Vilazodone organic pharmaceutical cocrystal and preparation method thereof

Abstract

The invention belongs to the field of organic pharmaceutical cocrystal technology and specifically relates to a vilazodone organic pharmaceutical cocrystal and a preparation method thereof. The pharmaceutical cocrystal uses vilazodone as an active component and glucide as a precursor. A basic structural unit of the vilazodone organic pharmaceutical cocrystal comprises four vilazodone molecules and four glucide molecules and a three-dimensional network structure of the vilazodone organic pharmaceutical cocrystal is formed by extending vilazodone molecule and glucide molecule in the direction of X, Y, and Z through hydrogen bond. Space group of the pharmaceutical cocrystal is monoclinic system with axial lengths of a=11.0269-11.1269, b=18.3006-18.4006, c=15.4106-15.4106 and axial angles of alpha=89.950 degrees-90.050 degrees, beta=100.631 degrees-100.731 degrees, gamma=89.950 degrees-90.050 degrees. According to the invention, formation of new crystalline phase of the pharmaceutical cocrystal not only retains the pharmacological properties of the drug but also provides possibilities for further increasing efficacy and bioavailability through modification of physical and chemical properties of the drug such as melting point, stability, solubility, dispersion rate and the like.

Description

technical field [0001] The invention belongs to the technical field of organic drug co-crystals, and in particular relates to a vilazodone 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 is a science ...

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

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