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Atorvastatin calcium tablet and preparation method thereof

A technology of atorvastatin calcium and calcium carbonate, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, pill delivery, etc., can solve the problems of atorvastatin calcium instability, affecting clinical efficacy, and poor water solubility. Achieve the effects of easy industrialization, short disintegration time and fast dissolution rate

Active Publication Date: 2013-02-13
HENAN RUNHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The clinical curative effect of atorvastatin calcium is definite, and the effect is remarkable, but the water solubility of this medicine is poor, and has strong bitter taste, is all sensitive to moisture, light, heat and low pH etc., especially can be degraded into Lactone
In order to overcome the defects of atorvastatin calcium, fillers, lubricants, stabilizers, disintegrants, binders and other substances are usually added to common atorvastatin calcium preparations on the market at present, but a large number of disintegrants It will cause instability of atorvastatin calcium in the preparation process and produce more related substances; less disintegrants will cause delayed disintegration and slow dissolution, which directly affects its clinical efficacy

Method used

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  • Atorvastatin calcium tablet and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0021] The atorvastatin calcium tablet of the present embodiment comprises the following components by mass: 7.22 parts of atorvastatin calcium, 22.01 parts of calcium carbonate, 21.87 parts of lactose, 40.67 parts of microcrystalline cellulose, and croscarmellose 6 parts of sodium cellulose, 1.33 parts of hydroxypropyl cellulose, 0.4 parts of polysorbate-800, and 0.5 parts of magnesium stearate.

[0022] The preparation method of the atorvastatin calcium tablet provided in this embodiment (tablet core weight 150mg, taking 1000 tablets as an example), comprises the following steps:

[0023] 1) Pass atorvastatin calcium through a 200-mesh sieve, pass lactose, microcrystalline cellulose, calcium carbonate, and croscarmellose sodium through a 80-mesh sieve, and set aside;

[0024] 2) Heat 10g of purified water to 50°C, add 0.6g of polysorbate-80, stir to dissolve completely, add 2.0g of hydroxypropyl cellulose (HPC-L), stir well, add 51g of purified water, and swell 4h, as an ad...

Embodiment 2

[0033] The atorvastatin calcium tablet of the present embodiment comprises the following components by mass: 7.22 parts of atorvastatin calcium, 22.01 parts of calcium carbonate, 21.87 parts of lactose, 40.67 parts of microcrystalline cellulose, and croscarmellose 6 parts of sodium cellulose, 1.33 parts of hydroxypropyl cellulose, 0.4 parts of polysorbate-800, and 0.5 parts of magnesium stearate.

[0034] The preparation method of the atorvastatin calcium tablet provided in this embodiment (tablet core weight 150mg, taking 1000 tablets as an example), comprises the following steps:

[0035] 1) Pass atorvastatin calcium through a 200-mesh sieve, pass lactose, microcrystalline cellulose, calcium carbonate, and croscarmellose sodium through a 80-mesh sieve, and set aside;

[0036] 2) Heat 12g of purified water to 50°C, add 0.6g of polysorbate-80, stir to dissolve completely, add 2.0g of hydroxypropyl cellulose (HPC-L), stir well, add 50g of purified water, and swell 5h, as an ad...

Embodiment 3

[0045] The atorvastatin calcium tablet of the present embodiment comprises the following components by mass: 7.22 parts of atorvastatin calcium, 22.01 parts of calcium carbonate, 21.87 parts of lactose, 40.67 parts of microcrystalline cellulose, and croscarmellose 6 parts of sodium cellulose, 1.33 parts of hydroxypropyl cellulose, 0.4 parts of polysorbate-800, and 0.5 parts of magnesium stearate.

[0046] The preparation method of the atorvastatin calcium tablet provided in this embodiment (tablet core weight 150mg, taking 1000 tablets as an example), comprises the following steps:

[0047] 1) Pass atorvastatin calcium through a 200-mesh sieve, pass lactose, microcrystalline cellulose, calcium carbonate, and croscarmellose sodium through a 80-mesh sieve, and set aside;

[0048] 2) Heat 15g of purified water to 50°C, add 0.6g of polysorbate-80, stir to dissolve completely, add 2.0g of hydroxypropyl cellulose (HPC-L), stir well, add 55g of purified water, and swell 6h, as an ad...

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Abstract

The invention discloses an atorvastatin calcium tablet and a preparation method thereof. The tablet consists of the following components in parts by mass: 7.22 parts of main medicine atorvastatin calcium, 84.55 parts of filler, 6 parts of disintegrating agent croscarmellose sodium, 1.33 parts of adhesive hydroxy propyl cellulose, 800.4 parts of cosolvent polysorbate and 0.5 part of lubricating agent magnesium stearate, wherein the filler comprises the following raw materials in parts by mass: 22.01 parts of calcium carbonate, 21.87 parts of milk sugar and 40.67 parts of microcrystalline cellulose. The atorvastatin calcium tablet has the characteristics of short disintegrating time, fast dissolving-out speed, high bioavailability and small particle diameter, and is convenient to take. Furthermore, the hardness of the tablet can reach 60-70N, so that the tablet is hardly broken, and therefore, the packing and transporting costs are reduced, and the industrialized popularization of the tablet is easily realized.

Description

technical field [0001] The invention relates to an atorvastatin calcium tablet and a preparation method of the tablet, belonging to the field of western medicine preparations. Background technique [0002] Atorvastatin calcium, chemical name [R-(R',R')-2-(4-fluorophenyl)-β,β-dihydroxy-5-(1-methylethyl)-3-benzene Calcium-4-[(aniline)carbonyl]-1-hydro-pyrrole-1-heptanoate trihydrate, whose hydrolyzate competitively inhibits the rate-limiting enzyme hydroxymethylglutaryl-CoA during cholesterol synthesis in vivo Reductase, which reduces the synthesis of cholesterol and increases the synthesis of low-density lipoprotein receptors. The main site of action is in the liver. As a result, it reduces blood cholesterol and low-density lipoprotein cholesterol, moderately reduces serum triglyceride levels and increases blood HDL levels. [0003] Atorvastatin calcium tablets have a good effect on hypercholesterolemia and coronary heart disease. Treatment of total cholesterol in patients...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/40A61K47/38A61P3/06
Inventor 高志亮
Owner HENAN RUNHONG PHARMA
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