龙胆总苷胃漂浮微丸制备及其体外释药特性研究  

Preparation of gentian total glycosides intragastric floating pellets and their characteristics of in vitro release

作　　者：王焱[1] 宋小玲[2] 陈银芳[2] 王金钱[3] 王跃生[3] 郑颖[1] 

机构地区：[1]澳门大学中华医药研究院,澳门999078 [2]江西中医学院,江西南昌330004 [3]中药固体制剂制造技术国家工程研究中心,江西南昌330006

出　　处：《中草药》2012年第9期1751-1755,共5页Chinese Traditional and Herbal Drugs

摘　　要：目的制备龙胆总苷胃漂浮微丸,并探讨其体外释药特性。方法采用助漂剂十六醇-微晶纤维素(7∶3),以离心造粒法制备空白丸芯(40～60目);采用HPMC-K15M为骨架材料和龙胆总苷等量混合以粉末层积法滚丸(20～30目);采用Eudragit NE 30D进行流化床包衣,制得龙胆总苷胃漂浮微丸;以龙胆苦苷为指标,《中国药典》2010年版二部附录XC"转篮法"和HPLC法,测定胃漂浮微丸12 h释放度,并用Higuchi等数学模型对释放度数据进行拟合,探讨龙胆总苷胃漂浮微丸释药特性。结果在人工胃液(pH 1.2)中,龙胆总苷胃漂浮微丸具有良好的漂浮性能和良好的缓释效果。累积释放率数据用Ritger-Peppas模型拟合度最高,相关系数R2>0.97,且0.43<n<0.85,说明龙胆总苷胃漂浮微丸释药过程是溶蚀与扩散协同作用。结论龙胆总苷制备胃漂浮微丸工艺可行,且能够达到胃滞留缓释的效果。Objective To prepare gentian total glycosides intragastric floating pellets （GGIFPs） and investigate their in vitro release characteristics. Methods Blank pellet core （40--60 meshes） was prepared with cetyl alcohol-microcrystalline cellulose （MCC, 7 ： 3） as floating agent using centrifugal granulation method; The pellets were developed using HPMC-K15M as skeleton material and mixed with equal amount of gentian total glycosides with powder stratification roll method （20---30 meshes）; The GGIFPs were obtained using Eudragit NE 30D fluidized bed coating. The release rate was detected using ＂rotating basket method＂ in Appendix XC of Chinese Pharmacopoeia 2010 （Ⅱ） and HPLC within 12 h taking gentiopicroside as index. The release data were fitted with mathematical models such as Higuchi to explore the release characteristics of GGIFPs. Results GGIFPs had good floating performance and sustained-release characteristics in simulated gastric fluid （pH 1.2）. The data of cumulative release rate fitted best with the Ritger-Peppas model, correlation coefficient R2 〉 0.97, and 0.43 〈 n 〈 0.85, which showed that the drug release process of GGIFPs was the synergy of dissolution and diffusion. Conclusion The technology for the preparation of GGIFPs is feasible and the sustained-release could be achieved in the process.

关 键 词：龙胆总苷 胃漂浮微丸 粉末层积法 体外释药 缓释 

分 类 号：R283.6[医药卫生—中药学]