中医学报2018，Vol.33Issue(3)：453-457,5.DOI:10.16368/j.issn.1674-8999.2018.03.109
三元乳癖消凝胶膏剂体外透皮给药研究
Study on Transdermal in Vitro Drug Delivery of Sanyuan Rupixiao Hydrogel Paste
摘要
Abstract
Objective:To study the behavior characteristics and mechanisms of the transdermal tetrahydropalmatine (THP) delivery in vitro of Sanyuan Rupixiao hydrogel paste,and to provide basis for clinical treatment of the hydrogel paste.Methods:The three formulations of optimized formulation (SRHP),containing 5％ azone (SRHP + A) without titanium dioxide (SRHP-T) formulations of Sanyuan Rupixiao hydrogel paste were manufactured in GMP approved workshops at the pilot scale.The amount of THP was determined by HPLC system.The vertical double chamber diffusion cells were used to investigate the behavior characteristics and mechanisms of the different formulations of Sanyuan Rupixiao hydrogel paste.Histological examination of skin samples after treatment with Sanyuan Rupixiao hydrogel paste was conducted on paraffin sections and then viewed by scanning electron microscope.Results:The THP can be detected in the receiving solution after the hydrogel paste sticking skin 0.5 h.The accumulative penetration amount of THP for SRHP,SRHP + A and SRHP-T were similar (t-test,P ＞ 0.05) during 0.5 h to 2.0 h.however,after 2.0h,the difference among them gradually obvious.At 48h,the accumulative penetration amount of THP(μg · cm-2) for SRHP,SRHP + A and SRHP-T wwas 7.154 3,4.774 8 and 3.988 6 (t-test,P ＜0.05),respectively.At 2 h,the permeation rate of THP reached peak value for SRHP,SRHP + A and SRHP-T.The permeation rate during 0 h to 24 h (JSRHP:0→24 =0.1782,JSRHP+A:0→24 =0.145 7,JSRHP-T:0→24 =0.103 6) higher than those during 24 h to 48 h (JSRHP:24→48 =0.119 9,JSRHP+A:24→48 =0.053 2,JSRHP-T:24→48 =0.077 7).Throughout the course of the experiment,the permeation rate of THP for SRHP (JSRHP:0→48 =0.149 1) was higher than that of SRHP + A (JSRHP + A:0→48 =0.099 4) and SRHP-T (JSRHP-T:0→48 =0.090 6) (t-test,P ＜ 0.05).The skin treated by hydrogel paste showed by scanning electron microscope that the skin surface was rough,the layered structure was loose and some keratinocytes desquamated,intercellular space was enlarged.Conclusion:The design of the prescription of Sanyuan Rupixiao hydrogel paste was reasonable,the permeability of THP through skin could be increased by disrupting the dense and orderly arrangement of the stratum corneum,and the drug was sustained release from the hydrogel paste and effective absorbed through skin.关键词
三元乳癖消凝胶膏剂/延胡索乙素/透皮给药/中药Key words
Sanyuan Rupixiao hydrogel paste/tetrahydropalmatine/transdermal drug delivery/Traditional Chinese Medicine分类
医药卫生引用本文复制引用
程玉钏,李伟泽,赵宁,韩文霞,付丽娜,梁泽,姚姣妮..三元乳癖消凝胶膏剂体外透皮给药研究[J].中医学报,2018,33(3):453-457,5.基金项目
国家自然科学基金项目(81303231) （81303231）
陕西省自然科学基金面上项目(2017JM8109) （2017JM8109）
山西省科技厅创新药物研制重大专项(20121101014) （20121101014）
