NDLI: Monitoring Polymorphic Phase Transitions in Flufenamic Acid Amorphous Solid Dispersions Using Hyphenated X-ray Diffraction-Differential Scanning Calorimetry.

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Monitoring Polymorphic Phase Transitions in Flufenamic Acid Amorphous Solid Dispersions Using Hyphenated X-ray Diffraction-Differential Scanning Calorimetry.

Content Provider	Europe PMC
Author	Pang, Yuying Buanz, Asma Gaisford, Simon Magdysyuk, Oxana V. Williams, Gareth R.
Copyright Year	2022
Abstract	Flufenamic acid (FFA) is a highlypolymorphic drug molecule withnine crystal structures reported in the Cambridge Structural Database.This study explores the use of synchrotron X-ray powder diffractioncombined with differential scanning calorimetry to study crystallizationand polymorphic phase transitions upon heating FFA–polymeramorphous solid dispersions (ASDs). Ethyl cellulose (EC, 4 cp) andhydroxypropylmethylcellulose (HPMC) grades with different viscositiesand substitution patterns were used to prepare dispersions with FFAat 5:1, 2:1, 1:1, and 1:5 w/w drug/polymer ratios by quench cooling.We employed a 6 cp HPMC 2910 material and two HPMC 2208 samples at4000 and 100 000 cp. Hyphenated X-ray diffraction (XRD)–differentialscanning calorimetry (DSC) studies show that the 6 and 100 000cp HPMCs and 4 cp EC polymers can stabilize FFA form IV by inhibitingthe transition to form I during heating. It appears that the polymersstabilize FFA in both amorphous and metastable forms via a combinationof intermolecular interactions and viscosity effects. Increasing thepolymer content of the ASD also inhibits polymorphic transitions,with drug/polymer ratios of 1:5 w/w resulting in FFA remaining amorphousduring heating. The comparison of FFA ASDs prepared with differentsamples of HPMCs and ECs suggests that the chemical substitution ofthe polymer (HPMC 2208 has 19–24% methoxy groups and 4–12%hydroxypropyl groups, while HPMC 2910 has 28–30% methoxy groupsand 7–12% hydroxypropyl groups) plays a more significant rolein directing polymorphic transitions than the viscosity. A previouslyunreported polymorph of FFA was also noted during heating but itsstructure could not be determined.
Related Links	https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC9097533&blobtype=pdf
ISSN	15438384
Journal	Molecular Pharmaceutics [Mol Pharm]
Volume Number	19
DOI	10.1021/acs.molpharmaceut.2c00016
PubMed Central reference number	PMC9097533
Issue Number	5
PubMed reference number	35347993
e-ISSN	15438392
Language	English
Publisher	American Chemical Society
Publisher Date	2022-03-29
Access Restriction	Open
Rights License	Permits the broadest form of re-use including for commercial purposes, provided that author attribution and integrity are maintained (https://creativecommons.org/licenses/by/4.0/). © 2022 American Chemical Society
Subject Keyword	amorphous solid dispersion hydroxypropylmethylcellulose ethyl cellulose flufenamic acid X-ray diffraction differential scanning calorimetry polymorphic transition
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Molecular Medicine Pharmaceutical Science

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