US 11,786,538 B2
Low benzalkonium chloride bimatoprost ophthalmic compositions with effective penetration and preservation properties
Mandar V. Shah, Rockaway, NJ (US); Veerappan Subramanian, Warren, NJ (US); Ilango Subramanian, Warren, NJ (US); and Aman Trehan, Hillsborough, NJ (US)
Assigned to Somerset Therapeutics, LLC, Hollywood, FL (US)
Filed by Somerset Therapeutics LLC, Hollywood, FL (US)
Filed on Dec. 8, 2020, as Appl. No. 17/114,936.
Claims priority of provisional application 62/946,900, filed on Dec. 11, 2019.
Prior Publication US 2021/0177863 A1, Jun. 17, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/5575 (2006.01); A61K 31/14 (2006.01); A61K 9/08 (2006.01); A61K 47/44 (2017.01); A61K 9/00 (2006.01); A61K 47/26 (2006.01); A61K 31/165 (2006.01); A61K 47/02 (2006.01); A61K 47/12 (2006.01); A61K 47/18 (2017.01)
CPC A61K 31/5575 (2013.01) [A61K 9/0048 (2013.01); A61K 9/08 (2013.01); A61K 31/14 (2013.01); A61K 31/165 (2013.01); A61K 47/02 (2013.01); A61K 47/12 (2013.01); A61K 47/186 (2013.01); A61K 47/26 (2013.01); A61K 47/44 (2013.01)] 20 Claims
 
1. A method of reducing elevated intraocular pressure in a mammal comprising administering an effective amount of an ophthalmologically suitable composition comprising (a) about 0.005%-about 0.02% of a bimatoprost compound; (b) 0.003-about 0.007% of a benzalkonium chloride primary penetration enhancer, (c) 0.75%-2.5% of at least one secondary penetration enhancer component comprising one or more ophthalmologically suitable polyoxyethylene sorbitan fatty acid esters and wherein the secondary penetration enhancer component detectably or significantly enhances penetration of the bimatoprost into a mammalian eye, wherein (d) the ratio of the one or more ophthalmologically suitable polyoxyethylene sorbitan fatty acid esters to the benzalkonium chloride is between 107:1 and 833:1, and wherein the administration of the composition results in a reduction of intraocular pressure in the mammalian eye that is at least statistically comparable to the same amount of a composition comprising the same amount of bimatoprost compound and at least 200% more benzalkonium chloride.