Calorimetric and spatial characterization of polymorphic transitions in caffeine using quasi‐isothermal MTDSC and localized thermomechanical analysis

Manduva, R.; Kett, Vicky L.; Banks, Simon R.; Wood, John G.; Reading, M.; Craig, Duncan Q.M.

doi:10.1002/jps.21048

Cited by 25 publications

(15 citation statements)

References 31 publications

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“…Caffeine is one of the most widely used psychoactive drug in the world and it is cheap and readily available (Sahoo, 2015). This common molecule is well known for polymorphism studies (Pirttimäki et al, 1993;Lehto and Laine, 1998;Manduva et al, 2008;Mazel et al, 2011) which presents a simple enantiotropic behaviour.…”

Section: Introductionmentioning

confidence: 99%

Processing-induced-transformations (PITs) during direct compression: Impact of tablet composition and compression load on phase transition of caffeine

Juban

Briançon

Puel

2016

International Journal of Pharmaceutics

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In the pharmaceutical field, solid-state transitions that may occur during manufacturing of pharmaceuticals are of great importance. The phase transition of a model API, caffeine Form I (CFI), was studied during direct compression process by analysing the impacts of the operating conditions (process and formulation). This work is focused on two formulation parameters: nature of the diluent and impact of the caffeine dilution, and one process parameter: the compression pressure that may impact the phase transition of CFI. Tablets were made from pure CFI and from binary mixture of CFI/diluent (microcrystalline cellulose or anhydrous dicalcium phosphate). A kinetic study performed during six months helped to highlight the influence of these parameters on the CFI transition degree. Results showed a triggering effect of the direct compression process, transformation was higher in tablets than in uncompressed powders. Whatever the pressure applied, CFI transition degree was almost constant and uniformly occurring throughout the tablet volume. Nevertheless, several differences on the evolution of the CFI transition degree were observed between binary mixtures of CFI/diluent. An analysis of the transition mechanism with a stretched exponential law of the Johnson-Mehl-Avrami model shows that tableting accelerates the polymorphic transition without modifying its mechanism controlled by nucleation only.

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Section: Introductionmentioning

confidence: 99%

Processing-induced-transformations (PITs) during direct compression: Impact of tablet composition and compression load on phase transition of caffeine

Juban

Briançon

Puel

2016

International Journal of Pharmaceutics

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“…dielectric analysis, DEA). Wybrane przykłady ilustrujące możliwość użycia analizy dielektrycznej i termomechanicznej w badaniu substancji i produktów farmaceutycznych zestawiono w tabeli 2 [18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34].…”

Section: Analiza Termomechaniczna I Dielektrycznaunclassified

Thermomechanical analysis and thermal dielectric analysis in pharmacy

Szynkaruk¹,

Wesołowski²

2019

Farm Pol.

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Tom 75 • nr 11 • 2019 jakim podlegają substancje stosowane do celów farmaceutycznych, tj. aktywne składniki farmaceutyczne (ang. active pharmaceutical ingredients, APIs), substancje pomocnicze, półprodukty i gotowe produkty farmaceutyczne [1-7]. Najważniejsze procesy, jakie z punktu widzenia farmacji mogą być badane tymi technikami, to przemiany fazowe-przemiana szklista, topnienie, krystalizacja, parowanie, sublimacja, dehydratacja i hydratacja, solwatacja i desolwatacja, polimorfizm i pseudopolimorfizm, a ponadto, reakcje M etody analizy termicznej, w szczególności różnicowa analiza termiczna (ang. Differential thermal analysis, DTA), różnicowa kalorymetria skaningowa (ang. differential scanning calorimetry, DSC) i analiza termograwimetryczna (ang. thermogravimetric analysis, TGA), są nowoczesnymi, skomputeryzowanymi i zautomatyzowanymi technikami analizy instrumentalnej, które umożliwiają badanie w różnych warunkach tem

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“…Kawakami and Ida, 21 applied MTDSC technique to demonstrate enantiotropic transitions in furosemide, tolbutamide and sulfanerazine, and thus explored the use of MTDSC in demonstrating enantiotropic transitions in well-known compounds. Manduva et al 22 investigated the polymorphic forms and kinetics of transitions in caffeine. Thus, the use of MTDSC in differentiating the polymorphs came into lime light.…”

Section: Polymorphic Studiesmentioning

confidence: 99%

Calculation of MTDSC signals, factors effecting the signals and applications in drug development

Syamala¹

2018

MOJBB

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In this paper the author emphasizes on the basic principle of Modulated Temperature Differential Scanning Calorimetry (MTDSC), advantages of MTDSC compared to conventional DSC, calculation of heat flow components and heat capacity components, factors effecting the MTDSC signals and application of MTDSC in drug development. MTDSC a sinusoidal modulation is overlaid on a conventional linear heating ramp, in which the sample temperature increases continuously with time. The linear heating rate gives the information same as the standard DSC, while the sinusoidal heating rate determines the fraction of the total heat flow corresponding to the changing heat rate. The total heat flow rate depends on heat capacity and change in heat capacity. This fraction of heat flow is called Reversing heat flow or the heat capacity component of the Total heat flow. The kinetic component is time dependent, also known as Non-reversing heat flow that does not respond to the changing heating rate. For accurate measurements of heat flow components and heat capacity components optimized experimental parameters must be chosen. MTDSC in particularly plays an preformulation studies to establish Tg, polymorphic forms, polymorphic transitions, ensure stability by drug excipient compatability studies and to determine enthalpy of polymorphic transitions.

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Calorimetric and spatial characterization of polymorphic transitions in caffeine using quasi‐isothermal MTDSC and localized thermomechanical analysis

Cited by 25 publications

References 31 publications

Processing-induced-transformations (PITs) during direct compression: Impact of tablet composition and compression load on phase transition of caffeine

Processing-induced-transformations (PITs) during direct compression: Impact of tablet composition and compression load on phase transition of caffeine

Thermomechanical analysis and thermal dielectric analysis in pharmacy

Calculation of MTDSC signals, factors effecting the signals and applications in drug development

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