Pharmaceutical compositions
Inventors
Brisander, Magnus • Demirbüker, Mustafa • Jesson, Gérald • Malmsten, Martin • Dérand, Helene
Assignees
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Publication Number
US-11241419-B2
Publication Date
2022-02-08
Expiration Date
Abstract
The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.
Core Innovation
The invention relates to a composition comprising particles in which a protein kinase inhibitor has a degree of amorphicity of 100% and is present in an amount of from about 10% by weight to about 70% by weight of the particles. The particles further include at least one polymeric stabilizing and matrix-forming component, and define a stable amorphous hybrid nanoparticle system.
The protein kinase inhibitor is dasatinib, dasatinib hydrate, dasatinib solvate, dasatinib salt, or combinations thereof. Optionally, at least one pharmaceutically acceptable solubilizer is included and, when present, is a physical mixture with the particles.
The disclosure addresses poorly water-soluble protein kinase inhibitors and links the amorphous 100% protein kinase inhibitor within polymeric stabilizing and matrix-forming particles, optionally together with a pharmaceutically acceptable solubilizer, to improved dissolution and solubility at intestinal and gastric pH.
Claims Coverage
The document identifies two independent claims. Each independent claim is directed to particulate pharmaceutical compositions defined by a protein kinase inhibitor having a degree of amorphicity of 100% at about 10–70% by weight, together with polymeric components, and with dasatinib forms specified in the claims.
Amorphous protein kinase inhibitor with polymeric stabilizing and matrix-forming component
Particles consist of a protein kinase inhibitor having a degree of amorphicity of 100% in an amount of from about 10% by weight to about 70% by weight of the particles, and at least one polymeric stabilizing and matrix-forming component.
Optional solubilizer as a physical mixture with the particles
At least one pharmaceutically acceptable solubilizer is optionally included, and when present is a physical mixture with the particles.
Dasatinib forms in the amorphous 100% protein kinase inhibitor particles
The protein kinase inhibitor is dasatinib, dasatinib hydrate, dasatinib solvate, dasatinib salt, or combinations thereof.
Copolyvidone as the polymeric matrix component
Particles consist of a protein kinase inhibitor having a degree of amorphicity of 100% in an amount of from about 10% by weight to about 70% by weight of the particles, and copolyvidone.
The claim coverage centers on particles containing a 100% amorphous protein kinase inhibitor at about 10–70% by weight together with polymeric stabilizing and matrix-forming components, including copolyvidone in one independent claim. Dasatinib is specified in several forms, and one independent claim further includes optional pharmaceutically acceptable solubilizer present as a physical mixture with the particles.
Stated Advantages
Improved dissolution and solubility at intestinal and gastric pH.
Documented Applications
Therapy for proliferative disorders by administering therapeutically effective amounts of the composition.
Use of the disclosed compositions to address poorly water-soluble protein kinase inhibitors.
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