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Preparation method of simvastatin tablet

A technology of simvastatin and simvastatin tablets, which is applied in the field of preparation of simvastatin tablets, can solve the problems of dissolution rate and content uniformity, less bone tissue absorption, and poor oral absorption, etc., so as to improve bioavailability , The effect of increasing the relative absorption capacity and increasing the specific surface area

Inactive Publication Date: 2014-12-24
哈药集团人民同泰医药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Simvastatin is a white or off-white powder, sensitive to light, heat, water, oxygen, etc., and has low water solubility, which greatly affects the absorption of the drug in the body, resulting in poor oral absorption and low bioavailability, thus affecting Its clinical efficacy
After oral administration, simvastatin is mainly metabolized by the liver, and its bioavailability is greatly reduced due to the first-pass effect of the liver, and the bone tissue absorption will be less, which is far from reaching the dose required for bone formation
At the same time, the main drug content of simvastatin preparation is less, generally 5-40mg / tablet, so that the dissolution rate and content uniformity index of the product cannot reach the ideal value

Method used

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  • Preparation method of simvastatin tablet
  • Preparation method of simvastatin tablet
  • Preparation method of simvastatin tablet

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Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0020] Raw material ratio:

[0021]

[0022] Preparation:

[0023] 1. The simvastatin raw material and lactose are ultrafinely pulverized at low temperature at a weight ratio of 1:5 into micropowders with a diameter less than 10 μm, and set aside;

[0024] 2. Combine the above-mentioned micronized mixed material with acid protective agent (citric acid), antioxidant (tert-butylanisole), lactose, microcrystalline cellulose, and croscarmellose sodium remaining in the prescription amount, Mix evenly, put it in a wet mixing granulator, add appropriate amount of water, wet mix and granulate, boil and dry below 60°C, and control the water content of the granules to 1-5%;

[0025] 3. Whole the simvastatin granules, add the prescribed amount of magnesium stearate, mix well, and press into 1000 tablets.

Embodiment approach 2

[0027] Raw material ratio:

[0028]

[0029] The preparation method is the same as the specific embodiment one.

Embodiment approach 3

[0031] Raw material ratio:

[0032]

[0033] The preparation method is the same as the specific embodiment one.

[0034] The simvastatin sheet prepared by three embodiments and the commercially available simvastatin sheet, in vitro test characteristics are:

[0035]

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Abstract

The invention relates to a preparation method of a simvastatin tablet. The simvastatin tablet is composed of simvastatin, an acidic protecting agent, an antioxidant agent, a filling agent, a disintegrating agent and a lubricant. The preparation method disclosed by the invention comprises the following steps: carrying out low-temperature superfine grinding on a simvastatin raw material and lactose in a weight ratio of 1 to (1-10), so that the particle size is reduced and the specific surface area is increased, and then the raw material is changed from a lipophilic material into a hydrophilic material; uniformly mixing the obtained mixed material with the acidic protecting agent and the antioxidant agent, the rest of lactose, microcrystalline celluloses and crosslinked carboxymethyl cellulose sodium, granulating by using a wet method, and carrying out fluidized drying while controlling the water content of a finished product grains at 1-5%, so that the simvastatin tablet is prepared. The prescription process is simple and easy to control, and prepared preparation is good in content uniformity, high in dissolution rate, good in absorption, and high in bioavailability in comparison with other preparations. The preparation method of the simvastatin tablet disclosed by the invention is good in good in reproducibility, large in productivity, and stable and controllable in quality, and can effectively guarantee the effectiveness of drugs and the safety of drug application of patients.

Description

technical field [0001] The invention relates to a preparation method of a pharmaceutical preparation, in particular to a preparation method of simvastatin tablets. Background technique [0002] Simvastatin is a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, clinically used as a blood lipid regulating drug. Simvastatin itself is inactive, and its side chain structure has a part similar to hydroxymethylglutaryl coenzyme A (HMG-CoA). The hydrolyzate after oral absorption can competitively inhibit the rate-limiting cholesterol synthesis process in the body. The enzyme hydroxymethylglutaryl-CoA reductase reduces the synthesis of cholesterol and increases the synthesis of low-density lipoprotein receptors. As a result, blood cholesterol and low-density lipoprotein cholesterol levels are reduced, and serum triglyceride levels and serum triglyceride levels are moderately reduced. Increase the level of high-density lipoprotein in the blood, thus exerting an effect o...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/366A61K47/10A61K47/12A61K47/22A61P3/06A61P9/10
Inventor 秦雅英范宁张红梅董立财
Owner 哈药集团人民同泰医药股份有限公司
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