眼用和厚朴酚包合物温敏原位凝胶的制备及性质研究  

Preparation and characterization of thermosensitive in situ gel system containing honokiol inclusion complex for ophthalmic drug delivery

作　　者：娄杰[1] 徐才兵[1] 田睿[2] 刘玉祺[1] 郭锋[1] 张良珂[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室,重庆400016 [2]重庆医科大学实验教学中心,重庆400016

出　　处：《第三军医大学学报》2013年第21期2340-2343,共4页Journal of Third Military Medical University

基　　金：重庆市自然科学基金(CSTC2012jjA10021);高等学校博士学科点专项科研基金(20125503120003);重庆医科大学大学生科研与创新实验项目(201244201229;201217);重庆市教育委员会科学技术研究项目(KJ110323)~~

摘　　要：目的研制温度敏感型眼用和厚朴酚羟丙基-β-环糊精包合物原位凝胶(HK-HPCD-Gel)。方法以溶液搅拌法制备和厚朴酚羟丙基-β-环糊精包合物(HK-HPCD),泊洛沙姆407(P407)和泊洛沙姆188(P188)为凝胶基质,冷溶法制备HK-HPCD-Gel;用不同方法分别考察凝胶的溶蚀与体外释药行为并进行数据拟合。结果制备得到的HK-HPCDGel在室温下黏度为(0.189 4±0.099 9)Pa·s,流动性较好的液体,在眼部生理条件(34.2±0.1)℃时能够发生相转变形成黏度为(2.0822±0.6172)Pa·s的半固体状态,延长制剂在眼部的滞留时间。凝胶溶蚀与体外释放数据拟合结果表明无膜溶出法更适用于凝胶的体外性质考察,并且包合物的加入能提高药物的溶解度。结论制得的温敏眼用和厚朴酚包合物原位凝胶能提高药物的溶解度,延长制剂在眼部的滞留时间,有良好的应用前景。Objective To prepare a thermosensitive in situ gel system containing honokiol inclusion complex（HK-HPCD-Gel） for ophthalmic drug delivery and identify its characteristics.Methods The honokiol inclusion complex（HK-HPCD） were prepared by solution mixing method.Poloxamer 407（P407）and Poloxamer 188（P188） were used as gel matrix,and the in situ gel system of HK-HPCD-Gel was obtained by cold-dissolving method.And in vitro release and erosion behavior studies were carried out to evaluate the characteristics of the system.Results The formulation was freely flowing liquid at room temperature with a viscosity of 0.189 4±0.099 9 Pa·s and converted to a firm gel at 34.2 ℃ with a higher viscosity of 2.082 2 ±0.617 2 Pa·s.The in vitro release and erosion study indicated that the membraneless method was more appropriate for in vitro studies of gels,and the HPCD enhanced the dissolution rate of HK.Conclusion The in situ gel system is able to improve the dissolution of drugs and prolongs the residence time of the formulation,which shows great potential in ocular application.

关 键 词：和厚朴酚 包合物 温敏原位凝胶 眼部给药 

分 类 号：R943[医药卫生—药剂学] R944.15[医药卫生—药学]