• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
ZHU Li, YANG Miao, ZHANG Qiang, KE Xue, WU Junlian. Preparation of posaconazole solid dispersion via hot-melt extrusion and preliminary evaluation in vitro[J]. Journal of China Pharmaceutical University, 2015, 46(3): 309-315. DOI: 10.11665/j.issn.1000-5048.20150308
Citation: ZHU Li, YANG Miao, ZHANG Qiang, KE Xue, WU Junlian. Preparation of posaconazole solid dispersion via hot-melt extrusion and preliminary evaluation in vitro[J]. Journal of China Pharmaceutical University, 2015, 46(3): 309-315. DOI: 10.11665/j.issn.1000-5048.20150308
shu

Preparation of posaconazole solid dispersion via hot-melt extrusion and preliminary evaluation in vitro

More Information
    Graphical Abstract
    • Abstract
  • Hot-melt extrusion technology was used to prepare solid dispersion of posaconazole for improving its dissolution. Solubility parameter, glass transition temperature and melting method were utilized to screen polymers. Using KollidonVA64, Soluplus, Eudragit L100 and combined carrier KollidonVA64-Eudragit L100 as polymer carrier, solid dispersion was prepared by hot-melt extrusion technology and characterized by drug dissolution. The formulation and process factor affecting dissolution were studied. The state of posaconazole in solid dispersion was characterized by differential scanning calorimetry and preliminary analysis of the stability was studied by influencing factors experiments. When using KollidonVA64-Eudragit L100(2 ∶8)as the carrier, 10 % triethyl citrate as the plasticizer and extrusion temperature of 150 °C, the dissolution of posaconazole was improved significantly. Drug was molecular or amorphous form in the carrier. Proportion of Eudragit L100 and KollidonVA64, temperature, drug loading and plasticizer influenced dissolution of posaconazole. Solid dispersion was stable for high temperature and strong light but sensitive to high humidity. Solid dispersion using hot-melt extrusion technology can significantly improve the dissolution of posaconazole.
    • FullText(HTML)
    • References (12)
  • [1]
    Mei D,Mei L,Liu M,et al.A review of posaconazole pharmacokinetic and pharmacodynamic studies[J].Clin Med J(临床药物治疗杂志),2014,12(3):15-22.
    [2]
    Li NN,Wang XQ.A review of posaconazole application in the treatment of invasive fungal disease[J].Chin J New Drugs(中国新药杂志),2014,23(23):2739-2746.
    [3]
    Fang LY,Wan J,Harris D.Oral pharmaceutical compositions in a solid dispersion comprising preferably posaconazole and HPMCAS:WO,588460A[P].2012-07-27[2015-01-22] .
    [4]
    Vo CL,Park C,Lee BJ.Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs[J].Eur J Pharm Biopharm,2013,85(3):799-813.
    [5]
    Yang R,Tang X,Huang HF.Hot-melt extrusion technique and its application in the drug delivery system[J].Chin J New Drugs(中国新药杂志),2007,16(4):279-283.
    [6]
    Sareen S,Mathew G,Joseph L.Improvement in solubility of poor water-soluble drugs by solid dispersion[J].Int J Pharm Investig,2012,2(1):12-17.
    [7]
    Liu X,Wen XG,Miao X,et al.Progress in the study on physical stability and anti-aging of soild dispersion[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(8):710-715.
    [8]
    Greenhalgh DJ,Williams AC,Timmins P,et al.Solubility parameters as predictors of miscibility in solid dispersions[J].J Pharm Sci,1999,88(11):1182-1190.
    [9]
    Chen YH,Wang QS,Ping QL,et al.Preparation of iguratimod solid dispersion via hot-melt extrusion and investigation of factors affecting dissolution profile[J].Chin Pharm J(中国药学杂志),2013,48(17):1272-1278.
    [10]
    Kim H,Likhari P,Kumari P,et al.High-performance liquid chromatographic analysis of the anti-fungal agent SCH 56592 in dog serum[J].J Chromatogr B Biomed Appl,2000,738(1):93-98.
    [11]
    Liu YS,Gao S,Ke X,et al.Recent research advances in solid dispersions of poor soluble drugs[J].Prog Pharm Sci(药学进展),2013,27(4):166-172.
    [12]
    Rumondor ACF,Stanford LA,Taylor LS.Effects of polymer type and storage relative humidity on the kinetics of felodipine crystallization from amorphous solid dispersions[J].Pharm Res,2009,26(12):2599-2606.
    • Related Articles

  • Related Articles

    [1]LIU Wenxin, LI Yan, YUAN Yaozuo, JIA Huanhuan, CHEN Minhui, ZHANG Jinlin. Analysis of the causes for abnormal dissolution of lansoprazole enteric-coated tablets by multiple techniques and different dimensions[J]. Journal of China Pharmaceutical University, 2024, 55(2): 224-229. DOI: 10.11665/j.issn.1000-5048.2023052401
    [2]CAO Jie, ZHU Zhiling, YUAN Meng, KE Xue. Effect and evaluation of microenvironment pH on dissolution behavior of indomethacin solid dispersion[J]. Journal of China Pharmaceutical University, 2019, 50(6): 686-693. DOI: 10.11665/j.issn.1000-5048.20190608
    [3]CHEN Jiahui, PING Qineng, SUN Minjie. Preparation of indomethacin-nicotinamide cocrystal by hot melt extrusion and its release in vitro[J]. Journal of China Pharmaceutical University, 2019, 50(2): 180-187. DOI: 10.11665/j.issn.1000-5048.20190208
    [4]ZHOU Shengyan, ZHANG Bowen, WEI Yuanfeng, QIAN Shuai, ZHANG Jianjun, GAO Yuan. Enhanced dissolution and oral bioavailability of baicalein by cocrystallization[J]. Journal of China Pharmaceutical University, 2018, 49(6): 682-688. DOI: 10.11665/j.issn.1000-5048.20180607
    [5]HONG Ziyue, SHI Shenyi, GUO Yushen, LIU Jianping. Preparation of itraconazole amorphous solid dispersion and preliminary evaluation in vitro[J]. Journal of China Pharmaceutical University, 2018, 49(2): 187-194. DOI: 10.11665/j.issn.1000-5048.20180208
    [6]Lü Wen-li, RONG Fei, PING Qi-neng. Preparation，dissolution and bioavailability of lycopene-Poloxamer 188 solid dispersion[J]. Journal of China Pharmaceutical University, 2009, 40(6): 514-518.
    [7]Characteristics of Enthalpy Change and Dissolution Improvement of Lornoxicam from Solid Dispersions[J]. Journal of China Pharmaceutical University, 2003, (5): 47-51.
    [8]Preparation of Oleanolic Acid Solid Dispersion Systems and Their Dissolution in vitro[J]. Journal of China Pharmaceutical University, 2003, (3): 42-45.
    [9]Study onthe Enhancement of Nitrendipine Dissolution by PEG6000 and Polysorbate 80[J]. Journal of China Pharmaceutical University, 2000, (1): 23-26.
    [10]HPLC Determination for Dissolution of Roxithromycin Capsules[J]. Journal of China Pharmaceutical University, 1997, (4): 59-61.

  • Cited by

    Periodical cited type(2)

    1. 宋伏洋，韩东，黄壮壮，李波，彭修娟，许刚，杨青，赵扬，王苗，李叶，朱勇乐，刘峰. 基于UPLC-Q-TOF-MS/MS技术及肝纤维化细胞模型的肝爽颗粒抗肝纤维化的药效成分筛选研究. 中南药学. 2024(05): 1157-1163 .
    2. 杨成，胡锴，韩鹏昭，宋军营，张振强，孙宁，王潘，谢治深，李中华. 天智颗粒的化学成分及入血成分定性分析. 中国药房. 2022(24): 2973-2977+2984 .

    Other cited types(2)

Catalog

    Get Citation
    XML
    Article views (1749) PDF downloads (1) Cited by(4)
    Turn off MathJax
    Article Contents
    Abstract
    References
    Related Articles

    Copyright © Journal of China Pharmaceutical University苏ICP备12050101号-2

    Address：24 Tongjia Lane, Nanjing City, Jiangsu Province （210009）Tel: 025-83271566E-mail: xuebao@cpu.edu.cn

    Supported by: Beijing Renhe Information Technology Co., Ltd.  Baidu Analytics

    Total visits：290288

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return