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Physicochemical changes and chemical degradation of gliclazide during twin-screw melt granulation.
Int J Pharm. 2022 May 10; 619:121702.IJ

Abstract

Using a miscible model formulation consisting of 80% gliclazide (GLZ) and 20% hydroxypropyl cellulose, we investigate how the twin-screw melt granulation process affects the chemical stability and process-induced physicochemical changes of the drug. No degradation was observed in the conveying section that leads to kneading element. Approximately 1/3 of the GLZ degradant was generated at the kneading section, while the remaining 2/3 was generated in the conveying section post-kneading and during cooling outside the barrel. A strong correlation was observed between the overall degradation and the temperature of the granules at the barrel exit. In the kneading section, the degradant content correlates best with the specific mechanical energy. With higher specific mechanical energies, the size of the GLZ crystals was reduced further, resulting in more surface defects. In the section post-kneading element, GLZ degradation correlates best with the granule temperature measured at the kneading section. This knowledge of drug degradation during twin-screw melt granulation can be used to develop processing strategies to maintain drug stability during and post processing.

Authors+Show Affiliations

Division of Molecular Pharmaceutics and Drug Delivery, the University of Texas at Austin, Austin, TX, United States.Department of Pharmaceutics, University of Minnesota, Minneapolis, MN, United States.Division of Molecular Pharmaceutics and Drug Delivery, the University of Texas at Austin, Austin, TX, United States.Pharmaceutical Technology, Ashland Specialty Ingredients, Wilmington, DE, United States.Pharmaceutical Technology, Ashland Specialty Ingredients, Wilmington, DE, United States.Pharmaceutical Technology, Ashland Specialty Ingredients, Wilmington, DE, United States.Pharmaceutical Technology, Ashland Specialty Ingredients, Wilmington, DE, United States.Pharmaceutical Technology, Ashland Specialty Ingredients, Wilmington, DE, United States.Division of Molecular Pharmaceutics and Drug Delivery, the University of Texas at Austin, Austin, TX, United States. Electronic address: feng.zhang@austin.utexas.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

35341908

Citation

Liu, Tongzhou, et al. "Physicochemical Changes and Chemical Degradation of Gliclazide During Twin-screw Melt Granulation." International Journal of Pharmaceutics, vol. 619, 2022, p. 121702.
Liu T, Kaur N, Chen B, et al. Physicochemical changes and chemical degradation of gliclazide during twin-screw melt granulation. Int J Pharm. 2022;619:121702.
Liu, T., Kaur, N., Chen, B., Phillips, B., Chang, S. Y., Yang, F., Bi, V., Durig, T., & Zhang, F. (2022). Physicochemical changes and chemical degradation of gliclazide during twin-screw melt granulation. International Journal of Pharmaceutics, 619, 121702. https://doi.org/10.1016/j.ijpharm.2022.121702
Liu T, et al. Physicochemical Changes and Chemical Degradation of Gliclazide During Twin-screw Melt Granulation. Int J Pharm. 2022 May 10;619:121702. PubMed PMID: 35341908.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical changes and chemical degradation of gliclazide during twin-screw melt granulation. AU - Liu,Tongzhou, AU - Kaur,Navpreet, AU - Chen,Beibei, AU - Phillips,Brian, AU - Chang,Shao-Yu, AU - Yang,Fengyuan, AU - Bi,Vivian, AU - Durig,Thomas, AU - Zhang,Feng, Y1 - 2022/03/25/ PY - 2022/02/10/received PY - 2022/03/20/revised PY - 2022/03/22/accepted PY - 2022/3/29/pubmed PY - 2022/4/29/medline PY - 2022/3/28/entrez SP - 121702 EP - 121702 JF - International journal of pharmaceutics JO - Int J Pharm VL - 619 N2 - Using a miscible model formulation consisting of 80% gliclazide (GLZ) and 20% hydroxypropyl cellulose, we investigate how the twin-screw melt granulation process affects the chemical stability and process-induced physicochemical changes of the drug. No degradation was observed in the conveying section that leads to kneading element. Approximately 1/3 of the GLZ degradant was generated at the kneading section, while the remaining 2/3 was generated in the conveying section post-kneading and during cooling outside the barrel. A strong correlation was observed between the overall degradation and the temperature of the granules at the barrel exit. In the kneading section, the degradant content correlates best with the specific mechanical energy. With higher specific mechanical energies, the size of the GLZ crystals was reduced further, resulting in more surface defects. In the section post-kneading element, GLZ degradation correlates best with the granule temperature measured at the kneading section. This knowledge of drug degradation during twin-screw melt granulation can be used to develop processing strategies to maintain drug stability during and post processing. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/35341908/Physicochemical_changes_and_chemical_degradation_of_gliclazide_during_twin_screw_melt_granulation_ DB - PRIME DP - Unbound Medicine ER -