RESUMEN
The solid state properties and dissolution behaviour of binary systems of mefloquine hydrochloride (MH) with betaCD were investigated. MH-betaCD interaction in the solution state was studied by phase solubility analysis and demonstrates the ability of 3CD to complex with MH giving AL type profile with 120.34 M-1 stability constant. The kneading method was adopted to prepare binary sytems of MH with betaCD in 1:1 molar ratio. The solid inclusion was characterized by differential scanning calorimetry, fourier transformation infrared spectroscopy and X-ray powder diffractometry. Experimental results confirmed the existence of 1:1 inclusion complex of MH with ICD. Aqueous solubility of MH was found to be enhanced by 118% for inclusion complex. The dissolution properties of binary systems were studied in simulated gastric fluid without enzyme and compared with MH alone. The inclusion complex of MH prepared with 3CD showed a dissolution rate several times faster than that of physical mixture and pure drug.
Asunto(s)
Antimaláricos/administración & dosificación , Antimaláricos/química , Mefloquina/administración & dosificación , Mefloquina/química , beta-Ciclodextrinas/química , Algoritmos , Antimaláricos/síntesis química , Rastreo Diferencial de Calorimetría , Cinética , Mefloquina/síntesis química , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos XRESUMEN
The solid-state properties and dissolution profile of bicalutamide beta-cyclodextrin (betaCD) inclusion complex were investigated. The phase solubility profile of bicalutamide with beta-cyclodextrin was classified as A(L)-type. Stability constant with 1:1 molar ratio was calculated from the phase solubility diagram and the aqueous solubility of bicalutamide was found to be enhanced by 86% for beta-cyclodextrin. Binary systems of bicalutamide with betaCD were prepared by the kneading method. The solid-state properties of the complex were characterized by differential scanning calorimetry, Fourier transformation-infrared spectroscopy and X-ray powder diffractometry. It could be concluded that bicalutamide could form an inclusion complex with beta-cyclodextrin. The dissolution profile of the inclusion complex was determined and compared with those of bicalutamide alone and its physical mixture. The dissolution rate of bicalutamide was significantly increased bycomplexation with betaCD, as compared with pure drug and physical mixture.