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Pharmaceutics 2018, 10(3), 114; https://doi.org/10.3390/pharmaceutics10030114

Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

1
Gedeon Richter Plc., Formulation R&D, Gyömrői Street 19-21, H-1103 Budapest, Hungary
2
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Budafoki út 8. 3, H-1103 Budapest, Hungary
*
Author to whom correspondence should be addressed.
Received: 15 June 2018 / Revised: 23 July 2018 / Accepted: 23 July 2018 / Published: 2 August 2018
(This article belongs to the Special Issue Electrospun and Electrosprayed Formulations for Drug Delivery)
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Abstract

Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was adopted as the fiber-forming polymer. Scanning electron microscopy (SEM) imaging was used to study the morphology of HSES and SNES samples. Different homogenization techniques were compared to maximize homogeneity: mixing in plastic bags and in a high-shear granulator resulting in low-shear mixing (LSM) and high-shear mixing (HSM). Drug content and homogeneity of the tablets were measured by UV-Vis spectrometry, the results revealed acceptably low-dose fluctuations especially with formulations homogenized with HSM. Sieve analysis was used on the final LSM and HSM powder mixtures in order to elucidate the observed differences between tablet homogeneity. Tablets containing drug-loaded electrospun fibers were also studied by Raman mapping demonstrating evenly distributed CAR within the corpus. View Full-Text
Keywords: carvedilol; poly (vinylpyrrolidone-co-vinyl acetate); high-speed electrospinning; high-shear mixing; homogenization; Raman mapping; sieve analysis carvedilol; poly (vinylpyrrolidone-co-vinyl acetate); high-speed electrospinning; high-shear mixing; homogenization; Raman mapping; sieve analysis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Fülöp, G.; Balogh, A.; Farkas, B.; Farkas, A.; Szabó, B.; Démuth, B.; Borbás, E.; Nagy, Z.K.; Marosi, G. Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation. Pharmaceutics 2018, 10, 114.

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