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Atorvastatin calcium tablet and preparation method thereof

A technology for atorvastatin calcium and tablets, which is applied in the field of atorvastatin calcium tablets and its preparation, can solve the problems of harsh preparation processing conditions, sensitivity to air environment factors, unstable biological activity, etc., and achieve improved bioabsorption Utilization, promotion of drug disintegration, and effect of reducing interfacial free energy

Active Publication Date: 2018-05-04
NUOWEIDE TIANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Although the research on atorvastatin calcium preparations in the prior art is mainly focused on improving the stability of atorvastatin calcium, enhancing its dissolution performance and improving cell availability, how to effectively improve the atorvastatin calcium preparations The problems of stability, dissolution performance and cell availability are still technical difficulties that need to be solved urgently in this field.
[0013] In addition, when preparing atorvastatin calcium, due to the high total amount of impurities of atorvastatin calcium in various crystal forms or non-crystalline forms, the optical purity is low, the bioavailability is small, and its conventional crystal form has Sensitivity to environmental factors, unstable biological activity, harsh preparation processing conditions and other shortcomings are difficult to solve simply by preparation technology, which poses another problem for those skilled in the art

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

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Effect test

Embodiment 1

[0063] The atorvastatin calcium tablet of the present embodiment comprises the component of following raw material:

[0064] 1 part by weight of atorvastatin calcium, 10 parts by weight of a filler, 40 parts by weight of a disintegrant, 24 parts by weight of a binder, 8 parts by weight of a lubricant, and 10 parts by weight of a calcium fortifier;

[0065] Wherein, the calcium fortifier is calcium carbonate; the filler is lactose; the disintegrant is crospovidone; the binder is pregelatinized starch; and the lubricant is silicon dioxide.

[0066] Its preparation method is as follows:

[0067] (1) Get atorvastatin calcium, filler, disintegrating agent, binding agent by selected parts by weight, with 2% of the total consumption of described disintegrating agent and described atorvastatin calcium, filler, The binder is mixed evenly, water is used as the granulation solvent, and spray granulation is used for granulation to obtain atorvastatin calcium drug-containing granules;

...

Embodiment 2

[0071] The atorvastatin calcium tablet of the present embodiment comprises the component of following raw material:

[0072] 10 parts by weight of atorvastatin calcium, 80 parts by weight of a filler, 30 parts by weight of a disintegrant, 5 parts by weight of a binder, 15 parts by weight of a lubricant, and 20 parts by weight of a calcium fortifier;

[0073] Wherein, the calcium fortifier is calcium hydrogen phosphate; the filler is pregelatinized starch; the disintegrant is magnesium aluminum silicate; the binder is dextran; and the lubricant is stearin Magnesium acid.

[0074] Its preparation method is as follows:

[0075] (1) Get atorvastatin calcium, filler, disintegrating agent, binding agent by selected parts by weight, with 98% of the total consumption of described disintegrating agent and described atorvastatin calcium, filler, The binder is mixed evenly, and ethanol is used as the granulation solvent, and spray granulation is used for granulation to obtain atorvasta...

Embodiment 3

[0079] The atorvastatin calcium tablet of the present embodiment comprises the component of following raw material:

[0080] 20 parts by weight of atorvastatin calcium, 45 parts by weight of filler, 20 parts by weight of disintegrant, 40 parts by weight of binder, 1 part by weight of lubricant, and 1 part by weight of calcium fortifier;

[0081] Wherein, the calcium fortifier is calcium sulfate; the filler is hydroxypropyl methylcellulose; the disintegrant is pregelatinized starch; the binder is gelatin; the lubricant is talcum powder .

[0082] Its preparation method is as follows:

[0083] (1) Get atorvastatin calcium, filler, disintegrating agent, binding agent by selected parts by weight, with 50% of the total consumption of described disintegrating agent and described atorvastatin calcium, filler, The binder is mixed evenly, acetone is used as the granulation solvent, and spray granulation is used for granulation to obtain atorvastatin calcium drug-containing granules; ...

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Abstract

The invention provides an atorvastatin calcium tablet which comprises the following components of raw materials in parts by weight: 1-20 parts of atorvastatin calcium, 10-80 parts of a filling agent,20-40 parts of a disintegrant, 5-40 parts of an adhesive, 1-15 parts of a lubricant and 1-20 parts of a calcium enhancing agent. The atorvastatin calcium tablet provided by the invention has the advantages of being high in stability, good in dissolubility, high in bioavailability, and the like, and is good in clinical application prospect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an atorvastatin calcium tablet and a preparation method thereof. Background technique [0002] Atorvastatin calcium, the English name is AtorvastatinCalcium, the chemical name is [R-(R,R)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl) base)-3-phenyl-4-[(aniline)carbonyl]-1-hydro-pyrrole-1-calcium heptanoate, whose molecular formula is (C 33 h 34 FN 2 0 5 ) 2 Ca, the molecular weight is 1155.34. Its structural formula is as follows: [0003] [0004] Atorvastatin calcium is a selective HMG-CoA reductase inhibitor, which competitively inhibits the synthesis and metabolism of cholesterol in tissue cells, feedback mediates the activity of low-density lipoprotein LDL receptors, and then promotes the synthesis of LDL in plasma Clearance reduces LDL levels in plasma. The drug can effectively reduce the total cholesterol (TC), low-density lipoprotein...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/40A61K47/02A61K47/12A61P3/06C07D207/34A61K33/06A61K33/10A61K33/42
CPCA61K9/2009A61K9/2013A61K31/40A61K33/06A61K33/10A61K33/42C07B2200/13C07D207/34A61K2300/00
Inventor 杨依军
Owner NUOWEIDE TIANJIN PHARMA
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