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Volume 15, Issue 2
  • ISSN: 2210-3031
  • E-ISSN: 2210-304X

Abstract

Aims

The study aims to develop a 3rd generation amorphous solid dispersion (ASD) of Apremilast (APST) employing the Design of Experiment (DoE) methodology, followed by a thorough assessment including pharmacokinetics.

Background

APST, classified as a BCS-Class IV molecule due to its low solubility and permeability, exhibits highly variable oral bioavailability across different species.

Objectives

In this study, a 3rd generation ASD of APST was developed using the DoE approach.

Methods

The miscibility of APST within polymers was assessed using solubility parameters and Flory Huggin equation. Phase solubility studies were conducted to identify the most suitable polymer-surfactant combination for maximizing drug solubility. The produced solid dispersions were characterized using FTIR, DSC, XRD, DVS, and SEM.

Results

The combination of APST and Soluplus® in a 1:5 ratio resulted in the highest improvement in solubility and dissolution, with vitamin E TGPS being identified as the most efficient surfactant. Stability studies were carried out, and findings revealed that the ASD remained stable under accelerated conditions for up to 3 months, suggesting its suitability for scaling up for industrial applications. predictions of the pharmacokinetics of APST following oral administration of solid dispersion formulations were determined by PBBM using GastroPlus™.

Conclusion

The simulation of oral absorption profiles for APST showed a significant improvement in both Cmax and AUC for the solid dispersion formulations compared to plain drugs. This study makes a significant contribution to the field of pharmaceutical science by addressing the formulation complexities inherent in poorly water-soluble compounds like APST.

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2024-09-19
2025-06-17

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Apremilast Amorphous Solid Dispersions: Formulation Optimization using QbD and Comprehensive In vitro-In silico Assessment
Drug Deliv Lett 15, 110 (2025); https://doi.org/10.2174/0122103031309026240905115815
/content/journals/ddl/10.2174/0122103031309026240905115815
/content/journals/ddl/10.2174/0122103031309026240905115815
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  • Article Type:     Research Article
Keyword(s): Amorphous solid dispersion; apremilast; DoE; GastroPlus; population modelling; simulation
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