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虫号: 1239153
注册: 2011-03-20
专业: 临床药理

[求助] 有高手可以翻译下这段吗？

Drug penetration through the biological
barrierTo construct chromatographic models simulating biological barriers, different stationary materials have been tested. To begin with, most studies were performed by RP-HPLC on octadecyl silica [10–13]. These chromatographic systems enabled correlations between logarithms of partition coefficients in n-octanol-water
partition system, log Po/wand chromatographic data (log kw or log k) to be obtained. Therefore, chromatographic retention parameters, as a result of adsorptionpartitioning phenomenon in RP systems, are regarded as lipophilicity descriptors of drugs. In the 1990s, Pidgeon’s group revealed a correlation between the chromatographic retention on immobilized artificial membranes (IAMs) formed by covalently bound lecithin to propylamine silica and their ability to predict human skin permeation [14]. Currently, a new generation of IAM-type columns with immobilized phosphatidylcholine or sphingomyelin that simulate the structure of cell membranes [15,16]are at researchers’
disposal. Such chromatographic systems can be considered as an ‘in vivo’ model of cellular barrier transgression by the drug. The cholesterol-bonded phase, owing to its similarity to immobilized artificial membranes, also enables utilization of chromatographic data to anticipate the process of the cell membrane permeation. Retention on the cholesterol column, as a combination of different interactions of analytes with the surface, reflects the so-called ‘phospholipophilicity’ of drugs. However, retention measured by IAM columns does not frequently depend linearly on the composition of the mobile phase as in conventional RP systems. Therefore, slight differences in the content of the organic solvent in the eluent will determine the quality of retention–activity relationships [17].
MLC also provides a fairly good model for in vivodrug partitioning. It has been demonstrated that RP-HPLC with micellar eluents credibly reflects complex interactions of drugs with their biological target. The problem of these assays includes high concentrations of surfactants and buffers that may damage the column. One solution is the use of ionic liquids with a small NaCl addition achieving micelle concentration in dilute solutions [18]. This proposal is worth considering, especially since MLC is the only technique that allows direct injection of serum samples.

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