Solvent shift method for anti-precipitant screening of poorly soluble drugs using biorelevant medium and dimethyl sulfoxide

Yamashita, Taro; Ozaki, Shunsuke; Kushida, Ikuo

doi:10.1016/j.ijpharm.2011.07.045

Cited by 64 publications

(34 citation statements)

References 18 publications

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“…[9,53] The miniaturised solvent-shift assay introduced by Yamashita et al is also interesting. [54] This method appears to be quite practical for studying excipient effects on drug precipitation and, as before, analytics are based on a subsequent HPLC step.…”

Section: Small-scale and Miniaturised Drug Dissolution Testing Using mentioning

confidence: 95%

Analytical technologies for real-time drug dissolution and precipitation testing on a small scale

Kuentz

2015

Journal of Pharmacy and Pharmacology

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Objectives This review focuses on real-time analytics of drug dissolution and precipitation testing on a comparatively small scale. Key findings Miniaturisation of test equipment is an important trend in pharmaceutics, and several small-scale experiments have been reported for drug dissolution and precipitation testing. Such tests typically employ analytics in realtime. Fibre optic ultraviolet (UV) analytics has become a well-established method in this field. Novel imaging techniques are emerging that use visible or UV light; also promising is Fourier transform infrared imaging based on attenuated total reflection. More information than just a rate constant is obtained from these methods. The early phase of a dissolution process can be assessed and drug precipitation may eventually be observed. Some real-time techniques are particularly well suited to studying drug precipitation during formulation dispersion; for example, turbidity, focused beam reflectance measurement and Raman spectroscopy. Summary Small-scale dissolution tests equipped with real-time analytics have become important to screen drug candidates as well as to study prototype formulations in early development. Future approaches are likely to combine different analytical techniques including imaging. Miniaturisation started with mini-vessels or small vials and future assays of dissolution research will probably more often reach the level of parallel well plates and microfluidic channels.

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Section: Small-scale and Miniaturised Drug Dissolution Testing Using mentioning

confidence: 95%

Analytical technologies for real-time drug dissolution and precipitation testing on a small scale

Kuentz

2015

Journal of Pharmacy and Pharmacology

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“…To evaluate the inhibitory effect of a polymer on the crystallization of supersaturated cilostazol using solvent-shift method, 35 we prepared a solution of cilostazol at 25 mg/mL in dimethyl sulfoxide (DMSO). To evaluate the inhibitory effect of a polymer on the crystallization of supersaturated cilostazol using solvent-shift method, 35 we prepared a solution of cilostazol at 25 mg/mL in dimethyl sulfoxide (DMSO).…”

Section: Preparation Of Hot-melt Extruded Amorphous Solidmentioning

confidence: 99%

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Lee

et al. 2019

Bulletin Korean Chem Soc

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“…To overcome this challenge, compounds are predissolved in an organic solvent such as dimethyl sulfoxide (DMSO) prior to dilution into the aqueous assay media. This can create a thermodynamically unstable supersaturated state [12] that can lead to precipitation or container surface adsorption [13,14].…”

Section: In Vitro Screening Support and Interpretationmentioning

confidence: 99%

Commentary: Why Pharmaceutical Scientists in Early Drug Discovery Are Critical for Influencing the Design and Selection of Optimal Drug Candidates

2017

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Abstract. This commentary reflects the collective view of pharmaceutical scientists from four different organizations with extensive experience in the field of drug discovery support. Herein, engaging discussion is presented on the current and future approaches for the selection of the most optimal and developable drug candidates. Over the past two decades, developability assessment programs have been implemented with the intention of improving physicochemical and metabolic properties. However, the complexity of both new drug targets and non-traditional drug candidates provides continuing challenges for developing formulations for optimal drug delivery. The need for more enabled technologies to deliver drug candidates has necessitated an even more active role for pharmaceutical scientists to influence many key molecular parameters during compound optimization and selection. This enhanced role begins at the early in vitro screening stages, where key learnings regarding the interplay of molecular structure and pharmaceutical property relationships can be derived. Performance of the drug candidates in formulations intended to support key in vivo studies provides important information on chemotype-formulation compatibility relationships. Structure modifications to support the selection of the solid form are also important to consider, and predictive in silico models are being rapidly developed in this area. Ultimately, the role of pharmaceutical scientists in drug discovery now extends beyond rapid solubility screening, early form assessment, and data delivery. This multidisciplinary role has evolved to include the practice of proactively taking part in the molecular design to better align solid form and formulation requirements to enhance developability potential.

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Solvent shift method for anti-precipitant screening of poorly soluble drugs using biorelevant medium and dimethyl sulfoxide

Cited by 64 publications

References 18 publications

Analytical technologies for real-time drug dissolution and precipitation testing on a small scale

Analytical technologies for real-time drug dissolution and precipitation testing on a small scale

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Commentary: Why Pharmaceutical Scientists in Early Drug Discovery Are Critical for Influencing the Design and Selection of Optimal Drug Candidates

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