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Publication Number
US-8592366-B2
Publication Date
2013-11-26
Expiration Date
Abstract
Acid-containing oral pharmaceutical compositions are provided wherein the pharmaceutical active agents are peptide compounds (i.e., those that include a plurality of amino acids and at least one peptide bond in their molecular structures). Certain barrier layers and/or particulate coated acid are used to reduce any adverse interactions that might otherwise occur between the acid of the compositions and other components of the composition. Use of these barrier layers and/or use of particulate coated acid is believed to promote a more simultaneous release of the components of the composition than is achieved by prior art acid-protection techniques, thus enhancing, and making more consistent, the bioavailability of the active peptide compounds.
Core Innovation
The invention relates to acid-containing oral peptide pharmaceutical compositions in which a physiologically active peptide agent is intermixed with coated acid particles. The coated acid particles comprise at least one pharmaceutically acceptable acid coated with a pharmaceutically acceptable protective coating to separate the acid from the active peptide agent in the composition, while the composition is transported through the stomach by an acid-resistant protective vehicle.
The composition also includes a water-soluble barrier layer that separates the coated acid particles from the protective vehicle, and the active peptide agent and the coated acid particles are in the same layer of the composition. The total acid quantity is defined by a functional pH-lowering test: if added to ten milliliters of 0.1 M aqueous sodium bicarbonate solution, the total acid is sufficient to lower the pH to no higher than 5.5.
The claims further specify pharmaceutically acceptable acids such as citric acid, tartaric acid, or an acid salt of an amino acid, with a protective coating including maltodextrin. The composition also includes a cellulose filler and a pharmaceutical binder for dry compression, while maintaining an acid-resistant protective vehicle effective for oral stomach passage and a water-soluble barrier layer to separate the coated acid particles from the vehicle.
Claims Coverage
Two independent claims define an oral pharmaceutical composition architecture combining coated acid particles, a stomach-protective acid-resistant vehicle, and a water-soluble barrier layer, with a functional total-acid pH-lowering requirement to no higher than pH 5.5 in a sodium bicarbonate test without counteracting base. Across the claims, the independent coverage includes separation of acid from peptide, same-layer intermixed arrangement, defined total-acid function, and specified vehicle/barrier elements.
Intermixed active peptide with coated acid particles separated by protective coating
An active peptide agent intermixed with coated acid particles, the coated acid particles comprising at least one pharmaceutically acceptable acid that is coated with a pharmaceutically acceptable protective coating to separate the acid from the active peptide agent in the composition.
Acid-resistant protective vehicle to prevent stomach protease contact
An acid-resistant protective vehicle effective to transport the pharmaceutical composition through the stomach of a patient while preventing contact between the active peptide agent and stomach proteases.
Water-soluble barrier layer separating coated acid particles from the protective vehicle
A water-soluble barrier layer that separates the coated acid particles from the protective vehicle, wherein the active peptide agent and the coated acid particles are in the same layer of the composition.
Total acid quantity defined by pH-lowering to no higher than 5.5 without counteracting base
Total acid in said pharmaceutical composition is in a quantity which, if added to ten milliliters of 0.1 M aqueous sodium bicarbonate solution, would be sufficient to lower the pH of said solution to no higher than 5.5, and wherein the composition does not include an amount of base which, if released together with the acid, would prevent the pH of said solution from dropping to 5.5 or below.
Specific coated acid selection and same-layer composition arrangement
Coated acid particles comprising citric acid, tartaric acid, or an acid salt of an amino acid that is coated with a pharmaceutically acceptable protective coating, wherein the protective coating separates the acid from the active peptide agent in the composition, and wherein the active peptide agent and the acid are in the same layer of the composition.
The independent claim set covers an oral peptide pharmaceutical composition where the peptide is protected from stomach proteases by an acid-resistant protective vehicle while an acid component is provided as coated acid particles with a protective coating that separates acid from peptide. The composition uses a water-soluble barrier layer to separate coated acid particles from the protective vehicle, places the peptide and coated acid particles in the same layer, and defines total acid by a sodium bicarbonate pH-lowering requirement to no higher than 5.5 without base that would prevent the pH drop.
Stated Advantages
Protects the active peptide agent from contact with stomach proteases while transporting the composition through the stomach.
Total acid is sufficient to lower pH of a sodium bicarbonate solution to no higher than 5.5 without including an amount of base that would prevent the pH from dropping to 5.5 or below.
Documented Applications
Oral delivery of a physiologically active peptide agent to a patient, including stomach passage using an acid-resistant protective vehicle.
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