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Lipophilicity in Drug. Action and Toxicology edited by. Vladimir Pliska. Bernard Testa. Han van de Waterbeemd. VCH. Weinheim • New York • Basel • Cambridge .
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Color plates demonstrating structural aspects, a vast number of references, and the straightforward presentation of the material make this volume a invaluable tool for all researchers involved in drug design or in the investigation of drug action. Read more Show all links. Allow this favorite library to be seen by others Keep this favorite library private. Find a copy in the library Finding libraries that hold this item This work features coverage of lipophilicity in drug action and toxicology.

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Lipophilicity in drug action and toxicology

Chemistry, Pharmaceutical. Lipids -- chemistry. Linked Data More info about Linked Data. All rights reserved. During procedure all analytes are washed out ues illustrated above of calibration compounds. Linear solvent strength LSS model allows tion and for enlarging a database. Additionally, the calculating log kW from retention data obtained in CHI values can also be projected to the logarithmic two gradient HPLC experiments 63 , in contrast, scale.

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Hence, relation assessment with log P or log the isocratically measured log k is time-consuming D parameters is facilitated. The parameter allows and requires several chromatographic runs. The comparison even of unrelated compounds. Good correlation was observed Vg is the gradient volume, Vd is dwell volume, Vm between log kW obtained by reversed phase gradient denotes dead volume.

Parameter kg obtained for run and value obtained by standard method of congeneric chemicals and the log kW data derived extrapolation. As concluded by Kaliszan, gradient from series of isocratic measurements showed a HPLC is a convenient method of efficient screening good correlation. The reliability of chromatographic of lipophilicity of drug candidates 65, One may use two appropriate tion of lipophilicity measurement by use of HPLC: gradient runs to determine both pKa and log kW.

Pharmacology: Basic Pharmacology, ANS, Endocrine

Another high throughput technique of pKa and log In isocratic method, previous estimation of kW determination has been presented by Wiczling et probable compound lipophilicity is essential to pre- al. These methods gain greater ic log k values as a function of the mobile phase attention nowadays. In contrast to a gradient run Chromatographic separation system for several retention measurements at varied organic lipophilicity estimation should model the octanol- solvent concentrations i.

Recently, Kaliszan has are needed, thus analyses take more time. It must be noted, that silica-based materials are Biomimetic stationary phases instable at higher pH, thus the investigation of basis As it was presented above, the use of new sta- analytes is unsatisfactory and lipophilicity determi- tionary phases in HPLC system seem to be effective nation of ionizable compounds on C or C-8 in prediction of octanol-water partition coefficient. It is silanol groups on the silica surface, which results in widely emphasized in the literature that for more asymmetrical peaks.

To limit interactions mentioned accurate description of compound distribution above, silica based stationary phases can be protect- between various compartments in vivo, application ed by polar groups. Alkylamide as well as carbamate of distinct types of lipophilicity is required Recently, more and more research attention is paid Giaginis and coworkers simulated octanol- to application in HPLC stationary phases that could water partitioning employing a base deactivated sil- directly mimic biologically important elements.

In addition, in the case of These biomimetic stationary phases include immo- basic drugs, n-decylamine was used as masking bilized drug-binding proteins, liposomes and mem- agent in the mobile phase. Moreover, Benhaim branes will be briefly characterized below. Polar amide group is introduced on the bonded stationary phases used in chromatography approach- alkyl chain close to silica surface, therefore, access es to mimic the partitioning into phospholipid bilay- of the solute is prevented.

Addition of n-octanol ers. IAM phases basical- extrapolated log kW. The surface of stationary phase is particularly grafted silica-polymer hybrid that reduces direct contact with free acidic silanol groups. Entirely devoid of reactive silanol groups is the polymer-based octadecylpolyvinyl ODP stationary phase which has been used for lipophilicity meas- urements by Donovan and Pescatore.

The retention behavior from a fast methanol-water gradient employing short polyvinyl alcohol columns demon- strated higher correlation with the log P than silane based columns Modern monolithic silica stationary phases overcome disadvantages of conventional particle based supports. Predominantly, considering time of analysis for very lipophilic compounds, which are strongly retained.

Mrkvickova 72 determined lipophilicity of potential antituberculotic agents using HPLC on monolithic stationary phase and cal- culated theoretical log P values for all compounds employing the chemical programs.

Technique sig- Figure 2. It has to be noted, that partitioning into years ago by Pidgeon et al. Properties of the most frequently used IAM octanol-water log P. This difference is of great stationary phases were reviewed in details by importance when lipophilicity of ionizable drugs is Taillardat- Bertschinger et al. Estimation of considered, as their partition in membranes is con- lipophilicity by IAM-HPLC is realized by isocratic siderably more effective than in octanol.

Lipophilicity In Drug Action And Toxicology 1996

Some and gradient methods. Even if using liposomes as stationary phases estimation. Our group used IAM cal difficulties due to limited stability of liposomes. Recently, Reinter et al. Barbato and cooworkers, who observed C18 and IAM columns, and partition coefficients this relationship for quinolone antibacterial agents, determined in phospholipid liposomes Above this value, no further determined in liposome systems. Barbato et al. To conclude, interaction mechanism Results showed that lipophilicity estimated by with serum-protein is complex and only partially IAM chromatography is more consistent with phar- governed by lipophilicity.

Immobilization of liposomes into surface of Therefore, HSA-HPLC provide potential to stimu- support particles and their use as stationary phases late plasma protein binding, as retention data pro- for HPLC leads to technique called immobilized vided by this technique incorporate also other mech- liposome chromatography ILC.

Liposomes as anism than lipophilicity, especially those of electro- spherical vesicles form by aggregation of phospho- static nature. Structural properties of lipo- which allow for including additional intermolecular somes were summarized in review of Plember van recognition forces, not encoded in traditional Balen et al. Comparison between recognition forces governing intermolecular interactions in biochemical and pharmacological process, and forces encoded in lipophilicity parameters obtained by different methods Electrically driven separation methods Capillary zone elecrophoresis CZE , the sim- Lipophilicity estimation can be also realized by plest form of CE, cannot be considered as lipophilic- electrically driven separation methods.