Therapeutic compounds, formulations, and uses thereof
Inventors
Alibhai, Imran • De Achaval, Sofia • LANGEVIN, Beverly C. • Zhou, Tian
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-11547683-B2
Publication Date
2023-01-10
Expiration Date
Abstract
Provided herein are compositions, formulations, and (e.g., oral) dosage forms comprising a compound of Formula (I). In specific instances, such compositions comprise an emulsifier, a solubilizer, a polyethylene glycol, a surfactant, and an antioxidant. In some instances, such compositions are useful for the treatment of fibrosis, cancer, and/or chronic inflammation.
Core Innovation
The invention relates to oral pharmaceutical compositions and oral dosage forms comprising a compound of Formula (I) and specific excipients in defined weight ratios. The compositions include a glyceride emulsifier, a solubilizer, polyethylene glycol (PEG), a surfactant, and an antioxidant, and the compound of Formula (I) is present in an amount of at least 50 mg in the composition.
A core aspect of the invention is the selection of excipient classes and defined weight-ratio relationships among the compound of Formula (I), a glyceride emulsifier, polyoxyl castor oil as a solubilizer, PEG, a polysorbate surfactant, and an antioxidant. The solubilizer is polyoxyl castor oil, the surfactant is polysorbate, and the disclosed compositions are described in relation to self-emulsifying drug dispersion (SEDD).
The document further includes characterization of a crystalline form of Formula (I) and formulation attributes associated with stability and performance. It also describes pharmaceutical compositions and oral dosage forms that are designed to address poor solubility and pill burden.
Claims Coverage
The independent claim centers on a pharmaceutical composition with at least 50 mg of a compound of Formula (I) combined with specified excipients in defined weight ratios. Two inventive features are identified across the claim content.
Pharmaceutical composition with defined excipient system and ratios
A pharmaceutical composition comprising at least 50 mg of a compound of Formula (I), a glyceride emulsifier in a weight ratio of about 1:1 to about 1:2, a polyoxyl castor oil solubilizer in a weight ratio of about 1:2 to about 1:4, a PEG component in a weight ratio of about 1:3 to about 1:5, a polysorbate surfactant in a weight ratio of about 1:1 to about 1:2, and an antioxidant in a weight ratio of compound of Formula (I) to surfactant of about 15:1 to about 25:1.
Oral capsule dosage form and therapeutic narrowing
The composition is narrowed to an oral capsule dosage form and oral administration for treating particular conditions.
The claim coverage focuses on an oral pharmaceutical composition of a compound of Formula (I) formulated with a glyceride emulsifier, polyoxyl castor oil solubilizer, PEG, polysorbate surfactant, and an antioxidant, with defined weight-ratio ranges and an oral capsule dosage form in the dependent claim content.
Stated Advantages
Improved Cmax and AUC versus a benchmark PEG400/Labrasol® (60:40) formulation.
Reduced pill burden.
Stability and performance associated with measurable formulation characteristics such as droplet size, polydispersity, and purity over storage.
Supports high compound loading.
Addresses poor solubility.
Documented Applications
Self-emulsifying drug dispersion (SEDD).
Oral administration for treating fibrosis, cancer, and chronic inflammation.
Treating STAT3-mediated disorders.
Interested in licensing this patent?