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-10350240-B2
Publication Date
2019-07-16
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 producing lanthanum dioxycarbonate (LDOC) compounds that include polymorphs of formula La2O2CO3 and/or La2CO5, where the LDOC includes 0.75% by weight or less of sodium and has particles having spherical morphology. The described material approach involves producing lanthanum carbonate hydroxide (LCH) and calcining to convert it to lanthanum oxycarbonate/lanthanum dioxycarbonate (LDOC).
The process uses a water-soluble lanthanum salt with a non-alkali-metal carbonate/bicarbonate, for example ammonium carbonate, and is characterized by reaction parameter constraints including temperature and pH. The approach is described as using carbonate excess and calcining, with resulting LDOC products having improved properties versus prior LDOC made from sodium carbonate.
The described improved properties include spherical morphology, phase purity and polymorph control by matching powder X-ray diffraction (PXRD/PXD) to specific ICDD patterns, higher surface area and porosity, reduced alkali/sodium contamination, and improved phosphate binding kinetics at elevated pH. The material properties are linked to pharmaceutical compositions and oral dosage forms for treating hyperphosphatemia and related chronic kidney disease (CKD) conditions.
Claims Coverage
The partial claim set includes two independent claims: one directed to a lanthanum dioxycarbonate compound and one directed to a pharmaceutical composition. Across the independent claims, the inventive features center on specific LDOC polymorph options and morphology, limited sodium content, specified porosity, and inclusion into defined oral dosage-form categories.
Lanthanum dioxycarbonate polymorph composition with limited sodium and spherical morphology
A lanthanum dioxycarbonate compound that includes a polymorph of formula La2O2CO3, a polymorph of formula La2CO5, or combinations thereof, wherein the compound includes 0.75% by weight or less of sodium, and has particles having spherical morphology.
Pharmaceutical composition with spherical particles and defined pore volume and/or sodium limits in specified oral dosage forms
A pharmaceutical composition comprising an effective amount of one or more lanthanum dioxycarbonate compounds and at least one pharmaceutically acceptable excipient, wherein the lanthanum dioxycarbonate compounds have particles having spherical morphology and have at least one of a pore volume of at least 0.015 cm3/g, or include 0.75% by weight or less of sodium, and wherein the pharmaceutical composition is a dosage form selected from the group consisting of swallow tablets, swallow caplets, compressed dosage forms, swallow hard gelatin capsules, swallow soft gel capsules, orally dissolvable tablets, orally dissolvable caplets, orally dissolvable hard gelatin capsules, orally dissolvable soft gelatin capsules, chewable tablets, chewable caplets, chewable capsules, powders, sprinkles, orally disintegrable films, foods, confections, gums, syrups, suspensions, emulsions, and dispersions.
Overall, the claim coverage ties LDOC polymorph options and spherical particle morphology to controlled sodium content and, in the composition claim, defined porosity via pore volume, then further limits the pharmaceutical composition to specific oral dosage-form categories with an effective amount of the defined LDOC plus a pharmaceutically acceptable excipient.
Stated Advantages
Improved properties versus prior LDOC made from sodium carbonate, including spherical morphology and phase/polymorph control by PXRD matching to specific ICDD patterns.
Reduced alkali/sodium contamination.
Higher surface area and porosity.
Improved phosphate binding kinetics at elevated pH.
Materials properties are linked to pharmaceutical compositions and oral dosage forms for treating hyperphosphatemia and related CKD conditions.
Documented Applications
Treating hyperphosphatemia and related chronic kidney disease (CKD) conditions, including end stage renal disease (ESRD) and secondary hyperparathyroidism, using pharmaceutical compositions in specified oral dosage forms.
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