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Niacin simvastatin sustained-release preparation and preparation method thereof

A sustained-release preparation and a technology of simvastatin, which are applied in the field of niacin-simvastatin sustained-release tablets and their preparation, can solve the problem that lovastatin does not have strong medicinal effect, increases density lipoprotein, cannot meet needs, etc. problems with reduced risk of side effects, good compressibility, and low incidence of hepatotoxicity and myopathy

Inactive Publication Date: 2009-09-02
YANGTAI PHARMA SHANDONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, what is disclosed therein is only the use of lovastatin as the immediate-release layer. The inventor has found through research that lovastatin does not have a strong drug effect when used in conjunction with niacin. According to the test, niacin+lovastatin The combined drugs of statins can only lower total cholesterol by 20.9%, lower density lipoprotein by 28.2%, lower triglyceride by only 23.8%, and raise density lipoprotein by only 23.8%. 23.5%, far lower than expected, and due to the defects in the structure of the double-layer tablet itself and its preparation process, the combined drug effect of the two is further reduced
Therefore, the drug cannot meet the needs of current medicine

Method used

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  • Niacin simvastatin sustained-release preparation and preparation method thereof
  • Niacin simvastatin sustained-release preparation and preparation method thereof
  • Niacin simvastatin sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation of embodiment 1. nicotinic acid (1000 consumptions)

[0054] prescription:

[0055] Niacin 500.0g

[0056] Microcrystalline Cellulose 50.0g

[0057] Pregelatinized starch 50.0g

[0058] 15% povidone K30 ethanol solution 150-250ml

[0059] Magnesium Stearate 6.0g

[0060] Preparation Process:

[0061] Weigh the prescribed amount of niacin, microcrystalline cellulose, and pregelatinized starch fully and evenly, add a binder to make a soft material, granulate, and dry at 50°C; for whole grains, add the prescribed amount of magnesium stearate to fully Mix well and compress into tablets.

[0062] Dissolution Determination:

[0063] According to the release assay method (the second method (two) of appendix X D of the Chinese Pharmacopoeia version in 2005), the first method device of the dissolution assay method is adopted, and 900ml of phosphate buffer (pH6.8) is used as solvent, and the rotating speed is 100 revolutions per minute,...

Embodiment 2

[0064] Embodiment 2. Preparation of Niacin Simvastatin Sustained-release Tablets (1000 Tablets Quantity)

[0065] Sustained release layer prescription:

[0066] Niacin 500.0g

[0067] Hypromellose K4MCR 75.0g

[0068] Hypromellose K100MCR 75.0g

[0069] Microcrystalline Cellulose 25.0g

[0070] 15% povidone K30 ethanol solution 150-250ml

[0071] Magnesium Stearate 6.0g

[0072] Film Coating Prescription:

[0073] Simvastatin 20.0g

[0074] Macrogol 6000 4.0g

[0075] Tween 80 2.0g

[0076] Gastric Opadry 20.0

[0077] 80% ethanol 400ml

[0078] Preparation Process:

[0079] Weigh the prescribed amount of niacin, microcrystalline cellulose, and hypromellose to be fully uniform, add a binder to make a soft material, granulate, and dry at 50°C; for whole granules, add the prescribed amount of magnesium stearate Mix well and press into tablets. Mix simvastatin and pharmaceutical auxiliary materials in proportion, prepa...

Embodiment 2～11

[0080] According to the release assay method (Chinese Pharmacopoeia version two appendix X D second method (two) method in 2005), the first method device of the dissolution assay method is adopted, with phosphate buffer (pH6.8) 900m as solvent, and the rotating speed is 100 revolutions per minute, operate according to the law. After 1, 3, 6, and 12 hours, accurately measure 10ml, filter, and take the subsequent filtrate to measure the release degree

[0081] The results showed that the nicotinic acid sustained-release tablets prepared with the ratio of niacin:hypromellose K4MCR:hypromellose K100MCR 100:15:15 had obvious sustained-release characteristics, and the drug release could last for 24 hours. This simvastatin has reached quick-release effect in 1 hour.

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Abstract

The invention relates to a niacin simvastatin slow-release preparation and a preparation method thereof. The slow-release preparation adopts the form of tablets, wherein a slow-release part of the preparation comprises simvastatin and pharmaceutical excipients, and a quick-release part of the preparation is taken as a coating to wrap a niacin slow-release part. Through a slow release technique, niacin is slowly released so as to reduce the toxic-side effects of the niacin. Meanwhile, after a coating technique is adopted, quick-release coating is performed, the quick-release part is good in 60-minute dissolution; and a slow-release layer forms gel which is released layer by layer and is insensitive to moisture, temperature and the like, so the quick-release coating has no obvious influence on the slow release of the niacin, and the synergy of the niacin and the simvastatin can reach optimum.

Description

technical field [0001] The invention relates to a nicotinic acid simvastatin sustained-release tablet and a preparation method thereof, belonging to the field of chemical pharmaceutical preparations. Background technique [0002] Niacin is one of the B vitamins, and it is collectively referred to as "vitamin PP" together with nicotinamide. The drug began to be used against pellagra at the beginning of this century. In 1955, it was discovered that it has the effect of lowering blood lipids. Taking large doses of niacin in humans can lower plasma cholesterol, so niacin is used as a drug for lowering blood lipids. [0003] The mechanism of action of niacin in lowering blood lipids is: niacin can not only inhibit the synthesis of very low-density lipoprotein (LDL), but also promote the decomposition of very low-density lipoprotein (VLDL), so that plasma very low-density lipoprotein (VLDL) Significantly decreased, and its transformant intermediate density lipoprotein (IDL) and ...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/366A61P3/06
Inventor 王海孟勇涛毛德香李铁军
Owner YANGTAI PHARMA SHANDONG
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