Taurodeoxycholate

Morimoto et al. [33] demonstrated that the ocular absorption of hydrophilic compounds over a wide range of molecular weights could be increased by 2 and 10 mM sodium taurocholate and sodium taurodeoxycholate in a dose-dependent manner. The compounds were glutathione (307 Da), 6-carboxyfluorescein (376 Da), FTTC-dextran (4 kDa), and insulin (5.7 kDa). Of the two bile salts, sodium taurodeoxycholate was more effective. At 10 mM, this bile salt increased the permeability of 6-carboxyfluorescein from 0.02% to 11%, glutathione from 0.08% to 6%, FITC-dextran from 0% to 0.07%, and insulin from 0.06% to 3.8%. Sodium taurocholate, on the other hand, increased the permeability to 0.13%, 0.38%, 0.0011%, and 0.14%, respectively. Taurodeoxycholate was more effective than taurocholate in the nasal epithelium as well [202], This difference in activities can possibly be attributed to their micelle-forming capability, which is higher for taurodeoxycholate, a dihydroxy bile salt [190],... 

A further group of AT-[(acyloxy)methyl] pro-moieties contains acidic and/or lipid-like substituents. Here again, most published results concern phenytoin. Thus, some phenytoin-lipid conjugates such as 8.183 and 8.186 (with R = various fatty acyl moieties) were reported [233]. Such prodrugs are, of course, insoluble in water but formed dispersions when briefly sonicated in EtOH/water mixtures containing sodium taurodeoxycholate. No significant hydrolysis was seen in buffer or plasma. In contrast, incubation with pancreatic lipase yielded the bis-deacyl derivatives (i.e., 8.182 and 8.185, respectively), with subsequent liberation of phenytoin the time for 50% liberation of phenytoin varied from 20 to 200 min under the conditions of the studies [233][234], The intermediates 8.182, 8.184, and 8.185 were also substrates for human and rat plasma hydrolases. 

TDCA taurodeoxycholic acid, TCDCA taurochenodeoxycholic acid,... 

Sodium taurocholate Sodium taurochenodeoxycholate A Sodium taurodeoxycholate... 

For phase equilibria experiments, either sodium taurodeoxycholate or an equimolar mixture of sodium taurocholate and sodium taurodeoxycholate was used, unless noted, as previous studies (8) had shown that the behavior of monoolein was similar in all of the bile salt conjugates. Previous studies (7) had also shown that the 1-monoolein and 2-monoolein behaved identically in bile salt solution. Therefore, 1-monoolein was used in all experiments because of its greater availability and stability (7). Lipids, dissolved in an appropriate solvent, were added to... 

For bile salt mixtures, total concentration of bile salts is given. TDC = sodium taurodeoxycholate. TC = sodium taurocholate. OA oleic acid. MO = monoolein. 

FIGURE 9 Electropherograms of the chiral resolution of (I) l-cyanobenz[/]isoindole (CBI)-selenomethionine and (II) CBI-selenoethionine enantiomers using a mixture of boric acid (10 mM) and phosphate buffer (30 mM, pH 7) as the mobile phase containing [i-cyclodextrin (30 mM) and taurodeoxycholic acid (50 mM) as CMPAs with sodium dodecyl sulfate (50 mM) as the mobile phase modifier (from Ref. 97). 

Bile salts used in permeation enhancement studies include the trihydroxy salts sodium cholate, sodium glycocholate, and sodium taurocholate (Figure 10.2) and the dihydroxy salts sodium deoxycholate, sodium glycodeoxycholate, and sodium taurodeoxycholate. Several in vitro permeation studies carried out in isolated animal buccal mucosa and in vivo bioavailability studies conducted in animals and human subjects have proven their potential as effective buccal permeation enhancers. 

Taurolihtocholic acid (TLCA) Taurodeoxycholic acid (TDCA) Taurocholic acid (TCA)... 

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