Sodium taurocholate

Sodium taurocholate [145-42-6] M 555.7. Purified by recrystn and gel chromatography using Sephadex LH-20. 

The structure of cholic acid helps us understand how bile salts such as sodium taurocholate promote the transport of lipids through a water-rich environment. The bottom face of the molecule bear s all of the polar groups, and the top face is exclusively hydrocarbon-like. Bile salts emulsify fats by forming micelles in which the fats are on the inside and the bile salts are on the outside. The hydrophobic face of the bile salt associates with the fat that is inside the micelle the hydrophilic face is in contact with water on the outside. 

Bile acids The organic acids in bile contains sodium glycocholate and sodium taurocholate, cholesterol, biliverdin and bilirubin, mucus, fat, lecithin, and cells and cellular debris. 

When diabetic rabbits (24) were treated with 50 IU of bovine insulin imbibed at 50 mg/g poly (acrylic acid) (Figure 14) no reduction in serum glucose over that achieved by the dry blend control could be detected. Pretreatment of the animals with oral doses of either a penetration enhancer, sodium taurocholate, or a protease inhibitor, aproteinin, failed to improve the insulin activity. One possible explanation for this unexpected lack of activity might be that the diseased animals exhibit impaired ileal absorption of fluids (25). 

Figure 14. Effect of oral delivery of an insulin/polyacid matrix to diabetic rabbits on serum glucose, with and without adjuvants (sodium taurocholate, aprotinin).

Figure 7.13 shows some of the structures of common bile acids. In low ionic strength solutions, sodium taurocholate forms tetrameric aggregates, with critical... 

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],... 

Conjunctival insulin absorption in rabbits estimated as plasma insulin levels after punctal occlusion was also shown to be increased by bile salts (sodium deoxycholate, glycocholate, and taurocholate) and a surfactant (polyoxyethylene-9-lauryl ether) [200], Their rank order of effectiveness at 1% was sodium deoxycholate > polyoxyethylene-9-lauryl ether > sodium glycocholate = sodium taurocholate. There was an 18-, 29-, 3-, and 3-fold increase, respectively, in conjunctival absorption. Sodium deoxycholate, a dihydroxy bile salt, was more effec-... 

Kouzuki, H., Suzuki, H., Ito, K., Ohashi, R., Sugiyama, Y., Contribution of sodium taurocholate cotransporting polypeptide to the uptake of its possible substrates into rat hepatocytes, J. Pharmacol. Exp. 

Fig. 21.14. In vitro dissolution rate versus saturation solubility for candersartan cilexitil in different concentrations of sodium taurocholate lecithin ratio 2.5 1.

A, crude bovine sodium taurocholate and , porcine bile extract. 

Several ehemical enhancers, such as sodium ethylenediaminetetraacetate and sodium taurocholate, oleic acid [37], polyoxyethylated nonionic surfactants, citric acid, and dihydroxy bile salts open the paracellular route, presumably by disruption of the intraeellular OJC funetion [37], The use of nitrie oxide is another approach [39], Moreover, manipulation of the cyclooxygenase pathway activities to trigger the release of eompounds like substance P may provide another means for altering colonic permeability [40],... 

Meaney, C., and O Driscoll, C., Mucus as a barrier to the permeability of hydrophilic and lipophilic compounds in the absence and presence of sodium taurocholate micellar systems using cell culture models, Eur. J. Pharm. Sci., 8 167-175 (1999). 

Figure 2.1 Hepatocyte basolateral bile acid transporters. Protein-bound bile acids returning in portal blood are taken up by the hepatocyte via the sodium taurocholate co-transporting polypeptide (NTCP) and organic-anion-transporting polypeptide (OATP). In cholestasis bile acids may be returned to blood by the multi-drug-resistance-associated protein 3 (MRP3).

Taurocholate stock solution dissolve 30 mg sodium taurocholate (MW 538) in 1 ml chloroform/methanol (2/1 v/v). 

Reaction buffer 0.1 M sodium acetate buffer pH 5.2 mix 79 ml 0.1 M acetate with 21 ml 0.1 M acetic acid and bring the pH to 5.2 with either acetate or acetic acid solution. Dissolve 20 mg sodium taurocholate in 10 ml of buffer to a final concentration of 0.2% (w/v). 

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