Application of Theoretical Solubility Calculations and Thermal and Spectroscopic Measurements to Guide the Processing of Triamcinolone Acetonide by Hot-Melt Extrusion DOI Creative Commons
Pedro A. Granados, Idejan P. Gross, Patrícia Medeiros de Souza

и другие.

Pharmaceutics, Год журнала: 2025, Номер 17(5), С. 586 - 586

Опубликована: Апрель 29, 2025

Background/Objectives: Triamcinolone acetonide (TA), a poorly water-soluble corticosteroid, presents formulation challenges due to limited membrane permeability. This study aimed identify suitable drug–polymer–plasticizer systems for TA using combined theoretical and experimental methods. Methods: Using Hansen solubility parameters, seven hot-melt extrusion (HME)-grade polymers four plasticizers were initially screened miscibility with TA. Based on Δδt values, polymers—Eudragit® L100 (EUD), Parteck® MXP (PVA), Plasdone® S-630 (PVPVA), Aquasolve™ AS-MG (HPMCAS)—along triethyl citrate (TEC), selected evaluation. Differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy assessed thermal behavior, miscibility, chemical compatibility. Results: Amorphous content was highest EUD (81.1%), followed by PVA (67.5%), PVPVA (45.6%), HPMCAS (8.5%). Thermal incompatibility TEC evaporation observed in PVA, PVPVA, systems. FTIR suggested should be avoided melt-based formulations degradation partial oxidation. No significant interactions detected samples heated 220 °C, aligning predictions. In contrast, the EUD–TEC system showed reactivity maintained TA’s structural integrity. Infrared bands at 1758 1802 cm−1 indicated minor anhydride formation above 160 °C evaporation. Conclusions: EUD/TEC identified as promising combination HME processing of work supports rational stable amorphous thermolabile drugs poor solubility.

Язык: Английский

Application of Theoretical Solubility Calculations and Thermal and Spectroscopic Measurements to Guide the Processing of Triamcinolone Acetonide by Hot-Melt Extrusion DOI Creative Commons
Pedro A. Granados, Idejan P. Gross, Patrícia Medeiros de Souza

и другие.

Pharmaceutics, Год журнала: 2025, Номер 17(5), С. 586 - 586

Опубликована: Апрель 29, 2025

Background/Objectives: Triamcinolone acetonide (TA), a poorly water-soluble corticosteroid, presents formulation challenges due to limited membrane permeability. This study aimed identify suitable drug–polymer–plasticizer systems for TA using combined theoretical and experimental methods. Methods: Using Hansen solubility parameters, seven hot-melt extrusion (HME)-grade polymers four plasticizers were initially screened miscibility with TA. Based on Δδt values, polymers—Eudragit® L100 (EUD), Parteck® MXP (PVA), Plasdone® S-630 (PVPVA), Aquasolve™ AS-MG (HPMCAS)—along triethyl citrate (TEC), selected evaluation. Differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy assessed thermal behavior, miscibility, chemical compatibility. Results: Amorphous content was highest EUD (81.1%), followed by PVA (67.5%), PVPVA (45.6%), HPMCAS (8.5%). Thermal incompatibility TEC evaporation observed in PVA, PVPVA, systems. FTIR suggested should be avoided melt-based formulations degradation partial oxidation. No significant interactions detected samples heated 220 °C, aligning predictions. In contrast, the EUD–TEC system showed reactivity maintained TA’s structural integrity. Infrared bands at 1758 1802 cm−1 indicated minor anhydride formation above 160 °C evaporation. Conclusions: EUD/TEC identified as promising combination HME processing of work supports rational stable amorphous thermolabile drugs poor solubility.

Язык: Английский

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