Hot-melt extrusion process impact on polymer choice of glyburide solid dispersions: The effect of wettability and dissolution

被引:29
|
作者
Alshafiee, Maen [1 ]
Aljammal, Mohammad K. [1 ]
Markl, Daniel [2 ]
Ward, Adam [1 ]
Walton, Karl [3 ]
Blunt, Liam [3 ]
Korde, Sachin [4 ]
Pagire, Sudhir K. [4 ]
Kelly, Adrian L. [4 ,5 ]
Paradkar, Anant [4 ]
Conway, Barbara R. [1 ]
Asare-Addo, Kofi [1 ]
机构
[1] Univ Huddersfield, Dept Pharm, Huddersfield HD1 3DH, W Yorkshire, England
[2] Univ Strathclyde, Strathclyde Inst Pharm & Biomed Sci, 161 Cathedral St, Glasgow G4 0RE, Lanark, Scotland
[3] Univ Huddersfield, EPSRC Future Metrol Hub, Huddersfield HD1 3DH, W Yorkshire, England
[4] Univ Bradford, Ctr Pharmaceut Engn Sci, Bradford, W Yorkshire, England
[5] Univ Bradford, IRC Polymer Sci & Technol, Bradford, W Yorkshire, England
基金
英国工程与自然科学研究理事会;
关键词
Solid dispersion; Glyburide; Hot-melt extrusion; Contact angle; Soluplus (R); Kollidon (R) VA64; WATER-SOLUBLE DRUGS; GLUCOSAMINE HCL; STATE BEHAVIORS; FORMULATION; RELEASE; BIOAVAILABILITY; POLYSACCHARIDE; LYOPHILIZATION; MISCIBILITY; PIROXICAM;
D O I
10.1016/j.ijpharm.2019.01.038
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to evaluate the choice of polymer and polymer level on the performance of the microstructure and wettability of hot-melt extruded solid dispersion of Glyburide (Gly) as a model drug. The produced solid dispersion were characterised using scanning electron microscopy (SEM), image analysis using a focus variation instrument (FVI), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Xray microtomography (X mu T), dynamic contact angle measurement and dissolution analysis using biorelevant dissolution media (FASSIF). SEM and focus variation analysis showed that the microstructure and surface morphology was significantly different between samples produced. This was confirmed by further analysis using X mu T which showed that an increase in polymer content brought about a decrease in the porosity of the hot-melt extruded dispersions. DSC suggested complete amorphorisation of Gly whereas XRPD suggested incomplete amorphorisation. The static and dynamic contact angle measurement correlated with the dissolution studies using FASSIF media indicating that the initial liquid imbibition process as captured by the dynamic contact angle directly affects the dissolution performance.
引用
收藏
页码:245 / 254
页数:10
相关论文
共 50 条
  • [41] Effect of plasticizers on manufacturing ritonavir/copovidone solid dispersions via hot-melt extrusion: Preformulation, physicochemical characterization, and pharmacokinetics in rats
    Zhao, Yanna
    Xie, Xuemei
    Zhao, Yuping
    Gao, Yan
    Cai, Chang
    Zhang, Qinxiu
    Ding, Zhuang
    Fan, Zhiping
    Zhang, Huaizhen
    Liu, Min
    Han, Jun
    EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2019, 127 : 60 - 70
  • [42] Amorphous-state characterization of efavirenz-polymer hot-melt extrusion systems for dissolution enhancement
    Sathigari, Sateesh Kumar
    Radhakrishnan, Vinod K.
    Davis, Virginia A.
    Parsons, Daniel L.
    Babu, R. Jayachandra
    JOURNAL OF PHARMACEUTICAL SCIENCES, 2012, 101 (09) : 3456 - 3464
  • [43] Upscaling of the hot-melt extrusion process: Comparison between laboratory scale and pilot scale production of solid dispersions with miconazole and Kollicoat® IR
    Guns, Sandra
    Mathot, Vincent
    Martens, Johan A.
    Van den Mooter, Guy
    EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2012, 81 (03) : 674 - 682
  • [44] Rheological Characterization of Molten Polymer-Drug Dispersions as a Predictive Tool for Pharmaceutical Hot-Melt Extrusion Processability
    Van Renterghem, Jeroen
    Vervaet, Chris
    De Beer, Thomas
    PHARMACEUTICAL RESEARCH, 2017, 34 (11) : 2312 - 2321
  • [45] Rheological Characterization of Molten Polymer-Drug Dispersions as a Predictive Tool for Pharmaceutical Hot-Melt Extrusion Processability
    Jeroen Van Renterghem
    Chris Vervaet
    Thomas De Beer
    Pharmaceutical Research, 2017, 34 : 2312 - 2321
  • [46] The applications of machine learning to predict the forming of chemically stable amorphous solid dispersions prepared by hot-melt extrusion
    Jiang, Junhuang
    Lu, Anqi
    Ma, Xiangyu
    Ouyang, Defang
    Williams III, Robert O.
    INTERNATIONAL JOURNAL OF PHARMACEUTICS-X, 2023, 5
  • [47] The Effect of Cooling on the Degree of Crystallinity, Solid-State Properties, and Dissolution Rate of Multi-Component Hot-Melt Extruded Solid Dispersions
    Hurley, Dean
    Davis, Mark
    Walker, Gavin M.
    Lyons, John G.
    Higginbotham, Clement L.
    PHARMACEUTICS, 2020, 12 (03)
  • [48] Production of spherical pellets by a hot-melt extrusion and spheronization process
    Young, CR
    Koleng, JJ
    McGinity, JW
    INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 242 (1-2) : 87 - 92
  • [49] Process monitoring and visualization solutions for hot-melt extrusion: a review
    Saerens, Lien
    Vervaet, Chris
    Remon, Jean Paul
    De Beer, Thomas
    JOURNAL OF PHARMACY AND PHARMACOLOGY, 2014, 66 (02) : 180 - 203
  • [50] Development of amorphous solid dispersions of cannabidiol: Influence of the carrier, the hot-melt extrusion parameters and the use of a crystallization inhibitor
    Jennotte, Olivier
    Koch, Nathan
    Lechanteur, Anna
    Evrard, Brigitte
    JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2022, 71