Phosphorus binder composition for treatment of hyperphosphatemia
Inventors
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-8759398-B2
Publication Date
2014-06-24
Expiration Date
Abstract
The present invention relates to oral pharmaceutical products which are useful for binding phosphorus in ingesta, and inhibiting absorption of phosphorus from the gastrointestinal tract of subjects. A method for binding phosphorus in ingesta and inhibiting its absorption from the gastrointestinal tract is also provided. The pharmaceutical products and methods of the present invention are particularly useful in the treatment of hyperphosphatemia of chronic uremia and reducing serum phosphorus levels in patients requiring such therapy.
Core Innovation
The invention relates to oral phosphate-binding compositions for inhibiting absorption of phosphorus-containing anions from the gastrointestinal tract of a subject. The compositions include a source of ionized calcium, a stool softener, and a non-gelatin capsule, and the source of ionized calcium is a calcium succinate composition. The approach is directed to treating hyperphosphatemia associated with chronic uremia and chronic kidney disease (CKD).
The quantity of the calcium succinate composition provides ionized calcium in a quantity sufficient to bind with phosphorus-containing anions in the gastrointestinal tract of the subject. The stool softener is selected from docusate and lactulose and is provided in an amount sufficient to reduce the incidence of constipation but not sufficient to increase the incidence of diarrhea.
The composition is characterized by stool softener compatibility and manufacturability constraints. The stool softener does not interfere with the binding of phosphorus-containing anions by ionized calcium and does not interfere with the manufacture of the composition. Dissolution of the composition in water at 37°C under U.S. Pharmacopeia Apparatus II conditions releases at least about 80% of the calcium as ionized calcium in 30 minutes.
Claims Coverage
The independent claim is directed to an oral phosphate-binding composition that inhibits absorption of phosphorus-containing anions from the gastrointestinal tract using ionized calcium from calcium succinate in combination with a stool softener, together with non-gelatin capsule form and dissolution-release requirements. A refinement adds a quantitative dosing constraint for ionized calcium per unit dose, for a total of four inventive features.
Calcium succinate ionized calcium with stool softener in non-gelatin capsule
A composition for inhibiting absorption of phosphorus-containing anions from the gastrointestinal tract of a subject consisting of a source of ionized calcium, a stool softener, and a non-gelatin capsule, wherein the source of ionized calcium is a calcium succinate composition and the quantity provides ionized calcium sufficient to bind with the phosphorus-containing anions.
Constipation-reducing stool softener without diarrhea increase and compatibility
The quantity of the stool softener is sufficient to reduce the incidence of constipation but not sufficient to increase the incidence of diarrhea, wherein the stool softener is selected from docusate and lactulose, and wherein the stool softener does not interfere with the binding of the phosphorus-containing anions by the ionized calcium and does not interfere with the manufacture of the composition.
Dissolution releasing ionized calcium from the composition
Dissolution of the composition in water at 37°C stirred at 50 RPM under the dissolution conditions described in U.S. Pharmacopeia for Apparatus II releases at least about 80% of the calcium in the composition as ionized calcium in 30 minutes.
Quantified ionized calcium per unit dose
A unit dose provides between 3 and 200 milliequivalents of ionized calcium.
Across the independent claim and its refinement, the inventive subject matter centers on inhibiting absorption of phosphorus-containing anions using ionized calcium derived from calcium succinate, paired with a docusate or lactulose stool softener sized to reduce constipation without increasing diarrhea, while maintaining phosphate binding and manufacturability, and achieving release of at least about 80% of calcium as ionized calcium within a defined Apparatus II dissolution time. The refinement further constrains ionized calcium delivered per unit dose.
Stated Advantages
Reduces the incidence of constipation without increasing the incidence of diarrhea.
Does not interfere with the binding of phosphorus-containing anions by ionized calcium.
Does not interfere with the manufacture of the composition.
Releases at least about 80% of calcium as ionized calcium in 30 minutes under the stated dissolution conditions.
Documented Applications
Treating hyperphosphatemia in subjects with chronic uremia and chronic kidney disease (CKD) by inhibiting absorption of phosphorus-containing anions from the gastrointestinal tract.
Interested in licensing this patent?