Solid state characterization of chloramphenicol palmitate. Raman spectroscopy applied to pharmaceutical polymorphs

Gamberini, Maria Cristina; Baraldi, Cecilia; Tinti, Anna; Rustichelli, Cecilia; Ferioli, Valeria; Gamberini, Gianfranco

doi:10.1016/j.molstruc.2005.10.012

Cited by 33 publications

(18 citation statements)

References 9 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In another study, three polymorphic forms of chloramphenicol palmitate were characterised using DRIFTS and Raman spectroscopy, and solid-state conversions between these forms were monitored upon heating, melting and cooling by hot-stage Raman microscopy. [94] Another similar study by this group showed the potential of hot-stage microscopy and Raman spectroscopy to characterise solid-state transformations between different solidstate forms of tamoxifen citrate after applying heating and cooling programmes to the drug. [95] In contrast to the previously mentioned studies, in two recent studies DSC was used to heat the samples to the desired temperatures and either in-situ Raman spectroscopy [96] or Raman microscopy [97] was used to monitor polymorphic transitions.…”

Section: Heatingmentioning

confidence: 98%

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

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

Section: Heatingmentioning

confidence: 98%

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

et al. 2009

View full text Add to dashboard Cite

show abstract

“…Chloramphenicol palmitate exists in three polymorphic forms [65,66,70,71], the stable form A (biologically inactive modification), the metastable form B (active modification) and the unstable form C [67], which recently have been fully characterized thanks to advances in analytical methods [68,69]. Polymorph A is the thermodynamically stable one, but its absorption in humans is significantly lower than that of polymorph B [72], because Form B dissolves faster than Form A, and has much higher solubility [73].…”

Section: Chloramphenicol Palmitatementioning

confidence: 99%

Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs

2015

View full text Add to dashboard Cite

Drugs with low water solubility are predisposed to poor and variable oral bioavailability and, therefore, to variability in clinical response, that might be overcome through an appropriate formulation of the drug. Polymorphs (anhydrous and solvate/hydrate forms) may resolve these bioavailability problems, but they can be a challenge to ensure physicochemical stability for the entire shelf life of the drug product. Since clinical failures of polymorph drugs have not been uncommon, and some of them have been entirely unexpected, the Food and Drug Administration (FDA) and the International Conference on Harmonization (ICH) has required preliminary and exhaustive screening studies to identify and characterize all the polymorph crystal forms for each drug. In the past, the polymorphism of many drugs was detected fortuitously or through manual time consuming methods; today, drug crystal engineering, in particular, combinatorial chemistry and high-throughput screening, makes it possible to easily and exhaustively identify stable polymorphic and/or hydrate/dehydrate forms of poorly soluble drugs, in order to overcome bioavailability related problems or clinical failures. This review describes the concepts involved, provides examples of drugs characterized by poor solubility for which polymorphism has proven important, outlines the state-of-the-art technologies and discusses the pertinent regulations.

show abstract

“…[9][10][11][12][13][14][15][16][17] Despite the similar information content of Raman and infrared absorption (IR) spectroscopies, Raman presents several advantages over IR. In the particular context of the present work, the most relevant advantage is the low Raman activity of water vibrations, whose strong infrared activity tends to mask a wide IR spectrum range.…”

Section: Introductionmentioning

confidence: 99%

Probing Pseudopolymorphic Transitions in Pharmaceutical Solids using Raman Spectroscopy: Hydration and Dehydration of Theophylline

Amado

Nolasco

Ribeiro‐Claro

2007

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Theophylline is known to undergo vapor phase induced hydrate-anhydrate pseudopolymorphic transformations, which can affect its bioavailability. In this work, the kinetics of the pseudopolymorphic transitions of theophylline crystals in different storage conditions is studied using a vibrational spectroscopic technique. While the hydration is a single-step process with a half-life time of ca. 5 h, the dehydration occurs through a two-step mechanism. In addition, the phase stability of hydrate-anhydrate systems in different relative humidity (RH) conditions was probed. The critical RH for anhydrous teophylline was found to be at ca. 79%, while the critical RH for dehydration is ca. 30%. ß

show abstract

Solid state characterization of chloramphenicol palmitate. Raman spectroscopy applied to pharmaceutical polymorphs

Cited by 33 publications

References 9 publications

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

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

Polymorph Impact on the Bioavailability and Stability of Poorly Soluble Drugs

Probing Pseudopolymorphic Transitions in Pharmaceutical Solids using Raman Spectroscopy: Hydration and Dehydration of Theophylline

Contact Info

Product

Resources

About