Delayed release deferiprone tablets and methods of using the same
Inventors
Sherman, Bernard Charles • Spino, Michael
Assignees
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Publication Number
US-11723874-B2
Publication Date
2023-08-15
Expiration Date
Abstract
The invention is directed to pharmaceutical compositions such as tablets that exhibit delayed release properties when administered as either whole or half tablets. The invention is also directed to delayed release tablets comprising deferiprone for oral administration, for which twice daily administration is bioequivalent to the same daily dose of an immediate release tablet administered thrice daily. The invention is also directed to methods of making and using the same.
Core Innovation
The invention relates to orally administering delayed-release deferiprone tablets that include both an enteric coating and an enteric polymer located in the tablet core. The tablets comprise a core having about 1000 mg deferiprone, an enteric polymer in an amount of about 1% to about 5% by weight of the core, a pH adjusting agent, and a glidant. The tablets further comprise an enteric coating that includes a plasticizer, an anti-tacking agent, an opacifying agent, and an enteric polymer.
A further aspect is the use of whole tablets or half tablets, including combinations thereof, while preserving delayed-release behavior after splitting. The core and coating component selections are defined to support delayed-release performance in comparison to immediate-release deferiprone dosing. The document describes in vitro dissolution behavior showing low dissolution in 0.1N HCl and high dissolution at intestinal pH.
The invention is positioned for treating transfusional iron overload using deferiprone in patients with transfusion-related conditions specified in the claims, including thalassemia syndromes and sickle cell disease. Human bioequivalence studies are described, including single-dose and steady-state multiple-dose comparisons, reporting comparable Cmax and AUC between twice daily delayed-release dosing and three times daily immediate-release dosing. The document additionally describes that whole versus half tablet administration is comparable.
Claims Coverage
The document includes three independent claims. All independent claims share the same tablet architecture and the same quantitative core constraints, with claim-to-claim differences primarily directed to the patient population.
Core includes deferiprone with core enteric polymer, pH adjusting agent, and glidant
A tablet comprising a core comprising about 1000 mg deferiprone, an enteric polymer in an amount of about 1% to about 5% by weight of the core, a pH adjusting agent, and a glidant.
Enteric coating includes plasticizer, anti-tacking agent, opacifying agent, and enteric polymer
A tablet comprising an enteric coating comprising a plasticizer, an anti-tacking agent, an opacifying agent, and an enteric polymer.
Treating transfusional iron overload in thalassemia syndromes with the specified tablet
A method for treating transfusional iron overload in a patient with thalassemia syndromes, comprising orally administering to the patient a tablet comprising the defined core and the defined enteric coating.
Treating transfusional iron overload in sickle cell disease with the specified tablet
A method for treating transfusional iron overload in a patient with sickle cell disease, comprising orally administering to the patient a tablet comprising the defined core and the defined enteric coating.
Treating transfusional iron overload with the specified tablet
A method for treating transfusional iron overload, comprising orally administering to the patient a tablet comprising the defined core and the defined enteric coating.
Across the independent claims, coverage is centered on an orally administered tablet with a deferiprone core containing an enteric polymer plus a pH adjusting agent and a glidant, together with an enteric coating containing a plasticizer, an anti-tacking agent, an opacifying agent, and an enteric polymer; the independent claims further assign the treating method to specific patient populations or to transfusional iron overload generally.
Stated Advantages
Comparable Cmax and AUC between twice daily delayed-release tablets and three times daily immediate-release Ferriprox® dosing.
Reduced dissolution in 0.1N HCl and increased dissolution at intestinal pH, supporting delayed-release behavior.
Whole and half tablet comparability in the described human bioequivalence context.
Reduced gastric distress is stated as a target benefit of the described dosing approach.
Documented Applications
Treating transfusional iron overload in patients with thalassemia syndromes by orally administering the delayed-release deferiprone tablet formulation.
Treating transfusional iron overload in patients with sickle cell disease by orally administering the delayed-release deferiprone tablet formulation.
Treating transfusional iron overload by orally administering the delayed-release deferiprone tablet formulation.
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