US 12,011,506 B2
Combination and uses and treatments thereof
Kenneth Churchill Campbell, Ware (GB); Urbain Alfons C. Delaet, Beerse (BE); James M. Goodrich, Research Triangle Park, NC (US); Juliette Segolène Guaquière, Ware (GB); Thomas Laughery, Research Triangle Park, NC (US); Dominique J. Limet, Brentford (GB); John C. Pottage, Collegeville, PA (US); Ludovic Sylvain Marc Renou, Stevenage (GB); Trevor R. Scott, Research Triangle Park, NC (US); Christian Seiler, Brentford (GB); and Mary Woodward, Ware (GB)
Assigned to ViiV Healthcare Company, Wilmington, DE (US); and Janssen Sciences Ireland UC, Little Island (IE)
Appl. No. 16/621,309
Filed by ViiV Healthcare Company, Wilmington, DE (US); and Janssen Sciences Ireland Unlimited Company, County Cork (IE)
PCT Filed Jun. 27, 2018, PCT No. PCT/IB2018/054769
§ 371(c)(1), (2) Date Dec. 11, 2019,
PCT Pub. No. WO2019/003150, PCT Pub. Date Jan. 3, 2019.
Claims priority of provisional application 62/589,576, filed on Nov. 22, 2017.
Claims priority of provisional application 62/535,290, filed on Jul. 21, 2017.
Claims priority of provisional application 62/527,169, filed on Jun. 30, 2017.
Claims priority of application No. 1717131 (GB), filed on Oct. 18, 2017; application No. 1719377 (GB), filed on Nov. 22, 2017; and application No. 1806490 (GB), filed on Apr. 20, 2018.
Prior Publication US 2020/0113838 A1, Apr. 16, 2020
Int. Cl. A61K 9/24 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/505 (2006.01); A61K 31/5365 (2006.01); A61P 31/18 (2006.01)
CPC A61K 9/209 (2013.01) [A61K 9/2095 (2013.01); A61K 9/28 (2013.01); A61K 31/505 (2013.01); A61K 31/5365 (2013.01); A61P 31/18 (2018.01)] 8 Claims
 
1. A bilayer tablet comprising
a) a first layer comprising dolutegravir sodium; and
b) a second layer comprising rilpivirine hydrochloride;
wherein said first layer and said second layer are in direct contact, and wherein the first layer consists of:
 
 
 Ingredient Mass (mg)
 
 
Intragranular
 
 Dolutegravir sodium 52.62
 
 D-mannitol 145.38
 
 Microcrystalline cellulose 60.00
 
 Povidone K29/32 15.00
 
 Sodium starch glycolate 15.00
 
 Purified water q.s.
Extragranular
 
 Sodium starch glycolate 6.00
 
 Sodium stearyl fumarate 6.00
 
and the second layer consists of:
 
 
 Ingredient Mass (mg)
 
 
Intragranular
 
 Rilpivirine hydrochloride 27.50
 
 Lactose monohydrate 55.145
 
 Croscarmellose sodium 1.10
 
 Povidone K30 3.25
 
 Polysorbate 20 0.35
 
 Purified water q.s.
Extragranular
 
 D-mannitol 57.755
 
 Silicified microcrystalline cellulose 40.00
 
 Sodium starch glycolate 12.90
 
 Magnesium stearate 2.00.