Sustained release heterodisperse hydrogel systems for insoluble drugs
AssigneeEdward Mendell Co., Inc.
InventorAnand R. Baichwal
Life of this patent
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Abstract
A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.
Claims22
A sustained release composition, comprising:
- an effective amount of a medicament having a solubility of less than about 10 g/l to render a therapeutic effect;
- admixed together with sustained release agglomerated particles comprising a gelling agent, an inert pharmaceutical diluent, the ratio of said inert diluent to said gelling agent being from about 1:8 to about 8:1, and a hydrophobic material selected from the group consisting of an alkylcellulose, a hydrophobic cellulosic material, a copolymer of acrylic and methacrylic acid esters, shellac, waxes, zein and mixtures of any of the foregoing, said hydrophobic material being included in an amount effective to slow the hydration of said gelling agent when said dosage form is exposed to an environmental fluid.
A sustained release oral solid dosage form for absorption of a therapeutically active medicament in the gastrointestinal tract, comprising:
- an effective amount of a medicament having a solubility of less than about 10 g/l to render a therapeutic effect;
- and
- a sustained release excipient comprising a gelling agent, an inert pharmaceutical diluent selected from the group consisting of monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert diluent to said gelling agent being from about 1:8 to about 8:1, said gelling agent and said inert pharmaceutical diluent being granulated with a hydrophobic material selected from the group consisting of an alkylcellulose, a hydrophobic cellulosic material, a copolymer of acrylic and methacrylic acid esters, shellac, waxes, zein and mixtures of any of the foregoing, prior to the incorporation of said medicament, said hydrophobic polymer being included in an amount effective to slow the hydration of said gelling agent when said dosage form is exposed to an environmental fluid.
A sustained release oral solid dosage form for absorption of a therapeutically active medicament in the gastrointestinal tract, comprising:
- an effective amount of a medicament having a solubility of less than about 10 g/l to render a therapeutic effect;
- and
- a sustained release excipient comprising xanthan gum, locust bean gum, an inert pharmaceutical diluent selected from the group consisting of monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert diluent to the total amount of said xanthan gum and said locust bean gum being from about 1:8 to about 8:1;
- and a hydrophobic material selected from the group consisting of an alkylcellulose, a hydrophobic cellulosic material, a copolymer of acrylic and methacrylic acid esters, shellac, waxes, zein and mixtures of any of the foregoing, said hydrophobic material being included in an amount effective to slow the hydration of said gelling agent when said dosage form is exposed to an environmental fluid.
A sustained release composition, comprising agglomerated particles comprising
- an effective amount of a medicament having a solubility of less than about 10 g/l to render a therapeutic effect;
- a gelling agent;
- an inert pharmaceutical diluent, the ratio of said inert diluent to said gelling agent being from about 1:8 to about 8:1;
- and
- a hydrophobic material selected from the group consisting of an alkylcellulose, a hydrophobic cellulosic material, a copolymer of acrylic and methacrylic acid esters, shellac, waxes, zein and mixtures of any of the foregoing, said hydrophobic polymer being included in an amount from about 1% to about 10% by weight of said composition.
A sustained release oral solid dosage form for providing an effective dose of nifedipine over a 24 hour period, comprising
- from about 20 mg to about 90 mg of nifedipine;
- xanthan gum and locust bean gum in a ratio from about 1:3 to about 3:1;
- an inert pharmaceutical diluent, the ratio of said inert diluent to the total amount of said xanthan gum and said locust bean gum being from about 1:8 to about 8:1;
- and
- a hydrophobic material selected from the group consisting of an alkylcellulose, a hydrophobic cellulosic material, a copolymer of acrylic and methacrylic acid esters, shellac, waxes, zein and mixtures of any of the foregoing, said hydrophobic polymer being included in an amount from about 1% to about 10% by weight of said dosage form.
Dependencies are inferred from the claim text.