Extended-release topiramate capsules

An extended-release topiramate capsule comprising:

• a capsule shell comprising a single population of coated particles;
• wherein each coated particle comprises a core and a coating thereon;
• wherein each particle core comprises a homogeneous mixture throughout its core, the mixture comprising:
• 10 wt-% to 80 wt-% of topiramate, based on the total weight of an uncoated particle core;
• 10 wt-% to 85 wt-% of one or more filler(s), based on the total weight of an uncoated particle core;
• and
• 1 wt-% to 10 wt-% of one or more binder(s), based on the total weight of an uncoated particle core;
• wherein the coating comprises:
• 45 wt-% to 80 wt-% of one or more release controlling agent(s), based on the total weight of the coating;
• 5 wt-% to 30 wt-% of one or more pore former(s), based on the total weight of the coating;
• and
• 5 wt-% to 30 wt-% of one or more plasticizer(s), based on the total weight of the coating;
• wherein, when a single dose is given to a healthy human subject, an AUC0-inf of 170 to 210 h·μg/mL within a 95% confidence interval, and a Cmax of 2 to 4 μg/mL within a 95% confidence interval are achieved in the subject's plasma.

An extended-release topiramate capsule comprising:

• a capsule shell comprising a single population of coated particles;
• wherein each coated particle comprises a core and a coating thereon;
• wherein each particle core comprises a homogeneous mixture throughout its core, the mixture comprising:
• 10 wt-% to 80 wt-% of topiramate, based on the total weight of an uncoated particle core;
• 10 wt-% to 85 wt-% of one or more filler(s), based on the total weight of an uncoated particle core;
• wherein the one or more filler(s) is selected from the group of microcrystalline cellulose, dibasic calcium phosphate, lactose, tribasic calcium phosphate, mannitol, and combinations thereof;
• and
• 1 wt-% to 10 wt-% of one or more binder(s), based on the total weight of an uncoated particle core;
• wherein the one or more binder(s) is selected from the group of hydroxypropyl methylcellulose, methylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, hydroxypropyl cellulose, hydroxyethylcellulose, polyvinyl pyrrolidine, starch, natural gum, and combinations thereof;
• wherein the coating comprises:
• 45 wt-% to 80 wt-% of one or more release control agent(s), based on the total weight of the coating;
• wherein the one or more release controlling agent(s) is selected from the group of ethylcellulose, polyvinyl acetate, polyacrylate and polymethacrylate, copolymers thereof, and combinations thereof;
• 5 wt-% to 30 wt-% of one or more pore former(s), based on the total weight of the coating;
• wherein the one or more pore former(s) is selected from the group of hypromellose, hydroxypropyl cellulose, methylcellulose, hydroxyethylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, polyethylene glycol, guar gum, xanthan gum, sodium alginate, polyvinylpyrrolidone, crospovidone, sodium starch glycolate, croscarmellose sodium, starch, mannitol, glucose, sucrose, fructose, mannose, galactose, sorbitol, dextran, sodium chloride, potassium chloride, calcium chloride, and combinations thereof;
• and
• 5 wt-% to 30 wt-% of one or more plasticizer(s), based on the total weight of the coating;
• wherein the one or more plasticizer(s) is selected from the group of diethyl phthalate, triethyl citrate, dibutyl sebacate, polyethylene glycol, triacetin, tributyl citrate, glycerol, propylene glycol, and combinations thereof;
• wherein, when a single dose is given to a healthy human subject, an AUC0-inf of 170 to 210 h·μg/mL within a 95% confidence interval, and a Cmax of 2 to 4 μg/mL within a 95% confidence interval are achieved in the subject's plasma.