脂溶性药物在O_W型微乳中的分配行为

脂溶性药物在O /W 型微乳中的分配行为

姚　静1

,顾晓天2

,周建平

13

,平其能1,卢　韵

1

(1.中国药科大学药剂教研室,江苏南京210009;2.南京师范大学分析测试中心,江苏南京210097)

摘要: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Grada mol 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。

关键词:微乳;荧光光谱法;增溶区域;界面膜;油核

中图分类号:R943.4 文献标识码:A 文章编号:0513-4870(2007)07-0768-06

收稿日期:2006210211.3

通讯作者　Tel:86-25-83271272,Fax:86-25-83301606,

E 2mail:zhouj pcpu@

D istr i buti on behavi or of li pophili c drugs

i n the oil 2i n 2water m i croe mulsi ons

Y AO J ing 1

,G U Xiao 2tian 2

,ZHOU J ian 2p ing 13

,P I N G Q i 2neng 1

,LU Yun

1

(1.D epart m ent of Phar m aceutics,China Phar m aceutical U niversity,N anjing 210009,China;

2.A nalysis and Testing Center ,N anjing N or m al U niversity,N anjing 210097,China )

Abstract:D istributi on behavi or of li pophilic drugs in the oil 2in 2water (O /W )m icr oe mulsi ons was

studied .Fluorescence s pectra analysis was perf or med t o investigate the effect of the compositi ons of m icr oe mulsi ons on the fluorescence s pectra of ar m illarisin and ofl oxacin which were used as the model drugs .The fluorescence s pectra of the model drugs in the m icr oe mulsi ons with vari ous a mount of the compositi ons were compared .The results showed that the ar m illarisin were both l ocalized in the interfacial fil m of m icr oe mulsi on syste m s with both phenyl m ethanol and PEG 400as the co 2surfactants,separately .Ofl oxacin was l ocalized in the interfacial fil m of m icr oe mulsi on syste m s with Grada mol GT CC as the oil phase,but in the oil pool of m icr oe mulsi on syste m s with oleic acid /olive oil (OA /OO )(1∶1)as the oil phase .Besides,it was found that the drug would have the tendency t o l ocate in the m icr oenvir onment where the compositi on with the largest s olubility t o model drug is l ocated,and its actual l ocalized positi on would be dependent on the a mount of this compositi on .The results indicate that the l ocalized regi on of li pophilic drug in the O /W m icr oe mulsi on syste m s is related with the s olubility of the model drug in vari ous compositi ons .

Key words:m icr oe mulsi on;fluorescence s pectra analysis;s olubilized regi on;interfacial fil m ;oil core

作为药剂学领域极具发展前景的药物载体系

统,近年来微乳一直受到广泛的关注[1]

,但关于微

乳中药物分配规律即其增溶区域的研究不多。一般

小分子溶质在微乳中的存在部位包括:油核、表面活性剂及助表面活性剂形成的界面膜层和水相。脂溶性小分子药物在水中难溶,存在于水相中的药量可以忽略不计。以往的研究认为脂溶性药物大多存在