gamma-cyclodextrin and montelukast

Montelukast (MLK), an oral antiasthmatic drug with growing use, requires special care in formulation and storage to avoid its degradation by action of light and water. This work investigates the increase in the stability of montelukast as the effect of molecular encapsulation with gamma-cyclodextrin (γ-CD) by means of a solvent-free method, cogrinding. As a first step, a 1:1 preferred stoichiometry is established for this hostguest system using a combination of molecular modeling and the continuous variation method. The solid 1:1 inclusion compound, γ-CD·MLK, is obtained by 2 comilling procedures. For comparison purposes, γ-CD·MLK is also prepared by a classical codissolution procedure and isolated by freeze-drying. Products were characterized by powder X-ray diffraction,

Topics: Acetates; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Cyclopropanes; Drug Compounding; Freeze Drying; gamma-Cyclodextrins; Microscopy, Electron, Scanning; Models, Molecular; Powders; Quinolines; Solubility; Spectroscopy, Fourier Transform Infrared; Sulfides; X-Ray Diffraction