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1. 发明授权

US11517534B2 Delayed release drug formulation 有权
公开(公告)号：US11517534B2
公开(公告)日：2022-12-06
申请号：US15612065
申请日：2017-06-02
申请人： Tillotts Pharma AG
发明人： Felipe Josè Oliveira Varum , Roberto Carlos Bravo González , Thomas Buser , Abdul Waseh Basit , Ana Cristina Freire
IPC分类号： A61K9/28 , A61K31/196 , A61K31/606 , A61K31/616 , A61K47/32 , A61K47/36 , A61K47/38 , A61K9/00 , A61K9/20
摘要： In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

2. 发明授权

US09364440B2 Delayed release drug formulation 有权
标题翻译：延迟释药制剂
公开(公告)号：US09364440B2
公开(公告)日：2016-06-14
申请号：US14398005
申请日：2013-04-29
申请人： TILLOTTS PHARMA AG
发明人： Roberto Carlos Bravo Gonzalez , Thomas Buser , Frederic Jean-Claude Goutte , Abdul Waseh Basit , Felipe Jose Oliveira Varum , Ana Cristina Freire
IPC分类号： A61K9/00 , A61K9/28 , A61K31/196 , A61K31/606 , A61K31/616 , A61K47/32 , A61K47/36 , A61K47/38
CPC分类号： A61K9/2886 , A61K9/0053 , A61K9/2013 , A61K9/2054 , A61K9/284 , A61K9/2846 , A61K9/2853 , A61K9/286 , A61K9/2866 , A61K9/288 , A61K9/2893 , A61K31/196 , A61K31/606 , A61K31/616 , A61K47/32 , A61K47/36 , A61K47/38
摘要： Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an outer layer and at least one layer between the core and the outer layer selected from the group consisting of an isolation layer and an inner layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralised polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. The isolation layer comprises a non-ionic polymer which is soluble in intestinal fluid or gastrointestinal fluid. The outer is applied directly to the inner layer or the isolation layer using a coating preparation formed by combining the first polymeric material in an aqueous medium with a second polymeric material in an organic medium. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.
摘要翻译：将药物延迟释放到结肠是由包含核心和核心涂层的延迟释放制剂实现的。核心包括药物，并且该涂层包括外层和在选自由隔离层和内层组成的组中的核心和外层之间的至少一层。外层包含易受结肠细菌攻击的第一聚合物材料和pH值约为pH5或更高的第二聚合物质的混合物。内层包括可溶于肠液或胃肠液的第三聚合物材料，所述第三聚合物材料选自至少部分中和的多元羧酸和非离子聚合物。在第三聚合物材料是非离子聚合物的实施方案中，内层包括缓冲剂和碱的至少一种。隔离层包含可溶于肠液或胃肠液的非离子聚合物。使用通过将水性介质中的第一聚合物材料与有机介质中的第二聚合物材料组合而形成的涂层制剂将外部直接施加到内层或隔离层。根据本发明的制剂的优点包括当暴露于结肠状况时药物的加速释放和给药后对药物释放的食物和/或酒精作用的降低或消除。

3. 发明授权

US10272048B2 Delayed release drug formulation 有权
公开(公告)号：US10272048B2
公开(公告)日：2019-04-30
申请号：US15267156
申请日：2016-09-16
申请人： Tillotts Pharma AG
发明人： Felipe Josè Oliveira Varum , Roberto Carlos Bravo González , Thomas Buser , Abdul Waseh Basit , Ana Cristina Freire
IPC分类号： A61K9/28 , A61K9/20 , A61K31/606 , A61K9/00 , A61K47/32 , A61K47/36 , A61K31/616 , A61K31/196 , A61K47/38
摘要： In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralized, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

4. 发明申请

US20150132380A1 A DELAYED RELEASE DRUG FORMULATION 有权
标题翻译：延迟释放药物配方
公开(公告)号：US20150132380A1
公开(公告)日：2015-05-14
申请号：US14398005
申请日：2013-04-29
申请人： TILLOTTS PHARMA AG
发明人： Roberto Carlos Bravo Gonzalez , Thomas Buser , Frederic Jean-Claude Goutte , Abdul Waseh Basit , Felipe Jose Oliveira Varum , Ana Cristina Freire
IPC分类号： A61K9/28 , A61K9/00 , A61K31/196
CPC分类号： A61K9/2886 , A61K9/0053 , A61K9/2013 , A61K9/2054 , A61K9/284 , A61K9/2846 , A61K9/2853 , A61K9/286 , A61K9/2866 , A61K9/288 , A61K9/2893 , A61K31/196 , A61K31/606 , A61K31/616 , A61K47/32 , A61K47/36 , A61K47/38
摘要： Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an outer layer and at least one layer between the core and the outer layer selected from the group consisting of an isolation layer and an inner layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralised polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. The isolation layer comprises a non-ionic polymer which is soluble in intestinal fluid or gastrointestinal fluid. The outer is applied directly to the inner layer or the isolation layer using a coating preparation formed by combining the first polymeric material in an aqueous medium with a second polymeric material in an organic medium. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.
摘要翻译：将药物延迟释放到结肠是由包含核心和核心涂层的延迟释放制剂实现的。核心包括药物，并且该涂层包括外层和在选自由隔离层和内层组成的组中的核心和外层之间的至少一层。外层包含易受结肠细菌攻击的第一聚合物材料和pH值约为pH5或更高的第二聚合物质的混合物。内层包括可溶于肠液或胃肠液的第三聚合物材料，所述第三聚合物材料选自至少部分中和的多元羧酸和非离子聚合物。在第三聚合物材料是非离子聚合物的实施方案中，内层包括缓冲剂和碱的至少一种。隔离层包含可溶于肠液或胃肠液的非离子聚合物。使用通过将水性介质中的第一聚合物材料与有机介质中的第二聚合物材料组合而形成的涂层制剂将外部直接施加到内层或隔离层。根据本发明的制剂的优点包括当暴露于结肠状况时药物的加速释放和给药后对药物释放的食物和/或酒精作用的降低或消除。

5. 发明授权

US11534406B2 Delayed release drug formulation 有权
公开(公告)号：US11534406B2
公开(公告)日：2022-12-27
申请号：US16823094
申请日：2020-03-18
申请人： Tillotts Pharma AG
发明人： Felipe José Oliveira Varum , Roberto Carlos Bravo González , Thomas Buser , Abdul Waseh Basit , Ana Cristina Freire
IPC分类号： A61K9/28 , A61K31/606 , A61K9/00 , A61K47/32 , A61K47/36 , A61K31/616 , A61K31/196 , A61K47/38 , A61K9/20
摘要： In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

6. 发明授权

US10799515B2 Delayed release drug formulation 有权
公开(公告)号：US10799515B2
公开(公告)日：2020-10-13
申请号：US15028863
申请日：2013-10-29
申请人： TILLOTTS PHARMA AG
发明人： Felipe Jose Oliveira Varum , Roberto Carlos Bravo Gonzalez , Thomas Buser , Abdul Waseh Basit , Ana Cristina Freire
IPC分类号： A61K31/606 , A61K9/28 , A61J3/00 , A61K9/00
摘要： In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

7. 发明申请

US20200214987A1 DELAYED RELEASE DRUG FORMULATION 审中-公开
公开(公告)号：US20200214987A1
公开(公告)日：2020-07-09
申请号：US16823094
申请日：2020-03-18
申请人： Tillotts Pharma AG
发明人： Felipe José OLIVEIRA VARUM , Roberto Carlos Bravo González , Thomas Buser , Abdul Waseh Basit , Ana Cristina Freire
IPC分类号： A61K9/28 , A61K31/606 , A61K9/00 , A61K47/32 , A61K47/36 , A61K31/616 , A61K31/196 , A61K47/38 , A61K9/20
摘要： In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

8. 发明授权

US10226430B2 Delayed release drug formulation 有权
公开(公告)号：US10226430B2
公开(公告)日：2019-03-12
申请号：US14397977
申请日：2013-04-29
申请人： TILLOTTS PHARMA AG
发明人： Roberto Carlos Bravo Gonzalez , Thomas Buser , Frederic Jean-Claude Goutte , Abdul Waseh Basit , Felipe Jose Oliveira Varum , Ana Cristina Freire
IPC分类号： A61K31/616 , A61K9/28 , A61K31/606 , A61K9/00 , A61K47/32 , A61K47/36 , A61K31/196 , A61K47/38 , A61K9/20
摘要： Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an inner layer and an outer layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralized polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.

9. 发明申请

US20150125525A1 DELAYED RELEASE DRUG FORMULATION 审中-公开
标题翻译：延迟释放药物配方
公开(公告)号：US20150125525A1
公开(公告)日：2015-05-07
申请号：US14397977
申请日：2013-04-29
申请人： TILLOTTS PHARMA AG
发明人： Roberto Carlos Bravo Gonzalez , Thomas Buser , Frederic Goutte , Abdul Waseh Basit , Felipe Jose, Oliveira Varum , Ana Cristina Freire
IPC分类号： A61K9/28 , A61K31/616
CPC分类号： A61K9/2886 , A61K9/0053 , A61K9/2013 , A61K9/2054 , A61K9/284 , A61K9/2846 , A61K9/2853 , A61K9/286 , A61K9/2866 , A61K9/288 , A61K9/2893 , A61K31/196 , A61K31/606 , A61K31/616 , A61K47/32 , A61K47/36 , A61K47/38
摘要： Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an inner layer and an outer layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralised polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.
摘要翻译：将药物延迟释放到结肠是由包含核心和核心涂层的延迟释放制剂实现的。核心包括药物，涂层包括内层和外层。外层包含易受结肠细菌攻击的第一聚合物材料和pH值约为pH5或更高的第二聚合物质的混合物。内层包括可溶于肠液或胃肠液的第三聚合物材料，所述第三聚合物材料选自至少部分中和的多元羧酸和非离子聚合物。在第三聚合物材料是非离子聚合物的实施方案中，内层包括缓冲剂和碱的至少一种。根据本发明的制剂的优点包括当暴露于结肠状况时药物的加速释放和给药后对药物释放的食物和/或酒精作用的降低或消除。

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