| 摘要 |
Crystalline form IV of agomelatine (N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide) is disclosed, wherein the crystalline form IV of agomelatine has powder X-ray diffraction diagram, measured using a diffractometer (copper anticathode) and expressed in terms of inter-planar distance d (17.524-3.190 A[deg]), Bragg's angle 2 theta (5.04-27.95 degree), intensity and relative intensity (expressed as a percentage with respect to the most intense ray). A process for the preparation of the crystalline form IV of agomelatine is disclosed, wherein agomelatine is heated at 110[deg.] C. until completely melted, is then rapidly cooled between 50 and 70[deg.] C, and is maintained for about 5 hours at 70[deg.] C until crystallisation occurs. A pharmaceutical composition comprising as active ingredient an effective amount of crystalline form IV of agomelatine is suitable for treating sleep disorders, stress, anxiety, seasonal affective disorders or severe depression, cardiovascular pathologies, pathologies of the digestive system, insomnia and fatigue due to jetlag, schizophrenia, panic attacks, melancholia, appetite disorders, obesity, insomnia, psychotic disorders, epilepsy, diabetes, Parkinson's disease, senile dementia, various disorders associated with normal or pathological ageing, migraine, memory loss, Alzheimer's disease, cerebral circulation disorders, and also in sexual dysfunction, as ovulation inhibitors, immunomodulators and cancers.
|
