Lanthanum carbonate hydroxide, lanthanum oxycarbonate and methods of their manufacture and use
Inventors
Gore, Ashok Yeshwant • Dixit, Milind • Mahalingam, Ravichandran • Schauer, Edward A. • Stewart, Matthew • Tandale, Rajendra • Singh, Ramsharan
Assignees
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Publication Number
US-11406663-B2
Publication Date
2022-08-09
Expiration Date
Abstract
The present invention is a method of producing a lanthanum carbonate hydroxide or lanthanum oxycarbonate which has improved properties. The method involves the use of a water soluble lanthanum and a water soluble non-alkali metal carbonate or bicarbonate. The resulting material can be used as a phosphate binder individually or for treating patients with hyperphosphatemia.
Core Innovation
The invention relates to improved manufacture of lanthanum carbonate hydroxide and conversion by calcination to lanthanum oxycarbonate and/or lanthanum dioxycarbonate. It describes using a water-soluble lanthanum salt together with a non-alkali metal carbonate and/or bicarbonate to form lanthanum carbonate hydroxide that is subsequently calcined to lanthanum carbonate/oxycarbonate solids. The approach is directed to producing lanthanum dioxycarbonate materials with controlled composition and particle properties, including spherical morphology and reduced residual sodium or alkali content.
The ammonium-based synthesis yields lanthanum carbonate hydroxide with higher surface area and porosity and a different spherical morphology compared with prior sodium-based routes. The polymorph content is reported as matching PXRD behavior to ICDD 26-815, whereas prior sodium-based methods are associated with ICDD 49-981. The material outputs are characterized in terms of phase and composition limits and properties such as pore volume and BET surface area, including targets for low sodium and constraints related to pore volume.
Calcined lanthanum oxycarbonate and lanthanum dioxycarbonate materials are further associated with improved phosphate binding kinetics at intestinal pH about 6.5. The document reports that phosphate binding behavior differs from lanthanum dioxycarbonate made via earlier sodium-carbonate routes and links phosphate binding performance to physical properties such as BET surface area, pore volume, and morphology. The resulting lanthanum compounds are incorporated into oral dosage forms, with characterization including PXRD, SEM, and N2 adsorption/BJH.
Claims Coverage
The independent claim covers a lanthanum dioxycarbonate material with spherical particles that meets at least one of two compositional or porosity thresholds. The dependent claim set refines the material by additional composition constraints and includes treatment and pharmaceutical composition claims for elevated blood phosphate with enumerated oral dosage forms.
Spherical lanthanum dioxycarbonate meeting sodium or pore-volume thresholds
A lanthanum dioxycarbonate having at least one of 0.75% by weight or less of sodium, or a pore volume of at least 0.015 cm3/g, and having particles with spherical morphology.
Lanthanum dioxycarbonate with sodium and pore-volume thresholds
A lanthanum dioxycarbonate having sodium content of 0.75% by weight or less and a pore volume of at least 0.015 cm3/g.
Treatment of abnormally elevated blood phosphate with a lanthanum dioxycarbonate pharmaceutical composition
A method for treating a condition characterized by abnormally elevated blood phosphate levels by administering a pharmaceutical composition containing an effective amount of lanthanum dioxycarbonate and at least one pharmaceutically acceptable excipient.
Pharmaceutical composition for kidney-related disorders with elevated blood phosphate
The pharmaceutical composition for treating a condition selected from hyperphosphatemia, chronic kidney disease, general kidney failure, end stage renal disease, or chronic renal insufficiency.
Dosage range and La2O2CO3 formula for lanthanum dioxycarbonate-containing compositions
A pharmaceutical composition including lanthanum dioxycarbonate at an amount ranging from about 125 mg to about 20,000 mg, where the lanthanum dioxycarbonate has the formula La2O2CO3.
Oral dosage forms and ingestible formats containing the composition
The pharmaceutical composition provided in oral dosage forms or ingestible formats including tablets, capsules, orally dissolvable forms, chewable forms, powders, films, foods, confections, gums, syrups, and suspension, emulsion, or dispersion preparations.
Across the independent material and dependent claims, the inventive coverage centers on spherical lanthanum dioxycarbonate with low sodium and/or high pore volume, and extends to pharmaceutical compositions for treating abnormally elevated blood phosphate in specified kidney-related conditions using enumerated oral dosage forms. Additional dependents specify La2O2CO3 identity and a defined dosage amount range.
Stated Advantages
Higher surface area and porosity compared with prior sodium-based routes.
Different spherical morphology compared with prior sodium-based routes.
Reduced residual sodium or alkali content.
Improved phosphate binding kinetics at intestinal pH about 6.5.
Phosphate binding behavior differs from lanthanum dioxycarbonate made via earlier sodium-carbonate routes.
Documented Applications
Treatment of a condition characterized by abnormally elevated blood phosphate levels by administering a pharmaceutical composition containing an effective amount of lanthanum dioxycarbonate and pharmaceutically acceptable excipients.
Treatment of hyperphosphatemia and kidney-related disorders selected from chronic kidney disease, general kidney failure, end stage renal disease, or chronic renal insufficiency.
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