US 12,133,911 B2
Formulations to achieve rapid dissolution of drug from spray-dried dispersions in capsules
Michael Mark Morgen, Bend, OR (US); and Aaron Keith Goodwin, Bend, OR (US)
Assigned to Capsugel Belgium NV, Bornem (BE)
Appl. No. 15/579,556
Filed by Capsugel Belgium NV, Bornem (BE)
PCT Filed May 26, 2016, PCT No. PCT/IB2016/053085
§ 371(c)(1), (2) Date Dec. 4, 2017,
PCT Pub. No. WO2016/198983, PCT Pub. Date Dec. 15, 2016.
Claims priority of provisional application 62/173,133, filed on Jun. 9, 2015.
Prior Publication US 2018/0161269 A1, Jun. 14, 2018
Int. Cl. A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 9/48 (2006.01); A61K 31/4166 (2006.01)
CPC A61K 9/0004 (2013.01) [A61K 9/1652 (2013.01); A61K 9/485 (2013.01); A61K 9/4858 (2013.01); A61K 31/4166 (2013.01)] 12 Claims
OG exemplary drawing
 
1. A dosage form comprising a dissolvable capsule and a fill material, said fill material comprising
a) a dispersion of an active agent and a polymer, said dispersion being granulated,
b) an osmogen, wherein the osmogen is magnesium chloride, magnesium sulfate, lithium chloride, sodium chloride, potassium chloride, potassium hydrogen phosphate, lithium dihydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, potassium sulfate, sodium carbonate, sodium sulfite, lithium sulfate, sodium sulfate, magnesium succinate, glucose, sucrose, maltose, xylitol, sorbitol, glycerol, urea, inositol, tartaric acid, lactitol, maltitol, erythritol, or combinations thereof, and
c) a glidant, wherein said glidant is silica, fumed silica, silicon dioxide, magnesium aluminosilicates, magnesium aluminometasilicates, or a mixture thereof, and comprises 0.5 wt % to 5 wt % of said fill material;
wherein said dispersion comprises 10 wt % to 90 wt % of said fill material, said osmogen comprises from 15 wt % to 40 wt % of said fill material, and wherein the osmogen has a water solubility of at least 2.5 mol/kg, and a molecular weight of less than 500 Da.