In Situ Measurement of Solvent-Mediated Phase Transformations During Dissolution Testing

Aaltonen, Jaakko; Heinänen, Paula; Peltonen, Leena; Kortejärvi, Hanna; Tanninen, Veli Pekka; Christiansen, Leena; Hirvonen, Jouni; Yliruusi, Jouko; Rantanen, Jukka

doi:10.1002/jps.20725

Cited by 91 publications

(89 citation statements)

References 22 publications

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“…Wet granulation NIR and Raman spectroscopy Theophylline, nitrofurantoin [121] Solution-mediated hydrate formation to theophylline monohydrate and nitrofurantoin monohydrate…”

Section: Solvatesmentioning

confidence: 99%

“…In a study that provided direct evidence of the effect of solid-state conversions on dissolution behaviour, in-line Raman spectroscopy was combined with a channel flow dissolution cell where powder compacts of the API were exposed to the dissolution medium. [121] The kinetics of theophylline and nitrofurantoin hydrate formation were studied quantitatively. In a subsequent study, the transformation from the theophylline anhydrate to the monohydrate during intrinsic dissolution testing was also studied in a rotating disc setup, using simulated gastric fluid (pH 1.2) as the dissolution medium.…”

Section: Raman Spectroscopymentioning

confidence: 99%

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Analysis of solid-state transformations of pharmaceutical compounds using vibrational spectroscopy

et al. 2009

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Objectives Solid-state transformations may occur during any stage of pharmaceutical processing and upon storage of a solid dosage form. Early detection and quantification of these transformations during the manufacture of solid dosage forms is important since the physical form of an active pharmaceutical ingredient can significantly influence its processing behaviour, including powder flow and compressibility, and biopharmaceutical properties such as solubility, dissolution rate and bioavailability. Key findings Vibrational spectroscopic techniques such as infrared, near-infrared, Raman and, most recently, terahertz pulsed spectroscopy have become popular for solidstate analysis since they are fast and non-destructive and allow solid-state changes to be probed at the molecular level. In particular, Raman and near-infrared spectroscopy, which require no sample preparation, are now commonly used coupled to fibreoptic probes and are able to characterise solid-state conversions in-line. Traditionally, uni-or bivariate approaches have been used to analyse spectroscopic data sets; however, recently the simultaneous detection of several solid-state forms has been increasingly performed using multivariate approaches where even overlapping spectral bands can be analysed. Summary This review discusses the applications of different vibrational spectroscopic techniques to detect and monitor solid-state transformations possible for crystalline polymorphs, hydrates and amorphous forms of pharmaceutical compounds. In this context, the theoretical basis of solid-state transformations and vibrational spectroscopy and common experimental approaches are described, including recent methods of data analysis.

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“…Wet granulation NIR and Raman spectroscopy Theophylline, nitrofurantoin [121] Solution-mediated hydrate formation to theophylline monohydrate and nitrofurantoin monohydrate…”

Section: Solvatesmentioning

confidence: 99%

Section: Raman Spectroscopymentioning

confidence: 99%

Analysis of solid-state transformations of pharmaceutical compounds using vibrational spectroscopy

et al. 2009

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“…The mechanism of modification can be best explained by solvent-solute interactions (20,28). Hydrogen bond formation, between solvent and solute, plays a key role in the formation of different solid-state morphology (19,20,28). Normally, there are three types of solvents used in routine morphology screening.…”

Section: ) C O M P L I E D W I T H D I H Y D R a T E F O R M O F A M mentioning

confidence: 99%

Solid-State Characterization and Interconversion of Recrystallized Amodiaquine Dihydrochloride in Aliphatic Monohydric Alcohols

2015

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Abstract. Amodiaquine dihydrochloride monohydrate (AQ-DM) was obtained by recrystallizing amodiaquine dihydrochloride dihydrate (AQ-DD) in methanol, ethanol, and n-propanol. Solid-state characterization of AQ-DD and AQ-DM was performed using X-ray powder diffractometry, Fourier transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetry. All recrystallized samples were identified as AQ-DM. Crystal habits of AQ-DD and AQ-DM were shown to be needle-like and rhombohedral crystals, respectively. When AQ-DD and AQ-DM were exposed to various relative humidity in dynamic vapor sorption apparatus, no solid-state interconversion was observed. However, AQ-DM showed higher solubility than AQ-DD when exposed to bulk water during solubility study, while excess AQ-DM was directly transformed back to a more stable AQ-DD structure. Heating AQ-DM sample to temperatures ≥190°C induced initial change to metastable amorphous form (AQ-DA) which was rapidly recrystallized to AQ-DD upon ≥80%RH moisture exposure. AQ-DD was able to be recrystallized in alcohols (C1-C3) as AQ-DM solid-state structure. In summary, AQ-DM was shown to have different solubility, moisture and temperature stability, and interconversion pathways when compared to AQ-DD. Thus, when AQ-DM was selected for any pharmaceutical applications, these critical transformation and property differences should be observed and closely monitored.

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“…wet granulation (1). Also recent studies with various pharmaceutical compounds have shown the influence of polymorphic conversions on the dissolution of drugs (2)(3)(4). The control of the polymorphic form is therefore of obvious importance in drug and dosage form development.…”

Section: Introductionmentioning

confidence: 99%

Visualizing Solvent Mediated Phase Transformation Behavior of Carbamazepine Polymorphs by Principal Component Analysis

2008

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Abstract. The purpose of this research is to gain a greater insight into the hydrate formation processes of different carbamazepine (CBZ) anhydrate forms in aqueous suspension, where principal component analysis (PCA) was applied for data analysis. The capability of PCA to visualize and to reveal simplified structures that often underlie large data sets are explored. Different CBZ polymorphs were dispersed separately in aqueous solution, and then recovered and measured by FT-Raman spectroscopy. PCA was employed for visualizing the dynamics of the phase transformation from each CBZ polymorph to the dihydrate (DH). As a comparison to PCA visualization, the transformation process of each CBZ polymorph was quantified using PLS modeling. The results demonstrated that PCA has advantages in presenting the original data in terms of the differences and similarities, and also directly identify the statistical patterns in the data even when the data set is large. These advantages provided greater insight into the measured Raman spectra as well as the phase transformation process of CBZ polymorphs to the DH in aqueous environment.

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In Situ Measurement of Solvent-Mediated Phase Transformations During Dissolution Testing

Cited by 91 publications

References 22 publications

Analysis of solid-state transformations of pharmaceutical compounds using vibrational spectroscopy

Analysis of solid-state transformations of pharmaceutical compounds using vibrational spectroscopy

Solid-State Characterization and Interconversion of Recrystallized Amodiaquine Dihydrochloride in Aliphatic Monohydric Alcohols

Visualizing Solvent Mediated Phase Transformation Behavior of Carbamazepine Polymorphs by Principal Component Analysis

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