氧化魔芋葡甘聚糖胃漂浮骨架片的制备与体外释药  

Preparation and in vitro release of oxidized konjac glucomannan gastric floating matrix tablets and properties

作　　者：李光英 龙晓燕[1,2] 徐宁 严全 LI Guang-ying;LONG Xiao-yan;XU Ning;YAN Quan(School of Life Sciences and Engineering,Southwest University of Science and Technology,Mianyang Sichuan 621010;Engineering Research Center of Biomass Materials,Ministry of Education,Mianyang Sichuan 621010)

机构地区：[1]西南科技大学生命科学与工程学院,四川绵阳621010 [2]西南科技大学生物质材料教育部工程研究中心,四川绵阳621010

出　　处：《中南药学》2020年第3期373-379,共7页Central South Pharmacy

基　　金：绵阳市科技计划项目(No.17YFNY008);龙山学术人才科研支持计划(NO.18LZX537);西南科技大学博士基金(No.15zx7119)。

摘　　要：目的制备合适浓度的氧化魔芋葡甘聚糖(OKGM)胃漂浮骨架片。方法以OKGM为骨架材料,盐酸环丙沙星为模式药物,利用溶胶-凝胶法及冷冻干燥技术制备OKGM胃漂浮骨架片。以迟滞时间和续漂时间为指标评价漂浮性能,以药物累积释放率评价释药行为,通过形貌、孔隙率、数学模型拟合及溶胀行为探讨释药机制。结果浓度为2%~8%的OKGM骨架片立即起漂,续漂时间<24 h;OKGM浓度≥20%,不能形成胃漂浮骨架片;浓度为10%~18%的OKGM骨架片立即起漂,续漂时间>24 h。模拟体外释药结果表明:浓度为10%~18%的OKGM骨架片24 h累积释药率<90%,在扫描电镜(SEM)下呈空间网络结构,孔隙率为(86.039±4.05)%^(71.802±11.63)%;浓度为10%~14%的OKGM骨架片释药以药物扩散为主,浓度为16%~18%的OKGM骨架片以骨架溶蚀为主;溶胀与溶蚀达平衡时,溶胀比为308.03%~629.75%。结论浓度为10%~18%的OKGM骨架片兼具良好的漂浮性能和药物缓释性能,浓度越大缓释效果越明显,可通过控制OKGM浓度来控制药物的释放。Objective To prepare suitable concentration of oxidized konjac glucomannan(OKGM) gastric floating matrix tablets. Methods Ciprofloxacin hydrochloride was used as a model drug. The OKGM gastric floating matrix tablets were prepared by sol-gel method and freeze-drying technique with OKGM as the matrix material. The floating performance was evaluated by the lag time and the continuation time, and the release behavior was evaluated by the drug cumulative release. The release mechanism was studied by SEM, porosity, mathematical model fitting and swelling behavior. Results OKGM matrix tablets(2%-8%) immediately floated and the floating time was < 24 h;when OKGM concentration was ≥ 20%, gastric floating matrix tablets failed to form;OKGM matrix tablets(10%-18%) immediately floated and the floating time was >24 h. The cumulative release rate of OKGM matrix tablets(10%-18%) was < 90% within 24 h. They had spatial network structure by SEM and their porosity was between(86.039±4.05)% and(71.802±11.63)%. The release mechanism of(10%-14%) OKGM matrix tablets showed drug diffusion and the release mechanism of(16%-18%) OKGM matrix tablets displayed matix erosion mainly. When the swelling and erosion reached the equilibrium, the swelling ratio ranged from 308.03% to 629.75%. Conclusion The OKGM gastric floating matrix tablets at 10%-18% show good floating performance and drug release properties. The higher the concentration, the better the sustained release. So the drug release can be regulated by controlling the concentration of OKGM.

关 键 词：氧化魔芋葡甘聚糖 盐酸环丙沙星 胃漂浮骨架片 漂浮性能 释药行为 

分 类 号：R493[医药卫生—康复医学] R94[医药卫生—临床医学]