Modified release pharmaceutical formulations comprising deferiprone
Inventors
Pertile, Marisa • Gazzaniga, Andrea • Cerea, Matteo • CIRILLI, Micol
Assignees
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Publication Number
US-12016850-B2
Publication Date
2024-06-25
Expiration Date
Abstract
The disclosure is directed to pharmaceutical compositions for oral administration comprising deferiprone. In particular, the disclosure is also directed to modified release tablets suitable either for twice daily administration or once daily administration. The disclosure is also directed to methods of making and using the same.
Core Innovation
The invention provides a delayed release tablet comprising a core and an enteric coating, where the core comprises deferiprone and a modifying release agent. The modifying release agent comprises glyceryl esters of long fatty acids, together with a lubricant and/or glidant and additional pharmaceutically acceptable excipients. The tablet is suitable for twice a day oral administration and is characterized by specific dissolution behavior in USP Apparatus Type I basket conditions.
The tablet releases less than about 20% of the deferiprone within 120 minutes at pH 1.2 and releases about 60% or more of the deferiprone within 180 minutes at pH 6.8, as measured by USP Apparatus Type I basket method at 100 rpm in 900 mL at 37°C. This establishes delayed/enteric performance consistent with reduced early release under acidic conditions and increased release under conditions representing later intestinal pH.
The design includes selection of glyceryl ester candidates for the modifying release agent, including glyceryl palmitostearate, glyceryl monostearate, glyceryl dibehenate, or combinations thereof. The enteric coating can comprise specified enteric polymer systems, and the approach is related to improved release reproducibility and reduction of gastric irritation compared with HPMC-AS.
Claims Coverage
The document includes one independent claim describing a delayed release tablet defined by formulation composition, enteric coating, and dissolution performance, with inventive features centered on a specific core composition and controlled dissolution at pH 1.2 and pH 6.8. Dependent claims further refine excipient selection, enteric coating composition, and manufacturing process options, and may restrict to use in specified iron-overload conditions.
Delayed release tablet with deferiprone core and enteric coating
A delayed release tablet comprising a core comprising deferiprone, a modifying release agent comprising glyceryl esters of long fatty acids, a lubricant and/or glidant, and additional pharmaceutically acceptable excipients; and an enteric coating, wherein the tablet is suitable for twice a day oral administration and releases less than about 20% of the deferiprone within 120 minutes at pH 1.2 and about 60% or more within 180 minutes at pH 6.8, measured by USP Apparatus Type I basket method.
Overall, the claim coverage is anchored by a delayed release tablet formulation that combines deferiprone with glyceryl esters of long fatty acids as the modifying release agent and uses an enteric coating to achieve defined dissolution limits at pH 1.2 and pH 6.8 under USP Apparatus Type I basket testing. Dependent refinements specify particular glyceryl ester modifying agents, lubricant/glidant choices, an enteric coating polymer system, and optional preparation routes.
Stated Advantages
Improves release reproducibility compared with HPMC-AS.
Reduces gastric irritation.
Documented Applications
Treatment of iron-overload diseases, including thalassemia, sickle cell anemia, and transfusional iron overload.
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