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New alfentanil composition for treatment of acute pain

A technology of composition and mixture, applied in directions such as drug combination, non-central analgesic, drug delivery, etc., can solve the problems such as short-term or long-term stability of alfentanil solution that are not reported

Inactive Publication Date: 2015-03-18
OREXO AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To the applicant's knowledge, there have been no reported problems with the short-term or long-term stability of alfentanil solutions for injection

Method used

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  • New alfentanil composition for treatment of acute pain
  • New alfentanil composition for treatment of acute pain
  • New alfentanil composition for treatment of acute pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] Alfentanil Sublingual Tablets - Granulated Carrier Particles

[0124] (a) carrier particle

[0125] (i) is composed of anhydrous citric acid (fine grain 16 / 40 grade, DSM, Basel, Switzerland) and mannitol (Pearlitol TM 400DC, Roquette, Lestrem, France) eight batches of carrier particles (for tablet batches 1 to 8 as identified in Tables 1 and 2 below) were prepared. Carrier particles were prepared as follows.

[0126] Grind the citric acid by hand using a pestle and mortar, then pass through a sieve. A fraction with a particle size between 90 μm and 180 μm is used in the granulation. First, follow the amounts below:

[0127] (i) 0.2502g citric acid and 199.8g mannitol;

[0128] (ii) 1.2524g citric acid and 198.8g mannitol; and

[0129] (iii) 2.5109g citric acid and 197.5g mannitol;

[0130] The citric acid and mannitol were dry mixed for about 1 minute in a small size intensive mixer (Braun electronic 4261, Braun AG, Germany).

[0131] These amounts were chosen...

Embodiment 2

[0152] Alfentanil Sublingual Tablets

Embodiment 21

[0153] Example 2.1 - Batches of Granulated Carrier Particles

[0154] (a) Prepared as follows containing anhydrous citric acid (fine particle grade 16 / 40, DSM, Basel, Switzerland) or trisodium citrate dihydrate (Citrique Belge, Belgium) and mannitol (Pearlitol TM 400DC, Roquette, Lestrem, France) granulated carrier particles.

[0155] First, citric acid and sodium citrate were milled using an air jet mill (Pilotmill-1; Food and Pharma Systems, Italy). Citric acid was milled to volume-based particle sizes (D(4,3)) of 4.3 μm and 99 μm, and sodium citrate was milled to particle sizes of 9.6 μm, 21 μm and 94 μm.

[0156] First, take the following amounts:

[0157] (i) 0.125g citric acid / citrate and 99.875g mannitol for a 100g batch (or 0.25g citric acid and 199.75g mannitol for a 200g batch); and

[0158] (ii) 2.502g citric acid and 97.498g mannitol for a 100g batch (or 5.004g citric acid and 194.996g mannitol for a 200g batch).

[0159] The citric acid / citrate and mannitol we...

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Abstract

There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising: (a) microparticles of alfentanil, or a pharmaceutically acceptable salt thereof, which microparticles are presented on the surfaces of larger carrier particles; (b) a water-soluble weak base; and (c) a compound which is a weak acid, which acid is presented in intimate mixture with the microparticles of alfentanil or salt thereof. The composition may further comprise a disintegrant. The acid is preferably citric acid.

Description

technical field [0001] The present invention relates to novel alfentanil-containing pharmaceutical compositions useful for the treatment of pain, especially acute pain, short-term pain associated with surgical, diagnostic and / or nursing-related procedures, and which can be transmucosally, especially Administered sublingually. Background technique [0002] Opioids are widely used as pain relievers in the medical field. In fact, it is currently recognized that no more effective therapeutic agent exists in alleviating moderate to severe pain. [0003] Opioid agonist analgesics are used to treat moderate to severe chronic cancer pain (often in combination with nonsteroidal anti-inflammatory drugs (NSAIDs)) as well as moderate to severe acute pain (eg, during recovery from surgery and breakthrough pain). Additionally, its use in the management of chronic, non-malignant pain is increasing. [0004] Furthermore, invasive surgical and / or diagnostic procedures often cause brief b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K31/454
CPCA61K9/006A61K9/2054A61K9/2077A61K9/1623A61K31/454A61K9/0056A61P25/04A61P29/00A61P29/02A61K9/2013A61K9/2018
Inventor A·彼得松E·施万B·约翰松
Owner OREXO AB