基本信息:
- 专利标题: COMPOSITIONS OF LOPINAVIR AND RITONAVIR
- 专利标题(中):LOPINAVIR和RITONAVIR的组合物
- 申请号:PCT/GB2012/052210 申请日:2012-09-07
- 公开(公告)号:WO2013034927A1 公开(公告)日:2013-03-14
- 发明人: GIARDIELLO, Marco Norman , MCDONALD, Thomas Oliver , OWEN, Andrew , RANNARD, Steven Paul
- 申请人: THE UNIVERSITY OF LIVERPOOL , GIARDIELLO, Marco Norman , MCDONALD, Thomas Oliver , OWEN, Andrew , RANNARD, Steven Paul
- 申请人地址: Foundation Building 765 Brownlow Hill Liverpool L69 7ZX GB
- 专利权人: THE UNIVERSITY OF LIVERPOOL,GIARDIELLO, Marco Norman,MCDONALD, Thomas Oliver,OWEN, Andrew,RANNARD, Steven Paul
- 当前专利权人: THE UNIVERSITY OF LIVERPOOL,GIARDIELLO, Marco Norman,MCDONALD, Thomas Oliver,OWEN, Andrew,RANNARD, Steven Paul
- 当前专利权人地址: Foundation Building 765 Brownlow Hill Liverpool L69 7ZX GB
- 代理机构: HARRISON GODDARD FOOTE
- 优先权: GB1115635.3 20110909
- 主分类号: A61K9/19
- IPC分类号: A61K9/19 ; A61K9/51 ; A61K31/536
摘要:
The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drugs lopinavir and ritonavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol- succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N- alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof. The present invention also relates to processes for preparing both the solid composition and the aqueous dispersion, as well as to their use in therapy for the treatment and/or prevention of retroviral infections such as human immunodeficiency virus (HIV).
摘要(中):
本发明涉及包含抗逆转录病毒药物洛匹那韦和利托那韦的纳米颗粒的固体组合物和水分散体。 该固体组合物和水分散体另外包含亲水性聚合物和表面活性剂的混合物。 表面活性剂选自维生素-E-聚乙二醇琥珀酸酯(Vit-E-PEG-琥珀酸酯),聚氧乙烯脱水山梨糖醇脂肪酸酯,N-烷基二甲基苄基氯化铵,脱氧胆酸钠,二辛基磺基琥珀酸钠,聚乙二醇-12-羟基硬脂酸酯, (PVA)以及聚氧乙烯和聚氧丙烯的嵌段共聚物,或其组合。 亲水性聚合物适宜地选自聚乙烯醇(PVA),聚乙烯醇 - 聚乙二醇接枝共聚物,聚氧乙烯和聚氧丙烯的嵌段共聚物,聚乙二醇,羟丙基甲基纤维素(HPMC)和聚乙烯吡咯烷酮或其组合。 本发明还涉及制备固体组合物和水分散体的方法,以及它们在治疗和/或预防逆转录病毒感染例如人类免疫缺陷病毒(HIV)的治疗中的用途。 p>
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K9/00 | 以特殊物理形状为特征的医药配制品 |
--------A61K9/10 | .分散液;乳剂 |
----------A61K9/19 | ..冻干的 |