摘要
目的 建立参芩凝胶中小檗碱、黄芩苷的经皮微量渗析取样方法,并对参芩凝胶的促渗工艺进行评价。方法以小檗碱、黄芩苷回收率、损失率为指标,采用增量法、减量法对灌注速度、取样间隔、灌注液浓度进行考察,研究反渗析法是否可应用于探针体内回收率的计算;将探针植入大鼠皮下,考察探针在12 h内的体内回收率稳定性;并通过透皮实验考察冰片对参芩凝胶透皮性能的影响。结果 灌注速度确定为1μL/min,取样间隔确定为30 min;灌注液浓度考察结果表明药物浓度对探针体外回收率无明显影响,同一浓度平行条件下,探针体外回收率与空白耗损率大致相等,说明反渗析法适用于计算探针体内回收率;探针植入皮下在12 h内回收率保持相对稳定。3%冰片能显著提升参芩凝胶中黄芩苷的透过量,对小檗碱的透过量也有一定的提升作用。结论 优选的微量渗析取样法可用于黄芩苷、小檗碱的经皮微量渗析取样的研究;冰片对参芩凝胶具有一定促渗作用。
Objective To establish a percutaneous microdialysis sampling method for berberine and baicalin in Shenqin gel, and to evaluate its permeation promoting process. Methods Taking the recovery rate and loss rate of berberine and baicalin as indexes, the perfusion rate, sampling interval and perfusion solution concentration were investigated by the increment method and the decrement method, so as to study whether the reverse dialysis method could be used to calculate the recovery rate of the probe in vivo. The probe was implanted subcutaneously in rats, and the stability of the recovery rate of the probe within 12 h in vivo was investigated. The effect of borneol on the transdermal performance of Shenqin gel was investigated by transdermal experiment. Results The perfusion rate was determined as 1 μL/min, and the sampling interval was determined as 30 min. The results of the perfusion solution concentration showed that the drug concentration had no obvious effect on the recovery rate of the probe in vitro, and the recovery rate of the probe in vitro was roughly equal to the loss rate under the same concentration parallel condition, indicating that the reverse dialysis method could be used to calculate the recovery rate of the probe in vivo. The recovery rate remained relatively stable within 12 h after the probe implantation. 3% borneol could significantly increase the transmission of baicalin in Shenqin gel, and also had a certain effect on the transmission of berberine. Conclusion The optimized microdialysis sampling method can be used to study percutaneous microdialysis sampling of baicalin and berberine. Borneol can promote the permeability of Shenqin gel.
作者
张建军
李洁环
王利胜
苏安宇
ZHANG Jianjun;LI Jiehuan;WANG Lisheng;SU Anyu(Guangdong Second Traditional Chinese Medicine Hospital(Guangdong Province Engineering Technology Research Institute of Traditional Chinese Medicine),Guangdong Provincial Key Laboratory of Research and Development in Traditional Chinese Medicine,Guangzhou 510095,China;School of Pharmaceutical Sciences,Guangzhou University of Chinese Medicine,Guangzhou 510006,China)
出处
《广东药科大学学报》
CAS
2023年第1期29-34,共6页
Journal of Guangdong Pharmaceutical University
基金
广东省中医药局科研项目(20194001)。
关键词
参芩凝胶
皮肤微透析
小檗碱
黄芩苷
促渗
Shenqin gel
skin microdialysis
berberine
baicalin
permeation promoting process
作者简介
张建军(1979-),男,博士,主任中药师,从事中药新药与制剂新技术研究。电话:020-83482147,Email:tiening1111@163.com。