黄芩苷固体分散体缓释微丸的制备及治疗结肠炎的药效学研究  

Preparation of Baicalin Solid Dispersion Sustained-release Microspheres and Pharmacological Study on the Treatment of Colitis

作　　者：顾雪梅 汪洁 胡磊 吕志阳 陈静 陈璟 GU Xuemei;WANG Jie;HU Lei;LYU Zhiyang;CHEN Jing;CHEN Jing(Nanjing University of Chinese Medicine Hanlin College,Taizhou 225300,China;School of Pharmacy,Jiangsu Food&Pharmaceutical Science College,Huai′an 223003,China)

机构地区：[1]南京中医药大学翰林学院,江苏泰州225300 [2]江苏食品药品职业技术学院药学院,江苏淮安223003

出　　处：《山东化工》2025年第1期5-10,共6页Shandong Chemical Industry

基　　金：2024年江苏高校青蓝工程优秀教学团队资助项目;2023年江苏省大学生创新创业项目(202313981002Y,202313981003Y);泰州市科技支撑项目(TS202232,TS202325)。

摘　　要：目的:优化黄芩苷固体分散体缓释微丸的制备工艺,初步考察其对结肠炎小鼠的治疗作用。方法:通过星点设计-响应面法优化黄芩苷固体分散体的处方工艺,运用挤出滚圆法制备黄芩苷固体分散体缓释微丸,并进行体外溶出度测定。结肠炎小鼠连续灌胃给药7 d,记录小鼠体质量变化和便血情况等,ELISA法检测小鼠结肠TNF-α、IL-1β含量。结果:固体分散体选定溶剂法为制备方法,载体材料为泊洛沙姆188,最优处方是载药比为3.03∶1,使用18 mL 40%乙醇溶解,搅拌37 min;缓释微丸最佳处方是20%乙基纤维素、20%微晶纤维素、5%羟丙甲纤维素为黏合剂,收率和圆整度较好。体外释放结果表明,固体分散体和缓释微丸中的药物基本完全溶出,但缓释微丸中的黄芩苷呈缓慢释放,其12 h内累计释放率为96.03%。药效学研究表明,黄芩苷固体分散体缓释微丸能减缓小鼠体质量下降,改善便血情况,减少结肠组织中IL-1β和TNF-α的表达。结论:制备的黄芩苷固体分散体缓释微丸具备一定的缓释性能,对结肠炎小鼠具有治疗作用。Objective:To optimize the preparation process of baicalin solid dispersion sustained-release microspheres and preliminarily investigate their therapeutic effects on colitis mice.Method:The prescription process of baicalin solid dispersion was optimized by star point design response surface methodology.The extrusion rolling method was used to prepare baicalin solid dispersion sustained-release pellets,and the in vitro dissolution rate was determined.Colitis mice were orally administered continuously for 7 days,and changes in body weight and rectal bleeding were recorded.ELISA was used to detect the levels of TNF-αand IL-1βin the mouse colon.Results:The solvent method was selected as the preparation method for the solid dispersion,and the carrier material was poloxamer 188.The optimal prescription was a drug loading ratio of 3.03∶1,dissolved in 18 mL of 40%ethanol,and stirred for 37 minutes.The optimal formula for sustained-release microspheres is 20%ethyl cellulose,20%microcrystalline cellulose,and 5%hydroxypropyl methylcellulose as the adhesive,with good yield and roundness.The in vitro release results showed that the drugs in the solid dispersion and sustained-release pellets were basically completely dissolved,but baicalin in the sustained-release pellets was slowly released,with a cumulative release rate of 96.03%within 12 hours.Pharmacodynamic studies have shown that baicalin solid dispersion sustained-release microspheres can slow down weight loss in mice,improve rectal bleeding,and reduce the expression of IL-1βand TNF-αin colon tissue.Conclusion:The prepared baicalin solid dispersion sustained-release microspheres have certain sustained-release properties and have therapeutic effects on colitis mice.

关 键 词：黄芩苷 固体分散体 缓释微丸 结肠炎 

分 类 号：TQ461[化学工程—制药化工] R943[医药卫生—药剂学]