Abstract

A co-crystal of rosiglitazone (Rsg) with berberine (Bbr), Rsg-Bbr, was prepared by the solvent evaporation method and characterized. The results showed that the electrostatic attraction existed between the nitrogen anion of rosiglitazone and the quaternary ammonium cation of berberine, and C-H···O hydrogen bonds were formed between Rsg and Bbr. In the crystal structure, rosiglitazone molecules stack into a supramolecular layer through π-π interactions while π-π interactions between berberine cations also result in a similar layer. The co-crystal presented a low moisture adsorption curve in the range of 0−95% relative humidity values at 25 °C. The improved dissolution rate of rosiglitazone in pH = 6.8 buffer solution could be achieved after forming co-crystal.

Highlights

  • The co-crystal has a history of more than 100 years, it has been used in the field of medicine in the last two decades [1]

  • Powder X-ray Diffraction (PXRD) were used for the preliminary detection of in thethe difference between andThe two Fourier-transform infrared (FT-IR)

  • Infrared spectroscopy is adifference simple and rapid test method theraw co-crystal screening experiment, spectroscopy andbetween rapid test method in the co-crystal screening experiment, it can Infrared preliminarily identify is thea simple difference the co-crystal and two materials by comparing it can preliminarily identify In thethe difference thethe co-crystal two materials by stretching comparing with individual components

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Summary

Introduction

The co-crystal has a history of more than 100 years, it has been used in the field of medicine in the last two decades [1]. It is worth noting that drug-drug co-crystals based on two APIs have attracted new attention in the pharmaceutical field recently [4,5,6]. This multidrug crystal is superior to traditional drug crystal because it is one drug that contains two APIs to achieve the effect of synergistic treatment for specific diseases [7]. The formation of reliable supramolecular synthons between two different chemical structures of APIs is essential for the rational design of drug-drug co-crystals [10]

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