Improvement of Water Solubility of Josamycin by Inclusion Complex with γ-Cyclodextrin

Abstract EN

Josamycin propionate (JMP) is an antibiotic belonging to the family of macrolide.

According to the Biopharmaceutical Classification System (BCS), this compound can be classed in class II, low solubility and high permeability.

In order to increase its apparent water solubility, inclusion complexation between Josamycin propionate and γ-cyclodextrin (γ-CD) was studied.

UV spectrophotometric method was employed to investigate the phase-solubility profile and the stability constant of the complexation in aqueous medium.

Solid state of the binary system prepared by coevaporation (in 50%-50% ethanol/water) has been characterized using powder X-ray diffraction (XRD) and Fourier transformation-infrared spectrometry (FTIR).

These techniques indicate that JMP forms an association complex with γ-CD.

The shift in the nuclear magnetic resonance spectroscopy (1H NMR) confirms the existence of the inclusion complex.

Also the results obtained showed an enhancement of the solubility in water of Josamycin propionate.