摘要
目的:考察不同浓度的薄荷脑对雪上一枝蒿甲素经皮促渗的药动学及体内外相关性。方法:分别制备含1%、3%、5%薄荷脑的雪上一枝蒿总碱凝胶,采用改良的Franz扩散池法进行体外释放及透皮研究;结合UPLC-MS/MS联用技术检测雪上一枝蒿甲素在小鼠血液中的药物浓度随时间的变化过程,并对其进行体内药动学研究;以体外24h溶出率为横坐标,AUC为纵坐标,对体外透皮结果与体内药动学结果进行回归分析。结果:与未加薄荷脑的雪上一枝蒿总碱凝胶相比,1%、3%、5%三种不同浓度薄荷脑的增渗倍数(ER)分别为2. 62、3. 26、4. 48,促渗雪上一枝蒿甲素的相对生物利用度分别为163. 39%、189. 16%、310. 69%,体内外相关系数为0. 9591。结论:体内外促渗效果一致,此方法可用于评价透皮给药系统体内外的相关性。
Objective： The study was carried out to investigate the pharmacokinetics and in vitro/in vivo correlation of Bullatine A with Different concentrations of menthol aspenetration enhancers（PE） following transdermal administration. Methods： ordinary gel of bullatine A total alkaloids containing 1%,3%,5% concentrations of menthol as PE were prepared. Single-chamber diffusion cell was used in vitro,In vivo tests,the changes of bullatine A in plasma of mice with time in ordinary gel of bullatine A total alkaloids were compared through UPLC-MS/MS,and their pharmacokinetic parameters were also compared andanalyzed. And the linear regression equation was figured through the concentration of cumulative in vitro and the concentration of cumulative absorption in vivo. Results： In comparison with negative control（no PE was added）,the ER with 1%,3%,5% concentrations of menthol as PE were determined to be 2. 62,3. 26,and 4. 48,the relative bioavailability values were determined to be 163. 39%,189. 16%,and 310. 69%,The correlation coefficients were measured to be 0. 9591. Conclusion： Promoting effect is the same in vivo and in vitro,and this method can be used to evaluate the correlation between in vitro and in vivo transdermal delivery.
作者
邓显仪
陈晓兰
吴玉梅
唐红艳
Deng Xianyi;Chen Xiaolan;Wu Yumei;Tang Hongyan(College of Pharmacy,GuiYang college of Traditional Chinese Medicine,Guiyang 55002)
出处
《中药药理与临床》
CAS
CSCD
北大核心
2018年第4期77-80,共4页
Pharmacology and Clinics of Chinese Materia Medica
基金
国家自然科学基金地区基金(No.81260646)
贵州省科学技术基金(黔科合J字[2012]2066号)
贵州省中医药管理局中医药
民族医药科学技术研究课题(QZYY2011-58)
贵阳中医学院博士基金项目
关键词
薄荷脑
促渗剂
雪上一枝蒿甲素
体内外相关性
menthol
penetration enhancers
Bullatine A
in vitro/in vivo correlation
