Stable non-disintegrating dosage forms and method of making same
First Claim
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1. A method of making a pharmacologically active dosage, comprising:
- (a) spray coating a plurality of substrates, comprising particles including at least one pharmacologically active agent, with a neutral lipid-based coating in an amount to provide microencapsulates having an active agent concentration at least about 50%; and
(b) directly compressing said microencapsulates resulting from step (a) in an amount of at least about 50% by weight microencapsulate to form a shelf stable non-disintegrable pharmacologically active dosage unit, which releases said active agent by dissolution over the therapeutic range.
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Abstract
The present invention is a stable, non-disintegrable dosage form which combines the benefits of a microencapsulated substrate with the convenience of direct compression. The present invention is also directed to methods for producing directly compressed microencapsulated dosage forms to provide modified release and dosage form stability. The dosage unit can have a high active load.
36 Citations
108 Claims
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1. A method of making a pharmacologically active dosage, comprising:
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(a) spray coating a plurality of substrates, comprising particles including at least one pharmacologically active agent, with a neutral lipid-based coating in an amount to provide microencapsulates having an active agent concentration at least about 50%; and (b) directly compressing said microencapsulates resulting from step (a) in an amount of at least about 50% by weight microencapsulate to form a shelf stable non-disintegrable pharmacologically active dosage unit, which releases said active agent by dissolution over the therapeutic range. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54)
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55. A pharmacologically active dosage unit comprising:
a compressed non-disintegrable tablet comprising a plurality of substrates microencapsulated in a neutral lipid-based coating, said substrates comprising at least one pharmacologically active ingredient in an amount to provide a concentration of active agent of at least about 50% in said microencapsulate, and said microencapsulate included in said dosage unit in an amount of at least 50% by weight of said dosage unit such that said active ingredient exhibits modified release by dissolution throughout the therapeutic range prescribed for treating a patient in need of said active ingredient. - View Dependent Claims (56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107)
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108. A pharmacologically active dosage unit comprising:
a compressed non-disintegrable tablet comprising a plurality of substrates microencapsulated in a neutral lipid-based coating, said substrates comprising at least one pharmacologically active ingredient in an amount to provide a concentration of active agent of at least about 50% in said microencapsulate, and said microencapsulate included in a one-component dosage unit in an amount of at least 50% by weight of said dosage unit such that said active ingredient exhibits modified release by dissolution throughout the therapeutic range prescribed for treating a patient in need of said active ingredient.
Specification