Preparation, in vitro and in vivo studies of Fraxini cortex thermosensitive in-situ-forming eye gel / 中国药学杂志

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.