Physicochemical study of inclusion of drug molecules in cyclodextrins

Doctoral Thesis


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University of Cape Town

Inclusion of drug molecules in cyclodextrins can significantly improve various aspects of their performance and has resulted in the use of cyclodextrins (CDs) for a wide variety of pharmaceutical applications. Consequently, the cyclodextrin inclusion of drugs has received great interest in the pharmaceutical and chemical fields. For this study the inclusion of nine pharmaceutical drugs with CDs was investigated in the solid state. The objectives of the study were i.) the preparation, ii.) determination of the chemical composition, iii.) analysis of thermal behaviour and iv.) investigation of the solid state features of the complexes. Ultraviolet spectrophotometry, elemental analysis and thermogravimetric analysis were the principal techniques used for determination of composition. Hot stage microscopy, differential scanning calorimetry and thermogravimetric analysis were the principal techniques used for the analysis of thermal behaviour. Single crystal x-ray diffraction and x-ray powder diffraction were the principal techniques used for investigation of structural features. This thesis reports the preparation by crystallisation from solution of eight beta cyclodextrin (β-CD) and four gamma cyclodextrin (γ-CD) inclusion complexes with selected drugs as guests, as well as the determination of their chemical compositions and analysis of their thermal behaviours. Investigation of the structural features of these complexes includes the determination of the crystal structures of five β-CD complexes and one γ-CD complex. The preparation of hydnoxypropyl-β-CD complexes by kneading and co-grinding is also reported.

Includes bibliographical references.