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Binding of artemether and lumefantrine to plasma proteins and erythrocytes.

Colussi, Danila and Parisot, Carole and Legay, Francois and Lefevre, Gilbert (1999) Binding of artemether and lumefantrine to plasma proteins and erythrocytes. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 9 (1). pp. 9-16. ISSN 0928-0987

Abstract

The serum/plasma protein binding and blood distribution of artemether and lumefantrine was studied in vitro. The techniques used were the erythrocyte partitioning and ultrafiltration methods with 1499%, respectively. Under physiological protein concentrations, the distribution in blood showed that 33% of artemether was bound to alpha(1)-acid glycoprotein, 17% to albumin, 12% to high density lipoproteins (HDL), 9.3% to low density lipoproteins (LDL) and 12% to very low density lipoproteins (VLDL), with binding capacities (nKa) of 3.2 x 10(5), 6.2 x 10(3), 2.1 x 10(5), 1.7 x 10(6) and 2.0 x 10(7) lmol(-1), respectively. 77% of lumefantrine was bound to HDL, 7.3% to LDL and 6.6% to VLDL, with binding capacities of 2.7 x 10(7), 2. 6 x 10(7) and 2.4 x 10(8) lmol(-1), respectively. A negligible fraction of lumefantrine was bound to albumin and alpha(1)-acid glycoprotein. The fraction in erythrocytes was around 10% for both artemether and lumefantrine.

Item Type: Article
Date Deposited: 31 Jan 2012 00:45
Last Modified: 01 Feb 2013 00:47
URI: https://oak.novartis.com/id/eprint/5178

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