Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs. / Andersson, Sara B. E.; Alvebratt, Caroline; Bevernage, Jan; Bonneau, Damien; Mathews, Claudia da Costa ; Dattani, Rikesh; Edueng, Khadijah; He, Yan; Holm, René; Madsen, Cecilie Maria; Müller, Thomas; Muenster, Uwe; Müllertz, Anette; Ojala, Krista; Rades, Thomas; Sieger, Peter; Bergström, Christel A. S.

In: Journal of Pharmaceutical Sciences, Vol. 105, No. 9, 09.2016, p. 2864-72.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Andersson, SBE, Alvebratt, C, Bevernage, J, Bonneau, D, Mathews, CDC, Dattani, R, Edueng, K, He, Y, Holm, R, Madsen, CM, Müller, T, Muenster, U, Müllertz, A, Ojala, K, Rades, T, Sieger, P & Bergström, CAS 2016, 'Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs', Journal of Pharmaceutical Sciences, vol. 105, no. 9, pp. 2864-72. https://doi.org/10.1016/j.xphs.2016.03.010

APA

Andersson, S. B. E., Alvebratt, C., Bevernage, J., Bonneau, D., Mathews, C. D. C., Dattani, R., ... Bergström, C. A. S. (2016). Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs. Journal of Pharmaceutical Sciences, 105(9), 2864-72. https://doi.org/10.1016/j.xphs.2016.03.010

Vancouver

Andersson SBE, Alvebratt C, Bevernage J, Bonneau D, Mathews CDC, Dattani R et al. Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs. Journal of Pharmaceutical Sciences. 2016 Sep;105(9):2864-72. https://doi.org/10.1016/j.xphs.2016.03.010

Author

Andersson, Sara B. E. ; Alvebratt, Caroline ; Bevernage, Jan ; Bonneau, Damien ; Mathews, Claudia da Costa ; Dattani, Rikesh ; Edueng, Khadijah ; He, Yan ; Holm, René ; Madsen, Cecilie Maria ; Müller, Thomas ; Muenster, Uwe ; Müllertz, Anette ; Ojala, Krista ; Rades, Thomas ; Sieger, Peter ; Bergström, Christel A. S. / Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs. In: Journal of Pharmaceutical Sciences. 2016 ; Vol. 105, No. 9. pp. 2864-72.

Bibtex

@article{8053a1d520df408aa04ed84c6b9e826b,
title = "Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs",
abstract = "The purpose of this study was to investigate the interlaboratory variability in determination of apparent solubility (Sapp) and intrinsic dissolution rate (IDR) using a miniaturized dissolution instrument. Three poorly water-soluble compounds were selected as reference compounds and measured at multiple laboratories using the same experimental protocol. Dissolution was studied in fasted-state simulated intestinal fluid and phosphate buffer (pH 6.5). An additional 6 compounds were used for the development of an IDR measurement guide, which was then validated with 5 compounds. The results clearly showed a need for a standardized protocol including both the experimental assay and the data analysis. Standardization at both these levels decreased the interlaboratory variability. The results also illustrated the difficulties in performing disc IDR on poorly water-soluble drugs because the concentrations reached are typically below the limit of detection. The following guidelines were established: for compounds with Sapp >1 mg/mL, the disc method is recommended. For compounds with Sapp <100 μg/mL, IDR is recommended to be performed using powder dissolution. Compounds in the interval 100 μg/mL to 1 mg/mL can be analyzed with either of these methods.",
keywords = "Journal Article",
author = "Andersson, {Sara B. E.} and Caroline Alvebratt and Jan Bevernage and Damien Bonneau and Mathews, {Claudia da Costa} and Rikesh Dattani and Khadijah Edueng and Yan He and Ren{\'e} Holm and Madsen, {Cecilie Maria} and Thomas M{\"u}ller and Uwe Muenster and Anette M{\"u}llertz and Krista Ojala and Thomas Rades and Peter Sieger and Bergstr{\"o}m, {Christel A. S.}",
note = "Copyright {\circledC} 2016 American Pharmacists Association{\circledR}. Published by Elsevier Inc. All rights reserved.",
year = "2016",
month = "9",
doi = "10.1016/j.xphs.2016.03.010",
language = "English",
volume = "105",
pages = "2864--72",
journal = "Journal of Pharmaceutical Sciences",
issn = "0022-3549",
publisher = "Elsevier",
number = "9",

}

RIS

TY - JOUR

T1 - Interlaboratory validation of small-scale solubility and dissolution measurements of poorly water-soluble drugs

AU - Andersson, Sara B. E.

AU - Alvebratt, Caroline

AU - Bevernage, Jan

AU - Bonneau, Damien

AU - Mathews, Claudia da Costa

AU - Dattani, Rikesh

AU - Edueng, Khadijah

AU - He, Yan

AU - Holm, René

AU - Madsen, Cecilie Maria

AU - Müller, Thomas

AU - Muenster, Uwe

AU - Müllertz, Anette

AU - Ojala, Krista

AU - Rades, Thomas

AU - Sieger, Peter

AU - Bergström, Christel A. S.

N1 - Copyright © 2016 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

PY - 2016/9

Y1 - 2016/9

N2 - The purpose of this study was to investigate the interlaboratory variability in determination of apparent solubility (Sapp) and intrinsic dissolution rate (IDR) using a miniaturized dissolution instrument. Three poorly water-soluble compounds were selected as reference compounds and measured at multiple laboratories using the same experimental protocol. Dissolution was studied in fasted-state simulated intestinal fluid and phosphate buffer (pH 6.5). An additional 6 compounds were used for the development of an IDR measurement guide, which was then validated with 5 compounds. The results clearly showed a need for a standardized protocol including both the experimental assay and the data analysis. Standardization at both these levels decreased the interlaboratory variability. The results also illustrated the difficulties in performing disc IDR on poorly water-soluble drugs because the concentrations reached are typically below the limit of detection. The following guidelines were established: for compounds with Sapp >1 mg/mL, the disc method is recommended. For compounds with Sapp <100 μg/mL, IDR is recommended to be performed using powder dissolution. Compounds in the interval 100 μg/mL to 1 mg/mL can be analyzed with either of these methods.

AB - The purpose of this study was to investigate the interlaboratory variability in determination of apparent solubility (Sapp) and intrinsic dissolution rate (IDR) using a miniaturized dissolution instrument. Three poorly water-soluble compounds were selected as reference compounds and measured at multiple laboratories using the same experimental protocol. Dissolution was studied in fasted-state simulated intestinal fluid and phosphate buffer (pH 6.5). An additional 6 compounds were used for the development of an IDR measurement guide, which was then validated with 5 compounds. The results clearly showed a need for a standardized protocol including both the experimental assay and the data analysis. Standardization at both these levels decreased the interlaboratory variability. The results also illustrated the difficulties in performing disc IDR on poorly water-soluble drugs because the concentrations reached are typically below the limit of detection. The following guidelines were established: for compounds with Sapp >1 mg/mL, the disc method is recommended. For compounds with Sapp <100 μg/mL, IDR is recommended to be performed using powder dissolution. Compounds in the interval 100 μg/mL to 1 mg/mL can be analyzed with either of these methods.

KW - Journal Article

U2 - 10.1016/j.xphs.2016.03.010

DO - 10.1016/j.xphs.2016.03.010

M3 - Journal article

C2 - 27112289

VL - 105

SP - 2864

EP - 2872

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

SN - 0022-3549

IS - 9

ER -

ID: 169382437