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Characterization of partition and thermodynamic properties of cephalosporins using micellar electrokinetic chromatography in glycodeoxycholic acid solution.

作者信息

Mrestani Y, Janich M, Rüttinger H H, Neubert R H

机构信息

Institute of Pharmaceutics and Biopharmaceutics, Martin-Luther-University, Halle/S., Germany.

出版信息

J Chromatogr A. 2000 Mar 24;873(2):237-46. doi: 10.1016/s0021-9673(99)01336-9.

Abstract

Micellar electrokinetic chromatography (MEKC) was introduced to evaluate the hydrophobicity of cephalosporins (cefpim, cefpirom, cefazolin, ceftazidim, cephradin, cefuroxim, cefotaxim, cephapirin and cephalothin). Partition coefficients of cephalosporins were calculated between a micelle and an aqueous phases from the measurement of the migration time, provided the critical micelle concentration and the phase ratio are known. Thermodynamic quantities such as enthalpy and entropy changes of micellar solubilization were calculated from the temperature dependence on the partition coefficients. Sodium glycodeoxycholate in low-salt aqueous solutions was employed to prepare a micellar solution. Substances for pharmaceutical purposes have to meet several requirements to be well-tolerated. Therefore, they are often derived from naturally occurring ones, e.g., from the bile salts in bile juice. The electrophoretic velocity of a micelle and the phase ratio between the micelle of the glycodeoxycholic acid and the aqueous phase were calculated. Partial specific volumes at different temperatures (from 20 to 45 degrees C) were measured using dynamic light scattering. The logarithm of the partition coefficients and the migration factor in the micellar system were correlated with the logarithm of the 1-octanol-water partition coefficients.

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