Preparation of Co-Amorphous Systems by Freeze-Drying
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Preparation of Co-Amorphous Systems by Freeze-Drying. / Wostry, Melvin; Plappert, Hanna; Grohganz, Holger.
In: Pharmaceutics, Vol. 12, No. 10, 941, 2020.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Preparation of Co-Amorphous Systems by Freeze-Drying
AU - Wostry, Melvin
AU - Plappert, Hanna
AU - Grohganz, Holger
PY - 2020
Y1 - 2020
N2 - Freeze-drying was evaluated as a production technique for co-amorphous systems of a poorly water-soluble drug. Naproxen was freeze-dried together with arginine and lysine as co-former. To increase the solubility of naproxen in the starting solution, the applicability of five surfactants was investigated, namely sodium dodecyl sulfate, pluronic F-127, polyoxyethylene (40) stearate, tween 20 and TPGS 1000. The influence of the surfactant type, surfactant concentration and total solid content to be freeze-dried on the solid state of the sample was investigated. X-ray powder diffraction and differential scanning calorimetry showed that the majority of systems formed co-amorphous one-phase systems. However, at higher surfactant concentrations, and depending on the surfactant type, surfactant reflections were observed in the XRPD analysis upon production. Crystallization of both naproxen and amino acid occurred from some combinations under storage. In conclusion, freeze-drying was shown to be a feasible technique for the production of a selection of co-amorphous drug-amino acid formulations.
AB - Freeze-drying was evaluated as a production technique for co-amorphous systems of a poorly water-soluble drug. Naproxen was freeze-dried together with arginine and lysine as co-former. To increase the solubility of naproxen in the starting solution, the applicability of five surfactants was investigated, namely sodium dodecyl sulfate, pluronic F-127, polyoxyethylene (40) stearate, tween 20 and TPGS 1000. The influence of the surfactant type, surfactant concentration and total solid content to be freeze-dried on the solid state of the sample was investigated. X-ray powder diffraction and differential scanning calorimetry showed that the majority of systems formed co-amorphous one-phase systems. However, at higher surfactant concentrations, and depending on the surfactant type, surfactant reflections were observed in the XRPD analysis upon production. Crystallization of both naproxen and amino acid occurred from some combinations under storage. In conclusion, freeze-drying was shown to be a feasible technique for the production of a selection of co-amorphous drug-amino acid formulations.
KW - co-amorphous
KW - freeze-drying
KW - surfactant
KW - WATER-SOLUBLE DRUGS
KW - AMINO-ACIDS
KW - ENHANCED DISSOLUTION
KW - BINARY-SYSTEMS
KW - STABILITY
KW - FORMULATIONS
KW - SOLUBILITY
KW - SACCHARIN
KW - BEHAVIOR
KW - IMPROVE
U2 - 10.3390/pharmaceutics12100941
DO - 10.3390/pharmaceutics12100941
M3 - Journal article
C2 - 33008124
VL - 12
JO - Pharmaceutics
JF - Pharmaceutics
SN - 1999-4923
IS - 10
M1 - 941
ER -
ID: 251313067