A sustained release composition comprising a methylcellulose
AssigneeDdp Specialty Electronic Materials US, LLC
InventorOliver Petermann
Life of this patent
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Abstract
A sustained release composition for oral administration comprises a physiologically active ingredient mixed with a methylcellulose, wherein the methylcellulose has anhydroglucose units joined by 1-4 linkages and wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that the s23/s26 is 0.27 or less, the composition further comprising a liquid diluent in a weight ratio of liquid diluent to active ingredient in the range of 0:1 to 0.85:1.
Claims16
A sustained release composition for oral administration comprising a physiologically active ingredient mixed with a methylcellulose, wherein
- the methylcellulose has anhydroglucose units joined by 1-4 linkages and wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that the s23/s26 is 0.27 or less,
- wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and
- wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups,
- the composition further comprising a liquid diluent in a weight ratio of liquid diluent to active ingredient in the range of 0:1 to 0.85:1.
Use of a methylcellulose composed of anhydroglucose units joined by 1-4 linkages, wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that the s23/s26 is 0.27 or less,
- wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and
- wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups,
- as an excipient of a polymeric matrix providing sustained release of an active ingredient from an oral solid dosage form.
A process for preparing a sustained release composition for oral administration comprising a physiologically active ingredient mixed with a methylcellulose, the process comprising
- (a) providing a solution of methylcellulose in a liquid diluent,
- (b) mixing the active ingredient in powder or crystalline form and optionally one or more solid excipients with the solution of methylcellulose in a weight ratio of liquid diluent to solids of 0.1:1 to 0.85:1, and
- (c) optionally drying the mixture of step (b) to a liquid content of less than 10% by weight of the mixture,
- said methylcellulose being composed of anhydroglucose units joined by 1-4 linkages,
- wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that the s23/s26 is 0.27 or less,
- wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and
- wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups.
Dependencies are inferred from the claim text.