公开(公告)号：US20140205650A1

公开(公告)日：2014-07-24

申请号：US14342931

申请日：2012-09-06

申请人： Thorsteinn Loftsson

发明人： Thorsteinn Loftsson

IPC分类号： A61K9/02 ,  A61K31/20 ,  A61K31/573 ,  A61K35/60 ,  A61K31/167 ,  A61K31/202 ,  A61K31/201

CPC分类号： A61K31/167 ,  A61K9/0031 ,  A61K9/02 ,  A61K9/025 ,  A61K31/20 ,  A61K31/201 ,  A61K31/202 ,  A61K31/573 ,  A61K35/60 ,  A61K47/14 ,  A61K47/44

摘要： The invention relates to coating of suppositories containing free unsaturated fatty acid, fatty acid ethyl ester and fatty acid monoglyceride that are susceptible to oxidative degradation. The coating retards oxidative degradation of unsaturated fatty acids and gives the suppository a non-oily and smooth surface. The coating will enhance the shelf-life of the suppository and allow their storage at room temperature for extended time period. The coating may or may not contain medicament such as local anesthetic or steroid. According to this invention chemically unstable fatty acids in coated suppositories can be used to stimulate the process of defecation or to treat disorders such as hemorrhoids, bacterial infections, viral infections and inflammations, as well as against fissura ani and pruritus ani. Furthermore, coating suppositories, that contain high concentrations of free fatty acids, can reduce acid induced rectal irritation.

摘要翻译： 本发明涉及含有易氧化降解的游离不饱和脂肪酸，脂肪酸乙酯和脂肪酸单甘油酯的栓剂的包衣。 涂层延缓了不饱和脂肪酸的氧化降解，使栓剂成为非油性和光滑的表面。 涂层将增强栓剂的保存期限，并允许其在室温下长时间储存​​。 涂层可以包含或可以不含有诸如局部麻醉剂或类固醇的药物。 根据本发明，涂覆的栓剂中的化学不稳定的脂肪酸可以用于刺激排便过程或治疗诸如痔疮，细菌感染，病毒感染和炎症的疾病，以及针对肛裂和瘙痒症。 此外，包含高浓度游离脂肪酸的涂层栓剂可以减少酸诱导的直肠刺激。

公开(公告)号：US20070020336A1

公开(公告)日：2007-01-25

申请号：US11489466

申请日：2006-07-20

申请人： Thorsteinn Loftsson ,  Einar Stefansson

发明人： Thorsteinn Loftsson ,  Einar Stefansson

IPC分类号： A61K38/13 ,  A61K38/39 ,  A61K31/724 ,  A61K31/717 ,  A61K31/573 ,  A61K31/5513 ,  A61K31/557 ,  A61K31/19 ,  A61K9/14

CPC分类号： A61K47/48969 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/10 ,  A61K31/404 ,  A61K31/42 ,  A61K31/5377 ,  A61K31/5513 ,  A61K31/565 ,  A61K31/573 ,  A61K31/58 ,  A61K38/13 ,  A61K47/6905 ,  A61K47/6951 ,  B82Y5/00 ,  Y10S514/914

摘要： The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist. Further, the invention provides a method for treating a condition of the posterior segment and/or anterior segment of the eye comprising applying to the eye surface, in an amount which delivers to said segment or segments a therapeutically effective amount of a drug suitable for treating said condition, an ophthalmic composition which is as defined above. Nasal compositions and methods and ophthalmic and nasal compositions in powder form are also provided.

摘要翻译： 本发明提供了一种眼用组合物，其为包含药物，环糊精和水的水性悬浮液，所述组合物的水相为溶液中约0.1％（w / v）至约90％（w / v） 溶解的药物和溶解的药物/环糊精复合物，以及作为固体药物/环糊精颗粒的约10％（w / v）至约99.9％（w / v）的药物的固相，悬浮于 水相; 固体颗粒的尺寸为约10nm至约1mm，药物/环糊精颗粒能够在施用于眼表面后24小时内溶解于水性泪液中。 水性眼睛悬浮液可以是滴眼液，眼凝胶或眼睛雾沫的形式。 此外，本发明提供了一种用于治疗眼部后段和/或前段的病症的方法，包括向眼表面施用一定量的量，其量递送至所述片段或分段治疗有效量的适于治疗的药物 所述病症，如上所述的眼用组合物。 还提供鼻组合物和方法以及粉末形式的眼和鼻组合物。

公开(公告)号：US4885174A

公开(公告)日：1989-12-05

申请号：US198798

申请日：1988-05-25

申请人： Nicholas Bodor ,  Thorsteinn Loftsson

发明人： Nicholas Bodor ,  Thorsteinn Loftsson

IPC分类号： A61K47/10 ,  A61K9/00 ,  A61K9/70 ,  A61K31/047 ,  A61K31/21 ,  A61K31/565 ,  A61K47/12

CPC分类号： A61K9/7023 ,  A61K31/21 ,  A61K31/565 ,  A61K47/10 ,  A61K47/12 ,  A61K9/0014 ,  Y10S514/947

摘要： Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

摘要翻译： 公开了包含药物活性成分和载体的药物制剂，其包含单独或与油酸组合的由2-乙基-1,3-己二醇组成的经皮穿透增强剂。 基于载体的重量，2-乙基-1,3-己二醇的存在量可以在约50％至100％的范围内。 油酸可以与2-乙基-1,3-己二醇组合使用，其量为载体重量的约1至40％，以提供经皮渗透增强方面的协同效应。 已经发现单独使用和/或与油酸组合使用的化合物2-乙基-1,3-己二醇显着增强了从透皮递送系统向患者递送药物。

公开(公告)号：US4764381A

公开(公告)日：1988-08-16

申请号：US806257

申请日：1985-12-06

申请人： Nicholas Bodor ,  Thorsteinn Loftsson

发明人： Nicholas Bodor ,  Thorsteinn Loftsson

IPC分类号： A61K47/10 ,  A61K9/00 ,  A61K9/70 ,  A61K31/047 ,  A61K31/21 ,  A61K31/565 ,  A61K47/12 ,  A61L15/03 ,  A61F13/00 ,  A61K9/06

CPC分类号： A61K9/7023 ,  A61K31/21 ,  A61K31/565 ,  A61K47/10 ,  A61K47/12 ,  A61K9/0014 ,  Y10S514/947

摘要： Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

摘要翻译： 公开了包含药物活性成分和载体的药物制剂，其包含单独或与油酸组合的由2-乙基-1,3-己二醇组成的经皮穿透增强剂。 基于载体的重量，2-乙基-1,3-己二醇的存在量可以在约50％至100％的范围内。 油酸可以与2-乙基-1,3-己二醇组合使用，其量为载体重量的约1至40％，以提供经皮渗透增强方面的协同效应。 已经发现单独使用和/或与油酸组合使用的化合物2-乙基-1,3-己二醇显着增强了从透皮递送系统向患者递送药物。

公开(公告)号：US08372425B2

公开(公告)日：2013-02-12

申请号：US12609845

申请日：2009-10-30

申请人： Thorsteinn Loftsson ,  Einar Stefansson

发明人： Thorsteinn Loftsson ,  Einar Stefansson

IPC分类号： A61K35/60 ,  A61K9/02

CPC分类号： A61K31/202 ,  A61K31/20 ,  A61K31/201

摘要： The invention relates to fatty acid stimulation of rectal mucosa initiating the process of defecation, acting as a laxative. Furthermore, the invention relates to the usage of free fatty acids, fatty acid mixtures and fatty acid extracts from marine lipids in pharmaceutical formulations such as suppositories, ointments, tablets and gelatin capsules for treatment and prevention of multiple disorders like constipation, hemorrhoids, bacterial infections (e.g. helicobacter pylori), viral infections (e.g. herpes simplex virus infections) and inflammations, as well as against fissura ani and pruritus ani.

公开(公告)号：US20120028944A1

公开(公告)日：2012-02-02

申请号：US13014964

申请日：2011-01-27

申请人： Thorsteinn Loftsson ,  Einar Stefansson

发明人： Thorsteinn Loftsson ,  Einar Stefansson

IPC分类号： A61K31/573 ,  A61K31/403 ,  A61K38/13 ,  A61K31/565 ,  A61P31/12 ,  A61K31/42 ,  A61K31/58 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61K31/506 ,  A61K31/5513

CPC分类号： A61K31/5377 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/10 ,  A61K31/404 ,  A61K31/42 ,  A61K31/5513 ,  A61K31/565 ,  A61K31/573 ,  A61K31/58 ,  A61K38/13 ,  A61K47/6905 ,  A61K47/6951 ,  B82Y5/00 ,  Y10S514/914

摘要： The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist. Further, the invention provides a method for treating a condition of the posterior segment and/or anterior segment of the eye comprising applying to the eye surface, in an amount which delivers to said segment or segments a therapeutically effective amount of a drug suitable for treating said condition, an ophthalmic composition which is as defined above. Nasal compositions and methods and ophthalmic and nasal compositions in powder form are also provided.

摘要翻译： 本发明提供了一种眼用组合物，其为包含药物，环糊精和水的水性悬浮液，所述组合物的水相为溶液中约0.1％（w / v）至约90％（w / v） 溶解的药物和溶解的药物/环糊精复合物，以及作为固体药物/环糊精颗粒的约10％（w / v）至约99.9％（w / v）的药物的固相，悬浮于 水相; 固体颗粒的尺寸为约10nm至约1mm，药物/环糊精颗粒能够在施用于眼表面后24小时内溶解于水性泪液中。 水性眼睛悬浮液可以是滴眼液，眼凝胶或眼睛雾沫的形式。 此外，本发明提供了一种用于治疗眼部后段和/或前段的病症的方法，包括向眼表面施用一定量的量，其量递送至所述片段或分段治疗有效量的适于治疗的药物 所述病症，如上所述的眼用组合物。 还提供鼻组合物和方法以及粉末形式的眼和鼻组合物。

公开(公告)号：US4983396A

公开(公告)日：1991-01-08

申请号：US412730

申请日：1989-09-26

申请人： Nicholas Bodor ,  Thorsteinn Loftsson

发明人： Nicholas Bodor ,  Thorsteinn Loftsson

IPC分类号： A61K9/70 ,  A61K31/21 ,  A61K31/565 ,  A61K47/10 ,  A61K47/12

CPC分类号： A61K31/565 ,  A61K31/21 ,  A61K47/10 ,  A61K47/12 ,  A61K9/7023 ,  Y10S514/947

摘要： Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

摘要翻译： 公开了包含药物活性成分和载体的药物制剂，其包含单独或与油酸组合的由2-乙基-1,3-己二醇组成的经皮穿透增强剂。 基于载体的重量，2-乙基-1,3-己二醇的存在量可以在约50％至100％的范围内。 油酸可以与2-乙基-1,3-己二醇组合使用，其量为载体重量的约1至40％，以提供经皮渗透增强方面的协同效应。 已经发现单独使用和/或与油酸组合使用的化合物2-乙基-1,3-己二醇显着增强了从透皮递送系统向患者递送药物。

公开(公告)号：US08633172B2

公开(公告)日：2014-01-21

申请号：US13758955

申请日：2013-02-04

申请人： Thorsteinn Loftsson ,  Einar Stefansson

发明人： Thorsteinn Loftsson ,  Einar Stefansson

IPC分类号： A61K31/724 ,  A61K31/715

CPC分类号： A61K47/48969 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/10 ,  A61K31/404 ,  A61K31/42 ,  A61K31/5377 ,  A61K31/5513 ,  A61K31/565 ,  A61K31/573 ,  A61K31/58 ,  A61K38/13 ,  A61K47/6905 ,  A61K47/6951 ,  B82Y5/00 ,  Y10S514/914

摘要： The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist. Further, the invention provides a method for treating a condition of the posterior segment and/or anterior segment of the eye comprising applying to the eye surface, in an amount which delivers to said segment or segments a therapeutically effective amount of a drug suitable for treating said condition, an ophthalmic composition which is as defined above. Nasal compositions and methods and ophthalmic and nasal compositions in powder form are also provided.

摘要翻译： 本发明提供了一种眼用组合物，其为包含药物，环糊精和水的水性悬浮液，所述组合物的水相为溶液中约0.1％（w / v）至约90％（w / v） 溶解的药物和溶解的药物/环糊精复合物，以及作为固体药物/环糊精颗粒的约10％（w / v）至约99.9％（w / v）的药物的固相，悬浮于 水相; 固体颗粒的尺寸为约10nm至约1mm，药物/环糊精颗粒能够在施用于眼表面后24小时内溶解于水性泪液中。 水性眼睛悬浮液可以是滴眼液，眼凝胶或眼睛雾沫的形式。 此外，本发明提供了一种用于治疗眼部后段和/或前段的病症的方法，包括向眼表面施用一定量的量，其量递送至所述片段或分段治疗有效量的适于治疗的药物 所述病症，如上所述的眼用组合物。 还提供鼻组合物和方法以及粉末形式的眼和鼻组合物。

公开(公告)号：US20100113387A1

公开(公告)日：2010-05-06

申请号：US12609845

申请日：2009-10-30

申请人： Thorsteinn Loftsson ,  Einar Stefansson

发明人： Thorsteinn Loftsson ,  Einar Stefansson

IPC分类号： A61K31/724 ,  A61K31/22 ,  A61K31/19 ,  A61K31/20 ,  A61K31/201 ,  A61P1/00 ,  A61K31/202 ,  A61P31/22

CPC分类号： A61K31/202 ,  A61K31/20 ,  A61K31/201

摘要： The invention relates to fatty acid stimulation of rectal mucosa initiating the process of defecation, acting as a laxative. Furthermore, the invention relates to the usage of free fatty acids, fatty acid mixtures and fatty acid extracts from marine lipids in pharmaceutical formulations such as suppositories, ointments, tablets and gelatin capsules for treatment and prevention of multiple disorders like constipation, hemorrhoids, bacterial infections (e.g. helicobacter pylori), viral infections (e.g. herpes simplex virus infections) and inflammations, as well as against fissura ani and pruritus ani.

摘要翻译： 本发明涉及直肠粘膜的脂肪酸刺激，引发排便过程，作为泻药。 此外，本发明涉及在诸如栓剂，软膏剂，片剂和明胶胶囊的药物制剂中来自海洋脂质的游离脂肪酸，脂肪酸混合物和脂肪酸提取物的用途，用于治疗和预防诸如便秘，痔疮，细菌感染 （例如幽门螺杆菌），病毒感染（例如单纯疱疹病毒感染）和炎症，以及针对烟草和瘙痒症。

公开(公告)号：US07115586B2

公开(公告)日：2006-10-03

申请号：US10272936

申请日：2002-10-18

申请人： Thorsteinn Loftsson

发明人： Thorsteinn Loftsson

IPC分类号： A61K31/724 ,  A61K31/19 ,  C08B30/18

CPC分类号： B82Y5/00 ,  A61K31/724 ,  A61K45/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/38 ,  A61K47/40 ,  A61K47/6951 ,  A61K2300/00

摘要： The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with β-cyclodextrin in an aqueous complexation medium comprising β-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with β-cyclodextrin and its inclusion complexes.