| 摘要 |
FIELD: medicine.SUBSTANCE: invention relates to a solid dispersion for apoptosis induction. Dispersion contains a compound of formula I,where: Rdenotes chlorine; Rand Rdenote H; Rand Rdenote methyl; Adenotes N and Adenotes CH; Rdenotes nitro; X denotes -NH-; Y denotes -(CH)-, where n=1; and Ris 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 ex |
