US 12,403,099 B2
Muco-adhesive, controlled release formulation of levodopa and/or esters of levodopa and uses thereof
Ann Hsu, Hayward, CA (US); Liang Dong, Hayward, CA (US); Amy Ding, Hayward, CA (US); and Suneel Gupta, Hayward, CA (US)
Assigned to Impax Laboratories, LLC, Bridgewater, NJ (US)
Filed by Impax Laboratories, LLC, Bridgewater, NJ (US)
Filed on Dec. 30, 2024, as Appl. No. 19/004,850.
Application 19/004,850 is a continuation of application No. 18/791,632, filed on Aug. 1, 2024, granted, now 12,178,919.
Application 18/791,632 is a continuation of application No. 18/131,715, filed on Apr. 6, 2023, granted, now 12,064,521.
Application 18/131,715 is a continuation of application No. 17/959,681, filed on Oct. 4, 2022, granted, now 11,666,538.
Application 17/959,681 is a continuation of application No. 17/372,434, filed on Jul. 10, 2021, granted, now 11,622,941.
Application 17/372,434 is a continuation of application No. 17/148,320, filed on Jan. 13, 2021, granted, now 11,357,733.
Application 17/148,320 is a continuation of application No. 16/573,634, filed on Sep. 17, 2019, granted, now 10,987,313.
Application 16/573,634 is a continuation in part of application No. 16/360,936, filed on Mar. 21, 2019, granted, now 10,688,058.
Application 16/360,936 is a continuation of application No. 15/092,086, filed on Apr. 6, 2016, granted, now 10,292,935.
Application 15/092,086 is a continuation in part of application No. PCT/US2014/059554, filed on Oct. 7, 2014.
Claims priority of provisional application 61/887,762, filed on Oct. 7, 2013.
Prior Publication US 2025/0134818 A1, May 1, 2025
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/48 (2006.01); A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 9/50 (2006.01); A61K 31/198 (2006.01); A61K 31/216 (2006.01); A61K 45/06 (2006.01)
CPC A61K 9/4808 (2013.01) [A61K 9/0053 (2013.01); A61K 9/1652 (2013.01); A61K 9/5026 (2013.01); A61K 9/5042 (2013.01); A61K 9/5073 (2013.01); A61K 31/198 (2013.01); A61K 31/216 (2013.01); A61K 45/06 (2013.01); Y02A 50/30 (2018.01)] 19 Claims
 
1. A capsule comprising 95 mg to 390 mg±10% of levodopa wherein the capsule contains:
(i) one or more immediate release components comprising levodopa and carbidopa, and
(ii) a plurality of controlled release components comprising:
(a) a core comprising levodopa, at least one filler, at least one binder and at least one surfactant;
(b) a controlled release coating comprising a controlled release polymer surrounding the core;
(c) a muco-adhesive coating comprising a poly (butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methylmethacrylate) surrounding the controlled release coating; and
(d) an enteric coating comprising an enteric polymer that dissolves at a pH greater than 5.5 surrounding the mucoadhesive coating; and
(iii) optionally additional glidant or lubricant,
wherein the plurality of controlled release components are free of carbidopa and pass through a 12 mesh screen and retained on a 25 mesh screen;
wherein the filler comprises about 1 wt % to about 50 wt % of the total weight of the controlled release components, the binder comprises about 0.1 wt % to about 15 wt % of the total weight of the controlled release components and the surfactant comprises about 0.1 wt % to about 15 wt % of the total weight of the controlled release components; and
wherein the ratio of levodopa in the plurality of controlled release components to levodopa in the one or more immediate release components is about 2:1 to about 3:1.