Cryomodification of drugs: Micronization and crystalline structures of 1-(aminomethyl)-cyclohexaneacetic acid

Cryochemical modification is a method of micronization and changing of the crystalline structure of organic substances that in application with drug substances may lead to the improvement of their biopharmacological properties. This method was successfully developed for a chemically labile compound named gabapentin 1-(aminomethyl)-cyclohexaneacetic acid]. According to the data obtained by X-ray diffraction, FTIR spectroscopy, and differential scanning calorimetry (DSC), the formation of two kinetically stable polymorphic modifications of gabapentin (forms with melting points of 157°C and 163°C), which are different from the initial commercial one (with a melting point of 153°C) was observed. These two forms are well known, but the advantage of this work is in developing a new method of their production that excludes the use of any solvents, which is very important for environmental safety.