公开(公告)号：US10603279B2

公开(公告)日：2020-03-31

申请号：US14343169

申请日：2012-09-07

申请人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith ,  James Long

发明人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith ,  James Long

IPC分类号： A61K31/513 ,  A61K9/16 ,  A61K9/14 ,  A61K9/51 ,  A61K9/19 ,  A61K45/06

摘要： The present invention relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug lopinavir. 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).

公开(公告)号：US20140212501A1

公开(公告)日：2014-07-31

申请号：US14343169

申请日：2012-09-07

申请人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith ,  James Long

发明人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith ,  James Long

IPC分类号： A61K31/513 ,  A61K9/16 ,  A61K9/14

CPC分类号： A61K9/1682 ,  A61K9/14 ,  A61K9/19 ,  A61K9/5138 ,  A61K31/513 ,  A61K45/06

摘要： The present invention relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug lopinavir. 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).

摘要翻译： 本发明涉及包含抗逆转录病毒药物洛匹那韦的纳米颗粒的固体组合物和水分散体。 固体组合物和水性分散体还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，聚乙烯醇 （PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。 亲水性聚合物适当地选自聚乙烯醇（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如人类免疫缺陷病毒（HIV）中的用途。

公开(公告)号：US09498438B2

公开(公告)日：2016-11-22

申请号：US14343203

申请日：2012-09-07

申请人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

发明人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

IPC分类号： A61K9/14 ,  A61K9/10 ,  A61K9/19 ,  A61K9/51 ,  A61K31/536 ,  A61K9/16

CPC分类号： A61K9/14 ,  A61K9/10 ,  A61K9/1682 ,  A61K9/19 ,  A61K9/5138 ,  A61K9/5192 ,  A61K31/536

摘要： The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug efavirenz. 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).

摘要翻译： 本发明涉及包含抗逆转录病毒药物依法韦仑的纳米颗粒的固体组合物和水性分散体。 固体组合物和水性分散体还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，聚乙烯醇 （PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。 亲水性聚合物适当地选自聚乙烯醇（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如人类免疫缺陷病毒（HIV）中的用途。

公开(公告)号：US09532979B2

公开(公告)日：2017-01-03

申请号：US14343453

申请日：2012-09-07

申请人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

发明人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

IPC分类号： A61K9/14 ,  A61K31/427 ,  A61K9/19 ,  A61K31/513 ,  A61K38/55 ,  A61K9/51

CPC分类号： A61K31/427 ,  A61K9/19 ,  A61K9/5138 ,  A61K9/5192 ,  A61K31/513 ,  A61K38/55 ,  Y02A50/411 ,  A61K2300/00

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).

摘要翻译： 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。 固体组合物和水性分散体还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，聚乙烯醇 （PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。 亲水性聚合物适当地选自聚乙烯醇（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如人类免疫缺陷病毒（HIV）中的用途。

公开(公告)号：US20140220141A1

公开(公告)日：2014-08-07

申请号：US14343453

申请日：2012-09-07

申请人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

发明人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

IPC分类号： A61K31/513 ,  A61K31/427

CPC分类号： A61K31/427 ,  A61K9/19 ,  A61K9/5138 ,  A61K9/5192 ,  A61K31/513 ,  A61K38/55 ,  Y02A50/411 ,  A61K2300/00

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).

摘要翻译： 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。 固体组合物和水性分散体还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，聚乙烯醇 （PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。 亲水性聚合物适当地选自聚乙烯醇（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如人类免疫缺陷病毒（HIV）中的用途。

公开(公告)号：US20140220140A1

公开(公告)日：2014-08-07

申请号：US14343203

申请日：2012-09-07

申请人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

发明人： Marco Norman Giardiello ,  Thomas Oliver McDonald ,  Andrew Owen ,  Steven Paul Rannard ,  Philip John Martin ,  Darren Lee Smith

IPC分类号： A61K31/536 ,  A61K9/16 ,  A61K9/14

CPC分类号： A61K9/14 ,  A61K9/10 ,  A61K9/1682 ,  A61K9/19 ,  A61K9/5138 ,  A61K9/5192 ,  A61K31/536

摘要： The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug efavirenz. 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).

摘要翻译： 本发明涉及包含抗逆转录病毒药物依法韦仑的纳米颗粒的固体组合物和水性分散体。 固体组合物和水性分散体还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，聚乙烯醇 （PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。 亲水性聚合物适当地选自聚乙烯醇（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如人类免疫缺陷病毒（HIV）中的用途。