The conjugated trihydroxy bile salts glycocholate and taurocholate removed approx. 20--30% of the plasma-membrane enzymes 5'-nucleotidase, alkaline phosphatase and alkaline phosphodiesterase I from isolated hepatocytes before the onset of lysis, as judged by release of the cytosolic enzyme lactate dehydrogenase. The conjugated dihydroxy bile salt glycodeoxycholate similarly removed 10--20% of t...

BACKGROUND Oral delivery of insulin is challenging and must overcome the barriers of gastric and enzymatic degradation as well as low permeation across the intestinal epithelium. The present study aimed to develop a liposomal delivery system containing glycocholate as an enzyme inhibitor and permeation enhancer for oral insulin delivery. METHODS Liposomes containing sodium glycocholate were p...

1. A micro-partition centrifugal ultrafiltration technique has been used to monitor the percentage of [14C]glycocholate, [3H]glycochenodeoxycholate and [3H]glycochenodeoxycholate-3-sulphate bound to serum proteins of patients with cholestatic liver disease. 2. In comparison with normal individuals the percentage of binding of [14C]glycocholate and, to a lesser extent, of [3H]glycochenodeoxychol...

Many of the transporters involved in the transport of bile acids in the enterohepatic circulation have been characterized. The basolateral bile-acid transporter of ileocytes and cholangiocytes remains an exception. It has been suggested that rat multidrug resistance protein 3 (Mrp3) fulfills this function. Here we analyse bile-salt transport by human MRP3. Membrane vesicles from insect ( Spodop...

1. The apparent renal clearance of intravenously injected [14C]glycocholate and [3H]chenodeoxycholate-3-sulphate was estimated in 22 patients with cholestasis. The degree of protein binding of the isotopes in serum from these patients was determined. The effects of pharmacological agents, changes in urine flow rate and pH on renal clearance was studied. 2. The mean renal clearance of [14C]glyco...

Serum bile salt measurements and intravenous clearance of glycocholate were performed in a woman with Dubin-Johnson syndrome. Fasting conjugated cholate concentration was raised and prolonged intravenous clearance of sodium glycocholate revealed a secondary rise in conjugated cholate concentration after two hours. The intravenous clearance of bromsulphthalein also showed a secondary rise. These...

The potential for nasal delivery of losartan, a drug with poor oral bioavailability, was investigated using Calu-3 cells. Epithelial permeation of the drug with or without dimethyl-beta-cyclodextrin (DM-beta-CD) and glycocholate was investigated. Possible transport mechanism of the compound and epithelial mucosal tolerance were screened. Reversibility of epithelial membrane perturbation was als...

The effectiveness of gentamicin administered by the intranasal route in healthy human volunteers was studied. Thirty minutes after gentamicin in a solution of 1% sodium glycocholate was administered at 2 mg/kg of body weight, gentamicin concentrations of 2.48 +/- 0.42 mg/ml were present in the sera. Serum concentrations decreased to 0.94 +/- 0.13 mg/ml at 180 min. No serious side effects were o...

The objective of this study was to investigate the potential of liposomes containing bile salts as an ophthalmic delivery system for tacrolimus to improve corneal permeability. Liposomes containing bile salts, including sodium taurocholate, sodium deoxycholate, and sodium glycocholate, were produced by the thin-film dispersion method with a particle size of approximately 100 nm and an entrapmen...