US 10,888,521 B2
Sustained release compositions using wax-like materials
Andrew Xian Chen, San Diego, CA (US); and Patricia D. Kigin, Scottsdale, AZ (US)
Assigned to Farnam Companies, Inc., Phoenix, AZ (US)
Filed by Andrew Xian Chen, San Diego, CA (US); and Patricia D. Kigin, Scottsdale, AZ (US)
Filed on Feb. 29, 2008, as Appl. No. 12/40,443.
Claims priority of provisional application 60/904,456, filed on Mar. 2, 2007.
Prior Publication US 2008/0220079 A1, Sep. 11, 2008
Int. Cl. A61K 9/16 (2006.01); A61K 31/7008 (2006.01); A61K 9/00 (2006.01); A61K 31/522 (2006.01); A61K 31/135 (2006.01); A61P 3/02 (2006.01)
CPC A61K 9/1617 (2013.01) [A61K 9/1652 (2013.01); A61K 9/1694 (2013.01); A61K 31/135 (2013.01); A61K 31/522 (2013.01); A61K 31/7008 (2013.01); A61K 9/0095 (2013.01)] 19 Claims
OG exemplary drawing
 
1. A composition comprising:
(a) an active ingredient, wherein the active ingredient is glucosamine or a pharmaceutically acceptable salt thereof;
(b) from about 5% to about 40% of a wax-like agent, wherein the wax-like agent is hydrogenated vegetable oil; and
(c) from about 5% to about 40% of a spheronizing agent, wherein the ratio of the wax-like agent to the spheronizing agent is in a range from about 3:1 to about 1:14 by weight and; wherein the spheronizing agent is a member selected from the group consisting of microcrystalline cellulose and a combination of microcrystalline cellulose and pregelatinized starch, and wherein the spheronizing agent together with the active ingredient and the wax-like agent form a cohesive plastic mass that is malleable and is subsequently extruded and spheronized;
wherein (i) the composition is in the form of pellets, without a sustained release barrier coating, wherein said pellets have an average diameter of about 0.1 mm to about 3 mm in size and are either spherical or cylindrical in shape; (ii) the composition has an in vitro dissolution rate of the active ingredient measured by standard USP basket method of about 10% to about 60% of the active ingredient released after 1 hour;
about 20% to about 70% of the active ingredient released after 2 hours;
about 30% to about 80% of the active ingredient released after 4 hours;
about 40% to about 90% of the active ingredient released after 8 hours;
about 50% to about 100% of the active ingredient released after 12 hours; and (iii) the in vitro dissolution rate of the active ingredient does not require the presence of a sustained release barrier coating on the pellets.