coating to the atorvastatin calcium pellets prepared in step (3), with a blast flow rate of 80m 3 / h, the air inlet temperature is 60°C, and the weight gain is ...

Embodiment 2

[0047] (1) Atorvastatin calcium coated pellets

[0048]

[0049] (2) Atorvastatin Calcium Tablets

[0050]

[0051]

[0052] Preparation Process:

[0053] (1) Dissolve atorvastatin calcium in methanol, add polacrilin potassium IRP-88 fine powder, ultrasonicate for 1h, frequency 26.4kHz, dry under reduced pressure at 50°C to remove solvent, pulverize, and pass through a 100-mesh sieve to obtain atorvastatin calcium Vastatin calcium solid dispersion;

[0054] (2) Swell Carbomer 971P in water completely, add triethanolamine to adjust the pH to 10.0, add the atorvastatin calcium solid dispersion prepared in step (1) and stir evenly, and spray dry to obtain atorvastatin calcium pellets ;

[0055] (3) Dissolve acrylic resin IV and ethyl cellulose in absolute ethanol as a coating liquid, and carry out fluidized bed bottom spray coating to the atorvastatin calcium pellets prepared in step (3), with a blast flow rate of 80m 3 / h, the air inlet temperature is 60°C, and the ...

Embodiment 3

[0058] (1) Atorvastatin calcium coated pellets

[0059]

[0060] (2) Atorvastatin Calcium Tablets

[0061]

[0062] Preparation Process:

[0063] (1) Dissolve atorvastatin calcium in methanol, add polacrilin potassium IRP-88 fine powder, ultrasonicate for 1h, frequency 26.4kHz, dry under reduced pressure at 50°C to remove solvent, pulverize, pass through a 100-mesh sieve to obtain atorvastatin Statin calcium solid dispersion;

[0064] (2) Swell Carbomer 971P in water completely, add triethanolamine to adjust the pH to 11.0, add the atorvastatin calcium solid dispersion prepared in step (1) and stir evenly, and spray dry to obtain atorvastatin calcium pellets ;

[0065] (3) Dissolve acrylic resin IV and ethyl cellulose in absolute ethanol as a coating liquid, and carry out fluidized bed bottom spray coating to the atorvastatin calcium pellets prepared in step (3), with a blast flow rate of 80m 3 / h, the air inlet temperature is 60°C, and the weight gain is 20%, to obt...

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Abstract

The invention discloses an atorvastatin calcium tablet and a preparation method thereof. The tablet is prepared from atorvastatin calcium, polacrilin potassium IRP-88, carbomer 971P, acrylic resin IV, ethyl cellulose and other pharmaceutically acceptable auxiliaries. According to the atorvastatin calcium tablet, the stability problem of atorvastatin calcium preparation and storage processes can be successfully solved, the atorvastatin calcium solid dispersion is prepared by adopting a solvent deposition technology, and the drug solubility can be greatly improved; and stomach discomfort and other side effects can be reduced by means of a semipermeable membrane coating.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a solid oral preparation, in particular to a tablet containing atorvastatin calcium and a preparation method thereof. Background technique [0002] Atorvastatin calcium (Atorvastatin Calcium) belongs to the inhibitor of hydroxymethylglutaryl CoA (HMG-CoA) reductase, which can reduce the concentration of cholesterol in plasma and serum lipoprotein by inhibiting the biosynthesis of HMG-COA reductase and cholesterol in the liver , and enhance the uptake and metabolism of low-density lipoprotein by increasing the hepatic low-density lipoprotein receptors on the cell surface. Atorvastatin calcium can effectively reduce plasma total cholesterol, low-density lipoprotein cholesterol, apolipoprotein and triglyceride in patients with homozygous and heterozygous familial hypercholesterolemia, nonfamilial cholesterolemia and mixed lipid metabolism disorders A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/40A61K47/32A61P3/06
Inventor 王雷陈磊
Owner NANJING CHIA TAI TIANQING PHARMA
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