Lyophilized compositions containing shingoglycolipid and process for preparing them

US6417167B1 · kind B1 · utility

Assignee

• KIRIN BEER KABUSHIKI KAISHA · JP

Inventors

• Kazutoshi Maruyama · Maebashi, JP
• Hideaki Nomura · Takasaki, JP
• Akihiko Takeuchi · Susono, JP

Key dates

• Filing date: Jul 5, 2001
• Grant date: Jul 9, 2002
• Expiry date: Jul 5, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K47/28
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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: whereinR1 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.