KETRON Nataniel D. (US),КЭТРОН Натаниэль Д. (US),LINDLI Devid Dzh. (US),ЛИНДЛИ Дэвид Дж. (US),MILLER Dzhonatan (US),МИЛЛЕР Джонатан (US),SHMITT Erik A. (US),ШМИТТ Эрик А. (US),TUN Pin (US),ТУН Пин (US,KETRON Nataniel D.,КЭТРОН Натаниэль Д.,LINDLI Devid Dzh.,ЛИНДЛИ Дэвид Дж.,MILLER Dzhonatan,МИЛЛЕР Джонатан,SHMITT Erik A.,ШМИТТ Эрик А.,TUN Pin,ТУН Пин
申请号：
RU2013124824/15
公开号：
RU0002598345C2
申请日:
2011.10.27
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: medicine.SUBSTANCE: invention relates to a solid dispersion for apoptosis induction. Dispersion contains a compound of formula I,where: R0 denotes chlorine； R1 and R2 denote H； R3 and R4 denote methyl； A1 denotes N and A2 denotes CH； R5 denotes nitro； X denotes -NH-； Y denotes -(CH2)n-, where n=1； and R6 is selected from a group consisting of tetrahydropyranyl and 4-hydroxy-4-methylcyclohexyl； or its pharmaceutically acceptable salt. Herewith 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. Water-soluble polymer carrier is selected from a group consisting of homopolymers and copolymers of N-vinillactams, cellulose esters, cellulose ethers, polyalkylene oxides with high molecular weight, polyacrylates, polymethacrylates, polyacrylamides, vinyl acetate polymers, grafted copolymers of ethylene glycol, polyvinyl caprolactam and polyvinyl acetate, oligo- and polysaccharides and mixtures thereof. Surfactant is selected from a group consisting of polyoxyethylene glycerides, monoesters of sorbitan fatty acids, polysorbates, α-tocopheryl-polyethylene glycol succinate (TPGS) and their mixtures. Also not more than 5 % of the compound of formula I or its pharmaceutically acceptable salt in a solid dispersion is in crystalline form as per X-ray diffraction analysis data. Also described are: a method of producing the solid dispersion, orally delivered pharmaceutical dosage form.EFFECT: solid dispersion is suitable for oral use by a person who needs it for treating a disease characterized by overexpression of one or more antiapoptosis proteins from the Bcl-2 family, for example, cancer.44 cl, 2 tbl, 17 exИзобретение относится к твердой дисперсии для индукции апоптоза. Дисперсия включает соединение формулы Iгде: R0 обозначает хлор； R1 и R2 обозначают Н； R3 и R4 обозначают мет
