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Simvastatin slow-release tablet and preparation method thereof

A technology for simvastatin and sustained-release tablets, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, and medical preparations containing active ingredients. Speed ​​and other issues, to achieve the effect of reducing the number of times of taking, not easy to pollute, and reducing fluctuations

Inactive Publication Date: 2009-12-02
JIAOZUO XIANDA TRADE
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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 preparations, they are all short-acting dosage forms, and there are following defects when administering: due to the short half-life of the short-acting dosage forms, the drug effect time is short , in order to give full play to its therapeutic effect, it needs to be administered several times a day, which is likely to 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

[0024] Embodiment 1: simvastatin sustained-release tablet as described in the present invention,

[0025] The formulations of the drug-loaded tablet cores are listed below:

[0026] Raw material amount

[0027] Simvastatin 10g

[0028] 80g pregelatinized starch

[0029] Starch 40g

[0030] Microcrystalline Cellulose 10g

[0031] 10% starch slurry 50g

[0032] The preparation method is as follows:

[0033] (1) Grinding, take 10g of simvastatin, and pulverize the taken simvastatin to 80 mesh with a pulverizer;

[0034] (2) sieve powder, get pregelatinized starch 80g, starch 40g and microcrystalline cellulose 10g and cross 80 mesh sieves for subsequent use respectively;

[0035] (3) Add the ground simvastatin and sieved pregelatinized starch, starch and 50g10% starch slurry into the one-step granulator, control the air pressure in the one-step boiling granulator to more than 0.4MPa, and pump the The rotation speed is 160 rpm, the air inlet temperature is 100°C, the outlet...

Embodiment 2

[0039] Embodiment 2: simvastatin sustained-release tablet as described in the present invention,

[0040] The formulations of the drug-loaded tablet cores are listed below:

[0041] Raw material amount

[0042] Simvastatin 7g

[0043] 60g pregelatinized starch

[0044] Starch 40g

[0045] Lactose 10g

[0046] Microcrystalline Cellulose 10g

[0047] Distilled water 40g

[0048] The preparation method is as follows:

[0049] (1) Grinding, take 7g of simvastatin and 10g of lactose, and pulverize the taken simvastatin and lactose to 80 mesh with a pulverizer;

[0050] (2) sieve powder, get pregelatinized starch 60g, starch 40g and microcrystalline cellulose 10g and cross 80 mesh sieves for subsequent use respectively;

[0051] (3) Add the ground simvastatin, lactose, sieved pregelatinized starch, starch and 40g of distilled water into the one-step granulator, control the air pressure in the one-step boiling granulator to above 0.5MPa, and the pump speed The temperature is 1...

Embodiment 3

[0055] Embodiment 3: simvastatin sustained-release tablet as described in the present invention,

[0056] The formulations of the drug-loaded tablet cores are listed below:

[0057] Raw material amount

[0058] Simvastatin 13g

[0059] 65g pregelatinized starch

[0060] Starch 50g

[0061] Dextrin 10g

[0062] Microcrystalline Cellulose 15g

[0063] Ethanol 60g

[0064] The preparation method is as follows:

[0065] (1) Grinding, get simvastatin 10g and dextrin 10g, pulverize the taken simvastatin and dextrin to 80 mesh with a pulverizer;

[0066] (2) sieve powder, get pregelatinized starch 65g, starch 50g and microcrystalline cellulose 15g and cross 80 mesh sieves for subsequent use respectively;

[0067] (3) Add the ground simvastatin, dextrin, sieved pregelatinized starch, starch and 60g ethanol to the one-step granulator, control the air pressure in the one-step boiling granulator to above 0.6MPa, and the pump The rotation speed is 200 rpm, the inlet air temperatu...

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PUM

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Abstract

The invention provides a simvastatin slow-release tablet and a preparation method thereof. The simvastatin slow-release tablet comprises a medicine-carrying tablet core and a coating layer coated outside the medicine-carrying tablet core, wherein the medicine-carrying tablet core comprises the following raw materials according to parts by weight: 7-13 parts of simvastatin, 120-140 parts of filler and 40-60 parts of adhesive; the existing short-acting simvastatin tablet is prepared into a coating type slow-release preparation form which controls the diffusion and dissolution of a medicine so as to delay the release of the medicine; after the medicine enters a human body, the coating layer slowly dissolves, so that the medicine is stably and durably released, the blood concentration is kept in a more stable effective state for a long time, the defect of large fluctuation of the effective blood concentration caused by the overlarge fluctuation of the blood concentration existing in the frequent administration of a conventional preparation form is avoided, and the toxic or side effect is reduced; and the simvastatin slow-release tablet is prepared in a closed one-step boiling granulator, thereby being hardly polluted, the quality of a finished product can be better guaranteed, and automatic control is convenient.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and relates to a chemical drug, in particular to a simvastatin sustained-release tablet and a preparation method of the sustained-release tablet. 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 levels. 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 str...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/366A61K47/36A61K47/38A61K47/40A61P3/06
Inventor 陈勇梅拥军杨军强
Owner JIAOZUO XIANDA TRADE
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