Preparation, characterization and dissolution enhancement of mefloquine hydrochloride-betaCD inclusion complex.

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.