Pharmaceuticals for oral delivery
Inventors
Carl, Stephen M. • Vrettos, John Stanley • Stern, William
Assignees
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Publication Number
US-9744140-B2
Publication Date
2017-08-29
Expiration Date
Abstract
The present invention provides pharmaceutical compositions suitable for oral delivery and methods of treating subjects in need thereof. The pharmaceutical compositions of the present invention enhance bioavailability of at least one compound classified as BCS Class II, BCS Class III or BCS Class IV.
Core Innovation
The invention provides a solid oral dosage form including at least one active pharmaceutical compound classified as BCS Class III, where the active pharmaceutical compound does not include a peptide bond in the molecular structure of the compound. The dosage form includes an absorption enhancer and coated citric acid particles from 100 mg to 500 mg, where the citric acid particles are coated with a water soluble coat that separates the citric acid from the active pharmaceutical compound and, when added to ten milliliters of 0.1 M aqueous sodium bicarbonate, acidifies the solution to a pH no higher than 5.5.
The dosage form further includes an enteric coating and a water soluble barrier positioned between the mixture and the enteric coating, thereby separating the mixture from the enteric coating. Oral administration of the dosage form provides a synergistic increase in systemic bioavailability of the active pharmaceutical compound compared to administration of a solid dosage form containing an equal dose of the active pharmaceutical compound without the absorption enhancer and the citric acid.
The disclosed use includes orally administering the solid oral dosage form to treat a bacterial infection in a subject in need thereof. The same combination of BCS Class III active compound, an absorption enhancer, coated citric acid particles with the specified water soluble coating behavior, an enteric coating, and a water soluble barrier between the mixture and the enteric coating is described in connection with the stated synergistic increase in systemic bioavailability versus a formulation lacking the absorption enhancer and citric acid.
Claims Coverage
The document includes two independent claims. Both claims are directed to a solid oral dosage form with the same core architecture and a claimed synergistic increase in systemic bioavailability, and the second independent claim additionally recites a method of treating a bacterial infection.
Solid oral dosage form with absorption enhancer, coated citric acid particles, enteric coating, and water soluble barrier for synergistic bioavailability
A solid oral dosage form comprising at least one BCS Class III active pharmaceutical compound without a peptide bond, an absorption enhancer, and coated citric acid particles from 100 mg to 500 mg with a water soluble coat that separates citric acid from the active pharmaceutical compound and acidifies 0.1 M aqueous sodium bicarbonate to pH no higher than 5.5, further comprising an enteric coating and a water soluble barrier positioned between the mixture and the enteric coating, wherein oral administration results in a synergistic increase in systemic bioavailability compared to administration of an equal dose without the absorption enhancer and the citric acid.
Oral method of treating bacterial infection using solid dosage form to achieve synergistic systemic bioavailability
A method of treating a bacterial infection comprising orally administering a solid oral dosage form including a mixture of at least one BCS Class III active antibacterial or antiviral compound without a peptide bond, an absorption enhancer, coated citric acid particles from 100 mg to 500 mg with a water soluble coat that separates citric acid from the active compound and acidifies 0.1 M aqueous sodium bicarbonate to pH no higher than 5.5, an enteric coating, and a water soluble barrier positioned between the mixture and the enteric coating, wherein oral administration results in a synergistic increase in systemic bioavailability compared to administration of an equal dose without the absorption enhancer and the citric acid.
Across both independent claims, the claimed inventive concept centers on combining an absorption enhancer with coated citric acid particles in a solid oral dosage form that is separated from an enteric coating by a water soluble barrier, enabling a claimed synergistic increase in systemic bioavailability of BCS Class III actives compared with the same dose without the absorption enhancer and citric acid. The second independent claim applies this dosage form to treating a bacterial infection.
Stated Advantages
Synergistic increase in systemic bioavailability of the active pharmaceutical compound compared to administration of an equal dose without the absorption enhancer and the citric acid.
Documented Applications
Treating a bacterial infection in a subject in need thereof by orally administering the solid oral dosage form.
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