US 12,285,411 B2
Pharmaceutical composition comprising eluxadoline, process of preparation and use thereof
Saravanan Kannusamy, Hyderabad (IN); Venkata Vijaya Narasimha Kishan Jayanthy, Hyderabad (IN); Aman Taqiuddin Mohammed, Hyderabad (IN); Raja Rao Chinta, Hyderabad (IN); and Sivakumaran Meenakshisunderam, Hyderabad (IN)
Assigned to Aurobindo Pharma Ltd, Hyderabad (IN)
Filed by Saravanan Kannusamy, Hyderabad (IN); Venkata Vijaya Narasimha Kishan Jayanthy, Hyderabad (IN); Aman Taqiuddin Mohammed, Hyderabad (IN); Raja Rao Chinta, Hyderabad (IN); and Sivakumaran Meenakshisunderam, Hyderabad (IN)
Filed on Sep. 8, 2020, as Appl. No. 17/014,675.
Claims priority of application No. 201941036255 (IN), filed on Sep. 10, 2019.
Prior Publication US 2021/0106563 A1, Apr. 15, 2021
Int. Cl. A61K 31/4164 (2006.01); A61K 9/00 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01)
CPC A61K 31/4164 (2013.01) [A61K 9/0053 (2013.01); A61K 9/2018 (2013.01); A61K 9/2027 (2013.01); A61K 9/2054 (2013.01); A61K 9/2095 (2013.01); A61K 9/2813 (2013.01); A61K 9/282 (2013.01)] 4 Claims
 
1. A pharmaceutical tablet composition comprising:
(a) Eluxadoline in an amount from 5 to 20% by weight of the total composition;
(b) diluents selected from combination of silicified microcrystalline cellulose in an amount from 60% to 70% by weight of the total composition and mannitol in an amount from 8% to 12% by weight of the total composition;
(c) hypromellose in an amount from 2% to 7% by weight of the total composition;
(d) crospovidone in an amount from 0% to 2.5% by weight of the total composition;
(e) colloidal silicon dioxide in an amount from 0.5% to 2% by weight of the total Composition;
(f) sodium stearyl fumarate in an amount from 1.5% to 3% by weight of the total Composition;
(g) optionally coating agent;
wherein extraction of the tablet composition with water or saline at 25° C. for up to 12 hours produces a concentration of eluxadoline of less than or approximately 1 mg/ml.