摘要
目的探索复方左旋肉碱涂膜剂相转变过程对其透皮特性的影响,为涂膜剂相转变产生的促渗作用提供理论依据。方法以辣椒碱、左旋肉碱累积透皮百分率为测定指标,用改良的Franz扩散池及离体兔皮进行透皮实验,高效液相色谱法测定不同时间透皮接收液中各成分的含量,绘制透皮曲线,分析透皮规律与特性。结果复方左旋肉碱涂膜剂相变前和相变后透皮动力学曲线皆为连续型函数,而相转变过程为非连续型函数,含透皮促进剂样品A与不含透皮促进剂样品B的透皮速度和透皮量参数95%置信区间重叠,差别皆无统计学意义,说明两者透皮速度和透皮量相同;而样品A和样品B与样品C(不含成膜材料)的透皮速度和透皮量参数95%置信区间未重叠,差别皆有统计学意义,以辣椒碱为指标,样品A和样品B的透皮速度分别是样品C的1. 459、1. 450倍;样品A和样品B的透皮量分别是样品C的2. 53、1. 907倍;以左旋肉碱为指标,样品A和样品B的透皮速度分别是样品C的1. 153、1. 169倍;样品A和样品B的透皮量分别是样品C的1. 722、1. 692倍。结论相转变过程可使复方左旋肉碱涂膜剂的透皮速度和透皮量徒增,徒增时间与涂膜剂成膜时间吻合,相转变过程产生的促渗作用远远大于加入透皮吸收穿透促进剂的促渗作用(P <0. 05)。
OBJECTIVE To explore the effect of phase transition process of compound L-carnitine plastics on the characters of transdermal absorption, provide a theoretical evidence for the penetration enhancing effect produced from phase transition process. METHODS The accumulated transdermal percentage of capsaicin and L-carnitine were used as measurement indicators, the experiment was finished by improved Franz diffuser and disembodied rabbit skin, the content of different components in transdermal receiving solution and in skin that received in different time was determined by HPLC, the curve of transdermal was drawn been drawn, the rule and the characters of transderulal were analyzed. RESULTS The transdermal dynamics curve before and after the phase transition of compound L-carnitine plastics is a kind of continuous function, while it become a kind of non-continuous function during the process of the phase transition. The 95% confidence interval of the parameters of transdermal velocity and amount between sample A with trans-dermal enhancer and sample B without transdermal enhancer shows overlap, the difference shows no statistical significance between sample A and B. It was showed that the sample A have the same transdermal rate and amount as B. While 95% confidence interval of the parameters of transdermal velocity and amount among sample A, B and C （without film-former materials） shows no overlap, the difference shows statistical significance among sample A, B and C. When the capsaicin was used as indicators, the transdermal rate of sample A and B respectively are 1. 459 times and 1. 450 times of C, the transdermal amount of sample A and B respectively are 2. 53 times and 1. 907 times of C. When the capsaicin was used as indicators, the transdermal rate of sample A and B respectively are 1. 153 times and 1. 169 times of C, the transdermal amount of sample A and B respectively are 1. 722 times and 1. 692 times of C.CONCLUSION Phase transition process can significantly increase both transdermal rate and tran
作者
陈光宇
刘平安
谢梦洲
杨崧
何群
CHEN Guang-yu;LIU Ping-an;XIE Meng-zhou;YANG Song;HE Qun(Engineering Center of Medicinal and Edible Functional Food,Hunan University of Chinese Medicine,Changsha 410208,China;College of Pharmacy of Hunan University of Chinese Medicine,Changsha 410208,China;Druggability of Traditional Chinese Medicine and Preparations,Key Laboratory of Hunan Province,Changsha 410208,China;Key Disciplinary of ＂The 12th Five-Year Plan＂ of Pharmacy in Hunan Province,Changsha 410208,China)
出处
《中国药学杂志》
CAS
CSCD
北大核心
2018年第18期1578-1583,共6页
Chinese Pharmaceutical Journal
基金
长沙市科技局计划项目资助(K0803123-21)
