Sirius Analytical Ltd.

Newhaven, United Kingdom

Sirius Analytical Ltd.

Newhaven, United Kingdom

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Rafols C.,University of Barcelona | Bosch E.,University of Barcelona | Ruiz R.,Sirius Analytical Ltd. | Box K.J.,Sirius Analytical Ltd. | Ventura C.,Instituto Superior Of Educacao E Ciencias
Journal of Chemical and Engineering Data | Year: 2012

Hydrophobicity values (log P o/w) determined both by potentiometry and by the conventional shake-flask method and aqueous pK a values obtained by potentiometry for seven isoniazid and nine benzimidazole derivatives are presented. Several of these compounds have strong hydrophilic or hydrophobic character, and some of them show two or more ionizable sites, sometimes very acidic or very basic. These facts have compelled us to work near the limits of the potentiometric technique, and therefore, a critical evaluation of the results obtained in these extreme working conditions is presented. Particularly, details about the potentiometric determination of log P o/w values of the most hydrophilic and most hydrophobic compounds are clearly described. © 2011 American Chemical Society.


Grant
Agency: European Commission | Branch: H2020 | Program: MSCA-RISE | Phase: MSCA-RISE-2014 | Award Amount: 216.00K | Year: 2015

The CRYDIS exchange programme will establish and support international and inter-sectoral transfer of knowledge and expertise in pharmaceutical and instrument science between several EU research institutes and industrial companies. It will also enhance understanding of the value of inter-sectoral exchange mechanisms for taking research to market. CRYDIS undertakes innovative, collaborative research on the clinically-important topic of dissolution of drug substance particles in bio-relevant media and the undesired subsequent nucleation and re-precipitation of the drug prior to its absorption. Using innovative advances in UV imaging technology, CRYDIS investigates the utility of novel dissolution assays as key tools to obtain fundamental data on the mechanism and kinetics of undesired nucleation and re-precipitation during or following dissolution, a significant problem for the pharmaceutical industry which struggles to obtain sufficient exposure to poorly soluble drug substances to ensure an effective dose is absorbed by the patient. The key technologies in this proposal offer a step change in capability and functionality, offering the potential to undertake more detailed studies of the dissolution/re-precipitation processes relevant to pharmaceutical materials. Access to this key technology and the further development of its capability offers the potential for breakthroughs in development of process understanding and of robust and widely applicable protocols. Additional value is brought to CRYDIS through close working with synergistic European networks, leveraging a greater knowledge input and impact outreach. Running parallel with the science programme, an innovation management work-package analyses effectiveness of the exchange mechanism in building a shared culture, transferring knowledge and developing understanding of processes that drive a product to market. The outcomes of this will be used to advise and drive potential future exchange activities.


Grant
Agency: European Commission | Branch: H2020 | Program: MSCA-ITN-ETN | Phase: MSCA-ITN-2015-ETN | Award Amount: 3.90M | Year: 2016

The European Pharma industry is a major contributor to EU well-being, both in public health and economic (sales >200 billion /year) terms. To maintain global leadership, it must respond to challenges from low-cost producers e.g. China by bringing new drug molecules to market in a streamlined, cost-effective manner. This strategy is underscored by recent initiatives of European regulators to expedite the approval of breakthrough drugs so patients can gain earlier access to life-saving drugs. To realise these goals, scientists with an integral understanding of drug development and regulatory approval processes are urgently needed. PEARRL will train 15 Early Stage Researchers (ESR) who can develop new bio-enabling formulations (better drugs), biorelevant and in silico methods to predict formulation performance in vivo (streamlined development) and serve as communication bridgers between research and regulatory science (accelerated approval), thus bringing Pharma and regulatory objectives to fruition. PEARRL brings a multi-sectorial team, comprising key European regulatory authorities, academic leaders in bio-enabling formulations and biopharmaceutics tools, and an array of Pharma companies with a wealth of combined experience in bringing molecules to market, together for the first time to deliver a unique research and training programme. Key PEARRL elements are individual research projects with synergistic output; exposure of all ESR to academia, industry and regulatory in secondments; and ongoing innovative learning via Online Portals, Science Slams and Boot Camps. Key PEARRL impacts will be availability of excellent pharmaceutical researchers; streamlined drug development with a higher success rate for the industrial partners; enriched academic research through cooperation with industry and regulatory; earlier availability of breakthrough medicines to patients; a competitive pharma industry in Europe and contributions to European public health interests.


PubMed | Prosonix, Sirius Analytical Ltd. and University of Bath
Type: Journal Article | Journal: AAPS PharmSciTech | Year: 2016

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 small-scale dissolution assay. A clear difference in dissolution/precipitation behaviour can be observed based on the characteristics of the coformer used.


Schonherr D.,University of Greifswald | Wollatz U.,University of Greifswald | Haznar-Garbacz D.,University of Greifswald | Hanke U.,University of Greifswald | And 6 more authors.
European Journal of Pharmaceutics and Biopharmaceutics | Year: 2015

The aim of this work was to determine pKa values and solubility properties of 34 active agents using the SiriusT3 apparatus. The selected drug substances belong to the groups of ACE-inhibitors, β-blockers, antidiabetics and lipid lowering substances. Experimentally obtained pKa and intrinsic solubility values were compared to calculated values (program ACD/ChemSketch) and pKa values to published data as well. Solubility-pH profiles were generated to visualise the substance solubility over the gastrointestinal pH range. The relationship between the solubility characteristic of a substance, its bioavailability and categorisation according to the Biopharmaceutics Classification System (BCS) was examined as well. The results showed a good agreement between experimentally obtained, calculated and published pKa values. The measured and calculated intrinsic solubility values indicated several major deviations. All solubility-pH profiles showed the expected shape and appearance for acids, bases or zwitterionic substances. The obtained results for the pKa and solubility measurements of the examined active agents may help to predict their physicochemical behaviour in vivo, and to understand the bioavailability of the substances according to their BCS categorisation. The easy and reproducible determination of pKa and solubility values makes the SiriusT3 apparatus a useful tool in early stages of drug and formulation development. © 2015 Elsevier B.V. All rights reserved.


PubMed | Novartis, University of Greifswald, Vivo Drug Delivery GmbH and Sirius Analytical Ltd.
Type: | Journal: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V | Year: 2015

The aim of this work was to determine pKa values and solubility properties of 34active agents using the SiriusT3 apparatus. The selected drug substances belong to the groups of ACE-inhibitors, -blockers, antidiabetics and lipid lowering substances. Experimentally obtained pKa and intrinsic solubility values were compared to calculated values (program ACD/ChemSketch) and pKa values to published data as well. Solubility-pH profiles were generated to visualise the substance solubility over the gastrointestinal pH range. The relationship between the solubility characteristic of a substance, its bioavailability and categorisation according to the Biopharmaceutics Classification System (BCS) was examined as well. The results showed a good agreement between experimentally obtained, calculated and published pKa values. The measured and calculated intrinsic solubility values indicated several major deviations. All solubility-pH profiles showed the expected shape and appearance for acids, bases or zwitterionic substances. The obtained results for the pKa and solubility measurements of the examined active agents may help to predict their physicochemical behaviour in vivo, and to understand the bioavailability of the substances according to their BCS categorisation. The easy and reproducible determination of pKa and solubility values makes the SiriusT3 apparatus a useful tool in early stages of drug and formulation development.


Comer J.,Sirius Analytical Ltd. | Box K.,Sirius Analytical Ltd. | Taylor R.,Sirius Analytical Ltd.
Chimica Oggi/Chemistry Today | Year: 2014

This article briefly introduces a number of experimental methods that can be used to investigate supersaturation and precipitation of small-molecule drugs. Methods include solubility measurements by pH-metric methods; controlled supersaturation studies by pH-metric and UV methods; studies of the solid state using polarised light microscopy; aqueous dissolution under changing pH conditions; and biphasic dissolution. Examples illustrate how the results may be used to guide decision-making during formulation.

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