US 12,251,465 B2
Dosage form comprising structured solid-solution framework of sparingly-soluble drug and method for manufacture thereof
Aron H. Blaesi, Cambridge, MA (US); and Nannaji Saka, Cambridge, MA (US)
Assigned to Aron H. Blaesi, Cambridge, MA (US)
Filed by Aron H. Blaesi, Cambridge, MA (US)
Filed on Mar. 19, 2021, as Appl. No. 17/207,587.
Application 17/207,587 is a continuation of application No. PCT/US2019/052030, filed on Sep. 19, 2019.
Claims priority of provisional application 62/733,624, filed on Sep. 19, 2018.
Claims priority of provisional application 62/856,073, filed on Jun. 2, 2019.
Claims priority of provisional application 62/893,178, filed on Aug. 28, 2019.
Prior Publication US 2021/0212943 A1, Jul. 15, 2021
Int. Cl. A61K 9/00 (2006.01); A61K 9/107 (2006.01); A61K 9/70 (2006.01); A61K 31/192 (2006.01); A61K 47/34 (2017.01); A61K 47/38 (2006.01); B29C 48/00 (2019.01); B29K 105/00 (2006.01)
CPC A61K 9/0092 (2013.01) [A61K 9/107 (2013.01); A61K 9/7007 (2013.01); A61K 31/192 (2013.01); A61K 47/34 (2013.01); A61K 47/38 (2013.01); B29C 48/001 (2019.02); B29C 48/022 (2019.02); B29K 2105/0035 (2013.01)] 34 Claims
OG exemplary drawing
 
1. A pharmaceutical dosage form comprising:
a drug-containing solid having an outer surface and an internal three dimensional structural framework of one or more orderly arranged structural elements, said framework being contiguous with and terminating at said outer surface;
said structural elements comprising particles, fibers, or sheets having segments spaced apart from adjoining segments, thereby defining free spaces, wherein a plurality of adjacent free spaces combine to define one or more interconnected free spaces forming an open pore network that extends over a length at least half the thickness of the drug-containing solid;
said structural elements further comprising dissolved molecules or dispersed nanometer-scale aggregates of at least one sparingly-soluble active ingredient in an excipient matrix; wherein
said excipient matrix comprises at least a water-soluble polymer carrier to carry the dissolved sparingly-soluble drug molecules and/or dispersed sparingly-soluble drug aggregates, and at least an amphiphilic polymer; whereby
upon immersion in a physiological fluid, said open pore network enables wetting of the structural framework, so that the fluid interdiffuses with the framework, and the amphiphilic polymer self-assembles as micelles, thereby enhancing drug solubility.