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Assignees
Member
VitalisVitalis develops infrastructure for integrating, resolving, and analyzing health data streams from multiple sources such as wearables, sensors, labs, and medical records to create a unified longitudinal health record. Initially focused on brain health and cumulative exposure monitoring, Vitalis emphasizes consent-driven, secure, and research-ready data practices. The platform is vendor-agnostic, supporting data portability, user privacy, and adaptability to high-stakes operational environments.
Vitalis develops infrastructure for integrating, resolving, and analyzing health data streams from multiple sources such as wearables, sensors, labs, and medical records to create a unified longitudinal health record. Initially focused on brain health and cumulative exposure monitoring, Vitalis emphasizes consent-driven, secure, and research-ready data practices. The platform is vendor-agnostic, supporting data portability, user privacy, and adaptability to high-stakes operational environments.
Publication Number
US-9226891-B2
Publication Date
2016-01-05
Expiration Date
Abstract
Disclosed are pharmaceutical compositions having a portion of aspirin for intraoral release and another aspirin for gastrointestinal release. The compositions can further include niacin. Methods of using such compositions to treat diseases or conditions suitably treated by niacin are also provided which result in reduced flushing.
Core Innovation
The disclosure describes anti-flush pharmaceutical compositions for niacin flushing reduction that split aspirin into two portions having different oral fate. A first portion comprising a first amount of aspirin disintegrates or dissolves intraorally to provide rapid release of the aspirin of the first portion, while a second portion comprising a second amount of aspirin is substantially more difficult than the first portion to disintegrate or dissolve intraorally but is ingestible and releasable in the gastrointestinal track of the subject.
In the disclosed compositions, the first amount of aspirin and the second amount of aspirin each constitutes at least 20% of the total amount of aspirin in the composition. Unit dose forms are described as tablets or capsules, including formulations in which the first portion dissolves across oral mucosa and releases rapidly while the second portion is harder and is formulated for dissolving in stomach, intestines, or further distal in the gastrointestinal tract.
Methods are also disclosed for administering niacin with reduced flushing and for administering aspirin with reduced side effects by using the two-portion aspirin regimen. The niacin administration includes an effective amount of niacin together with the first and second aspirin compositions for reduced flushing, with timing variations described as after administration or concurrently, including within 30 minutes following a meal.
Claims Coverage
The independent claims cover four main categories of inventive subject matter, totaling five independent claims: a two-portion aspirin pharmaceutical composition, a niacin administration method using two such aspirin compositions for reduced flushing, aspirin administration methods for reduced side effects using intraoral-and-GI released split aspirin, and a tablet architecture having an outer dissolving portion and a harder inner portion designed for GI dissolution.
Two-portion aspirin composition with intraoral rapid release and GI releasable portion
A pharmaceutical composition comprising a first portion comprising a first amount of aspirin and a second portion comprising a second amount of aspirin, wherein the first portion disintegrates or dissolves intraorally providing rapid release of the aspirin of the first portion, and the second portion is substantially more difficult than the first portion to disintegrate or dissolve intraorally but is ingestible and releasable in the gastrointestinal track, and wherein the first amount of aspirin and the second amount of aspirin each constitutes at least 20% of the total amount of aspirin in the composition.
Niacin administration using two aspirin compositions for reduced flushing
A method of administering niacin to a subject with reduced flushing, comprising administering an effective amount of niacin and a first composition and a second composition, wherein the first composition comprises a first amount of aspirin that disintegrates or dissolves intraorally providing rapid release of the aspirin of the first portion, wherein the second composition comprises a second amount of aspirin that is ingested and released in the gastrointestinal track, and wherein the first amount of aspirin and the second amount of aspirin each constitutes at least 20% of the total amount of aspirin administered.
Aspirin administration with reduced side effects using intraoral rapid release within 10 minutes and GI release portion
A method of administering aspirin to a subject with reduced side effects, comprising administering a first composition comprising a first amount of aspirin and a second composition comprising a second amount of aspirin, wherein the first composition disintegrates or dissolves intraorally within 10 minutes permitting rapid release of the aspirin of the first portion, wherein the second composition is ingested and released in the gastrointestinal track, and wherein the first amount of aspirin and the second amount of aspirin each constitutes at least 20% of the total amount of aspirin administered.
Aspirin administration with reduced side effects using an intraoral portion dissolving within 10 minutes and remaining GI released
A method of administering aspirin to a subject with reduced side effects, comprising administering a therapeutically effective amount of aspirin, wherein a portion of the aspirin disintegrates or dissolves intraorally within 10 minutes permitting rapid release of the aspirin in the portion, and the remaining aspirin is ingested and released in the gastrointestinal track, and wherein the portion of aspirin and the remaining portion of aspirin each constitutes at least 20% of the total amount of aspirin administered.
Tablet with outer oral cavity dissolving portion and harder inner GI-dissolving portion
A tablet comprising an outer portion comprising at least about 40 mg aspirin and an inner portion comprising at least about 40 mg aspirin, wherein the outer portion is formulated to dissolve in the oral cavity of a subject and to release the aspirin across the oral mucosa, and wherein the inner portion is harder than the outer portion and is formulated for dissolving in stomach, intestines, or further distal in the gastrointestinal tract.
Across the independent claims, the central inventive coverage is the split-dose aspirin concept: an intraorally disintegrating or dissolving portion for rapid aspirin release and a substantially harder portion that is ingestible and releasable in the gastrointestinal track, with each aspirin portion representing at least 20% of the total administered aspirin or specific tablet amounts for the tablet claim. The method claims further tie the split aspirin regimen to reduced flushing with niacin or reduced side effects with aspirin, including defined intraoral disintegration or dissolution timing constraints within 10 minutes.
Stated Advantages
Reduced niacin flushing, as evidenced by reduced Global Flush Severity Scale scores when aspirin is partially intraorally released and partially GI released.
Reduced side effects from aspirin, as characterized by the method claims for aspirin administration with reduced side effects.
Documented Applications
Administering niacin to a subject with reduced flushing using a first aspirin composition that disintegrates or dissolves intraorally and a second aspirin composition that is ingested and released in the gastrointestinal track.
Administering aspirin to a subject with reduced side effects by using a first aspirin composition that disintegrates or dissolves intraorally and a second composition that is ingested and released in the gastrointestinal track.
Forming a tablet with an outer portion that dissolves in the oral cavity to release aspirin across oral mucosa and a harder inner portion formulated for dissolving in stomach, intestines, or further distal gastrointestinal tract.
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