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Atorvastatin calcium tablet and preparation method thereof

A technology of atorvastatin calcium and calcium carbonate, applied in the field of medicine, can solve the problems of poor water solubility, easy degradation, and limited formulation development.

Inactive Publication Date: 2016-12-07
YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, atorvastatin calcium has special physical and chemical properties, its water solubility is poor, and it is relatively sensitive under high temperature, high humidity and light conditions; especially in acidic environment, it is easy to degrade into the corresponding lactone
The above characteristics make the storage and use of atorvastatin calcium very difficult, and also severely limit the development of related preparations

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

[0017] Embodiment 1 The preparation of atorvastatin calcium tablet of the present invention

[0018] Prescription Components and Functions of Atorvastatin Calcium Tablets

[0019]

[0020] Preparation Process:

[0021] 1. Take each raw and auxiliary material according to the prescription, and pass through a 100-mesh sieve;

[0022] 2. Preparation of adhesive: prepare an adhesive solution containing 2.4% w / w of Tween-80 and 3.0% w / w of highly substituted hydroxypropyl cellulose (viscosity range 6.0-10.0mpa.s);

[0023] 3. Mixing of raw and auxiliary materials: put microcrystalline cellulose pH101, atorvastatin calcium, internally added croscarmellose sodium, calcium carbonate, and lactose into the wet mixing granulator in sequence, and mix well;

[0024] 4. Granulation: put in binder solution, prepare soft material, and pass the soft material through a 20-mesh sieve;

[0025] 5. Drying: Put the wet granules in an oven and dry at 40°C to 60°C;

[0026] 6. Final blending o...

experiment example 1

[0030] Experimental Example 1 Atorvastatin Calcium Tablets Prepared According to Different Amounts of Raw Materials

[0031] Table 1 Prescription of Atorvastatin Calcium Tablets

[0032]

[0033] Prepare the tablets of prescriptions 1 to 6 according to the following process:

[0034] The above-mentioned prescription sieves atorvastatin calcium and other auxiliary materials for standby;

[0035] Precisely weigh the raw and auxiliary materials of each prescription, first mix the auxiliary materials except the main drug, and then deliver them in equal amounts.

[0036] Addition method mixes a small amount of the main ingredient and the premixed auxiliary materials evenly;

[0037] Put the mixed material in an appropriate container, add Tween-80-HPC solution, and granulate;

[0038] The wet granules were dried in a blast drying oven at 50°C;

[0039] After the dry granules are sized, an appropriate amount of croscarmellose sodium is added, mixed evenly, and magnesium steara...

experiment example 2

[0049] Experimental Example 2 Preparation of Atorvastatin Calcium Tablets Using Different Process Conditions

[0050] Atorvastatin calcium tablets were prepared according to the prescription and process of Example 1, and the two key process parameters of raw material micronization and granule drying temperature were investigated.

[0051] Table 3 Comparison of process conditions

[0052]

[0053] Table 4 Comparison of quality test results of atorvastatin calcium tablets prepared under different process conditions

[0054]

[0055] After micronizing atorvastatin calcium, its particle size distribution is as follows: D(v, 0.10) 0.355μm, D(v, 0.50) 2.014μm, D(v, 0.90) 11.147μm, that is, the atorvastatin calcium used in this project The particle size of statin calcium raw materials is about 1300 mesh. Comparing prescriptions 7 and 8: the micronization of raw materials is beneficial to the dissolution of the drug (atorvastatin calcium, which belongs to BCS class II).

[00...

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Abstract

The invention discloses an atorvastatin calcium tablet, which is prepared from the following raw and auxiliary materials in the weight ratio: 10-20 parts of atorvastatin calcium, 30-72 parts of calcium carbonate, microcrystalline cellulose pH 101 54-108 parts, 30-72 parts of lactose, 9-20.4 parts of croscarmellose sodium, 0.45-1.5 parts of polysorbate 80, 1.5-3 parts of high-substituted hydroxypropyl cellulose, 0.75 parts of magnesium stearate ~1.5 parts, Opadry YS‑1‑70404.5~15 parts. The inventor has fully considered the drug quality of atorvastatin calcium tablets and the simplicity of the production process, using a safe dose of alkaline pH agent calcium carbonate as a stabilizer, high-substituted hydroxypropyl cellulose aqueous solution as a binder, and wet granulation .

Description

technical field [0001] The invention relates to an atorvastatin calcium tablet and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Atorvastatin is a novel β-hydroxy-β-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor for the treatment of hypercholesterolemia and coronary heart disease or the combination of predisposing factors such as coronary heart disease Patients with hypercholesterolemia or mixed dyslipidemia. It reduces plasma cholesterol and serum lipoprotein concentrations by inhibiting the synthesis of HMG-CoA reductase and cholesterol in the liver, and enhances the uptake and metabolism of LDL by increasing the number of hepatic low-density lipoprotein (LDL) receptors on the cell surface. Compared with other statin drugs, atorvastatin calcium tablets have a stronger inhibitory effect on HMG-CoA reductase, and have a wide range of indications; at the same time, the drug has the largest effect on reducing liver lo...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/40A61K47/04A61K47/38A61K47/26A61K47/12A61P3/06A61P9/10
CPCA61K9/2009A61K9/2013A61K9/2018A61K9/2054A61K9/2866A61K31/40
Inventor 黄兴悦罗敏袁瑜李元波谭琨岭戴媚何晓王颖
Owner YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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