Comparison of pharmaceutical formulations: ATR-FTIR spectroscopic imaging to study drug-carrier interactions

Ewing, Andrew V.; Biggart, Gordon D.; Hale, Carwyn R.; Clarke, Graham S.; Kazarian, Sergei G.

doi:10.1016/j.ijpharm.2015.08.068

Cited by 31 publications

(12 citation statements)

References 45 publications

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“…The 3D image and IR reflectance spectrum of point of interest of SCS3 specifies the surface compositional homogeneity of EFV in pearlitol matrices. Use of FTIR imaging spectrum to understand distribution of API at microscale level been reported in literature previously (Alhijjaj et al, 2015;Ewing et al, 2015;Feng et al, 2015;Vo et al, 2016).…”

Section: Ftir Chemical Imaging Analysismentioning

confidence: 99%

Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate

Pawar

Fule

Maniruzzaman

et al. 2017

Materials Science and Engineering: C

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Poor aqueous solubility of drugs has emerged as a major issue for pharmaceutical scientists from many decades. The current study explores the manufacture and development of a thermodynamically stabilized solid crystal suspension (SCS) of poorly water soluble drug efavirenz via hot melt extrusion. Efavirenz is a non-nucleoside reverse transcriptase inhibitor and belongs to BCS class II. The SCS was prepared using pearlitol and xylitol as a crystalline carrier. The drug-excipient blend was processed by hot melt extrusion with up to 50% (w/w) drug loading. Physico-chemical characterization of the SCS conducted via a scanning electron microscopy, differential scanning calorimetry and hot stage microscopy confirmed that SCS are in crystalline state. Similarly, X-ray powder diffraction analysis revealed highly crystalline existence of pure drug, crystalline carriers and developed SCS. The FTIR chemical imaging analysis of SCS formulations showed a homogeneous drug distribution within respective crystalline carriers while an advanced chemical analysis via atomic force microscopy and Raman analysis complemented the foregoing findings. The developed SCS1 formulation showed up to 81 fold increase in the solubility and 4.1 fold increase in the dissolution rate of the drug compared to that of the bulk substance. Surprisingly, the developed SCS formulation remained stable for a period of more than one year at accelerated conditions inferred from dissolution studies. It can be concluded that the SCS approach can be used as an alternative contemporary technique to enhance the dissolution rates of many other poorly water-soluble drugs by means of thermal HME processing.

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Section: Ftir Chemical Imaging Analysismentioning

confidence: 99%

Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate

Pawar

Fule

Maniruzzaman

et al. 2017

Materials Science and Engineering: C

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“…This work presents specifically designed microfluidic devices that can be studied using macro-ATR-FTIR spectroscopic imaging to reveal important information about the behaviour of drug release. The reliability and robustness of ATR-FTIR spectroscopic imaging for the study of pharmaceutical tablets and formulations have been well established in recent years, 24,42,43 but this is the first time that micro-formulations have been studied in flowing channels.…”

Section: A Dissolution Of Micro-formulationsmentioning

confidence: 99%

Attenuated total reflection-Fourier transform infrared spectroscopic imaging of pharmaceuticals in microfluidic devices

2016

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The poor aqueous solubility of many active pharmaceutical ingredients presents challenges for effective drug delivery. In this study, the combination of attenuated total reflection (ATR)-FTIR spectroscopic imaging with specifically designed polydimethylsiloxane microfluidic devices to study drug release from pharmaceutical formulations has been developed. First, the high-throughput analysis of the dissolution of micro-formulations studied under flowing conditions has been introduced using a model formulation of ibuprofen and polyethylene glycol. The behaviour and release of the drug was monitored in situ under different pH conditions. In contrast to the neutral solution, where both the drug and excipient dissolved at a similar rate, structural change from the molecularly dispersed to a crystalline form of ibuprofen was characterised in the obtained spectroscopic images and the corresponding ATR-FTIR spectra for the experiments carried out in the acidic medium. Further investigations into the behaviour of the drug after its release from formulations (i.e., dissolved drug) were also undertaken. Different solutions of sodium ibuprofen dissolved in a neutral medium were studied upon contact with acidic conditions. The phase transition from a dissolved species of sodium ibuprofen to the formation of solid crystalline ibuprofen was revealed in the microfluidic channels. This innovative approach could offer a promising platform for high-throughput analysis of a range of micro-formulations, which are of current interest due to the advent of 3D printed pharmaceutical and microparticulate delivery systems. Furthermore, the ability to study dissolved drug in solution under flowing conditions can be useful for the studies of the diffusion of drugs into tissues or live cells.

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“…To this end, it is beneficial to combine standard USP-type dissolution tests with chemically specific, spectroscopic imaging-based analytical approaches such as attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopic imaging (21–24), magnetic resonance imaging (MRI) (25,26), UV imaging (27,28) and Raman imaging (29,30). These techniques allow the visualization of dynamic physico-chemical processes within a tablet under dissolution conditions, making it possible to elucidate phenomena that could not be easily identifiable from the USP release curve.…”

Section: Introductionmentioning

confidence: 99%

The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions

et al. 2016

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PurposeImaging methods were used as tools to provide an understanding of phenomena that occur during dissolution experiments, and ultimately to select the best ratio of two polymers in a matrix in terms of enhancement of the dissolution rate and prevention of crystallization during dissolution.MethodsMagnetic resonance imaging, ATR-FTIR spectroscopic imaging and Raman mapping have been used to study the release mechanism of a poorly water soluble drug, aprepitant, from multicomponent amorphous solid dispersions. Solid dispersions were prepared based on the combination of two selected polymers - Soluplus, as a solubilizer, and PVP, as a dissolution enhancer. Formulations were prepared in a ratio of Soluplus:PVP 1:10, 1:5, 1:3, and 1:1, in order to obtain favorable properties of the polymer carrier.ResultsThe crystallization of aprepitant during dissolution has occurred to a varying degree in the polymer ratios 1:10, 1:5, and 1:3, but the increasing presence of Soluplus in the formulation delayed the onset of crystallization. The Soluplus:PVP 1:1 solid dispersion proved to be the best matrix studied, combining the abilities of both polymers in a synergistic manner.ConclusionsAprepitant dissolution rate has been significantly enhanced. This study highlights the benefits of combining imaging methods in order to understand the release process.Electronic supplementary materialThe online version of this article (doi:10.1007/s11095-016-2018-x) contains supplementary material, which is available to authorized users.

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Comparison of pharmaceutical formulations: ATR-FTIR spectroscopic imaging to study drug-carrier interactions

Cited by 31 publications

References 45 publications

Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate

Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate

Attenuated total reflection-Fourier transform infrared spectroscopic imaging of pharmaceuticals in microfluidic devices

The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions

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