近年来,药剂学领域出现许多增加水难溶性药物溶解度和吸收的技术,其中自乳化释药系统(self-emulsifyung drug delivery systems,SEDDS)得到了广泛的发展[1,2].SEDDS是由药物、油、乳化剂及助溶剂等组成的一种油状混合物,在体外轻微振荡或体内胃肠道的蠕动下自发的形成一种热力学稳定的乳状液,其粒径大约100～300 nm,粒径小于100 nm的乳剂称为自微乳化释药系统(self-microemulsifying drug delivery systems,SMEDDS).与SEDDS相比,SMEDDS的最大优点是粒径小、溶液澄清透明、药物增溶量大、制剂更稳定.本文就SMEDDS的处方组成、结构与理化性质、质量评价以及应用等方面作一简要综述.

OBJECTIVETo prepare silybin lipid nanospheres (SLN) and to evaluate the properties of morphology, particle size and the silybin distribution in mice.METHODSilybin lipid nanospheres were prepared by thin film emulsion-high pressure homogenization technique. Concentrations of silybin in mice blood, liver, spleen, lung, kidney, brain, heart, stomach after oral administration were determined by high performance liquid chromatography.RESULTScanning electron micrograph showed that most of the SLN were spherical. The average diameter from photon correlation spectrometer was 148.9 nm with the polydispersity 0.17. Body distribution data indicated that SLN could increase the distribution of silybin in blood and liver, decrease the amount of silybin in stomach as compared with the preparation on market, and the drug targeting index (DTI) in liver was 1.81.CONCLUSIONSLN can increase the uptake of silybin in liver after oral administration, which must benefit the hepatitis treatment.

目的:建立高效液相色谱法 (HPLC)监测苯妥英钠血药浓度的方法。 方法:色谱条件:分离柱:Nova-PakC18 (3．9mm×150mm),流动相:甲醇-水(59 :41),检测波长:254nm。结果:苯妥英 钠在4．2～65．4μg／ml范围内与峰面积呈 良好的线性关系(r=0．9994),日内及日 间误差均小于6％,平均回收率达98． 8％。结论:本法操作简单、准确,可用于 苯妥英钠血药浓度的监测。

OBJECTIVE To prepare the PVP-lecithin-bile salt mixed nano-micelles containing silybin, and to evaluate the characters in vitro and pharmacokinetics in mice.METHODS The prepared nano-micelles were observed by transmission electron microscope. The Zeta potential and the diameters distribution of SLB nano-micelle were measured by photo correlation spectroscopy(PCS). The drug loading was determined by ultraviolet speetrophotometry. The SLB concentrations in mice blood samples were assayed by high-performance liquid chromatography (HPLC), and the data were analyzed with BAPP2.0 program package. RESULTS SLB nano-micelles were almost spherical, smaller than 100 nm with a mean diameter of 61.2 nm, and had a zetar potential of-44.8mV. The drug loading was 4.19 g·L-1. The concentration-time data fitted of with a two-compartment model showed that, in comparison with the control preparation, the SLB nano-micelles accederated Ka, shortened tmax,prolonged the mean residenced time(MRT), and increased the ρmax and AUC0-∞.CONCLUSION The PVP-lecithin-bile salt mixed nano-micelles can be used as a new carrier for poorly water-soluble drugs.