title: Solubility and release modulation effect of sulfamerazine ternary complexes with cyclodextrins and meglumine.
abstract: This study investigated the effect on solubility and release of ternary complexes of sulfamerazine (SMR) with β-(βCD), methyl-(MβCD) and hydroxypropyl-β-cyclodextrin (HPβCD) using meglumine (MEG) as the ternary component. The combination of MEG with MβCD resulted the best approach, with an increased effect (29-fold) of the aqueous solubility of SMR. The mode of inclusion was supported by 2D NMR, which indicated that real ternary complexes were formed between SMR, MEG and MβCD or HPβCD. Solid state analysis was performed using Fourier-transform infrared spectroscopy (FT IR), differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD), which demonstrated that different interactions occurred among SMR, MEG and MβCD or HPβCD in the ternary lyophilized systems. The ternary complexes with βCD and MβCD produced an additional retention effect on the release of SMR compared to the corresponding binary complexes, implying that they were clearly superior in terms of solubility and release modulation.
authors.affiliation: Unidad de Investigación y Desarrollo en Ciencia y Tecnología Farmacéutica (UNITEFA-CONICET), Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina; Departamento de Farmácia, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, Rodovia Araraquara-Jau km 1, 14800-900 Araraquara, SP, Brazil. Electronic address: caloisio@fcq.unc.edu.ar.
authors.forename: Carolina
authors.initials: C
authors.lastname: Aloisio
authors.affiliation: Departamento de Farmácia, Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, Rodovia Araraquara-Jau km 1, 14800-900 Araraquara, SP, Brazil. Electronic address: oliveiag@fcfar.unesp.br.
authors.forename: Anselmo Gomes
authors.initials: AG
authors.lastname: de Oliveira
authors.affiliation: Unidad de Investigación y Desarrollo en Ciencia y Tecnología Farmacéutica (UNITEFA-CONICET), Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina. Electronic address: mrlcor@fcq.unc.edu.ar.
authors.forename: Marcela
authors.initials: M
authors.lastname: Longhi
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D005612:Freeze Drying; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008536:Meglumine / Q000737:chemistry*; D033362:Powder Diffraction; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013416:Sulfamerazine / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D013818:Thermogravimetry; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D047392:beta-Cyclodextrins; C108732:methyl-beta-cyclodextrin; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D008536:Meglumine; D013416:Sulfamerazine
keywords: Cyclodextrin; In vitro-release; Solubility; Sulfamerazine; Ternary complex