Slow-release tablet of simvastatin and nicotinic acid and preparation method thereof

A technology for simvastatin and sustained-release tablets, which is applied in the field of compound simvastatin niacin sustained-release tablets and its preparation, can solve problems such as lowering TG, lowering LDL, and raising HDL-C, so as to reduce the number of times of taking medicine, reduce Toxic side effects, blood lipid level improvement effect

Inactive Publication Date: 2010-06-16
HARBIN PHARMA GROUP BIOLOGICAL ENG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] From the point of view of the mechanism of action, niacin affects the synthesis of cholesterol by inhibiting the synthesis of low-density lipoprotein. In large doses, it can increase HDL and lower TG, which has a significant effect, and at the same time has a slight effect of lowering LDL; Too high, often hepatotoxic
Simvastatin is an HMG-CoA reductase inhibitor, which competitively inhibits endogenous cholesterol synthesis rate-limiting enzyme HMG-CoA reductant, blocks intracellular mevalonate metabolic pathway, reduces intracellular cholesterol synthesis, and thus feeds back Sexual stimulation increases the number and activity of LDL receptors on the surface of cell membranes (mainly liver cells), which increases serum cholesterol clearance and significantly reduces LDL, but the effect of increasing HDL-C is weak

Method used

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  • Slow-release tablet of simvastatin and nicotinic acid and preparation method thereof
  • Slow-release tablet of simvastatin and nicotinic acid and preparation method thereof
  • Slow-release tablet of simvastatin and nicotinic acid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1. Simvastatin chip

[0027] Simvastatin 10g

[0028] Carboxymethyl Starch Sodium 10g

[0029] 20g pregelatinized starch

[0030] Microcrystalline Cellulose 30g

[0031] tert-butylhydroxyanisole 0.02g

[0032] Magnesium stearate 0.5g

[0033] 80% ethanol appropriate amount

[0034]

[0035] Makes 1000 pieces

[0036] 2. Niacin sustained-release layer

[0037] Niacin 500g

[0038] Hypromellose K 4 MCR 70g

[0039] Lactose 30g

[0040] Magnesium Stearate 4g

[0041] 60% ethanol appropriate amount

[0042]

[0043] Makes 1000 pieces

[0044] The preparation method of simvastatin immediate-release granules is:

[0045] Pass simvastatin through a 100-mesh sieve, and other auxiliary materials through a 80-mesh sieve, and set aside. Weigh simvastatin, carboxymethyl starch sodium, pregelatinized starch, microcrystalline cellulose, tert-butyl hydroxyanisole according to the prescription amount, first mix t...

Embodiment 2

[0049] 1. Simvastatin chip

[0050] Simvastatin 20g

[0051] Carboxymethyl Starch Sodium 10g

[0052] 20g pregelatinized starch

[0053] Microcrystalline Cellulose 30g

[0054] tert-butylhydroxyanisole 0.04g

[0055] Magnesium stearate 0.5g

[0056] 80% ethanol appropriate amount

[0057]

[0058] Makes 1000 pieces

[0059] 2. Niacin sustained-release layer

[0060] Niacin 750g

[0061] Hypromellose K 4 MCR 83g

[0062]Lactose 40g

[0063] Magnesium Stearate 4g

[0064]

[0065] 80% ethanol appropriate amount

[0066] Makes 1000 pieces

[0067] Embodiment 2 preparation method is the same as embodiment 1.

Embodiment 3

[0069] 1. Simvastatin chip

[0070] Simvastatin 10g

[0071] Carboxymethyl Starch Sodium 10g

[0072] 20g pregelatinized starch

[0073] Microcrystalline Cellulose 30g

[0074] tert-butylhydroxyanisole 0.02g

[0075] Magnesium stearate 0.5g

[0076] 80% ethanol appropriate amount

[0077]

[0078] Makes 1000 pieces

[0079] 2. Niacin sustained-release layer

[0080] Niacin 1000g

[0081] Hypromellose K 4 MCR 95g

[0082] Lactose 46g

[0083] Magnesium Stearate 6g

[0084]

[0085] 80% ethanol appropriate amount

[0086] Makes 1000 pieces

[0087] Embodiment 3 preparation method is the same as embodiment 1.

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Abstract

The invention provides a compound slow-release tablet of simvastatin and nicotinic acid and a preparation method thereof. The method prepares the slow-release nicotinic acid and the simvastatin into a compound tablet for the first time. In the compound tablet, each tablet contains 250-2000mg of nicotinic acid and 5-50mg of simvastatin. The compound tablet is prepared by the following steps: preparing a simvastatin quick-release tablet and preparing the compound slow-release tablet of the simvastatin and the nicotinic acid. The compound nicotinic acid slow-release tablet prepared by the method is suitable for the treatment of primary hypercholesteremia and mixed type blood lipid abnormality, takes the nicotinic acid as a slow-release part and the simvastatin as a quick-release part according to the respective properties, prepares a compound preparation, enables each component to exert a synergistic action in vivo, exerts the medicine effect furthest, can lower the side effect of the medicine, reduces the fluctuation of the blood concentration in vivo, reduces the administration frequency of a patient and has more obvious curative effect for relieving the hypercholesteremia in comparison with that of a method which only takes any one single-prescription preparation.

Description

technical field [0001] The invention relates to a compound simvastatin nicotinic acid sustained-release tablet and a preparation method thereof, belonging to the field of pharmaceutical preparations. technical background [0002] Primary hypercholesterolemia and mixed dyslipidemia is a common and frequently-occurring disease in clinic. Currently, the drugs for treating hyperlipidemia mainly include statins, fibrates and others. Statins can only raise high-density lipoprotein cholesterol (HDL-C) to a limited extent and lower triglycerides (TG) to a limited extent. Statins alone cannot achieve this goal for many patients with dyslipidemia, especially those with mixed dyslipidemia. Adequate lipid therapy targets. Niacin can significantly improve all major blood lipid components and restore them to normal. It is the only approved drug for lowering lipoprotein (a) Lp(a) and the most effective drug for raising HDL-C. However, due to the side effects of flushing and hepatotoxicit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/366A61K31/455A61P3/06
Inventor 葛存慧赵华南冷国庆李会成陈玉军段志强
Owner HARBIN PHARMA GROUP BIOLOGICAL ENG
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