胰岛素眼用温度敏感即型凝胶的制备及其体外释药考察

Study on the preparation and drug release in vitro of in-situ temperature sensitive gel of insulin

目的研制胰岛素(IL)的眼部原位凝胶(ISG),并对其体外性质进行考察,为进一步体内试验奠定基础。方法采用温敏性凝胶基质泊洛沙姆407和188制备IL-ISG,并测定其在模拟泪液稀释前和稀释后的胶凝温度,通过无膜溶出模型,考察其凝胶溶蚀及药物释放特性。结果 IL-ISG在模拟泪液稀释前和稀释后的胶凝温度分别为(30.4±0.2)℃、(34.2±0.4)℃,其凝胶溶蚀及体外释药均符合一级速率过程。结论 IL-ISG具有胶凝温度适宜,缓释效果明显的特性,值得进一步研发。

Objective To study the preparation and in vitro drug release of in-situ temperature sensitive gel of insulin（IL-ISG） in order to study further in vivo. Methods IL-ISG was prepared using T-sensitive polymers poloxamer 407 and 188 as bases.The gel temperature of IL-ISG before and after diluted by artificial tears was determined.The base dissolution and IL release in vitro were studied by membraneless dissolution model.Results The gel temperature of IL-ISG before and after diluted by artificial tears was（30.4±0.2） ℃ and（34.2±0.4） ℃,respectively.The base dissolution and IL release in vitro were both accorded with first-order models.Conclusion The IL-ISG has suitable gel temperature and significant sustained release property.It is valuable to study further.