通便水凝胶贴剂的处方优化及体外吸收促进剂的筛选  

Optimization of Prescription and in vitro Screening of Absorption Enhancers of Tongbian Hydrogel Patch

作　　者：王小宁[1] 任佩佩 李卫 马远涛[1] 赵阳光 张湛睿[1] WANG Xiaoning;REN Peipei;LI Wei;MA Yuantao;ZHAO Yangguang;ZHANG Zhanrui(College of Pharmacy,Xi'an Medical University,Xi'an 710021,China)

机构地区：[1]西安医学院药学院,陕西西安710021

出　　处：《现代中药研究与实践》2024年第1期63-67,共5页Research and Practice on Chinese Medicines

基　　金：陕西省教育厅青年创新团队项目(23JP156);陕西省科技厅自然科学研究项目(2024JC-YBMS-679);陕西省科技厅自然科学研究项目(2022JM-568);2021陕西省大学生创新创业训练项目(S202111840068);西安医学院2022年科研能力提升计划项目(2022NLTS060);2022陕西省大学生创新创业训练项目(S202211840077)。

摘　　要：目的研究通便水凝胶贴剂的最优处方,筛选有效的透皮吸收促进剂,提高药物的透皮吸收程度。方法以黏附性与皮肤残留量作为考察指标,通过正交试验筛选通便水凝胶贴剂的最优处方,用Franz扩散池进行大鼠离体皮肤渗透实验,用HPLC测定白术内酯Ⅰ与藁本内酯的透过量和透皮速率,考察透皮吸收促进剂对药物透皮速率的影响。结果以对贴剂成型影响较大的三个因素为考察对象,筛选出的最优处方为NP-8001.5 g、PAAS 0.5 g、EDTA-2Na 0.08 g、甘羟铝0.28 g、高岭土3 g、甘油15 g、PVPK904 g、酒石酸0.28 g、纯化水15 mL,以10%月桂氮[艹卓]酮+10%丙二醇作为透皮吸收促进剂制备的贴剂具有最好的透皮吸收效果。结论通便水凝胶贴剂处方稳定可行,透皮吸收效果好,为促进水凝胶贴剂的应用提供了理论依据。Objective To optimize the prescription of Tongbian hydrogel patch and investigate effective permeation enhancers to improve the drug transdermal absorption.Methods The optimal prescription of the Tongbian hydrogel patch was screened by orthogonal experiment with adhesion and skin residue as evaluation index.The in vitro skin permeation experiment of rats was conducted using Franz diffusion cells,and the permeation amount and transdermal rate of atractylenolide I and ligustilide were determined by HPLC to investigate the effect of permeation enhancers on the transdermal drug rate.Results After investigation of three factors that had a significant impact on the formation of patches,the optimal formula was NP-8001.5 g,PAAS 0.5 g,EDTA-2Na 0.08 g,glycerol 0.28 g,kaolin 3 g,glycerol 15 g,PVPK904 g,tartaric acid 0.28 g,purified water 15 mL,and the patch prepared with 10%lauryl alcohol+10%propylene glycol as permeation enhancers showed good transdermal absorption effects.Conclusion The prescription of Tongbian hydrogel patch is stable and feasible,and the effect of transdermal absorption is ideal,which provides a theoretical basis for promoting the application ofhydrogel patch.

关 键 词：功能性便秘 水凝胶贴剂 透皮吸收促进剂 白术内酯Ⅰ 藁本内酯 

分 类 号：R282.3[医药卫生—中药学]