去甲斑蝥素温敏型原位凝胶的制备及其体外释放特性  

Studies on preparation and drug release characteristics of norcantharidin temperature-sensitive in situ gel in vitro

作　　者：周峰[1] 谢明华[2] 周红琴 蔡鑫君[1] 倪坚军[1] 王增[4] 

机构地区：[1]浙江中医药大学附属中西医结合医院药剂科,杭州310003 [2]杭州市余杭区第一人民医院药剂科,杭州311100 [3]温州市鹿城精神病医院药剂科,温州325000 [4]浙江省肿瘤医院药剂科,杭州310022

出　　处：《中国临床药学杂志》2017年第3期177-180,共4页Chinese Journal of Clinical Pharmacy

基　　金：浙江省中医药科学研究基金计划(编号2016ZA038);杭州市科技发展计划项目(编号20140633B57);杭州市余杭区科技发展计划项目(编号2014003);浙江省中西医结合学会科研项目(编号2013LYZD007)

摘　　要：目的制备去甲斑蝥素温敏型原位凝胶并探讨其药剂学性质。方法以胶凝温度和体外溶蚀时间为指标,采用均匀设计确定最佳工艺,利用平衡透析法对去甲斑蝥素温敏型原位凝胶进行体外释放的评价。结果通过均匀设计实验,确定最优处方为泊洛沙姆407比例28%,泊洛沙姆188比例1.6%,羟丙甲基纤维素比例0.1%。制得的去甲斑蝥素温敏型原位凝胶的胶凝温度为34℃,体外溶蚀时间为210 min。去甲斑蝥素温敏型原位凝胶体外释药曲线为ln ln[100/(100-Q)]=0.694 0 ln t-0.761 7,r=0.997 1,符合Weibull方程。结论去甲斑蝥素温敏型原位凝胶,其性质稳定,具有显著的体外缓释特性。AIM To prepare temperature-sensitive situ gel of norcantharidin and investigate its pharmaceutical properties. METHODS Gel temperature and dissolution time in vitro were used as an index, using uniform design to determine the optimum process, and the release of noreantharidin temperature-sensitive in situ gel in vitro was evaluated by using the equilibrium dialysis method. RESULTS The optimal prescription was established as poloxamer 407 ratio of 28% , poloxamer 188 ratio of 1.6% , and hydroxypropyl methyl cellulose ratio of 0.1% after a uniform design experiment. The gelation temperature of prepared norcantharidin temperature-sensitive in situ gel was 34℃ and dissolution time in vitro was 210 min. The drug release curve of norcantharidin temperature-sensitive in situ gel in vitro was In In[ 100/（100 -Q）] =0.694 0 In t-0. 761 7, r =0.997 1, which was in line with the Weibull equation. CONCLUSION Norcantharidin temperature-sensitive in situ gel has a stable property and significant property of sustained-release in vitro.

关 键 词：去甲斑蝥素 温敏型原位凝胶 体外释放 

分 类 号：R943[医药卫生—药剂学]