Simultaneous UV Imaging and Raman Spectroscopy for the Measurement of Solvent-Mediated Phase Transformations During Dissolution Testing

Østergaard, Jesper; Wu, Jian; Naelapää, Kaisa; Boetker, Johan; Jensen, Henrik; Rantanen, Jukka

doi:10.1002/jps.23883

Cited by 39 publications

(36 citation statements)

References 43 publications

(98 reference statements)

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“…In future studies, confirmation of form changes by analysis of the solid form remaining at the end of the experiment could provide a clear description of the product remaining after the dissolution. Additionally, the use of in situ Raman technology, which is increasingly being used in tandem with small-scale dissolution methodologies, would directly reveal the nature of such form changes as the experiment progresses (28).…”

Section: Discussionmentioning

confidence: 99%

Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration

et al. 2015

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Abstract. The purpose of this study was to better understand the dissolution properties and precipitation behavior of pharmaceutical cocrystals of poorly soluble drugs for the potential for oral administration based on a small-scale dissolution assay. Carbamazepine and indomethacin cocrystals with saccharin and nicotinamide as coformers were prepared with the sonic slurry method. Dissolution of the poorly soluble drugs indomethacin and carbamazepine and their cocrystals was studied with a small-scale dissolution assay installed on a SiriusT3 instrument. Two methodologies were used: (i) surface dissolution of pressed tablet (3 mm) in 20 mL running for fixed times at four pH stages (pH 1.8, pH 3.9, pH 5.4, pH 7.3) and (ii) powder dissolution (2.6 mg) in 2 mL at a constant pH (pH 2). Improved dissolution and useful insights into precipitation kinetics of poorly soluble compounds from the cocrystal form can be revealed by the smallscale dissolution assay. A clear difference in dissolution/precipitation behaviour can be observed based on the characteristics of the coformer used.

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Section: Discussionmentioning

confidence: 99%

Small-Scale Assays for Studying Dissolution of Pharmaceutical Cocrystals for Oral Administration

et al. 2015

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“…Therefore, it is of great importance to better understand the affect of a dissolution medium on the solid-state properties of the drug [174–176]. Østergaard et al [177] applied simultaneously UV imaging with in-situ Raman spectroscopy for the characterisation of drug dissolution and solid state transformation during dissolution. They demonstrated that sodium naproxen (Fig.…”

Section: Drug Release Kineticsmentioning

confidence: 99%

“…( c ) Fractional sodium naproxen/naproxen form conversion as a function of time. The fractions of intermediate solid form 1, intermediate solid form 2, intermediate solid form 3, and naproxen are represented as (▼), (•), (∘) and (△), respectively (modified from [177]). …”

Section: Drug Release Kineticsmentioning

confidence: 99%

A Review of Disintegration Mechanisms and Measurement Techniques

2017

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Pharmaceutical solid dosage forms (tablets or capsules) are the predominant form to administer active pharmaceutical ingredients (APIs) to the patient. Tablets are typically powder compacts consisting of several different excipients in addition to the API. Excipients are added to a formulation in order to achieve the desired fill weight of a dosage form, to improve the processability or to affect the drug release behaviour in the body. These complex porous systems undergo different mechanisms when they come in contact with physiological fluids. The performance of a drug is primarily influenced by the disintegration and dissolution behaviour of the powder compact. The disintegration process is specifically critical for immediate-release dosage forms. Its mechanisms and the factors impacting disintegration are discussed and methods used to study the disintegration in-situ are presented. This review further summarises mathematical models used to simulate disintegration phenomena and to predict drug release kinetics.

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“…UV imaging has earlier been shown to provide useful information regarding drug dissolution processes (Boetker et al 2011;Ostergaard et al 2014;Ostergaard et al 2010), and further serves as an excellent visualization method of the dissolution of furosemide in biorelevant media (Gordon et al 2013;Nielsen et al 2013b). In the current work, UV imaging was employed to visualize the release and dissolution of ASSF from Eudragit ® L100-coated microwells on a compressed timescale compared to the release studies conducted using a µ-Diss profiler.…”

Section: Figmentioning

confidence: 99%