Utilization of salivary concentrations of ciprofloxacin in subjects with cystic fibrosis.

Ciprofloxacin, an orally-absorbed fluoroquinolone is effective against multiply resistant Pseudomonas aeruginosa in cystic fibrosis patients. It is the only practicable agent against extraintestinal salmonellosis and shigellosis in developing countries. However, concern with the risk of arthropathy in young children has restricted its use in pediatrics. Pharmacokinetic studies with ciprofloxacin are limited in the pediatric population. As a result, the dose and frequency of administration are not established in children. In this study the possibility of using salivary concentrations as surrogate measure of serum concentrations was investigated. A pediatric formulation of the drug (125 mg per capsule) was prepared and compared to 250 mg tablets. Relative bioavailability was 105% (tablet/capsule). The time to peak salivary concentration and elimination rate from saliva were significantly different from serum (p < 0.01 and p < 0.05 respectively). The linear regression analysis of post-peak concentrations in serum and saliva yielded a slope of 1.25 and correlation coefficient of 0.83. It was also found that salivary concentrations may be contaminated from drug retained in the oral cavity. The conclusion was drawn that salivary concentrations could not be reliably used as a surrogate measure of serum levels for therapeutic drug monitoring.