地肤子总皂苷凝胶剂的制备及体外透皮吸收实验研究

Study on preparation and transdermal drug delivery of total saponins of Fructus Kochiae Scopariae liposomal gel

制备地肤子总皂苷凝胶剂并研究其体外透皮吸收特点。采用乙醇回流法提取并采用大孔吸附树脂进行纯化得到地肤子总皂苷;采用离体透皮实验并采用紫外分光光度法测定接受液中总皂苷的含量,计算单位面积累积渗透量,分析药物透皮渗透的特点。结果表明,提取纯化工艺为:地肤子药材用8倍量70%乙醇,回流提取3次,每次2 h,合并提取液,过滤,浓缩至0.80 g/mL(W/V),装柱(D-101),用3倍柱体积水除杂,弃去水洗脱液,用4倍柱体积50%乙醇洗脱,收集洗脱液,回收乙醇;凝胶剂的制备工艺为:将卡波姆充分溶胀,制得空白凝胶,加入地肤子总皂苷溶液,混匀,即得;离体透皮实验研究中,地肤子总皂苷凝胶剂中总皂苷在1.5~9 h的透皮渗透速度基本稳定,但在前1.5 h内有较为明显的时滞现象。该方法制得的地肤子总皂苷凝胶剂,具有良好的成型性和稳定性及释药速度稳定的特点。

To preparation saponins of Fructus Kochiae Scopariae liposomal gel and study its percutaneous absorption characteristics in vitro. The total saponins of Fructus Kochiae Scopariae were extracted by ethanol refluxing and purified by macroreticular resin; The content of total saponins in the receiving solution was determined by ultraviolet spectrophotometry,the permeability per unit area was calculated by in vitro transdermal test and the transdermal permeation of the drug was analyzed. The result showed that the extraction and purification process as follows: Fructus Kochiae Scopariae was extracted with 8 times of 70% ethanol,refluxed for 3 times,and extracted for 2 h. The extracting solution were filtered,concentrated to 0. 80 g/mL( W/V)),the concentrating solution were eluted using water and 50% ethanol by macroreticular resin D101 and the ethanol eluents were collected; The preparation process of the gelling agent as follows: The carbomer were fully swolled to obtain a blank gel,adding Fructus Kochiae Scopariae saponin solution and mixing. In transdermal transdermal test,the transdermal permeation rate of total saponin in Kochia scoparia saponin was basically stable at 1. 5 ~ 9 h,but there was obvious lag in the first 1. 5 h. Kochia Scoparia saponins was prepared by the above method,its preparation process and in vitro transdermal absorption characteristics were studied. It has good formability and stability,it also has stable release rate.