公开(公告)号：US20190336447A1

公开(公告)日：2019-11-07

申请号：US16511380

申请日：2019-07-15

Applicant: FUJIFILM Corporation

Inventor： MAKOTO ONO ,  Kohei ONO ,  Takeshi MATSUMOTO ,  Mikinaga MORI

IPC: A61K9/127 ,  A61K31/7068 ,  B01J13/20 ,  B01J13/02 ,  A61K47/28 ,  A61K47/24

Abstract: Provided are a liposome composition which has a practically required long-term preservation stability, and which has a release rate of a drug on the order of several tens of hours due to releasability of a drug being able to be suitably controlled by rendering an inner water phase hyper-osmotic; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which the content of cholesterols is 10 mol % to 35 mol % with respect to the total amount of lipid components in the liposome composition, and each of the liposomes encapsulates a drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase.

公开(公告)号：US20170042810A1

公开(公告)日：2017-02-16

申请号：US15335640

申请日：2016-10-27

Applicant: FUJIFILM Corporation

Inventor： Takeshi MATSUMOTO ,  Kohei ONO ,  Makoto ONO ,  Kyoko SENGA

IPC: A61K9/127 ,  A61K31/519 ,  A61K31/7068

CPC classification number: A61K9/127 ,  A61K9/1278 ,  A61K31/519 ,  A61K31/7068 ,  A61K45/00 ,  A61K47/24 ,  A61K47/28

Abstract: Provided are a liposome composition which has a practically required long-term preservation stability, and which has a release rate of a drug on the order of several tens of hours due to releasability of a drug being able to be suitably controlled by rendering an inner water phase hyper-osmotic; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which each of the liposomes encapsulates a drug in a dissolved state, an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase, and a release rate of the drug from each of the liposomes is 10%/24 hr to 70%/24 hr in blood plasma at 37° C.; and a method for producing the same.

Abstract translation: 本发明提供一种脂质体组合物，其具有实际上所需的长期保存稳定性，并且由于能够通过使内部水分适当地控制药物的释放性，其具有几十小时数量级的药物的释放速率 相超渗透 及其制造方法。 根据本发明，可以提供一种脂质体组合物，其包括脂质体，其各自具有构成外部水相的内部水相和水溶液，并且其中分散有脂质体，其中每个脂质体包封 处于溶解状态的药物，内部水相的渗透压相对于外部水相的渗透压为2倍〜8倍，并且来自各脂质体的药物的释放速度为10％/ 24小时至70％/ 24小时在37℃的血浆中。 及其制造方法。

公开(公告)号：US20210100745A1

公开(公告)日：2021-04-08

申请号：US17121870

申请日：2020-12-15

Applicant: FUJIFILM Corporation

Inventor： Makoto ONO ,  Kohei ONO ,  Takeshi MATSUMOTO ,  Mikinaga MORI

IPC: A61K9/127 ,  A61K47/24 ,  A61K47/28 ,  B01J13/02 ,  B01J13/20 ,  A61K31/7068

Abstract: Provided are a liposome composition which has a practically required long-term preservation stability, and which has a release rate of a drug on the order of several tens of hours due to releasability of a drug being able to be suitably controlled by rendering an inner water phase hyper-osmotic; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which the content of cholesterols is 10 mol % to 35 mol % with respect to the total amount of lipid components in the liposome composition, and each of the liposomes encapsulates a drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase.

公开(公告)号：US20170202774A1

公开(公告)日：2017-07-20

申请号：US15474644

申请日：2017-03-30

Applicant: FUJIFILM Corporation

Inventor： Makoto ONO ,  Kohei ONO ,  Takeshi MATSUMOTO ,  Mikinaga MORI

IPC: A61K9/127 ,  A61K31/7068

CPC classification number: A61K9/127 ,  A61K9/1278 ,  A61K31/7068 ,  A61K47/24 ,  A61K47/28 ,  B82Y5/00

Abstract: Provided are a liposome composition in which an osmotic pressure of an inner water phase is 2-fold to 8-fold relative to the osmotic pressure of an outer water phase, and which encapsulates a water-soluble drug in a dissolved state, and also exhibits excellent preservation stability; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes obtained from lipids dissolved and emulsified in an organic solvent, each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which each of the liposomes encapsulates a water-soluble drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase; and a method for producing the same.

公开(公告)号：US20170042813A1

公开(公告)日：2017-02-16

申请号：US15336158

申请日：2016-10-27

Applicant: FUJIFILM Corporation

Inventor： Makoto ONO ,  Kohei ONO ,  Takeshi MATSUMOTO ,  Mikinaga MORI

IPC: A61K9/127 ,  A61K31/7068

CPC classification number: A61K9/127 ,  A61K9/1278 ,  A61K31/7068 ,  A61K47/24 ,  A61K47/28 ,  B82Y5/00

Abstract: Provided are a liposome composition in which an osmotic pressure of an inner water phase is 2-fold to 8-fold relative to the osmotic pressure of an outer water phase, and which encapsulates a water-soluble drug in a dissolved state, and also exhibits excellent preservation stability; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes obtained from lipids dissolved and emulsified in an organic solvent, each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which each of the liposomes encapsulates a water-soluble drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase; and a method for producing the same.

Abstract translation: 提供一种脂质体组合物，其中内水相的渗透压相对于外部水相的渗透压为2倍至8倍，并且将水溶性药物包封在溶解状态，并且还显示出 保存稳定性好; 及其制造方法。 根据本发明，可以提供一种脂质体组合物，其包括由在有机溶剂中溶解和乳化的脂质获得的脂质体，每个脂质体具有构成外部水相的内部水相和水溶液， 分散脂质体，其中每个脂质体包封溶解状态的水溶性药物，内部水相的渗透压相对于外部水相的渗透压为2倍至8倍; 及其制造方法。

公开(公告)号：US20170042812A1

公开(公告)日：2017-02-16

申请号：US15336131

申请日：2016-10-27

Applicant: FUJIFILM Corporation

Inventor： Makoto ONO ,  Kohei ONO ,  Yuuko IGARASI

IPC: A61K9/127 ,  A61K31/7068

CPC classification number: A61K9/127 ,  A61K8/14 ,  A61K9/1271 ,  A61K9/1277 ,  A61K31/7068 ,  A61K47/10 ,  A61K47/14 ,  A61K2800/10 ,  A61Q19/00 ,  B01J13/125 ,  Y10S977/773 ,  Y10S977/906 ,  Y10S977/907

Abstract: Provided is a method for producing a liposome having safety and stability. According to the present invention, it is possible to provide a method for producing a liposome, including a step of mixing an oil phase with at least one lipid dissolved in an organic solvent and a water phase and stirring an aqueous solution containing the lipids, and a step of evaporating the organic solvent from the aqueous solution containing the liposomes obtained in the stirring step, in which the organic solvent is a mixed solvent of a water-soluble organic solvent and an ester-based organic solvent.

Abstract translation: 提供一种具有安全性和稳定性的脂质体的制造方法。 根据本发明，可以提供一种生产脂质体的方法，包括将油相与溶于有机溶剂中的至少一种脂质和水相混合并搅拌含有脂质的水溶液的步骤，以及 从在搅拌步骤中得到的含有脂质体的水溶液中蒸发有机溶剂的步骤，其中有机溶剂是水溶性有机溶剂和酯类有机溶剂的混合溶剂。

公开(公告)号：US20170042811A1

公开(公告)日：2017-02-16

申请号：US15336057

申请日：2016-10-27

Applicant: FUJIFILM Corporation

Inventor： Makoto ONO ,  Kohei ONO ,  Takeshi MATSUMOTO ,  Mikinaga MORI

IPC: A61K9/127 ,  A61K31/7068

CPC classification number: A61K9/127 ,  A61K9/1278 ,  A61K31/7068 ,  A61K47/24 ,  A61K47/28 ,  B01J13/02 ,  B01J13/20 ,  Y10S977/773 ,  Y10S977/906 ,  Y10S977/907

Abstract: Provided are a liposome composition which has a practically required long-term preservation stability, and which has a release rate of a drug on the order of several tens of hours due to releasability of a drug being able to be suitably controlled by rendering an inner water phase hyper-osmotic; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which the content of cholesterols is 10 mol % to 35 mol % with respect to the total amount of lipid components in the liposome composition, and each of the liposomes encapsulates a drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase.

Abstract translation: 本发明提供一种脂质体组合物，其具有实际上所需的长期保存稳定性，并且由于能够通过使内部水分适当地控制药物的释放性，其具有几十小时数量级的药物的释放速率 相超渗透 及其制造方法。 根据本发明，可以提供一种脂质体组合物，其包括脂质体，其各自具有构成外部水相的内部水相和水溶液，并且其中分散有脂质体的胆固醇的含量为 相对于脂质体组合物中的脂质成分的总量为10〜35摩尔％，并且每个脂质体将药物包封在溶解状态，内部水相的渗透压为2倍至8倍， 相对于外部水相的渗透压折叠。