US 11,654,150 B2
Darunavir combination formulations
Urbain Alfons C. Delaet, Balen (BE); Philip Erna H. Heyns, Vosselaar (BE); Eugeen Maria Jozef Jans, Meerhout (BE); Roel Jos M. Mertens, Balan (BE); and Geert Van Der Avoort, Retie (BE)
Assigned to Janssen Sciences Ireland UC, Little Island (IE)
Filed by Janssen Sciences Ireland Unlimited Company, County Cork (IE); and Gilead Sciences, Inc., Foster City, CA (US)
Filed on Nov. 27, 2019, as Appl. No. 16/697,888.
Application 16/697,888 is a division of application No. 14/131,282, abandoned, previously published as PCT/EP2012/063249, filed on Jul. 6, 2012.
Claims priority of application No. 11173067 (EP), filed on Jul. 7, 2011.
Prior Publication US 2020/0093840 A1, Mar. 26, 2020
Int. Cl. A61K 31/635 (2006.01); A61K 31/5377 (2006.01); A61K 9/28 (2006.01); A61K 9/20 (2006.01); A61K 9/16 (2006.01)
CPC A61K 31/635 (2013.01) [A61K 9/2009 (2013.01); A61K 9/2054 (2013.01); A61K 9/2095 (2013.01); A61K 9/28 (2013.01); A61K 31/5377 (2013.01); A61K 9/1652 (2013.01)] 12 Claims
1. A process for preparing an oral dosage form comprising the steps of:
(a) providing a dried darunavir granulate consisting of:
(a) darunavir, and/or a pharmaceutically acceptable salt or solvate thereof,
(b) hypromellose, and
(c) water,
wherein the dried darunavir granulate is prepared by: (i) mixing water and hypromellose to form a first mixture, (ii) spraying the first mixture on a powder of darunavir and/or a pharmaceutically acceptable salt or solvate thereof, to form a wet darunavir granulate, and (iii) drying the wet darunavir granulate to produce the dried darunavir granulate, wherein the darunavir or pharmaceutically acceptable salt or solvate thereof is about 95% to about 99.9%, by weight relative to the total weight of the dried darunavir granulate;
(b) providing a second mixture comprising microcrystalline cellulose, silicon dioxide loaded with GS-9350, and a disintegrant;
(c) adding the dried darunavir granulate of step (a) to the second mixture of step (b) and dry-blending to form a blend;
(d) adding a lubricant to the blend and mixing to prepare a homogeneous mixture; and
(e) compressing the homogenous mixture to produce the oral dosage form.