Iloperidone-saccharin organic pharmaceutical co-crystal and preparation method thereof

Abstract

The invention belongs to the technical field of organic pharmaceutical co-crystals, and particularly relates to an iloperidone-saccharin organic pharmaceutical co-crystal and a preparation method thereof. The iloperidone is taken as a crude drug, and the saccharin is taken as a precursor; the basic structural unit of a co-crystal is composed of 4 iloperidone molecules and 4 saccharin molecules; an N-H / N hydrogen bond is formed by taking an H atom positioned on the pentatomic N of the saccharin molecules as a hydrogen bond donator and an N atom positioned on the piperidine ring of the iloperidone molecules as a hydrogen bond receptor in an X direction; ester group-containing six-membered rings contained in two adjacent iloperidone molecules have pi-pi accumulation action in a Y direction; an F-containing aromatic six-membered ring contained in the iloperidone molecule and the ester group-containing six-membered ring contained in the other iloperidone molecule have accumulation action along a Z direction on Y and Z surfaces; the space group of the pharmaceutical co-crystal is a triclinic crystal system; a selected solvent is ethanol and is prepared by adopting a solvent reflux-volatilization method; and a crystal is separated out in the volatilizing process of the solvent because the boiling point of the organic solvent is lower.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to an iloperidone-saccharin organic drug co-crystal and a preparation method thereof. Background technique [0002] In 1894, E. Fischer of Germany proposed the "lock-key" model based on the idea of ​​"selective interaction between molecules", which was the prototype of modern supramolecular science theory. In 1937, German K.L.Wolf et al. created the term "supramolecular" to describe highly ordered entities formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to them as The structural level of matter aggregation state is called "supramolecular". It was not until 1978 that Professor J.M.Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional research on the host-guest system rooted in organic chemistry. Supramolecular chemistry i...

AI Technical Summary

Problems solved by technology

Drug crystal form research and solid-state characterization of drugs are relatively mature and highly valued fields in the European and American pharmaceutical industry, but they are still in their infancy in the domestic pharmaceutical industry

Images