The amorphous state of pharmaceuticals obtained or transformed by milling: Sub-Tg features and rejuvenation

Descamps, Marc; Aumelas, A.; Desprez, Sylvain; willart, Jean-François

doi:10.1016/j.jnoncrysol.2014.08.055

Cited by 32 publications

(30 citation statements)

References 46 publications

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“…Thus, the life expectancy of the amorphous state has to be addressed and optimized to secure protocols of formulation (Bhugra and Pikal, 2008). In recent years, a great effort has been dedicated to the study of "crystal to glass transformation" induced by milling (Wojnarowska et al, 2013) (Descamps et al, 2015). To date, a streamlining of transformations reached by milling has not been attained even if some empirical rules are emerging from current investigations (Dujardin et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

“…Moreover, it has been reported that the higher the milling intensity, the better the efficiency of the amorphization process (Desprez and Descamps, 2006). In this way, we used the opportunity provided by molecular compounds to have their glass transition temperature located near room temperature to investigate the importance of the milling temperature with respect to T g .…”

Section: Introductionmentioning

confidence: 99%

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Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Schammé

Couvrat

Malpeli³

et al. 2016

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Schammé

Couvrat

Malpeli³

et al. 2016

International Journal of Pharmaceutics

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“…During the highly energy‐excited process, crystalline Ag 2 S and P 2 S 5 react with each other, leading to the formation of Ag 3 PS 4 glass. The milling approach has been applied to prepare glassy powder for energy storage, electrochemical devices, pharmaceutical manufacturing, etc . Despite some progress in studying the milling process, the mechanism of the milling‐derived amorphization has not been well understood.…”

Section: Introductionmentioning

confidence: 99%

Sub‐T_g enthalpy relaxation in a milling‐derived chalcogenide glass

2016

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In this work we succeeded in synthesizing a chalcogenide glass, that is, the Ag3PS4 glass, by milling the mixture of the crystalline Ag2S and P2S5 powder. In terms of potential energy, the glass was excited by the milling process. The evidence for the energy excitation was the occurrence of the sub‐Tg relaxation recorded by a differential scanning calorimeter (DSC). The relaxation behavior in the milling‐derived Ag3PS4 glass was found to significantly differ from that of a hyperquenched oxide glass. We observed two decoupled peaks of the energy release during a DSC scan, which are in contrast to the single asymmetric peak of the hyperquenched glass. The low‐temperature peak could be attributed to the β‐relaxation of the Ag–S ionic bonds, whereas the high‐temperature peak could arise from the α‐relaxation of the distorted rigid [PS4] units involving covalent bonds. The decoupling between the two peaks implies the fragile nature of the Ag3PS4 glass. Upon the dynamic heating and the sub‐Tg annealing we found that the relaxation of the Ag3PS4 glass is of high nonexponentiallity, and hence, of high structural heterogeneity.

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“…Nevertheless, when utilizing co-grinding method, there is one thing worthy of being considered. Solely grinding drug without excipient (mono-grinding) may also destroy the drug crystal structure by shear force, even into amorphous forms2829, then make more or less effect. Thus, to verify the effects of co-grinding on the drug properties were caused by the adding of macrocycles, the effect of mono-grinding on drug must be excluded.…”

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confidence: 99%

Co-grinding Effect on Crystalline Zaltoprofen with β-cyclodextrin/Cucurbit[7]uril in Tablet Formulation

Lin

et al. 2017

Sci Rep

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This work aimed to investigate the co-grinding effects of β-cyclodextrin (β-CD) and cucurbit[7]uril (CB[7]) on crystalline zaltoprofen (ZPF) in tablet formulation. Crystalline ZPF was prepared through anti-solvent recrystallization and fully analyzed through single-crystal X-ray diffraction. Co-ground dispersions and mono-ground ZPF were prepared using a ball grinding process. Results revealed that mono-ground ZPF slightly affected the solid state, solubility, and dissolution of crystalline ZPF. Co-ground dispersions exhibited completely amorphous states and elicited a significant reinforcing effect on drug solubility. UV-vis spectroscopy, XRPD, FT-IR, DSC, ssNMR, and molecular docking demonstrated the interactions in the amorphous product. Hardness tests on blank tablets with different β-CD and CB[7] contents suggested the addition of β-CD or CB[7] could enhance the compressibility of the powder mixture. Disintegration tests showed that CB[7] could efficiently shorten the disintegrating time. Dissolution tests indicated that β-CD and CB[7] could accelerate the drug dissolution rate via different mechanisms. Specifically, CB[7] could accelerate the dissolution rate by improving disintegration and β-CD showed a distinct advantage in solubility enhancement. Based on the comparative study on β-CD and CB[7] for tablet formulation combined with co-grinding, we found that CB[7] could be considered a promising drug delivery, which acted as a disintegrant.

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The amorphous state of pharmaceuticals obtained or transformed by milling: Sub-Tg features and rejuvenation

Cited by 32 publications

References 46 publications

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Sub‐T_g enthalpy relaxation in a milling‐derived chalcogenide glass

Co-grinding Effect on Crystalline Zaltoprofen with β-cyclodextrin/Cucurbit[7]uril in Tablet Formulation

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The amorphous state of pharmaceuticals obtained or transformed by milling: Sub-Tg features and rejuvenation

Cited by 32 publications

References 46 publications

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol

Sub‐Tg enthalpy relaxation in a milling‐derived chalcogenide glass

Co-grinding Effect on Crystalline Zaltoprofen with β-cyclodextrin/Cucurbit[7]uril in Tablet Formulation

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Sub‐T_g enthalpy relaxation in a milling‐derived chalcogenide glass