Using droplet-based microfluidic technology to study the precipitation of a poorly water-soluble weakly basic drug upon a pH-shift

Chemistry

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https://doi.org/10.1039/c2an36364j
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Keywords

NUCLEATION, HUMANS, DISSOLUTION, SYSTEM, FORMULATIONS, SOLUBILITY, SOLID DISPERSIONS, ABSORPTION

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Research output: Contribution to Journal/Magazine › Journal article › peer-review

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Using droplet-based microfluidic technology to study the precipitation of a poorly water-soluble weakly basic drug upon a pH-shift. / Edwards, Francine; Tsakmaka, Christina; Mohr, Stephan et al.
In: Analyst, Vol. 138, No. 1, 2013, p. 339-345.

Research output: Contribution to Journal/Magazine › Journal article › peer-review

Bibtex

@article{099b74f50a1040bda8fea226d42040c5,

title = "Using droplet-based microfluidic technology to study the precipitation of a poorly water-soluble weakly basic drug upon a pH-shift",

abstract = "The purpose of this study is to develop a droplet-based microfluidic device capable of monitoring drug precipitation upon a shift from gastric pH (pH 1.5) to intestinal pH (pH 6.5-7.0). The extent of precipitation occurring in droplets over time was measured using a novel on-chip laser scattering technique specifically developed for this study. The precipitation of ketoconazole, a poorly water-soluble basic drug, was investigated under different concentrations and pH values. It has been shown that the drug precipitates rapidly under supersaturation. Two water-soluble aqueous polymers, namely, polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) have been evaluated as precipitation inhibitors. HPMC was shown to be the most potent precipitation inhibitor. It is envisaged that the microfluidic pH-shift method developed in this study would form a proof-of-concept study, towards the development of a high throughput method for screening pharmaceutical excipients/precipitation inhibitors.",

keywords = "NUCLEATION, HUMANS, DISSOLUTION, SYSTEM, FORMULATIONS, SOLUBILITY, SOLID DISPERSIONS, ABSORPTION",

author = "Francine Edwards and Christina Tsakmaka and Stephan Mohr and Fielden, {Peter R.} and Goddard, {Nick J.} and Jonathan Booth and Tam, {Kin Y.}",

year = "2013",

doi = "10.1039/c2an36364j",

language = "English",

volume = "138",

pages = "339--345",

journal = "Analyst",

issn = "0003-2654",

publisher = "Royal Society of Chemistry",

number = "1",

}

RIS

TY - JOUR

T1 - Using droplet-based microfluidic technology to study the precipitation of a poorly water-soluble weakly basic drug upon a pH-shift

AU - Edwards, Francine

AU - Tsakmaka, Christina

AU - Mohr, Stephan

AU - Fielden, Peter R.

AU - Goddard, Nick J.

AU - Booth, Jonathan

AU - Tam, Kin Y.

PY - 2013

Y1 - 2013

N2 - The purpose of this study is to develop a droplet-based microfluidic device capable of monitoring drug precipitation upon a shift from gastric pH (pH 1.5) to intestinal pH (pH 6.5-7.0). The extent of precipitation occurring in droplets over time was measured using a novel on-chip laser scattering technique specifically developed for this study. The precipitation of ketoconazole, a poorly water-soluble basic drug, was investigated under different concentrations and pH values. It has been shown that the drug precipitates rapidly under supersaturation. Two water-soluble aqueous polymers, namely, polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) have been evaluated as precipitation inhibitors. HPMC was shown to be the most potent precipitation inhibitor. It is envisaged that the microfluidic pH-shift method developed in this study would form a proof-of-concept study, towards the development of a high throughput method for screening pharmaceutical excipients/precipitation inhibitors.

AB - The purpose of this study is to develop a droplet-based microfluidic device capable of monitoring drug precipitation upon a shift from gastric pH (pH 1.5) to intestinal pH (pH 6.5-7.0). The extent of precipitation occurring in droplets over time was measured using a novel on-chip laser scattering technique specifically developed for this study. The precipitation of ketoconazole, a poorly water-soluble basic drug, was investigated under different concentrations and pH values. It has been shown that the drug precipitates rapidly under supersaturation. Two water-soluble aqueous polymers, namely, polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) have been evaluated as precipitation inhibitors. HPMC was shown to be the most potent precipitation inhibitor. It is envisaged that the microfluidic pH-shift method developed in this study would form a proof-of-concept study, towards the development of a high throughput method for screening pharmaceutical excipients/precipitation inhibitors.

KW - NUCLEATION

KW - HUMANS

KW - DISSOLUTION

KW - SYSTEM

KW - FORMULATIONS

KW - SOLUBILITY

KW - SOLID DISPERSIONS

KW - ABSORPTION

U2 - 10.1039/c2an36364j

DO - 10.1039/c2an36364j

M3 - Journal article

VL - 138

SP - 339

EP - 345

JO - Analyst

JF - Analyst

SN - 0003-2654

IS - 1

ER -

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