Development and tableting of directly compressible powder from electrospun nanofibrous amorphous solid dispersion

被引:32
作者
Demuth, B. [1 ]
Farkas, A. [1 ]
Szabo, B. [1 ]
Balogh, A. [1 ]
Nagy, B. [2 ]
Vago, E. [3 ]
Vigh, T. [4 ]
Tinke, A. P. [5 ]
Kazsu, Z. [6 ]
Demeter, A. [6 ]
Bertels, J. [4 ]
Mensch, J. [4 ]
Van Dijck, A. [4 ]
Verreck, G. [4 ]
Van Assche, I. [4 ]
Marosi, G. [1 ]
Nagy, Z. K. [1 ]
机构
[1] Budapest Univ Technol & Econ BME, Dept Organ Chem & Technol, Muegyet Rkp 3, H-1111 Budapest, Hungary
[2] Quick2000 Ltd, Kabay Ju 29, H-4400 Tiszavasvari, Hungary
[3] Budapest Univ Technol & Econ BME, Dept Chem & Environm Proc Engn, Muegyet Rkp 3, H-1111 Budapest, Hungary
[4] Janssen R&D, Drug Prod Dev, Turnhoutseweg 30, B-2340 Beerse, Belgium
[5] Janssen R&D, Dept API Small Mol Dev Chem Technol & Proc Contro, Turnhoutseweg 30, B-2340 Beerse, Belgium
[6] Gedeon Richter Plc, Drug Polymorphism Res, Gyomroi Ut 30-32, H-1103 Budapest, Hungary
关键词
Nanoamorphous dispersion; Electrospinning; Stability; Tableting; Immediate release; SPRAY-DRYING FORMULATION; WATER-SOLUBLE DRUGS; DESIGN; ITRACONAZOLE; DISSOLUTION; FORMS;
D O I
10.1016/j.apt.2017.03.026
中图分类号
TQ [化学工业];
学科分类号
0817 ;
摘要
This work was carried out to explore the unknown area of converting non-woven fibres, prepared by high speed electrospinning, into a directly compressible blend by mixing with excipients. An experimental design, with independent variables of compression force and fillers fraction, was realized to investigate tabletability of electrospun material (EM) and to produce hard tablets with appropriate disintegration time. The models proved to be adequate; fitted to the results and predicted values well for the optimal tablet, which was found to be at 76.25% fillers fraction and 6 kN compression force. Besides standard characterizations, distribution of EM was investigated by Raman mapping and scanning electron microscopy revealing the propensity of EM to cover the surface of microcrystalline cellulose and not of mannitol. These analytical tools were also found to be useful at investigating the possible formation of the socalled gelling polymer network in tablets. Scanning electron microscopic pictures of tablets confirmed the maintenance of fibrous structure after compression. The moisture absorption of EM under increasing humidity was studied by dynamic vapour sorption measurement, which suggested good physical stability at 25 degrees C and 60% relative humidity (corroborated by modulated DSC). These results demonstrate the feasibility of a pharmaceutically acceptable downstream processing for EMs. (C) 2017 The Society of Powder Technology Japan. Published by Elsevier B.V. and The Society of Powder Technology Japan. All rights reserved.
引用
收藏
页码:1554 / 1563
页数:10
相关论文
共 44 条
[1]  
[Anonymous], EUR PAT
[2]  
[Anonymous], PHARM RES
[3]  
[Anonymous], AAPS ANN M EXP
[4]  
[Anonymous], MRS P, DOI [10.1557/PROC-1240-WW03-07, DOI 10.1557/PR0C-1240-WW03-07]
[5]   Can compression induce demixing in amorphous solid dispersions? A case study of naproxen-PVP K25 [J].
Ayenew, Zelalem ;
Paudel, Amrit ;
Van den Mooter, Guy .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2012, 81 (01) :207-213
[6]   In vitro dissolution-permeation evaluation of an electrospun cyclodextrin-based formulation of aripiprazole using μFlux™ [J].
Borbas, Eniko ;
Balogh, Attila ;
Bocz, Katalin ;
Mueller, Judit ;
Kiserdei, Eva ;
Vigh, Tamas ;
Sinko, Balint ;
Marosi, Attila ;
Halasz, Attila ;
Dohanyos, Zoltan ;
Szente, Lajos ;
Balogh, Gyoergy T. ;
Nagy, Zsombor K. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 491 (1-2) :180-189
[7]   Determining the critical relative humidity for moisture-induced phase transitions [J].
Burnett, DJ ;
Thielmann, F ;
Booth, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 287 (1-2) :123-133
[8]   PHARMACEUTICAL APPLICATIONS OF SOLID DISPERSION SYSTEMS [J].
CHIOU, WL ;
RIEGELMAN, S .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1971, 60 (09) :1281-+
[9]   Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning [J].
Demuth, B. ;
Farkas, A. ;
Pataki, H. ;
Balogh, A. ;
Szabo, B. ;
Borbas, E. ;
Soti, P. L. ;
Vigh, T. ;
Kiserdei, E. ;
Farkas, B. ;
Mensch, J. ;
Verreck, G. ;
Van Assche, I. ;
Marosi, G. ;
Nagy, Z. K. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 498 (1-2) :234-244
[10]   Downstream processing of polymer-based amorphous solid dispersions to generate tablet formulations [J].
Demuth, B. ;
Nagy, Z. K. ;
Balogh, A. ;
Vigh, T. ;
Marosi, G. ;
Verreck, G. ;
Van Assche, I. ;
Brewster, M. E. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 486 (1-2) :268-286