脂溶性药物在O/W型微乳中的分配行为

Distribution behavior of lipophilic drugs in the oil-in-water microemulsions

以亮菌甲素和氧氟沙星为模型药物,采用荧光光谱法考察微乳中各组分对药物荧光光谱的影响,以研究脂溶性小分子药物在O/W型微乳中的分配行为。结果显示在分别采用苯甲醇和PEG 400为助表面活性剂的微乳体系中,亮菌甲素主要存在于表面活性剂组成的界面膜中;氧氟沙星在油酸/橄榄油(1∶1)的微乳体系中的主要分布部位为油核,而在Gradamol GTCC为油相的微乳体系中主要存在于界面膜中;在各体系中药物均倾向于增溶在对药物溶解能力最强的组分所处的微环境中,具体的存在位置与该组分的用量有关。由此可见脂溶性药物在O/W型微乳中的存在部位可能取决于各组分对药物的溶解能力。

Distribution behavior of lipophilic drugs in the oil-in-water （O/W） microemulsions was studied. Fluorescence spectra analysis was performed to investigate the effect of the compositions of microemulsions on the fluorescence spectra of armillarisin and ofloxacin which were used as the model drugs. The fluorescence spectra of the model drugs in the microemulsions with various amount of the compositions were compared. The results showed that the armillarisin were both localized in the interfacial film of microemulsion systems with both phenylmethanol and PEG 400 as the co-surfactants, separately. Ofloxacin was localized in the interfacial film of microemulsion systems with Gradamol GTCC as the oil phase, but in the oil pool of microemulsion systems with oleic acid/olive oil （OA/OO） （ 1 ： 1 ） as the oil phase. Besides, it was found that the drug would have the tendency to locate in the microenvironment where the composition with the largest solubility to model drug is located, and its actual localized position would be dependent on the amount of this composition. The results indicate that the localized region of lipophilic drug in the O/W microemulsion systems is related with the solubility of the model drug in various compositions.