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Simvastatin nano suspension and preparation method thereof

A nano-suspension, simvastatin technology, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. narrow range, etc.

Inactive Publication Date: 2015-05-06
SHANGHAI SINE PHARMA LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The precipitation method has limited its use due to the need to screen suitable organic solvents, difficult process control, and organic solvent residues; the high-pressure homogenization method avoids the addition of organic solvents, but its homogenization cycle is long, equipment energy consumption is high, and it is easy to The disadvantages such as wear and tear are not widely used in industry; the grinding method has a wide range of applications, the prepared nanoparticles have a small particle size, narrow distribution range, simple preparation process, and easy large-scale industrial production, so there is a lot of room for development

Method used

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  • Simvastatin nano suspension and preparation method thereof

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preparation example Construction

[0049] Another aspect of the present invention provides a method for preparing the simvastatin nanosuspension of the present invention, the method comprising the following steps:

[0050] (1) Crush 1 part by weight of simvastatin;

[0051] (2) Dissolving 0.5-20 parts by weight of stabilizer in a solvent, and adding the simvastatin obtained in step (1) to obtain a suspension;

[0052] (3) Grind the suspension obtained in step (2) to obtain a nanosuspension,

[0053] The stabilizer is selected from lecithin, poloxamer 188, sodium lauryl sulfate, hydroxypropyl cellulose, hypromellose, polyvinylpyrrolidone, docusate sodium, and combinations thereof.

[0054] In the present invention, the pulverization step is conventional. A person of ordinary skill in the art can directly determine how to perform the pulverization step based on the description of the present invention combined with the prior art. In a preferred embodiment of the present invention, the pulverization step includes jet pulv...

Embodiment 1

[0083] Weigh PVP-K901.5g and SDS0.5g into 100ml of distilled water, dissolve it completely by ultrasound, slowly add 0.5g of simvastatin crushed by airflow under magnetic stirring, and cut for 5 minutes with a high-speed shearing machine at 10000rpm. Get the initial suspension. Then pour the initial suspension into the feed hopper for grinding. The grinding conditions are as follows: the particle size of the zirconia beads is 0.1 mm, the amount of zirconia beads is 60 ml, and the rotation speed is 3000 rpm. A sample was taken 20 minutes later, and the measured particle size was 286.6 nm and the potential was -28.5 mv.

Embodiment 2

[0085] Weigh 1.0g of HPMC and 0.5g of SDS into 100ml of distilled water, dissolve it completely by ultrasound, slowly add 0.5g of simvastatin crushed by airflow under magnetic stirring, and cut with a high-speed shearing machine at 10000rpm for 5 minutes. Suspension. Then pour the initial suspension into the feed hopper for grinding. The grinding conditions are as follows: the particle size of the zirconia beads is 0.1 mm, the amount of zirconia beads is 60 ml, and the rotation speed is 3000 rpm. A sample was taken after 20 minutes, and the particle size was 309.5 nm and the potential was -30.2 mv.

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Abstract

The invention relates to a simvastatin nano suspension and a preparation method thereof. The simvastatin nano suspension comprises the following components: 1 weight part of simvastatin and 0.5-20 weight parts of stabilizing agent; wherein the stabilizing agent is selected from lecithin, Poloxamer 188, sodium dodecyl sulfate, hydroxy propyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, docusate sodium and its combination.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of a simvastatin nano suspension and a spray-dried composition thereof. Background technique [0002] Simvastatin (SV) is a methylhydroxyglutaryl-coenzyme A (HMG-CoA) reductase inhibitor. It has a good effect on hyperlipidemia and coronary heart disease with few adverse reactions. It is currently the first choice among blood lipid regulating drugs. drug. The clinically used dosage forms are mainly tablets, capsules, dispersible tablets and dripping pills. However, simvastatin is almost insoluble in water, has poor oral absorption and low bioavailability. The use of solid dispersion, cyclodextrin inclusion compound, nanoparticle and self-microemulsion technology to improve its bioavailability has been reported. However, these drug delivery systems have their own shortcomings, which limit the industrialization prospects of preparations. Therefore, it i...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/24A61K47/34A61K47/20A61K47/38A61K47/32A61K31/366A61P3/06A61P9/10
Inventor 唐文燕廉云飞张军东曾泷彪季秀峰
Owner SHANGHAI SINE PHARMA LAB
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