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1. 发明授权

US06417167B1 Lyophilized compositions containing shingoglycolipid and process for preparing them 失效
标题翻译：含有胶质糖脂的冻干组合物及其制备方法
公开(公告)号：US06417167B1
公开(公告)日：2002-07-09
申请号：US09897992
申请日：2001-07-05
申请人： Kazutoshi Maruyama , Hideaki Nomura , Akihiko Takeuchi
发明人： Kazutoshi Maruyama , Hideaki Nomura , Akihiko Takeuchi
IPC分类号： A61K3170
CPC分类号： A61K31/7032 , A61K9/0019 , A61K9/19 , A61K47/183 , A61K47/26 , A61K47/28
摘要： The object of the present invention is to improve the solubility of sphingoglycolipids having low solubility in water. Disclosed is a lyophilized composition comprising the &agr;-glycosylceramide represented by the following formula (A) or a salt thereof, a polyoxysorbitan fatty acid ester and disaccharide or monosaccharide, and preferably additional deoxycholic acid or histidine, and a process for preparing it: wherein R1 represents H or OH; X denotes an integer in the range of 7-25; R2 represents any one of the substituents —CH2(CH2)YCH3, —CH(OH)(CH2)YCH3, —CH(OH)(CH2)YCH(CH3)2, —CH═CH(CH2)YCH3, or —CH(OH)(CH2)YCH(CH3)CH2CH3, wherein Y denotes an integer in the range of 5-17; either one of R3 or R4 represents H, and the other represents H, OH, NH2 or NHCOCH3; either one of R5 or R6 represents H, and the other represents OH; either one of R7 or R8 represents H, and the other represents OH; R9 represents H, CH3 or CH2OH.
摘要翻译：本发明的目的是改善在水中溶解度低的鞘糖脂的溶解度。公开了包含下式（A）表示的α-糖基神经酰胺或其盐，多脱氧山梨糖醇脂肪酸酯和二糖或单糖，优选其它脱氧胆酸或组氨酸的冻干组合物及其制备方法，其中R1表示 H或OH; X表示7-25的整数; R2表示取代基-CH2（CH2）YCH3，-CH（OH）（CH2）YCH3，-CH（OH）（CH2）YCH（ CH3）2，-CH = CH（CH2）YCH3或-CH（OH）（CH2）YCH（CH3）CH2CH3，其中Y表示5-17的整数; R3或R4中的任一个表示H，另一个表示H，OH，NH 2或NHCOCH 3; R5或R6中的任一个表示H，另一个表示OH; R7或R8中的任一个表示H，另一个表示OH; R9代表H，CH3或CH2OH。

2. 发明授权

US5597562A Oral dosage form of biologically active proteins 失效
标题翻译：生物活性蛋白质的口服剂型
公开(公告)号：US5597562A
公开(公告)日：1997-01-28
申请号：US167721
申请日：1993-12-15
申请人： Hideaki Nomura , Kazutoshi Maruyama
发明人： Hideaki Nomura , Kazutoshi Maruyama
IPC分类号： A61K9/16 , A61K9/20 , A61K9/28 , A61K9/48 , A61K9/50 , A61K9/54 , A61K38/00 , A61K38/18 , A61K38/19 , A61K38/22 , A61K47/12 , A61K47/18 , A61K47/20 , A61K47/26 , A61K47/34 , A61K47/38 , A61P7/00 , A61P7/06 , A61K45/05 , A61K9/64
CPC分类号： A61K9/5042 , A61K38/1816 , A61K38/193 , A61K9/1617 , A61K9/2013 , A61K9/2866 , A61K9/4858 , A61K9/4891
摘要： An oral dosage form comprising: (a) granulocyte colony stimulating factor or erythropoietin; (b) surfactant(s); (c) fatty acid(s); and (d) enteric material. The oral drug preparations provided by the present invention avoid inactivation of the principal ingredient during the process of pharmaceutical manufacturing and display enhanced absorption of the ingredient from the intestinal tract, particularly as a result of the addition of fatty acid(s) to the drug composition. As such, oral dosage forms of the present invention can allow for dosage reductions, facilitate accurate dose control, and increase the practical usefulness of the bioactive proteins.
摘要翻译：口服剂型，其包含：（a）粒细胞集落刺激因子或促红细胞生成素; （b）表面活性剂; （c）脂肪酸; 和（d）肠道材料。本发明提供的口服药物制剂避免了药物制造过程中主要成分的失活，并且显示了增加成分从肠道的吸收，特别是由于向药物组合物中加入了脂肪酸。因此，本发明的口服剂型可以允许减少剂量，促进准确的剂量控制，并增加生物活性蛋白质的实用性。

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