靛玉红固体分散体的制备及其体外溶出研究-第三军医大学学报.DOC

靛玉红固体分散体的制备及其体外溶出研究 蒋 苹，刘 芳，戴 青，陈 丹，刘松青 （400038 重庆，第三军医大学西南医院药剂科） [摘要] 目的 采用固体分散体技术制备难溶性药物靛玉红固体分散体，提高其体外溶出性能。方法 采用溶剂法制备靛玉红-聚乙烯吡咯烷酮（PVPK30）固体分散体；利用扫描电镜(SEM)和差示扫描量热法（DSC）鉴别药物在载体中的存在状态；以靛玉红的溶出百分量作为评价指标，研究靛玉红制成固体分散体后对溶出性能的影响。结果 扫描电镜和差示扫描量热法结果显示靛玉红在载体中以高度分散形式存在，制成固体分散体后药物的累计溶出度（36.93%）与原料药（4.81%）和物理混合物（11.42%）相比都有明显的提高。结论 靛玉红与聚乙烯吡咯烷酮（PVPK30）制成固体分散体，靛玉红的分散状态发生了改变，提高了其溶出性能。 [关键词] 靛玉红；聚乙烯吡咯烷酮；固体分散体；溶出性能 [中图法分类号] [文献标志码] A Preparation of indirubin solid dispersion and dissolution experiment in vitro Jiang Ping , Liu Fang, Dai Qing, Chen Dan, Liu Songqing (Department of Pharmacy, First Affiliated Hospital, Third Military Medical University, Chongqing, 400038, China) [Abstract] Objective To prepare the indirubin solid dispersion and to improve the dissolution of indirubin. Methods The solid dispersion was prepared with polyvinyplyrrolidone (PVPK30) as carrier by solvent evaporation, The status of indirubin existence in the dispersion form was studied by scanning electron microscope (SEM) and differential scanning calorimetry (DSC), the dissolution percentage of indirubin from the solid dispersion was used to evaluating the dissolution property. Results The SEM and DSC results showed that indirubin distributing in solid dispersion was in an amorphous state, the percentage of indirubin in solid dispersion(36.93%) was significately higher than indirubin power(4.81%) and physical mixture(11.42%) . Conclusion The dissolution of indirubin is improved by preparation of indirubin -PVPK-30 solid dispersion. [Key words] indirubin; polyvinylpyrrolidone; solid dispersion; dissolution 靛玉红是青黛、板蓝根、蓼蓝以及大青叶等植物的主要成分之一，可通过使白血病细胞肿胀、坏死而起到治疗慢性粒细胞白血病的作用[1]，具有疗效可靠，副作用小等特点[2]。但靛玉红为一双吲哚类药物，其分子为一刚性平面，导致靛玉红水溶性和脂溶性均较差，吸收不佳，临床应用受到一定限制[3]。固体分散体是将药物以分子、胶态、微晶或无定形状态高度分散于惰性载体中形成药物-载体的固体分散体系。具有增加药物的溶解性能、提高生物利用度的特点。目前，国内已将固体分散体广泛应用于制剂的研究[4-7]，故本课题采用固体分散技术制备难溶性药物靛玉红固体分散体并进行体外溶出实验，考察固体分散体增溶效果。 [通信作者] 刘松青，电话：（023E-mail: songqingliu@ 1 材料与方法 1.1 仪器与试药