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公开(公告)号：US07153838B2
公开(公告)日：2006-12-26
申请号：US09415890
申请日：1999-10-08
IPC分类号： A61K31/7008 , A61K9/07 , A61K25/02
CPC分类号： A61K47/18 , A61K9/0019 , A61K9/08 , A61K9/107 , A61K9/19 , Y10S514/937 , Y10S514/938 , Y10S514/943 , Y10S514/97 , Y10S514/974
摘要： An antifungal composition suitable for parenteral administration to a mammal includes an amount of pimaricin or an antifungal derivative thereof that is effective to inhibit the growth of a fungal infection in a mammal; a pharmaceutically acceptable dipolar aprotic solvent; and a pharmaceutically acceptable aqueous secondary solvent. The composition can be used in methods of preventing or treating a systemic fungal infection in a mammal. The composition can be prepared by dissolving pimaricin or an antifungal derivative thereof in the pharmaceutically acceptable dipolar aprotic solvent; adding to the solution a pharmaceutically acceptable aqueous secondary solvent; and in a preferred method, by subsequently lypohilizing the composition, whereby a dry, shelf-stable composition is produced. This dry composition can be reconstituted into an aqueous solution suitable for parenteral administration.
摘要翻译： 适合于向哺乳动物肠胃外给药的抗真菌组合物包括一定量的有效抑制哺乳动物真菌感染生长的派马林或其抗真菌衍生物; 药学上可接受的偶极非质子溶剂; 和药学上可接受的水性二级溶剂。 该组合物可用于预防或治疗哺乳动物全身真菌感染的方法。 该组合物可以通过将派马林或其抗真菌衍生物溶解在药学上可接受的偶极非质子溶剂中来制备; 向该溶液中加入药学上可接受的水性二级溶剂; 并且在优选的方法中，通过随后将组合物洗脱，由此产生干燥的，稳定的组合物。 该干组合物可以重构成适合肠胃外给药的水溶液。
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2.发明授权公开(公告)号：US07220726B2
公开(公告)日：2007-05-22
申请号：US10439252
申请日：2003-05-15
IPC分类号： A61K31/7008 , A61K9/107 , A61K25/02
CPC分类号： A61K47/18 , A61K9/0019 , A61K9/08 , A61K9/107 , A61K9/19 , Y10S514/937 , Y10S514/938 , Y10S514/943 , Y10S514/97 , Y10S514/974
摘要： An antifungal composition suitable for parenteral administration to a mammal includes an amount of pimaricin or an antifungal derivative thereof that is effective to inhibit the growth of a fungal infection in a mammal; a pharmaceutically acceptable dipolar aprotic solvent; and a pharmaceutically acceptable aqueous secondary solvent. The composition can be used in methods of preventing or treating a systemic fungal infection in a mammal. The composition can be prepared by dissolving pimaricin or an antifungal derivative thereof in the pharmaceutically acceptable dipolar aprotic solvent; adding to the solution a pharmaceutically acceptable aqueous secondary solvent; and in a preferred method, by subsequently lypohilizing the composition, whereby a dry, shelf-stable composition is produced. This dry composition can be reconstituted into an aqueous solution suitable for parenteral administration.
摘要翻译： 适合于向哺乳动物肠胃外给药的抗真菌组合物包括一定量的有效抑制哺乳动物真菌感染生长的派马林或其抗真菌衍生物; 药学上可接受的双极非质子溶剂; 和药学上可接受的水性二级溶剂。 该组合物可用于预防或治疗哺乳动物全身真菌感染的方法。 该组合物可以通过将派马林或其抗真菌衍生物溶解在药学上可接受的偶极非质子溶剂中来制备; 向该溶液中加入药学上可接受的水性二级溶剂; 并且在优选的方法中，通过随后将组合物洗脱，由此产生干燥的，稳定的组合物。 该干组合物可以重构成适合肠胃外给药的水溶液。
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公开(公告)号：US6045815A
公开(公告)日：2000-04-04
申请号：US911607
申请日：1997-08-15
IPC分类号： A61K9/08 , A61K9/107 , A61K9/19 , A61K31/7048 , A61K47/16 , A61K47/18 , A61K47/44 , A61P31/10 , A01N25/02
CPC分类号： A61K47/18 , A61K9/0019 , A61K9/08 , A61K9/107 , A61K9/19 , Y10S514/937 , Y10S514/938 , Y10S514/943 , Y10S514/97 , Y10S514/974
摘要： An antifungal composition suitable for parenteral administration to a mammal includes an amount of pimaricin or an antifungal derivative thereof that is effective to inhibit the growth of a fungal infection in a mammal; a pharmaceutically acceptable dipolar aprotic solvent; and a pharmaceutically acceptable aqueous secondary solvent. The composition can be used in methods of preventing or treating a systemic fungal infection in a mammal. The composition can be prepared by dissolving pimaricin or an antifungal derivative thereof in the pharmaceutically acceptable dipolar aprotic solvent; adding to the solution a pharmaceutically acceptable aqueous secondary solvent; and in a preferred method, by subsequently lypohilizing the composition, whereby a dry, shelf-stable composition is produced. This dry composition can be reconstituted into an aqueous solution suitable for parenteral administration.
摘要翻译： 适合于向哺乳动物肠胃外给药的抗真菌组合物包括一定量的有效抑制哺乳动物真菌感染生长的派马林或其抗真菌衍生物; 药学上可接受的偶极非质子溶剂; 和药学上可接受的水性二级溶剂。 该组合物可用于预防或治疗哺乳动物全身真菌感染的方法。 该组合物可以通过将派马林或其抗真菌衍生物溶解在药学上可接受的偶极非质子溶剂中来制备; 向该溶液中加入药学上可接受的水性二级溶剂; 并且在优选的方法中，通过随后将组合物洗脱，由此产生干燥的，稳定的组合物。 该干组合物可以重构成适合肠胃外给药的水溶液。
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4.发明授权Pharmaceutical formulations: liposomes incorporating aromatic polyene antibiotics 失效药物制剂：掺入芳香多烯抗生素的脂质体
公开(公告)号：US4999199A
公开(公告)日：1991-03-12
申请号：US269638
申请日：1988-11-10
IPC分类号： A61K9/127
摘要： The present invention involves a pharmaceutical formulation comprising a liposome having a therapeutically effective concentration of an aromatic polyene macrolide antibiotic. The aromatic polyene macrolide antibiotic usable in the practice of the present invention is selected from the group consisting of candicidin, hamycin, aurefungin, ascosin, ayfattin, azacolutin, DJ400-B, trichomycin, levorin, heptamycin, candimycin or perimycin. The most preferred aromatic polyene macrolide antibiotic is candicidin. An important aspect of the present invention is a method for treating disseminated fungal infection in an animal comprising administering to an animal such as a human a pharmaceutical formulation comprising a liposome having a therapeutically effective amount of aromatic polyene macrolide antibiotic as described above. The preferred method of such administering is parenteral and the therapeutically effective amount is between about 1 mg/kg body weight and about 20 mg/kg body weight, more preferably between about 2.5 mg/kg body weight and about 6 mg/kg body weight. The parenteral administration is intravenous, intraarterial, subcutaneous, intramuscular, intralymphatic, intraperitoneal or intrapleural. The microorganisms which may be treated by the methods of the present invention comprise C. albicans, C. tropicalis, C. neoformans, aspergillus, cryptococcus, phycomycetes, fusarium, or trichosporin.
摘要翻译： 本发明涉及包含具有治疗有效浓度的芳族多烯大环内酯抗生素的脂质体的药物制剂。 可用于本发明实践中的芳香族多烯大环内酯类抗生素选自念珠菌素，马铃薯霉素，aurefungin，ascosin，ayfattin，azacolutin，DJ400-B，trichomycin，levorin，庚霉素，candimycin或perimycin。 最优选的芳香族多烯大环内酯类抗生素是水cand啶。 本发明的一个重要方面是用于治疗动物中播散性真菌感染的方法，包括向动物如人类施用包含具有治疗有效量的如上所述的芳族多烯大环内酯类抗生素的脂质体的药物制剂。 这种施用的优选方法是肠胃外，治疗有效量为约1mg / kg体重与约20mg / kg体重之间，更优选约2.5mg / kg体重至约6mg / kg体重。 肠胃外给药是静脉内，动脉内，皮下，肌内，淋巴内，腹膜内或胸膜内。 可以通过本发明的方法处理的微生物包括白色念珠菌，热带热带弧菌，新生隐球菌，曲霉菌，隐球菌属，菌纲菌，镰孢菌素或trichosporin。
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