Highly compactable and durable direct compression excipients and excipient systems
Inventors
Tillotson, John • Propst, Cecil
Assignees
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Publication Number
US-11672763-B2
Publication Date
2023-06-13
Expiration Date
Abstract
The present invention relates to solid dispersions including, but not limited to, co-processed carbohydrates with different solubilities and concentrations, which have a microcrystalline plate structure. The solid dispersions, excipient systems and formulations of the present invention are highly compactable and durable and when compressed into solid dosage forms demonstrate uniform densification, low friability at low pressures, and and/or relatively constant low disintegration times at various hardnesses. The solid dosage forms of the present invention demonstrate superior organoleptics, disintegration, and/or robustness.
Core Innovation
The invention is directed to a solid dispersion comprising a combination of at least three polyols having different solubilities in water and/or concentrations, wherein the at least three polyols are co-spray dried to form a microcrystalline plate structure. The structure includes layered crystalline and/or eutectic amorphous deposits, with distinct zones comprising a core zone, a transition zone, and a surface zone. The zones are defined by co-crystallization relationships between first, second, and third polyols within the microcrystalline plate structure.
In the microcrystalline plate structure, the core zone comprises a first polyol, the transition zone comprises a second polyol co-crystallized with the first polyol, and the surface zone comprises a third polyol co-crystallized with the first polyol and the second polyol. The solid dispersion further includes about 5 wt % to about 25 wt % disintegrant. When the solid dispersion is compressed into a solid dosage form, it has a defined hardness and disintegrates in an oral cavity in less than about 30 seconds upon being placed in the oral cavity.
The related invention also provides a solid dosage form comprising an active ingredient and the solid dispersion, while maintaining the microcrystalline plate structure with crystalline and/or eutectic amorphous deposits and the distinct core/transition/surface zones defined by which polyol co-crystallizes. The solid dosage form has a hardness between about 13 kP and about 40 kP under a compression force between about 13 kN and about 35 kN, and disintegrates in the oral cavity in less than about 30 seconds.
Claims Coverage
The partial content provides two independent claims: a solid dispersion and a solid dosage form. Across the independent claims, the coverage centers on a co-spray dried multi-polyol microcrystalline plate structure with layered crystalline and/or eutectic amorphous deposits, distinct core/transition/surface zones, a defined disintegrant range, and oral disintegration and hardness constraints.
Co-spray dried multi-polyol microcrystalline plate structure
A solid dispersion wherein at least three polyols with different solubilities in water and/or concentrations are co-spray dried, producing a microcrystalline plate structure comprising layers of crystalline and/or eutectic amorphous deposits.
Distinct core, transition, and surface zones by polyol co-crystallization
The solid dispersion comprises distinct zones including a core zone with a first polyol, a transition zone with a second polyol co-crystallized with the first polyol, and a surface zone with a third polyol co-crystallized with the first polyol and the second polyol.
Disintegrant amount combined with hardness and oral disintegration performance
The solid dispersion further comprises about 5 wt % to about 25 wt % disintegrant and, when compressed into a solid dosage form, has a hardness between about 13 kP and about 40 kP under a compression force between about 13 kN and about 35 kN, and disintegrates in an oral cavity in less than about 30 seconds.
Solid dosage form with active ingredient using the defined solid dispersion
A solid dosage form comprising an active ingredient and the solid dispersion defined by at least three co-spray dried polyols forming a microcrystalline plate structure with distinct core/transition/surface zones, about 5 wt % to about 25 wt % disintegrant, hardness between about 13 kP and about 40 kP under about 13 kN to about 35 kN, and oral-cavity disintegration in less than about 30 seconds.
Taken together, the independent claims require a co-spray dried dispersion of at least three polyols forming a microcrystalline plate structure with layered crystalline and/or eutectic amorphous deposits and distinct core/transition/surface zones defined by polyol co-crystallization, along with an explicit disintegrant range and correlated hardness and oral-cavity disintegration performance. The solid dosage form additionally requires an active ingredient.
Stated Advantages
Highly compactable and durable tablets with uniform densification.
Low friability at low compression pressures.
Relatively constant or fast oral disintegration time across hardness.
Documented Applications
Solid dosage forms for oral cavity use, including fast disintegrating tablets, orally dispersible tablets, chewable tablets, swallow tablets, and lozenges.
Taste-mask or modified-release coated applications, where coating integrity is preserved during compaction.
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