引用本文:付训忠, 邹杰, 尹珍, 武侠均, 崔沙沙, 杜雯雯, 罗雷.介孔二氧化硅吲哚美辛固体分散体复合物的制备及质量评价[J].西南大学学报(自然科学版),2019,41(8):74~81
【打印本页】   【HTML】   【下载PDF全文】   查看/发表评论  【EndNote】   【RefMan】   【BibTex】
←前一篇|后一篇→ 过刊浏览    高级检索
本文已被:浏览 45次   下载 47 本文二维码信息
码上扫一扫!
分享到: 微信 更多
介孔二氧化硅吲哚美辛固体分散体复合物的制备及质量评价
付训忠, 邹杰, 尹珍, 武侠均, 崔沙沙, 杜雯雯, 罗雷1,2,3,4
1. 重庆医药工业研究院有限责任公司, 重庆 400061;2. 西南大学 药学院, 重庆 400715;3. 河北省兽药监察所, 石家庄 050051;4. 重庆市第九人民医院, 重庆 400700
摘要:
以吲哚美辛(IMC)为模型药物,选用聚乙烯吡咯烷酮k30(PVPk30)与介孔二氧化硅(SiO2)Syloid SP53D作为共同载体材料,制备介孔二氧化硅固体分散体复合物,以提高固体分散体中主药的载药量和溶出度.采用溶剂蒸发法制备IMC-PVPk30固体分散体(简称IMC-PVPk30),浸没-溶剂蒸发法制备IMC-SiO2固体分散体(简称IMC-SiO2)和IMC-PVPk30-SiO2固体分散体复合物(简称IMC-PVPk30-SiO2);利用差示扫描量热法(DSC)、扫描电镜(SEM)等方法对其表征;采用紫外-可见分光光度法测定固体分散体及其复合物的载药量与溶出度.DSC显示,制备的两种固体分散体及其复合物中,IMC的熔点峰均消失,表明固体分散体制备成功;SEM显示,IMC-PVPk30结构呈不规则的块状,而IMC-SiO2和IMC-PVPk30-SiO2的粒径大小均匀,且IMC,PVPk30与介孔二氧化硅复合在一起;在不同pH的溶出介质中,IMC-SiO2和IMC-PVPk30-SiO2的溶出率均高于IMC-PVPk30,且IMC-PVPk30-SiO2的溶出率最高.得出介孔二氧化硅吲哚美辛固体分散体复合物(IMC-PVPk30-SiO2)具有较高的载药率和溶出率,为改善固体分散体的稳定性和进一步提高难溶性药物溶出度提出了新的思路和方法.
关键词:  固体分散体  介孔二氧化硅  吲哚美辛  溶出度  稳定性
DOI:10.13718/j.cnki.xdzk.2019.08.012
分类号:R944
基金项目:国家自然科学基金青年科学基金项目(81503009);重庆市自然科学基金项目(cstc2016jcyjA1687).
Preparation and Quality Evaluation of Mesoporous Silica Indomethacin Solid Dispersion Composite
FU Xun-zhong, ZOU Jie, YIN Zhen, WU Xia-jun, CUI Sha-sha, DU Wen-wen, LUO Lei1,2,3,4
1. Chongqing Pharmaceutical Industry Research Institute Co., Ltd., Nan'an District, Chongqing 400061, China;2. School of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China;3. Hebei Province Veterinary Drug Supervision Institute, Shijiazhuang 050051, China;4. Chongqing Ninth People's Hospital, Beibei District, Chongqing 400700, China
Abstract:
Objective:To improve the drug loading efficiency, dissolution rate and stability of the main drug in the solid dispersion of mesoporous silica, polyvinylpyrrolidone k30 (PVPk30) and mesoporous SiO2 Syloid SP53D were applied as solid dispersion carriers for indomethacin (IMC) to prepare the drug-loaded mesoporous SiO2 solid dispersions (IMC-PVPk30-SiO2). Methods:IMC-PVPk30 solid dispersion was prepared with the solvent evaporation method; IMC-SiO2 solid dispersion and IMC-PVPk30-SiO2 solid dispersion composite were prepared with the immersion-solvent evaporation method. Then samples were characterized by differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The drug loading efficiency and dissolution rate of the solid dispersion and its complex were determined by ultraviolet-visible spectrophotometry. Results:The results of DSC showed that the melting peak of IMC disappeared practically between IMC-PVPk30, IMC-SiO2 and IMC-PVPk30-SiO2, suggesting that IMC existed in the amorphous state in these samples and the solid dispersions were prepared successfully. SEM showed that the IMC-PVPk30 structure was irregularly blocked, and the IMC-SiO2 and IMC-PVPk30-SiO2 had a nearly identical particle size. Compared with the mesoporous SiO2 materials, the particle size increased slightly, which indicated that IMC may be distributed on both the outer surface and the inner channel of SiO2. The dissolution determination experiment showed that the dissolution rates of IMC-SiO2 and IMC-PVPk30-SiO2 were higher than those of IMC-PVPk30 within 2 hours. Conclusion:The IMC silica solid dispersion composite (IMC-PVPk30-SiO2) has a high drug loading efficiency and dissolution rate, and it is expected to be a novel drug delivery system for poorly soluble drugs with better bioavailability.
Key words:  solid dispersion  mesoporous silica  indomethacine  dissolution rate  stability
手机扫一扫看