Physico-chemical solid-state characterization of omeprazole sodium: Thermal, spectroscopic and crystallinity studies

• Published in: Journal of pharmaceutical and biomedical analysis Vol. 49; no. 1; pp. 72 - 80
• Main Authors: Murakami, Fabio S., Lang, Karen L., Mendes, Cassiana, Cruz, Ariane P., Filho, Marco A.S. Carvalho, Silva, Marcos A.S.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 15.01.2009; Elsevier
• Subjects: Analysis; Analytical, structural and metabolic biochemistry; Biological and medical sciences; Calorimetry, Differential Scanning; Chemical Phenomena; Crystal structure; Crystallization; Drug Stability; Enzyme Inhibitors - chemistry; Fundamental and applied biological sciences. Psychology; General pharmacology; Hot Temperature; Hydrogen Bonding; Medical sciences; Microscopy, Electron, Scanning; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Omeprazole - chemistry; Omeprazole sodium; Pharmacology. Drug treatments; Powders; Solid-state characterization; Spectroscopy, Fourier Transform Infrared; Spectrum Analysis; Stereoisomerism; Thermogravimetry; Titrimetry; Water - chemistry; X-Ray Diffraction; Omeprazole sodium; Solid-state characterization; Crystal structure; Enzyme; H; Enzyme inhibitor; Antiulcer agent; K; Proton pump inhibitor; Characterization; Omeprazole; Solid state; Sodium; Benzimidazole derivatives; Antisecretory agent; exchanging ATPase; Hydrolases; Crystalline structure
• ISSN: 0731-7085; 1873-264X
• DOI: 10.1016/j.jpba.2008.10.005

The physical characterization of active pharmaceutical substances is crucial to the successful development of the final drug product. The different solid forms and variations in the degree of crystallinity can lead to significantly different physical and chemical properties, including color, morphology, stability, dissolution and bioavailability. In the case of omeprazole sodium (OMS), its chemical structures contain a specific number of water molecules (hydrate). The behavior of pharmaceutical hydrates has become the object of increasing attention over the past decade, primarily due to the potential impact of hydrates on the development process and dosage form performance. The present study was designed to characterize and evaluate the crystallinity of omeprazole sodium, dehydrated omeprazole sodium (DOMS) and omeprazole free base (OM) using a variety of techniques including thermal analysis (thermogravimetry/derivative thermogravimetry (TG/DTG) and differential scanning calorimetry (DSC)), diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy, scanning electron microscopy (SEM) and X-ray powder diffraction (XRPD). Furthermore, an NMR spectroscopy study was also carried out to clarify the conformation and crystal structure.