By a News Reporter-Staff News Editor at Pharma Business Week -- Data detailed on Pharmaceutical Science have been presented. According to news reporting out of Malov, Denmark, by NewsRx editors, research stated, "Liraglutide is a human glucagon-like peptide-1 (GLP-1) analogue approved for the treatment of type 2 diabetes. It is based on human GLP-1 with the addition of a 16-carbon fatty acid, which facilitates binding to plasma proteins, thus prolonging the elimination half-life and allowing once-daily administration."
Our news journalists obtained a quote from the research from Novo Nordisk, "It has not been possible to quantify liraglutide protein binding by ultrafiltration (the usual method of choice), as the lipophilic molecule becomes trapped in the filter membrane. Therefore, the aim of this study was to develop a methodology that could determine the extent of liraglutide binding to plasma proteins in vitro. We report here the details of a novel reiterated stepwise equilibrium dialysis assay that has successfully been used to quantify liraglutide plasma protein binding. The assay allowed quantification of liraglutide binding to proteins in purified plasma protein solutions and human plasma samples and was effective at plasma dilutions as low as 5%. At a clinically relevant liraglutide concentration (10(4) pM), greater than 98.9% of liraglutide was bound to protein. Specific binding to human serum albumin and 1-acid glycoprotein was 99.4% and 99.3%, respectively."
According to the news editors, the research concluded: "The novel methodology described herein could have an application in the quantification of plasma protein binding of other highly lipophilic drug molecules."
For more information on this research see: In vitro protein binding of liraglutide in human plasma determined by reiterated stepwise equilibrium dialysis. Journal of Pharmaceutical Sciences, 2013;102(8):2882-2888. Journal of Pharmaceutical Sciences can be contacted at: Wiley-Blackwell, 111 River St, Hoboken 07030-5774, NJ, USA. (Wiley-Blackwell - www.wiley.com/; Journal of Pharmaceutical Sciences - onlinelibrary.wiley.com/journal/10.1002/(ISSN)1520-6017)
Our news journalists report that additional information may be obtained by contacting A. Plum, Novo Nordisk AS, Chem & Isotope Lab, DK-2760 Malov, Denmark. Additional authors for this research include L.B. Jensen and J.B. Kristensen (see also Pharmaceutical Science).
Keywords for this news article include: Pharmaceutical Science, Malov, Europe, Denmark, Peptides, Proteins, Amino Acids
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