The Preparation And Quality Control Of Olanzapine Bulk

Olanzapine (OLN) is a new atypical antipsychotic drug, which is developed by Lilly and listed for the first time in1996in the United States. Its trade name is a tablet, called Zyprexa. Compared with other classic antipsychotics, OLN has good effect and small side effects, so it has widely clinical used for the treatment of mental illness.Based on the optimization process of key steps that used for synthesizing OLN, TBD and N-methyl piperazine which is purchased as raw material, without solvent, backflow reaction and vacuum distilling excessive N-methyl piperazine after completely reaction, three groups of OLN is synthesized at the end. The average yield is99.7%. Next, the three groups of OLN is crystallizated using ethanol, average yield is70.5%.Several important crystal forms of OLN are synthesized using different solvent and methods. Determine the stability of two main medicinal crystal forms, OLN crystal form I and form II. They all have good stability.Place three groups of OLN respectively in the condition of20℃and45℃for1,2,3,6,9months as the stability test. Use different high-performance liquid chromatography (HPLC) methods to determine assay and impurities of OLN. The assay of OLN is more than99%and the impurities content below0.4%.