Pharmacokinetics of Ketoconazole in Rats
Author Information
Author(s): Pu Jiang, He Jinsong, Xue Ru, Gao Ruiqi, Yu Yaoming, Feng Wanyong
Primary Institution: Bioduro-Sundia, Shanghai, China
Hypothesis
The study aims to explore the pharmacokinetic and metabolic profile of ketoconazole via topical ocular administration in rats.
Conclusion
Ketoconazole showed higher concentrations in ocular tissues compared to plasma, indicating its potential for topical use.
Supporting Evidence
- Ketoconazole reached a peak plasma concentration of 445 ng/mL at 5 minutes post-dose.
- The mean ketoconazole concentration in the cornea was significantly higher than in plasma.
- Nine metabolites were identified in rat plasma, with M3 and M11 being the most abundant.
- Ketoconazole concentrations decreased over time in all tissues measured.
Takeaway
This study looked at how a medicine called ketoconazole behaves in the eyes of rats when put in as eye drops, finding it stays in the eyes longer than in the blood.
Methodology
Nine male Sprague-Dawley rats were given ketoconazole eye drops, and their plasma and ocular tissues were analyzed at different time points.
Limitations
The study is limited to a small sample size of rats and may not directly translate to humans.
Participant Demographics
Nine male Sprague-Dawley rats aged 7 to 9 weeks.
Digital Object Identifier (DOI)
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