Extended release compositions comprising pyridostigmine
AssigneeAmneal Complex Products Research 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 gastroretentive dosage form comprising an immediate release portion and an extended release portion,
- wherein the immediate release portion comprises an immediate release drug layer containing pyridostigmine or a pharmaceutically acceptable salt thereof,
- wherein the extended release portion comprises a core, and a permeable elastic membrane comprising at least one orifice and surrounding the core,
- wherein the core comprises pyridostigmine or a pharmaceutically acceptable salt thereof, an acid, a gas-generating agent, and a swellable water-soluble hydrophilic polymer,
- wherein the permeable elastic membrane comprises a plasticizer and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride,
- wherein the copolymer is present in an amount of from about 70 wt % to about 95 wt % based on the total weight of the membrane.
An extended release gastroretentive pyridostigmine tablet comprising a core, and a permeable elastic membrane containing at least one orifice and, surrounding the core,
- wherein the core comprises pyridostigmine or a pharmaceutically acceptable salt thereof, an acid, a gas-generating agent, and a swellable water-soluble hydrophilic polymer,
- wherein the permeable elastic membrane comprises a plasticizer and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride,
- wherein the copolymer is present in an amount of from about 70 wt % to about 95 wt % based on the total weight of the membrane.
A therapeutic method for treating myasthenia gravis, the method comprising orally administering to a subject in need thereof a gastroretentive pyridostigmine tablet,
- wherein the tablet comprises an immediate release portion and an extended release portion,
- wherein the immediate release portion comprises an immediate release drug layer containing pyridostigmine or a pharmaceutically acceptable salt thereof,
- wherein the extended release portion comprises a core, and a permeable elastic membrane comprising at least one orifice and surrounding the core,
- wherein the core comprises pyridostigmine or a pharmaceutically acceptable salt thereof, an acid, a gas-generating agent, and a swellable, water-soluble hydrophilic polymer,
- wherein the permeable elastic membrane comprises a plasticizer and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride,
- wherein the copolymer is present in an amount of from about 70 wt % to about 95 wt % based on the total weight of the membrane.
A method for reducing GI side effects in a patient in need of a pyridostigmine composition, the method comprising:
- administering to the patient a gastroretentive pyridostigmine composition comprising an immediate release portion and an extended release portion, as a single tablet/day,
- wherein the immediate release portion comprises an immediate release drug layer containing pyridostigmine or a pharmaceutically acceptable salt thereof,
- wherein the extended release portion comprises a core, and a permeable elastic membrane containing at least one orifice surrounding the core,
- wherein the core comprises pyridostigmine or a pharmaceutically acceptable salt thereof, an acid, a gas-generating agent, and a swellable, water-soluble hydrophilic polymer,
- wherein the permeable elastic membrane comprises a plasticizer and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride,
- wherein the copolymer is present in an amount of from about 70 wt % to about 95 wt % based on the total weight of the membrane,
- wherein the composition provides an extended release of pyridostigmine or a pharmaceutically acceptable salt thereof for at least about 14 hours, and
- wherein the composition releases less than about 35% of pyridostigmine or a pharmaceutically acceptable salt thereof, within two hours of dissolution of the composition in 900 ml of dissolution medium comprising pH 5 buffer and 150 mM NaCl, measuring using USP Apparatus I, at 100 rpm and 37° C.
Dependencies are inferred from the claim text.