三七总皂苷离子敏感型鼻用原位凝胶的制备

Preparation of Panax notoginseng saponins ion-sensitive in situ nasal gel

目的制备离子敏感型三七总皂苷(PNS)鼻用原位凝胶。方法以去乙酰结冷胶为材料,采用旋转黏度计测定溶液-凝胶相转变特性筛选处方;采用HPLC法测定PNS中人参皂苷Rg1,并以不同动物模型对制剂进行安全性评价。结果离子敏感型原位凝胶的黏度随着去乙酰结冷胶质量分数的增加而上升,加入模拟鼻液后形成具有一定强度的凝胶。该制剂的pH值为6.0～6.5,人参皂苷Rg1在0.2～50μg/mL线性关系良好(r=0.999 5),平均回收率为101.72%,RSD为1.74%。本制剂能延长药物与鼻黏膜的接触时间。结论该制剂制备工艺简便,性质稳定,安全无明显刺激性,在PNS鼻腔给药方面表现出良好的发展潜力。

Objective To prepare an ion-sensitive in situ nasal gel of Panax notoginseng saponins（PNS）.Methods With deacetylated gellan gum as gel base,the solution-gelation conversion characteristics were investigated by rotational viscometer,and the content of ginsenoside Rg1 in PNS was determined by HPLC.Various animal models were used for the safety assessment of the preparations.Results The viscosity of ion-sensitive in situ gel increased with the increasing concentration of deacetylated gellan gum.Upon addition of simulated nasal fluid,gels with certain strengths were formed.The pH value of the preparation was 6.0-6.5,and the linear range of ginsenoside Rg1 was 0.2-50 μg/mL（r = 0.999 5）,with a mean recovery of 101.72% and RSD of 1.74%.The preparation could extend the drug contact time with the nasal mucosa.Conclusion PNS ion-sensitive in situ nasal gel is easy-to-prepare,stable and safe,and with limited irritation.It shows great potential in nasal delivery of PNS.