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Effects of thermal binders on chemical stabilities and tabletability of gabapentin granules prepared by twin-screw melt granulation.
Int J Pharm. 2019 Mar 25; 559:37-47.IJ

Abstract

The effect of thermal binders on the physicochemical properties of gabapentin, a thermally labile drug, in granules prepared using twin-screw melt granulation was investigated in this study. Hydroxypropyl cellulose (HPC), a thermoplastic high molecular-weight binder, was compared against conventional low molecular-weight semi-crystalline thermal binders PEG 8000 and Compritol. Both the chemical degradation and polymorph form change of gabapentin were analyzed. The effects of particle size and molecular weight of HPC on the properties of granules were also studied. To overcome the high melt viscosity of HPC, higher barrel temperatures and higher specific mechanical energy were required to attain suitable granules. As a result, higher levels of gabapentin degradant were observed in HPC-based formulations. However, gabapentin form change was not observed in all formulations. Smaller particle size and lower molecular weight of HPC led to faster granule growth. The tabletability of granules was insensitive to the variations in particle size and molecular weight of HPC. Gabapentin crystal size reduction, HPC size reduction, and HPC enrichment on granule surface were observed for HPC-based granules.

Authors+Show Affiliations

Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, A1920, Austin, TX 78712, USA.Division of Chemical Engineering, School of Engineering, the University of Texas at Austin, 200 E Dean Keeton St, Austin, TX 78712, USA.Foster Delivery Sciences, 45 Ridge Road, Putnam, CT 06260, USA.Department of Pharmaceutics, University of Minnesota, 308 SE Harvard St, Minneapolis, MN 55455, USA.Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, A1920, Austin, TX 78712, USA. Electronic address: feng.zhang@austin.utexas.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30660749

Citation

Kittikunakorn, Nada, et al. "Effects of Thermal Binders On Chemical Stabilities and Tabletability of Gabapentin Granules Prepared By Twin-screw Melt Granulation." International Journal of Pharmaceutics, vol. 559, 2019, pp. 37-47.
Kittikunakorn N, Koleng JJ, Listro T, et al. Effects of thermal binders on chemical stabilities and tabletability of gabapentin granules prepared by twin-screw melt granulation. Int J Pharm. 2019;559:37-47.
Kittikunakorn, N., Koleng, J. J., Listro, T., Calvin Sun, C., & Zhang, F. (2019). Effects of thermal binders on chemical stabilities and tabletability of gabapentin granules prepared by twin-screw melt granulation. International Journal of Pharmaceutics, 559, 37-47. https://doi.org/10.1016/j.ijpharm.2019.01.014
Kittikunakorn N, et al. Effects of Thermal Binders On Chemical Stabilities and Tabletability of Gabapentin Granules Prepared By Twin-screw Melt Granulation. Int J Pharm. 2019 Mar 25;559:37-47. PubMed PMID: 30660749.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of thermal binders on chemical stabilities and tabletability of gabapentin granules prepared by twin-screw melt granulation. AU - Kittikunakorn,Nada, AU - Koleng,J Joseph,3rd AU - Listro,Tony, AU - Calvin Sun,Changquan, AU - Zhang,Feng, Y1 - 2019/01/17/ PY - 2018/11/16/received PY - 2018/12/21/revised PY - 2019/01/11/accepted PY - 2019/1/21/pubmed PY - 2019/6/14/medline PY - 2019/1/21/entrez KW - Continuous manufacturing KW - Gabapentin KW - Hydroxypropyl cellulose KW - Tabletability KW - Twin-screw melt granulation SP - 37 EP - 47 JF - International journal of pharmaceutics JO - Int J Pharm VL - 559 N2 - The effect of thermal binders on the physicochemical properties of gabapentin, a thermally labile drug, in granules prepared using twin-screw melt granulation was investigated in this study. Hydroxypropyl cellulose (HPC), a thermoplastic high molecular-weight binder, was compared against conventional low molecular-weight semi-crystalline thermal binders PEG 8000 and Compritol. Both the chemical degradation and polymorph form change of gabapentin were analyzed. The effects of particle size and molecular weight of HPC on the properties of granules were also studied. To overcome the high melt viscosity of HPC, higher barrel temperatures and higher specific mechanical energy were required to attain suitable granules. As a result, higher levels of gabapentin degradant were observed in HPC-based formulations. However, gabapentin form change was not observed in all formulations. Smaller particle size and lower molecular weight of HPC led to faster granule growth. The tabletability of granules was insensitive to the variations in particle size and molecular weight of HPC. Gabapentin crystal size reduction, HPC size reduction, and HPC enrichment on granule surface were observed for HPC-based granules. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/30660749/Effects_of_thermal_binders_on_chemical_stabilities_and_tabletability_of_gabapentin_granules_prepared_by_twin_screw_melt_granulation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(19)30048-1 DB - PRIME DP - Unbound Medicine ER -