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A kind of atorvastatin calcium tablet and its preparation process

A technology of atorvastatin calcium and lubricant, which is applied in the field of atorvastatin calcium tablet and its preparation, can solve the problems of surfactant gastrointestinal irritation, failure to dissolve rapidly, and degradation of atorvastatin calcium. , to achieve the effect of improving disintegration rate and dissolution rate, improving various properties, and improving dissolution rate

Active Publication Date: 2021-04-09
福建东瑞制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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
[0010] 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
However, the tablet only dissolves 60% in 30 minutes in acid, and fails to dissolve rapidly completely.
At the same time, lactose is an acidic substance, which will lead to the degradation of atorvastatin calcium

Method used

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  • A kind of atorvastatin calcium tablet and its preparation process
  • A kind of atorvastatin calcium tablet and its preparation process
  • A kind of atorvastatin calcium tablet and its preparation process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] An atorvastatin calcium tablet, comprising the following components in parts by weight: 5 parts of atorvastatin calcium with a particle diameter of 30-40 μm, 40 parts of starch, 1 part of povidone, and 20 parts of crospovidone , 1 part of magnesium stearate, 3 parts of polyethylene glycol-4000.

[0070] Atorvastatin calcium tablets are prepared by the following method:

[0071] (1) Mix atorvastatin calcium, starch, 10% magnesium stearate, and crospovidone, first stir at 50r / min for 5min, and then 200r / min for 10min to obtain substance A;

[0072] (2) Heating purified water to 40°C, adding povidone and polyethylene glycol-4000 according to a mass ratio of 1:3, to obtain substance B;

[0073] (3) Mixing substance A and substance B, passing through a 16-mesh sieve to obtain wet granules;

[0074] (4) Dry the wet granules at 40°C, control the moisture to <2%, pass through a 20-mesh sieve for granulation, and obtain dry granules;

[0075] (5) Add the remaining 90% magnesi...

Embodiment 2

[0077] An atorvastatin calcium tablet, comprising the following components in parts by weight: 15 parts of atorvastatin calcium with a particle diameter of 30-40 μm, 70 parts of mannitol, 5 parts of hydroxypropyl cellulose, and carboxymethyl starch 35 parts of sodium, 5 parts of sodium stearate fumarate, 8 parts of polyethylene glycol-6000.

[0078] Atorvastatin calcium tablets are prepared by the following method:

[0079] (1) Mix atorvastatin calcium, mannitol, 20% sodium stearate fumarate, and sodium carboxymethyl starch, first stir at 100r / min for 10min, and then stir at 300r / min for 20min to obtain substance A;

[0080] (2) Heating purified water to 50°C, adding hydroxypropyl cellulose and polyethylene glycol-6000 according to the mass ratio of 1:10, to obtain substance B;

[0081] (3) mix substance A and substance B, pass through a 18-mesh sieve, and obtain wet granules;

[0082] (4) Dry the wet granules at 60°C, control the moisture to <2%, pass through a 20-mesh siev...

Embodiment 3

[0085] An atorvastatin calcium tablet, comprising the following components in parts by weight: 5 parts of atorvastatin calcium, 40 parts of microcrystalline cellulose, 1 part of binder, 20 parts of disintegrant, 1 part of silicon dioxide , 3 parts of macrogol-4000, 1 part of aspartame.

[0086] The particle size composition of the atorvastatin calcium is as follows: 30-40 μm: 5-10 μm=3:1;

[0087] The binder is a mixture of gelatin and hypromellose, and the mass ratio of the two is 1:1;

[0088] The disintegrant is a mixture of croscarmellose sodium, microcrystalline cellulose and low-substituted hydroxypropyl cellulose, and the mass ratio of the three is 1:3:2; agent, the croscarmellose sodium is an internal and external disintegrant (the mass ratio of the croscarmellose sodium and external disintegrant is 1:1), and the low-substituted hydroxypropyl cellulose Su is an internal disintegrant.

[0089] Atorvastatin calcium tablets are prepared by the following method:

[009...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, in particular to an atorvastatin calcium tablet and a preparation process thereof. The atorvastatin calcium tablet comprises the following components in parts by weight: 5-15 parts of atorvastatin calcium, 40-70 parts of filler, 1-5 parts of binder, 20-35 parts of disintegrant, 1-5 parts of lubricant, 3-8 parts of auxiliary agent. The invention has the advantages of good dispersibility, high disintegration rate and dissolution rate, and excellent stability of related substances.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an atorvastatin calcium tablet and a preparation process 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 At the same time, the levels of high-density lipoprotein choleste...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/40A61K47/40A61K47/38A61K47/10A61K47/32A61P3/06
CPCA61K9/2027A61K9/2031A61K9/205A61K9/2054A61K31/40A61P3/06
Inventor 吴志红林明聪
Owner 福建东瑞制药有限公司
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