Tags

Type your tag names separated by a space and hit enter

Effect of screw profile and processing conditions on physical transformation and chemical degradation of gabapentin during twin-screw melt granulation.
Eur J Pharm Sci. 2019 Apr 01; 131:243-253.EJ

Abstract

Twin-screw melt granulation (TSMG) was applied to process a powder blend consisting of 80% gabapentin (GABA) and 20% hydroxypropyl cellulose. The effect of screw profile and processing conditions on the process-induced transformation and chemical degradation of gabapentin was studied. When a neutral kneading block was used, gabapentin underwent polymorphic transformation. A forward kneading block in combination with processing under torque conditions was required to minimize chemical degradation and to inhibit polymorphic transformation of gabapentin. Both the size of the extruded granules and gabapentin degradant level correlated positively with the specific rate, the ratio between feed rate and screw speed. At higher specific rate, the barrel was filled to a greater extent. The material packing and compressive forces were enhanced, as proven by the increased rupturing of CAMES® sensor beads and GABA crystal size reduction. This resulted in more interaction between the powder particles and facilitated granule growth. Simultaneously, this also resulted in higher degradant level. To attain adequate tabletability, the specific rate must reach a threshold value. The development of an optimum TSMG process requires balancing processing parameters based on the physical and chemical stability of GABA as well as its tabletability.

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.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

30797938

Citation

Kittikunakorn, Nada, et al. "Effect of Screw Profile and Processing Conditions On Physical Transformation and Chemical Degradation of Gabapentin During Twin-screw Melt Granulation." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 131, 2019, pp. 243-253.
Kittikunakorn N, Sun CC, Zhang F. Effect of screw profile and processing conditions on physical transformation and chemical degradation of gabapentin during twin-screw melt granulation. Eur J Pharm Sci. 2019;131:243-253.
Kittikunakorn, N., Sun, C. C., & Zhang, F. (2019). Effect of screw profile and processing conditions on physical transformation and chemical degradation of gabapentin during twin-screw melt granulation. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 131, 243-253. https://doi.org/10.1016/j.ejps.2019.02.024
Kittikunakorn N, Sun CC, Zhang F. Effect of Screw Profile and Processing Conditions On Physical Transformation and Chemical Degradation of Gabapentin During Twin-screw Melt Granulation. Eur J Pharm Sci. 2019 Apr 1;131:243-253. PubMed PMID: 30797938.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of screw profile and processing conditions on physical transformation and chemical degradation of gabapentin during twin-screw melt granulation. AU - Kittikunakorn,Nada, AU - Sun,Changquan Calvin, AU - Zhang,Feng, Y1 - 2019/02/21/ PY - 2019/01/07/received PY - 2019/02/12/revised PY - 2019/02/16/accepted PY - 2019/2/25/pubmed PY - 2019/8/7/medline PY - 2019/2/25/entrez KW - Chemical degradation KW - Gabapentin KW - Process-induced transformation KW - System parameter KW - Twin-screw melt granulation SP - 243 EP - 253 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 131 N2 - Twin-screw melt granulation (TSMG) was applied to process a powder blend consisting of 80% gabapentin (GABA) and 20% hydroxypropyl cellulose. The effect of screw profile and processing conditions on the process-induced transformation and chemical degradation of gabapentin was studied. When a neutral kneading block was used, gabapentin underwent polymorphic transformation. A forward kneading block in combination with processing under torque conditions was required to minimize chemical degradation and to inhibit polymorphic transformation of gabapentin. Both the size of the extruded granules and gabapentin degradant level correlated positively with the specific rate, the ratio between feed rate and screw speed. At higher specific rate, the barrel was filled to a greater extent. The material packing and compressive forces were enhanced, as proven by the increased rupturing of CAMES® sensor beads and GABA crystal size reduction. This resulted in more interaction between the powder particles and facilitated granule growth. Simultaneously, this also resulted in higher degradant level. To attain adequate tabletability, the specific rate must reach a threshold value. The development of an optimum TSMG process requires balancing processing parameters based on the physical and chemical stability of GABA as well as its tabletability. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/30797938/Effect_of_screw_profile_and_processing_conditions_on_physical_transformation_and_chemical_degradation_of_gabapentin_during_twin_screw_melt_granulation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(19)30085-5 DB - PRIME DP - Unbound Medicine ER -