三七总皂苷传递体的制备及其治疗大鼠急性软组织损伤作用研究.PDF

·2070 · 中草药 Chinese Traditional and Herbal Drugs 第 46 卷 第 14 期 2015 年 7 月 三七总皂苷传递体的制备及其治疗大鼠急性软组织损伤作用研究 * 陈思思，郑杭生 ，王 娟，方 蓉，邢小静 浙江中医药大学药学院，浙江 杭州 310053 摘 要：目的 优化三七总皂苷（PNS ）传递体的处方，验证其治疗大鼠急性软组织损伤的作用。方法 采用薄膜分散法制 备 PNS 传递体，以传递体弹性为指标，通过均匀设计法优化其处方工艺；分别以挤出法、离心超滤法测定传递体的弹性与 包封率；通过对实验动物的损伤症候指数、血液流变学及组织形态学的观测评价传递体对大鼠急性软组织损伤的治疗作用， 并与阳性对照药青鹏软膏进行比较。结果 PNS 传递体最佳处方为 PNS 100 mg 、胆固醇 15 mg、大豆磷脂 120 mg、维生素 E 2 mg 、中药挥发油（柠檬烯-柠檬醛 4 ∶1）80 mg、水化液［磷酸盐缓冲液（PBS ），pH 5.0 ］10 mL；以最佳处方制得的成 品弹性为（2.74 ±0.32 ）min 、粒径为（123.60±0.36 ）nm 、Zeta 电位为（−36.67 ±2.29 ）mV ，人参皂苷Rg1 与人参皂苷 Rb1 的包封率分别为（82.42 ±0.69 ）%、（94.40 ±0.74 ）% ；药效学实验结果显示，与模型组相比PNS 传递体可显著降低实验动 物的损伤证候指数（P ＜0.01 ）、全血黏度及血浆黏度（P ＜0.05 ），有效改善病灶部位组织形态。结论 所得 PNS 传递体粒 径适宜，弹性与药物包封率良好，疗效确切。 关键词：三七总皂苷；传递体；薄膜分散法；弹性；急性软组织损伤 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2015)14 - 2070 - 06 DOI: 10.7501/j.issn.0253-2670.2015.14.009 Study on preparation of Panax notoginseng saponins transfersomes and their effects on acute soft tissue injury in rats CHEN Si-si, ZHENG Hang-sheng, WANG Juan, FANG Rong, XING Xiao-jing College of Pharmacy, Zhejiang University of Traditional Chinese Medicine, Hangzhou 310053, China Abstract: Objective To optimize the formulation of Panax notoginseng saponins (PNS) transfersomes and to verify their effects on acute soft tissue injury in rats. Methods Thin film dispersion method was employed to prepare PNS transfersomes. Based on the elasticity of transfersomes, PNS transfersomal formulation was optimized by a uniform experimental design. Extrusion method and centrifugation-ultrafiltration method were respectively adopted to determine the elasticity and the entrapment efficiency (EE) of PNS transfersomes. The therapeutic effects of PNS transfersomes on acute soft tissue injury in rats were evaluated by observing the indexes of injury symptom, the hemorheology and th