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1. 发明授权

US06726926B2 Gene-entrapped liposomes preparation and process for the preparation thereof 失效
标题翻译：基因截留的脂质体制备及其制备方法
公开(公告)号：US06726926B2
公开(公告)日：2004-04-27
申请号：US09790727
申请日：2001-02-23
申请人： Haruyoshi Yajima , Keizo Sakuda , Hideshi Ideno , Kunio Yagi , Nobuko Ohishi , Jun Yoshida
发明人： Haruyoshi Yajima , Keizo Sakuda , Hideshi Ideno , Kunio Yagi , Nobuko Ohishi , Jun Yoshida
IPC分类号： A61K9127
CPC分类号： A61K31/711 , A61K9/1271 , A61K9/1272 , C12N15/88
摘要： It provides a gene-entrapping liposome preparation which can be preserved over a long period of time, and a process for the preparation of the same. The preparation can be prepared by adding an aqueous solution of disaccharide to gene-entrapping liposomes. The frozen preparation can be preserved for 6 months or more at preservation temperature of −20° C., and the preparation shows excellent restoration ability in water and does not show reduction in biological activity. In the case of the lyophilized preparation, it can be preserved for longer time of about 1 year, shows excellent restoration ability in water, and does not show reduction in biological activity.
摘要翻译：它提供了可以长期保存的基因捕获脂质体制剂及其制备方法。该制剂可以通过将二糖水溶液加入到基因捕获的脂质体中来制备。冷冻制剂可在-20℃的保存温度下保存6个月以上，该制剂在水中显示出优异的恢复能力，并且不显示出生物活性的降低。在冻干制剂的情况下，其可以保存较长时间约1年，在水中显示出优异的恢复能力，并且不显示生物活性的降低。

2. 发明授权

US08889155B2 Gel composition for treating mycosis 有权
标题翻译：用于治疗真菌病的凝胶组合物
公开(公告)号：US08889155B2
公开(公告)日：2014-11-18
申请号：US12521483
申请日：2007-12-28
申请人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
发明人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
IPC分类号： A61K9/00 , A61K47/32 , A61K47/26 , A61K47/10 , A61K47/14 , A61K31/454 , A61K9/06
CPC分类号： A61K31/454 , A61K9/0014 , A61K9/06 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32
摘要： The present invention provides a stable gel composition for mycosis treatment, with increased absorption and permeation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin -1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol into a target site (skin and nail). The gel composition for mycosis treatment, comprises (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl) -1-(1H-1,2,4-triazol-1-yl)-butan-2-ol or an acid addition salt thereof, a lower alcohol, a polyhydric alcohol and a gel-forming polymer. The gel composition of the present invention increases permeation of the above compound into a target site and into the nail. The gel composition of the present invention allows the drug to be directly and rapidly absorbed and permeated into a target site in a constant manner, for mycosis treatment, particularly onychomycosis treatment.
摘要翻译：本发明提供了用于真菌病治疗的稳定凝胶组合物，其中（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H -1,2,4-三唑-1-基） - 丁-2-醇转化成靶位点（皮肤和指甲）。用于真菌病治疗的凝胶组合物包含（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H-1,2,4-三唑-1-基） - 丁基） - 丁-2-醇或其酸加成盐，低级醇，多元醇和凝胶形成聚合物。本发明的凝胶组合物增加了上述化合物渗透到靶部位和钉子中。本发明的凝胶组合物允许药物以恒定的方式直接且快速地吸收并渗透到靶位点，用于真菌病治疗，特别是甲真菌病治疗。

3. 发明申请

US20100317695A1 GEL COMPOSITION FOR TREATING MYCOSIS 有权
标题翻译：用于治疗糖皮质激素的凝胶组合物
公开(公告)号：US20100317695A1
公开(公告)日：2010-12-16
申请号：US12521483
申请日：2007-12-28
申请人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
发明人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
IPC分类号： A61K31/454 , A61P31/10
CPC分类号： A61K31/454 , A61K9/0014 , A61K9/06 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32
摘要： The present invention aims to provide a gel composition for mycosis treatment, which ensures good absorption and permeation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol into a target site (skin and nail). The present invention also aims to provide a gel composition for mycosis treatment, which is excellent in stability of this drug.It is a gel composition for mycosis treatment, which comprises (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol or an acid addition salt thereof, a lower alcohol, a polyhydric alcohol and a gel-forming polymer.The gel composition of the present invention is excellent in permeation of KP-103 into a target site and also excellent in permeation into the nail. Thus, the gel composition of the present invention allows the drug to be directly and rapidly absorbed and permeated into a target site in a constant manner, and thereby produces an excellent effect in mycosis treatment, particularly onychomycosis treatment.
摘要翻译：本发明旨在提供用于真菌病治疗的凝胶组合物，其确保（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1- （1H-1,2,4-三唑-1-基） - 丁-2-醇转化成靶位点（皮肤和指甲）。本发明的目的还在于提供一种用于真菌病治疗的凝胶组合物，该药物的稳定性优异。它是用于真菌病治疗的凝胶组合物，其包含（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H- 三唑-1-基） - 丁-2-醇或其酸加成盐，低级醇，多元醇和形成凝胶的聚合物。本发明的凝胶组合物的KP-103在目标部位的渗透性优异，对于指甲的渗透性优异。因此，本发明的凝胶组合物能够使药物以恒定的方式直接且快速地吸收并渗透到靶部位，从而在真菌病治疗，特别是甲真菌病治疗中产生优异的效果。

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