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Nitrofurantoin solubility in aqueous urea and creatinine solutions
Journal of Pharmaceutical Sciences
|June 1, 1976
Summary
Urea and creatinine enhance nitrofurantoin solubility in water, with interactions observed. This explains why crystalluria is absent despite high drug concentrations in urine.
Area of Science:
- Pharmaceutical Chemistry
- Physical Chemistry
Background:
- Nitrofurantoin is a widely used antibiotic.
- High concentrations of nitrofurantoin in urine can lead to crystalluria, a potential adverse effect.
- Understanding factors affecting nitrofurantoin solubility is crucial for optimizing its therapeutic use.
Purpose of the Study:
- To investigate the effects of urea and creatinine on nitrofurantoin solubility.
- To determine the influence of temperature and pH on these interactions.
- To elucidate the molecular mechanisms underlying solubility changes.
Main Methods:
- Solubility measurements of nitrofurantoin in aqueous solutions containing varying concentrations of urea and creatinine.
- Spectroscopic analyses (e.g., UV-Vis, NMR) to probe molecular interactions.
- Experiments conducted across a range of temperatures and pH values.
Main Results:
- Urea initially increased nitrofurantoin solubility up to a specific concentration (1.75-2.50%), dependent on temperature, then decreased it at higher concentrations.
- Creatinine significantly increased nitrofurantoin solubility across tested concentrations (0.05-1.6%).
- Spectral data indicated molecular interactions between nitrofurantoin and both urea and creatinine.
Conclusions:
- Urea and creatinine significantly influence nitrofurantoin solubility through molecular interactions.
- The combined effect of urea and creatinine in urine likely prevents nitrofurantoin crystalluria.
- These findings have implications for understanding nitrofurantoin pharmacokinetics and safety profiles.