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US 10,881,617 B1Granted
Extended release compositions comprising pyridostigmine
AssigneeKashiv Biosciences, LLC
InventorsSiva Ram Kiran Vaka, Namdev B. Shelke, Dipen Desai, Wantanee Phuapradit, Navnit H. Shah
Life of this patent
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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.
Claims17
A gastroretentive dosage form comprising an immediate release layer and an extended release component;
- wherein the immediate release layer comprises between about 10 mg and about 60 mg pyridostigmine bromide;
- and the extended release component comprises a core, a permeable elastic membrane surrounding the core, and an orifice passing through the permeable elastic membrane,
- 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 40 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, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride (1:2:0.2),
- wherein the copolymer is present in an amount of between about 70 wt % and about 95 wt % of the membrane composition,
- wherein the plasticizer is present in an amount of between about 5 wt % and about 25 wt % of the membrane composition, and
- wherein the dosage form provides an extended release of pyridostigmine bromide for at least about 14 hours.
4 more elements
A gastroretentive dosage form comprising an immediate release layer and an extended release component;
- wherein the immediate release layer comprises between about 10 mg and about 60 mg pyridostigmine bromide;
- and the extended release component comprises a core, a permeable elastic membrane surrounding the core, and an orifice passing through the permeable elastic membrane,
- 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 40 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, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride (1:2:0.2),
- wherein the copolymer is present in an amount of between about 70 wt % and about 95 wt % of the membrane composition,
- wherein the plasticizer is present in an amount of between about 5 wt % and about 25 wt % of the membrane composition, and
- wherein the dosage form, when administered into a dissolution medium comprising 0.001 N HCl and 10 mM NaCl, exhibits about 100% volume gain within about 30 minutes post-administration of the tablet into the dissolution medium.
4 more elements
A gastroretentive dosage form comprising an immediate release layer and an extended release component;
- wherein the immediate release layer comprises between about 10 mg and about 60 mg pyridostigmine bromide;
- and the extended release component comprises a core, a permeable elastic membrane surrounding the core, and an orifice passing through the permeable elastic membrane,
- 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 40 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, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride (1:2:0.2),
- wherein the copolymer is present in an amount of between about 70 wt % and about 95 wt % of the membrane composition,
- wherein the plasticizer is present in an amount of between about 5 wt % and about 25 wt % of the membrane composition, and
- wherein the dosage form, when administered into a dissolution medium comprising 0.001 N HCl and 10 mM NaCl, can withstand a compression force of at least 15N for about 8 hours post-administration, and can withstand a compression force of about ION or less at about 14 hours post-administration.
4 more elements
A gastroretentive dosage form comprising an immediate release layer and an extended release component;
- wherein the immediate release layer comprises between about 10 mg and about 60 mg pyridostigmine bromide;
- and the extended release component comprises a core, a permeable elastic membrane surrounding the core, and an orifice passing through the permeable elastic membrane,
- 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 40 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, and a copolymer based on ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride (1:2:0.2),
- wherein the copolymer is present in an amount of between about 70 wt % and about 95 wt % of the membrane composition,
- wherein the plasticizer is present in an amount of between about 5 wt % and about 25 wt % of the membrane composition, and
- wherein the dosage form, when administered into a dissolution medium comprising pH 4.5 acetate buffer and 10 mM NaCl, exhibits at least about 150% volume gain on floatation.
3 more elements
Dependencies are inferred from the claim text.