Amorphous-Amorphous Phase Separation in API/Polymer Formulations
Copyright policy )Amorphous-Amorphous Phase Separation in API/Polymer Formulations
The long-term stability of pharmaceutical formulations of poorly-soluble drugs in polymers determines their bioavailability and therapeutic applicability. However, these formulations do not only often tend to crystallize during storage, but also tend to undergo unwanted amorphous-amorphous phase separations (APS). Whereas the crystallization behavior of APIs in polymers has been measured and modeled during the last years, the APS phenomenon is still poorly understood. In this study, the crystallization behavior, APS, and glass-transition temperatures formulations of ibuprofen and felodipine in polymeric PLGA excipients exhibiting different ratios of lactic acid and glycolic acid monomers in the PLGA chain were investigated by means of hot-stage microscopy and DSC. APS and recrystallization was observed in ibuprofen/PLGA formulations, while only recrystallization occurred in felodipine/PLGA formulations. Based on a successful modeling of the crystallization behavior using the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT), the occurrence of APS was predicted in agreement with experimental findings.
- TU Dortmund University Germany
poorly water-soluble drug; amorphous solid dispersion; PLGA; thermodynamic model; phase behavior; amorphous-amorphous phase separation, thermodynamic model, info:eu-repo/classification/ddc/660, Polymers, Drug Compounding, Organic chemistry, Chemical Fractionation, Poorly water-soluble drug, Article, QD241-441, amorphous solid dispersion, phase behavior, Transition Temperature, Amorphous solid dispersion, amorphous-amorphous phase separation, Amorphous-amorphous phase separation, Calorimetry, Differential Scanning, Molecular Structure, 660, poorly water-soluble drug, PLGA, Thermodynamic model, Models, Chemical, Pharmaceutical Preparations, Solubility, Thermodynamics, Phase behavior, Algorithms
poorly water-soluble drug; amorphous solid dispersion; PLGA; thermodynamic model; phase behavior; amorphous-amorphous phase separation, thermodynamic model, info:eu-repo/classification/ddc/660, Polymers, Drug Compounding, Organic chemistry, Chemical Fractionation, Poorly water-soluble drug, Article, QD241-441, amorphous solid dispersion, phase behavior, Transition Temperature, Amorphous solid dispersion, amorphous-amorphous phase separation, Amorphous-amorphous phase separation, Calorimetry, Differential Scanning, Molecular Structure, 660, poorly water-soluble drug, PLGA, Thermodynamic model, Models, Chemical, Pharmaceutical Preparations, Solubility, Thermodynamics, Phase behavior, Algorithms
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