Sodium glycocholate

Sodium glycocholate [863-57-0] M 488.6. Dissolved in EtOH, filtered and concentrated to crystallisation, and recrystallised from a little EtOH. 

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. 

Although the ocular absorption of peptide as well as nonpeptide drugs is poor [96,196-198], the ocular route is by far the least studied for the usefulness of penetration enhancers. This is in part due to the perceived sensitivity of ocular tissues to irritation and the fear of corneal and conjunctival damage caused by the enhancers. Whereas the rat nasal epithelium may tolerate up to 5% sodium glycocholate [199], ocular administration of sodium glycocholate at a concentration of 2% and beyond induces reddening of the eye and tear production in rabbits (Kompella and Lee, unpublished observation). 

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-... 

Lewis, as already mentioned, used a solution of sodium glycocholate and determined the adsorption of the salt by a surface of paraffin oil. The interfacial tension solution—paraffin oil this was measured for a number of concentrations by the drop method just discussed, and the [Pg.42]

Those of complex constitution and high molecular weight, e.g., sodium glycocholate, Congo red, methyl orange, sodium oleate, which show adsorption 20—100 times larger than that calculated from the formula. 

Nielsen HM, Verhoef JC, Ponec M, Rassing MR (1999b) TR146 cells grown on filters as a model of human buccal epithelium Permeability of fluorescein isothiocyanate-labelled dextrans in the presence of sodium glycocholate. J Control Release 60 223-233... 

Senel S, Duchene D, Hincal AA, Capan Y, Ponchel G (1998) In vitro studies on enhancing effect of sodium glycocholate on transbuccal permeation of morphine hydrochloride. J Control Release 51 107-113... 

Faraj et al. [28] studied the effects of different concentrations of leucine enkephalin, peptidase inhibitors, and sodium glycocholate (GC) on the stability and absorption of leucine enkephalin in nasal cavities of rats. Based on the study, the rate and extent of formation of des-tyrosine leucine enkephalin... 

The addition of absorption enhancers, like bile salts (glycocholate), fatty acids (Unoleic acid), surfactants (lecithins, polyoxyethylene-9-lauryl ether or N-lauryl-P-D-maltopyra-noside) and chelators (EDTA) can significantly increase the absorption of various proteins. However, the application of enhancers is limited by their toxicity. For example polyoxyethyl-ene-9-lauryl ether and sodium glycocholate caused serious oedema, haemorrhage and inflammation of the lung after intratracheal instillation [39]. 

The interfacial tensions of a number of aqueous solutions against mercury have been measured by McLewis, Patrick and others. The tension was lowered by addition of all the solutes examined, including mercurous sulphate, salicylic acid, picric acid, neofuchsin, morphine hydrochloride, caffeine, aniline, sodium glycocholate. All of these substances except mercurous sulphate lower the surface See p. 36. 

Abbreviations OG, n-octyl- 3-D-glucopyranoside DM, dodecylmaltoside LM, w-lauryl-( -D-glucopyranoside Azone, 1-dodecyl azacyclohepatan-2-one, SCG, sodium glycocholate STDHF, sodium tauro-2425 dihydrofusidate UCDA, ursodeoxycholate CDCA, chenodeoxycholate SDS, sodium dodecylsulfate DMSO, dimethyl sulfoxide DMF, AV-dimethyl formamide DMAC, A At-dimethyl acetamide. 

Sodium glycocholate Sodium glycochenodeoxycholate A Sodium glycodeoxycholate... 

The enhancement of insulin absorption by sodium caprate (Ci0) in a closed loop model in rats showed the following rank of efficiency colon > ileum > jejunum > duodenum. On the other hand, sodium glycocholate affected the intestinal permeability in a different way. With this surfactant, the order of permeation enhancement was colon > jejunum > duodenum > ileum [95], These results show that the absorption site in the GI tract may strongly affect the effectiveness of permeation enhancer. 

Utsumi, I., K. Kono, and Y. Takeuchi. 1973. Effect of surfactants on drug absorption. IV. Mechanism of the action of sodium glycocholate on the absorption of benzoylthiamine disulfide in the presence of sodium laurylsulfate and polysorbate 80. Chem Pharm Bull (Tokyo) 21 2161. 

Morishita, M., et al. 1993. Site-dependent effect of aprotinin, sodium caprate, Na2EDTA and sodium glycocholate on intestinal absorption of insulin. Biol Pharm Bull 16 68. 

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. 

Trihydroxy bile salts have also been proven to be effective. Enhanced permeation of mannitol in TR 146 cells (a model for oral cavity mucosa) was noticed when the concentration of sodium taurocholate and sodium glycocholate was about 2- to 3-fold higher than their... 

Hayakawa, E., et al. 1989. Effect of sodium glycocholate and polyoxyethylene-9-lauryl ether on the hydrolysis of varying concentrations of insulin in the nasal homogenates of the albino rabbit. Life Sci 45 (2) 167. 

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