PRESERVATION OF API PARTICLES WITH FUNCTIONAL COATING OBTAINED BY MIXING PROCESSES WITHOUT SOLVENT IN AQUEOUS SUSPENSION Russian patent published in 2024 - IPC A61K9/14 A61K9/10 A61K31/167 A61K31/192 A61K47/44 A61K47/02 A61K47/26 A61K47/42 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to a pharmaceutical composition containing: a coated particle of an active pharmaceutical ingredient (API); containing: a first coating comprising one or more deformed components covering the API particle, where one or more deformed components contain 15–30 wt.% of one or more of carnauba wax, candelilla wax or synthetic wax; a second coating containing hydrophobic colloidal silicon dioxide, partially included and/or included in the first coating; where the coated API particles contain 0.5–10 wt.% hydrophobic colloidal silicon dioxide and the silicon dioxide provides a slower dissolution profile of the API compared to the API without silicon dioxide, also relates to a method of producing a pharmaceutical composition comprising: combining API particles with particles of a first coating material, wherein the first coating material contains one or more deformable components, wherein one or more deformed components contain 15–30 wt.% of one or more of carnauba wax, candelilla wax or synthetic wax; applying mechanical and/or thermal energy to the combination of API particles and particles of the first coating material to form an ordered mixture of API particles, including a discrete layer of particles of the first coating material on the surface of the API particles; applying mechanical and/or thermal energy to an ordered mixture of API particles and particles of the first coating material to deform one or more deformable components to form coated API particles, wherein the coated API particles comprise a continuous film of the first coating material surrounding each of the API particles; combining the coated API particles with particles of a second coating material containing hydrophobic colloidal silicon dioxide; application of mechanical and/or thermal energy to coated API particles with particles of second coating material for at least partial inclusion and/or inclusion of the second coating material into the first coating material to form the coated API particles containing the second coating, where the coated API particles contain 0.5–10 wt.% of hydrophobic colloidal silicon dioxide, where silicon dioxide provides a slower dissolution profile of the API compared to API without silicon dioxide; and mixing the coated API particles containing the second coating in a matrix solution/suspension to obtain a pharmaceutical suspension and a pharmaceutical composition obtained by said method.

EFFECT: group of inventions provides higher fluidity for functionally coated API particles in order to facilitate subsequent processing and provides higher strength of the coating, as evidenced by the slower dissolution profile of the coated API.

23 cl, 2 ex, 13 dwg