A process for the preparation of a high-melting the form of the chenodeoxycholic as well as high-melting, practically granular crystalline form of the chenodeoxycholic

摘要

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:PP(a) suspending at least one form of CDCA having a melting point of below 160° C. in a non-aromatic liquid hydrocarbon, preferably cyclohexane, to form a suspension having a boiling point of at least 65° C.;PP(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;P P(c) recovering the high-melting form of CDCA from the suspension. PP 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 compositions.