US 12,303,605 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. 10, 2024, as Appl. No. 18/975,144.
Application 18/975,144 is a continuation of application No. 18/911,732, filed on Oct. 10, 2024.
Application 18/911,732 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 2025/0099389 A1, Mar. 27, 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)] 26 Claims
 
1. A controlled release formulation comprising:
i) one or more immediate release components comprising levodopa and a decarboxylase inhibitor, and
ii) one or more controlled release components comprising levodopa wherein the one or more controlled release components are substantially free of a decarboxylase inhibitor,
wherein when the controlled release formulation is orally administered to a healthy subject in a single-dose crossover study with an immediate release oral carbidopa-levodopa-entacapone dosage form wherein the ratio of carbidopa to levodopa to entacapone in the immediate release carbidopa-levodopa-entacapone dosage form is 1:4:8, and the amount of levodopa orally administered with the controlled release formulation is 3.6 times the amount of levodopa administered with the immediate release carbidopa-levodopa-entacapone dosage form, a dose normalized levodopa AUC0-∞ value of about 55% to about 77% for the controlled release formulation is obtained compared to a dose normalized levodopa AUC0-∞ value obtained from the oral administration of the immediate release oral carbidopa-levodopa-entacapone dosage form.