Real-time UV imaging identifies the role of pH in insulin dissolution behavior in hydrogel-based subcutaneous tissue surrogate

Jensen, Sabrine S.; Jensen, Henrik; Cornett, Claus; Möller, E; Østergaard, Jesper

doi:10.1016/j.ejps.2014.12.015

Cited by 22 publications

(11 citation statements)

References 55 publications

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“…The study showed that the dissolved lidocaine seems to gather at the bottom of the quartz cell, which may be explained by the formation of a density gradient as lidocaine dissolves leading to natural convection [16]. Hydrogel matrixes have been shown to suppress natural convection due to density gradients [43,[48][49][50]. In the current study, the effect of introducing a 0.5% (w/v) agarose hydrogel at pH 7.4 as a dissolution medium on the dissolution behavior of a single lidocaine crystal under stagnant conditions was visualized.…”

Section: Effects Of Hydrogels On Density Effectsmentioning

confidence: 99%

Performance characteristics of UV imaging instrumentation for diffusion, dissolution and release testing studies

Jensen

Goodall

et al. 2016

Journal of Pharmaceutical and Biomedical Analysis

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UV imaging is capable of providing spatially and temporally resolved absorbance measurements, which is highly beneficial in drug diffusion, dissolution and release testing studies. For optimal planning and design of experiments, knowledge about the capabilities and limitations of the imaging system is required. The aim of this study was to characterize the performance of two commercially available UV imaging systems, the D100 and SDI. Lidocaine crystals, lidocaine containing solutions, and gels were applied in the practical assessment of the UV imaging systems. Dissolution of lidocaine from single crystals into phosphate buffer and 0.5% (w/v) agarose hydrogel at pH 7.4 was investigated to shed light on the importance of density gradients under dissolution conditions in the absence of convective flow. In addition, the resolution of the UV imaging systems was assessed by the use of grids. Resolution was found to be better in the vertical direction than the horizontal direction, consistent with the illumination geometry. The collimating lens in the SDI imaging system was shown to provide more uniform light intensity across the UV imaging area and resulted in better resolution as compared to the D100 imaging system (a system without a lens). Under optimal conditions, the resolution was determined to be 12.5 and 16.7 line pairs per mm (lp/mm) corresponding to line widths of 40μm and 30μm in the horizontal and vertical direction, respectively. Overall, the performance of the UV imaging systems was shown mainly to depend on collimation of light, the light path, the positioning of the object relative to the line of 100μm fibres which forms the light source, and the distance of the object from the sensor surface.

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Section: Effects Of Hydrogels On Density Effectsmentioning

confidence: 99%

Performance characteristics of UV imaging instrumentation for diffusion, dissolution and release testing studies

Jensen

Goodall

et al. 2016

Journal of Pharmaceutical and Biomedical Analysis

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“…The data can then be processed for measurement of the intrinsic dissolution rate (IDR) of the active compound (pure API or formulation), with the whole process typically taking around 20 min (26,27). The ActiPix™ SDI300 is a multipurpose UV area imaging system which enables quantitative imaging of surface dissolution for various applications such as pure active compound (19,21,23), transdermal patch (20), crystal (22,28), gels (29,30), polymer (31), cocrystal (32–34), excipient shielding (35), salt (36), drug-phospholipid complexes (37), oral strip film (38) and oily liquid (39). Using this system, temporal and high-resolution spatial data from the solid–liquid interface can be observed.…”

Section: Introductionmentioning

confidence: 99%

Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation

Long

Tang²,

Chokshi

et al. 2019

AAPS PharmSciTech

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The aim of this study is to investigate the dissolution properties of poorly soluble drugs from their pure form and their amorphous formulation under physiological relevant conditions for oral administration based on surface dissolution ultraviolet (UV) imaging. Dissolution of two poorly soluble drugs (cefuroxime axetil and itraconazole) and their amorphous formulations (Zinnat ® and Sporanox ® ) was studied with the Sirius Surface Dissolution Imager (SDI). Media simulating the fasted state conditions (compendial and biorelevant) with sequential media/flow rate change were used. The dissolution mechanism of cefuroxime axetil in simulated gastric fluid (SGF), fasted state simulated gastric fluid (FaSSGF) and simulated intestinal fluid (SIF) is predominantly swelling as opposed to the convective flow in fasted state simulated intestinal fluid (FaSSIF-V1), attributed to the effect of mixed micelles. For the itraconazole compact in biorelevant media, a clear upward diffusion of the dissolved itraconazole into the bulk buffer solution is observed. Dissolution of itraconazole from the Sporanox ® compact is affected by the polyethylene glycol (PEG) gelling layer and hydroxypropyl methylcellulose (HPMC) matrix, and a steady diffusional dissolution pattern is revealed. A visual representation and a quantitative assessment of dissolution properties of poorly soluble compounds and their amorphous formulation can be obtained with the use of surface dissolution imaging under in vivo relevant conditions.

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“…In vitro platforms capable of predicting bio-performance of parenteral depots for administration into soft tissue are desirable in formulation development. UV imaging-based approaches incorporating a hydrogel matrix as soft tissue model has been proposed for characterization of such depot systems [86][87][88][89][90][91][92].…”

Section: Parenteral Adminstrationmentioning

confidence: 99%

“…The selfassociation properties of human insulin were reflected in the diffusional transport, essentially determining the hydrodynamic radii corresponding to the insulin monomer, dimer and hexamer from the diffusion measurements conducted by UV imaging [90]. Changes in pH of the surrounding microenvironment during dissolution of amorphous insulin in agarose matrixes at pH 3.0, 5.4 and 7.4 [91] were investigated using the pH indicator method previously introduced [55]. Local pH changes reflecting protonation and deprotonation of dissolved insulin molecules were proposed to explain anomalous insulin dissolution profiles.…”

Section: Parenteral Adminstrationmentioning

confidence: 99%

Application of UV Imaging in Formulation Development

Sun

Østergaard

2016

Pharm Res

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Efficient drug delivery is dependent on the drug substance dissolving in the body fluids, being released from dosage forms and transported to the site of action. A fundamental understanding of the interplay between the physicochemical properties of the active compound and pharmaceutical excipients defining formulation behavior after exposure to the aqueous environments and pharmaceutical performance is critical in pharmaceutical development, manufacturing and quality control of drugs. UV imaging has been explored as a tool for qualitative and quantitative characterization of drug dissolution and release with the characteristic feature of providing real-time visualization of the solution phase drug transport in the vicinity of the formulation. Events occurring during drug dissolution and release, such as polymer swelling, drug precipitation/recrystallization, or solvent-mediated phase transitions related to the structural properties of the drug substance or formulation can be monitored. UV imaging is a non-intrusive and simple-to-operate analytical technique which holds potential for providing a mechanistic foundation for formulation development. This review aims to cover applications of UV imaging in the early and late phase pharmaceutical development with a special focus on the relation between structural properties and performance. Potential areas of future advancement and application are also discussed.

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Real-time UV imaging identifies the role of pH in insulin dissolution behavior in hydrogel-based subcutaneous tissue surrogate

Cited by 22 publications

References 55 publications

Performance characteristics of UV imaging instrumentation for diffusion, dissolution and release testing studies

Performance characteristics of UV imaging instrumentation for diffusion, dissolution and release testing studies

Surface Dissolution UV Imaging for Investigation of Dissolution of Poorly Soluble Drugs and Their Amorphous Formulation

Application of UV Imaging in Formulation Development

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