盐酸多西环素微球温敏凝胶剂的表征及对大鼠牙周炎的药效评价  

In vitro characteristics and pharmacodynamics evaluation on rats with periodontitis of doxycycline hydrochloride microspheres/temperature-sensitive gel

作　　者：郭家平[1] 李欧[2] 符旭东[1] GUO fla-ping LI Ou FU Xu-Dong(Wuhan General Hospital of Guangzhou Military, Hubei Wuhan 430070, China Hubei University of Medicine, Hubei Shiyan 442000, China)

机构地区：[1]广州军区武汉总医院,湖北武汉430070 [2]湖北医药学院,湖北十堰442000

出　　处：《临床口腔医学杂志》2016年第12期714-717,共4页Journal of Clinical Stomatology

基　　金：武汉市科技攻关计划(201161038346)

摘　　要：目的:评价盐酸多西环素(Doxycycline Hydrochloride,DXY)微球温敏凝胶剂(DXY-MS-GEL)的体外特性和对大鼠实验性牙周炎的治疗效果。方法:通过胶凝化温度和体外释药曲线评价DXY-MS-GEL的体外特性。采用内毒素隔日注射法建立Wistar大鼠牙周炎动物模型。将大鼠随机分为3组,空白对照组不予处理,实验组给以自制的DXY微球温敏性凝胶,阳性对照组给以盐酸米诺环素(派丽奥)软膏,隔日注射1次×5。末次给药后1 d测定牙龈出血指数、牙周指数、牙周探诊深度、菌斑指数、牙槽骨丧失量,观察组织病理学切片。结果:DXY-MS-GEL在室温下为自由流动的液体,37℃的平均凝胶时间为1.1±0.3 min,可持续释药24 h,体外释药曲线符合Higuchi方程,R^2=0.9948。与空白对照组相比,实验组和阳性对照组各观测指标差异均具有统计学意义(P<0.05),而实验组和阳性对照组之间对比差异无统计学意义。结论:DXY微球温敏性凝胶对牙周炎的局部治疗效果显著。Objective：To evaluate the characteristcs and pharmacodynamics of rats with periodontitis of doxycycline hydrocbloride（DXY） microspheres/temperature-sensitive gel （DXY-MS-GEL） in vitro. Methods ： DXY-MS-GEL was charac- terized by in vitro release profiles and gelation time. Endotoxin was injected to wistar rats every other day to establish the peri- odontifis animal model which were randomly divided into 3 groups. The blank control group（D） was not handling, experiment group（ G1 ）and positive control group（ G2 ）were given homemade DXY-MW-GEL and periocline ointment respectively,every 48 hours for 5 times. Periodontal index, probing depth, plaque index, amount of bone loss were measured and the histopatho- logical sections were observed on the first day after the last administration. Results：DXY-MW-GEL was a freely flowable liq- uid at room temperature and formed gel in （ 1.1±O. 3 ） rain at 37 ℃. Drug released from DXY-MW-GEL sustained for 24 hours and the release curve meeted higuchi fitting equation （ R^2 = 0. 9911 ）. The observed indexs of the experiment group （ G1 ）and the positve control group（ G2 ）were significant different from the balnk control group （D）（ P 〈 0. 05 ）, and there were no significant difference between G1 and G2 （ P 〉 0. 05 ）. Conclusion： DXYmicrospheres composited with temperature-sensitive gel is effective on periodontitis rats, and it is deserved to be developping furtherly.

关 键 词：盐酸多西环素 温敏凝胶 微球 牙周炎 壳聚糖 

分 类 号：R781.4[医药卫生—口腔医学]