UV imaging in pharmaceutical analysis

Østergaard, Jesper

doi:10.1016/j.jpba.2017.07.055

Cited by 40 publications

(28 citation statements)

References 90 publications

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“…The red rectangular insert in Figure 7a also depicts the initial higher IDR values that can alter reliable IDR values thereby highlighting the relevance of the use of the infinite focus variation microscope. A slight decrease in IDR over time with this imaging technique and the shape of the IDR plots as seen in Figure 7 have been observed by other authors and could account for some of the differences in values between the 10 min and 30 min time points (Hulse et al, 2012;Østergaard, 2018). This work therefore brings to light the fact that the actual disc surface in the IDR runs may not be a uniform smooth surface as thought when geometric assessment of the surface area for IDR calculations in the traditional way are conducted.…”

Section: Intrinsic Dissolution Ratesupporting

confidence: 77%

Direct imaging of the dissolution of salt forms of a carboxylic acid drug

Asare-Addo

Walton

Ward

et al. 2018

International Journal of Pharmaceutics

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The optimisation of the pharmaceutical properties of carboxylic acid drugs is often conducted by salt formation. Often, the salt with the best solubility is not chosen due to other factors such as stability, solubility, dissolution and bioavailability that are taken into consideration during the preformulation stage. This work uses advanced imaging techniques to give insights into the preformulation properties that can aid in the empirical approach often used in industry for the selection of salts. Gemfibrozil (GEM) was used as a model poorly soluble drug. Four salts of GEM were made using cyclopropylamine (CPROP), cyclobutylamine (CBUT), cyclopentylamine (CPENT) and cyclohexylamine (CHEX) as counterions. DSC, XRD and SEM were used to confirm and characterise salt formation. IDR obtained using UV-imaging up to 10 min for all the salts showed that an increase in the chain length of the counterion caused a decrease in the IDR. Past the 10 min mark, there was an increase in the IDR value for the CPROP salt, which was visualised using UV-imaging. The developed interfacial (surface) area ratio (Sdr) showed significant surface gains for the compacts. Full dosage form (capsule) imaging showed an improvement over the GEM for all the salts with an increase in chain length of the counterion bringing about a decrease in dissolution which correlated with the obtained UV-imaging IDR data.

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Section: Intrinsic Dissolution Ratesupporting

confidence: 77%

Direct imaging of the dissolution of salt forms of a carboxylic acid drug

Asare-Addo

Walton

Ward

et al. 2018

International Journal of Pharmaceutics

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“…Therefore, much research effort over the past two decades has been devoted to developing miniaturized experimental assays that allow for high throughput measurements of solubility and dissolution rate using small amounts of starting material. The main approaches and equipment available are (i) miniaturized dissolution vessels, flow-through cells, or microtiter plate-based methods with off-line determination of API concentration changes [8], (ii) imaging-based methods [9], and (iii) small-scale (sometimes) automated dissolution instruments with in situ API concentration determination by UV fiber optic probes [10][11][12][13]. The interested reader is referred to a recent review for a comprehensive description of all methods relevant for IDR determinations [3].…”

Section: Introductionmentioning

confidence: 99%

Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds in Biorelevant Dissolution Media

2020

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The intrinsic dissolution rate (IDR) of active pharmaceutical ingredients (API) is a key property that aids in early drug development, especially selecting formulation strategies to improve dissolution and thereby drug absorption in the intestine. Here, we developed a robust method for rapid, medium throughput screening of IDR and established the largest IDR dataset in open literature to date that can be used for pharmaceutical computational modeling. Eighteen compounds with diverse physicochemical properties were studied in both fasted and fed state simulated intestinal fluids. Dissolution profiles were measured in small-scale experimental assays using compound suspensions or discs. IDR measurements were not solely linked to API solubility in either dissolution media. Multivariate data analysis revealed that IDR strongly depends on compound partitioning into bile salt and phospholipid micelles in the simulated intestinal fluids, a process that in turn is governed by API lipophilicity, hydrophobicity, and ionization.

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“…The surface UV dissolution imaging is applicable as most pharmaceutical drug substances contain a UV chromophore. The intensity of the measured light is converted to absorbance, creating a high-resolution, real-time 2D absorbance and concentration map of dissolution events within the flow cell which presents a detailed view of the dissolution process occurring on the surface of the drug compact (25). 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).…”

Section: Introductionmentioning

confidence: 99%

“…Using this system, temporal and high-resolution spatial data from the solid–liquid interface can be observed. Measurement of this dissolution process has been described in length in the literature (19,22,25,29), and it offers insight into surface events such as boundary layer thickness, surface concentration, contour distribution, concentration gradient profiles and surface changes from swelling or gelling. The ActiPix™ SDI300 also supplies special insights into processes occurring in microns to millimetres from the surface, the crucial distance range for recognising dissolution.…”

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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UV imaging in pharmaceutical analysis

Cited by 40 publications

References 90 publications

Direct imaging of the dissolution of salt forms of a carboxylic acid drug

Direct imaging of the dissolution of salt forms of a carboxylic acid drug

Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds in Biorelevant Dissolution Media

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

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