戊己胃漂浮片中多指标成分的体外释放及体内滞留时间考察  

Investigation of in vitro Release Properties and in vivo Residence Time of Multi-Index Constituents from Wuji Gastric Floating Sustained-Release Tablets

作　　者：刘文[1] 王群[1] 陈中芬[1] 杨颂[1] 施晓伟[1] 

机构地区：[1]贵阳中医学院,贵阳550002

出　　处：《中国实验方剂学杂志》2013年第23期43-46,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：贵州省中药现代化科技产业研究开发专项(黔科合中药[2010]5016号)

摘　　要：目的： 考察戊己胃漂浮缓释片中4种成分的体外释放规律及其在家兔胃内的滞留时间。 方法： 采用浆法测定戊己胃漂浮缓释片的体外释放度，以含0.8%聚山梨酯-80的0.1 molmL-1盐酸溶液为释放介质，运用HPLC测定戊己胃漂浮缓释片中盐酸小檗碱、吴茱萸碱和吴茱萸次碱、芍药苷在12 h内的体外累积释放率，色谱条件为Thermo-ODS2-Hypersil色谱柱（4.6 mm250 mm，5 μm），流动相乙腈（A）-0.05 molL-1磷酸二氢钾（B）梯度洗脱（0~20 min，11%A;22~44 min，28%A;46~70 min，40%A），检测波长225 nm;对数正态分布模型、威布尔分布函数和Higuich方程进行溶出动力学模拟，利用γ-闪烁照相法考察戊己胃漂浮缓释片在家兔胃内的滞留时间。 结果： 4种成分的体外释放均符合Higuchi模型，戊己胃漂浮缓释片可在家兔胃内滞留6 h。 结论： 饱腹状态下，戊己胃漂浮缓释片在家兔胃内的滞留时间明显长于禁食状态下，提示食物可能对该制剂在胃内的滞留时间具有显著性影响。Objective： To investigate in vitro release properties and gastric residence time in rabbits of four ingredients from Wuji gastric floating sustained-release tablets. Method： In vitro release of Wuji gastric floating sustained-release tablets was determined by slurry method,with 0.1 mol mL-1 HCl solution containing 0.8% tween-80 as release mediator,cumulative release of paeoniflorin,berberine hydrochloride,evodiamine and rutaecarpin from Wuji gastric floating sustained-release tablets within 12 h were measured by HPLC,chromatographic conditions were as follows：Thermo-ODS2-Hypersil column（4.6 mm250 mm,5 μm）,mobile phase of acetonitrile（A）-0.05 mol L-1 potassium dihydrogen phosphate（B） with gradient elution program of （0-20 min,11% A;22-44 min,28% A;46-70 min,40% A）,detection wavelength 225 nm;Dissolution kinetics models were simulated by lognormal distribution model,Weibull function and Higuchi equation,and γ scintigraphy was adopted to detect gastric residence time in rabbits of Wuji gastric floating sustained-release tablets. Result： Cumulative release of four ingredients all fitted Higuchi equation,gastric residence time of this preparation was 6 h in rabbits. Conclusion： Under satiety state,gastric residence time in rabbits of Wuji gastric floating sustained-release tablets was significantly longer than fasting state,it revealed that food may have a significant impact on gastric residence time of this tablets.

关 键 词：戊己胃漂浮缓释片 释放度 释放机理 γ闪烁照相法 体内滞留时间 

分 类 号：R283.6[医药卫生—中药学]