A61K31/138

Use of Glutamate 2B Receptor Antagonists and Sigma Receptor Agonists as Antitussives
20220378769 · 2022-12-01 · ·

The use of glutamate 2b receptor antagonists and sigma receptor agonists as antitussives to treat or prevent a cough is disclosed. In preferred embodiments, the glutamate 2b receptor antagonist is ifenprodil or radiprodil. Preferred sigma receptor agonists include fluvoxamine, fluoxetine, excitalpram, and donepezil.

Use of Glutamate 2B Receptor Antagonists and Sigma Receptor Agonists as Antitussives
20220378769 · 2022-12-01 · ·

The use of glutamate 2b receptor antagonists and sigma receptor agonists as antitussives to treat or prevent a cough is disclosed. In preferred embodiments, the glutamate 2b receptor antagonist is ifenprodil or radiprodil. Preferred sigma receptor agonists include fluvoxamine, fluoxetine, excitalpram, and donepezil.

Method for improving aqueous solubility of water-insoluble or slightly water-soluble drugs

A method of increasing the solubility of a water-insoluble or slightly water-soluble hydrophobic organic compound in an aqueous solvent includes adding a saponin component selected from escin, glycyrrhizin, and Quillaya saponaria extract to the aqueous solvent in an amount sufficient to trigger the formation of micelles, wherein in a first step the hydrophobic organic compound is pre-dissolved in an organic solvent, and in a second step the organic solvent comprising the pre-dissolved compound is admixed to the aqueous solvent, whereby at least a part of the insoluble or slightly soluble hydrophobic organic compound gets solubilized and dissolved in the aqueous solvent, yielding an aqueous composition having an increased concentration of said organic compound dissolved therein. Also indicated are pharmaceutical or cosmetic compositions including a water-insoluble or slightly water-soluble organic compound dissolved in an aqueous solvent at substantially increased concentrations.

Method for improving aqueous solubility of water-insoluble or slightly water-soluble drugs

A method of increasing the solubility of a water-insoluble or slightly water-soluble hydrophobic organic compound in an aqueous solvent includes adding a saponin component selected from escin, glycyrrhizin, and Quillaya saponaria extract to the aqueous solvent in an amount sufficient to trigger the formation of micelles, wherein in a first step the hydrophobic organic compound is pre-dissolved in an organic solvent, and in a second step the organic solvent comprising the pre-dissolved compound is admixed to the aqueous solvent, whereby at least a part of the insoluble or slightly soluble hydrophobic organic compound gets solubilized and dissolved in the aqueous solvent, yielding an aqueous composition having an increased concentration of said organic compound dissolved therein. Also indicated are pharmaceutical or cosmetic compositions including a water-insoluble or slightly water-soluble organic compound dissolved in an aqueous solvent at substantially increased concentrations.

BRUSH PRODRUGS AND USES THEREOF

The present disclosure provides, in some aspects, macromonomers of Formula (I), and salts thereof; methods of preparing the macromonomers, and salts thereof; Brush prodrugs (polymers); methods of preparing the Brush prodrugs; compounds of Formula (II); conjugates of Formula (III), and salts thereof; pharmaceutical compositions comprising a Brush prodrug, or a conjugate or a salt thereof; kits comprising: a macromonomer or a salt thereof, a Brush prodrug, a compound, a conjugate or a salt thereof, or a pharmaceutical composition; methods of using the Brush prodrugs, or conjugates or salts thereof; and uses of the Brush prodrugs, and conjugates or salts thereof. These chemical entities may be useful in delivering pharmaceutical agents to a subject or cell.

BRUSH PRODRUGS AND USES THEREOF

The present disclosure provides, in some aspects, macromonomers of Formula (I), and salts thereof; methods of preparing the macromonomers, and salts thereof; Brush prodrugs (polymers); methods of preparing the Brush prodrugs; compounds of Formula (II); conjugates of Formula (III), and salts thereof; pharmaceutical compositions comprising a Brush prodrug, or a conjugate or a salt thereof; kits comprising: a macromonomer or a salt thereof, a Brush prodrug, a compound, a conjugate or a salt thereof, or a pharmaceutical composition; methods of using the Brush prodrugs, or conjugates or salts thereof; and uses of the Brush prodrugs, and conjugates or salts thereof. These chemical entities may be useful in delivering pharmaceutical agents to a subject or cell.

ORAL PHARMACEUTICAL COMPOSITION COMPRISING A MELT-AGGLOMERATED ACTIVE INGREDIENT CORE
20220370368 · 2022-11-24 ·

The invention relates to coated particles with a taste-masked drug substance. The particles comprise a core with a melt-agglomerated active pharmaceutical ingredient (API), optionally a thermolabile API, and a coating comprising a triglyceride and a surfactant. The particles exhibit immediate drug release and a storage-stable release profile. Moreover, the invention provides a hot-melt granulation and hot-melt coating method for manufacturing such coated particles, and pharmaceutical compositions comprising the coated particles. The method allows the granulation of APIs with small particle sizes (e.g., mean particle size below 150 μm, or even below 100 μm or 50 μm) into core particles, as well as coating said core particles, at moderate temperatures, thereby preventing the degradation of thermolabile active pharmaceutical ingredients.

ORAL PHARMACEUTICAL COMPOSITION COMPRISING A MELT-AGGLOMERATED ACTIVE INGREDIENT CORE
20220370368 · 2022-11-24 ·

The invention relates to coated particles with a taste-masked drug substance. The particles comprise a core with a melt-agglomerated active pharmaceutical ingredient (API), optionally a thermolabile API, and a coating comprising a triglyceride and a surfactant. The particles exhibit immediate drug release and a storage-stable release profile. Moreover, the invention provides a hot-melt granulation and hot-melt coating method for manufacturing such coated particles, and pharmaceutical compositions comprising the coated particles. The method allows the granulation of APIs with small particle sizes (e.g., mean particle size below 150 μm, or even below 100 μm or 50 μm) into core particles, as well as coating said core particles, at moderate temperatures, thereby preventing the degradation of thermolabile active pharmaceutical ingredients.

METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER
20220370397 · 2022-11-24 ·

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) one or more chemotherapeutic agents such as a checkpoint inhibitor or doxorubicin and/or cyclophosamide; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG)

METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER
20220370397 · 2022-11-24 ·

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) one or more chemotherapeutic agents such as a checkpoint inhibitor or doxorubicin and/or cyclophosamide; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG)