US 12,213,953 B2
Extended release midodrine hydrochloride compositions and methods of use
Yogesh Dandiker, Edina, MN (US); Maulik Kiritkumar Panchal, Maple Grove, MN (US); and Xiao Yu, Maple Grove, MN (US)
Assigned to XENAMED CORP., St. Paul, MN (US)
Appl. No. 16/956,273
Filed by XENAMED CORP., St. Paul, MN (US)
PCT Filed Dec. 21, 2018, PCT No. PCT/US2018/067323
§ 371(c)(1), (2) Date Jun. 19, 2020,
PCT Pub. No. WO2019/126770, PCT Pub. Date Jun. 27, 2019.
Claims priority of provisional application 62/609,842, filed on Dec. 22, 2017.
Claims priority of provisional application 62/618,374, filed on Jan. 17, 2018.
Prior Publication US 2020/0338025 A1, Oct. 29, 2020
Int. Cl. A61K 9/28 (2006.01); A61K 9/20 (2006.01); A61K 9/24 (2006.01); A61K 31/137 (2006.01); A61K 31/165 (2006.01); A61K 31/573 (2006.01); A61K 38/12 (2006.01)
CPC A61K 31/165 (2013.01) [A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2027 (2013.01); A61K 9/205 (2013.01); A61K 9/2054 (2013.01); A61K 9/2081 (2013.01); A61K 9/209 (2013.01); A61K 31/137 (2013.01); A61K 31/573 (2013.01); A61K 38/12 (2013.01)] 18 Claims
 
1. A pharmaceutical composition comprising:
a first release portion comprising an active agent in a range of about 20% to about 40% (w/w) of a total amount of the active agent in the composition;
a second release portion comprising the active agent in a range of about 60% to about 80% (w/w) of the total amount of the active agent in the composition; and
a rate controlling agent, wherein the rate controlling agent is selected from the group consisting of a water-soluble excipient, a water-insoluble excipient, a water permeable excipient, and a combination thereof, and wherein the rate controlling agent is present in a weight ratio of the active agent in the second release portion of the composition to the rate controlling agent of about 1:1 to about 1:30 (w/w);
wherein the in vitro release rate of the active agent, measured by an in vitro dissolution test comprises (i) a first release that is relatively fast and (ii) a second release, wherein the second release does not include a second rise in release rate that takes place about 5 hours to about 10 hours after start of the in vitro dissolution test,
wherein the active agent is selected from the group consisting of midodrine, a pharmaceutically acceptable salt of midodrine, desglymidodrine, a pharmaceutically acceptable salt of desglymidodrine, and any combination thereof; and
wherein the second release comprises a second rise in release rate that takes place about 2 to about 4.5 hours after start of the in vitro dissolution test.