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

PAGE 1 [收稿日期] [第一作者]杨人泽，副主任药师，学士，从事医院药学研究，TelE-mail：yrz626@163.com [通讯作者]*严金玲，主任药师，学士，从事医院药学研究，TelE-mail：gzyanjinling@163.com 熊果苷缓释乳膏的制备工艺优化及体外释放度考察 杨人泽[1]，丁乐[2]，严金玲[1]* （1赣南医学院第一附属医院，江西 赣州 341000 2赣州市妇幼保健院 341000 江西赣州） [摘要]目的：优化熊果苷缓释乳膏的制备工艺，并考察其体外释放度。方法：以平均乳滴数和乳膏均匀度为综合评价指标，选取乳化温度、乳化时间及搅拌速度为考察因素，采用正交设计优化熊果苷缓释乳膏的制备工艺；采用HPLC测定熊果苷含量，考察熊果苷缓释乳膏的体外释放度及稳定性。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。制得的熊果苷缓释乳膏具有明显的缓释作用和良好的稳定性。结论：优选的制备工艺稳定可行，所得样品具有良好的缓释效果，适用于熊果苷缓释乳膏的工业化生产。 [关键词] 熊果苷；制备工艺；缓释制剂；乳膏；稳定性 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 [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 熊果苷根据结构不同可分为α型和β型，均具有较好的美白效果，其化学名分别为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）[1]。其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，同时具有杀菌、消炎的作用，主要用于高级化妆品的制备[2-3]。目前化妆品市场中多应用β-熊果苷，但有报道称α-熊果苷的祛斑美白效果更佳[4-5]。制备缓释乳膏能延缓有效物质的释放, 延长有效物质的作用时间，从而减少使用次数，提高美白效果。目前市场上还未出现α-熊果苷的缓释乳膏。本课题组拟采用α-熊果苷制备熊果苷缓释乳膏。本试验以平均乳滴数