吴茱萸碱胃漂浮片制备及其对家兔胃黏膜损伤的保护作用  

Preparation of evodiamine gastric floating tablets and their protective effects on rabbit gastric mucosa injury

作　　者：张佩琛 方栋 郝海军 ZHANG Pei-chen;FANG Dong;HAO Hai-jun(Zhengzhou Shuqing Medical College,Zhengzhou 450064,China;Henan University,Zhengzhou 450000,China;Shanghai Leiyunshang Pharmaceutical Co.,Ltd.,Shanghai 201401,China)

机构地区：[1]郑州澍青医学高等专科学校,河南郑州450064 [2]河南大学,河南郑州450000 [3]上海雷允上药业有限公司,上海201401

出　　处：《中成药》2023年第11期3527-3533,共7页Chinese Traditional Patent Medicine

基　　金：上海市科委项目(21S21903400)。

摘　　要：目的制备吴茱萸碱胃漂浮片,并考察其对家兔胃黏膜损伤的保护作用。方法粉末压片法制备胃漂浮片。以HPMC K15M用量、十六醇用量、碳酸氢钠用量为影响因素,2、6、12 h内累积释放度的综合评分为评价指标,Box-Behnken响应面法优化处方。30只家兔随机分为正常组、模型组、吴茱萸碱胃漂浮片低剂量组(20 mg/kg)、吴茱萸碱胃漂浮片高剂量组(40 mg/kg)、西咪替丁组(20 mg/kg),灌胃给药13 d,第14天灌胃给予无水乙醇制备胃黏膜损伤模型,计算胃黏膜损伤指数、溃疡抑制率,观察胃组织病理变化。结果最佳处方为HPMC K15M用量25.5%,十六醇用量7.0%,碳酸氢钠用量13.6%,平均浮动滞后时间为76 s,漂浮时间为12 h,12 h内累积释放度大于90%,综合评分为1.6分。吴茱萸碱胃漂浮片高剂量组胃黏膜损伤指数为2.08±0.40,溃疡抑制率为58.56%,接近西咪替丁。结论吴茱萸碱胃漂浮片体外缓释作用明显,并且对家兔胃黏膜损伤具有保护作用。AIM To prepare evodiamine gastric floating tablets,and to investigate their protective effects on rabbit gastric mucosa injury.METHODS Powder compression method was adopted in the preparation of gastric floating tablets.With HPMC K15M consumption,hexadecanol consumption and sodium bicarbonate consumption as influencing factors,comprehensive score for accumulative release rates within 2,6,12 h as an evaluation index,the formulation was optimized by Box-Behnken response surface method.Thirty rabbits were randomly divided into normal group,model group,evodiamine gastric floating tablets low-dose group(20 mg/kg),evodiamine gastric floating tablets high-dose group(40 mg/kg),cimetidine group(20 mg/kg)and given intragastric administration for 13 d,the gastric mucosa injury model was established by intragastric administration of anhydrous ethanol at the 14th day,after which gastric mucosa injury index and ulcer inhibitory rate were calculated,and the pathological changes of gastric tissue were observed.RESULTS The optimal formulation was determined to be 25.5%for HPMC K15M consumption,7.0%for hexadecanol consumption,and 13.6%for sodium bicarbonate consumption,the average floating lag time,floating time,accumulative release rate within 12 h and comprehensive score were 76 s,12 h,more than 90%and 1.6,respectively.The evodiamine gastric floating tablets high-dose group demonstrated the gastric mucosa injury index and ulcer inhibitory rate of 2.08±0.40 and 58.56%,respectively,which approximated those of cimetidine.CONCLUSION Evodiamine gastric floating tablets display obvious in vitro sustained-release effects and protective effects on rabbit gastric mucosa injury.

关 键 词：吴茱萸碱 胃漂浮片 制备 胃黏膜损伤 粉末压片法 

分 类 号：R944[医药卫生—药剂学]