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Sustained release pharmaceutical composition

  • US 5,330,766 A
  • Filed: 01/21/1993
  • Issued: 07/19/1994
  • Est. Priority Date: 01/06/1989
  • Status: Expired due to Term
First Claim
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1. A method for the preparation of a sustained release pharmaceutical pellet composition for administration to a patient at a predetermined dosage and interval which comprises:

  • forming 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 coating said core element with an admixture of 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, the active ingredient blood level at steady state being at least 75% of maximum blood level for more than approximately 4 hours, and the time for reaching the maximum concentration of the active ingredient being between about 4 and about 30 hours.

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