US 11,752,106 B2
Pharmaceutical composition and administrations thereof
Eleni Dokou, Cambridge, MA (US); Shahla Jamzad, Belmont, MA (US); John P. Caesar, Jr., Lancaster, MA (US); Majed Fawaz, Foxboro, MA (US); Laura Das, Charlestown, MA (US); Chong-Hui Gu, Waban, MA (US); Patricia Nell Hurter, Harvard, MA (US); Meghna Jai Israni, Boston, MA (US); Meghan M. Johnston, Wakefield, MA (US); Dragutin Knezic, Watertown, MA (US); Andrew G. Kuzmission, Shrewsbury, MA (US); and HongRen Wang, Lexington, MA (US)
Assigned to Vertex Pharmaceuticals Incorporated, Boston, MA (US)
Filed by Vertex Pharmaceuticals Incorporated, Boston, MA (US)
Filed on Sep. 15, 2021, as Appl. No. 17/475,622.
Application 17/475,622 is a continuation of application No. 16/299,675, filed on Mar. 12, 2019, granted, now 11,147,770.
Application 16/299,675 is a continuation of application No. 15/181,114, filed on Jun. 13, 2016, granted, now 10,272,046, issued on Apr. 30, 2019.
Application 15/181,114 is a continuation of application No. 14/715,682, filed on May 19, 2015, abandoned.
Application 14/715,682 is a continuation of application No. 14/510,507, filed on Oct. 9, 2014, abandoned.
Application 14/510,507 is a continuation of application No. 14/286,856, filed on May 23, 2014, granted, now 8,883,206, issued on Nov. 11, 2014.
Application 14/286,856 is a continuation of application No. 13/779,654, filed on Feb. 27, 2013, abandoned.
Claims priority of provisional application 61/710,352, filed on Oct. 5, 2012.
Claims priority of provisional application 61/603,882, filed on Feb. 27, 2012.
Prior Publication US 2022/0241206 A1, Aug. 4, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/20 (2006.01); A61K 9/14 (2006.01); A61K 9/16 (2006.01); A61K 9/48 (2006.01); A61K 31/47 (2006.01); A61K 47/02 (2006.01); A61K 47/12 (2006.01); A61K 47/20 (2006.01); A61K 47/26 (2006.01); A61K 47/38 (2006.01); C07D 215/56 (2006.01); A61P 1/10 (2006.01); A61P 1/16 (2006.01); A61P 1/18 (2006.01); A61P 3/00 (2006.01); A61P 3/06 (2006.01); A61P 3/10 (2006.01); A61P 3/12 (2006.01); A61P 5/00 (2006.01); A61P 5/14 (2006.01); A61P 5/16 (2006.01); A61P 5/18 (2006.01); A61P 7/00 (2006.01); A61P 7/04 (2006.01); A61P 7/10 (2006.01); A61P 7/12 (2006.01); A61P 9/00 (2006.01); A61P 11/00 (2006.01); A61P 11/02 (2006.01); A61P 11/06 (2006.01); A61P 13/02 (2006.01); A61P 13/12 (2006.01); A61P 15/08 (2006.01); A61P 15/10 (2006.01); A61P 17/00 (2006.01); A61P 19/08 (2006.01); A61P 19/10 (2006.01); A61P 21/00 (2006.01); A61P 21/02 (2006.01); A61P 21/04 (2006.01); A61P 25/00 (2006.01); A61P 25/08 (2006.01); A61P 25/14 (2006.01); A61P 25/16 (2006.01); A61P 25/20 (2006.01); A61P 25/22 (2006.01); A61P 25/28 (2006.01); A61P 27/02 (2006.01); A61P 27/04 (2006.01); A61P 29/00 (2006.01); A61P 31/10 (2006.01); A61P 35/00 (2006.01); A61P 37/06 (2006.01); A61P 37/08 (2006.01); A61P 43/00 (2006.01); A61K 47/00 (2006.01)
CPC A61K 9/205 (2013.01) [A61K 9/143 (2013.01); A61K 9/145 (2013.01); A61K 9/146 (2013.01); A61K 9/1611 (2013.01); A61K 9/1617 (2013.01); A61K 9/1623 (2013.01); A61K 9/1652 (2013.01); A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2018 (2013.01); A61K 9/2054 (2013.01); A61K 9/2072 (2013.01); A61K 9/2077 (2013.01); A61K 9/485 (2013.01); A61K 9/4808 (2013.01); A61K 9/4858 (2013.01); A61K 9/4866 (2013.01); A61K 31/47 (2013.01); A61K 47/02 (2013.01); A61K 47/12 (2013.01); A61K 47/20 (2013.01); A61K 47/26 (2013.01); A61K 47/38 (2013.01); C07D 215/56 (2013.01)] 20 Claims
 
1. A pharmaceutical composition in a unit dose form comprising one or a plurality of granules, pellets, particles or mini-tablets, wherein the composition comprises:
(a) a solid dispersion in an amount from 30 to 40 percent by weight of the composition, wherein the solid dispersion comprises:
(i) about 80 wt % of substantially amorphous or amorphous N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) by weight of the dispersion,
(ii) about 19.5 wt % of hydroxypropylmethylcellulose acetate succinate (HPMCAS) by weight of the dispersion, and
(iii) about 0.5 wt % sodium lauryl sulfate (SLS) by weight of the dispersion;
(b) a binary filler, wherein the binary filler comprises mannitol and lactose in a ratio of about 1:3 mannitol to lactose;
(c) a sweetener, wherein the sweetener is sucralose;
(d) a disintegrant;
(e) a glidant; and
(f) a lubricant;
wherein the unit dose form comprises at least about 5 mg of substantially amorphous or amorphous Compound 1,
and wherein substantially amorphous Compound 1 has less than 15% crystallinity.