ABSTRACT
Objective To observe the efficacy of levofloxacin hydrochloride eye gel (LHEG) in treatment of Staphylococcus aureus keratitis in rabbits. Methods Sixty rabb received intrastromal injection of 10 μL bacterial suspension conta establish Staphylococcus aureus keratitis model. Forty-eight rabb into four groups; 24 h baseline group, phosphate buffer solution (PBS) control group, levofloxacin hydrochloride eye drop (LHED) group, and LHEG group. Rabbits in the 24 h baseline group received slit-lamp examination and were given clinical score, and their corneas were collected for histopathology examination and bacterial quantitation. The other three groups received treatment with PBS, LHED or LHEG three times a day for seven successive days. In the last day, rabbits in these three groups received the same examination as that in the 24 h baseline group. The clinical scores and cornea bacterial quantitation were analyzed with variance analysis, and a P value less than 0. 05 was considered as statistically significant Results Compared wth PBS control group, clinical symptoms of LHED group and LHEG group were significantly reduced (P = 0. 00) on the seventh day, with the clinical scores being (4. 21 ± 1. 10) and (3. 63±0. 86), respectively; the numbers of bacterial colonies were also significantly reduced in LHED group and LHEG group (P =0. 00), with the numbers being (4. 87 ± 0. 05) and (4. 64±0. 10) CFU, respectively. Moreover, LHEG group had a significantly better bacteriostatic effect than LHEG group (P =0. 00). Conclusion Local application of LHEG can greatly inhibk the growth of bacterial colony of Staphylococcus aureus and improve the clinical signs of keratitis, with the efficacy being better than that of routinely used LHED in rabbk model of Staphylococcus aureus keratitis.
ABSTRACT
OBJECTIVE: To study on characterization, irritation, the release mechanism and the elimination kinetics of Fraxini Cortex thermosensitive in-situ-forming eye gel (FC-ISG). METHODS: The non-membrane dissolution model was used to observe the release mechanism of FC-ISG. The stabilities of FC-ISG were investigated under following circumstances bright light, freeze test and accelerating test. Single-dose and multiple-dose irritations of FC-ISG were evaluated by draize test. The elimination kinetics of FC-ISG were analyzed by non-compartment model. RESULTS: FC-ISG showed good stability and non-stimulation to rabbit eyes. Drug release from FC-ISG was completely controlled by gel erosion, the release kinetics was coincided with zero-level release. AUC and MRT in FC-ISG group were significantly higher than those in control group (P<0.05). CONCLUSIONS: FC-ISG can improve the bioavailability of drug by prolonging the residence retention time of drug in cornea. FC-ISG shows a great potential in ocular application.