Characterization, inclusion mode, phase-solubility and in vitro release studies of inclusion binary complexes with cyclodextrins and binary system with meglumine using sulfamerazine as model drug

C. ALOISIO; A. GOMES DE OLIVEIRA; M.R. LONGHI

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY

TAYLOR & FRANCIS INC

Lugar: Londres; Año: 2014 vol. 40 p. 919 - 919

0363-9045

n order to investigate the effect on the aqueous solubility and release rate of sulfamerazine (SMR) as model drug, inclusion complexes with b-cyclodextrin (ßCD), methyl-b-cyclodextrin (MßCD) and hydroxypropyl-b-cyclodextrin (HPßCD) and a binary system with meglumine (MEG) were developed. The formation of 1:1 inclusion complexes of SMR with the CDs and a SMR:MEG binary system in solution and in solid state was revealed by phase solubility studies (PSS), nuclear magnetic resonance (NMR), Fourier-transform infrared spectroscopy (FT-IR), thermal analysis and X-Ray diffractometry (XRD) studies. The CDs solubilization of SMR could be improved by ionization of the drug molecule through pH adjustments. The higher apparent stability constants of SMR:CDs complexes were obtained in pH 2.00, demonstrating that CDs present more affinity for the unionized drug. The best approach for SMR solubility enhancement results from the combination of MEG and pH a