Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

被引:33
作者
Szabo, E. [1 ]
Demuth, B. [1 ]
Nagy, B. [1 ,4 ]
Molnar, K. [2 ,3 ]
Farkas, A. [1 ]
Szabo, B. [1 ]
Balogh, A. [1 ]
Hirsch, E. [1 ]
Nagy, B. [1 ,4 ]
Marosi, G. [1 ]
Nagy, Z. K. [1 ]
机构
[1] Budapest Univ Technol & Econ, Fac Chem Technol & Biotechnol, Dept Organ Chem & Technol, Muegyetem Rkp 3, H-1111 Budapest, Hungary
[2] Budapest Univ Technol & Econ, Dept Polymer Engn, Fac Mech Engn, Muegyetem Rkp 3, H-1111 Budapest, Hungary
[3] MTA BME Res Grp Composite Sci & Technol, Muegyetem Rkp 3, H-1111 Budapest, Hungary
[4] Quick 2000 Ltd, Kabay J 29, H-4400 Tiszavasvari, Hungary
来源
EXPRESS POLYMER LETTERS | 2018年 / 12卷 / 05期
关键词
industrial applications; high speed electrospinning; amorphous solid dispersions; tableting; continuous processing technologies; AMORPHOUS SOLID DISPERSIONS; WATER-SOLUBLE DRUGS; PROCESS ANALYTICAL TECHNOLOGY; DOSAGE FORMS; DISSOLUTION ENHANCEMENT; ORAL BIOAVAILABILITY; NIR SPECTROSCOPY; MELT EXTRUSION; IN-LINE; NANOFIBERS;
D O I
10.3144/expresspolymlett.2018.37
中图分类号
O63 [高分子化学(高聚物)];
学科分类号
070305 ; 080501 ; 081704 ;
摘要
Polymer-based electrospun amorphous solid dispersions (ASDs) were prepared and investigated from pharmaceutical application point of view. Spironolactone (SPIR) was used as model drug mixed in various concentrations with polymers suitable for fibre formation, such as vinylpyrrolidone-vinyl acetate copolymer, polyvinylpyrrolidone K30 and hydroxypropyl methylcellulose. Single needle electrospinning was applied at first for screening the composition of the prepared ASDs. Scaling-up the selected polymer-drug combination was accomplished by high speed electrospinning, the productivity of which enabled investigation of downstream processing to generate tablet formulation. The steps of a potential continuous production line (fibre collection, grinding, feeding and tableting) proved to be feasible with the electrospun ASD without any sign of crystallization. If crystalline drug was added into the ASD containing tablets as impurity strictly monotonous decrease of drug dissolution was observed in the function of the crystalline drug content. The capabilities of the non-destructive Raman and near-infrared spectroscopies, as fast quality assurance tools, were compared to each other in quantifying of crystalline SPIR content in the prepared tablets.
引用
收藏
页码:436 / 451
页数:16
相关论文
共 60 条
  • [1] A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY
    AMIDON, GL
    LENNERNAS, H
    SHAH, VP
    CRISON, JR
    [J]. PHARMACEUTICAL RESEARCH, 1995, 12 (03) : 413 - 420
  • [2] Balboni M.L., 2003, Pharmaceutical Technology, V27, P54
  • [3] Controlled-release solid dispersions of Eudragit® FS 100 and poorly soluble spironolactone prepared by electrospinning and melt extrusion
    Balogh, Attila
    Farkas, Balazs
    Domokos, Andras
    Farkas, Attila
    Demuth, Balazs
    Borbas, Enik
    Nagy, Brigitta
    Marosi, Gyorgy
    Nagy, Zsombor Kristof
    [J]. EUROPEAN POLYMER JOURNAL, 2017, 95 : 406 - 417
  • [4] AC and DC electrospinning of hydroxypropylmethylcellulose with polyethylene oxides as secondary polymer for improved drug dissolution
    Balogh, Attila
    Farkas, Balazs
    Verreck, Geert
    Mensch, Jurgen
    Borbas, Eniko
    Nagy, Brigitta
    Marosi, Gyorgy
    Nagy, Zsombor Kristof
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 505 (1-2) : 159 - 166
  • [5] Melt-Blown and Electrospun Drug-Loaded Polymer Fiber Mats for Dissolution Enhancement: A Comparative Study
    Balogh, Attila
    Farkas, Balazs
    Farago, Kornel
    Farkas, Attila
    Wagner, Istvan
    Van Assche, Ivo
    Verreck, Geert
    Nagy, Zsombor K.
    Marosi, Gyoergy
    [J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 104 (05) : 1767 - 1776
  • [6] Investigation and Mathematical Description of the Real Driving Force of Passive Transport of Drug Molecules from Supersaturated Solutions
    Borbas, Eniko
    Sinko, Balint
    Tsinman, Oksana
    Tsinman, Konstantin
    Kiserdei, Eva
    Demuth, Balazs
    Balogh, Attila
    Bodak, Brigitta
    Domokos, Andras
    Dargo, Gergo
    Balogh, Gyorgy T.
    Nagy, Zsombor K.
    [J]. MOLECULAR PHARMACEUTICS, 2016, 13 (11) : 3816 - 3826
  • [7] Future manufacturing approaches in the chemical and pharmaceutical industry
    Buchholz, Sigurd
    [J]. CHEMICAL ENGINEERING AND PROCESSING-PROCESS INTENSIFICATION, 2010, 49 (10) : 993 - 995
  • [8] Carr R.L., 1965, Chem. Eng, V72, P163, DOI DOI 10.1016/J.JAEROSCI.2007.10.003
  • [9] Electrospun poly lactic acid (PLA) fibres: Effect of different solvent systems on fibre morphology and diameter
    Casasola, R.
    Thomas, N. L.
    Trybala, A.
    Georgiadou, S.
    [J]. POLYMER, 2014, 55 (18) : 4728 - 4737
  • [10] Development, validation and comparison of near infrared and Raman spectroscopic methods for fast characterization of tablets with amlodipine and valsartan
    Casian, Tibor
    Reznek, Andra
    Vonica-Gligor, Andreea Loredana
    Van Renterghem, Jeroen
    De Beer, Thomas
    Tomuta, Ioan
    [J]. TALANTA, 2017, 167 : 333 - 343