A61K9/2027

Pharmaceutical tablet and production method thereof

An object of the present invention is to provide a pharmaceutical tablet having high tensile strength and excellent in immediate disintegrability. The pharmaceutical tablet of the present invention is obtained by a direct compression method, and contains an active ingredient, a polyvinyl alcohol resin, and a plasticizer other than water, wherein a content of the plasticizer is 1 to 8 parts by weight with respect to 100 parts by weight of the polyvinyl alcohol resin.

Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea

Provided herein are low impurity compositions comprising a compound represented by Formula (I): ##STR00001##
which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.

STABLE HOT-MELT EXTRUDATE CONTAINING VALSARTAN AND SACUBITRIL

The present invention relates to a solid unit dosage form for oral administration (tablet or granules) containing a solid dispersion of valsartan and sacubitril in a polymeric matrix. The solid dispersion is prepared by hot-melt extrusion and may contain the active ingredients preferably in a non-crystalline state. LCZ696, (pseudo)polymorphic forms thereof as well as the individual drugs, e.g. valsartan disodium and sacubitril monosodium, may be subjected to the hot-melt extrusion process.

PHARMACEUTICAL COMPOSITION COMPRISING AXITINIB

The present invention relates to an immediate release tablet composition comprising axitinib form IV characterized by an XRPD pattern comprising the peaks at about 8.9, 12.0, 14.6, 15.2, 15.7, 17.8, 19.1, 20.6, 21.6, 23.2, 24.2, 24.9, 26.1 and 27.5±0.1 degrees 2θ, when measured with Cu Kα1 radiation and one or more pharmaceutically acceptable excipients, wherein the composition exhibits a dissolution rate between 40% and 70% in 30 minutes when tested in 900 ml 0.01 N hydrochloric acid pH 2.0 at 37° C., 75 rpm in a USP apparatus II.

TREATMENTS OF ANGIOEDEMA

The present invention relates to treatments of angioedema, and specifically bradykinin-mediated angioedema non-hereditary (BK-AEnH). In particular, the present invention provides on-demand treatments of bradykinin-mediated angioedema non-hereditary (BK-AEnH) by orally administering a plasma kallikrein inhibitor to a patient in need thereof on-demand. Regular (or continuous) treatments of BK-AEnH are also provided.

LAXATIVE TABLET
20210401754 · 2021-12-30 ·

Provided is a laxative tablet which includes magnesium oxide as a main constituent, wherein (1) the particle size by volume of 50% (D50) of particles which emerge when the tablet is suspended in water is 70 μm or less as determined by laser diffractometry, (2) the particle size by volume of 90% (D90) of the particles which emerge when the tablet is suspended in water is 130 μm or less as determined by laser diffractometry, and (3) the dissolution time of the tablet when the tablet is suspended in water according to the Japanese Pharmacopoeia—general testing methods—dissolution testing methods is 10 seconds or less.

SUBSTITUTED 1,2,4-OXADIAZOLE, ITS APPLICATION AND A PHARMACEUTICAL PREPARATION COMPRISING IT

Disclosed are compounds effective against tuberculosis based on substituted 1,2,4-oxadiazoles of general formula I, where Y═S or CH.sub.2 and R=phenyl- or phenyl-substituted in positions 2, 3, 4, and 5 by one or several electron-acceptor groups or electron-donor groups. These compounds can be produced by easy syntheses and are characterized by low toxicity and high efficacy against mycobacteria, including multiresistant strains thereof. Also disclosed are a pharmaceutical preparation containing substituted 1,2,4-oxadiazole of formula I as an active substance as well as the use of this substituted 1,2,4-oxadiazole as an antituberculosis drug.

METHODS OF TREATING VIRALLY ASSOCIATED CANCERS WITH HISTONE DEACETYLASE INHIBITORS

Described herein are certain dosing schedules and amounts that effectively prevent and manage side effects associated with histone deacetylase inhibitor (HDACi) treatment. Optionally, these schedules and dosing regimens include treatment with an antiviral agent.

PROCASPASE-3 ACTIVATION AND IMMUNOTHERAPY FOR TREATMENT OF CANCER

The blood-brain barrier penetrant procaspase-3-activating drug, PAC-1, has been identified as an effective approach to inducing immune stimulatory destruction of cancer cells. PAC-1 induces cleavage of MLH1 in cancer cells, and studies show that inactivation of MLH1 leads to increased mutational burden and neoantigen presentation by major histocompatibility complex (MHC) products. Herein is described a mechanistic-based strategy to bring the power of immunotherapy in an effective fashion for treatment of cancer.

Parenteral Formulations of Dopamine Agonists
20210401824 · 2021-12-30 ·

This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.