Solid‐state properties and relationship between anhydrate and monohydrate of baclofen

Mirza, Sabiruddin; Miroshnyk, Inna; Rantanen, Jukka; Aaltonen, Jaakko; Harjula, Pasi; Kiljunen, Eero; Heinämäki, Jyrki; Yliruusi, Jouko

doi:10.1002/jps.20894

“…Crystalline polymorph in ethanol/water mixtures Raman spectroscopy Baclofen [127] Solution-mediated hydrate formation to baclofen monohydrate Wet granulation Raman spectroscopy Azithromycin [49] Hydrate formation to azithromycin monohydrate and dihydrate Storage experiments in a desiccator or humidity cell NIR spectroscopy Caffeine [128] Hydrate formation to a non-stoichiometric hydrate of caffeine, dehydrate formation Humidity cell NIR spectroscopy Risedronate sodium [129] Dehydrate formation of risedronate sodium hemi-pentahydrate Fluid-bed drying Raman spectroscopy Theophylline [130] Dehydrate formation of theophylline monohydrate Fluid-bed drying NIR and Raman spectroscopy Carbamazepine, piroxicam [131] Dehydrate formation of carbamazepine dihydrate and piroxicam monohydrate [82,135] Dehydrate formation of piroxicam monohydrate…”

Section: Raman Spectroscopymentioning

confidence: 99%

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

Heinz

¹

,

Strachan

²

,

Gordon

³

et al. 2009

View full text Add to dashboard Cite

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.

show abstract

“…Other hydrate formation studies characterised the solid‐state behaviour of baclofen during wet granulation experiments using a range of analytical techniques, including FTIR, NIR and Raman spectroscopy, 127 and conversions between different solid‐state forms of azithromycin, including the amorphous and hydrate forms, at different relative humidities using NIR spectroscopy and PLS regression 49 . NIR spectroscopy has also been used to study the influence of time, temperature and humidity on interconversions of the anhydrate/hydrate system of caffeine 128 .…”

Section: Introductionmentioning

confidence: 99%

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

Heinz

¹

,

Strachan

²

,

Gordon

³

et al. 2009

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

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.

show abstract

“…The solid‐state properties of the anhydrate and monohydrate forms of baclofen have been studied with the goal of understanding the processing‐induced phase transition associated with wet granulation of the compound 142. The crystal structure for the antimigraine agent zolmitripan has been reported,143 as have the structures of its solvates with chloroform144 and with its benzene solvate and phenol co‐crystal 145.…”

Section: Structural Characterization and Properties Of Polymorphs Andmentioning

confidence: 99%

Polymorphism and Solvatomorphism 2007

Brittain¹

2009

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Solid‐state properties and relationship between anhydrate and monohydrate of baclofen

Cited by 35 publications

References 17 publications

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

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

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

Polymorphism and Solvatomorphism 2007

Contact Info

Product

Resources

About