Key ocular pharmacokinetic parameters in rabbits included high conjunctival AUC and fast T~max~ in the sclera and retina.
Pharmaceuticals · 4 authors, 3 centres
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Key ocular pharmacokinetic parameters in rabbits included high conjunctival AUC and fast T~max~ in the sclera and retina.
Key ocular pharmacokinetic parameters in rabbits included high conjunctival AUC and fast T~max~ in the sclera and retina. The mean retina/plasma drug concentration ratios in rats ranged from 1.3 to 3.3, indicating preferential distribution to the retina. Systemic absorption after ocular administration was greater than after oral administration. Retinal concentrations in rabbits were expected to exceed the inhibitory concentration against hSGLT2 (IC~50~: 0.43 nM) for 24 hours, while systemic plasma levels remained low. The study limitations include a small number of animals, independent groups per time point, and dose level variability across species. The findings suggest ocular administration of enavogliflozin could deliver therapeutic levels to the target site with limited systemic exposure.