A61K9/2027

Anticancer compositions
11224575 · 2022-01-18 · ·

The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509, a poly(meth)acrylate copolymer and HPMCAS. In one aspect, the solid dispersion of ARN-509, a poly(meth)acrylate copolymer and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509, a poly(meth)acrylate copolymer and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509, a poly(meth)acrylate copolymer and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509, a poly(meth)acrylate copolymer and HPMCAS in a suitable solvent.

ORAL DOSAGE FORM

The present invention in general relates to a pharmaceutical dosage form comprising one or more granules, and a method for manufacturing thereof. The granules of the dosage form are prepared via the extrusion/spheronization technique using partially hydrolysed polyvinyl alcohol. These granules have the advantage that a high drug load can be contained therein.

Softgels with solid or gel-like polymeric fill matrix

Stable dosage forms, preferably of pharmaceutical formulations, that include a solid or semi-solid polymeric mass, which entraps active ingredients and can be formulated for oral administration in a mould, preferably in a softgel capsule.

OPIOID RECEPTOR MODULATOR DOSAGE FORMULATIONS

Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.

TOSYLACETATE BASED COMPOUNDS AND DERIVATIVES THEREOF AS PHGDH INHIBITORS

The present invention encompasses compounds of formula (I), wherein the groups R.sup.1 to R, A.sup.1 to A.sup.4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

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DISPERSIBLE COMPOSITIONS

The present invention is concerned with dispersible compositions comprising rilpivirine or a pharmaceutically acceptable acid addition salt thereof as an active ingredient. Such compositions are useful in the treatment of HIV infection and their dispersibility properties lend themselves to be useful in particular amongst the pediatric or geriatric population.

ORALLY DISINTEGRATING TABLET COMPRISING AMORPHOUS SOLID DISPERSION OF NILOTINIB

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor nilotinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer. In particular, the present disclosure provides a pharmaceutical composition in the form of an orally disintegrating tablet. In some embodiments, the pharmaceutical compositions can be administered without regard to food consumption. In other embodiments, the pharmaceutical compositions can be administered at a significantly lower dose as compared to a commercially available immediate-release nilotinib formulation, while providing a comparable therapeutic effect.

DUAL RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMBINATION OF A BETA-3 ADRENORECEPTOR AGONIST AND A MUSCARINIC RECEPTOR ANTAGONIST

The present invention relates to a pharmaceutical composition comprising a combination of mirabegron and solifenacin or their pharmaceutically acceptable salts, wherein the composition comprises mini-tablets, multiparticulates, inlay tablets, or bilayer tablets. The prior art discloses restrictive formulation techniques and suggests complexity for preparing the combination in a single formulation to achieve the desired technical attributes. The test formulations are stable and exhibit desired pharmaceutical technical attributes. The invention also relates to the use of the pharmaceutical composition of the present invention in the treatment of various diseases like overactive bladder and other related therapeutic indications.

Additive composition for orally disintegrating tablet

Provided is a novel additive for an orally disintegrating tablet which imparts a rapid disintegration property and a tablet hardness to the orally disintegrating tablet and a method for producing the same. An additive for an orally disintegrating tablet according to one embodiment of the present invention includes a D-mannitol, a low-substituted hydroxypropyl cellulose (excluding those having a mean particle size of 20 μm or less and a substitution degree of the hydroxypropoxy groups of 11%, having a mean particle size of 45 μm or less and a substitution degree of the hydroxypropoxy groups of 14% and having a mean particle size of 45 μm or less and a substitution degree of the hydroxypropoxy groups of 11% together with a 90% cumulated particle size of 100 μm or less), a crospovidone and a crystalline cellulose.

Oral delivery of GLP-1 peptide analogs

The present invention provides formulations for oral administration of GLP-1 peptide analogs, methods of making such formulations, and methods of treatment using such formulations.