Methotrexate: Existence of different types of solid

Chan, Hak‐Kim; Gonda, Igor

doi:10.1016/0378-5173(91)90140-j

Cited by 14 publications

(3 citation statements)

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“…The number of water molecules into unit cells could possibly range from two to four molecules in available commercial MTX [ 35 ]. In addition, thermal analysis indicated a characteristic dehydrate form with water loss at about 7.6 wt %, which was confirmed by XRD due to the characteristically well-defined diffraction peaks at 7.66 and 9.24, respectively [ 34 ].…”

Section: Resultsmentioning

confidence: 99%

“…This endothermic event (Δ H = 71 J·g −1 ) was observed in the DSC curve in the same temperature range. However, some author shave described the identification of two possible hydrate forms such as trihydrate and tetrahydrate [ 34 , 35 , 36 ]. An endothermic phase transition was observed in the range of 163–239 °C, which was attributed to the melting of a crystalline form, which was followed afterwards by thermal decomposition.…”

Section: Resultsmentioning

confidence: 99%

“…The presence of some MTX tetragonal crystals was confirmed by XRD analysis ( Figure 6 b). An anterior study performed by Hak-Kim and Gonda [ 34 ] described two different crystalline habits of a stable pseudopolimorphous (hydrate) with tetragonal crystalline form. The water content of these two hydrates indicated MTX crystals likely to be dihydrate (about 7.3 wt % H 2 O) and/or trihydrate (about 10.6 wt % H 2 O).…”

Section: Resultsmentioning

confidence: 99%

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Triethanolamine Stabilization of Methotrexate-β-Cyclodextrin Interactions in Ternary Complexes

Barbosa

Zoppi

Quevedo

et al. 2014

IJMS

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The interaction of methotrexate (MTX) with beta-cyclodextrin (β-CD) in the presence of triethanolamine (TEA) was investigated with the aim to elucidate the mechanism whereby self-assembly cyclodextrin systems work in association with this third component. Solubility diagram studies showed synergic increment of the MTX solubility to be about thirty-fold. Experiments using 2D ROESY and molecular modeling studies revealed the inclusion of aromatic ring III of the drug into β-CD cavity, in which TEA contributes by intensifying MTX interaction with β-CD and stabilizes MTX:β-CD:TEA ternary complex by electrostatic interaction. The maintenance of these interactions in solid phase was also studied in ternary MTX:β-CD:TEA and comparisons were made with freeze dried binary MTX:β-CD and physical mixtures. FTIR studies evidenced that MTX–β-CD interaction remained in solid ternary complexes, which was also supported by thermal (differential scanning calorimetry (DSC), thermogravimetric analysis (TG)/first derivative of TG analysis (DTG) and C,N,H elementary analysis) and structural (X-ray diffraction analysis, (XRD)) studies, mainly regarding the increment of drug stability. The efficient in vitro drug dissolution studies successfully demonstrated the contribution of ternary complexes, which highlights the importance of this possible new raw material for further applications in drug delivery systems.

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Section: Resultsmentioning

confidence: 99%