• 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
GU Nian, SHENG Xinyi, QIN Chao, CHEN Jintuo, XU Siyuan, YIN Lifang. Preparation and gastrointestinal absorption kinetics of tacrolimus solid dispersion[J]. Journal of China Pharmaceutical University, 2016, 47(6): 694-701. DOI: 10.11665/j.issn.1000-5048.20160611
Citation: GU Nian, SHENG Xinyi, QIN Chao, CHEN Jintuo, XU Siyuan, YIN Lifang. Preparation and gastrointestinal absorption kinetics of tacrolimus solid dispersion[J]. Journal of China Pharmaceutical University, 2016, 47(6): 694-701. DOI: 10.11665/j.issn.1000-5048.20160611
shu

Preparation and gastrointestinal absorption kinetics of tacrolimus solid dispersion

More Information
    Graphical Abstract
    • Abstract
  • To prepare tacrolimus solid dispersion to increase the solubility and bioavailability of tacrolimus. Tacrolimus solid dispersions were prepared by different water-soluble carriers, which were evaluated by in vitro drug dissolutions to select the optimal formulation. The optimal tacrolimus solid dispersion was evaluated by scanning electron microscopy(SEM), X-ray diffraction(XRD)and differential scanning calorimetry(DSC), and its gastrointestinal absorption kinetics was studied in rats. The results showed that tacrolimus solid dispersion with HPMC E3 as carrier had the fastest dissolution rate. SEM, XRD and DSC studies indicated that tacrolimus was distributed within the carrier HPMC E3 in amorphous form. Gastrointestinal absorption experiments in rats demonstrated that the optimal formulation remarkably increased oral absorption of tacrolimus. These results demonstrate that a novel tacrolimus solid dispersion with HPMC E3 as carrier may be an advantageous dosage form of tacrolimus, boosting the solubility and absorption in gastrointestinal tract.
    • FullText(HTML)
    • References (8)
  • [1]
    Liu F, Wei JF, Meng L, et al. New development in macrolide immunosuppressant[J].Chin New Drugs J(中国新药杂志),2014,22(1):61-66.
    [2]
    Liu YS,Gao S,Ke X,et al.Recent research advances in solid dispersions of poorly soluble drugs[J].Prog Pharm Sci(药学进展),2013,37(4):166-173.
    [3]
    Yan F,Ke X,Ping QN,et al.Preparation of baicalein solid dispersions and oral bioavailability in rats[J].J China Pharm Univ(中国药科大学学报),2008,39(5):406-411.
    [4]
    Zhang Q, Zhang MX, Zhang J, et al. Studies on the intestinal absorption kinetics of tacrolimus in rats[J].Chin Hosp Pharm J(中国医院药学杂志),2010,30(8):639-642.
    [5]
    Veloxis Pharma Inc.Modified release tacrolimus compositions:CN,1859910A[P].2006-11-08[2016-03-11] .
    [6]
    Arik D, Brady T, Gordon L, et al. Segmental-dependent membrane permeability along the intestine following oral drug administration:evaluation of a triple single-pass intestinal perfusion(TSPIP)approach in the rat[J].Eur J Pharm Sci,2009,36:320-329.
    [7]
    Ying J,Lyu Y,Du GH.New development in amorphous drug[J].Acta Pharm Sin(药学学报),2009,44(5):443-448.
    [8]
    Astellas Pharma Inc.Tacrolimus sustained release pharmaceutical composition:EP,2119442A[P].2009-11-18[2016-03-11] .
    • Related Articles

  • Related Articles

    [1]SUN Liting, ZHANG Weiguo, TONG Yue. Research progress on targeted protein S-palmitoylation modification in T cell immunotherapy[J]. Journal of China Pharmaceutical University, 2024, 55(1): 45-52. DOI: 10.11665/j.issn.1000-5048.2023112903
    [2]WANG Zhenghao, GAO Yafeng, ZHANG Lianjun, LIU Chang. Research progress of T cell anti-tumor function regulated by endoplasmic reticulum stress[J]. Journal of China Pharmaceutical University, 2022, 53(5): 518-524. DOI: 10.11665/j.issn.1000-5048.20220502
    [3]LUO Jianhua, XIA Xuefei, YAO Wenbing, TIAN Hong. Design and antitumor effect of nitrated T helper cell epitope vaccine CD47-NitraTh[J]. Journal of China Pharmaceutical University, 2019, 50(5): 614-621. DOI: 10.11665/j.issn.1000-5048.20190516
    [4]NING Hongyu, JIANG Tao, ZHANG Rui, HE Yu, YAO Wenbing, TIAN Hong. Effects of immunogenic HER2 on the differentiation of T-cell in mouse[J]. Journal of China Pharmaceutical University, 2018, 49(1): 102-108. DOI: 10.11665/j.issn.1000-5048.20180115
    [5]CHEN Yucong, GUO Wei, LEI Wen, GE Yaoyao, XUE Wenyao, LI Qianwen, GAO Xiangdong. Optimization of in vitro human follicular helper T cell differentiation condition[J]. Journal of China Pharmaceutical University, 2017, 48(6): 733-737. DOI: 10.11665/j.issn.1000-5048.20170616
    [6]WANG Chen, GUO Wei, WANG Xin, YU Dongmei, WANG Yuheng, YAO Wenbing. Condition of human Th17 cell differentiation induced in vitro[J]. Journal of China Pharmaceutical University, 2016, 47(1): 106-111. DOI: 10.11665/j.issn.1000-5048.20160116
    [7]CUI Ye, WANG Lu, SUN Qiong, ZHANG Can. In vitro evaluation of cationic liposomes prepared with oligopeptide-based lipids for plasmid DNA delivery[J]. Journal of China Pharmaceutical University, 2013, 44(4): 328-333. DOI: 10.11665/j.issn.1000-5048.20130408
    [8]Preparation of aFGF liposomes and their release behavior in vitro[J]. Journal of China Pharmaceutical University, 2010, 41(3): 248-252.
    [9]Effects of Epimedium Pubescens Flavonoids on Osteoblasts in vitro[J]. Journal of China Pharmaceutical University, 2002, (1): 50-52.
    [10]Study on the Preparation and Properties in Vitro of Fluorouracil Albumin Microspheres[J]. Journal of China Pharmaceutical University, 1999, (5): 353-356.

Catalog

    Get Citation
    PDF
    XML
    Article views (831) PDF downloads (2016) Cited by()
    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：300501

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return