US 11,701,350 B2
Dextromethorphan extended release pharmaceutical composition
Kiran Kumar Muppireddy, Portage, MI (US); Inderdeep Singh Bhatia, Kalamazoo, MI (US); Eric Cristopher Pattok, Grand Rapids, MI (US); Carlos O. Paz, Fairview, NJ (US); Bruce Duane Johnson, Byron Center, MI (US); and Lisa Kay Lupton, Kalamazoo, MI (US)
Assigned to L. PERRIGO COMPANY, Allegan, MI (US)
Filed by L. Perrigo Company, Allegan, MI (US)
Filed on Jul. 22, 2020, as Appl. No. 16/935,661.
Claims priority of provisional application 62/876,934, filed on Jul. 22, 2019.
Prior Publication US 2021/0023073 A1, Jan. 28, 2021
Int. Cl. A61K 31/485 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01)
CPC A61K 31/485 (2013.01) [A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2027 (2013.01); A61K 9/2031 (2013.01); A61K 9/2054 (2013.01); A61K 9/2826 (2013.01); A61K 9/2853 (2013.01)] 13 Claims
OG exemplary drawing
 
1. A sustained release pharmaceutical tablet composition comprising:
a) a core tablet sustained release formulation comprising
i. dextromethorphan HBr in an amount selected from about 12.50%, 17.44%, 18.40%, 23.26%, 23.28%, 23.37%, 23.50%, 23.83%, 25.00%, 25.75%, 26.02%, 26.67%, and 28.17% by weight of the composition;
ii. hydroxypropyl methylcellulose having an apparent viscosity of from about 2,663 to about 4,970 mPa·s at 2 wt % in water, a methyl substitution between about 22.0% and 24.0%, and a hydroxypropyl substitution between about 7.5% and 9.5%, in an amount selected from the group consisting of about 8.33%, 8.58%, 8.89%, 9.12%, 9.13%, 9.17%, 9.22%, 9.29%, 9.39%, 9.52%, 12.27%, 14.08%, 15.89%, 16.67%, 17.17%, 17.44%, 17.78%, 18.40%, 18.78%, 22.39%, 25.00%, 27.50%, 33.33%, and 33.91% by weight of the composition;
iii. hydroxypropyl methylcellulose having an apparent viscosity of from about 13,275 to about 24,780 mPa·s, a methyl substitution between about 22.0% and 24.0%, and a hydroxypropyl substitution between about 8.5% and 10.5%, in an amount selected from the group consisting of about 8.33%, 9.12%, 9.13%, 9.17%, 9.29%, 9.39%, 9.52%, 12.22%, 12.50%, 12.88%, 13.33%, 14.08%, 15.67%, 15.89%, 16.67%, 17.17%, 17.44%, 17.78%, 18.40%, 18.78%, and 23.01% by weight of the composition;
iv. lactose monohydrate in an amount selected from about 14.89%, 17.24%, 17.30%, 17.82%, 18.45%, 19.49%, 19.60%, 22.25%, 22.64%, 23.25%, 23.55%, 23.75%, 23.76%, 24.00%, 24.67%, 25.02%, 25.41%, 25.87%, 26.23%, 26.32%, 27.73%, 27.80%, 29.73%, 29.74%, 29.86%, 29.99%, 30.28%, 30.60%, and 40.67% by weight of the composition;
v. microcrystalline cellulose in an amount selected from about 0%, 13.53%, 15.46%, 15.89%, 16.67%, 17.22%, 17.39%, 18.14%, 18.22%, 19.24%, 19.31%, 19.60%, 20.21%, 20.34%, 20.65%, 20.67%, 20.75%, 20.84%, 20.95%, 21.04%, 21.26%, 21.70%, 23.25%, 23.61%, 25.47%, 26.23%, 26.59%, and 30.37% by weight of the composition;
vi. fumed silica in an amount selected from about 0.33%, 0.35%, 0.45%, 0.46%, 0.47%, 0.48%, 0.49%, or 0.50% by weight of the composition; and
vii. magnesium stearate in an amount selected from about 0.35%, 0.49%, 0.50%, 0.67%, 0.69%, 0.70%, 0.71%, 0.72%, 0.73%, and 0.75% by weight of the composition;
b) optionally, an active coating comprising:
i. dextromethorphan or a pharmaceutically acceptable salt thereof in an amount selected from about 1.86%, 4.11%, 4.12%, 4.15%, and 4.21% by weight of the composition;
ii. hydroxypropyl methylcellulose having an apparent viscosity range of about 2.4-7 mPa·s at 2 wt % in water, a methyl substitution range of about 28.0%-30.0%, and a hydroxypropyl substitution range of about 7.0%-12.0% in an amount selected from about 0%, 0.41%, 0.47%, and 0.91% by weight of the composition;
iii. polyvinyl pyrrolidone in an amount selected from about 0%, 0.41%, 0.91%, 1.37%, and 1.38% by weight of the composition;
iv. sodium lauryl sulfate in an amount selected from about 0%, 0.004%, 0.01%, and 0.06% by weight of the composition;
v. PEG 400 or PEG 8000 in an amount selected from about 0%, 0.20%, and 0.46% by weight of the composition;
and c) the film coating is absent or comprises a polymer and a plasticizer;
wherein the tablet has a volume of from about 0.0063 in3 to about 0.0183 in3, a surface area of from about 0.194 in2 to about 0.395 in2, and a surface area to volume ratio of from about 19.4 in−1 to about 31.0 in−1.