波棱瓜子总木脂素纳米混悬剂胶囊的保肝作用评价  

Hepatoprotective Effects of Total Lignans of Herpetospermum caudigerum Nanosuspension Capsules

作　　者：沈刚[1,2] 沈成英[2] 程玲[1,2] 张利红[2] 邱玲[1,2] 李娟娟[2] 袁海龙[2] 韩晋[2] 

机构地区：[1]成都中医药大学药学院,成都611137 [2]中国人民解放军第三0二医院,北京100039

出　　处：《中国药学杂志》2015年第12期1038-1042,共5页Chinese Pharmaceutical Journal

基　　金：国家新药创制重大专项(2015ZX09101025);北京市科委重点项目(Z14110700220000)

摘　　要：目的制备波棱瓜子总木脂素纳米混悬剂胶囊(NSC)及评价其保肝降酶的药效学性质,并与医院制剂肝能滴丸做比较。方法采用高压均质法制备波棱瓜子总木脂素纳米混悬剂(HTL-NS),采用冻干工艺将其固化后装胶囊,并对波棱瓜子总木脂素纳米混悬剂、冻干粉和波棱瓜子总木脂素纳米混悬剂胶囊进行表征。采用腹腔注射30%(v/v)四氯化碳制备大鼠急性肝损伤模型,依法测定血清中丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)水平;同时测定肝匀浆组织中超氧化物歧化酶(SOD)和丙二醛(MDA)的活性,并在光学显微镜下观察肝脏病理学变化。结果波棱瓜子总木脂素纳米混悬剂胶囊复溶后粒径、多分散指数及Zeta电位分别为(332±15)nm、(0.263±0.010)及(-23.8±3.8)m V。在等剂量时波棱瓜子总木脂素纳米混悬剂胶囊降低丙氨酸氨基转移酶和天冬氨酸氨基转移酶的水平,提高超氧化物歧化酶活性,降低丙二醛含量和改变肝脏病理变化程度明显优于肝能滴丸。结论波棱瓜子总木脂素纳米混悬剂胶囊保肝作用显著优于肝能滴丸,为波棱瓜子总木脂素剂型的进一步开发和临床运用提供了一定的参考价值。OBJECTIVE To prepare total lignans of Herpetospermumcaudigerum nanosuspension capsules（ NSC）,and study its hepatoprotective effect against acute live injury induced by carbon tetrachloride（ CCl4） in comparison with Ganneng dripping pills.METHODS TL-NS was prepared by high pressure homogenization technique,and characterized in terms of morphology and particle size et al. The serum levels of ALT and AST and the activities of SOD and MDA in liver tissue homogenates were measured in the rat model of acute liver injury induced by intraperitoneal injection of 30% CCl4,and the hepatic pathological morphology was observed by optical microscope. RESULTS After being dissolved,NSC was irregular spheroidal as observed by scanning electron microscopy,and the other quantitative values of physical and chemical characterization were within reasonable ranges. Compared with Ganneng dripping pils,the levels of ALT,AST and MDA of the rats treated with NSC were significantly lowered,and the activities of SOD in liver tissue was increased obviously. Histological observation showed that NSC could ameliorate the histological damages induced by CCl4.CONCLUSION The hepatoprotective effects of NSC are significantly better than Ganneng dripping pils. This study provides certain reference to the dosage form development and clinical application of total lignans.

关 键 词：波棱瓜子 总木脂素 纳米混悬剂胶囊 肝能滴丸 保肝作用 急性肝损伤 

分 类 号：R944[医药卫生—药剂学]