Process for preparing high-melting chenodeoxycholic acid

C - Chemistry – Metallurgy – 07 – J

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260/62

C07J 9/00 (2006.01)

Patent

CA 1132536

ABSTRACT OF THE DISCLOSURE A process for preparing a high-melting form of CDCA having a melting point of at least about 160°C is disclosed which comprises the steps of: a) suspending at least one form of CDCA having a melting point of below 160°C in a non-aromatic liquid hydro- carbon, preferably cyclohexane, to form a suspension having a boiling point of at least 65°C; b) heating the suspension to a sufficiently high temperature of between about 65 and about 140°C, preferably between about 75 and about 100°C, during a sufficiently long period of time for converting substantially all of the CDCA into the high-melting form; c) recovering the high-melting form of CDCA from the suspension. Low-melting amorphous and/or crystalline forms of CDCA, as well as CDCA-solvent inclusion complexes can be treated in the above-described process. The high-melting CDCA is obtained in form of a substantially granular powder, which is suitable to be formulated into therapeutical compo- sitions.

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