SOLID DISPERSIONS PRODUCED BY MELT EXTRUSION AND CONTAINING APOPTOSIS-INDUCING AGENT Russian patent published in 2016 - IPC A61K9/14 A61K9/20 A61K31/496 A61K47/02 A61K47/06 A61K47/32 A61P35/02 A61P35/00 C07D471/04 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a solid dispersion for apoptosis induction. The dispersion contains a compound of formula I , where: R⁰ means chlorine; R¹ and R² mean H; R³ and R⁴ mean methyl; A¹ means N, and A² mean CH; R⁵ means nitro; X means -NH-; Y means -(CH₂)_n-, where n = 1; and R⁶ is specified in a group consisting of tetrahydropyranyl and 4-hydroxy-4-methylcyclohexyl; or its pharmaceutically acceptable salt. The compound of Formula I or its pharmaceutically acceptable salt are dispersed in a solid matrix which contains (a) at least one pharmaceutically acceptable water-soluble polymer carrier, and (b) at least one pharmaceutically acceptable surfactant. At least 5% of the compound of Formula I or its pharmaceutically acceptable salt is presented in the crystalline form if studied by X-ray diffractometry. The compound or its pharmaceutically acceptable salt is presented in an amount equal to an amount of a parent compound from approximately 5% to approximately 15% by weight; at least one pharmaceutically acceptable water-soluble polymer carrier is presented in an amount from approximately 70% to approximately 85% by weight, and at least one pharmaceutically acceptable surfactant is presented in an amount from approximately 5% to approximately 15% by weight. There are also presented a method for producing dispersion and a pharmaceutical dosage form applicable for oral delivery.

EFFECT: solid dispersion is applicable for oral administration in the patient in need of treating a disease characterised by overexpression of one or more Bcl-2 family antiapoptotic proteins, eg cancer.

44 cl, 1 dwg, 17 tbl, 19 ex