Pharmcokinetic study of cyclosporin A in rabbit eyes by HPLC / 西安交通大学学报(医学版)

ABSTRACT

Objective To study the pharmacokinetic characters of cyclosporin A(CsA) in aqueous humor in rabbit after implanting different dosages of CsA in eyes and to provide a theoretical basis for the treatment of after cataract. Methods ECCE was performed in all rabbit eyes. CsA-MS was injected into the anterior chamber and the capsular bag in left eyes as expression group and MS was given in the same way in right eyes as control group. The concentration of CsA in the aqueous humor was monitored with high-performance liquid chromatogram. The follow-up period was 4 weeks. The samples were separated on a C18 column at 60℃ and detected at 210nm. The mobile phase was acetonitrile-water (67∶33). Results The correlation analysis showed a positive correlation within the range of 0.13-1.25mg/L (r=0.9951) and the detection limit was 0.13mg/L. The accuracy was 95.91% and the inter-day and intro-day precision was less than 5%. CsA in aqueous humor sustained a high concentration within 2 weeks. There were no significant differences in t1/2Ka and CL between the two dosage groups. AUC and Cmax increased in a dose-dependent manner. Conclusion The sustain-released CsA ophthalmic gels provided significant ocular bioavailability in rabbit eyes and they can reach the therapeutic dose in order to inhibit after cataract.