	US 12,263,148 B2
	Levodopa dosing regimen
Richard D'Souza, Morristown, NJ (US); Hester Visser, Neshanic Station, NJ (US); and Suneel Gupta, Hayward, CA (US)
Assigned to Amneal Pharmaceuticals, LLC, Bridgewater, NJ (US)
Filed by Amneal Pharmaceuticals, LLC, Bridgewater, NJ (US)
Filed on Aug. 13, 2024, as Appl. No. 18/802,458.
Application 18/802,458 is a continuation of application No. 18/634,040, filed on Apr. 12, 2024, granted, now 12,109,185.
Application 18/634,040 is a continuation of application No. 17/967,332, filed on Oct. 17, 2022, granted, now 11,986,449.
Application 17/967,332 is a continuation in part of application No. 17/558,337, filed on Dec. 21, 2021, granted, now 12,194,150.
Claims priority of provisional application 63/247,639, filed on Sep. 23, 2021.
Claims priority of provisional application 63/236,403, filed on Aug. 24, 2021.
Claims priority of provisional application 63/150,121, filed on Feb. 17, 2021.
Claims priority of provisional application 63/129,063, filed on Dec. 22, 2020.
Prior Publication US 2024/0398744 A1, Dec. 5, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/198 (2006.01); A61K 9/20 (2006.01); A61K 9/50 (2006.01); A61P 25/16 (2006.01)

CPC A61K 31/198 (2013.01) [A61K 9/5005 (2013.01); A61P 25/16 (2018.01)]

28 Claims

1. A method for treating a patient diagnosed with Parkinson's disease-comprising:

i) selecting a patient diagnosed with Parkinson's disease and being treated with oral immediate release levodopa tablets, administered three, four, five or more times a day for a total daily levodopa dose of greater than 500 mg;

ii) determining the most frequent immediate release levodopa dose from each administration of immediate release tablets of step (i);

iii) discontinuing the administration of the immediate release levodopa tablets to the patient of step (i); and

iv) orally administering one or more multiparticulate controlled release levodopa dosage forms thrice a day to the patient, wherein the amount of levodopa administered with each administration of the multiparticulate controlled release levodopa dosage form is 2.8 times the amount of levodopa the patient was receiving with each administration of the most frequent immediate release levodopa dose of step (ii);

wherein the patient after receiving treatment with the multiparticulate controlled release levodopa dosage form exhibits a decrease of at least 5% of the patient's total post dose “Off” time as compared to post dose of the oral immediate release levodopa tablets wherein the multiparticulate controlled release dosage form comprises:

(a) a plurality of controlled release components comprising levodopa, a controlled release material, and a coating comprising an enteric polymer surrounding the levodopa and controlled release material wherein the controlled release components pass through a 12 mesh screen; and

(b) an immediate release component comprising levodopa, and carbidopa; and

wherein the multiparticulate controlled release dosage form when administered to an adult human subject after an overnight fast and at a dose of 280 mg of levodopa and 70 mg of carbidopa produces a C_maxof from about 1410±418 ng/ml to about 1425±527 ng/ml

wherein the plurality of controlled release components are free of carbidopa; and

wherein the controlled release dosage form when tested using a USP Type I apparatus at 37° C.±0.5° C. with a rotational speed of 75 rpm and about 900 ml of simulated gastric fluid for 2 hours and pH 6.8 phosphate buffer thereafter, about 75% to about 100% of CD is released within 30 minutes; about 15% to about 45% of LD is released within 30 minutes and not less than 85% of the LD is released after 7 hours;

wherein

the simulated gastric fluid has a pH of from about 1 to about 4.0.