Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols

Research output: Contribution to journalJournal articleResearchpeer-review

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Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols. / Christensen, Janne Ørskov; Schultz, Kirsten; Mollgaard, Birgitte; Kristensen, Henning Gjelstrup; Mullertz, Anette.

In: European Journal of Pharmaceutical Sciences, Vol. 23, No. 3, 2004, p. 287-96.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Christensen, JØ, Schultz, K, Mollgaard, B, Kristensen, HG & Mullertz, A 2004, 'Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols', European Journal of Pharmaceutical Sciences, vol. 23, no. 3, pp. 287-96. https://doi.org/10.1016/j.ejps.2004.08.003

APA

Christensen, J. Ø., Schultz, K., Mollgaard, B., Kristensen, H. G., & Mullertz, A. (2004). Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols. European Journal of Pharmaceutical Sciences, 23(3), 287-96. https://doi.org/10.1016/j.ejps.2004.08.003

Vancouver

Christensen JØ, Schultz K, Mollgaard B, Kristensen HG, Mullertz A. Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols. European Journal of Pharmaceutical Sciences. 2004;23(3):287-96. https://doi.org/10.1016/j.ejps.2004.08.003

Author

Christensen, Janne Ørskov ; Schultz, Kirsten ; Mollgaard, Birgitte ; Kristensen, Henning Gjelstrup ; Mullertz, Anette. / Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols. In: European Journal of Pharmaceutical Sciences. 2004 ; Vol. 23, No. 3. pp. 287-96.

Bibtex

@article{189b2f40c5ec11dd9473000ea68e967b,
title = "Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols",
abstract = "The partitioning of poorly soluble drugs into an aqueous micellar phase was exploited using an in vitro lipid digestion model, simulating the events taking place during digestion of acylglycerols in the duodenum. The aqueous micellar phase was isolated after ultracentrifugation of samples obtained at different degrees of triacylglycerol hydrolysis. Flupentixol, 1'-[4-[1-(4-fluorophenyl)-1-H-indol-3-yl]-1-butyl]spiro[iso-benzofuran-1(3H), 4' piperidine] (LU 28-179) and probucol were studied. The effect of the alkyl chain length of the triacylglycerol was studied using a medium-chain triacylglycerol (MCT) and a long-chain triacylglycerol (LCT), respectively. In general, an oil solution was used as the lipid source in the model. Samples were analysed in regard to micellar size, lipid composition and drug concentration. During lipolysis, the content of lipolytic products in the aqueous micellar phase increased. The micellar size (R(H) approximately 3 nm) only increased when long-chain lipolytic products were incorporated in the mixed micelles (R(H) approximately 7.8 nm). Flupentixol was quickly transferred to the mixed micelles due to high solubility in this phase (100% released). A tendency towards higher solubilisation of LU 28-179, when it was administered in the LCT (approximately 24% released) compared to when it was administered in the MCT (approximately 15% released) at 70% hydrolysis, and a lagphase was observed. There was no difference in the solubilisation of probucol using MCT or LCT ( approximately 20% released), respectively. Differences in the physicochemical properties of the drugs resulted in differences in their distribution between the phases arising during lipolysis.",
author = "Christensen, {Janne {\O}rskov} and Kirsten Schultz and Birgitte Mollgaard and Kristensen, {Henning Gjelstrup} and Anette Mullertz",
note = "Keywords: Animals; Bile Acids and Salts; Flupenthixol; Indoles; Lipolysis; Micelles; Pancreatin; Pharmaceutical Preparations; Plant Oils; Probucol; Sesame Oil; Solubility; Spiro Compounds; Swine; Triglycerides; Ultracentrifugation; Water",
year = "2004",
doi = "10.1016/j.ejps.2004.08.003",
language = "English",
volume = "23",
pages = "287--96",
journal = "European Journal of Pharmaceutical Sciences",
issn = "0928-0987",
publisher = "Elsevier",
number = "3",

}

RIS

TY - JOUR

T1 - Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols

AU - Christensen, Janne Ørskov

AU - Schultz, Kirsten

AU - Mollgaard, Birgitte

AU - Kristensen, Henning Gjelstrup

AU - Mullertz, Anette

N1 - Keywords: Animals; Bile Acids and Salts; Flupenthixol; Indoles; Lipolysis; Micelles; Pancreatin; Pharmaceutical Preparations; Plant Oils; Probucol; Sesame Oil; Solubility; Spiro Compounds; Swine; Triglycerides; Ultracentrifugation; Water

PY - 2004

Y1 - 2004

N2 - The partitioning of poorly soluble drugs into an aqueous micellar phase was exploited using an in vitro lipid digestion model, simulating the events taking place during digestion of acylglycerols in the duodenum. The aqueous micellar phase was isolated after ultracentrifugation of samples obtained at different degrees of triacylglycerol hydrolysis. Flupentixol, 1'-[4-[1-(4-fluorophenyl)-1-H-indol-3-yl]-1-butyl]spiro[iso-benzofuran-1(3H), 4' piperidine] (LU 28-179) and probucol were studied. The effect of the alkyl chain length of the triacylglycerol was studied using a medium-chain triacylglycerol (MCT) and a long-chain triacylglycerol (LCT), respectively. In general, an oil solution was used as the lipid source in the model. Samples were analysed in regard to micellar size, lipid composition and drug concentration. During lipolysis, the content of lipolytic products in the aqueous micellar phase increased. The micellar size (R(H) approximately 3 nm) only increased when long-chain lipolytic products were incorporated in the mixed micelles (R(H) approximately 7.8 nm). Flupentixol was quickly transferred to the mixed micelles due to high solubility in this phase (100% released). A tendency towards higher solubilisation of LU 28-179, when it was administered in the LCT (approximately 24% released) compared to when it was administered in the MCT (approximately 15% released) at 70% hydrolysis, and a lagphase was observed. There was no difference in the solubilisation of probucol using MCT or LCT ( approximately 20% released), respectively. Differences in the physicochemical properties of the drugs resulted in differences in their distribution between the phases arising during lipolysis.

AB - The partitioning of poorly soluble drugs into an aqueous micellar phase was exploited using an in vitro lipid digestion model, simulating the events taking place during digestion of acylglycerols in the duodenum. The aqueous micellar phase was isolated after ultracentrifugation of samples obtained at different degrees of triacylglycerol hydrolysis. Flupentixol, 1'-[4-[1-(4-fluorophenyl)-1-H-indol-3-yl]-1-butyl]spiro[iso-benzofuran-1(3H), 4' piperidine] (LU 28-179) and probucol were studied. The effect of the alkyl chain length of the triacylglycerol was studied using a medium-chain triacylglycerol (MCT) and a long-chain triacylglycerol (LCT), respectively. In general, an oil solution was used as the lipid source in the model. Samples were analysed in regard to micellar size, lipid composition and drug concentration. During lipolysis, the content of lipolytic products in the aqueous micellar phase increased. The micellar size (R(H) approximately 3 nm) only increased when long-chain lipolytic products were incorporated in the mixed micelles (R(H) approximately 7.8 nm). Flupentixol was quickly transferred to the mixed micelles due to high solubility in this phase (100% released). A tendency towards higher solubilisation of LU 28-179, when it was administered in the LCT (approximately 24% released) compared to when it was administered in the MCT (approximately 15% released) at 70% hydrolysis, and a lagphase was observed. There was no difference in the solubilisation of probucol using MCT or LCT ( approximately 20% released), respectively. Differences in the physicochemical properties of the drugs resulted in differences in their distribution between the phases arising during lipolysis.

U2 - 10.1016/j.ejps.2004.08.003

DO - 10.1016/j.ejps.2004.08.003

M3 - Journal article

C2 - 15489130

VL - 23

SP - 287

EP - 296

JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 0928-0987

IS - 3

ER -

ID: 9013073