摘要
目的研究六合丹的体外透皮吸收性及两种透皮材料对盐酸小檗碱、大黄酸的透皮吸收差异。方法选用立式改良的Franz透皮扩散池,接收液为30%乙醇生理盐水,透皮材料为小鼠腹部皮肤及乳猪背部皮肤,采用HPLC测定盐酸小檗碱和大黄酸的含量,计算透皮吸收动力学参数。结果盐酸小檗碱和大黄酸中小鼠皮肤的Q24分别为174.804、24.323μg·cm^-2,Js为7.348、1.058μg·cm^-2·h^-1,T为53.39%、48.22%,采用小鼠皮肤时各透皮吸收参数分别是乳猪皮肤的3.25、2.37倍,3.15、2.51倍和3.21、3.73倍。盐酸小檗碱和大黄酸在24 h内的透皮吸收曲线均符合零级方程。结论小鼠皮肤对两种成分的透皮性能优于乳猪皮肤,两种成分的透皮过程与制剂中各成分的量无关,盐酸小檗碱的释药机制为扩散和溶出的协同作用,大黄酸以扩散为主,药物的体外透皮吸收性较稳定。
OBJECTIVE To investigate percutaneous absorbability of Liuhedan preparation(LP)and differences of the two kinds of transdermal materials on transdermal delivery of berberine hydrochloride and rhein.METHODS Vertical modified Franz transdermal diffusion cell was used,and the abdominal skins of mice and piglet’s dorsal skin were selected as transdermal materials to perform transdermal experiment in vitro with 30%normal saline.The contents of berberine hydrochloride and rhein in receptor fluid were determined at different times by HPLC to calculate the kinetic parameters of permeation.RESULTS Q24 of mouse skin in berberine hydrochloride and rhein was 174.804,24.323μg·cm^-2(3.25 times,2.37 times of piglets’skin),Js was 7.348,1.058μg·cm^-2·h^-1(3.15 times,2.51 times),T was 53.39,48.22%(3.21 times,3.73 times)respectively.The transdermal absorption curves of berberine hydrochloride and rhein in the LP were accorded with the Zero-order equation.CONCLUTION The transdermal performance of mouse skin is better than the excised minipigs skin.The transdermal absorption process is unrelated to the amount of each component,and the release mechanism of berberine hydrochloride is the synergistic effect of diffusion and dissolution,while rhein is diffusion,and the drug has stable transdermal absorption in vitro.This experiment provides reference for the study of ointment transdermal.
作者
常寒
董鉴霞
杨力
王逍
宋毅
费小凡
王曙
CHANG Han;DONG Jianxia;YANG Li;WANG Xiao;SONG Yi;FEI Xiaofan;WANG Shu(West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China;West China Hospital of Pharmacy,Sichnan University,Chengdu,Sichuan,610041 P.R.China)
出处
《华西药学杂志》
CAS
CSCD
2020年第6期599-603,共5页
West China Journal of Pharmaceutical Sciences
基金
四川省科技厅项目(编号:2015SZ0039)。
关键词
六合丹
盐酸小檗碱
大黄酸
急性胰腺炎
透皮材料
Franz扩散池法
透皮吸收
含量测定
累积透皮量
释药机制
协同作用
扩散
溶出
Liuhedan preparation
Berberine hydrochloride
Rhein
Acute pancreatitis
Transdermal material
Franz diffusion cell
Mice
Piglet
Transdemal absorbability
Contents determination
Accumulation transdermal amount
Release mechanism
Synergistic effect
Diffusion
Dissolution
