2024/02/15 by Shinji Oyama, Noriko Ogawa, Kaori Kawai +3
Biochemistry, Genetics and Molecular Biology · Chemistry · Pharmacology, Toxicology and Pharmaceutics · #Analytical Methods in Pharmaceuticals #Drug Solubulity and Delivery Systems #Protein purification and stability
paper · pdf · doi:10.1248/cpb.c23-00673
openalex publication_date 2024/02/15 · crossref created 2024/02/15 · crossref issued 2024/02/16 · crossref published 2024/02/16 · crossref published-print 2024/02/16 · crossref deposited 2024/02/17 · openalex created_date 2025/10/10 · crossref indexed 2026/07/31 · openalex updated_date 2026/07/31
A co-amorphous model drug was prepared by the spray-drying (SD) of probucol (PC) and atorvastatin calcium trihydrate salt (ATO) as low water solubility and co-former components, respectively. The physicochemical properties of the prepared samples were characterized by powder X-ray diffraction (PXRD) analysis, thermal analysis, Fourier transform infrared spectroscopy (FTIR), and dissolution tests. Stability tests were also conducted under a stress environment of 40 °C and 75% relative humidity. The results of PXRD measurements and thermal analysis suggested that PC and ATO form a co-amorphous system by SD. Thermal analysis also indicated an endothermic peak that followed an exotherm in amorphous PC and a physical mixture (PM) of amorphous PC and ATO; however, no endothermic peak was detected in the co-amorphous system. The dissolution profiles for PC in the co-amorphous sample composed of PC and ATO were improved compared to those for raw PC crystals or the PM. Stability tests indicated that the co-amorphous material formed by PC and ATO can be stored for 35 d without crystallization, whereas amorphous PC became crystallized within a day. Therefore, co-amorphization of PC and ATO prepared by SD is considered to be a useful method to improve the solubility of PC in water.