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Vibrational spectroscopy to support the link between rheology and continuous twin-screw melt granulation on molecular level: A case study.
Eur J Pharm Biopharm. 2016 Jun; 103:127-135.EJ

Abstract

Twin screw hot melt granulation (TSHMG) is an innovative and continuous drug formulation process allowing granulation of moisture sensitive drugs. However, due to the lack of experience and in-depth process understanding, this technique is not yet widely used. During the TSHMG process, the microstructure of the granules is generated and modified and strongly depends on the flow behavior of the material. Hence, rheology might be a suitable tool to simulate and examine this process. However, chemical interactions of the material are influencing the physical properties leading to the microstructure. In this research project it is spectroscopically investigated whether the heat applied in a rheometer induces the same molecular effects as these occurring during TSHMG of the model formulation caffeine anhydrous/Soluplus®. Hence, it is evaluated whether rheology can be used as a simulation tool to improve the understanding of the material behavior at molecular level during continuous melt granulation. Therefore, in-line Raman spectroscopy is executed during TSHMG and in situ Fourier Transform Infra-red (FTIR) during oscillatory rheological experiments. The results from the in-line Raman monitoring revealed polymorph transition of caffeine anhydrous during twin screw melt granulation with Soluplus® which is stimulated depending on the binder concentration and/or granulation temperature. A correlation was seen between the FTIR spectra obtained during the rheological temperature ramp and the in-line collected Raman spectra during the melt granulation runs. The polymorphic conversion of caffeine anhydrous could be detected in the same temperature range with both techniques, proving the comparability of plate-plate rheometry and hot melt granulation (HMG) for this case with the used parameter settings. Process simulation using rheology combined with in situ FTIR seems a promising approach to increase process understanding and to facilitate binder and parameter selection for TSHMG.

Authors+Show Affiliations

Laboratory of Pharmaceutical Process Analytical Technology, Department of Pharmaceutical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium. Electronic address: Tinne.Monteyne@UGent.be.Laboratory of Pharmaceutical Process Analytical Technology, Department of Pharmaceutical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium. Electronic address: Liza.Heeze@Ugent.be.Center for Material Characterization of Products, Thermo Fisher, Dieselstrasse 4, 76227 Karlsruhe, Germany. Electronic address: Klaus.Oldoerp@Thermofisher.com.Laboratory of Pharmaceutical Technology, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium. Electronic address: Chris.Vervaet@Ugent.be.Laboratory of Pharmaceutical Technology, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium. Electronic address: JeanPaul.Remon@Ugent.be.Laboratory of Pharmaceutical Process Analytical Technology, Department of Pharmaceutical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium. Electronic address: Thomas.Debeer@Ugent.be.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27040975

Citation

Monteyne, Tinne, et al. "Vibrational Spectroscopy to Support the Link Between Rheology and Continuous Twin-screw Melt Granulation On Molecular Level: a Case Study." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 103, 2016, pp. 127-135.
Monteyne T, Heeze L, Oldörp K, et al. Vibrational spectroscopy to support the link between rheology and continuous twin-screw melt granulation on molecular level: A case study. Eur J Pharm Biopharm. 2016;103:127-135.
Monteyne, T., Heeze, L., Oldörp, K., Vervaet, C., Remon, J. P., & De Beer, T. (2016). Vibrational spectroscopy to support the link between rheology and continuous twin-screw melt granulation on molecular level: A case study. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 103, 127-135. https://doi.org/10.1016/j.ejpb.2016.03.030
Monteyne T, et al. Vibrational Spectroscopy to Support the Link Between Rheology and Continuous Twin-screw Melt Granulation On Molecular Level: a Case Study. Eur J Pharm Biopharm. 2016;103:127-135. PubMed PMID: 27040975.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Vibrational spectroscopy to support the link between rheology and continuous twin-screw melt granulation on molecular level: A case study. AU - Monteyne,Tinne, AU - Heeze,Liza, AU - Oldörp,Klaus, AU - Vervaet,Chris, AU - Remon,Jean-Paul, AU - De Beer,Thomas, Y1 - 2016/04/01/ PY - 2016/01/13/received PY - 2016/03/18/revised PY - 2016/03/29/accepted PY - 2016/4/5/entrez PY - 2016/4/5/pubmed PY - 2017/2/28/medline KW - Caffeine anhydrous KW - Continuous twin-screw melt granulation KW - Polymorphism KW - Rheology KW - Vibrational spectroscopy SP - 127 EP - 135 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 103 N2 - Twin screw hot melt granulation (TSHMG) is an innovative and continuous drug formulation process allowing granulation of moisture sensitive drugs. However, due to the lack of experience and in-depth process understanding, this technique is not yet widely used. During the TSHMG process, the microstructure of the granules is generated and modified and strongly depends on the flow behavior of the material. Hence, rheology might be a suitable tool to simulate and examine this process. However, chemical interactions of the material are influencing the physical properties leading to the microstructure. In this research project it is spectroscopically investigated whether the heat applied in a rheometer induces the same molecular effects as these occurring during TSHMG of the model formulation caffeine anhydrous/Soluplus®. Hence, it is evaluated whether rheology can be used as a simulation tool to improve the understanding of the material behavior at molecular level during continuous melt granulation. Therefore, in-line Raman spectroscopy is executed during TSHMG and in situ Fourier Transform Infra-red (FTIR) during oscillatory rheological experiments. The results from the in-line Raman monitoring revealed polymorph transition of caffeine anhydrous during twin screw melt granulation with Soluplus® which is stimulated depending on the binder concentration and/or granulation temperature. A correlation was seen between the FTIR spectra obtained during the rheological temperature ramp and the in-line collected Raman spectra during the melt granulation runs. The polymorphic conversion of caffeine anhydrous could be detected in the same temperature range with both techniques, proving the comparability of plate-plate rheometry and hot melt granulation (HMG) for this case with the used parameter settings. Process simulation using rheology combined with in situ FTIR seems a promising approach to increase process understanding and to facilitate binder and parameter selection for TSHMG. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/27040975/Vibrational_spectroscopy_to_support_the_link_between_rheology_and_continuous_twin_screw_melt_granulation_on_molecular_level:_A_case_study_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(16)30120-5 DB - PRIME DP - Unbound Medicine ER -