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 

Abstract RU 2577859 C2

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

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RU 2 577 859 C2

Authors

Resh Ester

Khelig Peter

Lindli Devid Dzh.

Sanzgiri Jeshvant D.

Tun Pin

Dates

2016-03-20Published

2011-10-05Filed