熊果苷缓释乳膏的制备工艺优化及体外释放度考察 - 中国实验方剂学杂志.doc

熊果苷缓释乳膏制备工艺优化及体外释放度考察 杨人泽严金玲 （赣南医学院第一附属医院江西 赣州 341000） 摘要目的优化熊果苷缓释乳膏制备工艺，考察其体外释放度。方法平均乳滴数乳化温度、乳化时间搅拌速度采用正交设计优化熊果苷缓释乳膏的制备工艺；采用HPLC测定熊果苷熊果苷缓释乳膏的体外释放度。结果最佳制备工艺为乳化温度80 ℃，乳化时间20 min，搅拌速度为以1 200 r·min?1搅拌20 min，停止加热，以500 r·min?1搅拌直至冷却。制得熊果苷缓释乳膏有明显的缓释作用。结论的制备工艺稳定可行，所得样品良好的缓释效果熊果苷缓释乳膏。 关键词 熊果苷；制备工艺；缓释乳膏 Optimization of Preparation Technology and Investigation of in vitro Release of Arbutin Sustained-release Cream YANG Ren-ze[1] DING Le[2] YAN Jin-ling[1]* (1 The First Affiliated Hospital of Gannan Medical University,Ganzhou 341000,China 2 Gan Zhou Maternal and Child Health Hospital, Gan Zhou China 341000) [Abstract] Objective：To optimize the preparation of arbutin sustained-release cream preparation and investigate its release in vitro.Method：The technology was optimized by orthogonal test by emulsifying temperature, emulsifying time and agitating speed; the analysis of variance was performed by SAS 9.1; the release of arbutin sustained-release cream in vitro was determined by HPLC.Result：The optimum preparation procedure was: emulsifying temperature 80℃, emulsifying time 20 min and agitating with 1200 r·min?1 for 20 min then changed to 500 r·min?1. The samples showed a sustained-release property in vitro.Conclusion：The the obtained samples was stable and practical and had showed good sustained-release characteristics. [Key words] arbutin; preparation technology; sustained-release preparation; cream; stability 熊果苷结构不同可分为α型和β型，均具有美白效果，其化学名为4-羟基苯-α-D-吡喃葡萄糖苷（α-熊果苷）和4-羟苯基-β-D-吡喃葡萄糖苷（β-熊果苷）。能加速黑色素的分解与排泄，减少皮肤色素沉积，祛除色斑和雀斑，同时杀菌、消炎的作用，主要用于高级化妆品的制备[2]。目前化妆品市场应用β-熊果苷，报道α-熊果苷的祛斑美白效果更佳[]。缓释乳膏α-熊果苷缓释乳膏本采用α-熊果苷制备熊果苷乳膏平均乳滴数正交设计乳化温度、乳化时间搅拌速度工艺，考察体外释放度熊果苷缓释乳膏 α-熊果苷 β-熊果苷 图 熊果苷结构式 JJ-1型磁力电动搅拌器江苏金坛市医疗仪器厂2695-2489型高效液相色谱美国Waters公司MiliQ型纯水仪美国MiliQ公司α-熊果苷（郑州荔诺生物科技有限公司，批号XG003，含量99.08）Na2S（国药集团化学试剂有限公司液体石蜡（杭州炼油厂）单异硬脂酸甘油酯（北京华美互利生物化工有限公司PEG-30二聚羟基硬脂酸酯北京华美互利生物化工有限公司乙二胺四乙酸EDTA，上海鼎国有限公司），尼泊金乙酯上海迈普科化学有限公司BALB/c小鼠，体重20~25）g，由提供方法与结果 熊果苷缓释乳膏制备采用油水