Solid-state characterization of Felodipine–Soluplus amorphous solid dispersions

Jiannan LuDepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, the University of Mississippi, University, MS, USA,

Kristina CuellarDepartment of Chemistry and Biochemistry, The University of Mississippi, University, MS, USA,

Nathan I. HammerDepartment of Chemistry and Biochemistry, The University of Mississippi, University, MS, USA,

Seongbong JoDepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, the University of Mississippi, University, MS, USA,

Andreas GryczkeBASF SE, Global Development and Technical Marketing, Ludwigshafen, Germany,

Karl KolterBASF SE, R&D Product Management Excipients, Ludwigshafen, Germany,

Nigel LangleyBASF Corporation, Tarrytown, NY, USA, and

Michael A. RepkaDepartment of Pharmaceutics and Drug Delivery, School of Pharmacy, the University of Mississippi, University, MS, USA, ;Pii Center for Pharmaceutical Technology, School of Pharmacy, the University of Mississippi, University, MS, USACorrespondence[email protected]

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Abstract

The aim of the current study is to develop amorphous solid dispersion (SD) via hot melt extrusion technology to improve the solubility of a water-insoluble compound, felodipine (FEL). The solubility was dramatically increased by preparation of amorphous SDs via hot-melt extrusion with an amphiphilic polymer, Soluplus® (SOL). FEL was found to be miscible with SOL by calculating the solubility parameters. The solubility of FEL within SOL was determined to be in the range of 6.2–9.9% (w/w). Various techniques were applied to characterize the solid-state properties of the amorphous SDs. These included Fourier Transform Infrared Spectrometry spectroscopy and Raman spectroscopy to detect the formation of hydrogen bonding between the drug and the polymer. Scanning electron microscopy was performed to study the morphology of the SDs. Among all the hot-melt extrudates, FEL was found to be molecularly dispersed within the polymer matrix for the extrudates containing 10% drug, while few small crystals were detected in the 30 and 50% extrudates. In conclusion, solubility of FEL was enhanced while a homogeneous SD was achieved for 10% drug loading.

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Declaration of interest

The authors would like to thank the Pii Center for Pharmaceutical Technology and Grant Number P20GM104932 from the National Institute of General Medical Sciences (NIGMS), a component of NIH for contributions to this project.

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Solid-state characterization of Felodipine–Soluplus amorphous solid dispersions

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Solid-state characterization of Felodipine–Soluplus amorphous solid dispersions

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