[EN] MULTICOMPONENT CRYSTAL FORMULATIONS<br/>[FR] FORMULATIONS DE CRISTAL MULTICOMPOSANT
申请人:UNIV LIMERICK
公开号:WO2020201460A1
公开(公告)日:2020-10-08
A multicomponent crystal (or co-crystal) comprising a first active pharmaceutical ingredient and a second active pharmaceutical ingredient. The multicomponent crystal is formed / sustained by non- covalent interactions between the nitrogen-containing heterocycle alpha-substituted with an amino group of the first active pharmaceutical ingredient and a carboxylic acid group of the second active pharmaceutical ingredient, suitably as well as other further non-covalent interactions with other H-bond forming groups. The multicomponent crystal may provide an improved multidrug dosage form comprising lamotrigine and valproic acid as the first and second active pharmaceutical ingredients, respectively. A pharmaceutical composition comprising a therapeutically effective amount of the multicomponent crystal and a pharmaceutically acceptable excipient, and a method of forming the multicomponent crystal, are also provided.
一种多组分晶体(或共晶),包括第一种活性药物成分和第二种活性药物成分。该多组分晶体是由第一种活性药物成分的含氮杂环α-取代基与第二种活性药物成分的羧酸基之间的非共价相互作用形成/维持的,以及与其他形成氢键的基团的进一步非共价相互作用。该多组分晶体可以提供一种改进的多药剂量形式,包括拉莫三嗪和丙戊酸作为第一和第二种活性药物成分。还提供了一种包含治疗有效量多组分晶体和药学上可接受的赋形剂的制药组合物,以及形成多组分晶体的方法。