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基于药辅合一理念的川芎与当归挥发油透皮作用研究

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目的 结合中药挥发油"药辅合一"的特性优势,研究川芎挥发油(Chuanxiong Rhizoma volatile oil,LVO)、当归挥发油(Angelicae Sinensis Radix volatile oil,AVO)提取方式、质量控制及其经皮渗透性与促透皮作用。方法 采用正交设计优选挥发油提取工艺;通过LVO、AVO物理参数与指标成分含量检测进行其质量控制;采用Franz扩散池法进行体外透皮研究,高效液相色谱(HPLC)法测定指标成分藁本内酯与白藜芦醇(resveratrol,RSV)的含量,以稳态透皮速率(Jss)和增透倍数(EF)为评价指标,分别考察不同浓度LVO、AVO及混合使用经皮渗透性及促透皮作用的影响。结果 确定LVO、AVO提取工艺为8倍量水,蒸馏时间8 h,用乙酸乙酯收集,无水硫酸钠脱水后减压挥干;对LVO、AVO建立了完善的质量控制方法,其中包括性状、相对密度、pH值、旋光度、黏度及藁本内酯含量测定;LVO、AVO均具有良好的渗透性和促RSV体外透皮作用,10 h内Jss最大分别为(48。23±6。53)(27。84±3。03)μg·cm-2·h-1,EF值最大分别为4。51、19。34。结论 LVO、AVO单独和混合使用均具有良好的渗透性和促RSV透皮吸收作用,LVO的经皮渗透性明显高于AVO,而AVO的促渗透性则高于LVO。LVO、AVO良好的经皮渗透性与透皮吸收促进作用相结合,起到"药辅合一"的作用,具有良好的临床使用优势,为其在中药透皮给药制剂的开发和应用奠定基础。
Chuanxiong Rhizoma and Angelicase Sinensis Radix Volatile Oil Study and Transdermal Effect Based on the Concept of Unification of Drugs and Excipients
OBJECTIVE To study the extraction method,quality,transdermal permeability,and transdermal promoting effects of Chuanxiong Rhizoma Hort.volatile oil(LVO)and Angelicase Sinensis Radix volatile oil(AVO)combined with the characteristic advantages of"unification of drugs and excipients"of traditional Chinese medicine volatile oil.METHODS The orthogonal design was used to screen and optimize extraction process of LVO and AVO.Quality control was carried out by detecting the physical parame-ters and indicator component content of LVO and AVO.Franz diffusion cells were used to conduct the studies of skin permeation in vitro.The contents of ligustilide and resveratrol(RSV)were determined by HPLC,and the steady-state transdermal rate(Jss)and enhancement factor(EF)compared with blank were used as evaluation indicators.And the transdermal permeability and transdermal promoting effects of different concentrations of LVO,AVO and mixed were investigated respectively.RESULTS The extraction process for LVO and AVO involves 8 times the amount of water,heating and refluxing for 8 h,collecting with ethyl acetate,dehydra-ting anhydrous sodium sulfate,and then volatilizing under reduced pressure.Perfect quality control methods were established for LVO and AVO,including the properties,relative density,pH,optical rotation,viscosity and ligustilide content.LVO and AVO have good permeability and promote RSV transdermal effect in vitro,and the maximum Jss values within 10 h were(48.23±6.53)and(27.84±3.03),respectively,and the maximum EF values were 4.51 and 19.34,respectively.CONCLUSION LVO and AVO have good transdermal permeability and transdermal promoting effects of RSV when used alone or in combination.The transdermal permeability of LVO was significantly higher than that of AVO,while the transdermal promoting effects of AVO was higher than that of LVO.The combination of LVO and AVO's own pharmacological effects and good transdermal absorption promoting effect plays a role of"unification of drugs and excipients",which has a good advantage in clinical use,and lays a foundation for their development and application in transdermal drug delivery preparations of traditional Chinese medicine.

Chuanxiong Rhizoma Hort.Angelicase Sinensis Radixvolatile oilqualitytransdermal permeability

朱红梅、张爱军、李帅

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四川省中医药科学院,成都 610041

川芎 当归 挥发油 质量控制 经皮渗透

2024

中国药学杂志
中国药学会

中国药学杂志

CSTPCD北大核心
影响因子:0.957
ISSN:1001-2494
年,卷(期):2024.59(23)