Preparation of amorphous forms to increase the solubility of poorly soluble drugs using spray drying

• Main Author: Nannapaneni, Vijaysri
• Format: Others
• Published: Scholarly Commons 2011
• Subjects: Pharmacy sciences; Health and environmental sciences; Chemicals and Drugs; Chemistry; Medical Pharmacology; Medicinal-Pharmaceutical Chemistry; Medicine and Health Sciences; Pharmaceutical Preparations; Pharmacy and Pharmaceutical Sciences; Physical Sciences and Mathematics
• Online Access: https://scholarlycommons.pacific.edu/uop_etds/274; https://scholarlycommons.pacific.edu/cgi/viewcontent.cgi?article=1273&context=uop_etds

Spray drying is widely used in enhancing the aqueous solubility of poorly soluble compounds. In this study, the mechanism of solubility enhancement was characterized using three model drugs-naproxen, ketoprofen and furosemide. Physical mixtures of the model drug with polyvinylpyrrolidine and spray dried composites were subjected to Fourier Transform Infrared Sprectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and Powder X-ray Diffraction (XRPD). The data showed that the crystalline model drugs were converted to amorphous form upon spray drying, whereas the physical mixtures did not change their crystallinity. The effect of the amorphous forms produced by Spray drying on apparent solubility and intrinsic dissolution rate was determined. All the spray dried composites exhibited higher apparent solubility and intrinsic dissolution rate when compared to the pure drugs and their physical mixtures. The stability of the spray dried composites upon storage was also determined. The amorphous nature of the compounds in the spray dried composites were retained during 3 months storage as shown by FTIR, DSC and XRPD characterization and their apparent solubility and intrinsic dissolution rates also did not change.