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1. 发明申请

WO2004047801A2 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
标题翻译：梯度药物在脂质体中的加载方法
公开(公告)号：WO2004047801A2
公开(公告)日：2004-06-10
申请号：PCT/US2003/037964
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie , HU, Ning
发明人： JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie , HU, Ning
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.
摘要翻译：提供了用于将药剂（例如抗肿瘤剂）包封在脂质体中的方法，其优选具有高药物：脂质比率。脂质体可以通过使用跨膜pH梯度通过活性机制加载药物的过程来制备。使用这种技术，捕获效率接近100％。所使用的药物：脂质比率高于较老的传统脂质体制剂，并且药物从脂质体的释放速率降低。上样后，残余的酸用低温下碱可渗透的淬火剂淬灭。残留的酸性因此降低并且化学稳定性（例如抗水解）增强。在施用之前，脂质体和药剂的稳定性因此得以保持。然而，当脂质体在体内给药时存在pH梯度，因为猝灭剂迅速离开脂质体。

2. 发明申请

WO2004047800A3 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
公开(公告)号：WO2004047800A3
公开(公告)日：2004-06-10
申请号：PCT/US2003/037790
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , SULIVAN, Michele , YANG, Stephanie , HU, Ning , JENSEN, Gerard, M.
发明人： SULIVAN, Michele , YANG, Stephanie , HU, Ning , JENSEN, Gerard, M.
IPC分类号： A61K9/127
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

3. 发明申请

WO2005053605A2 THERAPEUTIC LIPOSOMES 审中-公开
标题翻译：治疗药物
公开(公告)号：WO2005053605A2
公开(公告)日：2005-06-16
申请号：PCT/US2004/029265
申请日：2004-09-09
申请人： GILEAD SCIENCES, INC. , JENSEN, Gerard, M. , HU, Ning , PETRASEK, Danny
发明人： JENSEN, Gerard, M. , HU, Ning , PETRASEK, Danny
IPC分类号： A61K
CPC分类号： A61K33/00 , A61K9/0019 , A61K9/0085 , A61K9/127 , A61K31/663 , A61K31/70 , A61K33/06 , A61K33/24 , A61K33/26 , A61K33/28 , A61K33/30 , A61K33/34 , A61K33/38 , A61K45/06
摘要： The invention provides methods for correcting an imbalance of one or more entities in a mammal, as well as therapeutic liposomes and compositions for use with such methods.
摘要翻译：本发明提供了用于校正哺乳动物中一种或多种实体的不平衡的方法，以及用于此类方法的治疗性脂质体和组合物。

4. 发明申请

WO2004047802A2 LIPOSOMAL FORMULATIONS 审中-公开
标题翻译：药物制剂
公开(公告)号：WO2004047802A2
公开(公告)日：2004-06-10
申请号：PCT/US2003/037965
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , JENSEN, Gerard, M. , HU, Ning , CHIANG, Su-Ming , SKENES, Craig, R. , FAHRNER, Richard
发明人： JENSEN, Gerard, M. , HU, Ning , CHIANG, Su-Ming , SKENES, Craig, R. , FAHRNER, Richard
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： The invention provides a formulation comprising a lipophobic therapeutic agent encapsulated in a liposome having improved efficacy and/or reduced toxicity.
摘要翻译：本发明提供一种包含脂质体包封在具有改善的功效和/或降低的毒性的脂质体的抑制剂的制剂。

5. 发明公开

EP1599183A2 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
标题翻译：脂质体的方法为药物的费用梯度。
公开(公告)号：EP1599183A2
公开(公告)日：2005-11-30
申请号：EP03787169.6
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , Jensen, Gerard M.
发明人： HU, Ning , JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

6. 发明公开

EP1567130A2 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
标题翻译：方法脂质体梯度药物CHARGE
公开(公告)号：EP1567130A2
公开(公告)日：2005-08-31
申请号：EP03790130.3
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC.
发明人： HU, Ning , JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

7. 发明公开

EP1565165A2 LIPOSOMAL FORMULATIONS 审中-公开
标题翻译： LIPOSOMZUBEREITUNGEN
公开(公告)号：EP1565165A2
公开(公告)日：2005-08-24
申请号：EP03796497.0
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC.
发明人： JENSEN, Gerard, M. , HU, Ning , CHIANG, Su-Ming , SKENES, Craig, R. , FAHRNER, Richard
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： The invention provides a formulation comprising a lipophobic therapeutic agent encapsulated in a liposome having improved efficacy and/or reduced toxicity.

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