不同促透剂对根皮素体外透皮吸收的影响(1)
[摘要] 目的 考察促透劑氮酮、薄荷醇、冰片、麝香酮对根皮素的透皮促进作用，为根皮素外用制剂研发提供依据。 方法 以18只2月龄雄性SD大鼠皮肤为渗透屏障，采用Franz扩散池进行体外透皮吸收实验，HPLC测定根皮素的含量，计算渗透动力学参数，评价不同促透剂对根皮素的促透作用。根皮素HPLC测定方法，色谱柱：Inertsil ODS -3(150 mm×4.6 mm，5 μm);流动相：乙腈-水(45∶55);流速：1.0 mL/min;检测波长：280 nm，进样量：20 μL，柱温：25℃。 结果 根皮素在0.1030～51.48 μg/mL浓度范围内回归方程为Y = 86.45C+3.901(r = 0.9999)。日内和日间精密度的RSD均<2.0%。氮酮、薄荷醇、冰片和麝香酮的浓度为4.0%时ER分别为8.825、13.561、6.540、3.466。 结论 氮酮、薄荷醇、冰片、麝香酮均对根皮素有促透作用，并且呈浓度依赖性，浓度在4.0%时促透作用最佳，筛选出根皮素的较优促透剂是薄荷醇。
[关键词] 根皮素;促透剂;透皮吸收;薄荷醇
[中图分类号] R914 [文献标识码] A [文章编号] 1673-7210(2019)11(b)-0004-05
Effect of different penetration enhancers on the transdermal absorption of phloretin
GUAN Bo1 HUANGFU Junru2 XU Yuan1 ZHOU Xuejiao3 LIU Xueying4 WANG Qingwei1
1.Department of Pharmacy， the Second Affiliated Hospital of Air Force Medical University， Shaanxi Province， Xi′an 710038， China; 2.Product Department， Ginwa Pharmaceutical Factory， Shaanxi Province， Xi′an 710065， China; 3.Department of Pharmacy， Xi′an Chest Hospital， Shaanxi Province， Xi′an 710075， China; 4.Department of Medicinal Chemistry and Pharmaceutical Analysis， School of Pharmacy， Air Force Medical University， Shaanxi Province， Xi′an 710032， China
[Abstract] Objective To investigate the effect of azone， menthol， borneol and muscone on the transdermal promotion of phloretin in order to provide basis for the research and development of external preparations of phloretin. Methods The skin of 18 male SD rats with 2-month-old as the permeation barrier， the Franz diffusion cell was used to conduct the in vitro transdermal absorption experiment. The content of phloretin was determined by HPLC， the permeation kinetic parameters were calculated， and the permeation promoting effect of different transdermal enhancers on phloretin was evaluated. HPLC method for the determination of phloretin was as followed， chromatographic column： Inertsil ODS-3 (150 mm×4.6 mm， 5 μm); mobile phase： acetonitrile water (45：55); flow rate： 1.0 mL/min; detection wavelength： 280 nm; injection volume： 20 μL; column temperature： 25℃. Results The regression equation of phloretin in the concentration range of 0.1030-51.48 μg/mL was Y = 86.45C+3.901 (r = 0.9999). RSD of intraday and intraday precision was less than 2.0%. When the concentrations of azone， menthol， borneol and muscone were 4.0%， ER was 8.825， 13.561， 6.540 and 3.466 respectively. Conclusion Azone， menthol， borneol and muscone can enhance the transdermal effect of phloretin in a concentration-dependent manner. 4.0% penetration enhancer has the best promoting effect. The better transdermal enhancer for phloretin is menthol., 百拇医药(关波 皇甫俊茹 徐媛)
[关键词] 根皮素;促透剂;透皮吸收;薄荷醇
[中图分类号] R914 [文献标识码] A [文章编号] 1673-7210(2019)11(b)-0004-05
Effect of different penetration enhancers on the transdermal absorption of phloretin
GUAN Bo1 HUANGFU Junru2 XU Yuan1 ZHOU Xuejiao3 LIU Xueying4 WANG Qingwei1
1.Department of Pharmacy， the Second Affiliated Hospital of Air Force Medical University， Shaanxi Province， Xi′an 710038， China; 2.Product Department， Ginwa Pharmaceutical Factory， Shaanxi Province， Xi′an 710065， China; 3.Department of Pharmacy， Xi′an Chest Hospital， Shaanxi Province， Xi′an 710075， China; 4.Department of Medicinal Chemistry and Pharmaceutical Analysis， School of Pharmacy， Air Force Medical University， Shaanxi Province， Xi′an 710032， China
[Abstract] Objective To investigate the effect of azone， menthol， borneol and muscone on the transdermal promotion of phloretin in order to provide basis for the research and development of external preparations of phloretin. Methods The skin of 18 male SD rats with 2-month-old as the permeation barrier， the Franz diffusion cell was used to conduct the in vitro transdermal absorption experiment. The content of phloretin was determined by HPLC， the permeation kinetic parameters were calculated， and the permeation promoting effect of different transdermal enhancers on phloretin was evaluated. HPLC method for the determination of phloretin was as followed， chromatographic column： Inertsil ODS-3 (150 mm×4.6 mm， 5 μm); mobile phase： acetonitrile water (45：55); flow rate： 1.0 mL/min; detection wavelength： 280 nm; injection volume： 20 μL; column temperature： 25℃. Results The regression equation of phloretin in the concentration range of 0.1030-51.48 μg/mL was Y = 86.45C+3.901 (r = 0.9999). RSD of intraday and intraday precision was less than 2.0%. When the concentrations of azone， menthol， borneol and muscone were 4.0%， ER was 8.825， 13.561， 6.540 and 3.466 respectively. Conclusion Azone， menthol， borneol and muscone can enhance the transdermal effect of phloretin in a concentration-dependent manner. 4.0% penetration enhancer has the best promoting effect. The better transdermal enhancer for phloretin is menthol., 百拇医药(关波 皇甫俊茹 徐媛)