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High-stability simvastatin tablets and preparation method thereof

A technology for simvastatin and tableting, which is applied in the field of high-stability simvastatin tablets and their preparation technology, and can solve the problems of tablet stability, unstable chemical structure, and difficulty in quality control.

Active Publication Date: 2014-12-17
SHANGHAI SINE WANXIANG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Since the molecule of simvastatin contains lactone bonds, its chemical structure is unstable, which easily causes tablet stability problems. The traditional preparation method has many restrictions on the selection and dosage of excipients, and it is not easy to control the quality in production.
[0004] When the applicant produced simvastatin tablets in the early stage, it used two dry pressing methods, and the products produced met the standards of the second part of the 2005 edition of the Chinese Pharmacopoeia; however, the 2010 edition of the Chinese Pharmacopoeia newly stipulated that simvastatin The single impurity of the tablet shall not exceed 1%, and the total impurity shall not exceed 3%. The simvastatin tablet produced according to the old double dry pressing method cannot meet this requirement; therefore, after the inventor tried a variety of preparation processes, he developed a A tablet-making process that first uses powder coating technology to coat simvastatin raw materials, and then mixes excipients and dry-presses, so that the stability of simvastatin tablets complies with the new regulations of the second part of the 2010 edition of the Chinese Pharmacopoeia

Method used

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  • High-stability simvastatin tablets and preparation method thereof
  • High-stability simvastatin tablets and preparation method thereof
  • High-stability simvastatin tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] (1) Raw material coating

[0026] A. Take 50g of simvastatin crude drug and pass through a 45-mesh sieve, put it in the boiling coating machine, and turn it on for heating;

[0027] B. Get 50g copovidone S630, 2g butylhydroxyanisole and 500g absolute ethanol to prepare coating solution;

[0028] c. When the temperature of the material in the boiling coating machine reaches 35°C, start spraying liquid, and control the temperature of the material below 40°C during the entire coating process until all spraying is completed;

[0029] d. After the coating is finished, the material is passed through a 30-mesh sieve, and particles larger than 30 mesh are removed;

[0030] (2) Tablet

[0031] A. Get 200g microcrystalline cellulose, 650g lactose, 15g magnesium stearate, and 20g micropowder silica gel and pass through a 30-mesh sieve;

[0032] b. Mix the sieved auxiliary materials and coated raw materials evenly;

[0033] c. Tablet pressing to obtain 10,000 high-stability sim...

Embodiment 2

[0035] (1) Raw material coating

[0036] A. Take 100g of simvastatin crude drug and pass through a 45-mesh sieve, put it in the boiling coating machine, and turn it on for heating;

[0037] B. Get 100g copovidone S630, 4g butylhydroxyanisole and 1000g absolute ethanol to prepare coating solution;

[0038] c. When the temperature of the material in the boiling coating machine reaches 35°C, start spraying liquid, and control the temperature of the material below 40°C during the entire coating process until all spraying is completed;

[0039] d. After the coating is finished, the material is passed through a 30-mesh sieve, and particles larger than 30 mesh are removed;

[0040] (2) Tablet

[0041] A. Get 500g microcrystalline cellulose, 1300g lactose, 30g magnesium stearate, and 40g micropowder silica gel and pass through a 30-mesh sieve;

[0042] b. Mix the sieved auxiliary materials and coated raw materials evenly;

[0043] c. Tablet pressing to obtain 10,000 high-stability...

Embodiment 3

[0045] (1) Raw material coating

[0046] A. Take 200g of simvastatin crude drug and pass through a 45-mesh sieve, put it in the boiling coating machine, and turn it on for heating;

[0047] B. Get 100g copovidone S630, 4g butylhydroxyanisole and 1000g absolute ethanol to prepare coating solution;

[0048] c. When the temperature of the material in the boiling coating machine reaches 35°C, start spraying liquid, and control the temperature of the material below 40°C during the entire coating process until all spraying is completed;

[0049] d. After the coating is finished, the material is passed through a 30-mesh sieve, and particles larger than 30 mesh are removed;

[0050] (2) Tablet

[0051] A. Get 400g microcrystalline cellulose, 1300g lactose, 30g magnesium stearate, and 40g micropowder silica gel and pass through a 30-mesh sieve;

[0052] b. Mix the sieved auxiliary materials and coated raw materials evenly;

[0053] c. Tablet pressing to obtain 10,000 high-stability...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to high-stability simvastatin tablets and a preparation method thereof. The high-stability simvastatin tablets prepared by adopting a two-time dry-pressing method can be used for solving the problems that the simvastatin tablets in the prior art have relatively poor stability, and the requirements on the selection and the use amount of auxiliary materials are relatively high.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a high-stability simvastatin tablet and a preparation process thereof. Background technique [0002] Simvastatin is an HMG-CoA reductase inhibitor, a powerful lipid-lowering drug that can reduce low-density lipoprotein (LDL) by up to 50%, and its dose is 5 mg to 80 mg. Simvastatin appeared in the late 1980s, and now in many countries, simvastatin has become a generic preparation and is widely used in clinical practice as the first choice of statins. [0003] Since the molecule of simvastatin contains lactone bonds, its chemical structure is unstable, which easily causes tablet stability problems. The traditional preparation method has many restrictions on the selection and dosage of excipients, and it is not easy to control the quality in production. [0004] When the applicant produced simvastatin tablets in the early stage, it used two dry pressing methods, and the products p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/366A61K47/38A61P3/06
Inventor 顾煜吴福荣史红顾振洪卢小玲李婧
Owner SHANGHAI SINE WANXIANG PHARMA