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Preparation method of high stability aprepitant composition

A high-stability technology of aprepitant, applied in the field of medicine, can solve the problems of increasing impurity content of aprepitant, affecting drug quality, and decreasing stability, so as to ensure physical stability, improve solubility, and reasonable cost Effect

Active Publication Date: 2018-05-15
CHENGDU BAIYU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the water solubility of aprepitant can be increased by wet grinding, the impurity content in aprepitant will increase during the grinding process, the stability will decrease, and the quality of the drug will be affected, and the wet grinding process involves the selection of solvents. Use, drying and other processes, the operation is complicated

Method used

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  • Preparation method of high stability aprepitant composition
  • Preparation method of high stability aprepitant composition
  • Preparation method of high stability aprepitant composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1. Preparation of the composition of the present invention

[0026] Pass 5.0g aprepitant and 0.5g hydroxypropyl cellulose SL type 3 times through a 60-mesh sieve, mix well, place in a refrigerated grinder to keep warm (-150℃) and grind for 1 hour to obtain aprepitant Tan composition.

Embodiment 2

[0027] Example 2. Preparation of the composition of the present invention

[0028] Pass 5.0g of aprepitant and 5.0g of hydroxypropylcellulose SL type 3 times through a 60-mesh screen, mix well, and place in a refrigerated grinder to keep warm (-170℃) and grind for 3 hours to obtain aprepitant. Tan composition.

Embodiment 3

[0029] Example 3. Preparation of the composition of the present invention

[0030] Pass 5.0g of aprepitant and 2.5g of hydroxypropyl cellulose SL type 3 times through a 60-mesh sieve. After mixing, place it in a refrigerated grinder to keep warm (-150℃) and grind for 1 hour to obtain aprepitant. Tan composition.

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PUM

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Abstract

The invention provides a preparation method of a high stability aprepitant composition. The preparation method comprises the following steps: grinding aprepitant and an auxiliary material between -170DEG C and -100 DEG C for 0.5-3h, and then performing granulating. The preparation method can improve solubility of an insoluble medicine, namely aprepitant, and increase dissolving-out speed of a preparation. Compared with the existing aprepitant capsule, the prepared aprepitant capsule can ensure physical stability of active ingredients, and a preparation technology of the preparation is simple,appropriate in cost and applicable to industrial mass production.

Description

Technical field [0001] The invention belongs to the field of medicine, and specifically relates to a method for preparing a high-stability aprepitant composition. Background technique [0002] Aprepitant, chemical name: 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy] -3-(4-Fluorophenyl)-4-morpholino]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one, the chemical structure is as follows: [0003] [0004] Aprepitant is the first neurokinin-1 (NK-1) receptor blocker antiemetic drug approved by the US FDA, trade name: EMEND. Clinical indications: combined with other antiemetic drugs to prevent acute and delayed nausea and vomiting caused by the initial and repeated application of highly emetic chemotherapeutics (HEC) including high-dose cisplatin; used to prevent the initial And nausea and vomiting caused by repeated application of moderate emetic chemotherapeutics (MEC); used alone for postoperative nausea and vomiting (PONV). [0005] Aprepitant has poor water solubility, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K31/5377A61P1/08
CPCA61K31/5377A61K47/38
Inventor 周家友赖庆宽黄劲甘林建
Owner CHENGDU BAIYU PHARMA CO LTD
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