Extended release compositions comprising pyridostigmine
AssigneeKashiv Biosciences, LLC
InventorsSiva Ram Kiran Vaka, Namdev B. Shelke, Dipen Desai, Wantanee Phuapradit, Navnit H. Shah
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Abstract
Extended release pyridostigmine dosage forms, suitable for maintaining stable plasma concentrations with reduced or minimized initial burst release/dose dumping of pyridostigmine, are provided. The dosage forms include matrix tablets, gastroretentive tablets, and pellets, the latter being suitable for dosing in capsules, tablets, and sachets, as well as for sprinkling on foodstuffs. The disclosure also provides methods for improving patient compliance by administering once-a-day extended release pyridostigmine bromide dosage forms that provide a superior controlled drug release.
Claims18
A method for treatment of myasthenia gravis comprising once a day administration of a gastroretentive dosage form comprising an immediate release layer and an extended release component to a person in need of treating myasthenia gravis;
- wherein the immediate release layer comprises between about 10 mg and about 60 mg pyridostigmine bromide;
- and the extended release component comprises a core and a permeable elastic membrane surrounding the core,
- wherein the core comprises between about 50 mg and about 400 mg pyridostigmine bromide, hypromellose in an amount of between about 5 wt % and about 35 wt %, based on the total weight of the core, succinic acid, a carbonate salt, and a bicarbonate salt,
- wherein the permeable elastic membrane comprises a plasticizer in an amount of between about 5 wt % and about 25 wt % of the membrane, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride in powder form (1:2:0.2), in an amount of between about 75 wt % and about 95 wt % of the membrane, and
- wherein the dosage form provides an extended release of pyridostigmine bromide for at least about 14 hours.
A method for treatment of myasthenia gravis comprising once a day administration of a gastroretentive dosage form comprising an immediate release layer and an extended release component to a person in need of treating myasthenia gravis;
- wherein the immediate release layer comprises between about 10 mg and about 60 mg pyridostigmine bromide;
- and the extended release component comprises a core and a permeable elastic membrane surrounding the core,
- wherein the core comprises between about 50 mg and about 400 mg pyridostigmine bromide, a high viscosity hypromellose in an amount of between about 5 wt % and about 35 wt %, based on the total weight of the core, succinic acid, a carbonate salt, and a bicarbonate salt,
- wherein the high viscosity hypromellose has a viscosity of between about, 2,700 mPa·s and about 5,040 mPa·s,
- wherein each of sodium bicarbonate and calcium carbonate is present in equimolar amounts with respect to succinic acid,
- wherein each of sodium bicarbonate, calcium carbonate, and succinic acid is present in an amount of between about 1 wt % and about 10 wt %, based on the total weight of the core,
- wherein the permeable elastic membrane comprises a plasticizer in an amount of between about 5 wt % and about 25 wt % of the membrane composition, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride in powder form (1:2:0.2), in an amount of between about 75 wt % and about 95 wt % of the membrane composition, and
- wherein the dosage form floats in about 40 minutes or less in pH 4.5 acetate buffer with 100 mM NaCl.
A method for treatment of myasthenia gravis comprising once a day administration of a gastroretentive dosage form comprising a core and a permeable elastic membrane surrounding the core to a person in need of treating myasthenia gravis,
- wherein the core comprises between about 50 mg and about 400 mg pyridostigmine bromide, hypromellose in an amount of between about 5 wt % and about 35 wt %, based on the total weight of the core, succinic acid, a carbonate salt, and a bicarbonate salt,
- wherein the hypromellose has a viscosity of between about, 2,700 mPa·s and about 5,040 mPa·s,
- wherein each of sodium bicarbonate and calcium carbonate is present in equimolar amounts with respect to succinic acid,
- wherein each of sodium bicarbonate, calcium carbonate, and succinic acid is present in an amount of between about 1 wt % and about 10 wt %, based on the total weight of the core,
- wherein the permeable elastic membrane comprises a plasticizer in an amount of between about 5 wt % and about 25 wt % of the membrane composition, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride in powder form (1:2:0.2), in an amount of between about 75 wt % and about 95 wt % of the membrane composition,
- wherein the dosage form floats in about 40 minutes or less in pH 4.5 acetate buffer with 100 mM NaCl, and
- wherein the dosage form provides an extended release of pyridostigmine bromide for at least about 14 hours.
Dependencies are inferred from the claim text.