US 11,878,081 B1
Pharmaceutical formulations of tafamidis
Nilesh Parikh, Irvine, CA (US); and William Hite, Winchester, CA (US)
Assigned to TaP Pharmaceuticals AG, Baar (CH)
Filed by TaP Pharmaceuticals, AG, Baar (CH)
Filed on Dec. 23, 2022, as Appl. No. 18/088,382.
Int. Cl. A61K 9/48 (2006.01); A61K 31/423 (2006.01)
CPC A61K 9/4866 (2013.01) [A61K 9/4858 (2013.01); A61K 31/423 (2013.01)] 12 Claims
1. A pharmaceutical, unit-dose formulation, suitable for oral administration, comprising:
from 1% w/w to 20% w/w of a tafamidis-fumaric acid co-crystal;
from 0.25% w/w to 2.5% w/w of an added organic acid dissolution enhancer;
from 77.5% w/w to 82.5% w/w of a polyethylene glycol (PEG), wherein the PEG has a molecular weight of 100 to 1000;
from 1% w/w to 10% w/w of a polysorbate that is polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, or a combination thereof; and
from 0.25% w/w to 2.75% w/w of a polyvinylpyrrolidone (PVP), wherein the PVP has a K value of 10 to 120;
wherein the formulation releases, within 15 minutes in modified FeSSIF pH 5.8 or in modified FaSSIF pH 6.5, at least 85% of the total tafamidis of the formulation, and
wherein the formulation releases, within 45 minutes in modified FeSSIF pH6.5, at least 90% of the total tafamidis of the formulation.