中国中药杂志

2009, v.34(21) 2730-2733

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丹皮酚微乳凝胶剂的制备及体外透皮特性研究
Preparation of paeonol microemulsion gel its and transdermal characterization in vitro

刘继勇;韩盈;杨明;朱全刚;胡晋红;
LIU Jiyong,HAN Ying,YANG Ming,ZHU Quangang,HU Jinhong* (Department of Pharmacy,Changhai Hospital,Second Military Medical University,Shanghai 200433,China)

摘要(Abstract):

目的:制备丹皮酚微乳和微乳凝胶剂,并对其含量、理化性质和体外透皮特性进行考察。方法:以IPM为油相,卵磷脂/APG为表面活性剂,1,2-丙二醇为助表面活性剂,在室温下采用磁力搅拌法滴加水到油相中,制备丹皮酚微乳。采用HPLC测定丹皮酚微乳中丹皮酚的含量。采用透射电镜和激光粒径测定仪分别测定微乳的形态和粒径。以卡波姆940为基质,制备丹皮酚微乳凝胶。采用Franz扩散池对微乳、微乳凝胶的体外透皮特性进行了考察。结果:制备的丹皮酚微乳为O/W型微乳,外观圆整、均匀,粒径32 nm,含量稳定。丹皮酚饱和水溶液、微乳、微乳凝胶的稳态渗透速率分别为47.846,103.760,70.401μg.cm-2.h-1,12 h的累积渗透量分别为657.179,1 266.484,881.217μg.cm-2。结论:丹皮酚微乳、微乳凝胶的12h累积渗透量和渗透速率均优于丹皮酚饱和水溶液,可为丹皮酚经皮给药提供一种新的剂型。
Objective: To prepare paeonol microemulsion and microemulsion gel,and investigate its content,physical and chemical properties.Their transdermal properties in vitro were studied as well.Method: IPM acted as oil phase,lecithin/APG as surfactant,1,2-propanediol as cosurfactant,water was added dropwise to the oil phase to prepare paeonol microemulsion at room temperature using magnetic stirring.HPLC method were used to determine the content of paeonol in paeonol microemulsion.Transmission electron microscopy and laser particle size analyzer were used to determine the shape and size of the microemulsion.Carbopol 940 was uesd as substrate to prepare paeonol microemulsion gel.Franz diffusion cell was used for characterizing the microemulsion and gel transdermal properties in vitro.Result: The paeonol microemulsion was O/W microemulsion.Its uniform particle size was 32 nm and was with roundness appearance and stable content.The steady-state permeation rates of paeonol saturated aqueous solution,microemulsion,and microemulsion gel were 47.846,103.760,70.401 μg·cm-2·h-1,and their 12 h cumulative amount of infiltration were 657.179,1 266.484,881.217 μg·cm-2,respectively.Conclusion: The 12 h cumulative infiltration and infiltration rate of paeonol microemulsion and microemulsion gel are better than the saturated aqueous solution.Paeonol microemulsion gel is a new dosage form for transdermal drug delivery.

关键词(KeyWords): 丹皮酚;微乳;微乳凝胶;经皮给药
paeonol;microemulsion;microemulsion gel;transdermal drug delivery

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基金项目(Foundation): 国家自然科学基金项目(30801557)

作者(Author): 刘继勇;韩盈;杨明;朱全刚;胡晋红;
LIU Jiyong,HAN Ying,YANG Ming,ZHU Quangang,HU Jinhong* (Department of Pharmacy,Changhai Hospital,Second Military Medical University,Shanghai 200433,China)

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