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Stabilised amorphous form of agomelatine, a process for its preparation and pharmaceutical compositions containing it.
专利权人:
LES LABORATOIRES SERVIER
发明人:
Lafargue, David,Lynch, Michael,Poirier, Cécile,Letellier, Philippe,Pean, Jean-Manuel,Luo, Ying,Shan, Hanbin,Shen, Yuhui
申请号:
NZ70580213
公开号:
NZ705802A
申请日:
2013.09.11
申请国别(地区):
NZ
年份:
2018
代理人:
摘要:
Disclosed is a stabilised amorphous form of agomelatine of formula (I) characterised in that the agomelatine is dispersed within a matrix selected from the group consisting of: 30%, 40% or 50% by weight of agomelatine in poly(methacrylic acid-co-methyl methacrylate) 1:1 (Eudragit L100) 30%, 35%, 40% or 50% by weight of agomelatine in poly(methacrylic acid-co-ethyl acrylate) 1:1 (Eudragit L100-55) 30%, 35% or 40% by weight of agomelatine in vinylpyrrolidone-vinyl acetate copolymer (Kollidon VA64) 30%, 35% or 40% by weight of agomelatine in polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus) 30% or 40% by weight of agomelatine in Polyvinyl Acetate Phthalate 30% by weight of agomelatine in 60:40 linear random copolymer of N-vinyl-2-pyrrolidone and vinyl acetate (Plasdone S630) and 30% by weight of agomelatine in HPMC acetyl succinate. Processes for obtaining the stabilised amorphous form, pharmaceutical compositions comprising the stabilised form, and uses of the stabilised form are also disclosed.
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