| Autor: | M. D. Likar, Russell H. Robins, Paul E. Fagerness, Richard J. Taylor, Yukio Hiyama |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Pharmacology
Magic angle Aqueous solution Chemistry Organic Chemistry Carbon-13 Analytical chemistry Pharmaceutical Science Nuclear magnetic resonance spectroscopy Dosage form Solvent Nuclear magnetic resonance Magic angle spinning Molecular Medicine lipids (amino acids peptides and proteins) Pharmacology (medical) Biotechnology Antibacterial agent |
| Zdroj: | Pharmaceutical Research. 10:75-79 |
| ISSN: | 0724-8741 |
| DOI: | 10.1023/a:1018925113721 |
| Popis: | Understanding how moisture interacts with a drug or formulation is a critical component of product development. This study demonstrates how water affects the 3′-gem-diol ↔ 3′-keto equilibrium in trospectomycin sulfate bulk drug and freeze-dried formulation, as probed by solid-state carbon-13 cross-polarization magic angle spinning (CP/MAS) and high-resolution nuclear magnetic resonance (NMR) spectroscopy. Drying the bulk drug or formulation to low water levels dehydrates trospectomycin sulfate from the diol to the keto form. Carbon-13 CP/MAS NMR spectroscopy measures the keto drug concentration in solid samples directly. The bulk drug, which contains approximately 16% water, is more than 90% in the 3′-diol form. Oven drying to 95%) of the drug is in the 3′-diol form. After equilibration at 60°C, however, the 3′-keto content increases to 7%, and in d 6-DMSO solvent at 25°C the drug is mostly (60%) in the 3′-keto form. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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