Mapping the Polymorphic Forms of Fexofenadine in Pharmaceutical Tablets Using near Infrared Chemical Imaging

Brondi, Ariadne M.; Terra, Luciana A.; Sabin, Guilherme P.; Garcia, Jerusa Simone; Poppi, Ronei J.; Trevisan, Marcello G.

doi:10.1255/jnirs.1094

Cited by 14 publications

(4 citation statements)

References 17 publications

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“…The major difference in the FTIR spectra of the two forms of FXD was observed as OH symmetrical stretching at 3399.48 cm −1 and several shifts in the fingerprint region between 400 cm −1 and 1800 cm −1 . All these observations showed good agreement with the values reported in the literature [30,31]. By compared with the PXRD and FTIR results reported in the literature, it was confirmed that phase-transformed solid form of FXD was crystalline Form II.…”

Section: Solid State Characterization Of Polymorphssupporting

confidence: 90%

Solid Form and Phase Transformation Properties of Fexofenadine Hydrochloride during Wet Granulation Process

Zhao

et al. 2021

Pharmaceutics

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The quality control of drug products during manufacturing processes is important, particularly the presence of different polymorphic forms in active pharmaceutical ingredients (APIs) during production, which could affect the performance of the formulated products. The objective of this study was to investigate the phase transformation of fexofenadine hydrochloride (FXD) and its influence on the quality and performance of the drug. Water addition was key controlling factor for the polymorphic conversion from Form I to Form II (hydrate) during the wet granulation process of FXD. Water-induced phase transformation of FXD was studied and quantified with XRD and thermal analysis. When FXD was mixed with water, it rapidly converted to Form II, while the conversion is retarded when FXD is formulated with excipients. In addition, the conversion was totally inhibited when the water content was <15% w/w. The relationship between phase transformation and water content was studied at the small scale, and it was also applicable for the scale-up during wet granulation. The effect of phase transition on the FXD tablet performance was investigated by evaluating granule characterization and dissolution behavior. It was shown that, during the transition, the dissolved FXD acted as a binder to improve the properties of granules, such as density and flowability. However, if the water was over added, it can lead to the incomplete release of the FXD during dissolution. In order to balance the quality attributes and the dissolution of granules, the phase transition of FXD and the water amount added should be controlled during wet granulation.

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Section: Solid State Characterization Of Polymorphssupporting

confidence: 90%

Solid Form and Phase Transformation Properties of Fexofenadine Hydrochloride during Wet Granulation Process

Zhao

et al. 2021

Pharmaceutics

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“…These augmented matrices can provide a greater amount of information, as well as solve problems related to rank-deficient matrices. 33,[35][36][37] Taking into account these precautions, we can verify that NIR-CI and chemometrics combination is an excellent alternative in pharmaceutical area, but several parameters must be optimized to obtain realistic and trustworthy chemical images. In this paper, we intend to study the effects of pixel size variation, initial estimation type and augmented matrix in pharmaceutical pellets analysis optimization by near infrared-chemical imaging (NIR-CI) and multivariate curve resolution with alternating least squares (MCR-ALS).…”

Section: Introductionmentioning

confidence: 88%

Optimization of Experimental Parameters in Analysis of Pharmaceutical Pellets by Near Infrared-Chemical Imaging (NIR-CI) and Multivariate Curve Resolution with Alternating Least Squares (MCR-ALS)

Da-Col¹,

Poppi²

2018

J. Braz. Chem. Soc.

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The quality control of pellets homogeneity cannot be assessed by conventional techniques and near infrared-chemical imaging combined with multivariate curve resolution with alternating least squares is an attractive alternative. In this study, composition and spatial distribution of pellets components were determined after assessment of experimental parameters. The use of a 25 μm intermediate pixel size, an initial estimation matrix with instrumental signals for pure substances and individual matrices provided a model with explained variance of more than 99% and a value of 0.00263 for percentage of lack of fit. In addition, the similarity between the pure substances spectra and those recovered by the model were 0.9501 for sucrose, 0.9480 for starch, 0.9910 for ketoprofen and 0.5941 for SiO 2 . Chemical images were generated and show that the pellet is composed of an inert nucleus of starch and cellulose, surrounded by a ketoprofen layer. All this information was obtained quickly, in minutes, being an excellent alternative for pellets analysis.

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“…Although studies solely aimed at the development of new analytical methods for the quantification of different solidstate forms are not the focus of this review, it should be mentioned here that imaging and non-imaging vibrational spectroscopy, in particular NIR and Raman spectroscopy, in conjunction with chemometric tools receives significant attention in analytical chemistry and for quality assurance applications [88][89][90][91][92][93][94][95][96][97][98][99][100]. While the traditional method of monitoring the area or height of a selected band or the area or height ratio of two bands gives satisfactory results in some cases, nowadays multivariate methods that use the entire spectrum, a spectral region or a combination of spectral regions are routinely applied, when accurate quantitative data are needed.…”

Section: Spectral Data Analysismentioning

confidence: 99%

Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals

Erxleben

2016

CPD

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Understanding the properties, stability and transformations of the solid-state forms of an active pharmaceutical ingredient (API) in the development pipeline is of crucial importance for process-development, formulation development and FDA approval. Investigation of the polymorphism and polymorphic stability is a routine part of the preformulation studies. Vibrational spectroscopy allows the real-time in situ monitoring of phase transformations and probes intermolecular interactions between API molecules, between API and polymer in amorphous solid dispersions or between API and coformer in cocrystals or coamorphous systems and thus plays a major role in efforts to gain a predictive understanding of the relative stability of solid-state forms and formulations. Infrared (IR), near-infrared (NIR) and Raman spectroscopies, alone or in combination with other analytical methods, are important tools for studying transformations between different crystalline forms, between the crystalline and amorphous form, between hydrate and anhydrous form and for investigating solid-state cocrystal formation. The development of simple-to-use and cost-effective instruments on the one hand and recent technological advances such as access to the low-frequency Raman range down to 5 cm-1, on the other, have led to an exponential growth of the literature in the field. This review discusses the application of IR, NIR and Raman spectroscopies in the study of solid-state transformations with a focus on the literature published over the last eight years.

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Mapping the Polymorphic Forms of Fexofenadine in Pharmaceutical Tablets Using near Infrared Chemical Imaging

Cited by 14 publications

References 17 publications

Solid Form and Phase Transformation Properties of Fexofenadine Hydrochloride during Wet Granulation Process

Solid Form and Phase Transformation Properties of Fexofenadine Hydrochloride during Wet Granulation Process

Optimization of Experimental Parameters in Analysis of Pharmaceutical Pellets by Near Infrared-Chemical Imaging (NIR-CI) and Multivariate Curve Resolution with Alternating Least Squares (MCR-ALS)

Application of Vibrational Spectroscopy to Study Solid-state Transformations of Pharmaceuticals

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