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A kind of aprepitant nano preparation and preparation method thereof

A prepitant and nano-preparation technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of uneven particle size distribution, large equipment loss, and long time required and other problems, to achieve the effects of simple production process, improved dissolution performance, and mild process conditions

Active Publication Date: 2021-07-13
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For example, in Chinese patent documents with publication numbers CN108030924A, CN107198690A, and CN107007568A, it is disclosed that aprepitant powder is prepared by grinding method, resulting in uneven particle size distribution; large equipment loss; long time required, which is not conducive to large-scale production
[0008] In the Chinese patent of CN102525880A, the aprepitant solid dispersion is prepared by hot-melt extrusion method, but the preparation process has a great influence on the stability of the drug, and the dissolution effect is not ideal from the published literature

Method used

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  • A kind of aprepitant nano preparation and preparation method thereof
  • A kind of aprepitant nano preparation and preparation method thereof
  • A kind of aprepitant nano preparation and preparation method thereof

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preparation example Construction

[0054] The preparation method of above-mentioned a kind of aprepitant nano-preparation of the present invention, comprises the following steps:

[0055] The drug solution is added to the aqueous solution containing auxiliary materials, and the aprepitant nano-preparation is prepared by combining the liquid phase precipitation technology with the spray drying technology.

[0056] According to some embodiments of the present invention, a preparation method of aprepitant nano-preparation comprises the following specific steps:

[0057] S1, dissolving aprepitant in a water-miscible organic solvent to prepare an aprepitant solution;

[0058] S2. Dissolving part of the water-soluble auxiliary materials in water to form a transparent aqueous solution; the mass ratio of aprepitant to the auxiliary materials used in this step is 1:0.5-4; if the auxiliary materials used in this step are surface active agent, then the surfactant quality is 1%-5% of the aprepitant quality;

[0059] S3, ...

Embodiment 1

[0072] A kind of aprepitant oral nano preparation, comprising the following components:

[0073] Aprepitant 300mg, excipients 635mg;

[0074] Wherein, the auxiliary materials include 500 mg of water-soluble vitamin E, 35 mg of hydroxypropyl methylcellulose, and 100 mg of microcrystalline cellulose, and the average particle size of the particles is 200 nm, and the aprepitant nanoparticles are coated with auxiliary material particles.

[0075] A preparation method of aprepitant oral nano-preparation, the steps are as follows:

[0076] S1, aprepitant bulk drug (scanning electron microscope picture as shown in figure 1 Shown) and acetone are made into the aprepitant acetone solution 20mL that concentration is 15mg / mL;

[0077] S2, water-soluble vitamin E and deionized water are made into 400mL of water-soluble vitamin E aqueous solution of 1.5mg / mL, add 35mg hydroxypropyl methylcellulose to aqueous solution simultaneously, obtain mixed liquor; The repitant acetone solution is p...

Embodiment 2

[0105] A kind of aprepitant oral nano preparation, comprising the following components:

[0106] Aprepitant 800mg, excipients 2600mg;

[0107] Wherein, the auxiliary materials include 1600 mg of polyvinylpyrrolidone, 200 mg of hypromellose and 800 mg of lactose monohydrate, the average particle diameter of the aprepitant nanoparticles is 300 nm, and the outer coating of the aprepitant nanoparticles is the auxiliary material particles.

[0108] A preparation method of aprepitant oral nano-preparation, the steps are as follows:

[0109] S1, the aprepitant bulk drug and dimethyl sulfoxide were made into 20 mL of aprepitant dimethyl sulfoxide solution with a concentration of 40 mg / mL;

[0110] S2, polyvinylpyrrolidone and deionized water are made into 400mL of polyvinylpyrrolidone aqueous solution of 4mg / mL;

[0111] S3. Open the internal circulation supergravity rotating packed bed, add the aprepitant dimethyl sulfoxide solution obtained in step S1 at a speed of 10mL / min, and t...

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Abstract

The invention discloses an aprepitant nano-formulation and a preparation method thereof. The aprepitant nano-formulation includes aprepitant and auxiliary materials; it is characterized in that, in parts by mass, the aprepitant 5-40 parts, 40-120 parts of auxiliary materials, the particle size of the aprepitant is less than or equal to 300nm, and the aprepitant nanoparticles are coated with auxiliary material particles. The dissolution performance of the preparation of the invention is greatly improved, and the dissolution rate of the drug in 15 minutes reaches 91%-94%; the permeability of the drug is also greatly improved, thereby improving its bioavailability; and the preparation method has a simple production process and can Mass production does not require high temperature, high pressure, chemical reaction and other methods that are easy to destroy pharmaceutical ingredients, and the process conditions are mild, which is conducive to industrialization.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an aprepitant nano-preparation and a preparation method thereof. Background technique [0002] Aprepitant (Aprepitant) is the first NK1 receptor antagonist approved by the FDA. It was developed by Merck, and its trade name is Emend. It is used for the treatment of acute or delayed nausea and vomiting caused by chemotherapy. At present, the drug has been approved for marketing in most countries around the world. [0003] Aprepitant chemical name: 5-[[(2R,3S)-2-[(1R)-1-[3,5-di(trifluoromethyl)phenyl]ethoxy]-3-(4 -fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one. Its molecular formula is C 23 h 21 f 7 N 4 o 3 , the relative molecular mass is 534.43, and the structural formula is as follows: [0004] [0005] Because aprepitant is almost insoluble in water, it belongs to Class IV drugs in the classification of biopharmaceuticals, t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/48A61K31/5377A61K47/38A61K47/22A61K47/32A61K47/26A61K47/36A61K47/20A61P1/08
CPCA61K9/0053A61K9/4858A61K9/4866A61K31/5377A61P1/08
Inventor 乐园李兴亚
Owner BEIJING UNIV OF CHEM TECH