Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions

被引:45
作者
Soti, Peter Lajos [1 ]
Bocz, Katalin [1 ]
Pataki, Hajnalka [1 ]
Eke, Zsuzsanna [2 ]
Farkas, Attila [1 ]
Verreck, Geert [3 ]
Kiss, Eva [4 ]
Fekete, Pal [1 ,5 ]
Vigh, Tamas [1 ]
Wagner, Istvan [1 ]
Nagy, Zsombor K. [1 ]
Marosi, Gyoergy [1 ]
机构
[1] Budapest Univ Technol & Econ, Dept Organ Chem & Technol, H-1111 Budapest, Hungary
[2] Eotvos Lorand Univ, Joint Res & Training Lab Separat Tech, H-1117 Budapest, Hungary
[3] Janssen Res & Dev, Beerse, Belgium
[4] Eotvos Lorand Univ, Inst Chem, H-1117 Budapest, Hungary
[5] Meditop Pharmaceut Ltd, H-2097 Pilisborosjeno, Hungary
关键词
Electrospinning; Electroblowing; Spray drying; Raman mapping; Rapid dissolution; Itraconazole; ORAL BIOAVAILABILITY; DISSOLUTION RATE; WATER; DRUG; RELEASE; ENHANCEMENT; DELIVERY; SUPERSATURATION; SOLUBILITY; ABSORPTION;
D O I
10.1016/j.ijpharm.2015.07.076
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Three solvent based methods: spray drying (SD), electrospinning (ES) and air-assisted electrospinning (electroblowing; EB) were used to prepare solid dispersions of itraconazole and Eudragit E. Samples with the same API/polymer ratios were prepared in order to make the three technologies comparable. The structure and morphology of solid dispersions were identified by scanning electron microscopy and solid phase analytical methods such as, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Raman chemical mapping. Moreover, the residual organic solvents of the solid products were determined by static headspace-gas chromatography/mass spectroscopy measurements and the wettability of samples was characterized by contact angle measurement. The pharmaceutical performance of the three dispersion type, evaluated by dissolution tests, proved to be very similar. According to XRPD and DSC analyses, made after the production, all the solid dispersions were free of any API crystal clusters but about 10 wt% drug crystallinity was observed after three months of storage in the case of the SD samples in contrast to the samples produced by ES and EB in which the polymer matrix preserved the API in amorphous state. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:23 / 30
页数:8
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