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PARTITIONING INTO OCTANOL
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TABLE 41 Compound Trp-Phe Trp-Trp Tryptophan Tylosin Valsartan Verapamil Warfarin
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(Continued) log PN 028 010 077 163 390 433 354 log PI log PI log D7:4 033 049 055 071 244 099 157 004 050 040 077 251 112 Ref 162, p 2 162, p 8 162, p 10 358 509 b 149
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Measurements at 25 C, 015 M ionic strength pION c Sirius Analytical Instruments
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PARTITIONING INTO LIPOSOMES
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The octanol water partition model has several limitations; notably, it is not very biological The alternative use of liposomes (which are vesicles with walls made of a phospholipid bilayer) has become more widespread [149,162,275, 380 444] Also, liposomes contain the main ingredients found in all biological membranes
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TETRAD OF EQUILIBRIA AND SURFACE ION PAIRING (SIP)
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Figure 51 shows a tetrad of equilibrium reactions related to the partitioning of a drug between an aqueous environment and that of the bilayer formed from phospholipids (Only half of the bilayer is shown in Fig 51) By now, these reaction types might be quite familiar to the reader The subscript mem designates the partitioning medium to be that of a vesicle formed from a phospholipid bilayer mem Equations (41) (44) apply The pKa in Fig 51 refers to the membrane oct pKa Its meaning is similar to that of pKa ; when the concentrations of the uncharged and the charged species in the membrane phase are equal, the aqueous mem pH at that point de nes pKa , which is described for a weak base as ! B mem H BH mem
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mem Ka
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B mem H BH mem
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Absorption and Drug Development: Solubility, Permeability, and Charge State By Alex Avdeef ISBN 0-471-423653 Copyright # 2003 John Wiley & Sons, Inc
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logPmemSIP
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Figure 51 Phospholipid membrane water tetrad equilibria Only half of a bilayer is shown [Avdeef, A, Curr Topics Med Chem, 1, 277 351 (2001) Reproduced with permission from Bentham Science Publishers, Ltd]
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mem The salt dependence of constants discussed in Section 42 also applies to the pKa SIP and log Pmem constants Although they are conditional, the dependence on ionic strength is subtle [433,442] It is thought that when a charged drug migrates into the lipid environment of a liposome, the counterion that at rst accompanies it may be exchanged with the zwitterionic phosphatidylcholine head groups, as suggested in Fig 51 As the nature of the ion pair may be different with liposome partitioning, the term surface ion pair (SIP) is used to denote it We use the term diffmem to designate the difference between the neutral species partitioning and the surface ion pair partitioning [see Eq (46)]
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LOCATION OF DRUGS PARTITIONED INTO BILAYERS
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There are no convenient databases for liposome log P values Most measured quantities need to be ferreted from original publications [149,162,376,381 387,443] The handbook edited by Cevc [380] is a comprehensive collection of properties of phospholipids, including extensive compilations of structural data from X-ray crystallographic studies Lipid-type distributions in various biological membranes have been reported [380,388,433]
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Based on the observed nuclear Overhauser effect in a 31 Pf1 Hg nuclear magnetic resonance (NMR) study of egg phosphatidylcholine (eggPC) bilayers, Yeagle et al [399] concluded that the N-methyl hydrogens were in close proximity to phosphate oxygens in neighboring phospholipids, suggesting that the surface of the bilayer was a shell of interlocking (intermolecular) electrostatic associations Added cholesterol bound below the polar head groups, and did not interact with them directly However, its presence indirectly broke up some of the surface structure, making the surface more polar and open to hydration Boulanger et al [420,421] studied the interactions of the local anesthetics procaine and tetracaine with eggPC multilamellar vesicles (MLV, 52 650 mM), as a function of pH, using deuterium nmr as a structural probe They proposed a three-site model, similar to that in Fig 51, except that the membrane-bound species (both charged and uncharged) had two different locations, one a weakly bound surface site (occupied at pH 55), and the other a strongly bound deeper site (occupied at pH 95) Membrane partition coef cients were estimated for both sites Westman et al [422] further elaborated the model by applying the Gouy Chapman theory When a charged drug partitions into the bilayer, a Cl is likely bound to the surface, to maintain charge neutrality They found unexpected low values of diffmem of 077 for tetracaine and 164 for procaine (see Section 47) Kelusky and Smith [423], also using deuterium NMR, proposed that at pH 55, there was an electrostatic bond formed between the protonated drug and the phosphate groups, ( P H3N and a hydrogen bond formed between the aminobenzene ), O proton and the acyl carbonyl oxygen At pH 95, the ionic bond breaks as the secondary amine moves deeper into the interior of the bilayer; however, the amino benzene H bond, ( CO H2N continues to be an anchoring point ), Bauerle and Seelig [395] studied the structural aspects of amlodipine (weak base, primary amine pKa 926 [162]) and nimodipine (nonionizable) binding to phospholipid bilayers, using NMR, microcalorimetry, and zeta-potential measurements They were able to see evidence of interactions of amlodipine with the cis double bond in the acyl chains They saw no clear evidence for ( P H3N electrostatic interactions ) O Herbette and co-workers [425 428,445] studied the structures of drugs bound to liposomes using a low-angle X-ray diffraction technique Although the structural