Agglomerated hydrophilic complexes with multi-phasic release characteristics
AssigneeEdward Mendell Co., Inc.
InventorsAnand R. Baichwal, John N. Staniforth
Life of this patent
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Abstract
The present invention relates to a controlled release formulation which includes a therapeutically active medicament, a heterodisperse gum matrix, a pharmaceutically acceptable diluent, and an effective amount of a pharmaceutically acceptable surfactant and/or wetting agent to provide a multi-phasic controlled release of a therapeutically active medicament. The invention also relates to a method of preparing the same.
Claims19
A controlled release multi-phasic pharmaceutical excipient, comprising:
- a heterodisperse gum matrix comprising a heteropolysaccharide gum and a homopolysaccharide gum capable of cross-linking said heteropolysaccharide in the presence of aqueous solutions, the ratio of said heteropolysaccharide gum to said homopolysaccharide gum being from about 1:3 to about 3:1;
- 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 heterodisperse gum matrix being from about 3:7 to about 7:3;
- and
- from 4 to about 20 percent by weight of a multi-phasic release promoting agent.
A controlled release multi-phasic pharmaceutical excipient, comprising:
- a heterodisperse gum matrix comprising xanthan gum and locust bean gum in a ratio from about 1:3 to about 3:1;
- 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 heterodisperse gum matrix being from about 3:7 to about 7:3;
- and
- from 2 to about 20 percent by weight of a multi-phasic release promoting agent selected from the group consisting of sodium lauryl sulfate, docusate sodium, and mixtures thereof.
A method for preparing a controlled release dosage form which exhibits multi-phasic release of a medicament incorporated therein, comprising:
- preparing a controlled release multi-phasic excipient by mixing (1) a heteropolysaccharide gum and a homopolysaccharide gum capable of cross-linking said heteropolysaccharide gum in the presence of aqueous solutions, such that the ratio of said heteropolysaccharide gum to said homopolysaccharide gum is from about 1:3 to about 3:1, with (ii) 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 heterodisperse gum matrix being from about 3:7 to about 7:3;
- and (iii) from 4 to about 20 percent by weight of a multi-phasic release promoting agent;
- adding a therapeutically effective amount of a medicament to said controlled release multi-phasic excipient;
- and tableting said mixture of controlled release multi-phasic excipient and medicament, said multi-phasic release promoting agent being included in an amount sufficient to provide a multi-phasic release of said medicament from said tablet when said tablet is exposed to aqueous fluids.
A method for preparing a controlled release dosage form which exhibits multi-phasic release of a medicament incorporated therein, comprising:
- preparing a controlled release multi-phasic excipient by mixing (1) xanthan gum and locust bean gum in a ratio of from about 1:3 to about 3:1, with (ii) 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 heterodisperse gum matrix being from about 3:7 to about 7:3;
- and (iii) from 4 to about 20 percent by weight of a multi-phasic release promoting agent selected from the group consisting of sodium lauryl sulfate, docusate sodium, and mixtures thereof;
- adding a therapeutically effective amount of a medicament to said controlled release multi-phasic excipient;
- and
- tableting said mixture of controlled release multi-phasic excipient and medicament, said multi-phasic release promoting agent being included in an amount sufficient to provide a multi-phasic release of said medicament from said tablet when said tablet is exposed to aqueous fluids.
Dependencies are inferred from the claim text.