大蒜素微乳的制备与质量研究

The study on preparation and quality of DATS microemulsion

目的研究稀释后可供静脉注射的大蒜素微乳的处方及制备工艺,并对大蒜素微乳进行质量评价。方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,绘制该系统的三元相图;在此基础上,进行处方筛选并确定最优的处方和该注射液的制备工艺;建立高效液相色谱法测定微乳中大蒜素的含量;分别考察大蒜素微乳的外观性状、pH值、离心稳定性、形态、粒径及粒度分布、稳定性等。结果该液相色谱含量测定方法简便、准确、可靠、切实可行;所制得的大蒜素微乳较稳定,外观澄明,略带淡蓝色乳光,为O/W型微乳,呈微弱酸性;球形完整,分散良好;粒径为14.9nm,稀释50倍后粒径为13.3nm,均呈Gauss分布。结论大蒜素微乳易于制备,较稳定,各项理化性质良好,质量易控。

Objective To prepare the dially trisulfide-loaded microemulsion （ME） for intravenous administration and evaluate its quality. Methods Ternary phase figure was plotted to evaluate the microemulsification existence area. Cremophor RH-40 was used as surfactant, ethanol as co-surfactant and oil acid as oil phase respectively. On the basis of ternary phase figure, the best formulation was obtained. HPLC method was employed to determine the content of DATS ME. The appearance, properties, pH value, centrifugal stability, morphology, particle size distribution and stability of DATS ME were reviewed and studied. Results The HPLC method was convenient, accurate, credible and practical for the determination of DATS. The prepared DATS ME had a good stability and a slight acidity. It was a translucent and achromatous solution with a visible sky-blue opalescence and confirmed to be O/W ME. Conclusions With stable physicochemical characteristics, DATS ME had a good stability and it was easy to prepare. The quality of DATS ME was easy to control.