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Kinetic estimation of solid state transition during isothermal and grinding processes among efavirenz polymorphs.
Heliyon. 2020 May; 6(5):e03876.H

Abstract

Investigation into the solid-state transition among drug polymorphs has been more intense lately. Many factors induce the transformation of polymorphs during manufacturing processes. Efavirenz (EFV), an AIDS therapy drug, has more than 23 polymorphs, but very little information has been reported on them. This study aimed to perform a characterisation of EFV polymorph properties and to predict the kinetics and mechanism of the polymorphic transformation of EFV during manufacturing processes. The bimorphism study was conducted by Differential Scanning Calorimetry (DSC) thermal analysis. The phase transition kinetics of the polymorphs was monitored by X-ray powder diffraction and the quantification of concomitant polymorphs was examined using Rietveld refinement with MAUD ver. 2.7 as a software aid. To predict the solid-state transition, correlation coefficients of solid-state kinetic models were fitted to the experimental data. The results show that Form I and Form II of EFV were thermodynamically shown to be monotropy related. By fitting the experimental data, it was found that isothermal treatment had the best model fit with the phase boundary reaction in the two-dimensional model (G2). Accordingly, by employing mechanical treatment (grinding), it was predicted that the transition mechanism is a second-ordered reaction (R2). The activation energy of the transition during isothermal treatment calculated by the Arrhenius plot was found to be 23.051 kJ mol-1; the half-lif of Form II at ambient temperature was 428.05 min (~7.1 h).

Authors+Show Affiliations

Department of Pharmaceutics, School of Pharmacy, Institute Technology of Bandung (ITB), Indonesia. Department of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Indonesia.Inorganic and Physical Chemistry Division, Faculty of Mathematics and Natural Sciences, ITB, Indonesia. Department of Chemistry, Faculty of Mathematics and Natural Sciences, University of Jenderal Achmad Jani (UNJANI), Indonesia.Department of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Indonesia.Inorganic and Physical Chemistry Division, Faculty of Mathematics and Natural Sciences, ITB, Indonesia. Research Center for Nanoscience and Nanotechnology, Institute Technology of Bandung (ITB), Indonesia.Department of Pharmaceutics, School of Pharmacy, Institute Technology of Bandung (ITB), Indonesia. Research Center for Nanoscience and Nanotechnology, Institute Technology of Bandung (ITB), Indonesia.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32405549

Citation

Wardhana, Yoga Windhu, et al. "Kinetic Estimation of Solid State Transition During Isothermal and Grinding Processes Among Efavirenz Polymorphs." Heliyon, vol. 6, no. 5, 2020, pp. e03876.
Wardhana YW, Hardian A, Chaerunisa AY, et al. Kinetic estimation of solid state transition during isothermal and grinding processes among efavirenz polymorphs. Heliyon. 2020;6(5):e03876.
Wardhana, Y. W., Hardian, A., Chaerunisa, A. Y., Suendo, V., & Soewandhi, S. N. (2020). Kinetic estimation of solid state transition during isothermal and grinding processes among efavirenz polymorphs. Heliyon, 6(5), e03876. https://doi.org/10.1016/j.heliyon.2020.e03876
Wardhana YW, et al. Kinetic Estimation of Solid State Transition During Isothermal and Grinding Processes Among Efavirenz Polymorphs. Heliyon. 2020;6(5):e03876. PubMed PMID: 32405549.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Kinetic estimation of solid state transition during isothermal and grinding processes among efavirenz polymorphs. AU - Wardhana,Yoga Windhu, AU - Hardian,Arie, AU - Chaerunisa,Anis Y, AU - Suendo,Veinardi, AU - Soewandhi,Sundani N, Y1 - 2020/05/05/ PY - 2020/02/11/received PY - 2020/03/16/revised PY - 2020/04/24/accepted PY - 2020/5/15/entrez PY - 2020/5/15/pubmed PY - 2020/5/15/medline KW - Bimorphism KW - Efavirenz KW - Grinding KW - Isothermal KW - Kinetics study KW - Materials characterization KW - Materials chemistry KW - Materials processing KW - Materials structure KW - Pharmaceutical chemistry KW - Physical chemistry KW - Rietveld refinement SP - e03876 EP - e03876 JF - Heliyon JO - Heliyon VL - 6 IS - 5 N2 - Investigation into the solid-state transition among drug polymorphs has been more intense lately. Many factors induce the transformation of polymorphs during manufacturing processes. Efavirenz (EFV), an AIDS therapy drug, has more than 23 polymorphs, but very little information has been reported on them. This study aimed to perform a characterisation of EFV polymorph properties and to predict the kinetics and mechanism of the polymorphic transformation of EFV during manufacturing processes. The bimorphism study was conducted by Differential Scanning Calorimetry (DSC) thermal analysis. The phase transition kinetics of the polymorphs was monitored by X-ray powder diffraction and the quantification of concomitant polymorphs was examined using Rietveld refinement with MAUD ver. 2.7 as a software aid. To predict the solid-state transition, correlation coefficients of solid-state kinetic models were fitted to the experimental data. The results show that Form I and Form II of EFV were thermodynamically shown to be monotropy related. By fitting the experimental data, it was found that isothermal treatment had the best model fit with the phase boundary reaction in the two-dimensional model (G2). Accordingly, by employing mechanical treatment (grinding), it was predicted that the transition mechanism is a second-ordered reaction (R2). The activation energy of the transition during isothermal treatment calculated by the Arrhenius plot was found to be 23.051 kJ mol-1; the half-lif of Form II at ambient temperature was 428.05 min (~7.1 h). SN - 2405-8440 UR - https://www.unboundmedicine.com/medline/citation/32405549/Kinetic_estimation_of_solid_state_transition_during_isothermal_and_grinding_processes_among_efavirenz_polymorphs L2 - https://linkinghub.elsevier.com/retrieve/pii/S2405-8440(20)30721-0 DB - PRIME DP - Unbound Medicine ER -
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