US 10,376,501 B2
Complexes of lumacaftor and its salts and derivatives, process for the preparation thereof and pharmaceutical compositions containing them
Richárd Balázs Kárpáti, Tatabánya (HU); Betti Szabóné Ordasi, Budapest (HU); Orsolya Basa-Dénes, Eger (HU); Erzsébet Réka Angi, Nagykovácsi (HU); Tamás Jordán, Öcsöd (HU); László Molnár, Biatorbágy (HU); Hristos Glavinas, Szeged (HU); Zsolt Ötvös, Csongrád (HU); and Genovéva Filipcsei, Budapest (HU)
Assigned to Druggability Technologies IP Holdco Limited, Msida (MT)
Filed by Druggability Technologies IP Holdco Limited, Swatar (MT)
Filed on Apr. 25, 2017, as Appl. No. 15/496,246.
Claims priority of provisional application 62/327,148, filed on Apr. 25, 2016.
Prior Publication US 2017/0326121 A1, Nov. 16, 2017
This patent is subject to a terminal disclaimer.
Int. Cl. A01N 43/40 (2006.01); A61K 31/443 (2006.01); A61K 31/192 (2006.01); A61K 9/20 (2006.01); A61K 45/06 (2006.01); A61K 9/14 (2006.01); A61K 31/445 (2006.01)
CPC A61K 31/443 (2013.01) [A61K 9/145 (2013.01); A61K 9/146 (2013.01); A61K 9/2013 (2013.01); A61K 9/2072 (2013.01); A61K 31/192 (2013.01); A61K 45/06 (2013.01)] 15 Claims
 
1. A stable complex comprising
i. Lumacaftor;
ii. At least 50% by weight of a complexation agent which is a copolymer of vinylpyrrolidone and vinyl acetate; and
iii. Sodium lauryl sulfate;
wherein the ratio of the copolymer:sodium lauryl sulfate:Lumacaftor is 9:1.2:2, and
wherein said complex has a particle size is between 10 nm and 500 nm, and possesses one or more among the following features:
a) has an apparent solubility in water of at least 1 mg/mL; and
b) has a PAMPA permeability of at least 2×10˜1 2 3 4 cm/s when dispersed in FaSSIF or FeSSIF biorelevant media, which does not decrease in time at least for 12 month.