Solid dispersion composition of fr-900506 substance

A - Human Necessities – 61 – K

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167/163, 167/232

A61K 31/445 (2006.01) A61K 9/14 (2006.01) A61K 47/00 (2006.01) C07D 498/18 (2006.01)

Patent

CA 1302279

ABSTRACT OF THE DISCLOSURE A solid dispersion comprising FR-900506 which is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxy- cyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27- tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9] octacos-18-ene-2,3,10,16-tetraone and a water soluble polymer. The preparation of FR-900506 by fermentation of a strain belonging to the genus Streptomyces is also disclosed. The dispersion possesses pharmacological activities such as immunosuppressive activity and anti- microbial activity and is therefore useful for the treatment and prevention of rejection by transplanta- tion, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases and the like. As used in the form of the above dispersion the ratio of absorption into blood is fully adequate and the dispersion has good bioavail- ability. The preparation of FR-900506 is also dis- closed.

533582

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