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US 5,378,474 AGranted
Sustained release pharmaceutical composition
AssigneeF. H. Faulding & Co. Limited
InventorsAngelo M. Morella, Mark C. Fisher
Life of this patent
Estimating the term…
Abstract
The present invention relates to a pharmaceutical pellet composition having a core element including at least one highly soluble active ingredient and a core coating which is partially soluble at a highly acidic pH. The pharmaceutical composition provides a slow release of active ingredient at a highly acidic pH and provides a constant, relatively faster rate of release at a more alkaline pH such as that of the intestine. Oral administration of the pharmaceutical pellet composition of the present invention to a patient is effective to deliver to the blood levels of active ingredient within the therapeutic range and to maintain such levels over an extended period of time.
Claims21
A sustained release pharmaceutical pellet composition for administration to a patient at a predetermined dosage and interval which comprises:
- a core element containing a therapeutically effective amount of at least one active ingredient having an aqueous solubility of at least 1 in 30 and a coating on said core element which comprises the following components:
- (a) from 1 to 85% by weight of a matrix polymer which is insoluble at a pH of from 1 to 7.5 and contributes to the control of the rate of release of the active ingredient in the stomach and intestines;
- (b) from 1 to 30% of an enteric polymer which is substantially insoluble at a pH of from 1 to 4, sufficient to delay the release of the active ingredient in the stomach, but which is soluble at a pH of from 6 to 7.5 so as not to substantially delay release in the intestines;
- (c) from 1 to 60% of a compound soluble at a pH of from 1 to 4, sufficient to enable initiation of release of the active ingredient in the stomach;
- said percentages being by weight based on the total weight of components (a), (b), and (c);
- the ratio of the components (a), (b), and (c) in said coating being such that a dose of the pellet composition delivers to the patient a therapeutically effective amount of said active ingredient over the course of said predetermined interval, so as to maintain an active ingredient blood level at steady state of at least 75% of maximum blood level for more than approximately 4 hours and so that the time at which the active ingredient reaches its maximum concentration is between about 4 and about 30 hours.
3 more elements
A sustained release pharmaceutical pellet composition for administration to a patient at a predetermined dosage and interval which comprises:
- a core element containing as the active ingredient a therapeutically effective amount of an acid addition salt of morphine and a coating on said core element which comprises the following components:
- (a) from 1% to 85% by weight of a matrix polymer which is insoluble at a pH of from 1 to 7.5 and contributes to the control of the rate of release of the active ingredient in the stomach and intestines;
- (b) from 1 to 30% of an enteric polymer which is substantially insoluble at a pH of from 1 to 4, sufficient to delay the release of the active ingredient in the stomach, but which is soluble at a pH of from 6 to 7.5 so as not to substantially delay release in the intestines;
- (c) from 1 to 60% of a compound soluble at a pH of from 1 to 4, sufficient to enable initiation of release of the active ingredient in the stomach;
- said percentages being by weight based on the total weight of components (a), (b), and (c);
- the ratio of the components (a), (b), and (c) in said coating being such that a dose of the pellet composition delivers to the patient a therapeutically effective amount of said active ingredient over the course of said predetermined interval, so as to maintain an active ingredient blood level at steady state of at least 75% of maximum blood level for more than approximately 4 hours and so that the time at which the active ingredient reaches its maximum concentration is between about 4 and about 30 hours.
3 more elements
A sustained release pharmaceutical pellet composition for administration to a patient at a predetermined dosage and interval which comprises:
- a core element containing a therapeutically effective amount of at least one active ingredient having an aqueous solubility of at least 1 in 30 and a coating on said core element which comprises the following components:
- (a) at least 35% by weight of a matrix polymer which is insoluble at a pH of from 1 to 7.5 and is composed of ethyl cellulose, a quaternary ammonium acrylic or methacrylic polymer, an acrylic or a methacrylic ester copolymer or a mixture thereof which contributes to the control of the release of the active ingredient in the stomach and intestines;
- (b) from 1 to 30% of an enteric polymer which is substantially insoluble at a pH of from 1 to 4, sufficient to delay the release of the active ingredient in the stomach, but which is soluble at a pH of from 6 to 7.5 so as not to substantially delay release in the intestines;
- (c) from 1 to 60% of a compound soluble at a pH of from 1 to 4, sufficient to enable initiation of release of the active ingredient in the stomach;
- said percentages being by weight based on the total weight of components (a), (b), and (c);
- the ratio of the components (a), (b), and (c) in said coating being such that a dose of the pellet composition delivers to the patient a therapeutically effective amount of said active ingredient over the course of said predetermined interval, so as to maintain an active ingredient blood level at steady state of at least 75% of maximum blood level for more than approximately 4 hours and so that the time at which the active ingredient reaches its maximum concentration is between about 4 and about 30 hours.
3 more elements
A sustained release pharmaceutical pellet composition for administration to a patient at a predetermined dosage and interval which comprises:
- a core element containing as the active ingredient a therapeutically effective amount of an acid addition salt of morphine and a coating on said core element which comprises the following components:
- (a) at least 35% by weight of a matrix polymer which is insoluble at a pH of from 1 to 7.5 and is composed of ethyl cellulose, a quaternary ammonium acrylic or methacrylic polymer, an acrylic or a methacrylic ester copolymer or a mixture thereof which contributes to the control of the release of the active ingredient in the stomach and intestines;
- (b) from 1 to 30% of an enteric polymer which is substantially insoluble at a pH of from 1 to 4, sufficient to delay the release of the active ingredient in the stomach, but which is soluble at a pH of from 6 to 7.5 so as not to substantially delay release in the intestines;
- (c) from 1 to 60% of a compound soluble at a pH of from 1 to 4, sufficient to enable initiation of release of the active ingredient in the stomach;
- said percentages being by weight based on the total weight of components (a), (b), and (c);
- the ratio of the components (a), (b), and (c) in said coating being such that a dose of the pellet composition delivers to the patient a therapeutically effective amount of said active ingredient over the course of said predetermined interval, so as to maintain an active ingredient blood level at steady state of at least 75% of maximum blood level for more than approximately 4 hours and so that the time at which the active ingredient reaches its maximum concentration is between about 4 and about 30 hours.
3 more elements
Dependencies are inferred from the claim text.