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Core-coated tablet for treating hypercholesteremia

A chip-packed technology for hypercholesterolemia, which is applied in the field of medicine and can solve problems such as the instability of atorvastatin calcium raw materials

Active Publication Date: 2022-01-11
SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The key issue in the development of atorvastatin calcium tablets is stability. The raw material of atorvastatin calcium is unstable and needs to maintain stability in an alkaline environment, and is sensitive to various factors such as oxidation, light, high temperature and high humidity. , prone to degradation impurities

Method used

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  • Core-coated tablet for treating hypercholesteremia
  • Core-coated tablet for treating hypercholesteremia
  • Core-coated tablet for treating hypercholesteremia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 1. Preparation of Atorvastatin Calcium Granules

[0023] The prescription consists of:

[0024] Atorvastatin Calcium 10g (calculated as atorvastatin) calcium carbonate 33g microcrystalline cellulose 30g lactose monohydrate 16g Tween 80 0.5g Hypromellose 2g Crospovidone 6g purified water Appropriate amount Magnesium stearate 1g Opadry 03k28487 3g production 1000 pieces

[0025] Preparation:

[0026] (1) Weigh Tween 80, prepare a 1% (W / W) solution with purified water, and stir until completely dissolved; (2) Granulation: add microcrystalline cellulose, Lactose, croscarmellose sodium, hydroxypropyl cellulose, atorvastatin calcium and calcium carbonate were mixed for 10 minutes; (3) adding the Tween 80 aqueous solution prepared in step (1), stirring and chopping (4) put the wet granules into the fluidized dryer and dry until the granule moisture is 1.0%-3.0%; Sieve for sizing, and collect the g...

Embodiment 3

[0035] 1. Preparation of atorvastatin calcium inner chip

[0036] The prescription consists of:

[0037]

[0038]

[0039] Preparation:

[0040] (1) Weigh Tween 80, prepare a 1% (W / W) solution with purified water, and stir until completely dissolved; (2) Granulation: add microcrystalline cellulose, Lactose, croscarmellose sodium, hydroxypropyl cellulose, atorvastatin calcium and calcium carbonate were mixed for 10 minutes; (3) adding the Tween 80 aqueous solution prepared in step (1), stirring and chopping (4) put the wet granules into the fluidized dryer and dry until the granule moisture is 1.0%-3.0%; Sieve for sizing, and collect the granules after sizing; (6) Add the granules and magnesium stearate in step (2), mix them with a three-dimensional mixer, discharge, and collect the mixed granules. (7) Tablet pressing: use a rotary tablet press machine, Round dimpled die-pressed tablet.

[0041] 2. Preparation of outer layer granules containing ezetimibe

[0042] Th...

Embodiment 4

[0049] After removing the packages of the packaged chips prepared in the above examples, they were placed at 60° C. for 15 days for investigation to measure the impurities. In addition, each embodiment was taken to make a coated chip, and the dissolution rate was measured respectively (0.3% sodium lauryl sulfate, pH4.5 acetate buffer, paddle method, 50 rpm, volume 900ml, sampling in 30 minutes). The results are shown in the table below.

[0050]

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Abstract

The invention discloses a core-coated tablet for treating hypercholesteremia and a preparation method thereof. The core-coated tablet is prepared by pressing an inner-layer core and outer-layer particles by a core-coated tablet press, the core-coated tablet contains effective components of ezetimibe and atorvastatin calcium, the inner-layer core is prepared by tabletting and coating atorvastatin calcium particles, and the outer-layer particles are prepared from ezetimibe, a filling agent, a disintegrating agent, an adhesive, a solubilizer and a lubricating agent. The core-coated tablet not only can solve the problem of convenient taking, but also can effectively avoid the interaction of the two main components and maintain the stability of the product.

Description

technical field [0001] The invention relates to an ezetimibe atorvastatin calcium tablet and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Ezetimibe Atorvastatin Calcium Tablets is a compound preparation, which is mainly used to reduce the level of total cholesterol (low-density lipoprotein cholesterol and triglyceride) and can increase the level of high-density lipoprotein cholesterol. It was developed by Merck of the United States The compound lipid-lowering drug, whose trade name is "LIPTRZET", was approved by the FDA on May 3, 2013. The compound preparation generally adopts two active ingredients in a single solid dosage form as separate entities, that is, a bilayer tablet. The two active ingredients have different action mechanisms, and when they are made into a compound formula, they have better curative effect and patient adaptability, and have broad market prospects. [0003] But unexpectedly, in the proce...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K47/38A61K47/26A61K47/32A61K31/40A61P3/06A61K31/397
CPCA61K9/209A61K9/2095A61K9/2018A61K9/2054A61K9/2027A61K31/40A61K31/397A61P3/06A61K2300/00
Inventor 张岱州李大伟刘正平陈倩倩纪红英毛楷凡赵仁永渠广民王丽丽林振广
Owner SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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