Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF3 Cites 6 Cited by
  • 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 nanosuspension, which improves the aprepitant Oral absorption of aprepitant, but the cost of this technology is very high, and there will be debris pollution from the grinder, which limits the promotion and use of aprepitant

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com