Pharmaceutical composition for modified release
Inventors
Takaishi, Yuuki • Nakamura, Soichiro • Takahashi, Yutaka • Nishizato, Takashi • Murayama, Daisuke • Murayama, Emiko • Sako, Kazuhiro
Assignees
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Publication Number
US-12097189-B1
Publication Date
2024-09-24
Expiration Date
Abstract
A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a maximum blood drug concentration (Cmax) when administered in fasted state is 400 ng/ml or less, is disclosed.
Core Innovation
The invention relates to a modified-release pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide (compound A) or salts thereof together with a sustained-release carrier, configured to reduce food effects by controlling pharmacokinetics. The disclosed approach targets fasted-state Cmax limits and compares food/fasted pharmacokinetic behavior to that of conventional immediate-release formulations.
The reduced food effect is defined in terms of the difference in a rate of decrease of Cmax compared to an immediate release formulation comprising the same compound A, with the reduced food effect expressed as a difference in rate of decrease of Cmax of 10% or more. The formulation provides continuous drug release for at least 4 hours after oral administration, and the immediate release formulation is a capsule comparator.
The sustained release hydrogel-forming formulation includes a carrier and is implemented using sustained-release hydrogel-forming formulation frameworks and related sustained-release design options. Examples include hydrogel-forming polymers with hydrophilic base additives, multilayered formulations, gel matrices including gum combinations, osmotic pump systems, swelling-polymer formulations, water-soluble polymer matrices, coating-membrane modified release, and insoluble-polymer matrices.
Claims Coverage
The independent claims are directed to methods of treating overactive bladder with reduced food effect using sustained-release hydrogel-forming tablets containing compound A, and comparing performance to an immediate release capsule using a defined Cmax-based criterion. Across the independent claims, the inventive features center on sustained-release hydrogel-forming oral dosage for at least 4 hours and reduction of the rate of decrease of Cmax versus an immediate release capsule comparator.
Sustained-release hydrogel-forming tablet for continuous drug release
Orally administering to a subject a tablet comprising compound A in a sustained release hydrogel-forming formulation comprising a carrier that provides continuous drug release for at least 4 hours after oral administration.
Reduced food effect defined by rate of decrease of Cmax versus immediate release capsule
Providing a reduced food effect compared to oral administration of an immediate release formulation comprising compound A, wherein the reduced food effect is a difference in a rate of decrease of Cmax of 10% or more, and wherein the immediate release formulation is a capsule.
Hydrogel-forming formulation components including polyethylene oxide and polyethylene glycol
Using a sustained release hydrogel-forming formulation characterized by including polyethylene oxide and polyethylene glycol, including specified polyethylene oxide average molecular weight ranges and selected polyethylene glycol species in dependent claim refinements.
The claim set focuses on an orally administered sustained release hydrogel-forming tablet with defined compound A tablet strength that delivers continuous drug release for at least 4 hours and achieves a reduced food effect versus an immediate release capsule, where the reduced food effect is expressed by a Cmax-based difference in a rate of decrease of Cmax criterion of 10% or more. Dependent claims further refine the hydrogel-forming formulation using polyethylene oxide and polyethylene glycol selection and molecular-weight or specific PEG options.
Stated Advantages
Reduced food effect compared with an immediate release formulation, including controlled fasted-state Cmax and reduced fed/fasted Cmax decreases.
Achieves continuous drug release for at least 4 hours after oral administration.
Reduced differences in pharmacokinetics, including reduced Cmax and AUC differences versus conventional immediate-release formulations.
Documented Applications
Treating overactive bladder in a subject by administering compound A as an orally administered tablet in a sustained release hydrogel-forming formulation with reduced food effect compared to an immediate release capsule.
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