Demonstration of a Shear-Based Solid-State Phase Transformation in a Small Molecular organic System: Chlorpropamide

Wildfong, Peter L.D.; Morris, Kenneth R.; Anderson, Carl A.; Short, Steven M.

doi:10.1002/jps.20920

“…In-situ Raman spectroscopy Paracetamol [97] Polymorphic transition between crystalline forms I, II and III Heating using DSC Raman microscopy Chlorpropamide [98] Polymorphic transformation of chlorpropamide form A to form C…”

Section: Heating Using Dscmentioning

confidence: 99%

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

Heinz

¹

,

Strachan

²

,

Gordon

³

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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“…The inverse relationship between particle size and dissolution rate has enabled the exploitation of particle size reduction as a method of enhancing aqueous dissolution [8]. Impact mills and fluid-energy mills are commonly used for particle size reduction; however, the high-energy input from these methods can induce unwanted or unanticipated phase changes (i.e., polymorphism [9], amorphization [10,11], etc.) with implications of physical instability [12].…”

Section: Introductionmentioning

confidence: 99%

Aqueous Solubility Enhancement Through Engineering of Binary Solid Composites: Pharmaceutical Applications

Moore

¹

,

Wildfong

²

2009

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Limits to the aqueous solubility of emerging new chemical entities, as well as older drug molecules, represent a barrier to solid oral dosage form development. Numerous techniques are conventionally employed in aqueous solubility enhancement, although a universal strategy has proven elusive. Formation of binary solid composites, such as eutectics or amorphous solid dispersions, offers an alternative to traditional solubility enhancement techniques. The reality of these systems, however, is that very few examples have been made commercially available, ultimately stemming from a lack of understanding regarding structural and thermodynamic stability-indicating phenomena associated with higher-energy solid materials. In the present work, a comprehensive structurally based review of the fundamental solid-state properties of binary composite materials is presented. Specific emphasis is placed on current topics of research in the area of binary composite formation and the relationship to the underutilization of this technology with the pharmaceutical industry.

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“…Another recent study investigated the mechanically induced transformation between the two structurally closely related enantiotropes of chlorpropamide as a function of the applied pressure during compaction using in‐situ Raman spectroscopy 98 . A PLS regression model involving binary mixtures of the two solid‐state forms was used for quantification.…”

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

Demonstration of a Shear-Based Solid-State Phase Transformation in a Small Molecular organic System: Chlorpropamide

Cited by 42 publications

References 39 publications

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

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

Aqueous Solubility Enhancement Through Engineering of Binary Solid Composites: Pharmaceutical Applications

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

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