US 12,239,660 B2
Therapeutic composition and methods
Stephen Taglienti, Ledgewood, NJ (US); and Steven L. Petruccelli, Watchung, NJ (US)
Assigned to Viscera Labs, Inc.
Filed by Viscera Labs, Inc., East Hanover, NJ (US)
Filed on Sep. 25, 2023, as Appl. No. 18/372,162.
Application 18/372,162 is a continuation of application No. 17/994,720, filed on Nov. 28, 2022, granted, now 11,813,283.
Application 17/994,720 is a continuation of application No. 16/788,563, filed on Feb. 12, 2020, granted, now 11,590,161, issued on Feb. 28, 2023.
Application 16/788,563 is a continuation in part of application No. 16/537,823, filed on Aug. 12, 2019, granted, now 11,524,029, issued on Dec. 13, 2022.
Claims priority of provisional application 62/804,312, filed on Feb. 12, 2019.
Claims priority of provisional application 62/736,715, filed on Sep. 26, 2018.
Claims priority of provisional application 62/718,055, filed on Aug. 13, 2018.
Prior Publication US 2024/0050464 A1, Feb. 15, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/785 (2006.01); A61K 9/00 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 45/06 (2006.01); A61P 3/08 (2006.01); A61P 3/10 (2006.01); A61P 9/00 (2006.01); A61P 9/10 (2006.01); A61P 9/12 (2006.01); A61P 17/04 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01)
CPC A61K 31/785 (2013.01) [A61K 9/0053 (2013.01); A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2054 (2013.01); A61K 9/282 (2013.01); A61K 9/2866 (2013.01); A61K 45/06 (2013.01); A61P 3/08 (2018.01); A61P 3/10 (2018.01); A61P 9/00 (2018.01); A61P 9/10 (2018.01); A61P 9/12 (2018.01); A61P 17/04 (2018.01); A61P 35/00 (2018.01); A61P 43/00 (2018.01)] 12 Claims
 
1. A method of treating a disorder related to elevated serum cholesterol concentration in a patient in need thereof comprising:
selecting a patient in need of treating a disorder related to elevated serum cholesterol concentration;
administering to the patient an oral drug delivery system comprising:
a) a core comprising:
a therapeutically effective amount of at least one active agent present in an amount of from about 50% to about 64% w/w of the core, wherein the at least one active agent is selected from the group consisting of colesevelam, pharmaceutically acceptable salts thereof, and combinations thereof, and
a drug release controlling component capable of providing release of the at least one active agent primarily in a region selected from the group consisting of a lower gastrointestinal tract, a large intestine, a jejunum, an ileum, a cecum, a colon, a rectum, and combinations thereof,
wherein the drug release controlling component comprises low viscosity hydroxypropyl methyl cellulose (HPMC) and high viscosity HPMC, and
comprises at least one erodible matrix material selected from the group consisting of hydroxypropyl methylcellulose phthalate (HPMCP), hydroxypropylmethylcellulose acetate succinate (HPMCAS), hydroxypropyl methyl cellulose acetate trimellitate (HPMCAT), ethylhydroxy ethylcellulose (EHEC), and combinations thereof, wherein said at least one erodible matrix material is present in a concentration of about 5% to about 15% w/w of the core;
b) a barrier coating encasing the core, wherein said barrier coating comprises HPMC, and
c) an enteric coating on the barrier coating comprising hypromellose acetate succinate, and further comprising a plasticizer,
wherein after ingestion by the patient the at least one active agent is released primarily in a region selected from the group consisting of the lower gastrointestinal tract, the large intestine, the jejunum, the ileum, the cecum, the colon, the rectm, and combinations thereof, and
further wherein the disorder related to elevated serum cholesterol concentration is prevented and/or treated in the patient.
 
7. A method for reducing elevated low-density lipoprotein cholesterol (LDL) concentration in a patient in need thereof comprising:
selecting a patient in need of reducing elevated LDL concentration;
administering to the patient an oral drug delivery system comprising:
a) a core comprising:
a therapeutically effective amount of at least one active agent present in an amount of from about 50% to about 64% w/w of the core, wherein the at least one active agent is selected from the group consisting of colesevelam, pharmaceutically acceptable salts thereof, and combinations thereof, and
a drug release controlling component capable of providing release of the at least one active agent primarily in a region selected from the group consisting of a lower gastrointestinal tract, a large intestine, a jejunum, an ileum, a cecum, a colon, a rectum, and combinations thereof,
wherein the drug release controlling component comprises low viscosity hydroxypropyl methyl cellulose (HPMC) and high viscosity HPMC, and
comprises at least one erodible matrix material selected from the group consisting of hydroxypropyl methylcellulose phthalate (HPMCP), hydroxypropylmethylcellulose acetate succinate (HPMCAS), hydroxypropyl methyl cellulose acetate trimellitate (HPMCAT), ethylhydroxy ethylcellulose (EHEC), and combinations thereof, wherein said at least one erodible matrix material is present in a concentration of about 5% to about 15% w/w of the core;
b) a barrier coating encasing the core, wherein said barrier coating comprises HPMC, and
c) an enteric coating on the barrier coating comprising hypromellose acetate succinate, and further comprising a plasticizer,
wherein after ingestion by the patient the at least one active agent is released primarily in a region selected from the group consisting of the lower gastrointestinal tract, the large intestine, the jejunum, the ileum, the cecum, the colon, the rectum, and combinations thereof, and further wherein the LDL concentration is reduced in the patient.