EP 3229785 A2 20171018 - NALOXONE MONOPREPARATION AND MULTI-LAYER TABLET
Title (en)
NALOXONE MONOPREPARATION AND MULTI-LAYER TABLET
Title (de)
NALOXON-MONOPRÄPARAT UND MEHRSCHICHTTABLETTE
Title (fr)
MONOPRÉPARATION DE NALOXONE ET COMPRIMÉ MULTICOUCHE
Publication
Application
Priority
- EP 14196775 A 20141208
- EP 2015078827 W 20151207
Abstract (en)
[origin: WO2016091805A2] The present invention relates to a solid, oral pharmaceutical composition comprising naloxone, or a pharmaceutically acceptable salt thereof as the active ingredient, the composition having a delayed release of said active ingredient. The composition can comprise a matrix containing glycerol di-behenic acid esters as matrix formers, with a mass ratio of naloxone to matrix former(s) of between 1:1 and 1:10, whereby the active ingredient naloxone has a delayed release. According to the invention, in order to provide a composition suitable for a dosage covering at least twelve hours for treating opioid-induced obstipation, the composition has an in-vitro release rate of the active ingredient, measured using a vane stirrer method according to Eur. Ph. at 75 U/min in 500 ml of 0.1 N hydrochloric acid at 37 °C, of 0 % to 75 % in 2 h, 3 % to 95 % in 4 h, 20 % to 100 % in 10 h, 30 % to 100 % in 16 h, 50 % to 100 % in 24 h and more than 80 % in 36 h, said composition having an IC50/Cmax value of at least 40. Preferably, the composition comprises a value for tmax (naloxone) / tmax (naloxone-3-glucuronoid) of at least 5. In an alternative embodiment, the composition can take the form of a multi-layer tablet.
IPC 8 full level
A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/485 (2006.01); A61P 1/10 (2006.01)
CPC (source: CN EP)
A61K 9/0002 (2013.01 - CN); A61K 9/2013 (2013.01 - CN EP); A61K 9/2086 (2013.01 - CN EP); A61K 9/209 (2013.01 - CN EP); A61K 31/485 (2013.01 - CN EP); A61P 1/10 (2017.12 - EP); A61P 25/04 (2017.12 - EP)
Citation (search report)
See references of WO 2016091805A2
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
DOCDB simple family (publication)
WO 2016091805 A2 20160616; WO 2016091805 A3 20161215; CN 107205943 A 20170926; EP 3229785 A2 20171018
DOCDB simple family (application)
EP 2015078827 W 20151207; CN 201580074337 A 20151207; EP 15817094 A 20151207