Aprepitant oral pharmaceutical preparation

A technology for aprepitant and pharmaceutical preparations, applied in the field of oral pharmaceutical preparations of aprepitant, can solve the problems of debris pollution of grinding machines, restrict the popularization and use of aprepitant, and high cost, achieve high stability, fill Market blank, the effect of improving the dissolution rate

Inactive Publication Date: 2016-05-04
北京颐诺赛医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aprepitant is almost insoluble in water, so the aprepitant tablet on the market now uses grinding technology to reduce the particle size of the aprepitant raw material to the nanometer level and prepare it into a nan...

Method used

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  • Aprepitant oral pharmaceutical preparation
  • Aprepitant oral pharmaceutical preparation
  • Aprepitant oral pharmaceutical preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] An oral tablet of Aprepitant, the formula is as follows:

[0034]

[0035] Dissolve aprepitant and hypromellose acetate succinate in absolute ethanol, dry under reduced pressure, and pass the dried product through a 150-mesh sieve to obtain a solid dispersion for use;

[0036] (2) Pass component C to component F through a 150 mesh sieve for use;

[0037] (3) Weigh the sieved solid dispersion, add lactose, croscarmellose sodium, silicon dioxide and magnesium stearate to it in sequence, mix well, and press into tablets.

Embodiment 2

[0039] An oral tablet of Aprepitant, the formula is as follows:

[0040]

[0041] Dissolve aprepitant and hypromellose phthalate in absolute ethanol, dry under reduced pressure, and pass the dried product through a 150-mesh sieve to obtain a solid dispersion for use;

[0042] (2) Pass component C to component F through a 150 mesh sieve for use;

[0043] (3) Weigh the sieved solid dispersion, add lactose, crospovidone, talc and magnesium stearate to it in sequence, mix well, and press into tablets.

Embodiment 3

[0045] An oral capsule of Aprepitant, the formula is as follows:

[0046]

[0047]

[0048] Dissolve aprepitant and hypromellose phthalate in absolute ethanol, dry under reduced pressure, and pass the dried product through a 150-mesh sieve to obtain a solid dispersion for use;

[0049] (2) Pass component C to component F through a 150 mesh sieve for use;

[0050] (3) Weigh the sieved solid dispersion, add microcrystalline cellulose, low-substituted hydroxypropyl cellulose and magnesium stearate to it in sequence, mix them evenly, and put them into HPMC capsule shells.

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Abstract

The invention discloses an aprepitant oral pharmaceutical preparation. The aprepitant oral pharmaceutical preparation comprises 15wt%-25wt% of aprepitant, 45wt%-75wt% of hydroxypropyl methylcellulose phthalate/hydroxypropyl methylcellulose acetate succinate, 10wt%-25wt% of microcrystalline cellulose, lactose or mannitol, 2wt%-8wt% of low-substituted hydroxypropyl cellulose as well as croscarmellose sodium and/or crospovidone, 0-2wt% of silicon dioxide and/or talc and 0-2wt% of magnesium stearate. The pharmaceutical preparation can be prepared in a form of tablets or capsules andhas high stability and good bioavailability.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an oral pharmaceutical preparation of aprepitant. Background technique [0002] Aprepitant, its full chemical name is 5-[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4 -Fluorophenyl)morpholin-4-ylmethyl]-3,4-dihydro-2H-1,2,4-triazol-3-one; Aprepitant; 5-(2(R)- (1(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3(S)-(4-fluorophenyl)morpholin-4-ylmethyl)-3, 4-dihydro-2H-1,2,4-triazol-3-one, is a selective high-affinity substance P / neurokinin-1 (NK1) receptor inhibitor, against serotonin ( 5HT3), dopamine and corticosteroid receptors have very low affinity. The drug can pass through the blood-brain barrier and bind to the NK1 receptor in the brain. It is clinically used as an antiemetic and emetic, especially for high-emetic anti-cancer chemotherapy drugs (including high-dose cisplatin therapy). Of acute and delayed nausea and vomiting. The molecular formula of Apre...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K9/20A61K9/48A61K47/38A61K47/26A61K47/12A61P1/08
CPCA61K9/4866A61K9/2054A61K31/5377
Inventor 王志云
Owner 北京颐诺赛医药科技有限公司
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