LYOPHILIZED COMPOSITIONS CONTAINING SPHINGOGLYCOLIPID AND PROCESS FOR PREPARING THEM - Patent Pending

(12) Patent Application: (11) CA 2280130
ABSTRACT:
An object of the invention is to improve the solubility of a glycosphingolipid having a low solubility in water by preparing a freeze-dried composition therefrom. The freeze-dried composition comprises an .alpha.-glycosylceramide represented by general formula (A) or a salt thereof, a polyoxysorbitan/fatty acid ester, and a disaccharide or monosaccharide and preferably further contains deoxycholic acid or histidine. On said formula, R1 is H or OH; X is an integer of 7 to 25; R2 is -CH2(CH2)YCH3, -CH(OH)(CH2)YCH3, CH(OH)(CH2)YCH(CH3)2, -CH=CH(CH2)YCH3, or -CH(OH)(CH2)YCH(CH3)CH2CH3 (where Y is an integer of 5 to 17); one of R3 and R4 is H and the other is H, OH, NH2, or NHCOCH3; one of R5 and R6 is H and the other is OH; one of R7 and R8 is H and the other is OH; and R9 is H, CH3, or CH2OH.
(72) Inventors (Country): MARUYAMA, KAZUTOSHI (Japan)
TAKEUCHI, AKIHIKO (Japan)
NOMURA, HIDEAKI (Japan)
(73) Owners (Country): KIRIN BEER KABUSHIKI KAISHA (Japan)
(71) Applicants (Country): KIRIN BEER KABUSHIKI KAISHA (Japan)
(74) Agent: FETHERSTONHAUGH & CO.
(45) Issued:
(86) PCT Filing Date: Feb. 4 , 1998
(87) PCT Publication Date: Aug. 13, 1998
Examination requested: Dec. 27, 2002
(51) International Class (IPC): A61K 9/14
A61K 31/70
Patent Cooperation Treaty (PCT): Yes (85) National Entry: Aug. 4 , 1999
(86) PCT Filing number: PCT/JP1998/000462
(87) International publication number: WO1998/034623
(30) Application priority data: Application No. Country Date
22585/1997 Japan Feb. 5 , 1997
Availability of licence: N/A
Language of filing: English