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目的研究秦皮温敏眼用即型凝胶的体外性质,刺激性,药物释放机制及眼部消除动力学。方法采用无膜溶蚀模型研究药物的释放机制。以凝胶外观、pH值、胶凝温度、含量等变化为指标考察强光照射、冷冻及加速实验条件下凝胶的稳定性。采用Draize眼部刺激性试验评价单次和多次给药后凝胶对兔眼的刺激性。使用统计矩法评价了药物在家兔眼部的消除动力学特征。结果该制剂稳定性好,无刺激,药物释放主要受胶凝溶蚀控制,符合零级动力学过程。药动学结果显示,凝胶组AUC和MRT明显高于滴眼液组(P<0.05)。结论秦皮温敏眼用即型凝胶可明显延长药物在眼部的滞留时间,提高药物的生物利用度,展现出良好的眼部应用前景。
Objective To study the in vitro properties, irritation, drug release mechanism and ocular elimination kinetics of Qinpi temperature-sensitive ophthalmic gels. Methods The membrane-free dissolution model was used to study the drug release mechanism. The stability of gels under light irradiation, freezing and accelerated experimental conditions was investigated by the changes of gel appearance, pH, gelation temperature and content. The Draize eye irritation test was used to assess the irritation of the rabbit eye to gels following single and multiple dosing. The statistical moment method was used to evaluate the elimination kinetics of the drug in rabbit eyes. Results The preparation showed good stability and no irritation. The drug release was mainly controlled by the gelation erosion and accorded with the zero-order kinetics. Pharmacokinetic results showed that AUC and MRT in the gel group were significantly higher than the eye drops group (P <0.05). Conclusions Qin skin temperature-sensitive ophthalmic gels can significantly extend the retention time of drugs in the eye and improve the bioavailability of drugs, showing a good eye application prospects.