大蒜素自微乳的制备与质量评价  

Preparation and quality evaluation of dially trisulfide self-microemulsifying drug delivery system

作　　者：徐云峰[1,2] 刘清飞[1] 陈曦[1] 罗国安[1] 王义明[1] 

机构地区：[1]清华大学医学院,北京100084 [2]江西中医学院,南昌330006

出　　处：《中国新药杂志》2008年第22期1940-1944,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30500666);清华大学裕元基金(2003BA310A03)

摘　　要：目的:制备大蒜素(DATS)自微乳制剂,并评价其质量。方法:采用伪三元相图法,以聚氧乙烯氢化蓖麻油RH-40为表面活性剂,无水乙醇为助表面活性剂,油酸为油相,绘制该系统的相图,在此基础上制备DATS自微乳;建立HPLC法测定DATS自微乳中DATS的含量;对自微乳的外观性状、相对密度、黏度、pH值、电导率、形态、粒径及粒度分布、Zeta电位、含量、配伍和稳定性等进行研究。结果:DATS自微乳为无色澄明液体,稳定性良好,相对密度为0.840 g.mL-1,黏度为5.447 mPa.s,遇水形成O/W型微乳,稀释250倍后电镜下观察成圆球形,平均粒径26.4 nm,Zeta电位0.398 mV,pH值5.62,电导率为8.37μs.cm-1,3批制剂的含量分别为31.77,31.45,32.15 mg.mL-1。DATS自微乳与葡萄糖注射液、氯化钠注射液等配伍稳定。结论:DATS自微乳制备工艺简单,性质稳定,质量易控。Objective：To prepare dially trisulfide（DATS） self-microemulsifying drug delivery system（SMEDDS） and evaluate its quality.Methods：Pseudo-ternary phase was used to evaluate the self-microemulsification existence area.The formulation and the preparation of DATS SMEDDS were studied.HPLC method was used to determine DATS SMEDDS.The appearance,density,viscosity,pH,electrical conductivity,morphology,particle size distribution,Zeta potential,contents,and stability of DATS SMEDDS were studied,respectively.Results：The DATS SMEDDS prepared was a translucent and achromatous solution with good stability.The density and viscosity were 0.840 g·mL^-1 and 5.447 mPa·s,respectively.After being diluted with water for 250 times,DATS SMEDDS consisted of small spherical drops with the mean size of 26.4 nm.Zeta potential,pH,and electrical conductivity were 0.398 mV,5.62,and 8.37 μs·cm^-1,respectively.The contents of three batches of DATS SMEDDS were 31.77 mg·mL^-1,31.45 mg·mL^-1 and 32.15 mg·m^-1,respectively.Diluted with glucose injection and sodium chloride injection,respectively,DATS SMEDDS were still stable.Conclusion：DATS SMEDDS,with good stability,was easy to prepare and the quality was easy to control.

关 键 词：大蒜素 自微乳 制备 质量评价 

分 类 号：R943.3[医药卫生—药剂学]