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

Fentanyl composition for treatment of acute pain

An acute and combination technology, applied in the direction of active ingredients of heterocyclic compounds, non-central analgesics, drug combinations, etc., can solve problems such as side effects

Inactive Publication Date: 2001-12-26
欧莱克斯欧公司
View PDF1 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is unfavorable and can lead to an overdose of the drug, which can cause side effects

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
  • Fentanyl composition for treatment of acute pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The invention will be described in more detail below with reference to examples, which give preferred but non-limiting embodiments. Example 1. Preparation of rapidly disintegrating tablets with bio / mucoadhesion promoting properties

[0055] Tablet batches of 1000 were prepared with the following composition: 81.5 g of mannitol and 2.0 g of Ac-Di-Sol(R) (disintegrant and bio / mucoadhesion promoter) were mixed with about 170 ml of absolute ethanol. The dried mixture was pressed through a metal sieve with a pore size of 1 mm and the resulting fraction having a particle size of about 250 to 450 microns was mixed with 500 mg of micronized fentanyl and 1.0 g of finely ground sodium lauryl sulfate (surfactant) 50 hours. The resulting mixture was mixed with 5.0 g of Avicel(R) Ph 101 and 10.0 g of sodium alginate (bio / mucoadhesion promoter and disintegrant) for 60 minutes. The resulting mixture was compressed under a pressure of 200 MPa into tablets, each weighing 100 mg and co...

Embodiment 2

[0056] The dissolution rate of the prepared tablets was determined according to USP XXIII (paddle method) at two different stirring speeds (25 and 100 rpm). Example 2. Preparation of rapidly disintegrating tablets with bio / mucoadhesion promoting properties

[0057] Tablet batches of 1000 were prepared with the following composition: 91.0 g of mannitol (granules with a particle size of 250-450 μm) were mixed with 1.0 g of sodium lauryl sulfate and 500 mg of micronized fentanyl in a V-blender 24 hours. It was then mixed with 5.0 g of Avicel(R) Ph101 and 2.0 g of Ac-Di-Sol(R) (used both as a disintegrant and as a bio / mucoadhesion promoter) for 2 hours. Finally, it is mixed with 0.5 g of magnesium stearate for 2 minutes. The formed tablet pellets were compressed into tablets under a pressure of 130 MPa, each containing 0.5 mg of fentanyl.

[0058] The disintegration time was tested using the apparatus described in Ph. Eur. (latest edition).

[0059] The measured disintegration...

Embodiment 3

[0062]A patient suffering from breakthrough pain due to cancer was administered 400 μg of fentanyl in the form of a sublingual tablet formulated as described in Example 1 . Plasma concentrations of fentanyl were monitored for 240 minutes after dosing and the results are shown in the accompanying drawings. It can be seen that the uptake of fentanyl is very rapid, reaching a maximum already after 5 minutes. This indicates that the sublingual formulation of the present invention allows rapid ingestion of the active ingredient, although only a small amount of liquid is available to dissolve the active ingredient in this route of administration. Example 4. Evaluation of biological / mucoadhesive properties

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
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

Pharmaceutical compositions for the treatment of acute pain via sublingual administration are disclosed. The composition contains an ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of substantially anhydrous, microparticles adhered to substantially water-soluble particles that are much larger than the fentanyl particles. The surface of the carrier particles. In a preferred embodiment, the composition also contains a bioadhesion and / or mucoadhesion promoter. The invention also relates to a method for the preparation of the composition and the use of the composition for the treatment of acute pain.

Description

field of invention [0001] The present invention relates to rapidly disintegrating pharmaceutical compositions for sublingual administration of fentanyl, methods of treating acute pain and methods of producing corresponding medicaments. Background of the invention [0002] Acute and / or severe pain is a common reason for emergency treatment or hospitalization. In cancer patients, nonsteroidal anti-inflammatory drugs (NSAIDs) are often used alone or in combination s ) and opiates to treat pain. Slow-release opiates (slow-release morphine or ketomidone or transdermal fentanyl) are usually given to cancer pain patients who require opioids. Cancer pain is characterized by periods of inappropriate analgesia (breakthrough pain). Its most common cause is due to increased physical activity of the patient. However, treatment of breakthrough pain with emergency doses of long-acting analgesics administered over a prolonged period can cause side effects such as excessive sedation, nau...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/00A61K9/16A61K31/445A61K31/4468A61K47/02A61K47/10A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/46A61P25/04
CPCA61K9/006A61K31/445A61P25/04A61P29/00A61K9/16
Inventor A·佩尔特松C·尼斯特伦H·伦纳奈斯B·伦纳奈斯T·赫德纳
Owner 欧莱克斯欧公司
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