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Blood-fat-lowering simvastatin sustained-release tablet and preparation method thereof

A technology for simvastatin and sustained-release tablets, applied in the field of simvastatin sustained-release tablets and their preparation, can solve the problems of large fluctuation of blood drug concentration, short drug effect time, short half-life and the like, achieve delayed release, control of blood lipids, low cost effect

Inactive Publication Date: 2017-10-24
江苏黄河药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] But when simvastatin plays a therapeutic role, because the existing simvastatin dosage forms are common tablets or capsules, all of which are short-acting dosage forms, there are following defects when administering: due to the short half-life of the short-acting dosage forms, The drug has a short duration of action. In order to give full play to its therapeutic effect, it needs to be administered several times a day, which may easily cause large fluctuations in blood drug concentration, leading to side effects such as headache, tachycardia, palpitations, and dizziness.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A blood lipid-lowering simvastatin sustained-release tablet, consisting of a core containing simvastatin and a coating layer wrapped outside the core, the core comprising the following materials in parts by weight: 12 parts of simvastatin, tangerine 50 parts of carbide of leather;

[0036] The present invention also provides a preparation method of the simvastatin sustained-release tablet, comprising the following steps:

[0037] (1) Soak the orange peel in salt water for 40 minutes, dry it, and carbonize it in an inert gas to obtain a porous carbon material. The concentration of the salt water is 10 g / mL, and the carbonization temperature is 600 ° C. The time is 5 hours;

[0038] (2) Mix simvastatin, porous carbon material, polyethylene glycol, castor oil, magnesium stearate, microcrystalline cellulose, gum arabic, ascorbic acid, and sodium dehydroacetate evenly, granulate, dry, and tablet , made into a tablet core containing simvastatin;

[0039] (3) Add 5 parts of...

Embodiment 2

[0042] A blood lipid-lowering simvastatin sustained-release tablet, consisting of a tablet core containing simvastatin and a coating layer wrapped outside the tablet core, the tablet core includes the following materials in parts by weight: 10 parts of simvastatin, aloe 50 parts of carbides;

[0043] The simvastatin sustained-release tablet also contains the following substances: microcrystalline cellulose, preservatives, antioxidants;

[0044] The present invention also provides a preparation method of the simvastatin sustained-release tablet, comprising the following steps:

[0045] (1) Soak Aloe Vera in salt water for 30 minutes, after drying, carbonize in an inert gas to obtain a porous carbon material, the concentration of the salt water is 5g / mL, the carbonization temperature is 300°C, and the carbonization time for 4 hours;

[0046] (2) After mixing simvastatin, porous carbon material, polyethylene glycol, glycerin, magnesium stearate, talcum powder, starch, karaya gu...

Embodiment 3

[0050] A blood lipid-lowering simvastatin sustained-release tablet, which consists of a tablet core containing simvastatin and a coating layer wrapped outside the tablet core, and the tablet core includes the following materials in parts by weight: 8 parts of simvastatin, laver 80 parts of carbides;

[0051] The present invention also provides a preparation method of the simvastatin sustained-release tablet, comprising the following steps:

[0052] (1) Soak laver in salt water for 10 minutes, after drying, carbonize in an inert gas to obtain a porous carbon material, the concentration of the salt water is 15g / mL, the carbonization temperature is 700°C, and the carbonization time for 8 hours;

[0053] (2) Mix simvastatin, porous carbon material, polyvinylpyrrolidone, glycerin, micropowdered silica gel, sucrose, arabinogalactan, and butyl hydroxyanisole hydroperoxide evenly, granulate, dry, and tablet. into a tablet core containing simvastatin;

[0054] (3) Add 5 parts of hyd...

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Abstract

The invention relates to the technical field of simvastatin sustained-release tablets and preparation thereof and in particular relates to a blood-fat-lowering simvastatin sustained-release tablet and a preparation method thereof. The blood-fat-lowering simvastatin sustained-release tablet is composed of a tablet core containing simvastatin and a coating layer coated outside the tablet core, wherein the tablet core comprises the following substances in parts by weight: 8-20 parts of simvastatin and 30-80 parts of plant carbide. The sustained-release tablet disclosed by the invention has the delayed-release and peace-release effects. The method is simple in process, wide in source of raw materials and favorable for industrial production.

Description

technical field [0001] The invention relates to the technical field of simvastatin sustained-release tablets and preparation thereof, in particular to a blood lipid-lowering simvastatin sustained-release tablet and a preparation method thereof. Background technique [0002] Simvastatin is a reductase inhibitor of methylhydroxyglutaryl coenzyme A (HMG-COA), inhibits the synthesis of endogenous cholesterol, and is a blood lipid regulator. Literature data show that simvastatin has the content of reducing cholesterol (TC) in hyperlipidemic rabbit serum, liver and aorta, reducing very low-density lipoprotein cholesterol (VLDL-C) and low-density lipoprotein cholesterol (LDL-C). C) Effect of level. Simvastatin is highly selective to the liver after oral administration, and its concentration in the liver is significantly higher than that in other non-target tissues. Most of simvastatin is absorbed through the liver tissue and converted into the active metabolite β-hydroxy acid stru...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/36A61K9/32A61K31/366A61K47/46A61K47/38A61K47/10A61P3/06A61P9/10
CPCA61K9/0002A61K9/2068A61K9/2853A61K9/2866A61K31/366
Inventor 朱正标陶元明张汉华李苗苗范小雪
Owner 江苏黄河药业股份有限公司
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