Solid-State Vitrification of Crystalline Griseofulvin by Mechanical Milling

willart, Jean-François; Carpentier, Laurent; Danède, Florence; Descamps, Marc

doi:10.1002/jps.23041

Cited by 46 publications

(44 citation statements)

References 29 publications

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“…There are three reported crystalline polymorphic forms of griseofulvin: the stable form I and the metastable forms II and III [32]. The amorphous form of griseofulvin can be prepared either by quench cooling or cryomilling [33,34]. The crystallization of amorphous forms of griseofulvin has previously been characterized using XRPD, DSC and isothermal microcalorimetry [35][36][37].…”

Section: Introductionmentioning

confidence: 99%

Use of low-frequency Raman spectroscopy and chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets

Mah

Fraser

Reish

et al. 2015

Vibrational Spectroscopy

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Section: Introductionmentioning

confidence: 99%

Use of low-frequency Raman spectroscopy and chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets

Mah

Fraser

Reish

et al. 2015

Vibrational Spectroscopy

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“…This can lead to the generation of a metastable polymorph, to increased disorder within a crystalline material or to a disordered amorphous state. [2][3][4] The latter two consequences are often undesirable and unintentional as these high energy forms will tend to revert back over time to the more energetically favoured crystalline state, with subsequent implications for processability, stability and performance. 5,6 The position of the glass transition temperature (Tg) of a material relative to the milling temperature has a direct influence on whether polymorphic transformation or amorphisation is observed upon milling.…”

Section: Introductionmentioning

confidence: 99%

Investigation of the Capacity of Low Glass Transition Temperature Excipients to Minimize Amorphization of Sulfadimidine on Comilling

Curtin

Amharar

et al. 2012

Mol. Pharmaceutics

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The co-processing of active pharmaceutical ingredient (API) with an excipient which has a high glass transition temperature (Tg) is a recognised strategy to stabilise the amorphous form of a drug. This work investigates whether co-processing a model API, sulfadimidine (SDM) with a series of low Tg excipients prevents or reduces amorphisation of the crystalline drug. It was hypothesised that these excipients could exert a Tg lowering effect, resulting in composite Tg values lower than that of the API alone and promote crystallisation of the drug. Milled SDM and co-milled SDM with glutaric acid (GA), adipic acid (AA), succinic acid (SA) and malic acid (MA) were characterised with respect to their thermal, X-Ray diffraction, spectroscopic and vapour sorption properties.SDM was predominantly amorphous when milled alone, with an amorphous content of 82 %.No amorphous content was detected by dynamic vapour sorption (DVS) on co-milling SDM with 50 % w/w GA, and amorphous content of the API was reduced by almost 30 %, relative to the API milled alone, on co-milling with 50 % w/w AA. In contrast, amorphisation of SDM was promoted on co-milling with 50 % w/w SA and MA, as indicated by near infrared (NIR) 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 2 spectroscopy. Results indicated that the API was completely amorphised in the SDM:MA comilled composite.The saturated solubility of GA and AA in the amorphous API was estimated by thermal methods.It was observed that the Tg of the co-melt quenched composites reached a minimum and levelled out at this solubility concentration. Maximum crystallinity of API on co-milling was reached at excipient concentrations comparable to the saturated concentration solubility of excipient in the API. Moreover, the closer the Hildebrand solubility parameter of the excipient to the API, the greater was the inhibition of API amorphisation on co-milling.The results reported here indicate that an excipient with a low Tg coupled with high solubility in the API can prevent or reduce the generation of an amorphous phase on co-milling.

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“…DSC studies have revealed the atypical bimodal crystallization of milled amorphous griseofulvin wherein the first exotherm occur prior to the T g (Trasi and Byrn 2012;Trasi et al 2010;Willart et al 2012). Such behavior was also noticed for other milled amorphous form of felodipine, sulfamerazine, piroxicam, hydrochlorothiazide (Chattoraj et al 2012).…”

Section: Crystallization Melting Crystallinity and Mixing Interactmentioning

confidence: 85%

Structural Characterization of Amorphous Solid Dispersions

Paudel

Meeus

Mooter

2014

Advances in Delivery Science and Technology

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Solid-State Vitrification of Crystalline Griseofulvin by Mechanical Milling

Cited by 46 publications

References 29 publications

Use of low-frequency Raman spectroscopy and chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets

Use of low-frequency Raman spectroscopy and chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets

Investigation of the Capacity of Low Glass Transition Temperature Excipients to Minimize Amorphization of Sulfadimidine on Comilling

Structural Characterization of Amorphous Solid Dispersions

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